Structures and Bioactivities of Dihydrochalcones from Metrodorea stipularis
2014
Burger, Marcela C de Melo | Fernandes, Joaõ Batista | da Silva, Maria F das Graças Fernandes | Escalante, Aster | Prudhomme, Jacques | Le Roch, Karine G. | Izidoro, Mario A. | Vieira, Paulo C.
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.
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