Pharmacokinetic study of major bioactive components in rats after oral administration of extract of Ilex hainanensis by high-performance liquid chromatography/electrospray ionization mass spectrometry

Ilex hainanensis Merr. is commonly used as a folk remedy for treating hypertension, dyslipidemia and inflammation in Traditional Chinese Medicine (TCMs) and it also has great potential to treat non-alcoholic fatty liver disease (NAFLD). Chlorogenic acid, kaempferol-7-O-β-d-glucoside, and ilexgenin A are three major bioactive components in I. hainanensis extract. In this study, a rapid, sensitive and convenient LC–MS method was developed for their simultaneous determination in the plasma of normal and NAFLD rats. The method was validated in terms of selectivity, linearity and sensitivity, and shows advantages in monitoring the pharmacokinetic behaviors of these three compounds. Results revealed the pharmacokinetic behaviors of chlorogenic acid, kaempferol-7-O-β-d-glucoside, and ilexgenin A could be significantly changed in NAFLD rats after oral administration of I. hainanensis extract compared with normal rats. The areas under the plasma concentration–time curve (AUC) and maximum plasma concentration (Cmax) of the three analytes were greatly decreased and the plasma clearance (CL) for kaempferol-7-O-β-d-glucoside, Ilexgenin A were greatly increased in NAFLD rats. Meanwhile, the mean residence time (MRT) of kaempferol-7-O-β-d-glucoside and Ilexgenin A were increased in the NAFLD rats. This is the first report on the determination of the major bioactive components in rat plasma after oral administration of I. hainanensis extract. These results provided a meaningful basis for evaluating the clinical application of this medicine.

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► A rapid, sensitive and convenient LC–MS method for simultaneous determination of chlorogenic acid, kaempferol-7-O-β-d-glucoside, and ilexgenin A in plasma was developed and validated.
► The method was applied to pharmacokinetics after oral administration of extract of Ilex hainanensis to rats.
► The differences of their pharmacokinetic behaviors in normal and NAFLD rats were investigated.