期刊文献+

MDCK-hMDR1细胞测定ML120B的细胞膜渗透性 被引量:1

Determination of passive permeability of ML120B using MDCK-hMDR1 cell culture
下载PDF
导出
摘要 目的测定ML120B的细胞膜渗透性。方法采用MDCK-hMDR1单层膜细胞测定ML120B的体外跨膜转运率及转运机制。结果药物的被动转运渗透性为678.9nm·s-1,不加P-糖蛋白(Pgp)抑制剂的外排率Efflux值为0.8,添加Pgp抑制剂的Efflux值为0.5。结论ML120B属于高渗透性药物,并不是Pgp的作用底物。 Objective To determine the passive permeability of ML120B. Methods MDCK-hMDR1 monolayer cells were used to determine the passive permeability of ML120B and its permeation mechanism. Results The passive permeability of ML120B was 678.9 nm·s-1 and the efflux ratio was 0.8 without Pgp inhibitor and 0.5 with Pgp inhibitor. Conclusions ML120B is a highly permeable compound and is not a Pgp substrate.
出处 《中国药剂学杂志(网络版)》 2009年第5期403-408,共6页 Chinese Journal of Pharmaceutics:Online Edition
关键词 药剂学 ML120B 渗透性 P-糖蛋白 MDCK-hMDR1 pharmaceutics ML120B passive permeability Pgp MDCK-hMDR1
  • 相关文献

参考文献8

  • 1刘瑶,曾苏.MDCK-MDR1细胞模型及其在药物透过研究中的应用进展[J].药学学报,2008,43(6):559-564. 被引量:24
  • 2Kimberley A. Lentz,Joseph W. Polli,Stephen A. Wring,Joan E. Humphreys,James E. Polli.Influence of Passive Permeability on Apparent P-glycoprotein Kinetics[J]. Pharmaceutical Research . 2000 (12)
  • 3NAQASHIMA K,SASSEVILLE V G,WEN D,et al.Rapid TNFR1-dependent lymphocyte depletion in vivo with a selective chemical inhibitor of IKKbeta. Blood . 2006
  • 4Noab BioDiscoveries. http://www.noabbiodiscoveries.com/assays/invitro/cell_permeability.pdf . 2008
  • 5Edwards,JE,Brouwer,KR,McNamara,PJ.GF120918, a P-glycoprotein modulator, increases the concentration of unbound amprenavir in the central nervous system in rats. Antimicrobial Agents and Chemotherapy . 2002
  • 6Tran,T. T.,Mittal,A.,Gales,T.,Maleeff,B.,Aldinger,T.,Polli,J. W.,Ayrton,A.,Ellens,H.,Bentz,J.An exact kinetic analysis of passive transport across a polarized confluent MDCK cell monolayer modeled as a single barrier. Journal of Pharmacological Sciences . 2004
  • 7Irvine JD,Takahashi L,Lockhart L,et al.MDCK (Madin-darby canine kidney) cells: a tool for membrane permeability screening. Journal of Pharmacological Sciences . 1999
  • 8Doan,K. M.,Humphreys,J. E.,Webster,L. O.,Wring,S. A.,Shampine,L. J.,Serabjit-Singh,C. J.,Adkison,K. K.,Polli,J. W.Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. Journal of Pharmacology and Experimental Therapeutics . 2002

二级参考文献37

  • 1Kessel D, Botterill V, Wodinsky I. Uptake and retention of daunomycin by mouse leukemic cells as factors in drug response [J]. Cancer Res, 1968,28:938 -941.
  • 2Biedler JL, Riehm H. Cellular resistance to actinomycin D in Chinese hamster cells in vitro: cross-resistance, radioautographic, and cytogenetic studies [ J ]. Cancer Res, 1970,30:1174 - 1184.
  • 3Juliano RL, Ling V. A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants [J]. Biochim Biophys Acta, 1976,455:152-162.
  • 4Braun A, Hammerle S, Suda K, et al. Cell cultures as tools in biopharmacy [ J]. Eur J Pharm Sci, 2000, 11 ( Suppl 2 ) : S51 - S60.
  • 5Veronesi B. Characterization of the MDCK cell line for screening neurotoxicants [ J ]. Neurotoxicology, 1996, 17:433 - 444.
  • 6Irvine JD, Takahashi L, Lockhart K, et al. MDCK ( Madin-Darby canine kidney) cells: a tool for membrane permeability screening [ J ]. J Pharm Sci, 1999,88:28 - 33.
  • 7Pastan I, Gottesman MM, Ueda K, et al. A retrovirus carrying an MDR1 cDNA confers multidrug resistance and poIarized expression of P-glycoprotein in MDCK cells [J]. Proc Natl Acad Sci USA, 1988,85:4486-4490.
  • 8Polli JW, Wring SA, Humphreys JE, et al. Rational use of in vitro P-glycoprotein assays in drug discovery [ J ]. J Pharmacol Exp Ther, 2001,299:620 - 628.
  • 9Simons K, lkonen E. Functional rafts in cell membranes [ J ]. Nature, 1997,387:569 - 572.
  • 10Luker GD, Pica CM, Kumar AS, et al. Effects of cholesterol and enantiomeric cholesterol on P-glycoprotein localization and function domains [ J]. Biochemistry, in low-density membrane 2000,39 : 7651 - 7661.

共引文献23

同被引文献3

引证文献1

二级引证文献5

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