Kanchan Divya M, Kale Smita S, Somani Gauresh S, Kaikini Aakruti A, Sathaye Sadhana
Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Mumbai, Maharashtra, India.
J Pharm Bioallied Sci. 2016 Oct-Dec;8(4):277-283. doi: 10.4103/0975-7406.199348.
Overactivation of aldose reductase (AR) enzyme has been implicated in the development of various diabetic complications. In the present study, the inhibitory effect of thymol was investigated on AR enzyme and its anti-cataract activity was also examined on isolated goat lens.
Various concentrations of thymol were incubated with AR enzyme prepared from isolated goat lens. Molecular docking studies were carried out using Schrodinger software to verify the binding of thymol with AR as well as to understand their binding pattern. Further, thymol was evaluated for its anti-cataract activity in high-glucose-induced cataract in isolated goat lens . Quercetin was maintained as standard (positive control) throughout the study.
Thymol showed potent inhibitory activity against goat lens AR enzyme with an IC value of 0.65 μg/ml. Docking studies revealed that thymol binds with AR in similar binding pattern as that of quercetin. The high-glucose-induced cataract in isolated goat lens was also improved by thymol treatment. Thymol was also able to significantly ( < 0.001) reduce the oxidative stress associated with cataract.
The results suggest that thymol may be a potential therapeutic approach in the prevention of diabetic complications through its AR inhibitory and antioxidant activities.
醛糖还原酶(AR)的过度激活与多种糖尿病并发症的发生有关。在本研究中,研究了百里香酚对AR酶的抑制作用,并在离体山羊晶状体上检测了其抗白内障活性。
将不同浓度的百里香酚与从离体山羊晶状体中制备的AR酶一起孵育。使用薛定谔软件进行分子对接研究,以验证百里香酚与AR的结合,并了解它们的结合模式。此外,在离体山羊晶状体的高糖诱导性白内障中评估了百里香酚的抗白内障活性。在整个研究过程中,槲皮素作为标准品(阳性对照)。
百里香酚对山羊晶状体AR酶显示出强效抑制活性,IC值为0.65μg/ml。对接研究表明,百里香酚与AR的结合模式与槲皮素相似。百里香酚处理也改善了离体山羊晶状体中高糖诱导的白内障。百里香酚还能够显著(<0.001)降低与白内障相关的氧化应激。
结果表明,百里香酚可能通过其AR抑制和抗氧化活性成为预防糖尿病并发症的潜在治疗方法。