subject:(Antimalarial activity)

Addis Ababa University

1. ABYOT, ENDALE. STUDIES ON ANTIMALARIAL ACTIVITY OF THE LEAF CONSTITUENT OF OTOSTEGIA INTEGRIFOLIA BENTH. (LAMIACEA) AGAINST PLASMODIUM BERGHEI IN MICE .

Degree: 2012, Addis Ababa University

URL: http://etd.aau.edu.et/dspace/handle/123456789/6069

► ABSTRACT Medicinal plants play an important role in the treatment of malaria especially in developing countries where resources are limited. A continued search for other… (more)

▼ ABSTRACT Medicinal plants play an important role in the treatment of malaria especially in developing countries where resources are limited. A continued search for other effective, safe and cheap plant-based antimalarial agents thus becomes imperative in the face of these difficulties. The leaves of Otostegia integrifolia Benth. are used traditionally as malarial remedy in Northern Ethiopia. This study was aimed to investigate the antimalarial potentials of the crude leaf extract, solvent fractions as well as isolated compound(s) in vivo in Plasmodium berghei infected mice to give scientific proof to the ethnobotanical claims. Leaves of O. integrifolia were collected and dried under the shade. The dried plant material was pulverized and extracted with 80% methanol. The dried crude extract was then further fractionated with different solvents. Both the crude extract and fractions were evaluated for their antimalarial activity in vivo, in 4-day suppressive assays against P. berghei in mice. Column chromatography was used to isolate compound/s from the most active fraction. The isolated compound was evaluated for its antimalarial activity in vivo, in 4-day suppressive assay against P. berghei and its structure elucidated using spectroscopic methods (MS and NMR). Preliminary phytochemical screening was performed using standard procedure. Acute and sub-acute toxicity studies of the crude extract were carried out in Swiss albino mice prior to antimalarial activity tests. No sign of toxicity was observed up on administration of the 80% methanol extract of the plant up to the highest dose (5000 mg/kg) given. Preliminary phytochemical screening showed the presence of saponins, flavonoids and other phenolic compounds in the hydroalcoholic leaf extract. The hydroalcoholic leaf extract (200, 400 and 600 mg/kg/day) and solvent fractions (200, 400 and 600 mg/kg/day) exhibited significant (P<0.01) antimalarial activity compared to the negative control group in four day suppression test with a considerable mean survival time. The highest parasite suppression (80.52%) was observed at 600 mg/kg /day for the crude extract, while the ethyl acetate fraction was found to be the most active among the solvent fractions and showed highest suppression (60.15%) at 600 mg/kg/day. The isolated compound also showed significant antimalarial (P<0.001) activity at the tested doses (25, 50 and 100 mg/kg/day) with chemosuppression of 50.13, 65.58, and 73.16%, respectively. Structural elucidation revealed that the isolated compound is a labdane type diterpenoid, 15,16-epoxy-3α,9α-dihydroxy-labda-13(16),14-diene. The crude extract, solvent fractions and the isolated compound possess considerable antiplasmodial activities which justify the use in ethnomedicine and can be exploited in the control of malaria Advisors/Committee Members: Kaleab Asres (Ph.D.) (advisor).

Subjects/Keywords: ANTIMALARIAL ACTIVITY; LEAF; OTOSTEGIA INTEGRIFOLIA

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APA (6^th Edition):

ABYOT, E. (2012). STUDIES ON ANTIMALARIAL ACTIVITY OF THE LEAF CONSTITUENT OF OTOSTEGIA INTEGRIFOLIA BENTH. (LAMIACEA) AGAINST PLASMODIUM BERGHEI IN MICE . (Thesis). Addis Ababa University. Retrieved from http://etd.aau.edu.et/dspace/handle/123456789/6069

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

ABYOT, ENDALE. “STUDIES ON ANTIMALARIAL ACTIVITY OF THE LEAF CONSTITUENT OF OTOSTEGIA INTEGRIFOLIA BENTH. (LAMIACEA) AGAINST PLASMODIUM BERGHEI IN MICE .” 2012. Thesis, Addis Ababa University. Accessed January 24, 2021. http://etd.aau.edu.et/dspace/handle/123456789/6069.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

ABYOT, ENDALE. “STUDIES ON ANTIMALARIAL ACTIVITY OF THE LEAF CONSTITUENT OF OTOSTEGIA INTEGRIFOLIA BENTH. (LAMIACEA) AGAINST PLASMODIUM BERGHEI IN MICE .” 2012. Web. 24 Jan 2021.

Vancouver:

ABYOT E. STUDIES ON ANTIMALARIAL ACTIVITY OF THE LEAF CONSTITUENT OF OTOSTEGIA INTEGRIFOLIA BENTH. (LAMIACEA) AGAINST PLASMODIUM BERGHEI IN MICE . [Internet] [Thesis]. Addis Ababa University; 2012. [cited 2021 Jan 24]. Available from: http://etd.aau.edu.et/dspace/handle/123456789/6069.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

ABYOT E. STUDIES ON ANTIMALARIAL ACTIVITY OF THE LEAF CONSTITUENT OF OTOSTEGIA INTEGRIFOLIA BENTH. (LAMIACEA) AGAINST PLASMODIUM BERGHEI IN MICE . [Thesis]. Addis Ababa University; 2012. Available from: http://etd.aau.edu.et/dspace/handle/123456789/6069

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Addis Ababa University

2. G/micheal, G/tsadik. Bioactivity guided fractionation and antimalarial activity of fractions of ethanol extract of Clerodendrum myricoides leaves in mice model .

Degree: 2013, Addis Ababa University

URL: http://etd.aau.edu.et/dspace/handle/123456789/413

► Malaria is one of the major health problems in the sub-Saharan African countries including Ethiopia. One of the reasons attributed for its increase is the… (more)

Subjects/Keywords: Antimalarial activity; BGF; C. myricoides; Medicinal plants

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

G/micheal, G. (2013). Bioactivity guided fractionation and antimalarial activity of fractions of ethanol extract of Clerodendrum myricoides leaves in mice model . (Thesis). Addis Ababa University. Retrieved from http://etd.aau.edu.et/dspace/handle/123456789/413

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

G/micheal, G/tsadik. “Bioactivity guided fractionation and antimalarial activity of fractions of ethanol extract of Clerodendrum myricoides leaves in mice model .” 2013. Thesis, Addis Ababa University. Accessed January 24, 2021. http://etd.aau.edu.et/dspace/handle/123456789/413.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

G/micheal, G/tsadik. “Bioactivity guided fractionation and antimalarial activity of fractions of ethanol extract of Clerodendrum myricoides leaves in mice model .” 2013. Web. 24 Jan 2021.

Vancouver:

G/micheal G. Bioactivity guided fractionation and antimalarial activity of fractions of ethanol extract of Clerodendrum myricoides leaves in mice model . [Internet] [Thesis]. Addis Ababa University; 2013. [cited 2021 Jan 24]. Available from: http://etd.aau.edu.et/dspace/handle/123456789/413.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

G/micheal G. Bioactivity guided fractionation and antimalarial activity of fractions of ethanol extract of Clerodendrum myricoides leaves in mice model . [Thesis]. Addis Ababa University; 2013. Available from: http://etd.aau.edu.et/dspace/handle/123456789/413

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Addis Ababa University

3. ABDU, TUHA. SYNTHESIS AND BIOLOGICAL SCREENING OF SOME PYRAZOLE DERIVATIVES AS ANTIMALARIAL AND ANTILEISHMANIAL AGENTS .

Degree: 2012, Addis Ababa University

URL: http://etd.aau.edu.et/dspace/handle/123456789/6214

► Malaria and leishmania are very common parasitic diseases of the developing world and drug resistance has hindered their efficient control. Pyrazole derivatives were synthesized using… (more)

Subjects/Keywords: pyrazole; in vivo antimalarial activity; in vitro antileishmanial activity

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

ABDU, T. (2012). SYNTHESIS AND BIOLOGICAL SCREENING OF SOME PYRAZOLE DERIVATIVES AS ANTIMALARIAL AND ANTILEISHMANIAL AGENTS . (Thesis). Addis Ababa University. Retrieved from http://etd.aau.edu.et/dspace/handle/123456789/6214

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

ABDU, TUHA. “SYNTHESIS AND BIOLOGICAL SCREENING OF SOME PYRAZOLE DERIVATIVES AS ANTIMALARIAL AND ANTILEISHMANIAL AGENTS .” 2012. Thesis, Addis Ababa University. Accessed January 24, 2021. http://etd.aau.edu.et/dspace/handle/123456789/6214.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

ABDU, TUHA. “SYNTHESIS AND BIOLOGICAL SCREENING OF SOME PYRAZOLE DERIVATIVES AS ANTIMALARIAL AND ANTILEISHMANIAL AGENTS .” 2012. Web. 24 Jan 2021.

Vancouver:

ABDU T. SYNTHESIS AND BIOLOGICAL SCREENING OF SOME PYRAZOLE DERIVATIVES AS ANTIMALARIAL AND ANTILEISHMANIAL AGENTS . [Internet] [Thesis]. Addis Ababa University; 2012. [cited 2021 Jan 24]. Available from: http://etd.aau.edu.et/dspace/handle/123456789/6214.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

ABDU T. SYNTHESIS AND BIOLOGICAL SCREENING OF SOME PYRAZOLE DERIVATIVES AS ANTIMALARIAL AND ANTILEISHMANIAL AGENTS . [Thesis]. Addis Ababa University; 2012. Available from: http://etd.aau.edu.et/dspace/handle/123456789/6214

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Addis Ababa University

4. ABDU, TUHA. SYNTHESIS AND BIOLOGICAL SCREENING OF SOME PYRAZOLE DERIVATIVES AS ANTIMALARIAL AND ANTILEISHMANIAL AGENTS .

Degree: 2012, Addis Ababa University

URL: http://etd.aau.edu.et/dspace/handle/123456789/6218

► Malaria and leishmania are very common parasitic diseases of the developing world and drug resistance has hindered their efficient control. Pyrazole derivatives were synthesized using… (more)

Subjects/Keywords: pyrazole; in vivo antimalarial activity; in vitro antileishmanial activity.

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

ABDU, T. (2012). SYNTHESIS AND BIOLOGICAL SCREENING OF SOME PYRAZOLE DERIVATIVES AS ANTIMALARIAL AND ANTILEISHMANIAL AGENTS . (Thesis). Addis Ababa University. Retrieved from http://etd.aau.edu.et/dspace/handle/123456789/6218

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

ABDU, TUHA. “SYNTHESIS AND BIOLOGICAL SCREENING OF SOME PYRAZOLE DERIVATIVES AS ANTIMALARIAL AND ANTILEISHMANIAL AGENTS .” 2012. Thesis, Addis Ababa University. Accessed January 24, 2021. http://etd.aau.edu.et/dspace/handle/123456789/6218.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

ABDU, TUHA. “SYNTHESIS AND BIOLOGICAL SCREENING OF SOME PYRAZOLE DERIVATIVES AS ANTIMALARIAL AND ANTILEISHMANIAL AGENTS .” 2012. Web. 24 Jan 2021.

