Weber W, Fischli W, Hochuli E, Kupfer E, Weibel E K
Pharma Research Division, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
J Antibiot (Tokyo). 1991 Feb;44(2):164-71. doi: 10.7164/antibiotics.44.164.
Anantin, a peptide binding to the receptor of the atrial natriuretic factor (ANF) was isolated from a strain of Streptomyces coerulescens. The molecule consists of 17 natural L-amino acids which form a peptidic ring system. It has a MW of 1,871.0. The chemical composition is C90H111N21O24. The compound was found to bind competitively to ANF-receptors from bovine adrenal cortex (Kd = 0.61 microM). Furthermore, it dose-dependently inhibited the ANF-induced intracellular cyclic guanosine monophosphate accumulation in bovine aorta smooth muscle cells. At the same concentration no agonistic effects were detectable in these cells. Thus, anantin is considered to be the first microbially produced antagonist of the cardiac hormone, ANF.
阿那替丁是一种与心钠素（ANF）受体结合的肽，从一株天蓝色链霉菌中分离得到。该分子由17个天然L-氨基酸组成，形成一个肽环系统。其分子量为1871.0。化学组成为C90H111N21O24。发现该化合物能与牛肾上腺皮质的ANF受体竞争性结合（解离常数Kd = 0.61微摩尔）。此外，它能剂量依赖性地抑制心钠素诱导的牛主动脉平滑肌细胞内环状鸟苷单磷酸的积累。在相同浓度下，在这些细胞中未检测到激动作用。因此，阿那替丁被认为是第一种由微生物产生的心脏激素心钠素的拮抗剂。
