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 ›› 2011, Vol. 23 ›› Issue (1): 142-145.

三种维药提取物对蛋白酪氨酸磷酸酶1B抑制作用的研究

刘禾培^1,2，窦君²，马纪¹，信学雷²，赵海清²，阿吉艾克拜尔•艾萨^2*

¹新疆大学生命科学与技术学院新疆生物资源基因工程国家重点实验室培育基地，乌鲁木齐 830046； ²中国科学院新疆理化技术研究所新疆植物资源化学重点实验室，乌鲁木齐 830011

收稿日期:2009-09-11 发布日期:2011-07-20
通讯作者: haji@ ms.xjb.ac.cn
基金资助:
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)

Inhibitory Effect of Extracts from Three Uyghur Medicine on the Protein Tyrosine Phosphatase 1B Activity

LIU He-pei^1,2, DOU Jun², MA Ji^1, XING Xue-lei², ZHAO Hai-qing², AISA Haji Akber^2*

¹State Key Laboratory Basis of Xinjiang Biological Resources and Genetic engineering, College of Life Science and Technology, Xinjiang University, Urumqi 830046, China; ²Xinjiang Key Laboratory of Plant Resources and Natural Products Chemistry, Xinjiang Technological Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China

Received:2009-09-11 Published:2011-07-20

摘要/Abstract

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-PTP1B _1-321），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20.2 μg/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（K_i）分别为为0.275 μg/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。

关键词: 维药, 蛋白酪氨酸磷酸酯酶1B, 抑制作用, 原核表达

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 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 (K_i) 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.

Key words: Uygur herbs, PTP1B, inhibition, prokaryotic expression system

刘禾培，窦君，马纪，信学雷，赵海清，阿吉艾克拜尔?艾萨. 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.

LIU He-Pei, DOU Jun, MA Ji, XIN Xue-Lei, ZHAO Hai-Qing, AISA Haji Akber. Inhibitory Effect of Extracts from Three Uyghur Medicine on the Protein Tyrosine Phosphatase 1B Activity[J]. NATURAL PRODUCT RESEARCH AND DEVELOPMENT, 2011, 23(1): 142-145.

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