Emori T, Hirata Y, Imai T, Eguchi S, Kanno K, Marumo F
Second Department of Internal Medicine, Tokyo Medical and Dental University, Japan.
Endocrinology. 1993 Dec;133(6):2474-80. doi: 10.1210/endo.133.6.8243267.
We studied the cellular mechanism by which natriuretic peptides inhibit the synthesis and release of endothelin-1 (ET-1) in cultured rat aortic endothelial cells (EC). Atrial natriuretic peptide (ANP) and brain natriuretic peptide (BNP) showed dose-dependent and equipotent effects on displacement of [125I]ANP binding and generation of cGMP production in rat EC, whereas C-type natriuretic peptide and biologically inactive ANP analog had lesser effects. ANP and BNP as well as 8-bromo-cGMP had potent inhibitory effects on immunoreactive ET-1 release, the transient increase in the intracellular Ca2+ concentration, and the formation of inositol 1,4,5-trisphosphate stimulated by thrombin in rat EC. A cGMP-dependent protein kinase inhibitor (KT5823), but not a cAMP-dependent protein kinase inhibitor (KT5720), completely abolished the inhibitory effect of ANP on thrombin-induced immunoreactive Et-1 release. Northern blot analysis using cDNA for rat prepro-ET-1 as a probe showed that ANP and 8-bromo-cGMP, but not C-type natriuretic peptide, inhibited thrombin-induced prepro-ET-1 mRNA expression, whose effect was abolished by KT5823. These data suggest that ANP and BNP inhibit the thrombin-induced synthesis and release of ET-1 in cultured rat aortic EC by blocking phosphoinositide breakdown, possibly via natriuretic peptides type A receptor-mediated cGMP-dependent mechanism.
我们研究了利钠肽在培养的大鼠主动脉内皮细胞(EC)中抑制内皮素-1(ET-1)合成与释放的细胞机制。心房利钠肽(ANP)和脑利钠肽(BNP)对大鼠内皮细胞中[125I]ANP结合的置换和cGMP生成具有剂量依赖性且等效的作用,而C型利钠肽和无生物学活性的ANP类似物的作用较小。ANP、BNP以及8-溴-cGMP对大鼠内皮细胞中免疫反应性ET-1释放、细胞内Ca2+浓度的短暂升高以及凝血酶刺激的肌醇1,4,5-三磷酸形成均有强大的抑制作用。一种cGMP依赖性蛋白激酶抑制剂(KT5823),而非cAMP依赖性蛋白激酶抑制剂(KT5720),完全消除了ANP对凝血酶诱导的免疫反应性Et-1释放的抑制作用。用大鼠前内皮素原-1的cDNA作为探针进行的Northern印迹分析表明,ANP和8-溴-cGMP,但不是C型利钠肽,抑制凝血酶诱导的前内皮素原-1 mRNA表达,其作用被KT5823消除。这些数据表明,ANP和BNP可能通过A型利钠肽受体介导的cGMP依赖性机制,阻断磷酸肌醇分解,从而抑制培养的大鼠主动脉内皮细胞中凝血酶诱导的ET-1合成与释放。