Pharmacological Sciences Research Lab, Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, Pakistan.
Department of Pharmacy, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad, Pakistan.
Inflammopharmacology. 2023 Aug;31(4):1977-1992. doi: 10.1007/s10787-023-01225-w. Epub 2023 May 5.
Paclitaxel (PTX) is an anti-microtubule agent, used for the treatment of various types of cancers; however, it produces painful neuropathy which limits its use. Many neuroprotective agents have been introduced to mitigate PTX-induced neuropathic pain (PINP), but they pose many adverse effects. The purpose of this study was to evaluate the pharmacological characteristics of soy isoflavone, and daidzein (DZ) in attenuating PINP. At the beginning of the investigation, the effect of DZ was confirmed through behavioral analysis, as it reduced pain hypersensitivity. Moreover, changes in the histological parameters were reversed by DZ administration along with vascular permeability. PTX administration upregulated transient receptor potential vanilloid 1 (TRPV1) channels and purinergic receptors (P2Y), contributing to hyperalgesia; but administration of DZ downregulated the TRPV1 and P2Y, thus reducing hyperalgesia. DZ increased nuclear factor erythroid-2-related factor 2 (Nrf2) and heme oxygenase-1 (HO-1), playing a pivotal role in the activation of the antioxidant pathway. DZ also decreased neuronal apoptosis by decreasing caspase-3 and Bcl2-associated X-protein (Bax), while simultaneously, increasing Bcl-2. PTX administration produced severe DNA damage, which was mitigated by DZ. Similarly, DZ administration resulted in inhibition of neuroinflammation by increasing antioxidant enzymes and reducing oxidative stress markers. PTX caused increased in production of pro-inflammatory mediators such as the cytokines production, while DZ inhibited the pro-inflammatory mediators. Additionally, in silico pharmacokinetic and toxicodynamic study of DZ was also conducted. In summary, DZ demonstrated significant neuroprotective activity against PTX induced neuropathic pain.
紫杉醇(PTX)是一种抗微管药物,用于治疗各种类型的癌症;然而,它会产生疼痛性神经病,限制了它的使用。已经引入了许多神经保护剂来减轻紫杉醇诱导的神经性疼痛(PINP),但它们存在许多不良反应。本研究旨在评估大豆异黄酮和大豆苷元(DZ)在减轻 PINP 中的药理特性。在研究开始时,通过行为分析证实了 DZ 的作用,因为它减轻了疼痛敏感性。此外,DZ 给药还可逆转组织学参数的变化,同时降低血管通透性。PTX 给药上调瞬时受体电位香草酸 1(TRPV1)通道和嘌呤能受体(P2Y),导致痛觉过敏;但 DZ 给药下调 TRPV1 和 P2Y,从而减轻痛觉过敏。DZ 增加核因子红细胞 2 相关因子 2(Nrf2)和血红素加氧酶-1(HO-1),在激活抗氧化途径中发挥关键作用。DZ 还通过降低半胱天冬酶-3 和 Bcl2 相关 X 蛋白(Bax)同时增加 Bcl-2 来减少神经元凋亡。PTX 给药产生严重的 DNA 损伤,DZ 减轻了这种损伤。同样,DZ 给药通过增加抗氧化酶和降低氧化应激标志物来抑制神经炎症。PTX 导致促炎介质如细胞因子的产生增加,而 DZ 抑制促炎介质。此外,还对 DZ 的计算机药代动力学和毒代动力学进行了研究。总之,DZ 对 PTX 诱导的神经性疼痛表现出显著的神经保护活性。