Departamento de Fisiologia e Farmacologia, Universidade Federal de Pernambuco, UFPE, Recife, Brazil.
Departamento de Entomologia, Laboratório de Ultraestrutura, Instituto Aggeu Magalhães-FIOCRUZ, Recife, Brazil.
IUBMB Life. 2020 Aug;72(8):1765-1779. doi: 10.1002/iub.2304. Epub 2020 May 24.
Parkinson's disease (PD) induced by environmental toxins involves a multifactorial cascade of harmful factors, thus motivating the search for therapeutic agents able to act on the greatest number of molecular targets. This study evaluated the efficacy of 50 mg/kg purified anacardic acids (AAs), isolated from cashew nut shell liquid, on multiple steps of oxidative stress and inflammation induced by rotenone in the substantia nigra (SN) and striatum. Adult mice were divided into four groups: Control, rotenone, AAs + rotenone, and AAs alone. Lipoperoxidation, nitric oxide (NO) levels, and reduced glutathione (GSH)/oxidized gluthatione (GSSG) ratio were evaluated. NF-kB-p65, pro-IL-1β, cleaved IL-1β, metalloproteinase-9, Tissue Inhibitory Factor-1 (TIMP-1), tyrosine hydroxylase (TH), and glial fibrillary acidic protein (GFAP) levels were assessed by Western blot. In silico studies were also made using the SwissADME web tool. Rotenone increased lipoperoxidation and NO production and reduced TH levels and GSH/GSSG ratio in both SN and striatum. It also enhanced NF-kB-p65, pro, and cleaved IL-1β, MMP-9, GFAP levels compared to control and AAs groups. The AAs alone reduced pro-IL-1β in the striatum while they augmented TIMP1 and reduced MMP-9 amounts in both regions. AAs reversed rotenone-induced effects on lipoperoxidation, NO production, and GSH/GSSG ratio, as well as increased TH and attenuated pro-IL-1β and MMP-9 levels in both regions, NF-kB-p65 in the SN and GFAP in the striatum. Altogether, the in vivo and in silico analysis reinforced multiple and defined molecular targets of AAs, identifying that they are promising neuroprotective drug candidates for PD, acting against oxidative and inflammatory conditions induced by rotenone.
帕金森病(PD)是由环境毒素引起的,涉及多种有害因素的级联反应,因此激发了寻找能够针对最多数量的分子靶点发挥作用的治疗药物的研究。本研究评估了 50mg/kg 从腰果壳液中分离出的纯化漆酚酸(AAs)对鱼藤酮在黑质(SN)和纹状体中诱导的氧化应激和炎症的多个步骤的疗效。成年小鼠分为四组:对照组、鱼藤酮组、AAs+鱼藤酮组和 AAs 单独组。评估了脂质过氧化、一氧化氮(NO)水平和还原型谷胱甘肽(GSH)/氧化型谷胱甘肽(GSSG)比值。通过 Western blot 评估 NF-kB-p65、前白细胞介素-1β(pro-IL-1β)、切割的白细胞介素-1β(cleaved IL-1β)、金属蛋白酶-9(MMP-9)、组织抑制剂 1(TIMP-1)、酪氨酸羟化酶(TH)和胶质纤维酸性蛋白(GFAP)的水平。还使用 SwissADME 网络工具进行了计算机模拟研究。鱼藤酮增加了 SN 和纹状体中的脂质过氧化和 NO 生成,并降低了 GSH/GSSG 比值、TH 水平。与对照组和 AAs 组相比,它还增强了 NF-kB-p65、前和切割的白细胞介素-1β、MMP-9、GFAP 的水平。AAs 单独减少了纹状体中的 pro-IL-1β,而在两个区域增加了 TIMP1 并减少了 MMP-9 的量。AAs 逆转了鱼藤酮对脂质过氧化、NO 生成和 GSH/GSSG 比值的影响,增加了 TH,并减弱了两个区域的 pro-IL-1β和 MMP-9 水平,SN 中的 NF-kB-p65 和纹状体中的 GFAP。总之,体内和计算机模拟分析强化了 AAs 的多个和明确的分子靶点,确定它们是对抗鱼藤酮诱导的氧化和炎症条件的有希望的神经保护候选药物。