Simultaneous quantification of ginsenoside Rg1 and its metabolites by HPLC-MS/MS: Rg1 excretion in rat bile, urine and feces

被引:25
作者
He, Chiyu [1 ]
Feng, Ru [1 ]
Sun, Yupeng [1 ]
Chu, Shifeng [1 ]
Chen, Ji [1 ]
Ma, Chao [2 ]
Fu, Jie [1 ]
Zhao, Zhenxiong [1 ]
Huang, Min [1 ]
Shou, Jiawen [1 ]
Li, Xiaoyang [1 ]
Wang, Yuzhu [1 ]
Hu, Jinfeng [1 ]
Wang, Yan [1 ]
Zhang, Juntian [1 ]
机构
[1] Chinese Acad Med Sci, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, Peoples R China
[2] Shimadzu China Co Ltd, Beijing Analyt Applicat Ctr, Beijing 100020, Peoples R China
基金
中国国家自然科学基金;
关键词
Ginsenoside Rg1; Ginsenoside Rh1; Protopanaxatriol; Excretion; LC-MS/MS; TRADITIONAL CHINESE MEDICINE; PANAX-NOTOGINSENG; ACTIVE SAPONINS; RG(1); PHARMACOKINETICS; PLASMA; PROTOPANAXATRIOL; IMPROVEMENT; ABSORPTION; RB-1;
D O I
10.1016/j.apsb.2016.05.001
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Ginsenoside Rg1 (Rg1), the major effective component of ginseng, has been shown to have multiple bioactivities, but low oral bioavailability. The aim of this study was to develop a simple, sensitive and rapid high performance liquid chromatography tandem mass spectrometry (LC-MS/MS) method, which could be used to validate and quantify the concentrations of Rg1 and its metabolites in Sprague-Dawley rat bile, urine, and feces after oral administration (25 mg/kg). Calibration curves offered satisfactory linearity (r> 0.995) within the determined ranges. Both intra-day and inter-day variances were less than 15%, and the accuracy was within 80-120%. The excretion recoveries of Rg1, ginsenoside Rh1 (Rh1), and protopanaxatriol (Ppt) in bile, urine, and feces combined were all greater than 70%. The fecal excretion recoveries of Rg1, Rh1, and Ppt were 40.11%, 22.19%, and 22.88%, respectively, whereas 6.88% of Rgl and 0.09% of Rhl were excreted in bile. Urinary excretion accounted for only 0.04% of Rgl. In conclusion, the observed excretion profiles for Rg1 and its metabolites after oral administration are helpful for understanding the poor oral bioavailability of Rgl and will aid further investigations of Rgl as a pharmacologically active component. (C) 2016 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND
引用
收藏
页码:593 / 599
页数:7
相关论文
共 23 条
[1]  
[Anonymous], CHINESE MED
[2]   Differentiation and authentication of Panax ginseng, Panax quinquefolius, and ginseng products by using HPLC/MS [J].
Chan, TWD ;
But, PPH ;
Cheng, SW ;
Kwok, IMY ;
Lau, FW ;
Xu, HX .
ANALYTICAL CHEMISTRY, 2000, 72 (06) :1281-1287
[3]  
Chen X., 2011, CHINESE J EXPT FORMU, V17, P210
[4]   Pharmacokinetics, Tissue Distribution, Metabolism, and Excretion of Ginsenoside Rg1 in Rats [J].
Feng, Liang ;
Wang, Ling ;
Hu, Changjiang ;
Jiang, Xuehua .
ARCHIVES OF PHARMACAL RESEARCH, 2010, 33 (12) :1975-1984
[5]  
Feng Liang, 2010, Yaoxue Xuebao, V45, P636
[6]  
Han Min, 2007, Yaoxue Xuebao, V42, P849
[7]   Ginsenoside-Rg1, one of the major active molecules from Panax ginseng, is a functional ligand of glucocorticoid receptor [J].
Lee, YJ ;
Chung, E ;
Lee, KY ;
Lee, YH ;
Huh, B ;
Lee, SK .
MOLECULAR AND CELLULAR ENDOCRINOLOGY, 1997, 133 (02) :135-140
[8]   High-performance liquid chromatographic assay for the active saponins from Panax notoginseng in rat tissues [J].
Li, L ;
Sheng, YX ;
Zhang, JL ;
Wang, SS ;
Guo, DA .
BIOMEDICAL CHROMATOGRAPHY, 2006, 20 (04) :327-335
[9]   HPLC determination of four active saponins from Panax notoginseng in rat serum and its application to pharmacokinetic studies [J].
Li, L ;
Sheng, YX ;
Zhang, JL ;
Wang, CS ;
Guo, D .
BIOMEDICAL CHROMATOGRAPHY, 2004, 18 (10) :849-856
[10]   Simultaneous determination of panax notoginsenoside R1, ginsenoside Rg1, Rd, Re and Rb1 in rat plasma by HPLC/ESI/MS: platform for the pharmacokinetic evaluation of total panax notoginsenoside, a typical kind of multiple constituent traditional Chinese medicine [J].
Li, Xiaoyu ;
Sun, Jianguo ;
Wang, Guangji ;
Hao, Haiping ;
Liang, Yan ;
Zheng, Yuanting ;
Yan, Bei ;
Sheng, Longsheng .
BIOMEDICAL CHROMATOGRAPHY, 2007, 21 (07) :735-746