Hydralazine

Hydralazine is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain^{[1][2][3][4][5]}.

References:

[1]. Arce C, et al. Hydralazine target: from blood vessels to the epigenome. J Transl Med. 2006;4:10. Published 2006 Feb 28.
[2]. Leiro JM, et al. Antioxidant activity and inhibitory effects of hydralazine on inducible NOS/COX-2 gene and protein expression in rat peritoneal macrophages. Int Immunopharmacol. 2004;4(2):163-177.
[3]. de Flora S, et al. In vivo and in vitro genotoxicity of three antihypertensive hydrazine derivatives (hydralazine, dihydralazine, and endralazine). Environ Mutagen. 1982;4(5):605-619.
[4]. Park J, et al. Neuroprotective role of hydralazine in rat spinal cord injury-attenuation of acrolein-mediated damage. J Neurochem. 2014;129(2):339-349. [Content Brief]
[5]. Bai L, et al. Attenuation of mouse somatic and emotional inflammatory pain by hydralazine through scavenging acrolein and inhibiting neuronal activation. Pain Physician. 2012;15(4):311-326.

Hydralazine 是一种口服有效、可透过血脑屏障的 DNA 甲基转移酶抑制剂，具有血管舒张、松弛动脉平滑肌、降血压的活性。Hydralazine 能通过介导 DNA 去甲基化重新激活沉默的抑癌基因，同时发挥神经保护和抗炎特性。Hydralazine 可抑制 NOS-2 (iNOS) 和 COX-2，减少 NO 和 PGE_E2 的生成；同时，清除活性氧、抑制巨噬细胞活化。Hydralazine 能够减轻运动功能障碍、神经性炎性疼痛以及福尔马林诱导的躯体和情绪性疼痛反应。此外，Hydralazine 可直接诱导 DNA 断裂和姐妹染色单体交换，表现出一定的诱变剂特征。Hydralazine 已被广泛应用于高血压、多种癌症 (如宫颈癌、白血病)、脊髓损伤及炎性疼痛机制的研究中。