Sinensetin

Sinensetin是α-葡萄糖苷酶的选择性抑制剂，IC50值为0.66 mg/ml[1]。

Sinensetin是一类主要的多甲氧基黄酮（PMF），主要存在于柑橘果皮中。据报道，sinensetin具有多种生物活性，包括抗真菌、抗突变、抗癌和抗炎[2][3]。

在人类细胞色素P450 1A2（CYP1A2）试验中，sinensetin处理可显著抑制CYP1A2活性[4]。使用Apostolidis改进的办法，sinensetin溶液与含有α-葡萄糖苷酶溶液的磷酸盐缓冲液（pH 6.9）在96孔板中25°C下孵育10 min可显著抑制α-葡萄糖苷酶[1]。在人脐静脉内皮细胞中，sinensetin处理可诱发细胞周期停滞于G0/G1期，从而抑制细胞增殖，表明其具有低毒性和抗血管生成活性[2]。在RAW 264.7细胞中，sinensetin可在蛋白水平调控κB-α表达，抑制炎症活性[3]。以sinensetin处理人类AGS胃癌细胞可提高p53和p21表达，引起增殖的抑制和细胞凋亡[5]。

在斑马鱼动物模型中，sinensetin处理可在mRNA水平下调与血管生成有关的flt1、kdrl和hras的表达[2]。

参考文献：
[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.