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Sinensetin is a selective inhibitor of α-glucosidase with IC50 value of 0.66 mg/ml [1].

Sinensetin is a family of the major polymethoxyflavones (PMFs) that mainly contained in the citrus peels. It has been reported that sinensetin has various bioactivities, including antifungal, antimutagenic, anticancer, and anti-inflammatory [2] [3].

When tested with human cytochrome P450 1A2 (CYP1A2), sinensetin treatment significantly inhibited the activity of CYP1A2 [4]. Using a method modified by Apostolidis, incubation of sinensetin solution and phosphate buffer (pH 6.9) containing α-glucosidase solution in 96-well plates at 25°C for 10 min markedly inhibitedα-glucosidase [1]. In Human umbilical vein endothelial cells, administration of sinensetin inhibited cell proliferation via inducing cell cycle arrest in the G0/G1 phase which means it has antiangiogenesis activity with low toxicity [2]. When tested with RAW 264.7 cells, sinensetin inhibited inflammatory activity through regulating κB-α expression in protein level [3]. Treated human AGS gastric cancer cells with sinensetin showed that it increased p53 and p21 expression and resulted in the inhibited proliferation and apoptosis [5].

In animal model of zebrafish, sinensetin treatment downregulated the expression of flt1, kdrl, and hras that associated with angiogenesis in mRNA level [2].

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