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氯酯醒对豚鼠母胎肺中胆碱磷酸转移酶活性的影响。

Effects of centrophenoxine on cholinephosphotransferase activity in maternal and fetal guinea pig lung.

作者信息

Stith I E, Nag S, Mukherjee S, Das S K

机构信息

Department of Biochemistry, Meharry Medical College, Nashville, TN 37208.

出版信息

Exp Lung Res. 1989 Jul;15(4):587-96. doi: 10.3109/01902148909069620.

Abstract

Cholinephosphotransferase activities of guinea pig lung mitochondria and microsomes are inhibited by centrophenoxine and one of its metabolites, p-chlorophenoxyacetate. 2-Dimethylaminoethanol, the second metabolite of centrophenoxine, has no inhibitory effect on the enzyme activity. The inhibition of enzyme activity by centrophenoxine is noncompetitive. Intravenous injection of centrophenoxine and p-chlorophenoxyacetate to pregnant animals causes inhibition of cholinephosphotransferase activity in adult lung but not in fetal lung. However, direct administration of centrophenoxine to the fetus after laparotomy causes inhibition of both subcellular enzyme activity in fetal lung. It is suggested that the drug injected to the pregnant animals does not reach the fetal lung or is metabolized. Furthermore, while centrophenoxine injection does not change the total phosphatidylcholine content of adult lung, the acyl group composition of phosphatidylcholine was modulated.

摘要

氯酯醒及其代谢产物对氯苯氧乙酸可抑制豚鼠肺线粒体和微粒体的胆碱磷酸转移酶活性。氯酯醒的另一种代谢产物二甲氨基乙醇对该酶活性无抑制作用。氯酯醒对酶活性的抑制作用是非竞争性的。给妊娠动物静脉注射氯酯醒和对氯苯氧乙酸会抑制成年动物肺中的胆碱磷酸转移酶活性,但对胎儿肺无此作用。然而,剖腹术后直接给胎儿注射氯酯醒会抑制胎儿肺中两种亚细胞酶的活性。这表明给妊娠动物注射的药物未到达胎儿肺或已被代谢。此外,虽然注射氯酯醒不会改变成年动物肺中总磷脂酰胆碱的含量,但磷脂酰胆碱的酰基组成会受到调节。

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