Department of Pharmacology, B. K. Mody Government Pharmacy College, Rajkot, Gujarat, India.
Indian J Pharmacol. 2022 Jan-Feb;54(1):46-50. doi: 10.4103/ijp.IJP_384_20.
The present study investigates the antiParkinsonian activity of dipeptidyl peptidase-4 (DPP-IV) inhibitor, linagliptin. The experimental Parkinson's disease (PD) was induced by administration of rotenone at a dose of 1.5 mg/kg at alternate day subcutaneously for 21 days. Standard drug (levodopa-200 mg/kg and carbidopa-50 mg/kg) and treatment drug (linagliptin-5 mg/kg, 10 mg/kg, and 20mg/kg) were administered orally daily 1 h before rotenone administration. In a rat rotenone model, linagliptin improved muscle coordination, motor performance, and corrected akinesia. Pretreatment with linagliptin showed significant higher levels of superoxide dismutase, catalase, and glutathione in brain homogenate of animals. Linagliptin significantly elevated the levels of striatal DA and active glucagon-like peptide 1 in brain homogenate of animals. Furthermore, linagliptin amended alterations induced by rotenone in the thiobarbituric acid reactive substances and inflammatory marker such as tumor necrosis factor-α level. The results of the present study indicate the neuroprotective potential of linagliptin for the management of PD might be due to remarkable improvement in motor functions, antioxidant, anti-inflammatory, anti-apoptotic, and neuroprotective mechanisms.
本研究探讨了二肽基肽酶-4（DPP-4）抑制剂利拉利汀的抗帕金森病活性。实验性帕金森病（PD）通过皮下每隔一天给予鱼藤酮 1.5mg/kg 21 天诱导。标准药物（左旋多巴 200mg/kg 和卡比多巴 50mg/kg）和治疗药物（利拉利汀 5mg/kg、10mg/kg 和 20mg/kg）在给予鱼藤酮前 1 小时口服给予。在大鼠鱼藤酮模型中，利拉利汀改善了肌肉协调性、运动表现，并纠正了运动不能。预先给予利拉利汀显示动物脑匀浆中超氧化物歧化酶、过氧化氢酶和谷胱甘肽水平显著升高。利拉利汀显著提高了动物脑匀浆中纹状体 DA 和活性胰高血糖素样肽 1 的水平。此外，利拉利汀纠正了鱼藤酮引起的硫代巴比妥酸反应物质和炎症标志物如肿瘤坏死因子-α水平的改变。本研究的结果表明，利拉利汀对 PD 的神经保护潜力可能是由于其在运动功能、抗氧化、抗炎、抗凋亡和神经保护机制方面的显著改善。
