Wang Zhigang, Tang Shuhan, Hattori Masao, Zhang Hailong, Wang Ping, Wu Xiuhong, Zhang Ning
Department of Pharmaceutical Analysis, Heilongjiang University of Chinese Medicine, Heping road 24, Harbin 150040, China; Institute of Natural Medicine, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan.
Institute of Natural Medicine, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan; Harbin Children Hospital, Youyi road 57, Harbin, China.
J Pharm Biomed Anal. 2017 Jul 15;141:173-179. doi: 10.1016/j.jpba.2017.03.069. Epub 2017 Apr 19.
A highly sensitive analytical method was developed to study the in vivo metabolism of paeoniflorin, one of the most principal components in traditional Chinese medicine. After hydrolyzation with sulfatase, the epimer metabolites 7S-paeonimetabolin I and 7R-paeonimetabolin I of paeoniflorin in rat plasma were successfully detected and well separated by LC-MS following picolinoyl derivatization for the first time. Borneol was used as the internal standard to quantify 7S-paeonimetabolin I and 7R-paeonimetabolin I in rat plasma. 7S-paeonimetabolin I and 7R-paeonimetabolin I show similar but different pharmacokinetic behavior. 7S-paeonimetabolin I reached the maximum mean plasma concentration of 45.7±4.6ng/mL at about 1.5h after oral administration of paeoniflorin at a dose of 5mg/kg, while 7R-paeonimetabolin I reached the maximum mean plasma concentration of 39.2±3.5ng/mL at about 1.5h. The full metabolic pathway of paeoniflorin in rats was proposed. The monoterpene compound paeoniflorin was found to be metabolized to the sulfate of 7S-paeonimetabolin I and 7R-paeonimetabolin I in vivo which maybe responsible for the pharmacological effect of paeoniflorin.
