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
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.
October 11, 2016: Bioorganic Chemistry