Department of Pharmacology and Personalised Medicine, School for Mental Health and Neuroscience (MHeNs), Maastricht University, Maastricht, the Netherlands.
Department of Pharmacology and Toxicology, School of Pharmacy, Zagazig University, Zagazig, Egypt.
PLoS Biol. 2020 Nov 10;18(11):e3000885. doi: 10.1371/journal.pbio.3000885. eCollection 2020 Nov.
Hypertension is the most important cause of death and disability in the elderly. In 9 out of 10 cases, the molecular cause, however, is unknown. One mechanistic hypothesis involves impaired endothelium-dependent vasodilation through reactive oxygen species (ROS) formation. Indeed, ROS forming NADPH oxidase (Nox) genes associate with hypertension, yet target validation has been negative. We re-investigate this association by molecular network analysis and identify NOX5, not present in rodents, as a sole neighbor to human vasodilatory endothelial nitric oxide (NO) signaling. In hypertensive patients, endothelial microparticles indeed contained higher levels of NOX5-but not NOX1, NOX2, or NOX4-with a bimodal distribution correlating with disease severity. Mechanistically, mice expressing human Nox5 in endothelial cells developed-upon aging-severe systolic hypertension and impaired endothelium-dependent vasodilation due to uncoupled NO synthase (NOS). We conclude that NOX5-induced uncoupling of endothelial NOS is a causal mechanism and theragnostic target of an age-related hypertension endotype. Nox5 knock-in (KI) mice represent the first mechanism-based animal model of hypertension.
高血压是老年人死亡和残疾的最重要原因。然而,在十分之九的病例中,其分子病因尚不清楚。一种机制假说涉及通过活性氧 (ROS) 形成导致内皮依赖性血管舒张受损。事实上,形成 ROS 的 NADPH 氧化酶 (Nox) 基因与高血压相关,但靶向验证一直为阴性。我们通过分子网络分析重新研究了这种关联,并确定了在啮齿动物中不存在的 NOX5 是人类血管舒张性内皮一氧化氮 (NO) 信号的唯一邻居。在高血压患者中,内皮微粒实际上确实含有更高水平的 NOX5-但不包括 NOX1、NOX2 或 NOX4-呈双峰分布,与疾病严重程度相关。从机制上讲,在血管内皮细胞中表达人 Nox5 的小鼠在衰老后会发展为严重的收缩期高血压,并由于一氧化氮合酶 (NOS) 脱偶联而导致内皮依赖性血管舒张受损。我们的结论是,NOX5 诱导的内皮 NOS 脱偶联是一种因果机制,也是与年龄相关的高血压表型的治疗靶点。Nox5 基因敲入 (KI) 小鼠代表了首个基于机制的高血压动物模型。