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隐丹参酮通过激活AMP活化蛋白激酶发挥抗糖尿病和抗肥胖作用。

Antidiabetes and antiobesity effect of cryptotanshinone via activation of AMP-activated protein kinase.

作者信息

Kim Eun Ju, Jung Seung-Nam, Son Kun Ho, Kim Sung Ran, Ha Tae Youl, Park Myoung Gyu, Jo In Gun, Park Jong Guk, Choe Wonchae, Kim Sung-Soo, Ha Joohun

机构信息

Department of Biochemistry and Molecular Biology, Medical Research Center for Bioreaction to Reactive Oxygen Species, Kyung Hee University School of Medicine, Seoul, Korea.

出版信息

Mol Pharmacol. 2007 Jul;72(1):62-72. doi: 10.1124/mol.107.034447. Epub 2007 Apr 11.

Abstract

Metabolic disorders, including type 2 diabetes and obesity, represent major health risks in industrialized countries. AMP-activated protein kinase (AMPK) has become the focus of a great deal of attention as a novel therapeutic target for the treatment of metabolic syndromes, because AMPK has been demonstrated to mediate, at least in part, the effects of a number of physiological and pharmacological factors that exert beneficial effects on these disorders. Thus, the identification of a compound that activates the AMPK pathway would contribute significantly to the treatment and management of such syndromes. In service of this goal, we have screened a variety of naturally occurring compounds and have identified one compound, cryptotanshinone, as a novel AMPK pathway activator. Cryptotanshinone was originally isolated from the dried roots of Salvia militorrhiza, an herb that is used extensively in Asian medicine and that is known to exert beneficial effects on the circulatory system. For the first time, in the present study, we have described the potent antidiabetic and antiobesity effects of cryptotanshinone, both in vitro and in vivo. Our findings suggest that the activation of the AMPK pathway might contribute to the development of novel therapeutic approaches for the treatment of metabolic disorders such as type 2 diabetes and obesity.

摘要

包括2型糖尿病和肥胖症在内的代谢紊乱是工业化国家主要的健康风险。作为治疗代谢综合征的新型治疗靶点,AMP激活的蛋白激酶(AMPK)已成为大量关注的焦点,因为已证明AMPK至少部分介导了一些对这些疾病产生有益作用的生理和药理因素的作用。因此,鉴定一种激活AMPK途径的化合物将对这类综合征的治疗和管理做出重大贡献。为实现这一目标,我们筛选了多种天然存在的化合物,并鉴定出一种化合物——隐丹参酮,作为一种新型的AMPK途径激活剂。隐丹参酮最初是从丹参的干燥根中分离出来的,丹参是一种在亚洲医学中广泛使用的草药,已知对循环系统有有益作用。在本研究中,我们首次描述了隐丹参酮在体外和体内的强效抗糖尿病和抗肥胖作用。我们的研究结果表明,AMPK途径的激活可能有助于开发治疗2型糖尿病和肥胖症等代谢紊乱的新型治疗方法。

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