Beijing University of Chinese Medicine, Beijing, 100029, China.
Beijing University of Chinese Medicine, Beijing, 100029, China.
Eur J Pharmacol. 2019 Jul 5;854:187-193. doi: 10.1016/j.ejphar.2019.04.005. Epub 2019 Apr 7.
Insulin resistance (IR) is the primary pathogenesis of Type 2 diabetes mellitus (T2DM). Scutellaria baicalensis Georgi is a traditional Chinese herbal medicine, often used in the clinical treatment of T2DM. Baicalein which is considered to have anti-IR effects is one of its active ingredients. IR-induced HepG2 cells were used to investigate the effect of baicalein on glucose metabolism and insulin-signaling pathway, using metformin as a positive control. We found that the use of both baicalein and metformin increased the glucose consumption of IR cells, as well as increasing the pyruvate kinase (PK) and glucokinase (GCK) activity. Also increased was the expression levels of insulin receptor (InsR), insulin receptor substrate-1 (IRS-1), phosphoinositide 3-kinase (PI3K), protein kinase B (AKT) pathway and glucose transporter 2 (GLUT2). Reduced expression levels were found in that of glucose 6 phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK) mRNA. The results confirmed that baicalein (10 and 10 mol/L) promotes glucose uptake and glycolysis, inhibits gluconeogenesis of hepatocytes to improve glucose metabolism, and may be as a result from regulation of InsR/IRS-1/PI3K/AKT pathway. Additionally, baicalein has large concentration range on inhibiting IR, and at lower concentrations has strong anti-IR hepatocyte activity.
胰岛素抵抗（IR）是 2 型糖尿病（T2DM）的主要发病机制。黄芩是一种传统的中药，常用于 T2DM 的临床治疗。黄芩素被认为具有抗 IR 作用，是其活性成分之一。使用 IR 诱导的 HepG2 细胞，用二甲双胍作为阳性对照，研究黄芩素对葡萄糖代谢和胰岛素信号通路的影响。我们发现，黄芩素和二甲双胍的使用都增加了 IR 细胞的葡萄糖消耗，同时增加了丙酮酸激酶（PK）和葡萄糖激酶（GCK）的活性。胰岛素受体（InsR）、胰岛素受体底物-1（IRS-1）、磷酸肌醇 3-激酶（PI3K）、蛋白激酶 B（AKT）通路和葡萄糖转运蛋白 2（GLUT2）的表达水平也增加了。葡萄糖 6 磷酸酶（G6Pase）和磷酸烯醇丙酮酸羧激酶（PEPCK）mRNA 的表达水平降低。结果证实，黄芩素（10 和 10 mol/L）促进葡萄糖摄取和糖酵解，抑制肝细胞的糖异生，改善葡萄糖代谢，可能是通过调节 InsR/IRS-1/PI3K/AKT 通路。此外，黄芩素对 IR 的抑制作用具有较大的浓度范围，在较低浓度时对 IR 肝细胞具有较强的活性。
