Abdelhady Rasha, Arab Hany H, Fakhr Eldeen Rasha R, Shalaby Heba Nasr, Nawwar Dalia A, Elhemely Mai Abdallah, Sayed Rabab H
Pharmacology and Toxicology Department, Faculty of Pharmacy, Fayoum University, Fayoum, Egypt.
Pharmacology and Toxicology Department, Faculty of Pharmacy, Egyptian Chinese University, Cairo, Egypt.
Arch Pharm (Weinheim). 2025 Apr;358(4):e3127. doi: 10.1002/ardp.202500023.
Tacrolimus (Tac) is an immunosuppressive drug used to reduce the risk of allograft rejection; however, it can induce renal injury. High mobility group box 1 (HMGB-1) protein, which induces inflammation through the aberrant stimulation of the Toll-like receptor 4 (TLR4)/myeloid differentiation primary response protein (MyD88)/nuclear factor kappa B (NF-κB) trajectory, could represent a molecular target for alleviating Tac-induced renal damage. The present study aimed to investigate the potential protective role of the GLP-1 agonist, dulaglutide (Dula), against Tac-induced nephrotoxicity in rats. Rats were administered Tac (5 mg/kg/day) and vehicle or Dula (0.2 mg/kg once a week) for 14 days. Treatment with Dula reduced serum creatinine plus blood urea nitrogen and attenuated Tac-induced renal histopathological changes. Dula treatment also hampered renal inflammation and restored redox homeostasis, as indicated by remarkably reduced tumor necrosis factor-alpha (TNF-α), interleukin-1β (IL-1β), malondialdehyde (MDA), and NADPH oxidase 1 levels alongside marked replenishment in reduced glutathione (GSH) content. These effects were mediated through the upregulation of miR-22 expression and the consequent inhibition of the HMGB-1/TLR4/MyD88/NF-κB trajectory. Collectively, Dula has been demonstrated to protect rats against Tac-induced nephrotoxicity by reducing inflammation, restoring redox homeostasis, and modulation of the miR-22/HMGB-1/TLR4/MyD88/NF-κB trajectory. Dula may be beneficial clinically in preventing Tac-induced renal injury.
他克莫司(Tac)是一种免疫抑制药物,用于降低同种异体移植排斥反应的风险;然而,它会诱发肾损伤。高迁移率族蛋白盒1(HMGB - 1)蛋白通过异常刺激Toll样受体4(TLR4)/髓样分化初级反应蛋白(MyD88)/核因子κB(NF - κB)信号通路诱导炎症,可能是减轻他克莫司诱导的肾损伤的分子靶点。本研究旨在探讨胰高血糖素样肽 - 1(GLP - 1)激动剂度拉糖肽(Dula)对大鼠他克莫司诱导的肾毒性的潜在保护作用。给大鼠连续14天给予他克莫司(5mg/kg/天)及溶剂或度拉糖肽(0.2mg/kg,每周一次)。度拉糖肽治疗降低了血清肌酐和血尿素氮水平,并减轻了他克莫司诱导的肾脏组织病理学变化。度拉糖肽治疗还抑制了肾脏炎症并恢复了氧化还原稳态,表现为肿瘤坏死因子 - α(TNF - α)、白细胞介素 - 1β(IL - 1β)、丙二醛(MDA)和NADPH氧化酶1水平显著降低,同时还原型谷胱甘肽(GSH)含量明显补充。这些作用是通过上调miR - 22表达并随后抑制HMGB - 1/TLR4/MyD88/NF - κB信号通路介导的。总体而言,已证明度拉糖肽可通过减轻炎症、恢复氧化还原稳态以及调节miR - 22/HMGB - 1/TLR4/MyD88/NF - κB信号通路来保护大鼠免受他克莫司诱导的肾毒性。度拉糖肽在临床上预防他克莫司诱导的肾损伤可能有益。