黄芩苷
黄芩
脂肪变性
肉碱
药理学
β氧化
类黄酮
生物化学
化学
内科学
医学
抗氧化剂
新陈代谢
中医药
高效液相色谱法
替代医学
病理
色谱法
作者
Jianye Dai,Kai Liang,Shan Zhao,Wentong Jia,Yuan Liu,Hong-Kun Wu,Lu Jia,Chen Cao,Tao Chen,Shentian Zhuang,Xiaomeng Hou,Shijie Zhou,Xiannian Zhang,Xiaowei Chen,Yanyi Huang,Rui‐Ping Xiao,Yanling Wang,Tuoping Luo,Junyu Xiao,Chu Wang
标识
DOI:10.1073/pnas.1801745115
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.
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