Tomlinson D R, Willars G B, Carrington A L
Department of Pharmacology, Queen Mary and Westfield College, London, U.K.
Pharmacol Ther. 1992;54(2):151-94. doi: 10.1016/0163-7258(92)90031-t.
Aldose reductase inhibitors impede flux of glucose through the sorbitol pathway in diabetes mellitus. They therefore reduce the accumulation of the pathway metabolites, sorbitol and fructose, reduce the impact of the flux on the cofactors used by the pathway and reduce other derived phenomena, such as osmotic stress and myo-inositol depletion. As drugs, their targets are the chronic complications of diabetes--neuropathy, retinopathy, nephropathy and vasculopathy. In experimental models there is proof of activity against biochemical, functional and structural defects in all of the involved tissues, but we await full clinical verification of this potential.
醛糖还原酶抑制剂可阻碍糖尿病患者体内葡萄糖通过山梨醇途径的代谢。因此,它们可减少该途径代谢产物山梨醇和果糖的蓄积,降低该途径代谢对所用辅助因子的影响,并减少其他衍生现象,如渗透压应激和肌醇耗竭。作为药物,它们的靶点是糖尿病的慢性并发症——神经病变、视网膜病变、肾病和血管病变。在实验模型中,已证实其对所有受累组织的生化、功能和结构缺陷均有作用,但我们仍在等待对这一潜力的全面临床验证。