Murphy D G, Davidson W S
Biochem Pharmacol. 1985 Aug 15;34(16):2961-5. doi: 10.1016/0006-2952(85)90022-x.
Several compounds that are known to inhibit mammalian aldose reductases were examined for their effects on chicken muscle aldose reductase (EC 1.1.1.21). Sorbinil was the most effective compound tested. Alrestatin and phenobarbital were effective inhibitors of the enzyme although their IC50 values were 10-fold more than that of Sorbinil. Indomethacin, diphenylhydantoin, phenacetin, and valproate were also inhibitors of chicken muscle aldose reductase but were less effective. These compounds are all non-competitive inhibitors with respect to substrate. Menadione bisulfite, a watersoluble analog of Vitamin K3 which is a substrate for carbonyl reductase but not aldose reductase, was a competitive inhibitor of chicken aldose reductase with respect to substrate. This observation is discussed with reference to the possible treatment of muscular dystrophy with specific inhibitor of aldose reductases.
研究了几种已知可抑制哺乳动物醛糖还原酶的化合物对鸡肌肉醛糖还原酶（EC 1.1.1.21）的作用。索比尼尔是所测试的最有效化合物。阿雷司他汀和苯巴比妥是该酶的有效抑制剂，尽管它们的IC50值比索比尼尔高10倍。吲哚美辛、苯妥英、非那西丁和丙戊酸盐也是鸡肌肉醛糖还原酶的抑制剂，但效果较差。这些化合物相对于底物均为非竞争性抑制剂。亚硫酸甲萘醌是维生素K3的水溶性类似物，它是羰基还原酶的底物而非醛糖还原酶的底物，相对于底物它是鸡醛糖还原酶的竞争性抑制剂。结合醛糖还原酶特异性抑制剂对肌肉萎缩症的可能治疗对该观察结果进行了讨论。
