Aldose reductase (AR) is an enzyme that catalyzes the rate limiting step of the polyol pathway of glucose metabolism. Besides reducing glucose to sorbitol, it reduces a number of lipid peroxidation derived aldehydes and their glutathione conjugates. Recent studies suggest that apart from its involvement in diabetic complications, it also has a pivotal role in inflammatory diseases such as atherosclerosis, sepsis, asthma, uveitis, and ovarian cancer. Furthermore, an excess of AR is found in different human cancers, such as liver, colon, breast, and cervical cancer. AR inhibitors have undergone up to phase-III clinical trials for diabetic complications. They are also reported as safe anti-inflammatory drugs. Therefore, future use of AR inhibitors in down-regulating major multi-diseases and inflammatory pathologies such as cancer and cardiovascular diseases could relieve some of the major health concerns worldwide.