文章基本信息

标题：Inhibitory Effect of Human Immunodeficiency Virus Protease Inhibtors on Multidrug Resistance Transporter P-Glycoproteins
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作者：Nobuaki SHIRAKI ; Akinobu HAMADA ; Kazuto YASUDA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2000
卷号：23
期号：12
页码：1528-1531
DOI：10.1248/bpb.23.1528
出版社：The Pharmaceutical Society of Japan
摘要：The objective of this study was to determine whether human immunodeficiency virus (HIV) protease inhibitors (saquinavir, ritonavir and nelfinavir) interact with other HIV protease inhibitors and/or HIV reverse transcriptase inhibitory (zidovudine, didanosine, lamivudine, zalcitabine and sanilvudine). We measured transport of nelfinavir, an HIV protease inhibitor which is known as a substrate for the multidrug resistance transporter P-glycoprotein(P-gp), in an epithelial monolayer model and K_i for P-gp of some drugs by a calcein flux assay. Transport in a basal to apical direction was 2-fold greater than apical to basal flux for nelfinavir, K_i for P-gp of a potent P-gp inhibitor cyclosporin A was 1.09 μM and those of ritonavir and nelfinavir were 111 μM and 28.6 μM, whereas all HIV reverse transcriptase inhibitors gave K_i values. These data show that nelfinavir, which is a substrate for P-gp, inhibits a P-gp function as a drug efflux pump and that HIV reverse transcriptase inhibitors do not inhibit P-gp.
关键词：P-glycoprotein;human immunodeficiency virus protease inhibitor;calcein-AM