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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Structures and Bioactivities of Dihydrochalcones from Metrodorea stipularis

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Author(s):
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]
Total Authors: 8
Affiliation:
[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
Total Affiliations: 3
Document type: Journal article
Source: Journal of Natural Products; v. 77, n. 11, p. 2418-2422, NOV 2014.
Web of Science Citations: 6
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 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)

FAPESP's process: 10/00496-8 - Study of Medicinal Plants for the Treatment of Parasitic Diseases Using Enzymes as Molecular Targets
Grantee:Marcela Carmen de Melo Burger
Support Opportunities: Scholarships in Brazil - Doctorate