University College of Pharmaceutical Sciences, Kakatiya University, Warangal, AP, 506009, India.
Phytother Res. 2014 Mar;28(3):317-33. doi: 10.1002/ptr.5000. Epub 2013 May 15.
Diabetic complications are attributed to hyperglycaemic condition which is in turn associated with the polyol pathway and advanced glycation end products. Aldose reductase (AR) is the principal enzyme of polyol pathway which plays a vital role in the development of diabetic complications. AR inhibitory activity can be screened by both in vitro and in vivo methods. In vitro assays for AR enzyme are further classified on the basis of the source of enzyme such as rat lens, rat kidney, cataracted human eye lens, bovine eyes and human recombinant AR enzymes, whereas the in vivo model is based on the determination of lens galactitol levels. A number of synthetic AR inhibitors (ARIs) including tolrestat and sorbinil have been developed, but all of these suffer from drawbacks such as poor permeation and safety issues. Therefore, pharmaceutical companies and many researchers have been carrying out research to find new, potent and safe ARIs from natural sources. Thus, many naturally occurring compounds have been reported to have AR inhibitory activity. The present review attempts to highlight phytochemicals and plant extracts with potential AR inhibitory activity. It also summarizes the classes of compounds which have proven AR inhibitory activity. Phytochemicals such as quercetin, kaempferol and ellagic acid are found to be the most promising ARIs. The exhaustive literature presented in this article clearly indicates the role of plant extracts and phytochemicals as potential ARIs.
糖尿病并发症归因于高血糖状态，而高血糖状态又与多元醇途径和糖基化终产物有关。醛糖还原酶（AR）是多元醇途径的主要酶，在糖尿病并发症的发展中起着至关重要的作用。可以通过体外和体内方法来筛选 AR 的抑制活性。用于 AR 酶的体外测定法还可以根据酶的来源进一步分类，例如大鼠晶状体、大鼠肾脏、白内障人眼晶状体、牛眼和人重组 AR 酶，而体内模型则基于晶状体半乳糖醇水平的测定。已经开发了许多合成的 AR 抑制剂（ARIs），包括托瑞司他和 sorbinil，但所有这些都存在渗透不良和安全问题等缺点。因此，制药公司和许多研究人员一直在进行研究，以从天然来源中寻找新的、有效和安全的 ARIs。因此，已经有许多天然存在的化合物被报道具有 AR 抑制活性。本综述试图强调具有潜在 AR 抑制活性的植物化学物质和植物提取物。它还总结了已被证明具有 AR 抑制活性的化合物类别。槲皮素、山奈酚和鞣花酸等植物化学物质被认为是最有前途的 ARIs。本文中呈现的详尽文献清楚地表明了植物提取物和植物化学物质作为潜在 ARIs 的作用。
