Department of Physiology and Morphology, Institute of Medicinal Chemistry, Hoshi University, Shinagawa-ku, Tokyo, 142-8501, Japan.
Pflugers Arch. 2012 Aug;464(2):205-15. doi: 10.1007/s00424-012-1131-x. Epub 2012 Jun 23.
Cardiovascular problems are a major cause of morbidity and mortality, mainly due to coronary artery disease and atherosclerosis, in type 2 diabetes mellitus. However, female gender is a protective factor in the development of, for example, atherosclerosis and hypertension. One of the female hormones, 17β-estradiol (E2), is known to protect against the cardiovascular injury resulting from endothelial dysfunction, but the mechanism by which it does so remains unknown. Our hypothesis was that E2-mediated activation of Akt and mitogen-activated protein kinase (MAPK), and the subsequent endothelial NO synthase (eNOS) phosphorylation, might protect the aorta in diabetic mellitus. The experimental type 2 diabetic model we employed to test that hypothesis (female mice given streptozotocin and nicotinamide) is here termed fDM. In fDM aortas, we examined the E2-induced relaxation response and the associated protein activities. In control (age-matched, nondiabetic) aortas, E2 induced a vascular relaxation response that was mediated via Akt/eNOS and mitogen-activated/ERK-activating kinase (MEK)/eNOS pathways. In fDM aortas (vs. control aortas), (a) the E2-induced relaxation was enhanced, (b) the mediation of the response was different (via Akt/eNOS and p38 MAPK/eNOS pathways), and (c) E2 stimulation increased p38 MAPK and eNOS phosphorylations, decreased MEK phosphorylation, but did not alter estrogen receptor activity. We infer that at least in fDM aortas, E2 has beneficial effects (enhanced vascular relaxation and protection) that are mediated through Akt activation and (compensating for reduced MEK activation) p38 MAPK activation, leading to enhanced eNOS phosphorylation.
心血管问题是发病率和死亡率的主要原因,主要是由于 2 型糖尿病中的冠状动脉疾病和动脉粥样硬化。然而,女性性别是发展的保护因素,例如动脉粥样硬化和高血压。一种女性激素,17β-雌二醇(E2),已知可防止内皮功能障碍引起的心血管损伤,但具体机制尚不清楚。我们的假设是,E2 介导的 Akt 和丝裂原激活蛋白激酶(MAPK)的激活,以及随后的内皮型一氧化氮合酶(eNOS)磷酸化,可能保护糖尿病中的主动脉。我们用来检验该假设的实验 2 型糖尿病模型(给予链脲佐菌素和烟酰胺的雌性小鼠)在这里称为 fDM。在 fDM 主动脉中,我们检查了 E2 诱导的松弛反应及其相关蛋白活性。在对照(年龄匹配的,非糖尿病)主动脉中,E2 诱导了一种通过 Akt/eNOS 和丝裂原激活/细胞外信号调节激酶(ERK)激活激酶(MEK)/eNOS 途径介导的血管松弛反应。在 fDM 主动脉中(与对照主动脉相比),(a)E2 诱导的松弛增强,(b)反应的介导途径不同(通过 Akt/eNOS 和 p38 MAPK/eNOS 途径),(c)E2 刺激增加了 p38 MAPK 和 eNOS 的磷酸化,降低了 MEK 的磷酸化,但没有改变雌激素受体的活性。我们推断,至少在 fDM 主动脉中,E2 具有有益作用(增强血管松弛和保护),这是通过 Akt 激活和(补偿 MEK 激活减少)p38 MAPK 激活介导的,导致增强的 eNOS 磷酸化。