n-acetylcarnosine and Stomach-Ulcer

Effects of CL-1700 (N-acetyl-L-carnosine aluminum) and its constituents, L-carnosine, N-acetyl-L-carnosine and Al(OH)3 on acute or chronic gastric lesions in intact rats and on gastric secretion in pylorus-ligated rats were studied. CL-1700 at 600 or 1,000 mg/kg p.o markedly inhibited Shay ulcers or indomethacin-induced erosions, but its constituents at the doses contained in CL-1700 did not. Also, CL-1700 at 300 mg/kg i.p. significantly inhibited water-immersion stress-induced erosions, but its constituents did not. CL-1700 at 600 mg/kg i.p. and Al(OH)3 at 143 mg/kg i.p. significantly inhibited Shay ulcers. CL-1700 at 1,000 mg/kg p.o. almost completely inhibited aspirin- or histamine-induced erosions, but both L-carnosine at 639 mg/kg p.o. and N-acetyl-L-carnosine at 817 mg/kg p.o. also markedly inhibited the formation of erosions. CL-1700 at 1,000 mg/kg p.o. increased the volume and raised the pH value, and the agent at 600 mg/kg i.p. reduced the acid output. CL-1700 at 1,000 mg/kg/day p.o. given twice daily for 3 weeks diminished the size of acetic acid ulcers and significantly increased the number of rats with healed ulcers.

Topics: Aluminum Hydroxide; Animals; Anti-Ulcer Agents; Aspirin; Carnosine; Dipeptides; Gastric Juice; Histamine; Humans; Indomethacin; Male; Rats; Stomach Ulcer; Stress, Psychological

Effects of a newly synthesized compound, N-acetyl-L-carnosine aluminum (CL-1700), on the formation of various types of acute gastric lesions were studied in rats. CL-1700 at 300 or 1,000 mg/kg (p.o.) significantly inhibited Shay ulcers and water-immersion stress- and aspirin-induced erosions in pylorus-ligated rats, and indomethacin- or phenylbutazone-induced erosions. CL-1700 had a weak effect on water-immersion stress-induced erosions in rats with an intact pylorus. CL-1700 at 100 or 300 mg/kg (i.p.) significantly inhibited Shay ulcers and water-immersion stress-induced erosions in rats with an intact pylorus. However, this compound (i.p.) had no effect on aspirin- and indomethacin-induced gastric erosions. CL-1700 at 1,000 mg/kg (i.d.) significantly reduced the gastric acid output in pylorus-ligated rats but at 300 or 1,000 mg/kg (p.o.) increased the volume, pepsin output and raised the pH value. The effects of CL-1700 on experimental gastric lesions were slightly weaker than those of aluminum sucrose sulfate but almost equal to or better than those of cimetidine. However, the effects of CL-1700 were much more potent than those of gefarnate. As CL-1700 appears to be a promising new anti-gastric lesion agent, the mechanisms of action are now under investigation.

Topics: Animals; Anti-Ulcer Agents; Aspirin; Carnosine; Dipeptides; Gastric Mucosa; Indomethacin; Male; Phenylbutazone; Rats; Rats, Inbred Strains; Stomach; Stomach Ulcer; Stress, Physiological