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Combinatorial Metabolism Notably Affects Human Systemic Exposure to Ginsenosides from Orally Administered Extract of Panax notoginseng Roots (Sanqi)

文献类型：期刊论文

作者Hu, Zheyi2; Yang, Junling2; Cheng, Chen2; Huang, Yuhong1; Du, Feifei2; Wang, Fengqing2; Niu, Wei2; Xu, Fang2; Jiang, Rongrong2; Gao, Xiumei1
刊名DRUG METABOLISM AND DISPOSITION
出版日期2013-07
卷号41期号:7页码:1457-1469
ISSN号0090-9556
DOI10.1124/dmd.113.051391
文献子类Article
英文摘要Ginsenosides are medicinal ingredients of the cardiovascular herb Panax notoginseng roots (Sanqi). Here, we implemented a human study (ChiCTR-ONC-09000603; www.chictr.org) to characterize pharmacokinetics and metabolism of ginsenosides from an orally ingested Sanqi-extract (a 1: 10 water extract of Sanqi) and the human plasma and urine samples were analyzed by liquid chromatography-mass spectrometry. Plasma and urinary compounds derived from ginsenosides included: 1) intestinally absorbed ginsenosides Ra-3, Rb-1, Rd, F-2, Rg(1), and notoginsenoside R-1; and 2) the deglycosylated products compound-K, 20(S)-protopanaxadiol, 20(S)-protopanaxatriol, and their oxidized metabolites. The systemic exposure levels of the first group compounds increased as the Sanqi-extract dose increased, but those of the second group compounds were dose-independent. The oxidized metabolites of 20(S)-protopanaxadiol and 20(S)-protopanaxatriol represented the major circulating forms of ginsenosides in the bloodstream, despite their large interindividual differences in exposure level. The metabolites were formed via combinatorial metabolism that consisted of a rate-limiting step of ginsenoside deglycosylation by the colonic microflora and a subsequent step of sapogenin oxidation by the enterohepatic cytochrome P450 enzymes. Significant accumulation of plasma ginsenosides and metabolites occurred in the human subjects receiving 3-week sub-chronic treatment with the Sanqi-extract. Plasma 20(S)-protopanaxadiol and 20(S)-protopanaxatriol could be used as pharmacokinetic markers to reflect the subjects' microbial activities, as well as the timely-changes and interindividual differences in plasma levels of their respective oxidized metabolites. The information gained from the current study is relevant to pharmacology and therapeutics of Sanqi.
WOS关键词HERBAL MEDICINES ; DRUGS ; PHARMACOKINETICS ; ABSORPTION ; RAT
资助项目National Science Fund of China for Distinguished Young Scholars[30925044] ; National Basic Research Program of China[2012CB518403] ; National Science and Technology Major Project of China "Key New Drug Creation and Manufacturing Program"[2009ZX09304-002] ; National Science and Technology Major Project of China "Key New Drug Creation and Manufacturing Program"[2012ZX09304007] ; National Science and Technology Major Project of China "Key New Drug Creation and Manufacturing Program"[2012ZX09303010] ; Knowledge Innovation Program of the Chinese Academy of Sciences[KSCX2-YW-R-191]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000320307100018
出版者AMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS
源URL[http://119.78.100.183/handle/2S10ELR8/277570]  
专题上海药物代谢研究中心
科研与新药推进处
通讯作者Li, Chuan
作者单位1.Tianjin Univ Tradit Chinese Med, Tianjin, Peoples R China;
2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China;
3.China Acad Chinese Med Sci, Inst Chinese Mat Med, Beijing, Peoples R China
推荐引用方式
GB/T 7714		 Hu, Zheyi,Yang, Junling,Cheng, Chen,et al. Combinatorial Metabolism Notably Affects Human Systemic Exposure to Ginsenosides from Orally Administered Extract of Panax notoginseng Roots (Sanqi)[J]. DRUG METABOLISM AND DISPOSITION,2013,41(7):1457-1469.
APA Hu, Zheyi.,Yang, Junling.,Cheng, Chen.,Huang, Yuhong.,Du, Feifei.,...&Li, Chuan.(2013).Combinatorial Metabolism Notably Affects Human Systemic Exposure to Ginsenosides from Orally Administered Extract of Panax notoginseng Roots (Sanqi).DRUG METABOLISM AND DISPOSITION,41(7),1457-1469.
MLA Hu, Zheyi,et al."Combinatorial Metabolism Notably Affects Human Systemic Exposure to Ginsenosides from Orally Administered Extract of Panax notoginseng Roots (Sanqi)".DRUG METABOLISM AND DISPOSITION 41.7(2013):1457-1469.

入库方式： OAI收割

来源：上海药物研究所

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