Pharmacokinetics of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside in rat using ultra-performance LC-quadrupole TOF-MS.
2,3,5,4'-Tetrahydroxystilbene-2-O-β-D-glucoside (THSG) from Polygoni multiflori has been demonstrated to possess a variety of pharmacological activities, including antioxidant, anti-inflammatory and hepatoprotective activities. Ultra-performance LC-quadrupole TOF-MS with MS Elevated Energy data collection technique and rapid resolution LC with diode array detection and ESI multistage MS(n) methods were developed for the pharmacokinetics, tissue distribution, metabolism, and excretion studies of THSG in rats following a single intravenous or oral dose. The three metabolites were identified by rapid resolution LC-MS(n). The concentrations of the THSG in rat plasma, bile, urine, feces, or tissue samples were determined by ultra-performance LC-MS. The results showed that THSG was rapidly distributed and eliminated from rat plasma. After the intravenous administration, THSG was mainly distributing in the liver, heart, and lung. For the rat, the major distribution tissues after oral administration were heart, kidney, liver, and lung. There was no long-term storage of THSG in rat tissues. Total recoveries of THSG within 24 h were low (0.1% in bile, 0.007% in urine, and 0.063% in feces) and THSG was excreted mainly in the forms of metabolites, which may resulted from biotransformation in the liver.
Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, the College of Life Sciences, Northwest University, Xi'an, Shaanxi, P. R. China. zyy@nwu.edu.cn
Ying-Yong
YY
Zhao
Li
L
Zhang
Ya-Long
YL
Feng
Dan-Qian
DQ
Chen
Zhi-Hui
ZH
Xi
Xiao
X
Du
Xu
X
Bai
Rui-Chao
RC
Lin
D000818:Animals; D001646:Bile / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D004365:Drugs, Chinese Herbal / Q000032:analysis / Q000493:pharmacokinetics*; D005243:Feces / Q000737:chemistry; D005960:Glucosides / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D008297:Male; D013058:Mass Spectrometry / Q000379:methods*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013267:Stilbenes / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D014018:Tissue Distribution
D004365:Drugs, Chinese Herbal; D005960:Glucosides; D013267:Stilbenes; C093026:2,3,5,4'-tetrahydroxystilbene 2-O-glucopyranoside