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].
References:
[1]. Mohamed, E.A., et al., Potent alpha-glucosidase and alpha-amylase inhibitory activities of standardized 50% ethanolic extracts and sinensetin from Orthosiphon stamineus Benth as anti-diabetic mechanism. BMC Complement Altern Med, 2012. 12: p. 176.
[2]. Lam, I.K., et al., In vitro and in vivo structure and activity relationship analysis of polymethoxylated flavonoids: identifying sinensetin as a novel antiangiogenesis agent. Mol Nutr Food Res, 2012. 56(6): p. 945-56.
[3]. Shin, H.S., et al., Sinensetin attenuates LPS-induced inflammation by regulating the protein level of IkappaB-alpha. Biosci Biotechnol Biochem, 2012. 76(4): p. 847-9.
[4]. Pan, Y., et al., In vitro effect of important herbal active constituents on human cytochrome P450 1A2 (CYP1A2) activity. Phytomedicine, 2014. 21(12): p. 1645-50.
[5]. Dong, Y., et al., [Effects of sinensetin on proliferation and apoptosis of human gastric cancer AGS cells]. Zhongguo Zhong Yao Za Zhi, 2011. 36(6): p. 790-4.
