Department of Pharmacology, School of Pharmaceutical Sciences, Jilin University, Changchun, PR China.
Department of Pharmacology, School of Pharmaceutical Sciences, Jilin University, Changchun, PR China.
J Pharmacol Sci. 2018 Sep;138(1):31-37. doi: 10.1016/j.jphs.2018.08.008. Epub 2018 Aug 26.
Parkinson's disease (PD) is characterized by the selective death of dopaminergic neurons. To avoid inconvenience of frequent administration caused by short half life and recurrence of symptoms such as tremor and bradykinesia incurred by drug elimination, a novel long-acting pramipexole transdermal patch has been made. In the present study, we evaluated the neuroprotective effects and underlying mechanisms of pramipexole patch (PPX patch) in a subacute PD mouse model induced by 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). The results showed that PPX patch treatment improved dyskinesia. MPTP-induced reduction of DA as well as its metabolites DOPAC and HVA in the striatum were prevented by PPX patch in a dose-dependent manner. PPX patch also restored the activity of antioxidant enzymes including SOD, GSH-Px and CAT in the striatum while reduced the content of MDA. Furthermore, PPX patch upregulated Nrf2/HO-1 expression. The protective effects of PPX patch was also associated with downregulation of the Bax/Bcl-2 ratio and Apaf-1, inhibition of cytochrome c release and inactivation of caspase-9 and caspase-3. In conclusion, our studies demonstrated that the long-acting pramipexole patch exerts its neuroprotective effects, at least in part, by inhibiting oxidative stress and mitochondrial apoptosis pathway and holds promise as a candidate drug.
帕金森病(PD)的特征是多巴胺能神经元的选择性死亡。为了避免因半衰期短和药物消除引起的震颤和运动迟缓等症状复发而导致的频繁给药带来的不便,一种新型的长效普拉克索透皮贴剂已经问世。在本研究中,我们评估了普拉克索贴剂(PPX 贴剂)在 1-甲基-4-苯基-1,2,3,6-四氢吡啶(MPTP)诱导的亚急性 PD 小鼠模型中的神经保护作用及其潜在机制。结果表明,PPX 贴剂治疗可改善运动障碍。PPX 贴剂以剂量依赖性方式防止 MPTP 诱导的纹状体中 DA 及其代谢物 DOPAC 和 HVA 的减少。PPX 贴剂还恢复了纹状体中抗氧化酶的活性,包括 SOD、GSH-Px 和 CAT,同时降低了 MDA 的含量。此外,PPX 贴剂上调了 Nrf2/HO-1 的表达。PPX 贴剂的保护作用还与 Bax/Bcl-2 比值和 Apaf-1 的下调、细胞色素 c 释放的抑制以及 caspase-9 和 caspase-3 的失活有关。总之,我们的研究表明,长效普拉克索贴剂通过抑制氧化应激和线粒体凋亡途径发挥其神经保护作用,有望成为一种候选药物。