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antimalarial

Open Access | Antiplasmodial Activity of Some Medicinal Plants Used in Sudanese Folk-medicine

June 8, 2010 - 09:34 -- Kabogo Ndegwa
Author(s): 
Ahmed el-HM, Nour BY, Mohammed YG, Khalid HS.
Reference: 
Environ Health Insights. 2010 Feb 4;4:1-6

Ten plants indigenous to Sudan and of common use in Sudanese folk-medicine, were examined in vitro for antimalarial activity against schizonts maturation of Plasmodium falciparum, the major human malaria parasite.

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Ethnopharmacological communication: In vitro and in vivo antimalarial and cytotoxic activity of five plants used in congolese traditional medicine

June 4, 2010 - 07:18 -- Patrick Sampao
Author(s): 
M. Lusakibanza, G. Mesia, G. Tona, S. Karemere, A. Lukuka, M. Tits, L. Angenot, M. Frédérich
Reference: 
Journal of Ethnopharmacology, Volume 129, Issue 3, 16 June 2010, Pages 398-402

The growth inhibition of Plasmodium falciparum strains was evaluated using the measurement of lactate dehydrogenase activity.

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Chemical genetics of Plasmodium falciparum

May 20, 2010 - 08:03 -- Kabogo Ndegwa
Author(s): 
W. Armand Guiguemde, Anang A. Shelat, David Bouck, Sandra Duffy, Gregory J. Crowther, Paul H. Davis, David C. Smithson, Michele Connelly, Julie Clark, Fangyi Zhu, et al.
Reference: 
Nature 465, 311-315 (20 May 2010)

To discover new antimalarial chemotypes, we have used a phenotypic forward chemical genetic approach to assay 309,474 chemicals. Here we disclose structures and biological activity of the entire library—many of which showed potent in vitro activity against drug-resistant P. falciparum strains—and detailed profiling of 172 representative candidates.

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Antimicrobial and antimalarial activity of Cussonia species (Araliaceae)

May 17, 2010 - 13:57 -- Patrick Sampao
Author(s): 
B.J. De Villiers, S.F. Van Vuuren, R.L. Van Zyl, B.-E. Van Wyk
Reference: 
Journal of Ethnopharmacology, Volume 129, Issue 2, 27 May 2010, Pages 189-196

Antimalarial sensitivity was studied using Plasmodium falciparum and the [3H]-hypoxanthine incorporation assay. Cytotoxic effects on a T-cell leukaemia (Jurkat) cell line were determined using the tetrazolium-based cellular toxicity assay.

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Mechanism-Based Inhibitors of the Aspartyl Protease Plasmepsin II as Potential Antimalarial Agents

May 10, 2010 - 09:29 -- Kabogo Ndegwa
Author(s): 
D Gupta, RS Yedidi, S Varghese, LC Kovari, PM Woster
Reference: 
J Med Chem May 3, 2010

Four aspartyl proteases known as plasmepsins are involved in the degradation of hemoglobin by Plasmodium falciparum, which causes a large percentage of malaria deaths. The enzyme plasmepsin II (PlmII) is the most extensively studied of these aspartyl proteases and catalyzes the initial step in the breakdown of hemoglobin by the parasite.

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Update: Monitoring antimalarial resistance: launching a cooperative effort

April 28, 2010 - 15:43 -- Patrick Sampao
Author(s): 
Carol Hopkins Sibley, Philippe J. Guerin, Pascal Ringwald
Reference: 
Trends in Parasitology, Volume 26, Issue 5, May 2010, Pages 221-224

A collaborative effort between the Global Malaria Program of the World Health Organization (WHO) and the WorldWide Antimalarial Resistance Network (WWARN) has recently been launched.

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Inhibition of Plasmodium falciparum pH regulation by small molecule indole derivatives results in rapid parasite death

March 11, 2010 - 14:00 -- Patrick Sampao
Author(s): 
Donelly A. van Schalkwyk, Xie W.A. Chan, Paola Misiano, Stefania Gagliardi, Carlo Farina, Kevin J. Saliba
Reference: 
Biochemical Pharmacology, Volume 79, Issue 9, 1 May 2010

The V-type H+-ATPase is critical during the intraerythrocytic stage of the human malaria parasite Plasmodium falciparum. Our data support the disruption of parasite pH regulation through inhibition of its V-type H+-ATPase as an antimalarial approach.

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Characterization of the two major CYP450 metabolites of ozonide (1,2,4-trioxolane) OZ277

March 5, 2010 - 09:10 -- Kabogo Ndegwa
Author(s): 
Lin Zhou, André Alker, Jonathan L. Vennerstrom et al.
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 18, Issue 5, 1 March 2008, Pages 1555-1558

The antimalarial synthetic ozonide OZ277 (RBx11160) was hydroxylated by human liver microsomes at the distal bridgehead carbon atoms of the spiroadamantane substructure to form two carbinol metabolites devoid of antimalarial activity.

An efficient route into synthetically challenging bridged achiral 1,2,4,5-tetraoxanes with antimalarial activity

March 5, 2010 - 09:01 -- Kabogo Ndegwa
Author(s): 
Gemma L. Ellis, Richard Amewu, Charlotte Hall, Karen Rimmer, Steven A. Ward, Paul M. O’Neill
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 18, Issue 5, 1 March 2008, Pages 1720-1724

Using this methodology a range of bridged tetraoxanes which display good in vitro antimalarial activity were synthesized.

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Antimalarial Asexual Stage-Specific and Gametocytocidal Activities of HIV Protease Inhibitors

February 25, 2010 - 21:41 -- Kabogo Ndegwa
Author(s): 
Christopher L. Peatey, Katherine T. Andrews, Nina Eickel, Timothy MacDonald, Alice S. Butterworth, Katharine R. Trenholme, Donald L. Gardiner, James S. McCarthy, and Tina S. Skinner-Adams
Reference: 
Antimicrobial Agents and Chemotherapy, March 2010, Pages 1334-1337, Volume. 54, No. 3

The stage-specific antimalarial activities of a panel of antiretroviral protease inhibitors (PIs), including two nonpeptidic PIs (tipranavir and darunavir), were tested in vitro against Plasmodium falciparum.

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