title: Simultaneous determination of tectorigenin and its metabolites in rat plasma by ultra performance liquid chromatography/quadrupole time-of-flight mass spectrometry.
abstract: 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 (130mg/kg). The plasma concentrations reached maximal values of 6.20±2.05μmol/L at 0.96±0.68h for Te-7G-4'S, 4.42±1.36μmol/L at 1.92±2.15h for Te-diS, 33.50±4.89μmol/L at 0.75±0.67h for Te-7G, 3.28±1.01μmol/L at 0.75±0.67h for Te-4'G, 12.80±2.80μmol/L at 0.85±1.54h for Te-7S, and 12.0±0.63μmol/L at 0.23±0.15h 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.
authors.affiliation: Department of Traditional Chinese Medicine, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.
authors.forename: Shen
authors.initials: S
authors.lastname: Wang
authors.forename: Tianxing
authors.initials: T
authors.lastname: Gong
authors.forename: Jing
authors.initials: J
authors.lastname: Lu
authors.forename: Yoshihiro
authors.initials: Y
authors.lastname: Kano
authors.forename: Dan
authors.initials: D
authors.lastname: Yuan
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D035264:Flowers / Q000737:chemistry; D027621:Iridaceae / Q000737:chemistry*; D007529:Isoflavones / Q000097:blood* / Q000378:metabolism*; D008297:Male; D013058:Mass Spectrometry / Q000379:methods*; D010936:Plant Extracts / Q000097:blood* / Q000378:metabolism*; D029908:Pueraria / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D007529:Isoflavones; D010936:Plant Extracts; C120039:tectorigenin
keywords: AUC; C(max); CL; DAD; EIM; ESI; F; Glucuronidation; IS; LLOQ; LOQ; MRT; PLNO; Plasma pharmacokinetics; Q-TOFMS; QC; RE; RSD; Rat; Sulfation; T(max); Te-4′G; Te-4′S; Te-7G; Te-7G-4′S; Te-7S; Te-diS; Tectorigenin; U-HPLC; U-HPLC/Q-TOFMS; V; area under the curve; bioavailability; clearance; demethyl-Te-G; demethyl-tectorigenin-O-glucuronide; diode-array detector; distribution volume; electrospray ionization; extractive ion monitoring; half-life of elimination; internal standard; limit of quantitation; lower limit of quantitation; mean residence time; methoxyl-Te-G; methoxyl-tectorigenin-O-glucuronide; partial loop needle overfill; peak plasma concentration; quadrupole time-of-flight mass spectrometry; quality control; relative error; relative standard deviation; t(1/2); tectorigenin-4′-O-glucuronide; tectorigenin-4′-O-sulfate; tectorigenin-7-O-glucuronide; tectorigenin-7-O-glucuronide-4′-O-sulfate; tectorigenin-7-O-sulfate; tectorigenin-di-O-sulfate; time to maximum plasma concentration; ultra performance liquid chromatography