title: 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.
abstract: 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.
authors: State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China.
authors: Jie
authors: J
authors: Yang
authors: Fang
authors: F
authors: Lv
authors: Xiao-qing
authors: XQ
authors: Chen
authors: Wei-xi
authors: WX
authors: Cui
authors: Li-hong
authors: LH
authors: Chen
authors: Xiao-dong
authors: XD
authors: Wen
authors: Qiang
authors: Q
authors: Wang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001685:Biological Factors / Q000097:blood / Q000493:pharmacokinetics*; D002726:Chlorogenic Acid / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D004195:Disease Models, Animal; D004365:Drugs, Chinese Herbal / Q000493:pharmacokinetics* / Q000494:pharmacology; D005234:Fatty Liver / Q000097:blood / Q000188:drug therapy / Q000378:metabolism; D006027:Glycosides / Q000097:blood / Q000493:pharmacokinetics; D030017:Ilex / Q000737:chemistry*; D044949:Kaempferols / Q000097:blood / Q000493:pharmacokinetics; D008297:Male; D008516:Medicine, Chinese Traditional; D065626:Non-alcoholic Fatty Liver Disease; D010936:Plant Extracts / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology; D018515:Plant Leaves / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D021241:Spectrometry, Mass, Electrospray Ionization / Q000379:methods*; D014315:Triterpenes / Q000097:blood / Q000493:pharmacokinetics
chemical_list: D001685:Biological Factors; D004365:Drugs, Chinese Herbal; D006027:Glycosides; D044949:Kaempferols; D010936:Plant Extracts; D014315:Triterpenes; C468850:ilexgenin A; C511993:kaempferol-3-O-(6-trans-caffeoyl)-beta-D-glucopyranosyl-(1- 2)-beta-D-glucopyranoside-7-O-beta-D-glucopyranoside; D002726:Chlorogenic Acid