Whaley-Connell Adam, Habibi Javad, Nistala Ravi, Hayden Melvin R, Pulakat Lakshmi, Sinak Catherine, Locher Bonnie, Ferrario Carlos M, Sowers James R
Harry S. Truman VA Medical Center, University of Missouri-Columbia School of Medicine, Columbia, MO 65211, USA.
Regul Pept. 2012 Jun 10;176(1-3):36-44. doi: 10.1016/j.regpep.2012.03.002. Epub 2012 Mar 29.
Enhanced renin-angiotensin-aldosterone system (RAAS) activation contributes to proteinuria and chronic kidney disease by increasing glomerular and tubulointerstitial oxidative stress, promotion of fibrosis. Renin activation is the rate limiting step in angiotensin (Ang II) and aldosterone generation, and recent work suggests direct renin inhibition improves proteinuria comparable to that seen with Ang type 1 receptor (AT(1)R) blockade. This is important as, even with contemporary use of AT(1)R blockade, the burden of kidney disease remains high. Thereby, we sought to determine if combination of direct renin inhibition with AT(1)R blockade in vivo, via greater attenuation of kidney oxidative stress, would attenuate glomerular and proximal tubule injury to a greater extent than either intervention alone. We utilized the transgenic Ren2 rat with increased tissue RAS activity and higher serum levels of aldosterone, which manifests hypertension and proteinuria. Ren2 rats were treated with renin inhibition (aliskiren), AT(1)R blockade (valsartan), the combination (aliskiren+valsartan), or vehicle for 21days. Compared to Sprague-Dawley controls, Ren2 rats displayed increased systolic pressure (SBP), circulating aldosterone, proteinuria and greater urine levels of the proximal tubule protein excretory marker beta-N-acetylglucosaminidase (β-NAG). These functional and biochemical alterations were accompanied by increases in kidney tissue NADPH oxidase subunit Rac1 and 3-nitrotyrosine (3-NT) content as well as fibronectin and collagen type III. These findings occurred in conjunction with reductions in the podocyte-specific protein podocin as well as the proximal tubule-specific megalin. Further, in transgenic animals there was increased tubulointerstitial fibrosis on light microscopy as well as ultrastructural findings of glomerular podocyte foot-process effacement and reduced tubular apical endosomal/lysosomal activity. Combination therapy led to greater reductions in SBP and serum aldosterone, but did not result in greater improvement in markers of glomerular and tubular injury (i.e. β-NAG) compared to either intervention alone. Further, combination therapy did not improve markers of oxidative stress and podocyte and proximal tubule integrity in this transgenic model of RAAS-mediated kidney damage despite greater reductions in serum aldosterone and BP levels.
增强的肾素-血管紧张素-醛固酮系统(RAAS)激活通过增加肾小球和肾小管间质氧化应激、促进纤维化,导致蛋白尿和慢性肾脏病。肾素激活是血管紧张素(Ang II)和醛固酮生成的限速步骤,最近的研究表明,直接抑制肾素可改善蛋白尿,效果与1型血管紧张素受体(AT(1)R)阻断剂相当。这一点很重要,因为即使当代使用AT(1)R阻断剂,肾脏疾病的负担仍然很高。因此,我们试图确定在体内将直接肾素抑制与AT(1)R阻断相结合,通过更大程度地减轻肾脏氧化应激,是否会比单独的任何一种干预措施更能减轻肾小球和近端小管损伤。我们使用了组织RAS活性增加且血清醛固酮水平较高的转基因Ren2大鼠,其表现为高血压和蛋白尿。将Ren2大鼠用肾素抑制剂(阿利吉仑)、AT(1)R阻断剂(缬沙坦)、联合用药(阿利吉仑+缬沙坦)或赋形剂治疗21天。与Sprague-Dawley对照相比,Ren2大鼠收缩压(SBP)升高、循环醛固酮增加、蛋白尿增多,近端小管蛋白排泄标志物β-N-乙酰氨基葡萄糖苷酶(β-NAG)尿水平更高。这些功能和生化改变伴随着肾组织NADPH氧化酶亚基Rac1和3-硝基酪氨酸(3-NT)含量以及纤连蛋白和III型胶原增加。这些发现同时伴随着足细胞特异性蛋白足突蛋白以及近端小管特异性巨膜蛋白减少。此外,在转基因动物中,光镜下肾小管间质纤维化增加,同时有肾小球足细胞足突消失和肾小管顶端内体/溶酶体活性降低的超微结构表现。联合治疗导致SBP和血清醛固酮更大程度降低,但与单独的任何一种干预措施相比,并未使肾小球和肾小管损伤标志物(即β-NAG)有更大改善。此外,在这个RAAS介导肾损伤的转基因模型中,尽管血清醛固酮和血压水平有更大程度降低,但联合治疗并未改善氧化应激标志物以及足细胞和近端小管完整性。