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3,4-二羟基苯乙酮(DHAP)是从秃毛冬青叶中分离的有效成份。临床试用对冠心病患者心绞痛有较好的疗效。动物实验表明,DHAP能抑制血小板聚集和释放反应,升高富含血小板血浆(PRP)中cAMP水平。本文以~3H-cAMP转化为~3H-腺苷来表示血小板磷酸二酯酶(PDE)的活性,观察到DHAP(10,50,100,200μg/ml)均能明显抑制血小板PDE活性、抑制效应与药物浓度成正相关,而对腺苷酸环化酶活性无明显影响。DHAP升高血小板cAMP水平的机理是抑制了血小板PDE的活性。抑制血小板功能和升高血小板cAMP水平可能是DHAP能缓解冠心病病人心绞痛的机理。
3,4-Dihydroxyacetophenone (DHAP) is an active ingredient isolated from the bald-headed holly leaf. Clinical trials of angina pectoris in patients with coronary heart disease have a good effect. Animal experiments show that DHAP can inhibit platelet aggregation and release response, elevated platelet-rich plasma (PRP) cAMP levels. In this paper, ~ 3H-cAMP was converted to ~ 3H-adenosine to show the activity of platelet phosphodiesterase (PDE). It was observed that DHAP (10,50,100,200μg / ml) could obviously inhibit the activity of platelet PDE. The inhibitory effect and drug concentration A positive correlation, but no significant effect on adenylate cyclase activity. The mechanism by which DHAP increases platelet cAMP levels is to inhibit platelet PDE activity. Inhibition of platelet function and elevated platelet cAMP levels may be DHAP can relieve angina pectoris in patients with coronary heart disease mechanism.