Fahmi Alaa N A, Shehatou George S G, Shebl Abdelhadi M, Salem Hatem A
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, Egypt.
Department of Pathology, Faculty of Medicine, Mansoura University, Mansoura, Egypt.
Naunyn Schmiedebergs Arch Pharmacol. 2016 Aug;389(8):819-30. doi: 10.1007/s00210-016-1258-y. Epub 2016 May 23.
The aim of the present study was to investigate possible renoprotective effects of febuxostat, a highly potent xanthine oxidase inhibitor, against cisplatin (CIS)-induced acute kidney injury in rats. Male Sprague Dawley rats were randomly assigned into four groups of six rats each, as follows: normal control; CIS, received a single intraperitoneal injection of CIS (7.5 mg/kg); [febuxostat 10 + CIS] and [febuxostat 15 + CIS], received febuxostat (10 and 15 mg/kg/day, respectively, orally) for 14 days, starting 7 days before CIS injection. At the end of experiment, 24-h urine output was collected and serum was separated for biochemical assessments. Kidney tissue homogenate was prepared for determination of oxidative stress-related parameters, nitric oxide (NO), and tumor necrosis factor-α (TNF-α). Moreover, histological alterations of kidney tissues were evaluated. Serum creatinine, blood urea, and urinary total protein were significantly elevated, while serum albumin and creatinine clearance were significantly reduced, in CIS-intoxicated rats, indicating depressed renal function. CIS administration also elicited renal oxidative stress, evidenced by increased malondialdehyde content and depleted levels of reduced glutathione and superoxide dismutase activity. Moreover, enhancement of renal levels of the pro-inflammatory TNF-α indicated renal inflammation. CIS-administered rats also showed increased serum lactate dehydrogenase activity and reduced renal NO bioavailability. Febuxostat dose-dependently improved or restored these changes to near-normal (e.g., mean ± SD of serum creatinine levels in control, CIS, [febuxostat 10 + CIS] and [febuxostat 15 + CIS] groups were 0.78 ± 0.19, 3.28 ± 2.0 (P < 0.01 versus control group), 1.03 ± 0.36 (P < 0.01 versus CIS group), and 0.93 ± 0.21 (P < 0.01 versus CIS group) mg/dl, respectively, and blood urea levels for the different groups were 36.80 ± 4.36, 236.10 ± 89.19 (P < 0.0001 versus control group), 114.50 ± 78.63 (P < 0.05 versus CIS group), and 60.91 ± 14.30 (P < 0.001 versus CIS group) mg/dl, respectively). Histological analysis of renal tissues also demonstrated that febuxostat offered a dose-dependent renoprotection. The present study suggests that antioxidant, anti-inflammatory, and cytoprotective mechanisms potentially mediate the renoprotective effects of febuxostat in CIS-administered rats, presenting febuxostat as a promising combinatorial strategy for cancer patients undergoing CIS chemotherapy.
本研究的目的是探讨高效黄嘌呤氧化酶抑制剂非布司他对顺铂(CIS)诱导的大鼠急性肾损伤可能的肾脏保护作用。雄性Sprague Dawley大鼠被随机分为四组,每组六只,如下:正常对照组;CIS组,接受单次腹腔注射CIS(7.5 mg/kg);[非布司他10 + CIS]组和[非布司他15 + CIS]组,在注射CIS前7天开始,分别口服非布司他(10和15 mg/kg/天),持续14天。实验结束时,收集24小时尿量并分离血清进行生化评估。制备肾组织匀浆以测定氧化应激相关参数、一氧化氮(NO)和肿瘤坏死因子-α(TNF-α)。此外,评估肾组织的组织学改变。在CIS中毒的大鼠中,血清肌酐、血尿素和尿总蛋白显著升高,而血清白蛋白和肌酐清除率显著降低,表明肾功能受损。给予CIS还引发了肾脏氧化应激,表现为丙二醛含量增加以及还原型谷胱甘肽水平降低和超氧化物歧化酶活性下降。此外,促炎细胞因子TNF-α肾水平的升高表明肾脏存在炎症。给予CIS的大鼠还表现出血清乳酸脱氢酶活性增加和肾脏NO生物利用度降低。非布司他剂量依赖性地改善或使这些变化恢复至接近正常水平(例如,对照组、CIS组、[非布司他10 + CIS]组和[非布司他15 + CIS]组血清肌酐水平的平均值±标准差分别为0.78±0.19、3.28±2.0(与对照组相比,P < 0.01)、1.03±0.36(与CIS组相比,P < 0.01)和0.93±0.21(与CIS组相比,P < 0.01)mg/dl,不同组的血尿素水平分别为36.80±4.36、236.10±89.19(与对照组相比,P < 0.0001)、114.50±78.63(与CIS组相比,P < 0.05)和60.91±14.30(与CIS组相比,P < 0.001)mg/dl)。肾组织的组织学分析也表明非布司他具有剂量依赖性的肾脏保护作用。本研究表明,抗氧化、抗炎和细胞保护机制可能介导了非布司他对给予CIS大鼠的肾脏保护作用,这表明非布司他是接受CIS化疗的癌症患者一种有前景的联合治疗策略。