三种维药提取物对蛋白酪氨酸磷酸酶1B抑制作用的研究

摘要

Protein tyrosine phosphatase-1 B is one of new drug targets against insulin sensitizer. In this study, we investigated the inhibitory effect of petroleumether extracts from 3 Uygur herbs,including Ziziphora Clinopodioides Lam. ,Helichrysum arenarium (Lima.) Moench,and Ver-nohia anthelmintica (L.) willd,on the PTP1B activity and the mode of inhibition. The results showed that recombinant PTP1 B was highly expressed by the prokaryotic expression system and its molecular weigh was 40.8 kDa. Three extracts showed different inhibitory effects on the PTP1B activity,with IC50 values of 20.2 μg/mL, 12.65 μg/mL,and 9.7 μg/mL,respectively. The enzyme kinetic studies revealed non-competitive type of inhibition,competitive type of inhibition, and mixed competitive type of inhibition with the inhibitory constants (Ki) of 0.275 μg/mL, 1.245 μg/mL,and 0. 192 μg/mL,respectively. The study will provide support for further exploration and utilization of Uygur herbs.%蛋白酪氨酸磷酸酶1B(PTP1B)是胰岛索增敏的新靶点之一.本文研究了芳香新塔花、沙生蜡菊、驱虫斑鸠菊等3种维药石油醚提取物对PTP1B活性的影响及其对酶的抑制类型.结果表明,所构建的原核表达系统能高表达重组PTP1B(his-PTP1B1-321),分子量为40.8 kDa.3种维药提取物对PTP1B均表现出不同程度的抑制活性,其IC50值分别为20.2μg/mL,12.65 μg/mL和9.7 μg/mL.芳香新塔花提取物抑制作用类型为非竞争性,沙生蜡菊提取物是竞争性,驱虫斑鸠菊提取物为混合性竞争抑制;抑制常数(K1)分别为为0.275 ug/mL,1.245 μg/mL,0.192 μg/mL.本研究结果将为维药的进一步开发和利用提供了理论依据.