Vancouver:

ABDU T. SYNTHESIS AND BIOLOGICAL SCREENING OF SOME PYRAZOLE DERIVATIVES AS ANTIMALARIAL AND ANTILEISHMANIAL AGENTS . [Internet] [Thesis]. Addis Ababa University; 2012. [cited 2021 Jan 24]. Available from: http://etd.aau.edu.et/dspace/handle/123456789/6218.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

ABDU T. SYNTHESIS AND BIOLOGICAL SCREENING OF SOME PYRAZOLE DERIVATIVES AS ANTIMALARIAL AND ANTILEISHMANIAL AGENTS . [Thesis]. Addis Ababa University; 2012. Available from: http://etd.aau.edu.et/dspace/handle/123456789/6218

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

5. Singh, Shailja. Crystallographic spectroscopic and antimalarial activity of 4 aminoquinoline derivatives; -.

Degree: Chemistry, 2013, University of Delhi

URL: http://shodhganga.inflibnet.ac.in/handle/10603/31890

Availabl

Reference p.200-203

Advisors/Committee Members: Awasthi, Satish Kumar.

Subjects/Keywords: antimalarial activity; Crystallographic; derivatives; spectroscopic

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Singh, S. (2013). Crystallographic spectroscopic and antimalarial activity of 4 aminoquinoline derivatives; -. (Thesis). University of Delhi. Retrieved from http://shodhganga.inflibnet.ac.in/handle/10603/31890

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Singh, Shailja. “Crystallographic spectroscopic and antimalarial activity of 4 aminoquinoline derivatives; -.” 2013. Thesis, University of Delhi. Accessed January 24, 2021. http://shodhganga.inflibnet.ac.in/handle/10603/31890.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Singh, Shailja. “Crystallographic spectroscopic and antimalarial activity of 4 aminoquinoline derivatives; -.” 2013. Web. 24 Jan 2021.

Vancouver:

Singh S. Crystallographic spectroscopic and antimalarial activity of 4 aminoquinoline derivatives; -. [Internet] [Thesis]. University of Delhi; 2013. [cited 2021 Jan 24]. Available from: http://shodhganga.inflibnet.ac.in/handle/10603/31890.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Singh S. Crystallographic spectroscopic and antimalarial activity of 4 aminoquinoline derivatives; -. [Thesis]. University of Delhi; 2013. Available from: http://shodhganga.inflibnet.ac.in/handle/10603/31890

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Addis Ababa University

6. Andualem, Getie. EVALUATION OF ANTIMALARIAL ACTIVITY OF SEEDS OF DODONAEA ANGUSTIFOLIA AND LEAVES OF ENTADA ABYSSINICA AGAINST PLASMODIUM BERGHEI IN SWISS ALBINO MICE.

Degree: 2012, Addis Ababa University

URL: http://etd.aau.edu.et/dspace/handle/123456789/346

► In the face of antimalarial drug resistance, there is need to develop more effective antimalarial drugs that are inexpensive. In this respect, traditional medicinal plant-based… (more)

Subjects/Keywords: Plasmodium berghei; in vivo; Entada abyssinica; Dodonaea anqustifolia; antimalarial activity

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Andualem, G. (2012). EVALUATION OF ANTIMALARIAL ACTIVITY OF SEEDS OF DODONAEA ANGUSTIFOLIA AND LEAVES OF ENTADA ABYSSINICA AGAINST PLASMODIUM BERGHEI IN SWISS ALBINO MICE. (Thesis). Addis Ababa University. Retrieved from http://etd.aau.edu.et/dspace/handle/123456789/346

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Andualem, Getie. “EVALUATION OF ANTIMALARIAL ACTIVITY OF SEEDS OF DODONAEA ANGUSTIFOLIA AND LEAVES OF ENTADA ABYSSINICA AGAINST PLASMODIUM BERGHEI IN SWISS ALBINO MICE. ” 2012. Thesis, Addis Ababa University. Accessed January 24, 2021. http://etd.aau.edu.et/dspace/handle/123456789/346.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Andualem, Getie. “EVALUATION OF ANTIMALARIAL ACTIVITY OF SEEDS OF DODONAEA ANGUSTIFOLIA AND LEAVES OF ENTADA ABYSSINICA AGAINST PLASMODIUM BERGHEI IN SWISS ALBINO MICE. ” 2012. Web. 24 Jan 2021.

Vancouver:

Andualem G. EVALUATION OF ANTIMALARIAL ACTIVITY OF SEEDS OF DODONAEA ANGUSTIFOLIA AND LEAVES OF ENTADA ABYSSINICA AGAINST PLASMODIUM BERGHEI IN SWISS ALBINO MICE. [Internet] [Thesis]. Addis Ababa University; 2012. [cited 2021 Jan 24]. Available from: http://etd.aau.edu.et/dspace/handle/123456789/346.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Andualem G. EVALUATION OF ANTIMALARIAL ACTIVITY OF SEEDS OF DODONAEA ANGUSTIFOLIA AND LEAVES OF ENTADA ABYSSINICA AGAINST PLASMODIUM BERGHEI IN SWISS ALBINO MICE. [Thesis]. Addis Ababa University; 2012. Available from: http://etd.aau.edu.et/dspace/handle/123456789/346

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Addis Ababa University

7. Selamawit, Fantahun. IN-VIVO ANTI-PLASMODIUM ACTIVITY OF CRUDE EXTRACTS AND SOLVENT FRACTIONS OF STRYCHNOS MITIS LEAVES IN PLASMODIUM BERGHEI INFECTED MICE.

Degree: 2015, Addis Ababa University

URL: http://etd.aau.edu.et/dspace/handle/123456789/7689

► Malaria is a major public health problem in the world which is responsible for death of millions particularly in sub-Saharan Africa. Today, the control of… (more)

▼ Malaria is a major public health problem in the world which is responsible for death of millions particularly in sub-Saharan Africa. Today, the control of malaria has become gradually more complex due to the spread of drug-resistant parasites. Medicinal plants are the unquestionable source of effective antimalarias. The present study was aimed to evaluate antiplasmodial activity and determine acute toxicity of Strychnos mitis in P.berghi infected mice. All extracts revealed no obvious acute toxicities on mice up to the highest (2000mg/kg) dose given. The crude aqueous extract, crude hydromethanolic extract, N – hexane fraction of crude hydromethanolic extract, chloroform fraction of crude hydromethanolic extract and aqueous fraction of crude hydromethanolic extract of the leaf of Strychnos mitis significantly (p<0.01) inhibited parasite load. At highest dose (600mg/kg) both aqueous and hydromethanolic extracts showed higher percentage suppression 95.5% and 93.97% respectively, which is comparable to CQ(25mg/kg)(100%). All doses of crude extracts and fractions of S.mitis leave prolong the survival time of infected mice dose dependently. The higher two doses of the crude aqueous extract, hydromethanolic extract, chloroform fraction and aqueous fraction prevented the weight loss in a dose dependent manner. Whereas all doses of N- hexane fraction prevented loss of body weight not dose dependently. The crude aqueous extract at (400mg/kg and 600mg/kg) and hydromethanolic extract at all dose level significantly (p<0.01) prevented the expected reduction in PCV. Crude aqueous extract at (600mg/kg) and hydromethanolic extract at all dose level significantly prevented temperature reduction. The phytochemical screening of the crude aqueous extract showed the presence of Alkaloids, Anthraquinones, Glycosides, Terpenoids, Saponins, Tannins and Phenols. The results of this study provide support for the traditional therapeutic value for treatment of malaria Advisors/Committee Members: Eyasu Maekonnen (Prof.) (advisor).

Subjects/Keywords: Strychnos mitis; crude extract; fraction; Plasmodium berghei; Antimalarial activity.

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APA (6^th Edition):

Selamawit, F. (2015). IN-VIVO ANTI-PLASMODIUM ACTIVITY OF CRUDE EXTRACTS AND SOLVENT FRACTIONS OF STRYCHNOS MITIS LEAVES IN PLASMODIUM BERGHEI INFECTED MICE. (Thesis). Addis Ababa University. Retrieved from http://etd.aau.edu.et/dspace/handle/123456789/7689

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Selamawit, Fantahun. “IN-VIVO ANTI-PLASMODIUM ACTIVITY OF CRUDE EXTRACTS AND SOLVENT FRACTIONS OF STRYCHNOS MITIS LEAVES IN PLASMODIUM BERGHEI INFECTED MICE. ” 2015. Thesis, Addis Ababa University. Accessed January 24, 2021. http://etd.aau.edu.et/dspace/handle/123456789/7689.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Selamawit, Fantahun. “IN-VIVO ANTI-PLASMODIUM ACTIVITY OF CRUDE EXTRACTS AND SOLVENT FRACTIONS OF STRYCHNOS MITIS LEAVES IN PLASMODIUM BERGHEI INFECTED MICE. ” 2015. Web. 24 Jan 2021.

Vancouver:

Selamawit F. IN-VIVO ANTI-PLASMODIUM ACTIVITY OF CRUDE EXTRACTS AND SOLVENT FRACTIONS OF STRYCHNOS MITIS LEAVES IN PLASMODIUM BERGHEI INFECTED MICE. [Internet] [Thesis]. Addis Ababa University; 2015. [cited 2021 Jan 24]. Available from: http://etd.aau.edu.et/dspace/handle/123456789/7689.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Selamawit F. IN-VIVO ANTI-PLASMODIUM ACTIVITY OF CRUDE EXTRACTS AND SOLVENT FRACTIONS OF STRYCHNOS MITIS LEAVES IN PLASMODIUM BERGHEI INFECTED MICE. [Thesis]. Addis Ababa University; 2015. Available from: http://etd.aau.edu.et/dspace/handle/123456789/7689

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Addis Ababa University

8. Dawit, Dikasso. In Vivo Anti-Malarial Activity of the Hydroalcoholic Extracts of Asparagus Africanus, Withania Somnifera and Laganaria Vulgaris in Mice .

Degree: 2005, Addis Ababa University

URL: http://etd.aau.edu.et/dspace/handle/123456789/5672

► Malaria is a major public health problem in the world in general and developing world in particular. It is known to cause 1-2 million deaths… (more)

Subjects/Keywords: acute toxicity; in vivo; antimalarial activity

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Dawit, D. (2005). In Vivo Anti-Malarial Activity of the Hydroalcoholic Extracts of Asparagus Africanus, Withania Somnifera and Laganaria Vulgaris in Mice . (Thesis). Addis Ababa University. Retrieved from http://etd.aau.edu.et/dspace/handle/123456789/5672

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Dawit, Dikasso. “In Vivo Anti-Malarial Activity of the Hydroalcoholic Extracts of Asparagus Africanus, Withania Somnifera and Laganaria Vulgaris in Mice .” 2005. Thesis, Addis Ababa University. Accessed January 24, 2021. http://etd.aau.edu.et/dspace/handle/123456789/5672.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Dawit, Dikasso. “In Vivo Anti-Malarial Activity of the Hydroalcoholic Extracts of Asparagus Africanus, Withania Somnifera and Laganaria Vulgaris in Mice .” 2005. Web. 24 Jan 2021.

