Cytoprotective activity of deboxamet: a possible interference with prostaglandin and prostacyclin metabolism in rat gastric mucosa.
Deboxamet (5-methoxy-2-methyl-3-indolyl-acetohydroxamic acid) is a new synthetic drug with anti-ulcer and anti-secretory activity. The authors evaluated the ability of deboxamet to protect the rat gastric mucosa against the intensive necroses induced experimentally by absolute ethanol, NaCl (25%), HCl (0.6 N), acetylsalicylic acid plus HCl, and sodium taurocholate plus HCl. Deboxamet, as compared with pirenzepine, sulglycotide and PGE2, displayed a cytoprotective activity against these necrotizing agents. The involvement of deboxamet with prostacyclin metabolism was also investigated. In order to assess the presence of PGI2-like substances, extracts of mucosa from rats treated orally with deboxamet and sulglycotide were assayed i) on isolated rabbit mesenteric artery, ii) for hypotensive effect in anaesthetized rat, and iii) for anti-platelet activity. Deboxamet, like sulglycotide, was able to raise the availability of prostacyclins in the rat gastric mucosa, which is an important action in maintaining its cellular integrity. However, our results cannot determine whether this activity is due to an enhanced biosynthesis or a decreased degradation of prostacyclins.
Franzone
J S
JS
Research Laboratories, Istituto Biologico Chemioterapico ABC, S.p.A., Turin, Italy.
Cirillo
R
R
Cravanzola
C
C
D000818:Animals; D000897:Anti-Ulcer Agents / Q000494:pharmacology*; D001794:Blood Pressure; D002229:Carbenoxolone / Q000494:pharmacology; D011464:Epoprostenol / Q000378:metabolism*; D005753:Gastric Mucosa / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D066298:In Vitro Techniques; D007211:Indoles / Q000494:pharmacology*; D008297:Male; D008638:Mesenteric Arteries / Q000187:drug effects; D009336:Necrosis; D010975:Platelet Aggregation Inhibitors; D011453:Prostaglandins / Q000378:metabolism*; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D012795:Sialoglycoproteins / Q000494:pharmacology
D000897:Anti-Ulcer Agents; D007211:Indoles; D010975:Platelet Aggregation Inhibitors; D011453:Prostaglandins; D012795:Sialoglycoproteins; C009354:sulglicotide; D011464:Epoprostenol; D002229:Carbenoxolone; C058616:deboxamet