Institute of Basic Medical Sciences, National Cheng Kung University, Tainan, Taiwan; Cardiovascular Research Center, National Cheng Kung University, Tainan, Taiwan.
Department of Medical Laboratory Science and Biotechnology, National Cheng Kung University, Tainan, Taiwan; Research Center of Infectious Disease and Signaling, National Cheng Kung University, Tainan, Taiwan.
Am J Pathol. 2014 Feb;184(2):442-53. doi: 10.1016/j.ajpath.2013.10.020. Epub 2013 Nov 26.
Much concern has arisen regarding critical adverse effects of thiazolidinediones (TZDs), including rosiglitazone and pioglitazone, on cardiac tissue. Although TZD-induced cardiac hypertrophy (CH) has been attributed to an increase in plasma volume or a change in cardiac nutrient preference, causative roles have not been established. To test the hypothesis that volume expansion directly mediates rosiglitazone-induced CH, mice were fed a high-fat diet with rosiglitazone, and cardiac and metabolic consequences were examined. Rosiglitazone treatment induced volume expansion and CH in wild-type and PPARγ heterozygous knockout (Pparg(+/-)) mice, but not in mice defective for ligand binding (Pparg(P465L/+)). Cotreatment with the diuretic furosemide in wild-type mice attenuated rosiglitazone-induced CH, hypertrophic gene reprogramming, cardiomyocyte apoptosis, hypertrophy-related signal activation, and left ventricular dysfunction. Similar changes were observed in mice treated with pioglitazone. The diuretics spironolactone and trichlormethiazide, but not amiloride, attenuated rosiglitazone effects on volume expansion and CH. Interestingly, expression of glucose and lipid metabolism genes in the heart was altered by rosiglitazone, but these changes were not attenuated by furosemide cotreatment. Importantly, rosiglitazone-mediated whole-body metabolic improvements were not affected by furosemide cotreatment. We conclude that releasing plasma volume reduces adverse effects of TZD-induced volume expansion and cardiac events without compromising TZD actions in metabolic switch in the heart and whole-body insulin sensitivity.
人们对噻唑烷二酮类药物(TZDs),包括罗格列酮和吡格列酮,对心脏组织的严重不良影响产生了极大的关注。虽然 TZD 引起的心肌肥厚(CH)归因于血浆体积增加或心脏营养偏好改变,但尚未确定其因果关系。为了检验直接介导罗格列酮诱导的 CH 的容积扩张假说,我们用高脂肪饮食喂养小鼠,并检查心脏和代谢后果。罗格列酮治疗诱导野生型和 PPARγ 杂合子敲除(Pparg(+/-))小鼠的容积扩张和 CH,但不诱导配体结合缺陷(Pparg(P465L/+))的小鼠发生 CH。在野生型小鼠中,用利尿剂呋塞米共同治疗可减轻罗格列酮诱导的 CH、肥厚基因重编程、心肌细胞凋亡、肥大相关信号激活和左心室功能障碍。用吡格列酮治疗的小鼠也观察到类似的变化。利尿剂螺内酯和三氯甲噻嗪,但不是阿米洛利,可减轻罗格列酮对容积扩张和 CH 的作用。有趣的是,罗格列酮改变了心脏中葡萄糖和脂质代谢基因的表达,但这些变化不受呋塞米共同治疗的影响。重要的是,罗格列酮介导的全身代谢改善不受呋塞米共同治疗的影响。我们得出结论,释放血浆容量可减轻 TZD 诱导的容积扩张和心脏事件的不良影响,而不影响 TZD 在心脏和全身胰岛素敏感性的代谢转换中的作用。