Vancouver:

Dawit D. In Vivo Anti-Malarial Activity of the Hydroalcoholic Extracts of Asparagus Africanus, Withania Somnifera and Laganaria Vulgaris in Mice . [Internet] [Thesis]. Addis Ababa University; 2005. [cited 2021 Jan 24]. Available from: http://etd.aau.edu.et/dspace/handle/123456789/5672.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Dawit D. In Vivo Anti-Malarial Activity of the Hydroalcoholic Extracts of Asparagus Africanus, Withania Somnifera and Laganaria Vulgaris in Mice . [Thesis]. Addis Ababa University; 2005. Available from: http://etd.aau.edu.et/dspace/handle/123456789/5672

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Curtin University of Technology

9. Whittell, Louise Renee'. The synthesis and biological evaluation of novel analogues of isocryptolepine .

Degree: 2011, Curtin University of Technology

URL: http://hdl.handle.net/20.500.11937/2558

► This thesis investigates the potential of the alkaloid isocryptolepine 16 as a lead compound in antimalarial drug development. Fifteen derivatives of the parent alkaloid were… (more)

▼ This thesis investigates the potential of the alkaloid isocryptolepine 16 as a lead compound in antimalarial drug development. Fifteen derivatives of the parent alkaloid were prepared and fully characterised, twelve of which were novel compounds. A select group of compounds were subsequently evaluated for both antimalarial activity and cytotoxicity.Three previously reported synthetic methodologies to the parent alkaloid were initially investigated; wherein two approaches were able to be reproduced or improved. These two synthetic methodologies were subsequently applied to the preparation of derivatives. The first of these methodologies, the Jonckers Method, involved two consecutive palladium catalysed coupling reactions. During the course of these investigations it was found that these two reactions could be combined into a single ‘domino’ reaction resulting in a reduction in the number of steps required to prepare the parent alkaloid. This methodology was then applied to the preparation of both ring-substituted and structural isomers. The second methodology, The Molina Method, involved a benzotriazole-mediated strategy and was applicable to preparing isocryptolepine derivatives with ring substituents on the quinoline ring. Finally a method for selective electrophilic aromatic substitution was developed and applied to the preparation of a further range of halogenated derivatives.Eight of the prepared derivatives were selected for biological evaluation. Antimalarial activity was assessed against a chloroquine sensitive and resistant strain of P. falciparum, whilst cytotoxicity was evaluated against mouse embryonic fibroblasts (3T3 cells). All compounds were found to be more active compared to the parent alkaloid against the chloroquine resistant strain of P. falciparum; specifically 8-bromo-2-chloroisocryptolepine 107 (IC[subscript]50 = 85 nM) and 8-bromo-3-chloroisocryptolepine 105 (IC[subscript]50 = 100 nM) were the most potent. Cytotoxicity evaluations revealed that ring substitution did not enhance cytotoxicity and the most potent antimalarial derivative, 8-bromo-2-chloroisocryptolepine 107 (IC[subscript]50 = 9.01 μM), displayed a 4-fold reduction in cytotoxicity.In conclusion, isocryptolepine 16 and its derivatives have significant potential as antimalarial lead compounds, with many derivatives possessing enhanced bioactivity versus the parent. This study has also identified 8-bromo-2-chloroisocryptolepine 107 to be a very promising lead compound which warrants further biological or pharmaceutical investigation.

Subjects/Keywords: lead compound; halogenated derivatives; Molina Method; antimalarial activity; antimalarial drug development; selective electrophilic aromatic substitution; alkaloid isocryptolepine 16; cytotoxicity; Jonckers Method; synthetic methodologies

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Whittell, L. R. (2011). The synthesis and biological evaluation of novel analogues of isocryptolepine . (Thesis). Curtin University of Technology. Retrieved from http://hdl.handle.net/20.500.11937/2558

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Whittell, Louise Renee'. “The synthesis and biological evaluation of novel analogues of isocryptolepine .” 2011. Thesis, Curtin University of Technology. Accessed January 24, 2021. http://hdl.handle.net/20.500.11937/2558.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Whittell, Louise Renee'. “The synthesis and biological evaluation of novel analogues of isocryptolepine .” 2011. Web. 24 Jan 2021.

Vancouver:

Whittell LR. The synthesis and biological evaluation of novel analogues of isocryptolepine . [Internet] [Thesis]. Curtin University of Technology; 2011. [cited 2021 Jan 24]. Available from: http://hdl.handle.net/20.500.11937/2558.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Whittell LR. The synthesis and biological evaluation of novel analogues of isocryptolepine . [Thesis]. Curtin University of Technology; 2011. Available from: http://hdl.handle.net/20.500.11937/2558

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Universidade do Rio Grande do Norte

10. Wanderley, Bruno Mattos Silva. Atividade antiplasmódica e toxicológica de plantas medicinais usadas popularmente no Brasil : uma abordagem etnobotânica .

Degree: 2012, Universidade do Rio Grande do Norte

URL: http://repositorio.ufrn.br/handle/123456789/13090

► Malaria is a disease of global distribution, recognized by governments around the world as a serious public health problem, affecting more than 109 countries and… (more)

▼ Malaria is a disease of global distribution, recognized by governments around the world as a serious public health problem, affecting more than 109 countries and territories and endangering more than 3.3 billion people. The economic costs of this disease are also relevant: the African continent itself has malaria-related costs of about $ 12 billion annually. Nowadays, in addition to chloroquine, Plasmodium falciparum is resistant to many drugs used in the treatment of malaria, such as amodiaquine, mefloquine, quinine and sulfadoxine-pyrimethamine; resistance of Plasmodium vivax to treatments, although less studied, is also reported. Nature, in general, is responsible for the production of most known organic substances, and the plant kingdom is responsible for the most of the chemical diversity known and reported in the literature. Most medicinal plants commercialized in Brazil, however, are of exotic origin, which makes the search for endemic medicinal plants, besides a patent necessity, a fascinating subject of academic research and development. This study aimed to: (i) verify the antimalarial activity of ethanolic and hydroalcoholic extracts of Boerhavia paniculata Rich. And acetonic extract of Clethra scabra Pers. in Swiss albino mice infected by Plasmodium berghei NK65, (ii) observe possible combined effects between the course of infection by P. berghei NK65 and administration of these extracts in Swiss albino mice, and (iii) conduct a preliminary study of the acute toxicity of these extracts in Swiss albino mice. All extracts notable pharmacological activities - with parasite infections inhibitions ranging from 22% to 54%.These characteristics suggest that the activities are relevant, although comparatively lower than the activity displayed by the positive control group (always above 90%). The general framework of survival analysis demonstrates an overall reduction in survival times for all groups. Necroscopy has not pointed no change in color, shape, size and/or consistency in the evaluated organs - the only exception was the livers of rats submitted to treatment to hydroalcoholic extracts: these organs have been presented in a slightly congestive aspect with mass increasing roughly 28% higher than the other two groups and a p-value of 0.0365. The 250 mg/Kg ethanolic group has been pointed out by the Dunn s post test, as the only class with simultaneous inequalities (p<0.05) between positive and negative control groups. The extracts, notably ethanol extract, have, in fact, a vestigial antimalarial activity, although well below from the ones perceived to chloroquine-treated groups; nevertheless, the survival times of the animals fed with the extracts do not rise by presence of such therapy. Both the toxicopharmacological studies of the synergism between the clinical course of malaria and administration of extracts and the isolated evaluation of toxicity allow us to affirm the absence of toxicity of the extracts at the level of CNS and ANS, as well as their non-influence on food and water consumption patterns,… Advisors/Committee Members: Andrade Neto, Valter Ferreira de (advisor), CPF:59626305487 (advisor), http://lattes.cnpq.br/4863082845974813 (advisor).

Subjects/Keywords: Malária. Resistência. Atividade antimalárica. Clethra scabra Pers.. Boerhavia paniculata Rich; Malaria. Resistance. Antimalarial activity. Clethra scabra Pers.. Boerhavia paniculata Rich

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Wanderley, B. M. S. (2012). Atividade antiplasmódica e toxicológica de plantas medicinais usadas popularmente no Brasil : uma abordagem etnobotânica . (Thesis). Universidade do Rio Grande do Norte. Retrieved from http://repositorio.ufrn.br/handle/123456789/13090

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Wanderley, Bruno Mattos Silva. “Atividade antiplasmódica e toxicológica de plantas medicinais usadas popularmente no Brasil : uma abordagem etnobotânica .” 2012. Thesis, Universidade do Rio Grande do Norte. Accessed January 24, 2021. http://repositorio.ufrn.br/handle/123456789/13090.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Wanderley, Bruno Mattos Silva. “Atividade antiplasmódica e toxicológica de plantas medicinais usadas popularmente no Brasil : uma abordagem etnobotânica .” 2012. Web. 24 Jan 2021.

Vancouver:

Wanderley BMS. Atividade antiplasmódica e toxicológica de plantas medicinais usadas popularmente no Brasil : uma abordagem etnobotânica . [Internet] [Thesis]. Universidade do Rio Grande do Norte; 2012. [cited 2021 Jan 24]. Available from: http://repositorio.ufrn.br/handle/123456789/13090.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Wanderley BMS. Atividade antiplasmódica e toxicológica de plantas medicinais usadas popularmente no Brasil : uma abordagem etnobotânica . [Thesis]. Universidade do Rio Grande do Norte; 2012. Available from: http://repositorio.ufrn.br/handle/123456789/13090

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

University of Nairobi

11. Ochora, Ongeri D. Antimalarial Activity, Acute Toxicity And Phytochemical Investigations Of Plant Extracts From Four Plants In Kenyan Biodiversity .

Degree: 2013, University of Nairobi

URL: http://erepository.uonbi.ac.ke:8080/xmlui/handle/123456789/60842

► Malaria is a major and constant public health problem in the world, especially in developing countries. In Kenya, more than half of the population is… (more)

▼ Malaria is a major and constant public health problem in the world, especially in developing countries. In Kenya, more than half of the population is exposed to malaria with minimal opportunities for treatment. This is increased by emergence of resistant vectors (female Anopheles spp.) and multidrug-resistant strains of malaria causing parasite, thereby calling for alternatives. Plants contain secondary metabolites that are a probable source of natural compounds which could have antimalarial activity. In this study, the antimalarial activities of aqueous and organic plant extracts were determined, acute toxicity evaluated using the mouse model and major phytochemical compounds in the extracts investigated. Crude extracts were prepared from four plant species; Commiphora schimperi (Berg.) Engl. (Burseraceae), Ricinus communis L. (Euphorbiaceae), Grewia hexamita Burret. (Tiliaceae) and Securidaca longependuculata Fres. (Polygalaceae) collected from Msambweni district, Kenyan. Adult healthy Swiss mice (Mus musculus L.) were infected intraperitoneally with Plasmodium berghei (ANKA) to induce malaria and then treated orally at 100 mg/kg of each crude plant extracts according to the Peter’s 4-day suppressive test. The negative control was treated with distilled water and the positive with chloroquine (CQ). Healthy Swiss female mice were used for acute toxicity testing as per Organisation for Economic Co-operation and Development (OECD) guidelines. To determine the presence of secondary metabolites in all extracts, Thin Layer Chromatography (TLC) was used. The means obtained from the 4-day suppressive test were analyzed using student’s t-test and Analysis of Variance (ANOVA).Among the four plants, S. longependuculata had the highest chemosuppression level of 91.03%. Extracts from C. schimperi, R. communis and G. hexaminta were safe at 2000 mg/kg and were considered non toxic to mice while S. longependuculata was considered non toxic at 300 mg/kg during a 24 hour period. Alkaloids and flavonoids were present in all extracts while Sesquiterpene lactones were absent in all the extracts. Saponins were present in both extracts of S. longependuculata and organic extracts of G. hexamita only.The current study provides insights into in vivo antimalarial activity and acute toxicity of organic and aqueous crude extracts from the four plants. These results support a rational rather than random approach to the selection of antimalarial screening candidates, and have identified a number of promising species for further investigation as plant based antimalarial agents.

