醛糖还原酶抑制剂索比尼尔与糖尿病并发症的抗争

Sorbinil, an Aldose Reductase Inhibitor, in Fighting Against Diabetic Complications.

作者信息

Huang Qi, Liu Qiong, Ouyang Dongsheng

机构信息

Department of Clinical Pharmacology, Xiangya Hospital of Central South University, Changsha 410008, China.

Department of Pharmacy, Xiangya Hospital of Central South University, Changsha, Hunan 410008, China.

出版信息

Med Chem. 2019;15(1):3-7. doi: 10.2174/1573406414666180524082445.

DOI:10.2174/1573406414666180524082445

PMID:29792152

Abstract

BACKGROUND

Aldose reductase (AR) is involved in the pathogenesis of diabetes, which is one of the major threats to global public health.

OBJECTIVE

In this review article, we have discussed the role of sorbinil, an AR inhibitor (ARI), in preventing diabetic complications.

RESULTS

AR contributes in diabetes by generating excess intracellular superoxide and other mediators of oxidative stress through polyol pathway. Inhibition of AR activity thus might be a potential approach for the management of diabetic complications. Experimental evidences indicated that sorbinil can decrease AR activity and inhibit polyol pathway. Both in vitro and animal model studies reported the efficacy of sorbinil in controlling the progression of diabetes. Moreover, Sorbinil has been found to be comparatively safer than other ARIs for human use. But, it is still in earlyphase testing for the treatment of diabetic complications clinically.

CONCLUSION

Sorbinil is an effective ARI, which could play therapeutic role in treating diabetes and diabetic complications. However, advanced clinical trials are required for sorbinil so that it could be applied with the lowest efficacious dose in humans.

摘要

背景

醛糖还原酶（AR）参与糖尿病的发病机制，糖尿病是全球公共卫生面临的主要威胁之一。

目的

在这篇综述文章中，我们讨论了AR抑制剂（ARI）索比尼尔在预防糖尿病并发症中的作用。

结果

AR通过多元醇途径产生过量的细胞内超氧化物和其他氧化应激介质，从而在糖尿病中发挥作用。因此，抑制AR活性可能是管理糖尿病并发症的一种潜在方法。实验证据表明，索比尼尔可以降低AR活性并抑制多元醇途径。体外和动物模型研究均报道了索比尼尔在控制糖尿病进展方面的疗效。此外，已发现索比尼尔在人类使用中比其他ARI相对更安全。但是，其在临床上治疗糖尿病并发症仍处于早期试验阶段。