Key Laboratory of Cerebrocranial Disease, Incubation Base of National Key Laboratory, Ningxia Medical University, Yinchuan 750000, China; Department of Pharmacology, College of Pharmacy, Wuhan University, Wuhan 430072, China; Department of Pharmacology, College of Pharmacy, Ningxia Medical University, Yinchuan 750000, China.
Department of Anesthesiology, Shenzhen Second People's Hospital, The First Affiliated Hospital of Shenzhen University, Shenzhen 518035, China.
Biochem Pharmacol. 2024 Jul;225:116320. doi: 10.1016/j.bcp.2024.116320. Epub 2024 May 25.
TMP269, a class IIA histone deacetylase inhibitor with selectivity, that has a protective effect on the central nervous system, yet its specific mechanism of action remains ambiguous. Although major depressive disorder (MDD) is highly prevalent, its pathophysiology is poorly understood. Recent evidence suggests that histone deacetylase 5 plays a key role in the pathological process of depression and the fact that preclinical studies have shown HDAC5 to be a potential antidepressant target, the search for natural drugs or small molecule compounds that can target HDAC5 may be a potential therapeutic strategy for the treatment of depression. In addition, we examined the role of the Brain-derived neurotrophic factor (BDNF), an important neurotrophic factor for neuronal survival and growth, as a potential downstream target of HDAC5. We found downward revision of HDAC5 levels in the hippocampus ameliorated depressive-like behavior in LH (Learned helplessness) mice. Furthermore, injection of HDAC5 overexpressing adenoviral vectors in the hippocampal dentate gyrus of wild-type mice produced a somewhat depressive-like phenotype. Pharmacological, immunofluorescence and biochemical experiments showed that TMP269 could produce antidepressant effects by inhibiting mouse hippocampal HDAC5 and thus modulating its downstream BDNF. Over all, TMP269 mitigated LH-induced depressive-like behaviors and abnormalities in synapse formation and neurogenesis within the hippocampus. These findings suggest potential beneficial effects of TMP269 on depression.
TMP269 是一种选择性的 IIA 组蛋白去乙酰化酶抑制剂,对中枢神经系统具有保护作用,但具体作用机制尚不清楚。尽管重度抑郁症(MDD)的发病率很高,但它的病理生理学仍不清楚。最近的证据表明,组蛋白去乙酰化酶 5 在抑郁症的病理过程中起着关键作用,而且临床前研究表明 HDAC5 是一种潜在的抗抑郁靶点,因此寻找可以靶向 HDAC5 的天然药物或小分子化合物可能是治疗抑郁症的一种潜在治疗策略。此外,我们还研究了脑源性神经营养因子(BDNF)的作用,BDNF 是神经元存活和生长的重要神经营养因子,作为 HDAC5 的潜在下游靶点。我们发现,海马体中 HDAC5 水平的下调改善了 LH(习得性无助)小鼠的抑郁样行为。此外,在野生型小鼠海马齿状回注射过表达 HDAC5 的腺相关病毒载体,会产生一些类似抑郁的表型。药理学、免疫荧光和生化实验表明,TMP269 可以通过抑制小鼠海马体中的 HDAC5 产生抗抑郁作用,从而调节其下游的 BDNF。总的来说,TMP269 减轻了 LH 诱导的抑郁样行为以及海马体中突触形成和神经发生的异常。这些发现表明 TMP269 可能对抑郁症有有益的影响。