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非甾体抗炎药对人胎盘NAD及NADP相关的15-羟基前列腺素脱氢酶的抑制作用。

Inhibition of the human placental NAD- and NADP-linked 15-hydroxyprostaglandin dehydrogenases by nonsteroidal anti-inflammatory drugs.

作者信息

Jarabak J

机构信息

Department of Medicine, University of Chicago School of Medicine, Illinois 60637.

出版信息

Prostaglandins. 1988 Mar;35(3):403-11. doi: 10.1016/0090-6980(88)90131-1.

DOI:10.1016/0090-6980(88)90131-1
PMID:3375453
Abstract

A number of nonsteroidal anti-inflammatory drugs are non-competitive or mixed inhibitors of human placental NAD- and NADP-linked 15-hydroxyprostaglandin dehydrogenases. Cis- and trans-sulindac sulfide and cis- and trans-sulindac inhibit the NAD-linked enzyme as well or better than they inhibit various cyclooxygenases in vitro. The remainder of the compounds tested are at least one order of magnitude less effective as inhibitors of the 15-hydroxyprostaglandin dehydrogenases than they are as inhibitors of cyclooxygenases. Cis- and trans-sulindac sulfide are sufficiently strong inhibitors of the NAD-linked enzyme (Kis of 7.8 microM and 6.8 microM respectively) to raise the possibility that they might also inhibit this enzyme in vivo.

摘要

多种非甾体抗炎药是人类胎盘NAD和NADP连接的15-羟基前列腺素脱氢酶的非竞争性或混合性抑制剂。顺式和反式舒林酸硫化物以及顺式和反式舒林酸在体外抑制NAD连接的酶的效果与它们抑制各种环氧化酶的效果相同或更好。所测试的其余化合物作为15-羟基前列腺素脱氢酶抑制剂的效力比它们作为环氧化酶抑制剂的效力至少低一个数量级。顺式和反式舒林酸硫化物是NAD连接酶的足够强的抑制剂(分别为7.8 microM和6.8 microM的抑制常数),这增加了它们在体内也可能抑制这种酶的可能性。

相似文献

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Prostaglandins. 1988 Mar;35(3):403-11. doi: 10.1016/0090-6980(88)90131-1.
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