Trypanocidal and leishmanicidal activity of six limonoids

Dietmar Steverding, Lazare S Sidjui, Éden Ramalho Ferreira, Bathelemy Ngameni Ngameni, Gabriel N Folefoc, Valérie Mahiou-Leddet, Evelyne Ollivier, G. Richard Stephenson, Thomas Storr, Kevin Tyler

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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.

Original languageEnglish
Pages (from-to)606–611
Number of pages6
JournalJournal of Natural Medicines
Volume74
Issue number3
Early online date10 Apr 2020
DOIs
Publication statusPublished - Jun 2020

Keywords

  • African trypanosomiasis
  • BLOOD-STREAM FORMS
  • Leishmania major
  • Leishmaniasis
  • Limonoids
  • ROOTS
  • TRYPANOSOMA-BRUCEI
  • Trypanosoma brucei

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