Structures and Bioactivities of Dihydrochalcones from Metrodorea stipularis

Autor(es)

de Melo Burger, Marcela C. ^[1] ; Fernandes, Joao Batista ^[1] ; das Gracas Fernandes da Silva, Maria F. ^[1] ; Escalante, Aster ^[2] ; Prudhomme, Jacques ^[2] ; Le Roch, Karine G. ^[2] ; Izidoro, Mario A. ^[3] ; Vieira, Paulo C. ^[1]

Afiliação do(s) autor(es)

^[1] Univ Fed Sao Carlos, Dept Quim, BR-13565905 Sao Carlos, SP - Brazil

^[2] Univ Calif Riverside, Dept Cell Biol & Neurosci, Riverside, CA 92521 - USA

^[3] Univ Fed Sao Paulo, BR-04039002 Sao Paulo - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Journal of Natural Products; v. 77, n. 11, p. 2418-2422, NOV 2014.
• Citações Web of Science: 6

Resumo

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 mu M 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 mu M. The dihydrochalcones showed good selectivity in their inhibitory activities against the cysteine proteases. (AU)

• Processo FAPESP: 10/00496-8 - Estudo de Plantas Medicinais para o Tratamento de Doenças Parasitárias Usando Enzimas como Alvos Moleculares
• Beneficiário: Marcela Carmen de Melo Burger
• Modalidade de apoio: Bolsas no Brasil - Doutorado