大环内酯类抗生素共霉素A对胃H⁺，K⁺-ATP酶、胃酸分泌及溃疡形成的抑制作用。

Inhibitory effects of copiamycin A, a macrocyclic lactone antibiotic, on gastric H+,K(+)-ATPase, acid secretion and ulcer formation.

作者信息

Hamagishi Y, Kawano K, Kamei H, Oki T

机构信息

Bristol-Myers Squibb Research Institute, Tokyo, Japan.

出版信息

Jpn J Pharmacol. 1991 Feb;55(2):283-6. doi: 10.1254/jjp.55.283.

DOI:10.1254/jjp.55.283

PMID:1648641

Abstract

When 17 macrocyclic lactone antibiotics were examined for their abilities to inhibit gastric H+,K(+)-ATPase, copiamycin A was found to have the strongest and relatively specific activity with IC50s of 15.7 micrograms/ml and greater than 100 micrograms/ml against the hog gastric H+,K(+)-ATPase and the dog kidney Na+,K(+)-ATPase, respectively. Furthermore, this antibiotic inhibited the histamine-induced gastric acid secretion in the isolated gastric mucosal membrane of guinea pigs and the gastric ulcer formation in pylorus-ligated rats.

摘要

当检测17种大环内酯类抗生素抑制胃H⁺，K⁺-ATP酶的能力时，发现副霉素A具有最强且相对特异的活性，对猪胃H⁺，K⁺-ATP酶和犬肾Na⁺，K⁺-ATP酶的半数抑制浓度（IC50）分别为15.7微克/毫升和大于100微克/毫升。此外，这种抗生素抑制豚鼠离体胃黏膜中组胺诱导的胃酸分泌以及幽门结扎大鼠的胃溃疡形成。