前列腺素抑制血清催产素酶活性的研究

Ashim C. Roy, Michael Yeang, Sultan M.M. Karim
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引用次数: 7

摘要

以s -berizyl-l-半胱氨酸-对硝基苯胺为底物,研究了前列腺素等化合物对体外人血清催产素酶(EC 3.4.11.3)活性的影响。PGE1、PGE2和PGF2α显著抑制血清催产素酶活性,且呈剂量相关,效价递减。cGMP、8-溴-cGMP、吲哚美辛、磷酸多酚维甙、高渗盐水和尿素也有活性。cAMP、db-cAMP、8-溴-cAMP、db-cCMP、5 ' -AMP、5 ' -ADP、5 ' -ATP、5 ' -GDP、5 ' -GTP、阿司匹林、水杨酸钠、对乙酰氨基酚、茶碱和IBMX对酶活性没有抑制作用。结果表明,前列腺素的催产作用可能是由于,至少部分,抑制催产素酶的活性。
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Inhibition of serum oxytocinase activity by prostaglandins

The effect of prostaglandins (PGs) and other compounds on human serum oxytocinase (EC 3.4.11.3) activity in vitro was studied by a sensitive assay using S-berizyl-l-cysteine-p-nitroanilide as substrate. PGE1, PGE2 and PGF significantly inhibited serum oxytocinase activity in a dose-related manner and in decreasing order of potency. cGMP, 8-bromo-cGMP, indomethacin, polyphloretin phosphate, hypertonic saline and urea were also active. cAMP, db-cAMP, 8-bromo-cAMP, db-cCMP, 5′-AMP, 5′-ADP, 5′-ATP, 5′-GDP, 5′-GTP, aspirin, sodium salicylate, paracetamol, theophylline and IBMX did not inhibit the enzyme activity. The results suggest that the oxytocic action of prostaglandins may be due, at least in part, to an inhibition of oxytocinase activity.

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