Anggård E E, Botting R M, Vane J R
William Harvey Research Institute, St. Bartholomew's Hospital Medical College, London, UK.
Blood Vessels. 1990;27(2-5):269-81.
The endothelins (ETs) are a family of newly discovered peptides with potent vasoconstrictor properties. They were first discovered in cultured endothelial cells but ET expression has since been found in many other tissues such as brain and kidney. They are peptides with 21 amino acids formed by hydrolytic cleavage of a larger peptide, big ET. Release of ETs from cultured endothelial cells is modulated by a variety of chemical and physical stimuli and as no storage sites have been identified it is suggested that endothelin release is regulated at the level of transcription or translation. Both big ET and ET-1 are found circulating in the blood. The levels are elevated in shock, myocardial infarction and kidney failure indicative of enhanced formation in these diseases. The literature now abounds with reports on actions of the ETs in vitro and in vivo. The vasoconstrictor properties are powerful and long-lasting. Several studies also show a mitogenic effect, indicating a possible trophic role. It is likely that in the next few years the development of inhibitors of endothelin synthesis and/or action will be of importance in unravelling the role of the ETs.
内皮素（ETs）是新发现的一类具有强大血管收缩特性的肽。它们最初是在培养的内皮细胞中发现的，但此后在许多其他组织如脑和肾中也发现了ET的表达。它们是由一种较大的肽——大内皮素经水解切割形成的含有21个氨基酸的肽。培养的内皮细胞释放ETs受多种化学和物理刺激的调节，由于尚未发现储存位点，提示内皮素的释放是在转录或翻译水平上进行调控的。大内皮素和ET-1都存在于血液循环中。在休克、心肌梗死和肾衰竭时其水平升高，表明在这些疾病中其生成增加。目前关于ETs在体外和体内作用的报道大量涌现。其血管收缩特性强大且持久。多项研究还显示有促有丝分裂作用，表明可能具有营养作用。在未来几年，内皮素合成和/或作用抑制剂的开发对于阐明ETs的作用可能具有重要意义。