Subjects/Keywords: In vivo Antimalarial activity; Acute toxicity; Phytochemical analysis; Musculus; Plasmodium berghei; Commiphora schimperi; Ricinus communis; Grewia; Hexaminta; Securidaca longependuculata

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Ochora, O. D. (2013). Antimalarial Activity, Acute Toxicity And Phytochemical Investigations Of Plant Extracts From Four Plants In Kenyan Biodiversity . (Thesis). University of Nairobi. Retrieved from http://erepository.uonbi.ac.ke:8080/xmlui/handle/123456789/60842

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Ochora, Ongeri D. “Antimalarial Activity, Acute Toxicity And Phytochemical Investigations Of Plant Extracts From Four Plants In Kenyan Biodiversity .” 2013. Thesis, University of Nairobi. Accessed January 24, 2021. http://erepository.uonbi.ac.ke:8080/xmlui/handle/123456789/60842.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Ochora, Ongeri D. “Antimalarial Activity, Acute Toxicity And Phytochemical Investigations Of Plant Extracts From Four Plants In Kenyan Biodiversity .” 2013. Web. 24 Jan 2021.

Vancouver:

Ochora OD. Antimalarial Activity, Acute Toxicity And Phytochemical Investigations Of Plant Extracts From Four Plants In Kenyan Biodiversity . [Internet] [Thesis]. University of Nairobi; 2013. [cited 2021 Jan 24]. Available from: http://erepository.uonbi.ac.ke:8080/xmlui/handle/123456789/60842.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Ochora OD. Antimalarial Activity, Acute Toxicity And Phytochemical Investigations Of Plant Extracts From Four Plants In Kenyan Biodiversity . [Thesis]. University of Nairobi; 2013. Available from: http://erepository.uonbi.ac.ke:8080/xmlui/handle/123456789/60842

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Universidade do Rio Grande do Norte

12. Wanderley, Bruno Mattos Silva. Atividade antiplasmódica e toxicológica de plantas medicinais usadas popularmente no Brasil : uma abordagem etnobotânica .

Degree: 2012, Universidade do Rio Grande do Norte

URL: http://repositorio.ufrn.br/handle/123456789/13090

► Malaria is a disease of global distribution, recognized by governments around the world as a serious public health problem, affecting more than 109 countries and… (more)

▼ Malaria is a disease of global distribution, recognized by governments around the world as a serious public health problem, affecting more than 109 countries and territories and endangering more than 3.3 billion people. The economic costs of this disease are also relevant: the African continent itself has malaria-related costs of about $ 12 billion annually. Nowadays, in addition to chloroquine, Plasmodium falciparum is resistant to many drugs used in the treatment of malaria, such as amodiaquine, mefloquine, quinine and sulfadoxine-pyrimethamine; resistance of Plasmodium vivax to treatments, although less studied, is also reported. Nature, in general, is responsible for the production of most known organic substances, and the plant kingdom is responsible for the most of the chemical diversity known and reported in the literature. Most medicinal plants commercialized in Brazil, however, are of exotic origin, which makes the search for endemic medicinal plants, besides a patent necessity, a fascinating subject of academic research and development. This study aimed to: (i) verify the antimalarial activity of ethanolic and hydroalcoholic extracts of Boerhavia paniculata Rich. And acetonic extract of Clethra scabra Pers. in Swiss albino mice infected by Plasmodium berghei NK65, (ii) observe possible combined effects between the course of infection by P. berghei NK65 and administration of these extracts in Swiss albino mice, and (iii) conduct a preliminary study of the acute toxicity of these extracts in Swiss albino mice. All extracts notable pharmacological activities - with parasite infections inhibitions ranging from 22% to 54%.These characteristics suggest that the activities are relevant, although comparatively lower than the activity displayed by the positive control group (always above 90%). The general framework of survival analysis demonstrates an overall reduction in survival times for all groups. Necroscopy has not pointed no change in color, shape, size and/or consistency in the evaluated organs - the only exception was the livers of rats submitted to treatment to hydroalcoholic extracts: these organs have been presented in a slightly congestive aspect with mass increasing roughly 28% higher than the other two groups and a p-value of 0.0365. The 250 mg/Kg ethanolic group has been pointed out by the Dunn s post test, as the only class with simultaneous inequalities (p<0.05) between positive and negative control groups. The extracts, notably ethanol extract, have, in fact, a vestigial antimalarial activity, although well below from the ones perceived to chloroquine-treated groups; nevertheless, the survival times of the animals fed with the extracts do not rise by presence of such therapy. Both the toxicopharmacological studies of the synergism between the clinical course of malaria and administration of extracts and the isolated evaluation of toxicity allow us to affirm the absence of toxicity of the extracts at the level of CNS and ANS, as well as their non-influence on food and water consumption patterns,… Advisors/Committee Members: Andrade Neto, Valter Ferreira de (advisor), CPF:59626305487 (advisor), http://lattes.cnpq.br/4863082845974813 (advisor).

Subjects/Keywords: Malária. Resistência. Atividade antimalárica. Clethra scabra Pers.. Boerhavia paniculata Rich; Malaria. Resistance. Antimalarial activity. Clethra scabra Pers.. Boerhavia paniculata Rich

Record Details Similar Records Cite « Share

❌

APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Wanderley, B. M. S. (2012). Atividade antiplasmódica e toxicológica de plantas medicinais usadas popularmente no Brasil : uma abordagem etnobotânica . (Masters Thesis). Universidade do Rio Grande do Norte. Retrieved from http://repositorio.ufrn.br/handle/123456789/13090

Chicago Manual of Style (16^th Edition):

Wanderley, Bruno Mattos Silva. “Atividade antiplasmódica e toxicológica de plantas medicinais usadas popularmente no Brasil : uma abordagem etnobotânica .” 2012. Masters Thesis, Universidade do Rio Grande do Norte. Accessed January 24, 2021. http://repositorio.ufrn.br/handle/123456789/13090.

MLA Handbook (7^th Edition):

Wanderley, Bruno Mattos Silva. “Atividade antiplasmódica e toxicológica de plantas medicinais usadas popularmente no Brasil : uma abordagem etnobotânica .” 2012. Web. 24 Jan 2021.

Vancouver:

Wanderley BMS. Atividade antiplasmódica e toxicológica de plantas medicinais usadas popularmente no Brasil : uma abordagem etnobotânica . [Internet] [Masters thesis]. Universidade do Rio Grande do Norte; 2012. [cited 2021 Jan 24]. Available from: http://repositorio.ufrn.br/handle/123456789/13090.

Council of Science Editors:

Wanderley BMS. Atividade antiplasmódica e toxicológica de plantas medicinais usadas popularmente no Brasil : uma abordagem etnobotânica . [Masters Thesis]. Universidade do Rio Grande do Norte; 2012. Available from: http://repositorio.ufrn.br/handle/123456789/13090

13. Mahadeo, Keshika. Étude métabolomique et valorisation pharmacologique et biotechnologique d'éspèces du genre Psiadia endémiques de la Réunion et de l'ile Maurice : Metabolomic study and pharmacological and biotechnological valorization of species of the Psiadia genus endemic to Reunion and Mauritius.

Degree: Docteur es, Chimie, 2018, La Réunion

URL: http://www.theses.fr/2018LARE0001

►

Les travaux de thèse présentés dans ce manuscrit portent sur l’étude chimique de plantes du genre Psiadia. Trois axes de recherche ont été menés parallèlement… (more)

▼

Les travaux de thèse présentés dans ce manuscrit portent sur l’étude chimique de plantes du genre Psiadia. Trois axes de recherche ont été menés parallèlement à savoir (1) une étude chimiotaxonomique à partir de 11 espèces du genre Psiadia endémiques de La Réunion, (2) un criblage biologique réalisé sur 16 espèces du genre Psiadia dont 11 endémiques de La Réunion et 5 endémiques de Maurice et (3) une étude phytochimique ciblée sur l’espèce Psiadia arguta endémique de Maurice. Le premier axe comportant l'étude chimiotaxonomique menée par une approche métabolomique avait pour objectif d'identifier des marqueurs chimiotaxonomiques. Cette étude a été effectuée à partir des analyses CG-SM et CG-DIF des composés volatils et des analyses RMN 1H des composés non volatils de 11 espèces endémiques de La Réunion récoltées sur différents lieux géographiques et au cours des saisons estivale et hivernale. Une analyse intra-espèce a permis d'étudier la variabilité saisonnière et/ou géographique de la composition chimique de chaque espèce. Une analyse inter-espèces a conduit à deux classifications différentes des 11 espèces selon leur composition en métabolites volatils et non volatils. Le deuxième axe avait pour objectif d'identifier parmi 11 espèces du genre Psiadia endémiques de La Réunion et 5 espèces endémiques de Maurice, les espèces présentant une ou des activités biologiques prometteuses. Les cibles biologiques choisies ont été le parasite Plasmodium falciparum responsable du paludisme, la lignée cellulaire humaine cancéreuse HeLa responsable du cancer du col de l'utérus et l'enzyme HRP (Horseradish peroxydase) intervenant dans la réponse inflammatoire. À l'issue de ce criblage, 5 espèces se sont révélées prometteuses : les espèces réunionnaises P. amygdalina et P. anchusifolia et les espèces mauriciennes P. arguta et P. lithospermifolia pour l'activité antiplasmodiale, ainsi que l'espèce réunionnaise P. dentata pour les trois activités testées. Le troisième axe consacré à une étude phytochimique de P. arguta réalisée par un fractionnement bioguidé de l'extrait brut a conduit à l'isolement et à l'identification de 16 terpénoïdes : 2 triterpènes et 14 diterpènes de structure labdane dont 4 sont de structure nouvelle. Cinq diterpènes se sont révélés particulièrement actifs contre le parasite P. falciparum : l'acétate de labda-13(E)-en-8α-ol-15-yle, l'acétate de labdan-8α-ol-15-yle, le 13-épi-sclaréol, le labda-13(E)-ène-8α,15-diol et le (8R,13S)-labdane-8,15-diol. Par ailleurs, une étude métabolomique menée par RMN 1H sur des plantules de P. arguta cultivées in vitro et acclimatées a permis l'étude des facteurs influençant la production de ces composés bioactifs.

