Roy A C, Yeang M, Karim S M
Prostaglandins Med. 1981 Jun;6(6):577-87. doi: 10.1016/0161-4630(81)90119-1.
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-benzyl-L-cysteine-p-nitroanilide as substrate. PGE1, PGE2 and PGF2 alpha 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-cGMP, 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.
采用以S-苄基-L-半胱氨酸-对硝基苯胺为底物的灵敏检测法,研究了前列腺素(PGs)及其他化合物对人血清催产素酶(EC 3.4.11.3)体外活性的影响。PGE1、PGE2和PGF2α以剂量相关方式显著抑制血清催产素酶活性,且效力依次降低。环磷酸鸟苷(cGMP)、8-溴环磷酸鸟苷(8-bromo-cGMP)、吲哚美辛、聚磷酸根皮苷、高渗盐水和尿素也有活性。环磷酸腺苷(cAMP)、二丁酰环磷酸腺苷(db-cAMP)、8-溴环磷酸腺苷(8-bromo-cAMP)、二丁酰环磷酸鸟苷(db-cGMP)、5'-腺苷酸(5'-AMP)、5'-二磷酸腺苷(5'-ADP)、5'-三磷酸腺苷(5'-ATP)、5'-鸟苷二磷酸(5'-GDP)、5'-鸟苷三磷酸(5'-GTP)、阿司匹林、水杨酸钠、对乙酰氨基酚、茶碱和异丁基甲基黄嘌呤不抑制该酶活性。结果表明,前列腺素的催产作用可能至少部分归因于对催产素酶活性的抑制。