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Trypanocidal and leishmanicidal activity of six limonoids

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 m...

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Bibliographic Details
Published in:Journal of natural medicines 2020-06, Vol.74 (3), p.606-611
Main Authors: Steverding, Dietmar, Sidjui, Lazare S., Ferreira, Éden Ramalho, Ngameni, Bathelemy, Folefoc, Gabriel N., Mahiou-Leddet, Valérie, Ollivier, Evelyne, Stephenson, G. Richard, Storr, Thomas E., Tyler, Kevin M.
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Language:English
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Summary: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.
ISSN:1340-3443
1861-0293
DOI:10.1007/s11418-020-01408-7