The present work describes the chemical composition of the plant genus Psiadia and focuses on three research topics: (1) a chemotaxonomic study of 11 species endemic to Reunion island, (2) a biological screening of 16 Psiadia species among which 11 are endemic to Reunion and 5 are endemic to Mauritius and (3) a phytochemical investigation of Psiadia arguta,…

Advisors/Committee Members: Gauvin-Bialecki, Anne (thesis director), Frédérich, Michel (thesis director).

Subjects/Keywords: Psiadia; Psiadia arguta; Métabolomique; Rmn; Activité antipaludique; Activité anti-Inflammatoire; Activité anticancéreuse; Diterpènes; Psiadia; Psiadia arguta; Metabolomic; Nmr; Antimalarial activity; Anti-Inflammatory activity; Anticancer activity; Diterpenes

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Mahadeo, K. (2018). Étude métabolomique et valorisation pharmacologique et biotechnologique d'éspèces du genre Psiadia endémiques de la Réunion et de l'ile Maurice : Metabolomic study and pharmacological and biotechnological valorization of species of the Psiadia genus endemic to Reunion and Mauritius. (Doctoral Dissertation). La Réunion. Retrieved from http://www.theses.fr/2018LARE0001

Chicago Manual of Style (16^th Edition):

Mahadeo, Keshika. “Étude métabolomique et valorisation pharmacologique et biotechnologique d'éspèces du genre Psiadia endémiques de la Réunion et de l'ile Maurice : Metabolomic study and pharmacological and biotechnological valorization of species of the Psiadia genus endemic to Reunion and Mauritius.” 2018. Doctoral Dissertation, La Réunion. Accessed January 24, 2021. http://www.theses.fr/2018LARE0001.

MLA Handbook (7^th Edition):

Mahadeo, Keshika. “Étude métabolomique et valorisation pharmacologique et biotechnologique d'éspèces du genre Psiadia endémiques de la Réunion et de l'ile Maurice : Metabolomic study and pharmacological and biotechnological valorization of species of the Psiadia genus endemic to Reunion and Mauritius.” 2018. Web. 24 Jan 2021.

Vancouver:

Mahadeo K. Étude métabolomique et valorisation pharmacologique et biotechnologique d'éspèces du genre Psiadia endémiques de la Réunion et de l'ile Maurice : Metabolomic study and pharmacological and biotechnological valorization of species of the Psiadia genus endemic to Reunion and Mauritius. [Internet] [Doctoral dissertation]. La Réunion; 2018. [cited 2021 Jan 24]. Available from: http://www.theses.fr/2018LARE0001.

Council of Science Editors:

Mahadeo K. Étude métabolomique et valorisation pharmacologique et biotechnologique d'éspèces du genre Psiadia endémiques de la Réunion et de l'ile Maurice : Metabolomic study and pharmacological and biotechnological valorization of species of the Psiadia genus endemic to Reunion and Mauritius. [Doctoral Dissertation]. La Réunion; 2018. Available from: http://www.theses.fr/2018LARE0001

14. Nicolli Bellotti de Souza. Avaliação da atividade antiplasmodial de análogos da cloroquina.

Degree: 2011, Universidade Federal de Juiz de Fora

URL: http://www.bdtd.ufjf.br/tde_busca/arquivo.php?codArquivo=985

►

A malária é causada por protozoários do gênero Plasmodium e é responsável por 250 milhões de casos e 1 milhão de mortes anualmente. Um dos… (more)

▼

A malária é causada por protozoários do gênero Plasmodium e é responsável por 250 milhões de casos e 1 milhão de mortes anualmente. Um dos principais empecilhos para o controle da doença é o desenvolvimento de resistência do parasito aos fármacos comumente usados, o que torna urgente a pesquisa por novos antimaláricos. Nesse contexto, análogos de cloroquina acoplados a 6-mercaptopurina e a alquil aminas e complexos de platina foram avaliados quanto a atividade antimalárica utilizando o teste supressivo descrito por Peters em modelo murino de infecção por Plasmodium berghei NK65. Tais análogos exibiram altos valores de supressão da parasitemia, entre 60% e 94% em comparação com o controle não tradado. Considerando o papel imunossupressor de derivados de purina, o análogo de cloroquina acoplado a 6-mercaptopurina MPQUI foi avaliado quanto a aspectos imunológicos (contagem de leucócitos específicos, dosagem de TNF-α e IL-10), não interferindo na resposta imune tendo como base os parâmetros analisados. Portanto, esses análogos devem ser objetos de futuras pesquisas, podendo fornecer novos antimaláricos, já que apresentaram-se promissores e não influenciaram a resposta imune nos parâmetros analisados

Malaria is caused by protozoan parasites of the genus Plasmodium and is responsible for 250 million cases and 1 million deaths annually. One of the main obstacles for the disease control is the development of resistance by the parasite to the commonly used antimalarials, what makes the research for new ones urgent. In this context, chloroquine analogs attached to 6-mercaptopurine and to alkyl-amines and platinum complexes were evaluated for their antimalarial activity using the 4-day suppressive test described by Peters which was carried out in mice infected with Plasmodium berghei NK65. These analogs exhibited high values of parasitemia suppression, which ranged from 60% to 94% in comparison to untreated control. Considering the immune suppressor role of purine derivates, the chloroquine analog attached to 6-mercaptopurine MPQUI was evaluated for immunological aspects (specific leukocytes count, TNF-α and IL-10 measurements in sera of mice), revealing no interference in the immune response considering these parameters. Therefore, these analogs may be objects of further research, aiming at new antimalarials, since they were shown to be promising and did not influence the immune response in the parameters analyzed

Advisors/Committee Members: Adilson David da Silva, Clarice Abramo, Antoniana Ursine Krettli.

Subjects/Keywords: PARASITOLOGIA; Malária; Plasmodium berghei; Atividade antimalárica; Análogos de cloroquina; Alquil-aminas; Complexos de Platina; 6-mercaptopurina; Malaria; Plasmodium berghei; Antimalarial activity; Chloroquine analogs; Alkyl-amines; Platinum complexes; 6-mercaptopurine

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Souza, N. B. d. (2011). Avaliação da atividade antiplasmodial de análogos da cloroquina. (Thesis). Universidade Federal de Juiz de Fora. Retrieved from http://www.bdtd.ufjf.br/tde_busca/arquivo.php?codArquivo=985

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Souza, Nicolli Bellotti de. “Avaliação da atividade antiplasmodial de análogos da cloroquina.” 2011. Thesis, Universidade Federal de Juiz de Fora. Accessed January 24, 2021. http://www.bdtd.ufjf.br/tde_busca/arquivo.php?codArquivo=985.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Souza, Nicolli Bellotti de. “Avaliação da atividade antiplasmodial de análogos da cloroquina.” 2011. Web. 24 Jan 2021.

Vancouver:

Souza NBd. Avaliação da atividade antiplasmodial de análogos da cloroquina. [Internet] [Thesis]. Universidade Federal de Juiz de Fora; 2011. [cited 2021 Jan 24]. Available from: http://www.bdtd.ufjf.br/tde_busca/arquivo.php?codArquivo=985.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Souza NBd. Avaliação da atividade antiplasmodial de análogos da cloroquina. [Thesis]. Universidade Federal de Juiz de Fora; 2011. Available from: http://www.bdtd.ufjf.br/tde_busca/arquivo.php?codArquivo=985

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Universidade do Estado do Rio de Janeiro

15. Graziela da Silva Mello. Avaliação do potencial antimalárico de Norantea brasiliensis Choisy (Marcgraviaceae) cultivada in vitro e in vivo .

Degree: Master, 2012, Universidade do Estado do Rio de Janeiro

URL: http://www.bdtd.uerj.br/tde_busca/arquivo.php?codArquivo=8936 ;

►

A malária é uma doença infecciosa causada por protozoários do gênero Plasmodium, transmitidos ao homem, principalmente, através da picada do mosquito infectado. O tratamento é… (more)

▼

A malária é uma doença infecciosa causada por protozoários do gênero Plasmodium, transmitidos ao homem, principalmente, através da picada do mosquito infectado. O tratamento é realizado por meio do uso de drogas, como a cloroquina, uma vez que não há vacina eficiente contra a doença. Porém, a resistência dos parasitos aos medicamentos tem levado à busca por novas substâncias com atividade antimalárica, inclusive de origem vegetal. Nesse contexto, o presente trabalho teve por objetivo avaliar a atividade antimalárica de extratos metanólicos de Norantea brasiliensis cultivada sob condições in vivo e in vitro, espécie nativa ocorrente em restingas, com potencial medicinal já comprovado para várias atividades. Foram desenvolvidos protocolos de calogênese e cultura de raízes da espécie visando à definição de um sistema de produção de metabólitos. Para a cultura in vitro, explantes foram inoculados em meio líquido e sólido contendo diferentes fitorreguladores e concentrações. A partir da cultura de tecidos, foram testados extratos do material produzido biotecnologicamente para comparação com o material botânico cultivado no campo. Os testes sobre o potencial antimalárico foram realizados in vivo, utilizando-se camundongos infectados pelo Plasmodium berghei ANKA, e in vitro utilizando o Plasmodium falciparum. Em seguida foram administrados a cloroquina e os extratos vegetais. A parasitemia foi observada seguindo os protocolos já estabelecidos pelo Laboratório de Imunofarmacologia do Instituto Oswaldo Cruz (IOC). Resultados mostraram que explantes foliares e caulinares de plantas germinadas in vitro, inoculados em meio sólido B5 suplementado com 2,0 mg.mL-1 de ANA, são as melhores fontes para a produção de raízes, apresentando maiores valores de peso fresco e peso seco, mostrando-se um sistema promissor para a produção in vitro de metabólitos da espécie. A avaliação da atividade antimalárica in vivo revelou seu potencial a partir de extrato de raízes de planta cultivada in vivo, na concentração de 50 mg/kg apresentando redução significativa da parasitemia quando comparada com o controle não tratado. Paralelamente, nos testes in vitro a concentração de 100 μg/kg do extrato de raízes de planta cultivada in vivo apresentou diferença significativa quando comparada com as outras concentrações testadas e o controle negativo. Além disso, há uma tendência de aumento do efeito inibitório conforme o aumento da concentração do extrato. Os resultados indicam o potencial de atividade antimalárica em raízes de N. brasiliensis, sendo este estudo o primeiro realizado para a espécie

Malaria is an infectious disease caused by protozoa of the genus Plasmodium, transmitted to humans primarily through the bite of an infected mosquito. The treatment is accomplished through the use of drugs such as chloroquine, since there is no effective vaccine against the disease. However, the resistance of parasites to drugs has led to the search for new antimalarial substances, including vegetable. In this context, this study aimed to evaluate the…

Advisors/Committee Members: Andrea Furtado Macedo, Claudia Simões Gurgel, Silvia Amaral Gonçalves da Silva, Valber da Silva Frutuoso, Norma Albarello.

