Griffiths R J, Moore P K
Br J Pharmacol. 1983 Oct;80(2):395-402. doi: 10.1111/j.1476-5381.1983.tb10046.x.
The enzymatic catabolism of prostacyclin (PGI2) to 6 oxo prostaglandin E1 (6 oxo PGE1) was studied in platelet-rich and platelet-poor-plasma of rat, rabbit, guinea-pig and man. Rat, rabbit and human platelets convert PGI2 to a product with biological activity and thin layer chromatographic mobility identical to that of authentic 6 oxo PGE1. Platelets from these species also converted 9 beta-[3H]-PGI2 to non-radioactive 6 oxo PGE1 as shown by the progressive loss of extracted radioactivity following incubation. Formation of 6 oxo PGE1 was inhibited by the flavonoid drugs, rutin and naringenin. Guinea-pig platelets did not convert PGI2 to 6 oxo PGE1. Rat, rabbit and guinea-pig platelets do not spontaneously release a 6 oxo PGE1-like substance when incubated at 37 degrees C in the absence of added PGI2 or aggregating agents. The relevance of these findings to the possible physiological and pathophysiological roles of 6 oxo PGE1 in the regulation of platelet function is discussed.
在大鼠、兔子、豚鼠和人类富含血小板和血小板减少的血浆中,研究了前列环素(PGI2)向6-氧代前列腺素E1(6-氧代PGE1)的酶促分解代谢。大鼠、兔子和人类血小板将PGI2转化为一种具有生物活性且薄层色谱迁移率与真实6-氧代PGE1相同的产物。这些物种的血小板还将9β-[3H]-PGI2转化为非放射性的6-氧代PGE1,孵育后提取的放射性逐渐损失即表明了这一点。黄酮类药物芦丁和柚皮苷可抑制6-氧代PGE1的形成。豚鼠血小板不会将PGI2转化为6-氧代PGE1。在37℃、无添加PGI2或聚集剂的情况下孵育时,大鼠、兔子和豚鼠血小板不会自发释放一种类似6-氧代PGE1的物质。讨论了这些发现与6-氧代PGE1在调节血小板功能中可能的生理和病理生理作用的相关性。