Bender Shawn B, DeMarco Vincent G, Padilla Jaume, Jenkins Nathan T, Habibi Javad, Garro Mona, Pulakat Lakshmi, Aroor Annayya R, Jaffe Iris Z, Sowers James R
From the Research Service, Harry S. Truman Memorial Veterans' Hospital, Columbia, MO (S.B.B., V.G.D.M., J.H., M.G., L.P., A.R.A., J.R.S.); Department of Biomedical Sciences (S.B.B.), Dalton Cardiovascular Research Center (S.B.B., J.P., J.R.S.), and Department of Nutrition and Exercise Physiology (J.P.), University of Missouri, Columbia; Division of Endocrinology, Diabetes and Metabolism (V.G.D.M., J.H., M.G., A.R.A., J.R.S.) and Division of Cardiovascular Medicine (L.P.), Department of Medicine, Department of Medical Pharmacology and Physiology (V.G.D.M., L.P., J.R.S.), and Department of Child Health (J.P.), University of Missouri School of Medicine, Columbia; Department of Kinesiology, University of Georgia, Athens, GA (N.T.J.); and Molecular Cardiology Research Institute, Tufts Medical Center, Boston, MA (I.Z.J.).
Hypertension. 2015 May;65(5):1082-8. doi: 10.1161/HYPERTENSIONAHA.114.04912. Epub 2015 Feb 23.
Patients with obesity and diabetes mellitus exhibit a high prevalence of cardiac diastolic dysfunction (DD), an independent predictor of cardiovascular events for which no evidence-based treatment exists. In light of renin-angiotensin-aldosterone system activation in obesity and the cardioprotective action of mineralocorticoid receptor (MR) antagonists in systolic heart failure, we examined the hypothesis that MR blockade with a blood pressure-independent low-dose spironolactone (LSp) would treat obesity-associated DD in the Zucker obese (ZO) rat. Treatment of ZO rats exhibiting established DD with LSp normalized cardiac diastolic function, assessed by echocardiography. This was associated with reduced cardiac fibrosis, but not reduced hypertrophy, and restoration of endothelium-dependent vasodilation of isolated coronary arterioles via a nitric oxide-independent mechanism. Further mechanistic studies revealed that LSp reduced cardiac oxidative stress and improved endothelial insulin signaling, with no change in arteriolar stiffness. Infusion of Sprague-Dawley rats with the MR agonist aldosterone reproduced the DD noted in ZO rats. In addition, improved cardiac function in ZO-LSp rats was associated with attenuated systemic and adipose inflammation and an anti-inflammatory shift in cardiac immune cell mRNAs. Specifically, LSp increased cardiac markers of alternatively activated macrophages and regulatory T cells. ZO-LSp rats had unchanged blood pressure, serum potassium, systemic insulin sensitivity, or obesity-associated kidney injury, assessed by proteinuria. Taken together, these data demonstrate that MR antagonism effectively treats established obesity-related DD via blood pressure-independent mechanisms. These findings help identify a particular population with DD that might benefit from MR antagonist therapy, specifically patients with obesity and insulin resistance.
肥胖和糖尿病患者心脏舒张功能障碍(DD)的患病率很高,这是一种心血管事件的独立预测因素,目前尚无循证治疗方法。鉴于肥胖中肾素-血管紧张素-醛固酮系统的激活以及盐皮质激素受体(MR)拮抗剂在收缩性心力衰竭中的心脏保护作用,我们检验了以下假设:使用与血压无关的低剂量螺内酯(LSp)进行MR阻断可治疗Zucker肥胖(ZO)大鼠的肥胖相关DD。用LSp治疗已出现DD的ZO大鼠,通过超声心动图评估,其心脏舒张功能恢复正常。这与心脏纤维化减轻有关,但与心肌肥厚减轻无关,并且通过一种不依赖一氧化氮的机制恢复了离体冠状动脉小动脉的内皮依赖性血管舒张。进一步的机制研究表明,LSp降低了心脏氧化应激并改善了内皮胰岛素信号传导,而小动脉僵硬度没有变化。给Sprague-Dawley大鼠输注MR激动剂醛固酮可重现ZO大鼠中观察到的DD。此外,ZO-LSp大鼠心脏功能的改善与全身和脂肪炎症减轻以及心脏免疫细胞mRNA的抗炎转变有关。具体而言,LSp增加了交替激活的巨噬细胞和调节性T细胞的心脏标志物。通过蛋白尿评估,ZO-LSp大鼠的血压、血清钾、全身胰岛素敏感性或肥胖相关肾损伤均未改变。综上所述,这些数据表明,MR拮抗作用通过与血压无关的机制有效治疗已确立的肥胖相关DD。这些发现有助于确定可能从MR拮抗剂治疗中获益的特定DD人群,特别是肥胖和胰岛素抵抗患者。