期刊文献+

隐丹参酮在Caco-2细胞模型中的吸收机制 被引量:9

Transport mechanism of cryptotanshinone across Caco-2 monolayer model
暂未订购
导出
摘要 目的研究隐丹参酮在Caco-2细胞模型中的吸收机制。方法用Caco-2细胞单层模型研究隐丹参酮的双向转运,并考察时间、药物浓度及抑制剂对隐丹参酮吸收的影响。用高效液相色谱法检测药物浓度,计算其表观渗透系数。结果隐丹参酮在Caco-2细胞模型中,从单层细胞层顶端到基底端的转运大于基底端到顶端的转运,随时间和浓度的增加,药物吸收呈饱和趋势,且可被其结构类似物丹参酮IIA竞争性抑制。结论隐丹参酮在Caco-2细胞模型中的吸收主要是由载体介导的主动转运,且该主动转运的载体位于Caco-2细胞单层的顶端。 Objective to investigate the absorption mechanism of cryptotan- shinone by using Caco -2 monolayer model. Methods Caco -2 cell monolayer model was used to investigate the bi - directional transport of cryptotanshinone. The effect of time, drug concentration and inhibitors on the absorption of cryptotanshinone was studied. Drug concentration was measured by HPLC and the apparent permeability coefficients (Papp)were calculated. Results The apical to basolateral ( AB ) permeability ( Papp ) of cryptotanshinone was bigger than the basolateral to apical (BA) permeability (Papp). The absorption of cryptotanshinone could be of saturation and inhibited by tanshinone IIg. Conclusion The absorption of cryptotanshinone in Caco -2 cell model was an active transportation mediated by transporter, which mainly located in the apical side of Caco -2 cell monolayer.
出处 《中国临床药理学杂志》 CAS CSCD 北大核心 2005年第4期268-271,共4页 The Chinese Journal of Clinical Pharmacology
基金 广州市重大项目--创新药物药理毒理评价研究技术平台资助项目(2003Z2-E4071)
关键词 隐丹参酮 CACO-2细胞模型 主动转运 cryptotanshinone Caco - 2 cell model active transport
  • 相关文献

参考文献12

  • 1薛明,崔颖,汪汉卿,罗永江,张彬,周宗田.隐丹参酮及其代谢物在猪体内的药代动力学研究[J].药学学报,1999,34(2):81-84. 被引量:37
  • 2Yang HT, Wang GJ. Transport and uptake characteristics of a new derivative of berberine (CPU -86017 ) by human intestinal epithelial cell line: Caco - 2 [ J ]. Acta Pharmacol Sin ,2003 ; 24: 1185 - 1191.
  • 3Yamashita S, Furubayashi T, Kataoka M , et al. Optimized conditions for prediction of intestinal drug permeability using Caco -2 cells [ J ]. Eur J Pharm Sci, 2000; 10:195 -204.
  • 4杨晓改,王夔,杨晓达,王夔,杨晓达,王夔,杨晓达,袁兰.用Caco_2细胞单层模型比较两种具类胰岛素效应的氧钒配合物的小肠吸收能力[J].科学通报,2002,47(20):1550-1555. 被引量:15
  • 5Xue M, Cui Y, Wang HQ, et al. Reversed- phase liquid chromatographic determination of cryptotanshinone and its active metabolite in pig plasma and urine[J]. J Pharm Biomed Anal, 1999; 21:207 - 213.
  • 6Artursson P, Karlsson J. Correlation between oral drug absorption in human and apparent drug permeability coefficients in human intestinal epithelial (Caco - 2) cells [ J]. Biochem Biophys Res Commun, 1991;175: 880 - 885.
  • 7关溯,陈孝,黄民.Caco-2细胞模型——药物吸收研究的有效“工具”[J].中国药理学通报,2004,20(6):609-614. 被引量:38
  • 8Zhu ZB, Makhija SK, Lu B, et al. Transport across a polarized monolayer of Caco - 2 cells by transferrin receptor - mediated adenovirus transcytosis [ J ]. Virology, 2004; 325:116 - 128.
  • 9袁媛,蒋学华,周静,杨俊毅,王彩琴.丹参酮Ⅱ_A在大鼠体肠的吸收机理[J].华西药学杂志,2002,17(4):246-248. 被引量:25
  • 10Hilgers AR, Smith DP, Biermacher JJ, et al. Predicting oral absorption of drugs: a case study with a novel class of antimicrobial agents [J]. Pharm Res, 2003; 20:1149-1155.

二级参考文献45

  • 1张锡源.丹参注射液静脉滴注治疗急性腹泻91例[J].中国中西医结合杂志,1993,13(2):109-109. 被引量:19
  • 2高玉桂 宋玉梅 等.丹参酮的药理[J].药学学报,1979,14(2):75-81.
  • 3房其年 张佩玲 等.丹参抗菌有效成分的研究[J].化学学报,1976,34:197-197.
  • 4夏文江 成章瑞.MCPKP-药物动力学室分析的一种微机程序[J].中国药理学报,1988,9:188-188.
  • 5罗厚蔚 盛龙生 等.抗分技杆菌活性成份——丹参酮的胆汁排泄与内转化[J].药学学报,1983,18:1-1.
  • 6谢明智 申竹芳.隐丹参酮的吸收、分布、排泄和代谢[J].药学学报,1983,18(2):90-96.
  • 7Gan LS,Thankker DR.Applications of the Caco-2 model in the design and development of biochemical and physical barriers posed by the intestinal epithelium.Adv Drug Delivery Rev,1997;23(1~3):77~98
  • 8Workshop on oral drug delivery:Interface between discovery and development-report and recommendations,national institute of general medical sciences.Bethesda MD,1993
  • 9Stenberg P,Bergstrom CA,Luthman K,Artursson P.Theoretical predictions of drug absorption in drug discovery and development.Clin Pharmacokinet,2002;41(11):877~99
  • 10Annette B,Sibylle H,Kayoshi S et al.Cell cultures as tools in biopharmacy.Eur J Pharm Sci,2000;11(Suppl 2):51~60

共引文献108

同被引文献128

引证文献9

二级引证文献54

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部