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.

Autor: Kumatia EK; Department of Phytochemistry, Centre for Plant Medicine Research, P.O. Box 73, Mampong-Akuapem, Ghana. kofi2rhyme@yahoo.com.; Department of Quality Management, Centre for Plant Medicine Research, Mampong-Akuapem, Ghana. kofi2rhyme@yahoo.com., Zoiku FK; Department of Epidemiology, College of Health Science, Noguchi Memorial Institute for Medical Research, University of Ghana, Accra, Ghana., Asase A; Plant Development Department, Centre for Plant Medicine Research, Mampong-Akuapem, Ghana., Tung NH; Faculty of Pharmacy, Phenikaa University, Hanoi, 12116, Vietnam. tung.nguyenhuu@phenikaa-uni.edu.vn.
Jazyk: angličtina
Zdroj: Malaria journal [Malar J] 2023 Sep 09; Vol. 22 (1), pp. 264. Date of Electronic Publication: 2023 Sep 09.
DOI: 10.1186/s12936-023-04678-0
Abstrakt: Background: The 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).
Methods: The 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.
Results: Heptaphylline and imperatorin produced trophozoitocidal, schizonticidal and gametocytocidal activities with IC 50 s 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 CC 50S 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.
Conclusion: Heptaphylline 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.
(© 2023. BioMed Central Ltd., part of Springer Nature.)
Databáze: MEDLINE
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