Structures and bioactivities of dihydrochalcones from Metrodorea stipularis.
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.
Departamento de Química, Universidade Federal de São Carlos , Rod. Washington Luís, Km 235, 13565-905 São Carlos, SP, Brazil.
Marcela C de Melo
MC
Burger
João Batista
JB
Fernandes
Maria F das Graças Fernandes
MF
da Silva
Aster
A
Escalante
Jacques
J
Prudhomme
Karine G
KG
Le Roch
Mario A
MA
Izidoro
Paulo C
PC
Vieira
D000962:Antimalarials / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D001938:Brazil; D002401:Cathepsin B / Q000037:antagonists & inhibitors; D056668:Cathepsin L / Q000037:antagonists & inhibitors; D047188:Chalcones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D018547:Plant Stems / Q000737:chemistry; D010963:Plasmodium falciparum / Q000187:drug effects; D014349:Trypanosoma cruzi / Q000187:drug effects
D000962:Antimalarials; D000981:Antiprotozoal Agents; D047188:Chalcones; D002401:Cathepsin B; D056668:Cathepsin L; C015812:dihydrochalcone