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学科主题: 物理化学
题名: Intestinal Transport of Pure Diester-type Alkaloids from an Aconite Extract across the Caco-2 Cell Monolayer Model
作者: Li, Na1, 2;  Tsao, Rong3;  Sui, Zhigang2;  Ma, Jingwei1;  Liu, Zhiqiang4;  Liu, Zhongying1
通讯作者: ZhongyingLiu
关键词: Aconitum species ;  Ranunculaceae ;  Aconitum alkaloids ;  intestinal transport ;  Caco-2 cell monolayer ;  P-glycoprotein
刊名: PLANTA MEDICA
发表日期: 2012-05-01
DOI: 10.1055/s-0031-1298368
卷: 78, 期:7, 页:692-697
收录类别: SCI
文章类型: Article
部门归属: 18
项目归属: 1806
产权排名: 2,1
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Plant Sciences ;  Chemistry, Medicinal ;  Pharmacology & Pharmacy
研究领域[WOS]: Plant Sciences ;  Pharmacology & Pharmacy
英文摘要: Aconitine (AC), mesaconitine (MA), and hypaconitine (HA) are the active alkaloids identified in aconite tuber, an important traditional Chinese medicine. The study is aimed to investigate their intestinal transport profiles and potential interaction during the intestinal absorption using the Caco-2 cell monolayer model. All three alkaloids had good permeability with P-app values greater than 1 x 10(-6) cm.s(-1). However, AC, MA, and HA in a mixture and as an extract, in both cases with the same content of alkaloids, showed higher transport efficiency in the apical to basolateral, and lower transport efficiency in the basolateral to apical directions. Digoxin, as a P-glycoprotein (P-gp) substrate, was substantially effluxed in the basolateral to apical direction but inhibited by the three alkaloids. Furthermore, the backwards transport of MA and HA was inhibited by the P-gp inhibitor verapamil. These observations indicated that the three alkaloids may not only be P-gp inhibitors but also its substrates; they interact with each other and can potentially enhance their own bioavailability when taken concomitantly.
关键词[WOS]: PERFORMANCE LIQUID-CHROMATOGRAPHY ;  P-GLYCOPROTEIN ;  QUANTITATIVE-DETERMINATION ;  DRUG INTERACTIONS ;  IN-VITRO ;  DITERPENOID ALKALOIDS ;  MEDIATED TRANSPORT ;  HYPACONITINE ;  PERMEABILITY ;  MESACONITINE
语种: 英语
WOS记录号: WOS:000303838000008
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/118383
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Jilin Univ, Coll Pharm, Changchun 130021, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116012, Peoples R China
3.Agr & Agri Food Canada, Guelph Food Res Ctr, Guelph, ON, Canada
4.Chinese Acad Sci, Changchun Inst Appl Chem, Changchun Ctr Mass Spectrometry, Changchun 130022, Peoples R China

Recommended Citation:
Li, Na,Tsao, Rong,Sui, Zhigang,et al. Intestinal Transport of Pure Diester-type Alkaloids from an Aconite Extract across the Caco-2 Cell Monolayer Model[J]. PLANTA MEDICA,2012,78(7):692-697.
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