Baicalin, a natural LSD1 inhibitor.
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 IC50of 3.01μM and showed strong LSD1 inhibitory effect in cells. Baicalin may serve as a template for designing flavone-based LSD1 inhibitors.
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.
Yi-Chao
YC
Zheng
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.
Dan-Dan
DD
Shen
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.
Meng
M
Ren
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.
Xue-Qi
XQ
Liu
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.
Zhi-Ru
ZR
Wang
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.
Ying
Y
Liu
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.
Qian-Na
QN
Zhang
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.
Li-Juan
LJ
Zhao
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.
Li-Jie
LJ
Zhao
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.
Jin-Lian
JL
Ma
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.
Bin
B
Yu
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. Electronic address: liuhm@zzu.edu.cn.
Hong-Min
HM
Liu
D001688:Biological Products / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D005419:Flavonoids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D056466:Histone Demethylases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
D001688:Biological Products; D004791:Enzyme Inhibitors; D005419:Flavonoids; C038044:baicalin; D056466:Histone Demethylases; C495195:KDM1A protein, human
Baicalin; Inhibitor; LSD1