RESUMEN
This paper evaluated the inhibitory effect of 3-O-[ß-d-glucopyranosyl-(1â4)-ß-d-glucuronopyranosyl] oleanolic acid 28-O-ß-d-glucopyranosyl ester (PFS), a major saponin isolated from Polyscias fruticosa leaves, on α-amylase and α-glucosidase, and its potential for reducing the postprandial blood glucose level in mice. In enzyme inhibition assays, PFS strongly inhibited porcine pancreas α-amylase and yeast α-glucosidase. Using the Lineweaver-Burk equation, we found that PFS inhibited porcine pancreas α-amylase in a mixed noncompetitive mode, and yeast α-glucosidase via noncompetitive inhibition. In the sucrose tolerance test, PFS at 100 mg/kg body weight significantly decreased the postprandial blood glucose level in mice fed a high-sucrose diet. These findings suggest that P. fruticosa leaves and their major saponin PFS can be used to prevent and treat diabetes and its complications.
Asunto(s)
Araliaceae/química , Hipoglucemiantes/farmacología , Hojas de la Planta/química , Saponinas/farmacología , Animales , Araliaceae/clasificación , Femenino , Hipoglucemiantes/aislamiento & purificación , Masculino , Ratones , Ratones Endogámicos BALB C , Saponinas/aislamiento & purificaciónRESUMEN
BACKGROUND: This study evaluated the cytotoxic activity of extracts from Caesalpinia sappan heartwood against multiple cancer cell lines using an MTT cell viability assay. The cell death though induction of apoptosis was as indicated by DNA fragmentation and caspase-3 enzyme activation. RESULTS: A methanol extract from C. sappan (MECS) showed cytotoxic activity against several of the cancer cell lines. The most potent activity exhibited by the MECS was against HeLa cells with an IC50 value of 26.5 ± 3.2 µg/mL. Treatment of HeLa cells with various MECS concentrations resulted in growth inhibition and induction of apoptosis, as indicated by DNA fragmentation and caspase-3 enzyme activation. CONCLUSION: This study is the first report of the anticancer properties of the heartwood of C. sappan native to Vietnam. Our findings demonstrate that C. sappan heartwood may have beneficial applications in the field of anticancer drug discovery.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Apoptosis , Caesalpinia/química , Extractos Vegetales/farmacología , Haz Vascular de Plantas/metabolismo , Animales , Antineoplásicos Fitogénicos/aislamiento & purificación , Caspasa 3/metabolismo , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular , Citotoxinas/farmacología , Fragmentación del ADN , Ensayos de Selección de Medicamentos Antitumorales/métodos , Activación Enzimática/efectos de los fármacos , Femenino , Formazáns , Inhibidores de Crecimiento/farmacología , Células HeLa , Humanos , Indicadores y Reactivos , Concentración 50 Inhibidora , Metanol , Ratones Endogámicos C57BL , Sales de Tetrazolio , VietnamRESUMEN
BACKGROUND: This study evaluated the cytotoxic activity of extracts from Caesalpinia sappan heartwood against multiple cancer cell lines using an MTT cell viability assay. The cell death though induction of apoptosis was as indicated by DNA fragmentation and caspase-3 enzyme activation. RESULTS: A methanol extract from C. sappan (MECS) showed cytotoxic activity against several of the cancer cell lines. The most potent activity exhibited by the MECS was against HeLa cells with an IC50 value of 26.5 ± 3.2 µg/mL. Treatment of HeLa cells with various MECS concentrations resulted in growth inhibition and induction of apoptosis, as indicated by DNA fragmentation and caspase-3 enzyme activation. CONCLUSION: This study is the first report of the anticancer properties of the heartwood of C. sappan native to Vietnam. Our findings demonstrate that C. sappan heartwood may have beneficial applications in the field of anticancer drug discovery.