文章基本信息

标题：Inhibition of Bovine Leukocyte Thioltransferase by Anti-inflammatory Drugs and Anti-histaminic Drugs
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作者：Tadashi MIZOGUCHI ; Tohru NISHINAKA ; Gen UCHIDA 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：1993
卷号：16
期号：9
页码：840-842
DOI：10.1248/bpb.16.840
出版社：The Pharmaceutical Society of Japan
摘要：Thioltransferase was partially purified from bovine leukocyte using sonication, heat treatment at pH 5.1, Sephadex G-50 gel filtration and isoelectric focusing techniques. Isoelectric point (pI) of 8.3 for leukocyte thioltransferase was quite different from pI of 6.5 for erythrocyte enzyme. Bovine leukocyte thioltransferase was employed in a study on the influence of 12 anti-inflammatory drugs and 7 anti-histaminic drugs. Piroxicam which is a well-known anti-inflammatory drug demonstrated the most powerful inhibitory effect on enzyme activity. Inhibition of piroxicam was noncompetitive, and the K_i value measured 55.0 μM in the experiment involving bovine leukocyte enzyme. Tranilast which is a typical anti-histaminic drug most strongly inhibited the enzyme activity and the K_i value of the medicine was 20.3 μM (noncompetitive). Bovine liver and erythrocyte thioltransferases also were effectively inhibited by both medicines similar to leukocyte enzyme.
关键词：thioltransferase;leukocyte;inhibition;Ki;tranilast;piroxicam