Chemoproteomics reveals baicalin activates hepatic CPT1 to ameliorate diet-induced obesity and hepatic steatosis
文献类型：期刊论文
| 作者 | Dai, Jianye1,2,3; Liang, Kai3,4; Zhao, Shan2,3; Jia, Wentong5,6; Liu, Yuan1,2,3; Wu, Hongkun7; Lv, Jia3,7; Cao, Chen8; Chen, Tao8; Zhuang, Shentian1,2,3 |
| 刊名 | PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
 |
| 出版日期 | 2018-06-26 |
| 卷号 | 115期号:26页码:E5896-E5905 |
| ISSN号 | 0027-8424 |
| 关键词 | Baicalin Cpt1 Obesity Chemical Proteomics Steatosis |
| DOI | 10.1073/pnas.1801745115 |
| 英文摘要 | Obesity and related metabolic diseases are becoming worldwide epidemics that lead to increased death rates and heavy health care costs. Effective treatment options have not been found yet. Here, based on the observation that baicalin, a flavonoid from the herbal medicine Scutellaria baicalensis, has unique antisteatosis activity, we performed quantitative chemoproteomic profiling and identified carnitine palmitoyltransferase 1 (CPT1), the controlling enzyme for fatty acid oxidation, as the key target of baicalin. The flavonoid directly activated hepatic CPT1 with isoform selectivity to accelerate the lipid influx into mitochondria for oxidation. Chronic treatment of baicalin ameliorated diet-induced obesity (DIO) and hepatic steatosis and led to systemic improvement of other metabolic disorders. Disruption of the predicted binding site of baicalin on CPT1 completely abolished the beneficial effect of the flavonoid. Our discovery of baicalin as an allosteric CPT1 activator opens new opportunities for pharmacological treatment of DIO and associated sequelae. |
| 语种 | 英语 |
| 出版者 | NATL ACAD SCIENCES |
| WOS记录号 | WOS:000436245000011 |
| 源URL | [http://ir.iccas.ac.cn/handle/121111/42525]  |
| 专题 | 中国科学院化学研究所 |
| 通讯作者 | Wang, Chu |
| 作者单位 | 1.Peking Univ, Synthet & Funct Biomol Ctr, Beijing 100871, Peoples R China 2.Peking Univ, Coll Chem & Mol Engn, Beijing Natl Lab Mol Sci, Key Lab Bioorgan Chem & Mol Engn,Minist Educ, Beijing 100871, Peoples R China 3.Peking Tsinghua Ctr Life Sci, Beijing 100871, Peoples R China 4.Peking Univ, Sch Life Sci, Beijing 100871, Peoples R China 5.Chinese Acad Sci, Inst Zool, State Key Lab Stem Cells & Reprod Biol, Beijing 100101, Peoples R China 6.Univ Chinese Acad Sci, Beijing 101408, Peoples R China 7.Peking Univ, Inst Mol Med, Beijing 100871, Peoples R China 8.Peking Univ, Coll Engn, Beijing 100871, Peoples R China |
| 推荐引用方式 GB/T 7714 | Dai, Jianye,Liang, Kai,Zhao, Shan,et al. Chemoproteomics reveals baicalin activates hepatic CPT1 to ameliorate diet-induced obesity and hepatic steatosis[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA,2018,115(26):E5896-E5905. |
| APA | Dai, Jianye.,Liang, Kai.,Zhao, Shan.,Jia, Wentong.,Liu, Yuan.,...&Wang, Chu.(2018).Chemoproteomics reveals baicalin activates hepatic CPT1 to ameliorate diet-induced obesity and hepatic steatosis.PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA,115(26),E5896-E5905. |
| MLA | Dai, Jianye,et al."Chemoproteomics reveals baicalin activates hepatic CPT1 to ameliorate diet-induced obesity and hepatic steatosis".PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA 115.26(2018):E5896-E5905. |
入库方式： OAI收割
来源：化学研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。