Qian Sichong, Zhang Chen, Li Wenbo, Song Shiyang, Lin Guanqiao, Cheng Zixiu, Zhou Wenjun, Yin Huiqi, Li Haiyang, Shen Hu-Ying, Sun Zheng
Department of Cardiovascular Surgery, Beijing Anzhen Hospital, Capital Medical University, Beijing, China.
Department of Medicine - Endocrinology, Baylor College of Medicine, Houston, Texas, USA.
bioRxiv. 2024 Dec 30:2024.12.29.630635. doi: 10.1101/2024.12.29.630635.
The cardioprotective effects of histone deacetylase (HDAC) inhibitors (HDIs) are at odds with the deleterious effects of HDAC depletion. Here, we use HDAC3 as a prototype HDAC to address this contradiction. We show that adult-onset cardiac-specific depletion of HDAC3 in mice causes cardiac hypertrophy and contractile dysfunction on a high-fat diet (HFD), excluding developmental disruption as a major reason for the contradiction. Genetically abolishing HDAC3 enzymatic activity without affecting its protein level does not cause cardiac dysfunction on HFD. HDAC3 depletion causes robust downregulation of lipid oxidation/bioenergetic genes and upregulation of antioxidant/anti-apoptotic genes. In contrast, HDAC3 enzyme activity abolishment causes much milder changes in far fewer genes. The abnormal gene expression is cardiomyocyte-autonomous and can be rescued by an enzyme-dead HDAC3 mutant but not by an HDAC3 mutant (Δ33-70) that lacks interaction with the nuclear-envelope protein lamina-associated polypeptide 2β (LAP2β). Tethering LAP2β to the HDAC3 Δ33-70 mutant restored its ability to rescue gene expression. Finally, HDAC3 depletion, not loss of HDAC3 enzymatic activity, exacerbates cardiac contractile functions upon aortic constriction. These results suggest that the cardiac function of HDAC3 in adults is not attributable to its enzyme activity, which has implications for understanding the cardioprotective effects of HDIs.
组蛋白去乙酰化酶(HDAC)抑制剂(HDIs)的心脏保护作用与HDAC缺失的有害作用相互矛盾。在此,我们以HDAC3作为HDAC的原型来解决这一矛盾。我们发现,成年小鼠心脏特异性缺失HDAC3会在高脂饮食(HFD)条件下导致心脏肥大和收缩功能障碍,排除了发育干扰是造成这种矛盾的主要原因。在不影响其蛋白水平的情况下通过基因手段消除HDAC3的酶活性,在高脂饮食条件下不会导致心脏功能障碍。HDAC3缺失会导致脂质氧化/生物能量基因的强烈下调以及抗氧化/抗凋亡基因的上调。相比之下,消除HDAC3的酶活性只会导致更少基因发生程度轻得多的变化。这种异常的基因表达是心肌细胞自主性的,并且可以被无酶活性的HDAC3突变体挽救,但不能被缺乏与核膜蛋白核纤层相关多肽2β(LAP2β)相互作用的HDAC3突变体(Δ33 - 70)挽救。将LAP2β与HDAC3 Δ33 - 70突变体拴系在一起可恢复其挽救基因表达的能力。最后,HDAC3的缺失而非HDAC3酶活性的丧失会加剧主动脉缩窄后的心脏收缩功能。这些结果表明,成年期HDAC3的心脏功能并非归因于其酶活性,这对于理解HDIs的心脏保护作用具有重要意义。