Department of Pharmacology, Faculty of Medicine, Zagazig University, Zagazig, Egypt.
Naunyn Schmiedebergs Arch Pharmacol. 2017 Nov;390(11):1145-1153. doi: 10.1007/s00210-017-1414-z. Epub 2017 Aug 5.
Doxorubicin (Dox)-induced cardiotoxicity constitutes the major adverse effect that limited its use. We investigated the possible protective effects of liraglutide on Dox-induced cardiotoxicity in rats. Rats were divided into the following groups: control group rats received normal saline [1 ml/kg, intraperitoneal (i.p.)]; doxorubicin group rats received doxorubicin (1.25 mg/kg, i.p.), four times per week for 4 weeks; and liraglutide group rats received doxorubicin (1.25 mg/kg, i.p.) four times per week for 4 weeks then received liraglutide (100 μg/kg, i.p) daily for 4 weeks. At the end of the study, animals were sacrificed and serum creatine kinase-MB (CK-MB) and troponin I levels were determined. Malondialdehyde (MDA), superoxide dismutase (SOD), tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and caspase-3 levels of the heart were determined. Cardiac AMPK, phosphorylated-Akt, tissue growth factor-β1 (TGF-β1), and GSK3-β levels of the heart were determined. Hematoxylin and eosin (H&E) stained sections form the heart were examined as well as immunohistochemical sections for detection of Bcl-2 expression. Dox treatment increased serum level of troponin I and CK-MB while decreased SOD activity, decreased AMPK, and p-Akt cardiac levels with increased in MDA, IL-6, TNF-α,GSK-3b, TGFB1, and caspase-3 levels in the heart with inflammation and necrosis in cardiac histopathology with decreased Bcl-2. Treatment with liraglutide decreased troponin I and CK-MB while increased SOD activity, AMPK, p-Akt with decrements in MDA, IL-6, TNF-α, GSK-3β, TGF-β1, and caspase-3 levels with attenuation of inflammation and necrosis while increased Bcl-2 expression. Liraglutide may thus represent a new clinical tool for the treatment of Dox-induced cardiotoxicity.
多柔比星(Dox)诱导的心脏毒性是其主要的不良反应,限制了其应用。我们研究了利拉鲁肽对大鼠多柔比星心脏毒性的可能保护作用。大鼠分为以下几组:对照组大鼠给予生理盐水[1ml/kg,腹腔内(i.p.)];多柔比星组大鼠给予多柔比星(1.25mg/kg,i.p.),每周 4 次,共 4 周;利拉鲁肽组大鼠给予多柔比星(1.25mg/kg,i.p.)每周 4 次,共 4 周,然后给予利拉鲁肽(100μg/kg,i.p.)每日 1 次,共 4 周。研究结束时,处死动物,测定血清肌酸激酶同工酶(CK-MB)和肌钙蛋白 I 水平。测定心脏丙二醛(MDA)、超氧化物歧化酶(SOD)、肿瘤坏死因子-α(TNF-α)、白细胞介素-6(IL-6)和半胱氨酸天冬氨酸蛋白酶-3(caspase-3)水平。测定心脏 AMPK、磷酸化-Akt、组织生长因子-β1(TGF-β1)和 GSK3-β水平。心脏苏木精和伊红(H&E)染色切片以及免疫组织化学切片检测 Bcl-2 表达。多柔比星治疗增加了血清肌钙蛋白 I 和 CK-MB 水平,降低了 SOD 活性,降低了心脏 AMPK 和磷酸化-Akt 水平,增加了 MDA、IL-6、TNF-α、GSK-3b、TGFB1 和 caspase-3 水平,导致心脏组织病理学中的炎症和坏死,Bcl-2 减少。利拉鲁肽治疗降低了肌钙蛋白 I 和 CK-MB 水平,增加了 SOD 活性,AMPK 和磷酸化-Akt 水平,降低了 MDA、IL-6、TNF-α、GSK-3β、TGF-β1 和 caspase-3 水平,减轻了炎症和坏死,增加了 Bcl-2 表达。因此,利拉鲁肽可能成为治疗多柔比星心脏毒性的一种新的临床工具。