Departamento de Farmacología, Cinvestav-IPN, Apdo. Postal 14-740, México 07360, D.F. México.
Can J Physiol Pharmacol. 2012 Nov;90(11):1469-78. doi: 10.1139/y2012-125. Epub 2012 Nov 12.
Allopurinol is an inhibitor of xanthine oxidase (XO), and XO is an enzyme that generates great amounts of reactive oxygen species. The aim of this work was to evaluate the efficacy of allopurinol to prevent experimental cirrhosis. Fibrosis and cirrhosis were induced by common bile duct ligation (BDL) for 4 weeks in rats. Animals were divided into 4 groups: sham-operated rats (SHAM); BDL group; BDL plus allopurinol (100 mg·kg⁻¹, p.o.), and SHAM plus allopurinol treatment. Alanine aminotransferase, γ-glutamyl transpeptidase, and alkaline phosphatase were increased in BDL rats but were preserved normal by allopurinol. XO activity was prevented by allopurinol; however, lipophilic and hydrophilic oxidative stress was not prevented by the drug. Allopurinol partially suppresses nuclear factor-κB (NF-κB) nuclear translocation and transforming growth factor-β (TGF-β) expression, and increased the active form of matrix metalloproteinase-13 (MMP-13). Moreover, collagen production induced by BDL was partially but significantly reduced by allopurinol. These findings suggest that allopurinol possesses a hepatoprotective effect probably by modulating proteins such as NF-κB, TGF-β, and MMP-13, helping to protect against liver damage induced by chronic cholestasis and a mechanism independent of oxidative stress.
别嘌醇是黄嘌呤氧化酶 (XO) 的抑制剂,而 XO 是一种产生大量活性氧的酶。本工作旨在评估别嘌醇预防实验性肝硬化的疗效。通过胆总管结扎 (BDL) 在大鼠中诱导 4 周的纤维化和肝硬化。动物分为 4 组:假手术大鼠 (SHAM);BDL 组;BDL 加别嘌醇(100mg·kg⁻¹,po),以及 SHAM 加别嘌醇治疗。BDL 大鼠丙氨酸氨基转移酶、γ-谷氨酰转肽酶和碱性磷酸酶升高,但别嘌醇可使其保持正常。别嘌醇可预防 XO 活性;然而,亲脂性和亲水性氧化应激并未被该药物预防。别嘌醇部分抑制核因子-κB (NF-κB) 核易位和转化生长因子-β (TGF-β) 的表达,并增加基质金属蛋白酶-13 (MMP-13) 的活性形式。此外,BDL 诱导的胶原产生被别嘌醇部分但显著减少。这些发现表明,别嘌醇具有肝保护作用,可能通过调节 NF-κB、TGF-β 和 MMP-13 等蛋白来帮助防止慢性胆汁淤积引起的肝损伤,其机制与氧化应激无关。