Baicalin, a natural LSD1 inhibitor.

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 IC50 of 3.01μM and showed strong LSD1 inhibitory effect in cells. Baicalin may serve as a template for designing flavone-based LSD1 inhibitors.

• Authors: Yi-Chao Zheng, Dan-Dan Shen, Meng Ren, Xue-Qi Liu, Zhi-Ru Wang, Ying Liu, Qian-Na Zhang, Li-Juan Zhao, Li-Jie Zhao, Jin-Lian Ma, Bin Yu, Hong-Min Liu
• Journal: Bioorganic chemistry (Bioorg Chem) Vol. 69 Pg. 129-131 (12 2016) ISSN: 1090-2120 [Electronic] United States
• PMID: 27814566 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2016 Elsevier Inc. All rights reserved.

Chemical References

• Biological Products
• Enzyme Inhibitors
• Flavonoids
• baicalin
• Histone Demethylases
• KDM1A protein, human

Topics

• Biological Products (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Dose-Response Relationship, Drug
• Enzyme Inhibitors (chemical synthesis, chemistry, pharmacology)
• Flavonoids (chemical synthesis, chemistry, pharmacology)
• Histone Demethylases (antagonists & inhibitors, metabolism)
• Humans
• Molecular Conformation
• Structure-Activity Relationship