Inhibitory Effects of Copiamycin A, a Macrocyclic Lactone Antibiotic, on Gastric H+, K+-ATPase, Acid Secretion and Ulcer Formation

Yasutaro Hamagishi; Kimio Kawano; Hideo Kamei; Toshikazu Oki

doi:10.1254/jjp.55.283

The Japanese Journal of Pharmacology

Online ISSN : 1347-3506
Print ISSN : 0021-5198
ISSN-L : 0021-5198

Inhibitory Effects of Copiamycin A, a Macrocyclic Lactone Antibiotic, on Gastric H⁺, K⁺-ATPase, Acid Secretion and Ulcer Formation

Yasutaro Hamagishi, Kimio Kawano, Hideo Kamei, Toshikazu Oki

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JOURNAL FREE ACCESS

1991 Volume 55 Issue 2 Pages 283-286

DOI https://doi.org/10.1254/jjp.55.283

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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 μg/ml and > 100 μg/ml against the hog gastric H⁺, K⁺-ATPase and the dog kidney Na⁺, K⁺-APTase, 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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