Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 1 de 1
Filter
Add more filters










Database
Language
Publication year range
1.
Bioorg Med Chem Lett ; 26(7): 1772-5, 2016 Apr 01.
Article in English | MEDLINE | ID: mdl-26906638

ABSTRACT

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).


Subject(s)
Antiparasitic Agents/chemistry , Antiparasitic Agents/pharmacology , Leishmania mexicana/drug effects , Plants/chemistry , Trypanosoma cruzi/drug effects , Alkaloids/chemistry , Alkaloids/pharmacology , Anthraquinones/chemistry , Anthraquinones/pharmacology , Antiprotozoal Agents/chemistry , Antiprotozoal Agents/pharmacology , Chagas Disease/drug therapy , Chalcones/chemistry , Chalcones/pharmacology , Flavanones/chemistry , Flavanones/pharmacology , Humans , Leishmaniasis, Cutaneous/drug therapy , Moraceae/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Rubiaceae/chemistry , Structure-Activity Relationship , Trypanocidal Agents/chemistry , Trypanocidal Agents/pharmacology , Zanthoxylum/chemistry
SELECTION OF CITATIONS
SEARCH DETAIL
...