Kondo Y, Torii K, Itoh Z, Omura S
Department of Physical Biochemistry, College of Medical Technology, Gunma University, Maebashi, Japan.
Biochem Biophys Res Commun. 1988 Jan 29;150(2):877-82. doi: 10.1016/0006-291x(88)90474-3.
Erythromycin, one of the macrolide antibiotics, and its derivatives had been found to mimic actions of exogenous motilin, a gastrointestinal peptide hormone. We found that some of the macrolide compounds inhibited the specific binding of 125I-motilin to rabbit duodenum muscle at 15 C in a dose-dependent fashion. The inhibitory activity of several macrolides examined did not relate to their antibacterial activity but to their motilin-like activity. A 50% inhibition by EM536, a non-antibacterial erythromycin derivative with the highest motilin-like activity, was obtained at 3-40 nM and little higher than that of non-radioactive motilin (5-6 nM) under the present conditions. The results suggest that erythromycin and its derivatives mimic physiological actions of motilin by acting as agonists for a motilin receptor.
红霉素是大环内酯类抗生素之一，其衍生物已被发现可模拟外源性胃动素（一种胃肠肽激素）的作用。我们发现，一些大环内酯类化合物在15℃时以剂量依赖性方式抑制125I-胃动素与兔十二指肠肌肉的特异性结合。所检测的几种大环内酯类药物的抑制活性与其抗菌活性无关，而与其胃动素样活性有关。在本实验条件下，具有最高胃动素样活性的非抗菌性红霉素衍生物EM536在3-40 nM时产生50%的抑制作用，略高于非放射性胃动素（5-6 nM）。结果表明，红霉素及其衍生物通过作为胃动素受体的激动剂来模拟胃动素的生理作用。
