Lee Tsung-Ming, Lin Mei-Shu, Chang Nen-Chung
Cardiology Section, Department of Medicine, Taipei Medical University and Chi-Mei Medical Center, Taipei, Taiwan.
Am J Physiol Heart Circ Physiol. 2007 Aug;293(2):H968-77. doi: 10.1152/ajpheart.00891.2006. Epub 2007 Mar 30.
Histone deacetylase (HDAC) determines the acetylation status of histones and, thereby, controls the regulation of gene expression. HDAC inhibitors have been shown to inhibit cardiomyocyte growth in vitro and in vivo. We assessed whether HDAC inhibitors exert a beneficial effect on the remodeling heart in infarcted rats. At 24 h after ligation of the left anterior descending artery, male Wistar rats were randomized to vehicle, HDAC inhibitors [valproic acid (VPA) and tributyrin], an agonist of HDAC (theophylline), VPA + theophylline, or tributyrin + theophylline for 4 wk. Significant ventricular hypertrophy was detected as increased myocyte size at the border zone isolated by enzymatic dissociation after infarction. Cardiomyocyte hypertrophy and collagen formation at the remote region and border zone were significantly attenuated by VPA and tributyrin with a similar potency compared with that induced by the vehicle. Left ventricular shortening fraction was significantly higher in the VPA- and tributyrin-treated groups than in the vehicle-treated group. Increased synthesis of atrial natriuretic peptide mRNA after infarction was confirmed by RT-PCR, consistent with the results of immunohistochemistry and Western blot for acetyl histone H4. The beneficial effects of VPA and tributyrin were abolished by theophylline, implicating HDAC as the relevant target. Inhibition of HDAC by VPA or tributyrin can attenuate ventricular remodeling after infarction. This might provide a worthwhile therapeutic target.
组蛋白去乙酰化酶(HDAC)决定组蛋白的乙酰化状态,从而控制基因表达的调控。已表明HDAC抑制剂在体外和体内均可抑制心肌细胞生长。我们评估了HDAC抑制剂对梗死大鼠心脏重塑是否具有有益作用。在结扎左冠状动脉前降支24小时后,将雄性Wistar大鼠随机分为给予溶剂、HDAC抑制剂[丙戊酸(VPA)和三丁酸甘油酯]、HDAC激动剂(茶碱)、VPA + 茶碱或三丁酸甘油酯 + 茶碱组,持续4周。梗死发生后,通过酶解分离梗死边缘区的心肌细胞,检测到明显的心室肥大表现为细胞大小增加。与给予溶剂相比,VPA和三丁酸甘油酯以相似效力显著减轻了远隔区域和边缘区的心肌细胞肥大及胶原形成。VPA和三丁酸甘油酯治疗组的左心室缩短分数显著高于溶剂治疗组。梗死发生后心房利钠肽mRNA合成增加通过逆转录聚合酶链反应得以证实,这与乙酰化组蛋白H4的免疫组织化学和蛋白质印迹结果一致。茶碱消除了VPA和三丁酸甘油酯的有益作用,提示HDAC是相关靶点。VPA或三丁酸甘油酯抑制HDAC可减轻梗死后心室重塑。这可能提供一个有价值的治疗靶点。