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

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.

• Authors: Y Hamagishi, K Kawano, H Kamei, T Oki
• Journal: Japanese journal of pharmacology (Jpn J Pharmacol) Vol. 55 Issue 2 Pg. 283-6 (Feb 1991) ISSN: 0021-5198 [Print] Japan
• PMID: 1648641 (Publication Type: Journal Article)

Chemical References

• Anti-Bacterial Agents
• Lactones
• copiamycin
• Adenosine Triphosphatases
• H(+)-K(+)-Exchanging ATPase
• Sodium-Potassium-Exchanging ATPase

Topics

• Adenosine Triphosphatases (metabolism)
• Animals
• Anti-Bacterial Agents (pharmacology)
• Disease Models, Animal
• Dogs
• Gastric Acid (metabolism)
• Gastric Mucosa (drug effects, enzymology)
• Guinea Pigs
• H(+)-K(+)-Exchanging ATPase
• Kidney (enzymology)
• Lactones (pharmacology)
• Pylorus (surgery)
• Rats
• Rats, Inbred Strains
• Sodium-Potassium-Exchanging ATPase (metabolism)
• Stomach Ulcer (metabolism, prevention & control)
• Swine