Anti-malarial activity of the alkaloid, heptaphylline, and the furanocoumarin, imperatorin, from Clausena anisata against human Plasmodium falciparum malaria parasites: ex vivo trophozoitocidal, schizonticidal and gametocytocidal approach

Malaria Journal

Research

Felix Kwame Zoiku¹  Emmanuel Kofi Kumatia²  Nguyen Huu Tung³  Alex Asase⁴ 

[1] Department of Epidemiology, College of Health Science, Noguchi Memorial Institute for Medical Research, University of Ghana, Accra, Ghana;Department of Phytochemistry, Centre for Plant Medicine Research, P.O. Box 73, Mampong-Akuapem, Ghana;Department of Quality Management, Centre for Plant Medicine Research, Mampong-Akuapem, Ghana;Faculty of Pharmacy, Phenikaa University, 12116, Hanoi, Vietnam;Plant Development Department, Centre for Plant Medicine Research, Mampong-Akuapem, Ghana;

关键词: Malaria;    Alkaloid;    Coumarin;    Plasmodium;    Trophozoite;    Schizont;    Gametocyte;    Cytotoxicity;    Selectivity index;   

DOI  :  10.1186/s12936-023-04678-0

 received in 2023-04-21, accepted in 2023-08-17,  发布年份 2023

来源: Springer

【 摘 要 】

BackgroundThe erythrocytic stage of the life cycle of the malaria parasite, Plasmodium falciparum, consists of trophozoite, schizont and gametocyte stages in humans. Various anti-malarial agents target different stages of the parasite to produce treatment outcomes. This study reports on the stage-specific anti-malarial activity of heptaphylline and imperatorin against human P. falciparum in addition to their cytotoxicity and selectivity indices (SI).MethodsThe compounds were isolated from Clausena anisata using column chromatography and their structures elucidated using NMR spectroscopy. The anti-malarial activity was determined by measuring the trophozoitocidal, schizonticidal and gametocytocidal activities of the compounds using the SYBR green assay. Cytotoxicity was evaluated using the tetrazolium-based colorimetric assay.ResultsHeptaphylline and imperatorin produced trophozoitocidal, schizonticidal and gametocytocidal activities with IC50s of 1.57 (0.2317)–26.92 (0.3144) µM with those of artesunate (the standard drug) being 0.00024 (0.0036)–0.0070 (0.0013) µM. In the cytotoxicity assay, the compounds produced CC50S greater than 350 µM and SI of 13.76–235.90. Also, the trophozoitocidal and schizonticidal activities of the compounds were more pronounced than their gametocytocidal activity. Imperatorin was 42.04% more trophozoitocidal than hepthaphyline. However, hepthaphyline has more schizonticidal and gametocytocidal properties than imperatorin.ConclusionHeptaphylline and imperatorin are promising anti-malarial agents, since they possess potent anti-malarial activity with weak cytotoxicity on RBCs. However, imperatorin is a better anti-malarial prophylactic agent whereas heptaphylline is a better malaria treatment agent.

【 授权许可】

CC BY   
© BioMed Central Ltd., part of Springer Nature 2023

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