Li Hong-Liang, Liu Chen, de Couto Geoffrey, Ouzounian Maral, Sun Mei, Wang Ai-Bing, Huang Yue, He Cheng-Wei, Shi Yu, Chen Xin, Nghiem Mai P, Liu Youan, Chen Manyin, Dawood Fayez, Fukuoka Masahiro, Maekawa Yuichiro, Zhang Liyong, Leask Andrew, Ghosh Asish K, Kirshenbaum Lorrie A, Liu Peter P
Division of Cardiology, Heart and Stroke/Richard Lewar Centre of Excellence, University Health Network, University of Toronto, Toronto, Ontario, Canada.
J Clin Invest. 2008 Mar;118(3):879-93. doi: 10.1172/JCI32865.
Chromatin remodeling, particularly histone acetylation, plays a critical role in the progression of pathological cardiac hypertrophy and heart failure. We hypothesized that curcumin, a natural polyphenolic compound abundant in the spice turmeric and a known suppressor of histone acetylation, would suppress cardiac hypertrophy through the disruption of p300 histone acetyltransferase-dependent (p300-HAT-dependent) transcriptional activation. We tested this hypothesis using primary cultured rat cardiac myocytes and fibroblasts as well as two well-established mouse models of cardiac hypertrophy. Curcumin blocked phenylephrin-induced (PE-induced) cardiac hypertrophy in vitro in a dose-dependent manner. Furthermore, curcumin both prevented and reversed mouse cardiac hypertrophy induced by aortic banding (AB) and PE infusion, as assessed by heart weight/BW and lung weight/BW ratios, echocardiographic parameters, and gene expression of hypertrophic markers. Further investigation demonstrated that curcumin abrogated histone acetylation, GATA4 acetylation, and DNA-binding activity through blocking p300-HAT activity. Curcumin also blocked AB-induced inflammation and fibrosis through disrupting p300-HAT-dependent signaling pathways. Our results indicate that curcumin has the potential to protect against cardiac hypertrophy, inflammation, and fibrosis through suppression of p300-HAT activity and downstream GATA4, NF-kappaB, and TGF-beta-Smad signaling pathways.
染色质重塑,尤其是组蛋白乙酰化,在病理性心肌肥大和心力衰竭的进展中起关键作用。我们推测,姜黄素是一种在香料姜黄中含量丰富的天然多酚化合物,也是一种已知的组蛋白乙酰化抑制剂,它会通过破坏p300组蛋白乙酰转移酶依赖性(p300-HAT依赖性)转录激活来抑制心肌肥大。我们使用原代培养的大鼠心肌细胞和成纤维细胞以及两种成熟的心肌肥大小鼠模型来验证这一假设。姜黄素在体外以剂量依赖性方式阻断苯肾上腺素诱导(PE诱导)的心肌肥大。此外,通过心脏重量/体重和肺重量/体重比值、超声心动图参数以及肥大标志物的基因表达评估,姜黄素既能预防又能逆转主动脉缩窄(AB)和PE输注诱导的小鼠心肌肥大。进一步研究表明,姜黄素通过阻断p300-HAT活性消除组蛋白乙酰化、GATA4乙酰化和DNA结合活性。姜黄素还通过破坏p300-HAT依赖性信号通路来阻断AB诱导的炎症和纤维化。我们的结果表明,姜黄素具有通过抑制p300-HAT活性以及下游GATA4、NF-κB和TGF-β-Smad信号通路来预防心肌肥大、炎症和纤维化的潜力。