摘要
蛋白酪氨酸磷酸酶1B(PTP1B)是胰岛素增敏的新靶点之一。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,12.65μg/mL和9.7μg/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(Ki)分别为为0.275μg/mL,1.245μg/mL,0.192μg/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。
Protein tyrosine phosphatase-1B 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 Lain. , Helichrysum arenarium （ Linn. ） Moench, and Ver-nohia anthelmintica （ L. ） willd, on the PTP1B activity and the mode of inhibition. The results showed that recombinant PTP1B 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.
出处
《天然产物研究与开发》
CAS
CSCD
2011年第1期142-145,共4页
Natural Product Research and Development
基金
中国科学院
国家外国专家局创新团队国际合作伙伴计划
新疆维吾尔自治区高技术研究与发展计划(200611109)
国家科技支撑计划(2007BAI30B03)
