Simultaneous determination of tectorigenin and its metabolites in rat plasma by ultra performance liquid chromatography/quadrupole time-of-flight mass spectrometry

被引:21
作者
Wang, Shen [1 ]
Gong, Tianxing [2 ]
Lu, Jing [1 ]
Kano, Yoshihiro [1 ]
Yuan, Dan [1 ]
机构
[1] Shenyang Pharmaceut Univ, Dept Tradit Chinese Med, Shenyang 110016, Peoples R China
[2] Univ British Columbia, Dept Mat Engn, Vancouver, BC V6T 1Z4, Canada
来源
JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES | 2013年 / 933卷
关键词
Tectorigenin; Plasma pharmacokinetics; Glucuronidation; Sulfation; Rat; U-HPLC/Q-TOFMS; ISOFLAVONE METABOLITES; CONJUGATED METABOLITES; ORAL BIOAVAILABILITY; SMALL-INTESTINE; PUERARIAE FLOS; TECTORIDIN; GENISTEIN; IDENTIFICATION; DISPOSITION; ABSORPTION;
D O I
10.1016/j.jchromb.2013.06.009
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
Tectorigenin is a major isoflavone found in the flowers of Pueraria thomsonii Benth. and the rhizomes of Belamcanda chinensis (L) DC. It possesses hepatoprotective, estrogenic, hypoglycemic and anti-inflammatory activities. In the present study, the plasma pharmacokinetic profile of tectorigenin in rats was evaluated. We developed a selective and accurate U-HPLC/Q-TOFMS method for the simultaneous characterization of nine tectorigenin metabolites, and quantitation of six major metabolites in rat plasma, including tectorigenin-7-O-glucuronide-4'-O-sulfate (Te-7G-4'S), tectorigenin-di-O-sulfate (Te-diS), tectorigenin-7-O-glucuronide (Te-7G), tectorigenin-4'-O-glucuronide (Te-4'G), tectorigenin-7-O-sulfate (Te-7S) and tectorigenin after oral administration of tectorigenin (130 mg/kg). The plasma concentrations reached maximal values of 6.20 +/- 2.05 mu mol/L at 0.96 +/- 0.68 h for Te-7G-4'S, 4.42 +/- 1.36 mu mol/L at 1.92 +/- 2.15 h for Te-diS, 33.50 +/- 4.89 mu mol/L at 0.75 +/- 0.67 h for Te-7G, 3.28 +/- 1.01 mu mol/L at 0.75 +/- 0.67 h for Te-4'G, 12.80 +/- 2.80 mu mol/L at 0.85 +/- 1.54 h for Te-7S, and 12.0 +/- 0.63 mu mol/L at 0.23 +/- 0.15 h for tectorigenin, respectively. Enterohepatic recirculation resulted in double or triple peaks concentration curve/time profiles of the metabolites. Since the total plasma concentrations of tectorigenin conjugated metabolites were much higher than that of the tectorigenin aglycone, an extensive phase II metabolism plays an important role in the pharmacokinetics of tectorigenin in vivo. (C) 2013 Elsevier B.V. All rights reserved.
引用
收藏
页码:50 / 58
页数:9
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