Heart Institute (InCor), University of São Paulo Medical School, São Paulo, São Paulo, Brazil.
Department of Nephrology (LIM-12), University of São Paulo Medical School, São Paulo, São Paulo, Brazil.
Eur J Pharmacol. 2017 Sep 15;811:38-47. doi: 10.1016/j.ejphar.2017.05.054. Epub 2017 May 30.
Accumulating evidence from clinical and experimental studies indicates that the incretin glucagon-like peptide-1 (GLP-1) elicits blood-pressure lowering effects via its diuretic, natriuretic and vasodilatory properties. The present study investigated whether acute infusion of GLP-1 induces diuresis and natriuresis in spontaneously hypertensive rats (SHRs). Additionally, we examined whether GLP-1 influences the vascular reactivity of the renal arteries of normotensive and hypertensive rats and elucidated the underlying mechanisms. We found that the increase in urinary output and urinary sodium excretion in response to systemic infusion of GLP-1 for 30min in SHRs was much less pronounced than in normotensive rats. The diuretic and natriuretic actions of GLP-1 in normotensive rats were accompanied by increases in GFR and RBF and a reduction in RVR through activation of the cAMP signaling pathway. However, no changes in renal hemodynamics were observed in SHRs. Similarly, GLP-1 induced an endothelium-independent relaxation effect in the renal arteries of normotensive rats, whereas the renal vasculature of SHRs was unresponsive to this vasodilator. The absence of a GLP-1-induced renal artery vasodilator effect in SHRs was associated with lower expression of the GLP-1 receptor, blunted GLP-1-induced increases in cAMP production and higher activity and expression of the GLP-1 inactivating enzyme dipeptidyl peptidase IV relative to the renal arteries of normotensive rats. Collectively, these results demonstrate that the renal acute responses to GLP-1 are attenuated in SHRs. Thus, chronic treatment with incretin-based agents may rely upon the upregulation of GLP-1/GLP-1 receptor signaling in the kidneys of hypertensive patients and experimental models.
越来越多的临床和实验研究证据表明,肠促胰岛素胰高血糖素样肽-1(GLP-1)通过其利尿、利钠和血管舒张特性引起降压作用。本研究旨在探讨 GLP-1 急性输注是否会引起自发性高血压大鼠(SHR)的利尿和利钠作用。此外,我们还研究了 GLP-1 是否会影响正常血压和高血压大鼠的肾动脉血管反应,并阐明了潜在的机制。我们发现,与正常血压大鼠相比,GLP-1 全身输注 30 分钟后,SHR 尿排量和尿钠排泄的增加幅度要小得多。GLP-1 在正常血压大鼠中的利尿和利钠作用伴随着 GFR 和 RBF 的增加,以及通过激活 cAMP 信号通路降低 RVR。然而,在 SHR 中没有观察到肾血液动力学的变化。同样,GLP-1 在正常血压大鼠的肾动脉中引起非内皮依赖性舒张作用,而 SHR 的肾血管对这种血管扩张剂无反应。SHR 中 GLP-1 诱导的肾动脉血管舒张作用缺失与 GLP-1 受体表达降低、GLP-1 诱导的 cAMP 产生增加减弱以及 GLP-1 失活酶二肽基肽酶 IV 的活性和表达升高有关。总之,这些结果表明,GLP-1 在 SHR 中的肾脏急性反应减弱。因此,基于肠促胰岛素的药物的慢性治疗可能依赖于高血压患者和实验模型肾脏中 GLP-1/GLP-1 受体信号的上调。