单胺氧化酶抑制剂体外筛选模型的建立

Establishment of the screening model for monoamine oxidase inhibitors in vitro

目的建立一种可筛选对单胺氧化酶(MAO)有抑制作用药物的体外模型,用于评价药物对单胺氧化酶的影响。方法以5-羟色胺(5-HT)和苄胺分别作为单胺氧化酶A(MAO-A)和单胺氧化酶B(MAO-B)的反应底物,采用紫外分光光度法,分别在280、242 nm测定吸光度,计算药物对酶的抑制率。结果建立的模型筛选了17种药物,其中15种药物对MAO-A有抑制作用,13种药物对MAO-B有抑制作用。结论此模型操作简单,重复性好,可用于大规模体外筛选MAO-A和MAO-B的抑制药物,指导临床合理使用此类制剂。

AIM To establish a filterable in vitro model for monoamine oxidase （MAO） inhibitory drugs for eval- uating the effects of drugs on monoamine oxidase. METHODS With 5-hydroxytryptamine （5-HT） and benzylamine as reaction substrates for MAO-A and MAO-B, 280 nm and 242 nm absorbance of UV spectrophotometry was measured to calculate the inhibition rate of the drug. RESULTS A total of 17 drugs were screened, among them, 15 kinds showed MAO-A inhibition,and 13 kinds showed MAO-B inhibition. CONCLUSION This model is simple to operate, and can be used for large-scale screening in vitro MAO-A and MAO-B inhibitory drugs, and to guide the rational use of such preparations.