Simultaneous Determination Of Two Galangin Metabolites From Alpinia Officinarum Hance In Rat Plasma By Uf Lc-Ms/Ms And Its Application In Pharmacokinetics Study

Galangin has multiple pharmacological efficacies, such as anti-cancer, antiinflammation and anti-oxidation. Galangin can be rapidly converted into glucuronidated metabolites in vivo. This study aimed to establish an UFLC-MS/MS analytical method to simultaneously determine the concentrations of two glucuronidated metabolites of galangin, galangin-3-O-beta-D-glucuronic acid (GG-1) and galangin-7O-beta-D-glucuronic acid (GG-2) in rat plasma. After oral administration of galangal extract (0.3 g/kg), blood samples were collected from the orbital sinus, then treated by methanol precipitation and further gradient-eluted with Phenomenex Kinetex 2.6 mm XB-C18 column. The mass spectrometer was manipulated in the negative electrospray ionization (ESI) and selected multiple reaction monitoring (MRM) mode for the analytes. The precursor-to-product ion pairs applied for GG-1, GG-2 and chrysin (as the internal standard, IS) were m/z 445.2 -> 269.0, 445.2 -> 268.9 and 253.0 -> 142.9, respectively. The results showed that the linear ranges for both GG-1 and GG-2 were 2.0-2000.0 ng/mL (r 2 > 0 :995). The inter-and intra-day precision were 89.3%-109.2%, RSD was less than 15%, and the repeatability was good. The recoveries of both metabolites and IS were over 89%, and matrix effect was within 15%. The validated analytical method was further applied to study the pharmacokinetic profiles of GG-1 and GG-2 in vivo. The pharmacokinetic parameters suggested that Tmax of GG-1 was equivalent to that of GG-2, and MRT0-t, t(1)/(2) of GG-2 were a little higher than those of GG-1. Importantly, AUC(0-t) and Cmax of GG-2 were almost twice as those of GG-1. In short, the validated UFLCMS/MS analytical method was feasible to simultaneously determine two galangin metabolites GG-1 and GG-2 in rat plasma and further analyze in vivo metabolism of galangin.