Department of Emergency and Critical Care, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China.
West Coast University, School of Pharmacy, Los Angeles, CA, 90004, USA.
Hypertens Res. 2019 Jul;42(7):960-969. doi: 10.1038/s41440-019-0212-z. Epub 2019 Jan 21.
Metformin is an antidiabetic drug. However, the pleiotropic beneficial effects of metformin in nondiabetic models still need to be defined. The objective of this study is to investigate the effect of metformin on angiotensin II (Ang II)-induced hypertension and cardiovascular diseases. Mice were infused with Ang II (400 ng/kg per min) with or without metformin for 2 weeks. Mice infused with angiotensin II displayed an increase in blood pressure associated with enhanced vascular endoplasmic reticulum (ER) stress markers, which were blunted after metformin treatment. Moreover, hypertension-induced reduction in phosphorylated AMPK, endothelial nitric oxide synthase (eNOs) phosphorylation, and endothelium-dependent relaxation (EDR) in mesenteric resistance arteries (MRA) were rescued after metformin treatment. Infusion of ER stress inducer (tunicamycin, Tun) in control mice induced ER stress in MRA and reduced phosphorylation of AMPK, eNOS synthase phosphorylation, and EDR in MRA without affecting systolic blood pressure (SBP). All these factors were reversed subsequently with metformin treatment. ER stress inhibition by metformin improves vascular function in hypertension. Therefore, metformin could be a potential therapy for cardiovascular diseases in hypertension independent of its effects on diabetes.
二甲双胍是一种抗糖尿病药物。然而,二甲双胍在非糖尿病模型中的多效有益作用仍有待确定。本研究的目的是研究二甲双胍对血管紧张素 II(Ang II)诱导的高血压和心血管疾病的影响。用 Ang II(400ng/kg/min)输注小鼠,同时或不给予二甲双胍,共 2 周。输注 Ang II 的小鼠血压升高,伴有血管内质网(ER)应激标志物增强,而给予二甲双胍治疗后则减弱。此外,高血压诱导的肠系膜阻力动脉(MRA)中磷酸化 AMPK、内皮型一氧化氮合酶(eNOS)磷酸化和内皮依赖性舒张(EDR)减少,经二甲双胍治疗后得到恢复。在对照小鼠中输注 ER 应激诱导剂(衣霉素,Tun)会在 MRA 中引起 ER 应激,并降低 MRA 中磷酸化 AMPK、eNOS 合酶磷酸化和 EDR,而不影响收缩压(SBP)。所有这些因素随后均随着二甲双胍治疗而逆转。二甲双胍抑制 ER 应激可改善高血压中的血管功能。因此,二甲双胍可能是一种独立于其对糖尿病的作用的治疗高血压相关心血管疾病的潜在疗法。