Chemoproteomics reveals baicalin activates hepatic CPT1 to ameliorate diet-induced obesity and hepatic steatosis
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- Jianye Dai
- Synthetic and Functional Biomolecules Center, Peking University, 100871 Beijing, China;
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- Kai Liang
- Peking-Tsinghua Center for Life Sciences, 100871 Beijing, China;
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- Shan Zhao
- Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, 100871 Beijing, China;
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- Wentong Jia
- State Key Laboratory of Stem Cells and Reproductive Biology, Institute of Zoology, Chinese Academy of Sciences, 100101 Beijing, China;
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- Yuan Liu
- Synthetic and Functional Biomolecules Center, Peking University, 100871 Beijing, China;
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- Hongkun Wu
- Institute of Molecular Medicine, Peking University, 100871 Beijing, China;
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- Jia Lv
- Peking-Tsinghua Center for Life Sciences, 100871 Beijing, China;
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- Chen Cao
- College of Engineering, Peking University, 100871 Beijing, China
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- Tao Chen
- College of Engineering, Peking University, 100871 Beijing, China
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- Shentian Zhuang
- Synthetic and Functional Biomolecules Center, Peking University, 100871 Beijing, China;
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- Xiaomeng Hou
- Synthetic and Functional Biomolecules Center, Peking University, 100871 Beijing, China;
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- Shijie Zhou
- Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, 100871 Beijing, China;
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- Xiannian Zhang
- College of Engineering, Peking University, 100871 Beijing, China
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- Xiao-Wei Chen
- Peking-Tsinghua Center for Life Sciences, 100871 Beijing, China;
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- Yanyi Huang
- Peking-Tsinghua Center for Life Sciences, 100871 Beijing, China;
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- Rui-Ping Xiao
- Peking-Tsinghua Center for Life Sciences, 100871 Beijing, China;
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- Yan-Ling Wang
- State Key Laboratory of Stem Cells and Reproductive Biology, Institute of Zoology, Chinese Academy of Sciences, 100101 Beijing, China;
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- Tuoping Luo
- Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, 100871 Beijing, China;
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- Junyu Xiao
- Peking-Tsinghua Center for Life Sciences, 100871 Beijing, China;
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- Chu Wang
- Synthetic and Functional Biomolecules Center, Peking University, 100871 Beijing, China;
書誌事項
- 公開日
- 2018-06-11
- 権利情報
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- http://www.pnas.org/site/aboutpnas/licenses.xhtml
- DOI
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- 10.1073/pnas.1801745115
- 公開者
- Proceedings of the National Academy of Sciences
この論文をさがす
説明
<jats:title>Significance</jats:title> <jats:p> Baicalin is a major flavonoid component from the herbal medicine <jats:italic>Scutellaria baicalensis</jats:italic> that has been shown to have an antisteatosis effect. Through quantitative chemoproteomic profiling, we discovered that baicalin acts as a natural allosteric activator of carnitine palmitoyltransferase 1 (CPT1), the rate-limiting enzyme of fatty acid β-oxidation (FAO). By directly binding to CPT1 and activating its activity to accelerate fatty acid degradation, baicalin can significantly ameliorate symptoms associated with hepatic steatosis and reduce diet-induced obesity (DIO). Our study provides an example of a natural product agonist for CPT1. The results provide mechanistic insights to explain the bioactivity of baicalin in reducing lipid accumulation and introduce exciting opportunities for developing novel flavonoid-based FAO activators for pharmacologically treating DIO and associated metabolic disorders. </jats:p>
収録刊行物
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- Proceedings of the National Academy of Sciences
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Proceedings of the National Academy of Sciences 115 (26), 2018-06-11
Proceedings of the National Academy of Sciences
