Absorption and Disposition of Ginsenosides after Oral Administration of Panax notoginseng Extract to Rats

doi:10.1124/dmd.109.029819

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 上海药物代谢研究中心

	Absorption and Disposition of Ginsenosides after Oral Administration of Panax notoginseng Extract to Rats
	Liu, Houfu 2; Yang, Junling; Du, Feifei ; Gao, Xiumei 3; Ma, Xutao 3; Huang, Yuhong 3; Xu, Fang ; Niu, Wei ; Wang, Fengqing ; Mao, Yu
刊名	DRUG METABOLISM AND DISPOSITION
	2009-12
卷号	37 期号:12 页码:2290-2298
ISSN号	0090-9556
DOI	10.1124/dmd.109.029819
文献子类	Article
英文摘要	Panax notoginseng (Sanqi) is a cardiovascular herb containing ginsenosides that are believed to be responsible for the therapeutic effects of Sanqi. The aim of this study was to evaluate rat exposure to ginsenosides after oral administration of Sanqi extract and to identify the key factors affecting their absorption and disposition. Ginsenosides were administered to rats, either in the form of Sanqi extract or as pure chemicals. The ginsenosides Ra-3, Rb-1, Rd, Re, Rg(1), and notoginsenoside R-1 were the major saponins present in the herbal extract. Systemic exposure to ginsenosides Ra-3, Rb-1, and Rd after oral administration of the extract was significantly greater than that to the other compounds. Considerable colonic deglycosylation of the ginsenosides occurred, but the plasma levels of deglycosylated metabolites were low in rats. Poor membrane permeability and active biliary excretion are the two primary factors limiting systemic exposure to most ginsenosides and their deglycosylated metabolites. In contrast with other ginsenosides, biliary excretion of ginsenosides Ra-3 and Rb-1 was passive. Meanwhile, the active biliary excretion of ginsenoside Rd was significantly slower than that of other saponins. Slow biliary excretion, inefficient metabolism, and slow renal excretion resulted in long-circulating and thus relatively high exposure levels for these three ginsenosides. For these reasons, plasma ginsenosides Ra-3, Rb-1, and Rd were identified as pharmacokinetic markers for indicating rat systemic exposure to Sanqi extract. This is a systematic investigation of the absorption and disposition of ginsenosides from an herb, the information gained from which is important for linking Sanqi administration to its medicinal effects.
资助项目	National Basic Research Program of China[2005CB523403] ; National Science and Technology Major Project of China[2009ZX09304-002] ; National Science Fund of China for Distinguished Young Scholars[30925044] ; National Natural Science Foundation of China[90209044] ; Shanghai Science and Technology Major Project[08DZ1980200]
WOS关键词	TRADITIONAL CHINESE MEDICINE ; 4 ACTIVE SAPONINS ; INTESTINAL BACTERIA ; GINSENG SAPONINS ; HERBAL MEDICINE ; BIOAVAILABILITY ; PERFORMANCE ; METABOLISM ; PLASMA ; EXCRETION
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	AMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS
WOS记录号	WOS:000271935200004
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/279074]
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.Chinese Acad Sci, Shanghai Ctr DMPK Res, Shanghai Inst Mat Med, SIBS, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Grad Sch, Shanghai 201203, Peoples R China; 3.Tianjin Univ Tradit Chinese Med, Tianjin, Peoples R China; 4.Tianjin Inst Pharmaceut Res, Tianjin State Key Lab Pharmacodynam & Pharmacokin, Tianjin, Peoples R China
推荐引用方式 GB/T 7714	Liu, Houfu,Yang, Junling,Du, Feifei,et al. Absorption and Disposition of Ginsenosides after Oral Administration of Panax notoginseng Extract to Rats[J]. DRUG METABOLISM AND DISPOSITION,2009,37(12):2290-2298.
APA	Liu, Houfu.,Yang, Junling.,Du, Feifei.,Gao, Xiumei.,Ma, Xutao.,...&Li, Chuan.(2009).Absorption and Disposition of Ginsenosides after Oral Administration of Panax notoginseng Extract to Rats.DRUG METABOLISM AND DISPOSITION,37(12),2290-2298.
MLA	Liu, Houfu,et al."Absorption and Disposition of Ginsenosides after Oral Administration of Panax notoginseng Extract to Rats".DRUG METABOLISM AND DISPOSITION 37.12(2009):2290-2298.