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 (GI50) 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 GI50 values between 2.5 and 2.9 μM. Only compounds 1 and 3 showed moderate cytotoxicity against HL-60 cells with MIC and GI50 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 GI50 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.
Highlights
Trypanosomiasis and leishmaniasis are devastating diseases for both humans and their domestic animals
Effective and better-tolerated chemotherapies are urgently needed for the treatment of trypanosomiasis and leishmaniasis
We investigated the trypanocidal and leishmanicidal activity of six limonoids (Fig. 1, compounds 1–6) isolated from the roots of P. kotschyi
Summary
Trypanosomiasis and leishmaniasis are devastating diseases for both humans and their domestic animals. Mucosal ulcers, and internal organ damage) in humans worldwide [3] These parasites are kinetoplastid protozoans and are transmitted to their mammalian host by insect vectors. Treatment of these parasitoses relies on chemotherapy but only a few drugs are available. Plants that are used in traditional medicine are promising starting materials for the discovery of natural compounds with trypanocidal and leishmanicidal activity. One such plant is Pseudocedrela kotschyi (Schweinf.) Harms (Meliaceae), which is used for the treatment of trypanosomiasis in the Kaduna state of Nigeria [6]. The 1H-NMR and 13C-NMR spectra of 1–6 are shown in Supplementary Figures S1–6
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