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

  • Jpn J Pharmacol. 1991 Feb;55(2):283-6. doi: 10.1254/jjp.55.283.
Y Hamagishi  1 ,  K Kawano ,  H Kamei ,  T Oki
Affiliations
  • 1. Bristol-Myers Squibb Research Institute, Tokyo, Japan.
PMID: 1648641 DOI: 10.1254/jjp.55.283
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.

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