摘要
口服药物必须通过肠壁,然后通过肝脏进入全身循环前。在这个过程中,药物受到不同的过程,可能决定治疗价值。与活性药物在肠上皮细胞代谢酶和药物转运体的肠道屏障的药物生物利用度的确定起着重要的作用。越来越多的信息表明,药物代谢酶和转运蛋白在人的胃肠道(GI)变量的分布,所形成的不同环节具体胃肠屏障特性。在这篇综述中,药物代谢酶和转运蛋白在人类健康和疾病的胃肠道以及监管方面:遗传,miRNA表达,DNA甲基化的概述。在胃肠道的特定片段的药物代谢酶和转运体之间独特的相互作用,使药物释放更精确的以GI向更完整的生物利用度和药物相互作用进行预测。
关键词: 药物代谢酶,药物转运蛋白,胃肠道。
Current Medicinal Chemistry
Title:Expression and Regulation of Drug Transporters and Metabolizing Enzymes in the Human Gastrointestinal Tract
Volume: 23 Issue: 39
Author(s): M. Drozdzik, S. Oswald
Affiliation:
关键词: 药物代谢酶,药物转运蛋白,胃肠道。
摘要: Orally administered drugs must pass through the intestinal wall and then through the liver before reaching systemic circulation. During this process drugs are subjected to different processes that may determine the therapeutic value. The intestinal barrier with active drug metabolizing enzymes and drug transporters in enterocytes plays an important role in the determination of drug bioavailability. Accumulating information demonstrates variable distribution of drug metabolizing enzymes and transporters along the human gastrointestinal tract (GI), that creates specific barrier characteristics in different segments of the GI. In this review, expression of drug metabolizing enzymes and transporters in the healthy and diseased human GI as well as their regulatory aspects: genetic, miRNA, DNA methylation are outlined. The knowledge of unique interplay between drug metabolizing enzymes and transporters in specific segments of the GI tract allows more precise definition of drug release sites within the GI in order to assure more complete bioavailability and prediction of drug interactions.
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Cite this article as:
M. Drozdzik, S. Oswald , Expression and Regulation of Drug Transporters and Metabolizing Enzymes in the Human Gastrointestinal Tract, Current Medicinal Chemistry 2016; 23 (39) . https://dx.doi.org/10.2174/0929867323666161024154457
DOI https://dx.doi.org/10.2174/0929867323666161024154457 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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