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

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 co...

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Main Authors: Chiyu He, Ru Feng, Yupeng Sun, Shifeng Chu, Ji Chen, Chao Ma, Jie Fu, Zhenxiong Zhao, Min Huang, Jiawen Shou, Xiaoyang Li, Yuzhu Wang, Jinfeng Hu, Yan Wang, Juntian Zhang
Format: Article
Language:English
Published: Elsevier 2016-10-01
Series:Acta Pharmaceutica Sinica B
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S2211383516301769
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author Chiyu He
Ru Feng
Yupeng Sun
Shifeng Chu
Ji Chen
Chao Ma
Jie Fu
Zhenxiong Zhao
Min Huang
Jiawen Shou
Xiaoyang Li
Yuzhu Wang
Jinfeng Hu
Yan Wang
Juntian Zhang
author_facet Chiyu He
Ru Feng
Yupeng Sun
Shifeng Chu
Ji Chen
Chao Ma
Jie Fu
Zhenxiong Zhao
Min Huang
Jiawen Shou
Xiaoyang Li
Yuzhu Wang
Jinfeng Hu
Yan Wang
Juntian Zhang
author_sort Chiyu He
collection DOAJ
description 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 Rg1 and 0.09% of Rh1 were excreted in bile. Urinary excretion accounted for only 0.04% of Rg1. In conclusion, the observed excretion profiles for Rg1 and its metabolites after oral administration are helpful for understanding the poor oral bioavailability of Rg1 and will aid further investigations of Rg1 as a pharmacologically active component.
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spelling doaj.art-a6272b64f5ca4b60ab9cc8a2a6d645282022-12-21T22:59:39ZengElsevierActa Pharmaceutica Sinica B2211-38352211-38432016-10-016659359910.1016/j.apsb.2016.05.001Simultaneous quantification of ginsenoside Rg1 and its metabolites by HPLC–MS/MS: Rg1 excretion in rat bile, urine and fecesChiyu He0Ru Feng1Yupeng Sun2Shifeng Chu3Ji Chen4Chao Ma5Jie Fu6Zhenxiong Zhao7Min Huang8Jiawen Shou9Xiaoyang Li10Yuzhu Wang11Jinfeng Hu12Yan Wang13Juntian Zhang14State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, ChinaState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, ChinaState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, ChinaState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, ChinaState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, ChinaBeijing Analytical Application Center, Shimadzu (China) Co., Ltd., Beijing 100020, ChinaState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, ChinaState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, ChinaState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, ChinaState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, ChinaState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, ChinaState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, ChinaState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, ChinaState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, ChinaState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, ChinaGinsenoside 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 Rg1 and 0.09% of Rh1 were excreted in bile. Urinary excretion accounted for only 0.04% of Rg1. In conclusion, the observed excretion profiles for Rg1 and its metabolites after oral administration are helpful for understanding the poor oral bioavailability of Rg1 and will aid further investigations of Rg1 as a pharmacologically active component.http://www.sciencedirect.com/science/article/pii/S2211383516301769Ginsenoside Rg1Ginsenoside Rh1ProtopanaxatriolExcretionLC–MS/MS
spellingShingle Chiyu He
Ru Feng
Yupeng Sun
Shifeng Chu
Ji Chen
Chao Ma
Jie Fu
Zhenxiong Zhao
Min Huang
Jiawen Shou
Xiaoyang Li
Yuzhu Wang
Jinfeng Hu
Yan Wang
Juntian Zhang
Simultaneous quantification of ginsenoside Rg1 and its metabolites by HPLC–MS/MS: Rg1 excretion in rat bile, urine and feces
Acta Pharmaceutica Sinica B
Ginsenoside Rg1
Ginsenoside Rh1
Protopanaxatriol
Excretion
LC–MS/MS
title Simultaneous quantification of ginsenoside Rg1 and its metabolites by HPLC–MS/MS: Rg1 excretion in rat bile, urine and feces
title_full Simultaneous quantification of ginsenoside Rg1 and its metabolites by HPLC–MS/MS: Rg1 excretion in rat bile, urine and feces
title_fullStr Simultaneous quantification of ginsenoside Rg1 and its metabolites by HPLC–MS/MS: Rg1 excretion in rat bile, urine and feces
title_full_unstemmed Simultaneous quantification of ginsenoside Rg1 and its metabolites by HPLC–MS/MS: Rg1 excretion in rat bile, urine and feces
title_short Simultaneous quantification of ginsenoside Rg1 and its metabolites by HPLC–MS/MS: Rg1 excretion in rat bile, urine and feces
title_sort simultaneous quantification of ginsenoside rg1 and its metabolites by hplc ms ms rg1 excretion in rat bile urine and feces
topic Ginsenoside Rg1
Ginsenoside Rh1
Protopanaxatriol
Excretion
LC–MS/MS
url http://www.sciencedirect.com/science/article/pii/S2211383516301769
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