某些黄酮类药物对前列环素转化为6-氧代前列腺素E1的影响。

The effect of some flavone drugs on the conversion of prostacyclin to 6-oxoprostaglandin E1.

作者信息

Moore P K, Griffiths R J, Lofts F J

出版信息

Biochem Pharmacol. 1983 Sep 15;32(18):2813-7. doi: 10.1016/0006-2952(83)90097-7.

Abstract

Flavonoid drugs (rutin, naringenin and quercetin) were compared with indomethacin and sulphasalazine as inhibitors of rat and rabbit renal 9-hydroxyprostaglandin dehydrogenase, prostaglandin synthesis (bovine seminal vesicle microsomes) and inactivation (rabbit colon 100,000 g supernatant), vascular PGI2 formation (rat aortic rings) and for effects on platelet aggregation and on the isolated rat stomach strip. Rutin and naringenin potently inhibited rabbit renal conversion of PGI2 and PGF2 alpha to 6-oxoPGE1 and PGE2, respectively, but had no effect on rat renal 9-hydroxyprostaglandin dehydrogenase activity, prostaglandin breakdown, vascular PGI2 synthesis, platelet aggregation or the anti-aggregatory effect of PGI2 and 6-oxoPGE1. High concentrations (100 microM) of both drugs inhibited the spasmogenic effect of PGI2 on the rat stomach strip. Naringenin and quercetin (1 mM) inhibited whilst rutin (1 mM) stimulated microsomal prostaglandin synthesis. These results suggest that rutin and naringenin may be useful experimental tools to study the biological roles of 6-oxoPGE1.

摘要

将黄酮类药物（芦丁、柚皮素和槲皮素）与吲哚美辛和柳氮磺胺吡啶作为大鼠和家兔肾9-羟基前列腺素脱氢酶的抑制剂、前列腺素合成（牛精囊微粒体）和失活（家兔结肠100,000g上清液）、血管前列环素（PGI2）形成（大鼠主动脉环）的抑制剂进行比较，并观察它们对血小板聚集和离体大鼠胃条的影响。芦丁和柚皮素分别有效抑制家兔肾中PGI2和PGF2α向6-氧代前列腺素E1（6-oxoPGE1）和前列腺素E2（PGE2）的转化，但对大鼠肾9-羟基前列腺素脱氢酶活性、前列腺素分解、血管PGI2合成、血小板聚集或PGI2和6-氧代前列腺素E1的抗聚集作用无影响。两种药物的高浓度（100μM）均抑制PGI2对大鼠胃条的致痉挛作用。柚皮素和槲皮素（1mM）抑制而芦丁（1mM）刺激微粒体前列腺素合成。这些结果表明，芦丁和柚皮素可能是研究6-氧代前列腺素E1生物学作用的有用实验工具。