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黄芩素,一种天然 LSD1 抑制剂。

Baicalin, a natural LSD1 inhibitor.

机构信息

Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Zhengzhou, Henan 450001, PR China; Co-Innovation Center of Henan Province for New Drug R & D and Preclinical Safety, Zhengzhou, Henan 450001, PR China; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan 450001, PR China.

Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Zhengzhou, Henan 450001, PR China; Co-Innovation Center of Henan Province for New Drug R & D and Preclinical Safety, Zhengzhou, Henan 450001, PR China; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, Henan 450001, PR China.

出版信息

Bioorg Chem. 2016 Dec;69:129-131. doi: 10.1016/j.bioorg.2016.10.004. Epub 2016 Oct 11.

Abstract

Baicalin is one of the active ingredients in the skullcap, with a variety of pharmacological effects, such as blood pressure reduction, sedation, liver-protection, gallbladder-protection, anti-bacteria, and anti-inflammation. In our study, baicalin was first characterized as a LSD1 inhibitor with an IC of 3.01μM and showed strong LSD1 inhibitory effect in cells. Baicalin may serve as a template for designing flavone-based LSD1 inhibitors.

摘要

黄芩苷是黄芩的一种活性成分,具有多种药理作用,如降血压、镇静、保肝、利胆、抗菌、抗炎等。在我们的研究中,黄芩苷首先被鉴定为 LSD1 抑制剂,其 IC 为 3.01μM,并在细胞中表现出很强的 LSD1 抑制作用。黄芩苷可能成为设计基于黄酮类的 LSD1 抑制剂的模板。

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