Kornel L, Kanamarlapudi N, Ramsay C, Travers T, Kamath S, Taff D J, Patel N, Packer W, Raynor W J
J Steroid Biochem. 1983 Jul;19(1A):333-44.
Data from clinical and experimental studies indicate that mechanism(s) for action of mineralocorticoids, other than renal, must be involved in the overall effect of mineralocorticoids on circulation--increased peripheral resistance and hypertension. We have postulated existence of such a mechanism in the arterial wall and have looked for the evidence for its presence. We have found high affinity, specific binders for mineralocorticoids, and glucocorticoids, with characteristics of steroid receptors, in the cytosol of rabbit aorta and femoral and carotid arteries. These binders possess physico-chemical properties of steroid receptors and, moreover, they translocate to cell nuclei (as steroid-receptor complexes) and bind to relatively specific "acceptor-sites" on nuclear chromatin. This provides evidence for the existence in the arterial wall of a molecular mechanism for a direct in situ action of mineralocorticoids and glucocorticoids. The mineralocorticoid receptors are not present in veins. We have also found that chronically elevated levels of 11-desoxycorticosterone (DOC) result in a marked increase in permeability of arterial smooth muscle cell membrane to sodium ions; this is in accord with findings of other investigators in the rat. This change presumably leads, through a chain of biochemical events, to increased arterial and arteriolar smooth muscle contractility, increased peripheral resistance and hypertension. Study is in progress to determine whether the effect of DOC on arterial smooth muscle cell-membrane permeability to electrolytes is elicited through the receptor-mediated mechanism for the in situ action of mineralocorticoids in the arterial wall. It is postulated that this mechanism is primarily responsible for "mineralocorticoid hypertension", but may well be instrumental also in pathogeneses of various other forms of hypertension, including "essential".
临床和实验研究数据表明,盐皮质激素发挥作用的机制(除了在肾脏中的机制外)必定参与了盐皮质激素对循环系统的整体作用——外周阻力增加和高血压。我们推测动脉壁中存在这样一种机制,并一直在寻找其存在的证据。我们在兔主动脉、股动脉和颈动脉的胞质溶胶中发现了对盐皮质激素和糖皮质激素具有高亲和力的特异性结合物,这些结合物具有类固醇受体的特征。这些结合物具有类固醇受体的物理化学性质,而且它们会转移到细胞核(作为类固醇 - 受体复合物)并与核染色质上相对特异性的“受体位点”结合。这为动脉壁中存在盐皮质激素和糖皮质激素直接原位作用的分子机制提供了证据。静脉中不存在盐皮质激素受体。我们还发现,11 - 脱氧皮质酮(DOC)的长期升高会导致动脉平滑肌细胞膜对钠离子的通透性显著增加;这与其他研究者在大鼠中的发现一致。这种变化大概通过一系列生化事件导致动脉和小动脉平滑肌收缩力增加、外周阻力增加和高血压。目前正在进行研究,以确定DOC对动脉平滑肌细胞膜电解质通透性的影响是否是通过盐皮质激素在动脉壁原位作用的受体介导机制引发的。据推测,这种机制主要导致“盐皮质激素性高血压”,但很可能在包括“原发性”在内的各种其他形式高血压的发病机制中也起作用。