Influence of the methanolic extract from Abutilon indicum leaves in normal and streptozotocin-induced diabetic rats

The methanolic leaf extract of Abutilon indicum (AI) was investigated for hypoglycemic effect in normal and streptozotocin-induced diabetic rats. The chemical screening of the extract showed that phenoliccompounds and flavonoid contents were 1.04 ± 0.01 mg/g and 59.92 ± 3.88 g/g extract, respectively. A single oral administration of the extract at a dose of 500 mg/kg significantly decreased the bloodglucose concentrations in both normal and diabetic rats after 2 h administration. Metformin was used as the reference drug and reduced the blood glucose only in diabetic rats. To clarify the involvedmechanism, normal rats were orally administered with sucrose and maltose at a dose of 3 g/kg with or without AI extract. The postprandial elevation in the blood glucose concentrations at 30 min after theadministration of sucrose with the extract was significantly suppressed when compared with the control group. No significant change in blood glucose concentrations was observed in maltose-loading rats. An in vitro study indicated that AI extract inhibited -glucosidases, the disaccharide-digesting enzyme in the small intestine. The extract showed a potent sucrase inhibitory activity with IC50 of 2.45 ±0.13 mg/ml while the extract was less potent on the maltase inhibition. The results suggested that the extract from AI extract would be effective for lowering and suppressing elevation of blood glucose

Hit-to-Lead Development of the Chamigrane Endoperoxide Merulin A for the Treatment of African Sleeping Sickness

Background: Human African trypanosomiasis (HAT) is an infectious disease with a large global health burden occurring primarily in Central and Eastern Africa. Most current treatments have poor blood brain barrier (BBB) penetration, which prevent them from

Hit-to-Lead Development of the Chamigrane Endoperoxide Merulin A for the Treatment of African Sleeping Sickness

Background: Human African trypanosomiasis (HAT) is an infectious disease with a large global health burden occurring primarily in Central and Eastern Africa. Most current treatments have poor blood brain barrier (BBB) penetration, which prevent them from

Synthesis and biological properties of a rhodacyanine derivative, Ssj-127, having high efficacy against malaria protozoa

One of rhodacyanine derivatives, SSJ-127 (1), showed a complete cure of a mouse model infected with Plasmodium berghei by subcutaneous administration. The synthesis, in vitro activities against several protozoa and in vivo antimalarial test and PK study of SSJ-127 (1) are reporte