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  • 标题:Electrophysiological Studies on the Mechanism for Enhanced Intestinal Transport of Water-Soluble Compounds by Antibiotic Peptide Bacitracin
  • 本地全文:下载
  • 作者:Ying-Shu QUAN ; Daisuke KURIBAYASHI ; Yuko NAKAMOTO
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1999
  • 卷号:22
  • 期号:8
  • 页码:841-845
  • DOI:10.1248/bpb.22.841
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Bacitracin is an antibacterial cyclic dodecapeptide produced by Bacillus licheniformin. Besides antibacterial activity, it is reported to have a protease inhibitory activity and an absorption enhancing action. Here we determined the effects of bacitracin on transport of water-soluble dye fluoresceinisothiocyanate (FITC)-dextran across the rat intestinal mucosal membrane using an electrophysiological technique. Bacitracin enhanced the intestinal mucosal-to-serosal transport of FITC-dextran in concentration-dependent and pH-dependent manners. In particular, the addition of bacitracin to the mucosal side led to a remarkable enhancement of FITC-dextran transport across the colonic membrane. Furthermore, its exhibition of transport enhancement required the existence of metal divalent cations, Ca2+ and Mg2+, in the mucosal compartment. Electrophysiological study using voltageclamp technique revealed that a relatively lower concentration of bacitracin (5 mM) enhanced the transport of 6-carboxyfluorescein via a paracellular pathway in the colonic membrane and higher concentration of bacitracin (20 mM) affects both transcellular and paracellular routes, resulting in significant enhancement of 6-carboxyfluorescein across the colonic membrane. These findings might provide the useful information for enhancing the intestinal transport of poorly a sbsorbable drugs by bacitracin which has multiple functions.
  • 关键词:bacitracin;fluoresceinisothiocynate (FITC)-dextran;Ussing type chamber;electrophysiology;voltage clamp method;passive transport
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