从人脑提纯了醛糖还原酶,应用酶动力学的方法研究了四种药物对此酶的抑制作用。结果表明索比尼尔,阿司他丁和苯巴比妥是人脑醛糖还原酶的完全性非竞争性抑制剂,四甲烯戊二酸是此酶的部分性非竞争性抑制剂。从抑制曲线及四种药物的抑制常数(Ki)可知,索比尼尔是人脑醛糖还原酶最有效的抑制剂,阿司他丁次之。根据苯巴比妥的Ki和它的毒性作用推测,此药似不宜以醛糖作为原酶的抑制剂应用于临床。 Purification of aldose reductase from the human brain, the use of enzyme kinetics method of the four drugs on the inhibition of this enzyme. The results indicate that sobinil, astrozine, and phenobarbital are complete, noncompetitive inhibitors of human brain aldose reductase, a partial noncompetitive inhibitor of this enzyme. From the inhibition curve and the inhibition constants (Ki) of the four drugs, sobrinir is the most potent inhibitor of human brain aldose reductase, followed by as low as aspirin. According to the phenobarbital Ki and its toxic effects speculated that the drug seems not suitable for use as an inhibitor of aldose as a clinical enzyme.