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Trypanocidal and leishmanicidal activity of six limonoids.

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 ?M. Kotschyienone A (1) was found to be the most active compound with a minimal inhibition concentration (MIC) value of 10 ?M and GI₅₀ values between 2.5 and 2.9 ?M. Only compounds 1 and 3 showed moderate cytotoxicity against HL-60 cells with MIC and GI₅₀ values of 100 ?M and 31.5-46.2 ?M, respectively. Compound 1 was also found to show activity against intracellular amastigotes of L. major with a GI₅₀ value of 1.5 ?M. The results suggest that limonoids have potential as drug candidates for the development of new treatments against trypanosomiasis and leishmaniasis.

SUBMITTER: Steverding D

PROVIDER: S-EPMC7253382 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature

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Trypanocidal and leishmanicidal activity of six limonoids.

Steverding Dietmar D Sidjui Lazare S LS Ferreira Éden Ramalho ÉR Ngameni Bathelemy B Folefoc Gabriel N GN Mahiou-Leddet Valérie V Ollivier Evelyne E Stephenson G Richard GR Storr Thomas E TE Tyler Kevin M KM

Journal of natural medicines 20200410 3

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<sub>50</sub>) values for the trypanocidal and leishmanicidal a ...[more]

PMID: 32277328

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Project description:The rationale inspiring the discovery of lead compounds for the treatment of human parasitic protozoan diseases from natural sources is the well-established use of medicinal plants in various systems of traditional medicine. On this basis, we decided to select an overlooked medicinal plant growing in central Italy, Marrubium incanum Desr. (Lamiaceae), which has been used as a traditional remedy against protozoan diseases, and to investigate its potential against Human African trypanosomiasis (HAT). For this purpose, we assayed three extracts of different polarities obtained from the aerial parts of M. incanum-namely, water (MarrInc-H2O), ethanol (MarrInc-EtOH) and dichloromethane (MarrInc-CH2Cl2)-against Trypanosoma brucei (TC221), with the aim to discover lead compounds for the development of antitrypanosomal drugs. Their selectivity index (SI) was determined on mammalian cells (BALB/3T3 mouse fibroblasts) as a counter-screen for toxicity. The preliminary screening selected the MarrInc-CH2Cl2 extract as the most promising candidate against HAT, showing an IC50 value of 28 ?g/mL. On this basis, column chromatography coupled with the NMR spectroscopy of a MarrInc-CH2Cl2 extract led to the isolation and identification of five compounds i.e. 1-?-linolenoyl-2-palmitoyl-3-stearoyl-sn- glycerol (1), 1-linoleoyl-2-palmitoyl-3-stearoyl-sn-glycerol (2), stigmasterol (3), palmitic acid (4), and salvigenin (5). Notably, compounds 3 and 5 were tested on T. brucei, with the latter being five-fold more active than the MarrInc-CH2Cl2 extract (IC50 = 5.41 ± 0.85 and 28 ± 1.4 ?g/mL, respectively). Furthermore, the SI for salvigenin was >18.5, showing a preferential effect on target cells compared with the dichloromethane extract (>3.6). Conversely, stigmasterol was found to be inactive. To complete the work, also the more polar MarrInc-EtOH extract was analyzed, giving evidence for the presence of 2?-O-allopyranosyl-cosmosiin (6), verbascoside (7), and samioside (8). Our findings shed light on the phytochemistry of this overlooked species and its antiprotozoal potential, providing evidence for the promising role of flavonoids such as salvigenin for the treatment of protozoal diseases.

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Trypanocidal and leishmanicidal activity of six limonoids.

Publications

Trypanocidal and leishmanicidal activity of six limonoids.

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