Monge J C
St. Michael's Hospital and University of Toronto, Ontario, Canada.
J Cardiovasc Pharmacol. 1998;32 Suppl 2:S36-42. doi: 10.1097/00005344-199800004-00006.
Endothelin-1 (ET-1) is the most potent vasoconstrictor yet described. The active 21-amino-acid peptide is derived from the conversion of the inactive precursor "Big ET-1" by an enzyme called endothelin-converting enzyme. In addition to its potent action as a vasoconstrictor, endothelin promotes growth and proliferation of smooth muscle and myocardial hypertrophy. ET-1 levels are elevated in acute myocardial infarction (MI), atherosclerosis, renal failure, diabetes, pulmonary hypertension, and congestive heart failure (CHF). ET-1 levels correlate extremely well with the seriousness of the pathophysiologic condition. ET-1 levels at 72 h post MI accurately predict long-term survival. In patients with heart failure, ET-1 levels also predict long-term outcome, with the prognosis being severely compromised in patients with elevated ET-1 levels. Levels of plasma big ET-1 have been demonstrated to predict 1-year mortality and have been shown to be a better predictor of 1-year outcome than plasma atrial natriuretic peptide and norepinephrine, NYHA class, age, and echocardiographic left ventricular parameters. Although a small number of studies have reported beneficial effects of ACE inhibitors on ET-1 levels in animal models, most reports in humans have not found an effect of ACE inhibitors on ET-1 levels. Only one ACE inhibitor, fosinopril, has been shown to be effective in normalizing ET-1 levels in clinically relevant situations, such as the long-term study of patients with CHF. This observation may point to a superior role of fosinopril compared with other ACE inhibitors in CHF patients and may indicate beneficial effects of fosinopril beyond blood pressure control.
内皮素-1(ET-1)是目前已知的最强效血管收缩剂。这种由21个氨基酸组成的活性肽是由一种名为内皮素转换酶的酶将无活性前体“大ET-1”转化而来。除了作为血管收缩剂的强大作用外,内皮素还能促进平滑肌生长和增殖以及心肌肥大。急性心肌梗死(MI)、动脉粥样硬化、肾衰竭、糖尿病、肺动脉高压和充血性心力衰竭(CHF)患者的ET-1水平会升高。ET-1水平与病理生理状况的严重程度密切相关。心肌梗死后72小时的ET-1水平能准确预测长期生存率。在心力衰竭患者中,ET-1水平也能预测长期预后,ET-1水平升高的患者预后严重受损。血浆大ET-1水平已被证明可预测1年死亡率,并且已显示其比血浆心房利钠肽、去甲肾上腺素、纽约心脏协会(NYHA)分级、年龄和超声心动图左心室参数更能预测1年预后。尽管少数研究报告了血管紧张素转换酶(ACE)抑制剂在动物模型中对ET-1水平有有益作用,但大多数关于人类的报告并未发现ACE抑制剂对ET-1水平有影响。只有一种ACE抑制剂福辛普利在临床相关情况下(如对CHF患者的长期研究)被证明能有效使ET-1水平正常化。这一观察结果可能表明福辛普利在CHF患者中比其他ACE抑制剂具有更优越的作用,并且可能表明福辛普利除了控制血压外还有有益作用。