Subjects/Keywords: BOTANICA; Plant medicinal; Atividade antimalárica; Cultura in vitro de raízes; Marcgraviacea - Cultivo; Antimaláricos; Malária; Fertilização in vitro; N. brasiliensis; Planta medicinal; N.brasiliensis; In vitro roots culture; Antimalarial activity

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Mello, G. d. S. (2012). Avaliação do potencial antimalárico de Norantea brasiliensis Choisy (Marcgraviaceae) cultivada in vitro e in vivo . (Masters Thesis). Universidade do Estado do Rio de Janeiro. Retrieved from http://www.bdtd.uerj.br/tde_busca/arquivo.php?codArquivo=8936 ;

Chicago Manual of Style (16^th Edition):

Mello, Graziela da Silva. “Avaliação do potencial antimalárico de Norantea brasiliensis Choisy (Marcgraviaceae) cultivada in vitro e in vivo .” 2012. Masters Thesis, Universidade do Estado do Rio de Janeiro. Accessed January 24, 2021. http://www.bdtd.uerj.br/tde_busca/arquivo.php?codArquivo=8936 ;.

MLA Handbook (7^th Edition):

Mello, Graziela da Silva. “Avaliação do potencial antimalárico de Norantea brasiliensis Choisy (Marcgraviaceae) cultivada in vitro e in vivo .” 2012. Web. 24 Jan 2021.

Vancouver:

Mello GdS. Avaliação do potencial antimalárico de Norantea brasiliensis Choisy (Marcgraviaceae) cultivada in vitro e in vivo . [Internet] [Masters thesis]. Universidade do Estado do Rio de Janeiro; 2012. [cited 2021 Jan 24]. Available from: http://www.bdtd.uerj.br/tde_busca/arquivo.php?codArquivo=8936 ;.

Council of Science Editors:

Mello GdS. Avaliação do potencial antimalárico de Norantea brasiliensis Choisy (Marcgraviaceae) cultivada in vitro e in vivo . [Masters Thesis]. Universidade do Estado do Rio de Janeiro; 2012. Available from: http://www.bdtd.uerj.br/tde_busca/arquivo.php?codArquivo=8936 ;

Virginia Tech

16. Ghavami, Maryam. Antimalarial Agents: New Mechanisms of Actions for Old and New Drugs.

Degree: PhD, Chemistry, 2018, Virginia Tech

URL: http://hdl.handle.net/10919/96192

► Worldwide, malaria is one of the deadliest diseases. In 2016 it sickened 216 million people and caused 445,000 deaths. In order to control the spread… (more)

▼ Worldwide, malaria is one of the deadliest diseases. In 2016 it sickened 216 million people and caused 445,000 deaths. In order to control the spread of this deadly diseases to human, we can either target the mosquito vector (Anopheles gambiae) or the parasite (Plasmodium falciparum). Due to recent emergence of resistance to current insecticides and antimalarial drugs there is a pressing need to discover and develop new agents that engage new targets in these organisms. To circumvent the effect of resistance to pyrethroid insecticides on the efficacy of insecticide treated nets (ITNs), the use of acetylcholinesterase (AChE) inhibitors on ITNs has drawn attention. In the first project, we explored a small library of g- substituted oxoisoxazole- 2(3H)-carboxamides and isoxazol-3-yl carbamates, and nitriles as AChE inhibitors targeting wild- type (G3) and resistant (Akron) An. gambiae mosquito. In total 23 compounds were synthesized and evaluated. Both carbamates and carboximides with a 2-cyclopropylethyl side chain (1-87a and 1-88a) were extremely toxic to Akron mosquitos, yet these compounds did not exhibit appreciable selectivity between human and An. gambiae AChE. Unfortunately, none of the nitriles showed appreciable toxicity to G3 strain of the mosquitoes, nor did they inhibit An. gambiae AChE. In the second project, conducted in collaboration with Professor Michael Klemba, we focused on the mode of action of an established antimalarial drug, Mefloquine (MQ). Dr. Klemba's recently developed amino acid efflux assay was used to determine the effect of MQ and its open-ring analogs on hemoglobin endocytosis and catabolism in P. falciparum-infected erythrocytes. In total 26 MQ analogs were synthesized and 18 were studied in depth to determine their potency to inhibit leucine (Leu) efflux and parasite growth (SYBR Green). An excellent correlation (R2 = 0.98) over nearly 4 log units was seen for these 18 compounds in the two assays. These data are consistent with the hypothesis that the antimalarial action of these compounds principally derives from inhibition of hemoglobin endocytosis. After this observation, a number of photo-affinity probes were designed and synthesized in hopes of isolating the molecular target of MQ. These analogs are currently being used by Dr. Klemba in pull-down experiments. In the third project, conducted in collaboration with Professor Belen Cassera, we sought to optimize a new antimalarial drug lead that would circumvent current resistance mechanisms. In Plasmodium parasites, the methylerythritol phosphate (MEP) pathway is known to be essential for its growth. This pathway is absent in humans, presenting the opportunity to develop potentially safe and effective therapeutic candidates. Previous work in the Cassera and Carlier lab had established that MMV008138 was the only compound in the Malaria Box that targeted the MEP pathway and that it was (1R,3S)-configured. My research expanded previous efforts in the Carlier group and produced synthesis of 73 analogs of MMV008138 (3-21a'1) that… Advisors/Committee Members: Carlier, Paul R. (committeechair), Kingston, David G. I. (committee member), Santos, Webster (committee member), Tanko, James M. (committee member).

Subjects/Keywords: Malaria; Antimalarial; Acetylcholinesterase; Heterocyclic carbamates and carboxamides; Nitriles; Mefloquine; Mode of action; Leu efflux; Photo affinity probe; IspD; MEP pathway; MMV008138; Structure- activity relationship

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Ghavami, M. (2018). Antimalarial Agents: New Mechanisms of Actions for Old and New Drugs. (Doctoral Dissertation). Virginia Tech. Retrieved from http://hdl.handle.net/10919/96192

Chicago Manual of Style (16^th Edition):

Ghavami, Maryam. “Antimalarial Agents: New Mechanisms of Actions for Old and New Drugs.” 2018. Doctoral Dissertation, Virginia Tech. Accessed January 24, 2021. http://hdl.handle.net/10919/96192.

MLA Handbook (7^th Edition):

Ghavami, Maryam. “Antimalarial Agents: New Mechanisms of Actions for Old and New Drugs.” 2018. Web. 24 Jan 2021.

Vancouver:

Ghavami M. Antimalarial Agents: New Mechanisms of Actions for Old and New Drugs. [Internet] [Doctoral dissertation]. Virginia Tech; 2018. [cited 2021 Jan 24]. Available from: http://hdl.handle.net/10919/96192.

Council of Science Editors:

Ghavami M. Antimalarial Agents: New Mechanisms of Actions for Old and New Drugs. [Doctoral Dissertation]. Virginia Tech; 2018. Available from: http://hdl.handle.net/10919/96192

17. LIU MEI. Investigations on the antimalarial activity of alkoxylated and hydroxylated chalcones.

Degree: 2003, National University of Singapore

URL: http://scholarbank.nus.edu.sg/handle/10635/13520

Subjects/Keywords: antimalarial activty; alkoxylated chalcones; hydroxylated chalcones; structure-activity relationship; mode of action; antileishmanial activity.

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

MEI, L. (2003). Investigations on the antimalarial activity of alkoxylated and hydroxylated chalcones. (Thesis). National University of Singapore. Retrieved from http://scholarbank.nus.edu.sg/handle/10635/13520

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

MEI, LIU. “Investigations on the antimalarial activity of alkoxylated and hydroxylated chalcones.” 2003. Thesis, National University of Singapore. Accessed January 24, 2021. http://scholarbank.nus.edu.sg/handle/10635/13520.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

MEI, LIU. “Investigations on the antimalarial activity of alkoxylated and hydroxylated chalcones.” 2003. Web. 24 Jan 2021.

Vancouver:

MEI L. Investigations on the antimalarial activity of alkoxylated and hydroxylated chalcones. [Internet] [Thesis]. National University of Singapore; 2003. [cited 2021 Jan 24]. Available from: http://scholarbank.nus.edu.sg/handle/10635/13520.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

MEI L. Investigations on the antimalarial activity of alkoxylated and hydroxylated chalcones. [Thesis]. National University of Singapore; 2003. Available from: http://scholarbank.nus.edu.sg/handle/10635/13520

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

18. Campos, Pierre-Éric. Biodiversité des invertébrés marins : de l'isolement à la modélisation moléculaire de métabolites secondaires pour la découverte de nouveaux candidats médicaments : Biodiversity of marine invertebrates : from isolation to molecular modeling of secondary metabolites for the discovery of new drug candidates.

Degree: Docteur es, Chimie, 2017, Université de la Réunion

URL: http://www.theses.fr/2017LARE0007

►

Les travaux de thèse exposés dans ce manuscrit portent sur l'étude chimique de quatre éponges marines collectées à Madagascar : Monanchora unguiculata, Amphimedon sp., Aulospongus… (more)

▼

Les travaux de thèse exposés dans ce manuscrit portent sur l'étude chimique de quatre éponges marines collectées à Madagascar : Monanchora unguiculata, Amphimedon sp., Aulospongus gardineri et Biemna laboutei. Pour les trois premières, l'extraction, l'isolement et l'identification des métabolites secondaires par différentes techniques chromatographiques (CLMP, CLHP…) et spectroscopiques (UV-visible, SMHR, RMN 1D et 2D…) ont été envisagés. Quinze métabolites secondaires de type alcaloïdes guanidiniques, dérivés de la bromotyrosine, N-acyléthanolamines et polyynes, ont été isolés de ces éponges. Huit sont de structures nouvelles. La valorisation des molécules isolées a ensuite été envisagée via l'évaluation de leurs activités biologiques. Deux d'entres elles, la fromiamycaline (M70) et la ptilomycaline F (MU7) ont montré une excellente activité antipaludique et quatre, la fromiamycaline (M70) et les ptilomycalines E (MU6), G (MU8) et H (MU9) une cytotoxicité sur cellules KB prometteuse. L'étude de la dernière éponge, Biemna laboutei, portait sur des molécules précédemment isolées au sein du LCSNSA. Les travaux entrepris comprenaient une vérification des configurations relatives de neuf alcaloïdes guanidiniques déterminées par RMN grâce à la probabilité DP4+. Les configurations relatives déterminées par RMN de sept des molécules ont ainsi pu être confirmées et trois d'entre elles, les nétamines G (E8), P (E17) et R (E19) ont fait l'objet d'une étude plus approfondie par modélisation moléculaire afin de déterminer leur configuration absolue par comparaison de leur spectre de Dichroïsme Circulaire Électronique expérimental avec un spectre calculé.

