尼古丁和可替宁对前列环素和血栓素生物合成的体外效应。

The in vitro effects of nicotine and cotinine on prostacyclin and thromboxane biosynthesis.

作者信息

Chahine R, Calderone A, Navarro-Delmasure C

机构信息

Centre de recherche, Hôpital du sacré coeur de Montréal, Québec, Canada.

出版信息

Prostaglandins Leukot Essent Fatty Acids. 1990 Aug;40(4):261-6. doi: 10.1016/0952-3278(90)90047-o.

DOI:10.1016/0952-3278(90)90047-o

PMID:2274564

Abstract

The comparative effects of nicotine and cotinine on the biosynthesis of prostacyclin (PGI2) and thromboxane A2 (TXA2) in the horse aorta and platelet microsomes were studied. TXB2 and 6-keto PGF1a stable metabolites of TXA2 and PGI2 respectively were determined by radioimmunoassay. TXA2 production in the presence of either nicotine or cotinine treatment was not altered. However, a dose dependent inhibition of PGI2 biosynthesis, and a dose dependent stimulation of PGI2 biosynthesis, was observed in the presence of nicotine and cotinine respectively. Moreover, cotinine (10b3 M) was able to prevent the inhibitory effect of nicotine on PGI2 synthetase when preincubated with horse aorta microsomes. It appears that cotinine, the major nicotine metabolite resulting from a breakdown process, could be useful for the organism, at least for the cardiovascular system.

摘要

研究了尼古丁和可替宁对马主动脉和血小板微粒体中前列环素（PGI2）和血栓素A2（TXA2）生物合成的比较作用。分别通过放射免疫分析法测定TXA2和PGI2的稳定代谢产物TXB2和6-酮PGF1α。在尼古丁或可替宁处理的情况下，TXA2的产生没有改变。然而，分别在尼古丁和可替宁存在的情况下，观察到PGI2生物合成的剂量依赖性抑制和剂量依赖性刺激。此外，当与马主动脉微粒体预孵育时，可替宁（10b3 M）能够预防尼古丁对PGI2合成酶的抑制作用。看来，可替宁作为尼古丁分解过程产生的主要代谢产物，可能对机体有用，至少对心血管系统是有用的。