Trypanocidal and leishmanicidal activity of six limonoids

Steverding, Dietmar, Sidjui, Lazare S, Ferreira, Éden Ramalho, Ngameni, Bathelemy Ngameni, Folefoc, Gabriel N, Mahiou-Leddet, Valérie, Ollivier, Evelyne, Stephenson, G. Richard, Storr, Thomas and Tyler, Kevin (2020) Trypanocidal and leishmanicidal activity of six limonoids. Journal of Natural Medicines, 74. 606–611. ISSN 1340-3443

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Abstract

Six limonoids [kotschyienone A and B (1, 2), 7-deacetylgedunin (3), 7-deacetyl-7-oxogedunin (4), andirobin (5) and methyl angolensate (6)] were investigated for their trypanocidal and leishmanicidal activities using bloodstream forms of Trypanosoma brucei and promastigotes of Leishmania major. Whereas all compounds showed anti-trypanosomal activity, only compounds 1–4 displayed anti-leishmanial activity. The 50% growth inhibition (GI 50) values for the trypanocidal and leishmanicidal activity of the compounds ranged between 2.5 and 14.9 μM. Kotschyienone A (1) was found to be the most active compound with a minimal inhibition concentration (MIC) value of 10 μM and GI 50 values between 2.5 and 2.9 μM. Only compounds 1 and 3 showed moderate cytotoxicity against HL-60 cells with MIC and GI 50 values of 100 μM and 31.5–46.2 μM, respectively. Compound 1 was also found to show activity against intracellular amastigotes of L. major with a GI 50 value of 1.5 μM. The results suggest that limonoids have potential as drug candidates for the development of new treatments against trypanosomiasis and leishmaniasis.

Item Type: Article
Uncontrolled Keywords: african trypanosomiasis,blood-stream forms,leishmania major,leishmaniasis,limonoids,roots,trypanosoma-brucei,trypanosoma brucei
Faculty \ School: Faculty of Medicine and Health Sciences > Norwich Medical School
Faculty of Science > School of Chemistry
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Depositing User: LivePure Connector
Date Deposited: 04 Apr 2020 00:45
Last Modified: 30 May 2020 00:03
URI: https://ueaeprints.uea.ac.uk/id/eprint/74708
DOI: 10.1007/s11418-020-01408-7

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