Systemic and cerebral exposure to and pharmacokinetics of flavonols and terpene lactones after dosing standardized Ginkgo biloba leaf extracts to rats via different routes of administration
文献类型：期刊论文
| 作者 | Chen, Feng2,3,4; Li, Li2; Xu, Fang2; Sun, Yan2; Du, Feifei2; Ma, Xutao2; Zhong, Chenchun2; Li, Xiuxue2; Wang, Fengqing2; Zhang, Nating2 |
| 刊名 | BRITISH JOURNAL OF PHARMACOLOGY
 |
| 出版日期 | 2013-09 |
| 卷号 | 170期号:2页码:440-457 |
| 关键词 | Ginkgo biloba GBE50 ShuXueNing injection flavonols terpene lactones systemic exposure cerebral exposure pharmacokinetics route of administration PK markers |
| ISSN号 | 0007-1188 |
| DOI | 10.1111/bph.12285 |
| 文献子类 | Article |
| 英文摘要 | BACKGROUND AND PURPOSE Flavonols and terpene lactones are putatively responsible for the properties of Ginkgo biloba leaf extracts that relate to prevention and treatment of cardiovascular disease and cerebral insufficiency. Here, we characterized rat systemic and cerebral exposure to these ginkgo compounds after dosing, as well as the compounds' pharmacokinetics. EXPERIMENTAL APPROACH Rats received single or multiple doses of ShuXueNing injection (prepared from GBE50 for intravenous administration) or GBE50 (a standardized extract of G.biloba leaves for oral administration). Brain delivery of the ginkgo compounds was assessed with microdialysis. Various rat samples were analysed using liquid chromatography/mass spectrometry. KEY RESULTS Slow terminal elimination features of the flavonols counterbalanced the influence of poor oral bioavailability on their systemic exposure levels, which also resulted in significant accumulation of the compounds in plasma during the subchronic treatment with ShuXueNing injection and GBE50. Unlike the flavonols, the terpene lactones had poor enterohepatic circulation due to their rapid renal excretion and unknown metabolism. The flavonol glycosides occurred as major forms in plasma after dosing with ShuXueNing injection, while the flavonol aglycone conjugates were predominant in plasma after dosing with GBE50. Cerebral exposure was negligible for the flavonols and low for the terpene lactones. CONCLUSION AND IMPLICATIONS Unlike the significant systemic exposure levels, the levels of cerebral exposure to the flavonols and terpene lactones are low. The elimination kinetic differences between the two classes of ginkgo compounds influence their relative systemic exposure levels. The information gained is relevant to linking ginkgo administration to the medicinal effects. |
| WOS关键词 | ADHESION MOLECULE EXPRESSION ; ALZHEIMERS-DISEASE ; ENDOTHELIAL-CELLS ; CORONARY-ARTERY ; EGB 761(R) ; IN-VIVO ; QUERCETIN ; BRAIN ; PLASMA ; BIOAVAILABILITY |
| 资助项目 | National Natural Science Fund of China for Distinguished Young Scholars[30925044] ; Shanghai Science and Technology Major Project[07DZ19703] ; National Science & Technology Major Project 'Key New Drug Creation and Manufacturing Program'[2009ZX09304-002] ; National Natural Science Fund of China[30772772] ; National Natural Science Fund of China[30873120] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000323540200019 |
| 出版者 | WILEY-BLACKWELL |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277485]  |
| 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.China Acad Chinese Med Sci, Inst Chinese Mat Med, Beijing, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 3.Univ Chinese Acad Sci, Shanghai, Peoples R China; 4.Hainan Med Univ, Haikou, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Chen, Feng,Li, Li,Xu, Fang,et al. Systemic and cerebral exposure to and pharmacokinetics of flavonols and terpene lactones after dosing standardized Ginkgo biloba leaf extracts to rats via different routes of administration[J]. BRITISH JOURNAL OF PHARMACOLOGY,2013,170(2):440-457. |
| APA | Chen, Feng.,Li, Li.,Xu, Fang.,Sun, Yan.,Du, Feifei.,...&Li, Chuan.(2013).Systemic and cerebral exposure to and pharmacokinetics of flavonols and terpene lactones after dosing standardized Ginkgo biloba leaf extracts to rats via different routes of administration.BRITISH JOURNAL OF PHARMACOLOGY,170(2),440-457. |
| MLA | Chen, Feng,et al."Systemic and cerebral exposure to and pharmacokinetics of flavonols and terpene lactones after dosing standardized Ginkgo biloba leaf extracts to rats via different routes of administration".BRITISH JOURNAL OF PHARMACOLOGY 170.2(2013):440-457. |
入库方式： OAI收割
来源：上海药物研究所
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