Kulkarni F S, Eakins H M, Saber W L, Eakins K E
Prostaglandins. 1977 Oct;14(4):689-700. doi: 10.1016/0090-6980(77)90196-4.
Indomethacin-treated bovine iris-ciliary body microsomes (IBIM) have been studied for their ability to convert PG endoperoxides into either thromboxane-A2 (TxA2)-like or prostacyclin (PGI2)-like activity. The biological activity of the ocular tissue microsomes were compared with either indomethacin-treated human platelet microsomes (for TxA2-like activity) or rabbit aorta microsomes (for PGI2-like activity) under appropriate incubation conditions. No evidence could be found for the formation of TxA2-like activity from PG endoperoxides by the IBIM. In contrast, when the IBIM were incubated with PGH2 for 1 min at 22 degrees C without cofactors, PGI2-like activity was produced, causing profound relaxation of the isolated dog coronary artery preparation without contracting the rabbit aorta and inhibiting arachidonic acid-induced platelet aggregation. Equivalent quantities of boiled IBIM failed to alter the biological activity of PGH2 under identical conditions. Tranylcypromine (500 microgram/ml) completely abolished the appearance of PGI2-like activity. Furthermore, the PGI2-like activity found was stable for 10 min at 22 degrees C at pH 8.5 but completely lost under similar conditions at pH 5.5. It is concluded that microsomal preparations of normal bovine iris-ciliary body can synthesize PGI2-like activity in substantial amounts but not TxA2-like activity.
已对吲哚美辛处理的牛虹膜睫状体微粒体(IBIM)将前列腺素(PG)内过氧化物转化为血栓素A2(TxA2)样或前列环素(PGI2)样活性的能力进行了研究。在适当的孵育条件下,将眼组织微粒体的生物活性与吲哚美辛处理的人血小板微粒体(用于TxA2样活性)或兔主动脉微粒体(用于PGI2样活性)进行了比较。未发现IBIM能将PG内过氧化物转化为TxA2样活性。相反,当IBIM在22℃下与PGH2孵育1分钟且无辅助因子时,会产生PGI2样活性,使离体犬冠状动脉制剂显著舒张,而不会使兔主动脉收缩,也不会抑制花生四烯酸诱导的血小板聚集。等量煮沸的IBIM在相同条件下未能改变PGH2的生物活性。反苯环丙胺(500微克/毫升)完全消除了PGI2样活性的出现。此外,所发现的PGI2样活性在22℃、pH 8.5时可稳定10分钟,但在pH 5.5的类似条件下会完全丧失。结论是,正常牛虹膜睫状体的微粒体制剂可大量合成PGI2样活性,但不能合成TxA2样活性。