Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi
| Autor: | Victor Kuete, Milene Höehr de Moraes, Louis P. Sandjo, Bonaventure T. Ngadjui, Blaise C. Kamdoum, Mário Steindel |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
Zanthoxylum
0301 basic medicine Antiparasitic medicine.drug_class Trypanosoma cruzi Metabolite Leishmania mexicana Clinical Biochemistry Antiprotozoal Agents Leishmaniasis Cutaneous Pharmaceutical Science Anthraquinones Rubiaceae Pharmacology Moraceae 01 natural sciences Biochemistry Damnacanthal Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound Alkaloids Chalcones Drug Discovery medicine Humans Chagas Disease Amastigote Molecular Biology IC50 Antiparasitic Agents biology Plant Extracts 010405 organic chemistry Organic Chemistry Plants Eriodictyol biology.organism_classification Trypanocidal Agents 0104 chemical sciences 030104 developmental biology chemistry Flavanones Antiprotozoal Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 26:1772-1775 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2016.02.044 |
| Popis: | Six plant metabolites including isobavachalcone (1), 4-hydroxylonchocarpine (2), and (E)-1-(2,2-dimethyl-2H-chromen-6-yl)-3-(4-hydroxyphenyl)prop-2-en-1-one (3), 6,8-(di-3-methyl-but-2-enyl)eriodictyol (4), damnacanthal (5), and buesgenine (6) were evaluated for their leishmanicidal and trypanocidal activities against intracellular amastigotes of Leishmania amazonensis and Trypanosoma cruzi. Compounds 2-4 and 6 displayed antileishmanial activity while 3 and 5 showed trypanocidal effect. The leishmanicidal activity of 6 was expressed with the lowest IC50 (5.70μg/mL) whereas the most trypanocidal metabolite (5) showed its activity with IC50 at 11.14μg/mL. In addition, antiprotozoal effect of mixtures of 1-6 prepared at different ratios (3:1, 1:1, and 1:3) was also investigated. Interestingly, 1 and 2 initially inactive against T. cruzi, displayed trypanocidal activities when mixed together. This activity increased when 3 (13.63μg/mL) was combined with 1 in ratios 1:1 (10.01μg/mL) and 3:1 (7.78μg/mL). Moreover, the leishmanicidal effect of 4 against L. amazonensis increased in the mixture 6/4 (1:3). |
| Databáze: | OpenAIRE |
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