Zhang Qingfen, Saito Yoshihiko, Naya Noriyuki, Imagawa Keiichi, Somekawa Satoshi, Kawata Hiroyuki, Takeda Yukiji, Uemura Shiro, Kishimoto Ichiro, Nakao Kazuwa
First Department of Internal Medicine, Nara Medical University, Nara, Japan.
Hypertens Res. 2008 Jun;31(6):1251-6. doi: 10.1291/hypres.31.1251.
Mineralocorticoid receptor (MR) blockers attenuate cardiac remodeling in experimental models of heart failure, myocardial infarction and pressure-overload, in which the renin-angiotensin-aldosterone system is activated. Mice lacking the gene encoding guanylyl cyclase-A (GC-A), a common receptor for atrial and brain natriuretic peptide (ANP and BNP, respectively), show marked cardiac hypertrophy and fibrosis, which are almost completely inhibited by both genetic and pharmacological blockade of type 1 angiotensin II receptors. However, the effect of eplerenone, a specific MR blocker, on cardiac remodeling in GC-A knockout (GC-A KO) mice remains unknown. Male 12-week-old GC-A KO mice were assigned to control, eplerenone and hydralazine groups (n=6-7/group). Treatment with eplerenone at a dose of 100 mg/kg body weight/d reduced heart weight/body weight ratios, interstitial fibrosis and blood pressure to levels similar to those seen in wild type mice, in association with reduced transcription of atrial natriuretic peptide, brain natriuretic peptide, transforming growth factor-beta1, collagen I and collagen III. Although hydralazine (5 mg/kg body weight/d) exerted a similar effect on blood pressure, it did not inhibit the cardiac remodeling in GC-A KO mice. In conclusion, eplerenone attenuates cardiac remodeling in GC-A KO mice, most likely in a blood pressure-independent manner, which suggests that signaling downstream of MR is involved in the ventricular remodeling of GC-A KO mice.
盐皮质激素受体(MR)阻滞剂可减轻心力衰竭、心肌梗死和压力超负荷实验模型中的心脏重塑,这些模型中肾素-血管紧张素-醛固酮系统被激活。缺乏编码鸟苷酸环化酶-A(GC-A)基因的小鼠,GC-A是心房利钠肽和脑利钠肽(分别为ANP和BNP)的共同受体,表现出明显的心脏肥大和纤维化,而1型血管紧张素II受体的基因和药理学阻断几乎完全抑制了这些症状。然而,依普利酮(一种特异性MR阻滞剂)对GC-A基因敲除(GC-A KO)小鼠心脏重塑的影响尚不清楚。将12周龄雄性GC-A KO小鼠分为对照组、依普利酮组和肼屈嗪组(每组n = 6 - 7)。以100 mg/kg体重/天的剂量给予依普利酮治疗,可使心脏重量/体重比、间质纤维化和血压降低至与野生型小鼠相似的水平,同时心房利钠肽、脑利钠肽、转化生长因子-β1、I型胶原和III型胶原的转录减少。尽管肼屈嗪(5 mg/kg体重/天)对血压有类似作用,但它并未抑制GC-A KO小鼠的心脏重塑。总之,依普利酮可减轻GC-A KO小鼠的心脏重塑,很可能是以血压非依赖性方式,这表明MR下游信号传导参与了GC-A KO小鼠的心室重塑。