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 language | English |
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Pages (from-to) | 606–611 |
Number of pages | 6 |
Journal | Journal of Natural Medicines |
Volume | 74 |
Issue number | 3 |
Early online date | 10 Apr 2020 |
DOIs | |
Publication status | Published - Jun 2020 |
Keywords
- African trypanosomiasis
- BLOOD-STREAM FORMS
- Leishmania major
- Leishmaniasis
- Limonoids
- ROOTS
- TRYPANOSOMA-BRUCEI
- Trypanosoma brucei
Profiles
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G.Richard Stephenson
- School of Chemistry, Pharmacy and Pharmacology - Emeritus Professor
- Chemistry of Materials and Catalysis - Member
Person: Honorary, Research Group Member
-
Kevin Tyler
- Norwich Medical School - Associate Professor
- Metabolic Health - Member
- Gastroenterology and Gut Biology - Member
- Pathogen Biology Group - Member
Person: Research Group Member, Research Centre Member, Academic, Teaching & Research