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蛋白酪氨酸磷酸酶1B(PTP1B)在胰岛素信号通路中起负调控作用,PTP1B过表达使胰岛素受体蛋白酪氨酸去磷酸化而导致机体对胰岛素不敏感,继而产生2型糖尿病胰岛素抵抗。因此,PTP1B是筛选治疗糖尿病活性成分的重要靶点。本文通过体外人源PTP1B抑制剂筛选模型,以活性为导向对新疆两种特有独尾草进行抑制活性筛选。结果表明,两种独尾草属植物均具有良好的PTP1B抑制活性(IC_(50)分别为17.85和33.76μg/m L),在阿尔泰独尾草进一步分离得到化合物大黄酚-8-甲基乙酯,抑制活性为26.15±0.5μM,酶反应动力学研究表明其抑制类型为混合型抑制,抑制常数Ki值为39.12±8.56μM。本研究为异翅独尾草的进一步分离提供了理论依据。
Protein tyrosine phosphatase 1B (PTP1B) plays a negative regulatory role in the insulin signaling pathway. Overexpression of PTP1B dephosphorylates the insulin receptor tyrosine, resulting in insulin-insensitivity of the body and consequent insulin-type 2 diabetes. Therefore, PTP1B is an important target for screening active ingredients for the treatment of diabetes. In this paper, in vitro screening of human PTP1B inhibitors model, activity-oriented screening of two endemic Xinjiang Uttar Pradesh inhibition activity screening. The results showed that both of the two genus Elymus plants had good PTP1B inhibitory activity (IC 50 (17.85 and 33.76 μg / m L, respectively), and the compound chrysophanol 8-methyl ethyl Ester, the inhibitory activity was 26.15 ± 0.5μM. The kinetics of enzyme reaction showed that the inhibition type was mixed inhibition, and the inhibition constant Ki value was 39.12 ± 8.56μM. This study provides a theoretical basis for the further separation of Eupatex.