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Absorption, liver first-pass effect, pharmacokinetics and tissue distribution of calycosin-7-O-beta-D-glucopyranoside (C7G) and its major active metabolite, calycosin, following oral administration of C7G in rats by LC-MS/MS

文献类型：期刊论文

作者Tian, Xiaoting1,2; Chen, Shuoji1,2,3; Zhang, Yuanyuan4; Chen, Luying1,2; Guo, Xiaozhen1,2; Xu, Zhou1,2; Liu, Huan1,2; Hu, Pei1,2; Chen, Zhenyuan1,2; Li, Zhixiong1,2
刊名JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
出版日期2018-01-30
卷号148页码:350-354
关键词Calycosin-7-O-beta-D-glucopyranoside Calycosin Pharmacokinetics Liver first-pass effect Tissue distribution
ISSN号0731-7085
DOI10.1016/j.jpba.2017.10.027
文献子类Article
英文摘要Previously, we discovered calycosin, an extensively distributed metabolite of Calycosin-7-O-beta-nglucopyranoside (C7G), elicited stronger anti-virus activity than C7G. However, the pharmacokinetics and tissue distribution of C7G and calycosin remained obscure on C7G treatments. In this study, a liquid chromatography tandem mass spectrometry method was established and validated for the simultaneous determination of C7G and calycosin, and it was applied to the pharmacokinetics and tissue distribution of C7G and calycosin following oral administration of C7G at 120 mg/kg in rats. Consequently, the exposure of C7G and calycosin was both similarly low in the systemic plasma, but the levels of calycosin were 53.5 folds higher than that of C7G in the portal vein plasma, corresponding to the liver extraction ratio (ER) of C7G and calycosin at 0.3% and 98.5% respectively. Therefore, our results revealed that liver first-pass effect played the predominant role in the poor circulating levels of calycosin on C7G treatments, whereas the intestinal first-pass effect was predominant for those of C7G. In contrast to no observation of C7G, the calycosin levels were 212.1, 30.5 and 4.7 folds higher in the liver, kidney and heart than its circulating levels, respectively. The high tissue distribution of calycosin provided new hints and evidences to the pharmacological mechanisms of C7G and Astragali Radix. (C) 2017 Elsevier B.V. All rights reserved.
WOS关键词ANTIVIRAL ACTIVITIES ; CELLS ; IDENTIFICATION
资助项目National Natural Science Foundation of China[81374052] ; Shanghai Science and Technology Foundation[14401900700] ; National Natural Science Foundation for Young Scientists of China[81603280] ; National Natural Science Foundation for Young Scientists of China[81602998]
WOS研究方向Chemistry ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000417771700043
出版者ELSEVIER SCIENCE BV
源URL[http://119.78.100.183/handle/2S10ELR8/279943]  
专题上海中药现代化研究中心
通讯作者Li, Zhixiong; Huang, Chenggang
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China;
3.Shanghai Normal Univ, Coll Life & Environm Sci, Shanghai 201203, Peoples R China;
4.Sichuan Univ, West China Sch Basic Med Sci & Forens Med, Chengdu 610041, Sichuan, Peoples R China
推荐引用方式
GB/T 7714		 Tian, Xiaoting,Chen, Shuoji,Zhang, Yuanyuan,et al. Absorption, liver first-pass effect, pharmacokinetics and tissue distribution of calycosin-7-O-beta-D-glucopyranoside (C7G) and its major active metabolite, calycosin, following oral administration of C7G in rats by LC-MS/MS[J]. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,2018,148:350-354.
APA Tian, Xiaoting.,Chen, Shuoji.,Zhang, Yuanyuan.,Chen, Luying.,Guo, Xiaozhen.,...&Huang, Chenggang.(2018).Absorption, liver first-pass effect, pharmacokinetics and tissue distribution of calycosin-7-O-beta-D-glucopyranoside (C7G) and its major active metabolite, calycosin, following oral administration of C7G in rats by LC-MS/MS.JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,148,350-354.
MLA Tian, Xiaoting,et al."Absorption, liver first-pass effect, pharmacokinetics and tissue distribution of calycosin-7-O-beta-D-glucopyranoside (C7G) and its major active metabolite, calycosin, following oral administration of C7G in rats by LC-MS/MS".JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS 148(2018):350-354.

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来源：上海药物研究所

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