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学科主题: 生命有机化学
题名: Molecular matchmaking between the popular weight-loss herb Hoodia gordonii and GPR119, a potential drug target for metabolic disorder AMERICA
其他题名: 蝴蝶亚仙人掌孕甾皂苷与GPR119受体的相互作用及其在代谢紊乱疾病中的潜在应用
作者: ZHANG SHUYONG1; Ma YY(马玉勇)1; LI JING1; Ma JJ(马君君)1; Yu B(俞飚)1; Xie X(谢欣)1
通讯作者: 俞飚 ; 谢欣
刊名: Proc. Natl. Acad. Sci. U. S. A.
发表日期: 2014
DOI: 10.1073/pnas.1324130111
卷: 111, 期:40, 页:14571-14576
收录类别: SCI
英文摘要: African cactiform Hoodia gordonii (Asclepiadaceae) has been used for thousands of years by Xhomani Bushmen as an anorexant during hunting trips and has been proposed as a new agent for the management of body weight. However, its in vivo targets and molecular mechanisms remain elusive. GPR119, a G protein-coupled receptor highly expressed in pancreatic beta cells and intestinal L cells, has been demonstrated to facilitate glucose-stimulated insulin secretion (GSIS) and represents a novel and attractive target for the therapy of metabolic disorders. Here, we disclose that Gordonoside F (a steroid glycoside isolated from H. gordonii), but not the widely known P57, activates specifically GPR119. Successful synthesis of Gordonoside F facilitates further characterization of this compound. Gordonoside F promotes GSIS both in vitro and in vivo and reduces food intake in mice. These effects are mediated by GPR119 because GPR119 knockout prevents the therapeutic effects of Gordonoside F. Interestingly, the appetite-suppressing effect of Hoodia extract was also partially blocked by GPR119 knockout. Our results demonstrate for the first time, to our knowledge, that GPR119 is a direct target and one of the major mechanisms underlying the therapeutic effect of the popular "weight loss" herb H. gordonii. Given the long history of safe application of this herb in weight control, it is foreseeable that the novel scaffold of Gordonoside F provides a promising opportunity to develop new drugs in treating metabolic diseases.
语种: 英语
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/38956
Appears in Collections:生命有机化学国家重点实验室_期刊论文

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作者单位: 1.同济大学
2.中科院上海药物研究所
3.中科院上海有机化学研究所

Recommended Citation:
ZHANG SHUYONG,Ma YY,LI JING,et al. Molecular matchmaking between the popular weight-loss herb Hoodia gordonii and GPR119, a potential drug target for metabolic disorder AMERICA[J]. Proc. Natl. Acad. Sci. U. S. A.,2014,111(40):14571-14576.
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