The work described in this manuscript concerns the chemical study of four sponges from Madagascar: Monanchora unguiculata, Amphimedon sp., Aulospongus gardineri and Biemna laboutei. For the first three sponges, the study was devoted to the extraction, isolation and identification of secondary metabolites by various chromatographic (MPLC, HPLC…) and spectroscopic (UV, HRMS, 1D and 2D NMR…) techniques. Fitfteen secondary metabolites including guanidine alkaloids, bromotyrosin derivated, N-acylethanolamines and polyynes were isolated from these sponges. Eight are new molecules. The biological activities of the isolated compounds were then evaluated. Two of them, fromiamycalin (M70) and ptilomycalin F (MU7) showed a very good antimalarial activity and four of them, fromiamycalin (M70) and ptilomycalins E (MU6), G (MU8) and H (MU9) a promising cytotoxicity against KB cells. The study of the last sponge, Biemna laboutei, was performed on molecules already isolated in the LCSNSA. This work included the determination of the relative configuration of nine guanidine alkaloids by using the DP4+ probability. The relative configuration of seven molecules was confirmed. Three of them, netamines G (E8), P (E17) and R (E19) were selected for a study by molecular modeling to determine their absolute configuration by comparison of their experimental Electronic Circular Dichroism spectrum with…

Advisors/Committee Members: Illien, Bertrand (thesis director), Gauvin-Bialecki, Anne (thesis director).

Subjects/Keywords: Océan Indien; Éponges marines; Monanchora unguiculata; Amphimedon sp; Aulospongus gardineri; Biemna laboutei; Métabolites secondaires; Activité antipaludique; Indian Ocean; Marine sponges; Monanchora unguiculata; Amphimedon sp; Aulospongus gardineri; Biemna laboutei; Secondary metabolites; Antimalarial activity

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Campos, P. (2017). Biodiversité des invertébrés marins : de l'isolement à la modélisation moléculaire de métabolites secondaires pour la découverte de nouveaux candidats médicaments : Biodiversity of marine invertebrates : from isolation to molecular modeling of secondary metabolites for the discovery of new drug candidates. (Doctoral Dissertation). Université de la Réunion. Retrieved from http://www.theses.fr/2017LARE0007

Chicago Manual of Style (16^th Edition):

Campos, Pierre-Éric. “Biodiversité des invertébrés marins : de l'isolement à la modélisation moléculaire de métabolites secondaires pour la découverte de nouveaux candidats médicaments : Biodiversity of marine invertebrates : from isolation to molecular modeling of secondary metabolites for the discovery of new drug candidates.” 2017. Doctoral Dissertation, Université de la Réunion. Accessed January 24, 2021. http://www.theses.fr/2017LARE0007.

MLA Handbook (7^th Edition):

Campos, Pierre-Éric. “Biodiversité des invertébrés marins : de l'isolement à la modélisation moléculaire de métabolites secondaires pour la découverte de nouveaux candidats médicaments : Biodiversity of marine invertebrates : from isolation to molecular modeling of secondary metabolites for the discovery of new drug candidates.” 2017. Web. 24 Jan 2021.

Vancouver:

Campos P. Biodiversité des invertébrés marins : de l'isolement à la modélisation moléculaire de métabolites secondaires pour la découverte de nouveaux candidats médicaments : Biodiversity of marine invertebrates : from isolation to molecular modeling of secondary metabolites for the discovery of new drug candidates. [Internet] [Doctoral dissertation]. Université de la Réunion; 2017. [cited 2021 Jan 24]. Available from: http://www.theses.fr/2017LARE0007.

Council of Science Editors:

Campos P. Biodiversité des invertébrés marins : de l'isolement à la modélisation moléculaire de métabolites secondaires pour la découverte de nouveaux candidats médicaments : Biodiversity of marine invertebrates : from isolation to molecular modeling of secondary metabolites for the discovery of new drug candidates. [Doctoral Dissertation]. Université de la Réunion; 2017. Available from: http://www.theses.fr/2017LARE0007

19. Perez Llanos , Francy Johanna. Development of a novel mid throughput platform for the search of compounds against P. falciparum parasite in metagenomes.

Degree: 2015, Universidad de los Andes

URL: http://documentodegrado.uniandes.edu.co/documentos/201210449_fecha_2013_12_05_hora_09_40_49_parte_1.pdf

► La malaria es una enfermedad importante en salud pública a nivel mundial debido al alto endemismo, muertes producidas y al desarrollo de la resistencia a… (more)

▼ La malaria es una enfermedad importante en salud pública a nivel mundial debido al alto endemismo, muertes producidas y al desarrollo de la resistencia a los medicamentos antimaláricos por el parasito que la causa. Por lo tanto el descubrimiento de nuevos compuestos antimaláricos es una prioridad de la investigación en salud. Como respuesta a esta necesidad, se están explorando nuevas alternativas para el control de la malaria. Un caso específico es este estudio, con el objetivo de desarrollar una plataforma para la exploración de compuestos antimaláricos en metagenomas. Para configurar los componentes básicos de este enfoque informamos: 1) El establecimiento y estandarización del crecimiento de un clon bioluminiscente de P. falciparum en microplacas de múltiples pocillos para la rápida determinación de viabilidad y compuestos, seguido del uso práctico de este sistema para la detección y análisis del comportamiento antimalárico de 1780 extractos bacterianos totales de clones fosmidicos que contienen ADN del medio ambiente para detectar actividades antimaláricas diferenciales codificadas en 23 librerías metagenomicas. Al mismo tiempo hemos validado y optimizado una herramienta genética construida para evaluar el potencial de tener actividad en un extracto bacteriano metagenómico. Esta herramienta fue desarrollada y probada para ser una prueba concepto de control positivo para la selección de actividades antimaláricas. Se compone de un gen sintético del péptido antimalárico Dermaseptina 4 clonado en un inserto metagenomico dentro de un vector fosmidico (llamado pCC2FOS-076-DS4) alojado en E.coli EPI300. Se confirmó la transcripción de DS4 en este contexto, el extracto bacteriano derivado de la transformante incluyendo todas las mejoras inhibió el crecimiento del parásito bioluminiscente remarcando su potencial como herramienta genética para perfeccionar los umbrales de discriminación comparativa más fina de actividades antimaláricas en la plataforma desarrollada. Advisors/Committee Members: Restrepo Restrepo Silvia (advisor), Howard Armando Junca Díaz (advisor).

Subjects/Keywords: Malaria; Bioluminescent parasite; Antimalarial activity; E. coli EPI300; Dermaseptin 4; Bacterial extract; Parasite growth inhibition.

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Perez Llanos , F. J. (2015). Development of a novel mid throughput platform for the search of compounds against P. falciparum parasite in metagenomes. (Thesis). Universidad de los Andes. Retrieved from http://documentodegrado.uniandes.edu.co/documentos/201210449_fecha_2013_12_05_hora_09_40_49_parte_1.pdf

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Perez Llanos , Francy Johanna. “Development of a novel mid throughput platform for the search of compounds against P. falciparum parasite in metagenomes. ” 2015. Thesis, Universidad de los Andes. Accessed January 24, 2021. http://documentodegrado.uniandes.edu.co/documentos/201210449_fecha_2013_12_05_hora_09_40_49_parte_1.pdf.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Perez Llanos , Francy Johanna. “Development of a novel mid throughput platform for the search of compounds against P. falciparum parasite in metagenomes. ” 2015. Web. 24 Jan 2021.

Vancouver:

Perez Llanos FJ. Development of a novel mid throughput platform for the search of compounds against P. falciparum parasite in metagenomes. [Internet] [Thesis]. Universidad de los Andes; 2015. [cited 2021 Jan 24]. Available from: http://documentodegrado.uniandes.edu.co/documentos/201210449_fecha_2013_12_05_hora_09_40_49_parte_1.pdf.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Perez Llanos FJ. Development of a novel mid throughput platform for the search of compounds against P. falciparum parasite in metagenomes. [Thesis]. Universidad de los Andes; 2015. Available from: http://documentodegrado.uniandes.edu.co/documentos/201210449_fecha_2013_12_05_hora_09_40_49_parte_1.pdf

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

University of Melbourne

20. TEGUH, SILVIA. Synthesis and investigation of activities and modes of action of antimalarial compounds.

Degree: 2015, University of Melbourne

URL: http://hdl.handle.net/11343/55614

► Syntheses, structure-activity relationships and mode of action investigations of a novel compound series of conjugated quinoline-indole, revealed that they are active against blood stages of… (more)

Subjects/Keywords: quinoline; indole; organic synthesis; artemisinin; click chemistry; bioconjugation; mitochondria; P. falciparum; malaria; structure-activity relationship; bait and probe; mode of action; antiplasmodial pulse assay; hematin; delocalised lipophilic cation; antimalarial compound; Bicyclo[6,1,0]non-4-yn-9-yl-artemisinin; artemisinin-azide; mitotracker

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

TEGUH, S. (2015). Synthesis and investigation of activities and modes of action of antimalarial compounds. (Doctoral Dissertation). University of Melbourne. Retrieved from http://hdl.handle.net/11343/55614

Chicago Manual of Style (16^th Edition):

TEGUH, SILVIA. “Synthesis and investigation of activities and modes of action of antimalarial compounds.” 2015. Doctoral Dissertation, University of Melbourne. Accessed January 24, 2021. http://hdl.handle.net/11343/55614.

MLA Handbook (7^th Edition):

TEGUH, SILVIA. “Synthesis and investigation of activities and modes of action of antimalarial compounds.” 2015. Web. 24 Jan 2021.

Vancouver:

TEGUH S. Synthesis and investigation of activities and modes of action of antimalarial compounds. [Internet] [Doctoral dissertation]. University of Melbourne; 2015. [cited 2021 Jan 24]. Available from: http://hdl.handle.net/11343/55614.

Council of Science Editors:

TEGUH S. Synthesis and investigation of activities and modes of action of antimalarial compounds. [Doctoral Dissertation]. University of Melbourne; 2015. Available from: http://hdl.handle.net/11343/55614

21. Liu, Lixuan. MMV008138 and analogs: potential novel antimalarial agents for P. falciparum.

Degree: MS, Chemistry, 2018, Virginia Tech

URL: http://hdl.handle.net/10919/95315

► Malaria is a severe and deadly mosquito-borne disease. Although treatable, the continuous emergence of multi-drug resistant parasite strains urgently calls for the development of novel… (more)

▼ Malaria is a severe and deadly mosquito-borne disease. Although treatable, the continuous emergence of multi-drug resistant parasite strains urgently calls for the development of novel antimalarial agents. P. falciparum parasites synthesize essential isoprenoid precursors, isopentenyl pyrophosphate (IPP) and dimethylallyl pyrophosphate (DMAPP), via a non-mevalonate pathway: the methylerythritol phosphate (MEP) pathway. This pathway is not utilized by humans. Thus, compounds that target the MEP pathway and disrupt isoprenoid biosynthesis in P. falciparum hold promise as potent and safe new antimalarial agents, that engage new targets. Previously, we and others identified MMV008138 from the Malaria Box as a MEP pathway targeting compound. Later work revealed that it targets the IspD enzyme within the MEP pathway. Work in the Carlier group has established preliminary structure-activity relationship (SAR) of MMV008138: 1) (1R,3S)-configuration is required; 2) 2', 4'-disubstitution of the D-ring with small, electronegative substituents; 3) functional importance of carboxylate acid at C3. In this work, I aim to gain further insight into the C3 SAR and A-ring SAR of lead compound MMV008138. Synthesized acid bioisosteres and A-ring analogs of MMV008138 were evaluated in their ability to inhibit P. falciparum parasite growth. We showed that the C3 substituent of MMV008138 has a very tight SAR, and likely interacts with a very constricted pocket within the PfIspD enzyme. A-ring modifications are limited to certain positions of MMV001838 and need to be sterically small. However, we have yet to identify a modification that significantly improves drug lead potency. Future work will continue towards understanding the A-ring SAR of MMV008138, as well as D-ring SAR and C1-SAR. Efforts will also be directed towards finding analogs with improved potency, transport and metabolic stability. Advisors/Committee Members: Carlier, Paul R. (committeechair), Tanko, James M. (committee member), Kingston, David G. I. (committee member).

