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Alternative Titleinhibitory effect of extracts from three uyghur medicine on the protein tyrosine phosphatase 1b activity
刘禾培; 窦君; 马纪; 信学雷; 赵海清; 阿吉艾克拜尔·艾萨
Source Publication天然产物研究与开发

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。

Other Abstract

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 Lam., 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 mug/mL,12.65 mug/mL, and 9.7 mug/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 mug/mL,1.245 mug/mL, and 0.192 mug/mL, respectively. The study will provide support for further exploration and utilization of Uygur herbs

Keyword维药 蛋白酪氨酸磷酸酯酶1b 抑制作用 原核表达
Subject AreaPlant Sciences ; General & Internal Medicine ; Pharmacology & Pharmacy (Provided By Thomson Reuters)
Indexed ByCSCD
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Document Type期刊论文
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刘禾培,窦君,马纪,等. 三种维药提取物对蛋白酪氨酸磷酸酶1B抑制作用的研究[J]. 天然产物研究与开发,2011,23(1):142-145.
APA 刘禾培,窦君,马纪,信学雷,赵海清,&阿吉艾克拜尔·艾萨.(2011).三种维药提取物对蛋白酪氨酸磷酸酶1B抑制作用的研究.天然产物研究与开发,23(1),142-145.
MLA 刘禾培,et al."三种维药提取物对蛋白酪氨酸磷酸酶1B抑制作用的研究".天然产物研究与开发 23.1(2011):142-145.
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