The activities of suaveolol and other compounds from Hyptis suaveolens and Momordica charantia against the aetiological agents of African trypanosomiasis, leishmaniasis and malaria

Oaikhena, Enimie E.; Yahaya, Umar A.; Abdulsalami, Sani M.; Egbe, Nkechi L.; Adeyemi, Modupe M.; Ungogo, Marzuq A.; Ebiloma, Godwin U.; Zoiku, Felix K.; Fordjour, Prince A.; Elati, Hamza A.A.; Quashie, Neils B.; Igoli, John O.; Gray, Alexander I.; Lawson, Christopher; Ferro, Valerie A.; de Koning, Harry P.

Abstract

African trypanosomiasis and malaria are among the most severe health challenges to humans and livestock in Africa and new drugs are needed. Leaves of Hyptis suaveolens Kuntze (Lamiaceae) and Momordica charantia L. (Cucurbitaceae) were extracted with hexane, ethyl acetate, and then methanol, and subjected to silica gel column chromatography. Structures of six isolated compounds were elucidated through NMR and HR-EIMS spectrometry. Callistrisic acid, dehydroabietinol, suaveolic acid, suaveolol, and a mixture of suaveolol and suaveolic acid (SSA) were obtained from H. suaveolens, while karavilagenin D and momordicin I acetate were obtained from M. charantia. The isolated biomolecules were tested against trypomastigotes of Trypanosoma brucei brucei and T. congolense, and against Plasmodium falciparum. The most promising EC50 values were obtained for the purified suaveolol fraction, at 2.7 1± 0.36 μg/mL, and SSA, exhibiting an EC50 of 1.56 ± 0.17 μg/mL against T. b. brucei trypomastigotes. Suaveolic acid had low activity against T. b. brucei but displayed moderate activity against T. congolense trypomastigotes at 11.1 ± 0.5 μg/mL. Suaveolol and SSA were also tested against T. evansi, T. equiperdum, Leishmania major and L. mexicana but the antileishmanial activity was low. Neither of the active compounds, nor the mixture of the two, displayed any cytotoxic effect on human foreskin fibroblast (HFF) cells at even the highest concentration tested, being 200 μg/mL. We conclude that suaveolol and its mixture possessed significant and selective trypanocidal activity.

Citation

Oaikhena, E. E., Yahaya, U. A., Abdulsalami, S. M., Egbe, N. L., Adeyemi, M. M., Ungogo, M. A., …de Koning, H. P. (2024). The activities of suaveolol and other compounds from Hyptis suaveolens and Momordica charantia against the aetiological agents of African trypanosomiasis, leishmaniasis and malaria. Experimental Parasitology, 263-264, Article 108807. https://doi.org/10.1016/j.exppara.2024.108807

• Journal Article Type: Article
• Acceptance Date: Jul 20, 2024
• Online Publication Date: Jul 21, 2024
• Publication Date: Jul 21, 2024
• Deposit Date: Aug 21, 2024
• Publicly Available Date: Aug 21, 2024
• Journal: Experimental Parasitology
• Print ISSN: 0014-4894
• Publisher: Elsevier
• Peer Reviewed: Peer Reviewed
• Volume: 263-264
• Article Number: 108807
• DOI: https://doi.org/10.1016/j.exppara.2024.108807