Subjects/Keywords: malaria; antimalarial; P. falciparum; MEP pathway; IspD; MMV008138; structure-activity relationship

…need to develop new antimalarial agents that are of high activity and safe to administer. As… …FR900098 (12) �� ... �� …8 Table 2. In vitro activity study of DOX, FOS (11… …for Novel Antimalarial Development 1.1 Malaria 1.1.1 Malaria and Malaria Parasites Malaria… …also contributes to reducing malaria transmission. Antimalarial development is critical to… …clinically and historically important antimalarial agents include: quinine, chloroquine, mefloquine…

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APA (6^th Edition):

Liu, L. (2018). MMV008138 and analogs: potential novel antimalarial agents for P. falciparum. (Masters Thesis). Virginia Tech. Retrieved from http://hdl.handle.net/10919/95315

Chicago Manual of Style (16^th Edition):

Liu, Lixuan. “MMV008138 and analogs: potential novel antimalarial agents for P. falciparum.” 2018. Masters Thesis, Virginia Tech. Accessed January 24, 2021. http://hdl.handle.net/10919/95315.

MLA Handbook (7^th Edition):

Liu, Lixuan. “MMV008138 and analogs: potential novel antimalarial agents for P. falciparum.” 2018. Web. 24 Jan 2021.

Vancouver:

Liu L. MMV008138 and analogs: potential novel antimalarial agents for P. falciparum. [Internet] [Masters thesis]. Virginia Tech; 2018. [cited 2021 Jan 24]. Available from: http://hdl.handle.net/10919/95315.

Council of Science Editors:

Liu L. MMV008138 and analogs: potential novel antimalarial agents for P. falciparum. [Masters Thesis]. Virginia Tech; 2018. Available from: http://hdl.handle.net/10919/95315

University of KwaZulu-Natal

22. Nyaba, Zoxolo Nokulunga. Antiplasmodial activity of Warburgia salutaris (Bertol. F.) Chiov. (Cannelaceae).

Degree: 2017, University of KwaZulu-Natal

URL: https://researchspace.ukzn.ac.za/handle/10413/16620

Abstract available in PDF file. Advisors/Committee Members: Simelane, Mthokozisi Blessing Cedric. (advisor), Murambiwa, Pretty. (advisor).

Subjects/Keywords: Theses - Biochemistry.; Antimalarials.; Warburgia salutaris.; Medicinal plants - South Africa.; Plasmodium falciparum.; Warburia salutaris.; Molecular docking.; Plasmodium berghei.; Mukaadial acetate.; Antiplasmodial activity.; Antimalarial drugs.; Malaria.

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Nyaba, Z. N. (2017). Antiplasmodial activity of Warburgia salutaris (Bertol. F.) Chiov. (Cannelaceae). (Thesis). University of KwaZulu-Natal. Retrieved from https://researchspace.ukzn.ac.za/handle/10413/16620

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Nyaba, Zoxolo Nokulunga. “Antiplasmodial activity of Warburgia salutaris (Bertol. F.) Chiov. (Cannelaceae).” 2017. Thesis, University of KwaZulu-Natal. Accessed January 24, 2021. https://researchspace.ukzn.ac.za/handle/10413/16620.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Nyaba, Zoxolo Nokulunga. “Antiplasmodial activity of Warburgia salutaris (Bertol. F.) Chiov. (Cannelaceae).” 2017. Web. 24 Jan 2021.

Vancouver:

Nyaba ZN. Antiplasmodial activity of Warburgia salutaris (Bertol. F.) Chiov. (Cannelaceae). [Internet] [Thesis]. University of KwaZulu-Natal; 2017. [cited 2021 Jan 24]. Available from: https://researchspace.ukzn.ac.za/handle/10413/16620.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Nyaba ZN. Antiplasmodial activity of Warburgia salutaris (Bertol. F.) Chiov. (Cannelaceae). [Thesis]. University of KwaZulu-Natal; 2017. Available from: https://researchspace.ukzn.ac.za/handle/10413/16620

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

23. Nyo Mi Swe. Benz[f]indole誘導体の新規な反応性と生理活性物質合成への展開 : 抗マラリアおよび抗グリオーマ作用を指向した新規化合物の合成 : New Findings in the Reactivity of Benz[f]indole and Development for the Synthesis of Pharmacologically Active Compounds : Synthesis towards the Novel Compounds Directed Antimalarial and Antiglioma Activity.

Degree: 博士(薬学), 2017, International University of Health and Welfare / 国際医療福祉大学

URL: http://id.nii.ac.jp/1065/00000826/

平成28年度

Subjects/Keywords: benz[f]indole; 求電子置換反応; 抗マラリア作用; 抗グリオーマ作用; benz[f]indole; electrophilic substitution reaction; antimalarial activity; antiglioma activity

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

Swe, N. M. (2017). Benz[f]indole誘導体の新規な反応性と生理活性物質合成への展開 : 抗マラリアおよび抗グリオーマ作用を指向した新規化合物の合成 : New Findings in the Reactivity of Benz[f]indole and Development for the Synthesis of Pharmacologically Active Compounds : Synthesis towards the Novel Compounds Directed Antimalarial and Antiglioma Activity. (Thesis). International University of Health and Welfare / 国際医療福祉大学. Retrieved from http://id.nii.ac.jp/1065/00000826/

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

Swe, Nyo Mi. “Benz[f]indole誘導体の新規な反応性と生理活性物質合成への展開 : 抗マラリアおよび抗グリオーマ作用を指向した新規化合物の合成 : New Findings in the Reactivity of Benz[f]indole and Development for the Synthesis of Pharmacologically Active Compounds : Synthesis towards the Novel Compounds Directed Antimalarial and Antiglioma Activity.” 2017. Thesis, International University of Health and Welfare / 国際医療福祉大学. Accessed January 24, 2021. http://id.nii.ac.jp/1065/00000826/.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

Swe, Nyo Mi. “Benz[f]indole誘導体の新規な反応性と生理活性物質合成への展開 : 抗マラリアおよび抗グリオーマ作用を指向した新規化合物の合成 : New Findings in the Reactivity of Benz[f]indole and Development for the Synthesis of Pharmacologically Active Compounds : Synthesis towards the Novel Compounds Directed Antimalarial and Antiglioma Activity.” 2017. Web. 24 Jan 2021.

Vancouver:

Swe NM. Benz[f]indole誘導体の新規な反応性と生理活性物質合成への展開 : 抗マラリアおよび抗グリオーマ作用を指向した新規化合物の合成 : New Findings in the Reactivity of Benz[f]indole and Development for the Synthesis of Pharmacologically Active Compounds : Synthesis towards the Novel Compounds Directed Antimalarial and Antiglioma Activity. [Internet] [Thesis]. International University of Health and Welfare / 国際医療福祉大学; 2017. [cited 2021 Jan 24]. Available from: http://id.nii.ac.jp/1065/00000826/.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

Council of Science Editors:

Swe NM. Benz[f]indole誘導体の新規な反応性と生理活性物質合成への展開 : 抗マラリアおよび抗グリオーマ作用を指向した新規化合物の合成 : New Findings in the Reactivity of Benz[f]indole and Development for the Synthesis of Pharmacologically Active Compounds : Synthesis towards the Novel Compounds Directed Antimalarial and Antiglioma Activity. [Thesis]. International University of Health and Welfare / 国際医療福祉大学; 2017. Available from: http://id.nii.ac.jp/1065/00000826/

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation

24. 鳥居塚, 洋輔. ヒガンバナ科植物含有Lycorine型アルカロイドに関する化学的研究 : Chemical studies on the Lycorine-type alkaloids from the Amaryllidaceae plants.

Degree: Chiba University / 千葉大学

URL: http://opac.ll.chiba-u.jp/da/curator/900060052/

研究科: 千葉大学大学院薬学研究院

修了年:2009

学位:千大院医薬博甲第薬87号

Advisors/Committee Members: 千葉大学大学院薬学研究院.

Subjects/Keywords: Lycorine; Alkaloid; Antitrypanosomal activity; Antimalarial activity; AChE inhibition; Structure-activity relationship; Natural product synthesis; リコリン; アルカロイド; 抗トリパノソーマ原虫活性; 抗マラリア原虫活性; アセチルコリンエステラーゼ阻害活性; 構造活性相関; 天然物合成

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APA · Chicago · MLA · Vancouver · CSE | Export to Zotero / EndNote / Reference Manager

APA (6^th Edition):

鳥居塚, �. (n.d.). ヒガンバナ科植物含有Lycorine型アルカロイドに関する化学的研究 : Chemical studies on the Lycorine-type alkaloids from the Amaryllidaceae plants. (Thesis). Chiba University / 千葉大学. Retrieved from http://opac.ll.chiba-u.jp/da/curator/900060052/

Note: this citation may be lacking information needed for this citation format:
No year of publication.
Not specified: Masters Thesis or Doctoral Dissertation

Chicago Manual of Style (16^th Edition):

鳥居塚, 洋輔. “ヒガンバナ科植物含有Lycorine型アルカロイドに関する化学的研究 : Chemical studies on the Lycorine-type alkaloids from the Amaryllidaceae plants.” Thesis, Chiba University / 千葉大学. Accessed January 24, 2021. http://opac.ll.chiba-u.jp/da/curator/900060052/.

Note: this citation may be lacking information needed for this citation format:
No year of publication.
Not specified: Masters Thesis or Doctoral Dissertation

MLA Handbook (7^th Edition):

鳥居塚, 洋輔. “ヒガンバナ科植物含有Lycorine型アルカロイドに関する化学的研究 : Chemical studies on the Lycorine-type alkaloids from the Amaryllidaceae plants.” Web. 24 Jan 2021.

Note: this citation may be lacking information needed for this citation format:
No year of publication.

Vancouver:

鳥居塚 �. ヒガンバナ科植物含有Lycorine型アルカロイドに関する化学的研究 : Chemical studies on the Lycorine-type alkaloids from the Amaryllidaceae plants. [Internet] [Thesis]. Chiba University / 千葉大学; [cited 2021 Jan 24]. Available from: http://opac.ll.chiba-u.jp/da/curator/900060052/.

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation
No year of publication.

Council of Science Editors:

鳥居塚 �. ヒガンバナ科植物含有Lycorine型アルカロイドに関する化学的研究 : Chemical studies on the Lycorine-type alkaloids from the Amaryllidaceae plants. [Thesis]. Chiba University / 千葉大学; Available from: http://opac.ll.chiba-u.jp/da/curator/900060052/

Note: this citation may be lacking information needed for this citation format:
Not specified: Masters Thesis or Doctoral Dissertation
No year of publication.

Open Access Theses and Dissertations