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Structures and Bioactivities of Dihydrochalcones from Metrodorea stipularis

Author:
Burger, Marcela C. de Melo, Fernandes, João Batista, da Silva, Maria F. das Graças Fernandes, Escalante, Aster, Prudhomme, Jacques, Le Roch, Karine G., Izidoro, Mario A., Vieira, Paulo C.
Source:
Journal of natural products 2014 v.77 no.11 pp. 2418-2422
ISSN:
1520-6025
Subject:
Plasmodium falciparum, Trypanosoma cruzi, antimalarials, bioactive properties, cathepsins, cruzipain, inhibitory concentration 50
Abstract:
Metrodorea stipularis stem extracts were studied in the search for possible antichagastic, antimalarial, and antitumoral compounds using cruzain from Trypanosoma cruzi, Plasmodium falciparum, and cathepsins B and L, as molecular targets, respectively. Dihydrochalcones 1, 2, 3, and 4 showed significant inhibitory activity against all the targets. Compounds 1–4 displayed IC₅₀ values ranging from 7.7 to 21.6 μM against cruzain; dihydrochalcones 2 and 4 inhibited the growth of three different strains of P. falciparum in low micromolar concentrations; and against cathepsins B and L these compounds presented good inhibitory activity with IC₅₀ values ranging from 1.0 to 14.9 μM. The dihydrochalcones showed good selectivity in their inhibitory activities against the cysteine proteases.
Agid:
5494208