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业已证明,皮质甾体类抗炎药可抑制磷酸酯酶A_2(PL-A_2)的活性,在炎症和血小板聚集过程中,PL-A_2活性增高,所以PL-A_2在这些过程中似起重要作用。如这假设成立,则PL-A_2抑制剂应有治疗意义。作者通过观察除皮质甾体类以外,其它PL-A_2抑制剂(罂粟碱、阿的平、BPB(P-溴苯酰溴)和CB_(874)[2,3-二溴(4’-环己基-3’-氯)-苯基-4-氧代丁酸]是否有抗炎和/或抗血小板聚集作用来证实此假设。实验方法:(1)以凝血酶或钙离子载体蛋白A_(23187)激活~(14)C花生四烯酸标记的狗血小板,观察PL-A_2抑制剂对标记血小板磷酸酯水解,花生四烯酸的释放以及PG合成的影响,并测定药物对纯化PL-A_2水解2-[(1-
It has been demonstrated that corticosteroid anti-inflammatory drugs can inhibit the activity of phosphatase A 2 (PL-A 2) and PL-A 2 activity during inflammation and platelet aggregation, so PL-A 2 may play an important role in these processes . If this hypothesis holds, PL-A 2 inhibitors should have therapeutic implications. The authors investigated the effects of other PL-A 2 inhibitors (papaverine, alprenorphine, BPB and CB_ (874) [2,3-dibromo Hexyl-3’-chloro) -phenyl-4-oxobutanoic acid] to confirm this hypothesis.Experimental methods: (1) The thrombin or calcium ionophore protein A_ ( The effect of PL-A 2 inhibitor on platelet phospholipid hydrolysis, arachidonic acid release and PG synthesis was observed and the effect of drug on the purification of PL-A 2 Hydrolysis of 2 - [(1-