sofalcone and Peptic-Ulcer

Topics: Anti-Inflammatory Agents, Non-Steroidal; Anti-Ulcer Agents; Bicarbonates; Carnosine; Chalcone; Chalcones; Diterpenes; Enprostil; Gastric Mucosa; Helicobacter Infections; Helicobacter pylori; Humans; Mucus; Organometallic Compounds; Peptic Ulcer; Piperidines; Prostaglandins; Sucralfate

Topics: Amoxicillin; Anti-Ulcer Agents; Chalcone; Chalcones; Clarithromycin; Drug Resistance, Bacterial; Drug Therapy, Combination; Helicobacter Infections; Helicobacter pylori; Humans; Omeprazole; Peptic Ulcer; Treatment Outcome

Topics: Anti-Ulcer Agents; Catechin; Chalcone; Chalcones; Flavonoids; Humans; Peptic Ulcer; Plants

The mucoprotective agents, sofalcone and polaprezinc have anti-Helicobacter pylori (H pylori) activities. We determined the therapeutic effects of sofalcone and polaprezinc when combined with rabeprazole, amoxicillin and clarithromycin for Helicobacter pylori infection.. One hundred and sixty-five consecutive outpatients with peptic ulcer and H pylori infection were randomly assigned to one of the following three groups and medicated for 7 d. Group A: triple therapy with rabeprazole (10 mg twice daily), clarithromycin (200 mg twice daily) and amoxicillin (750 mg twice daily). Group B: sofalcone (100 mg thrice daily) plus the triple therapy. Group C: polaprezinc (150 mg twice daily) plus the triple therapy. Eradication was considered successful if (13)C-urea breath test was negative at least 4 wk after cessation of eradication regimens or successive famotidine in the cases of active peptic ulcer.. On intention-to-treat basis, H pylori cure was achieved in 43 of 55 (78.2%) patients, 47 of 54 (87.0%) and 45 of 56 (80.4%) for the groups A, B and C respectively. Using per protocol analysis, the eradication rates were 81.1% (43/53), 94.0% (47/50) and 84.9% (45/53) respectively. There was a significant difference in the cure rates between group A and B. Adverse events occurred in 10, 12 and 11 patients, from groups A, B and C respectively, but the events were generally mild.. The addition of sofalcone, but not polaprezinc, significantly increased the cure rate of H pylori infection when combined with the rabeprazole-amoxicillin-clarithromycin regimen.

Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Adult; Aged; Amoxicillin; Anti-Bacterial Agents; Anti-Ulcer Agents; Benzimidazoles; Chalcone; Chalcones; Clarithromycin; Drug Therapy, Combination; Female; Gastric Mucosa; Helicobacter Infections; Helicobacter pylori; Humans; Male; Middle Aged; Omeprazole; Peptic Ulcer; Rabeprazole

To assess the effects of the mucoprotective drug sofalcone, which has direct and indirect effects on Helicobacter pylori in vitro, the eradication rate, adverse effects, and the quality of healing peptic ulcers were evaluated. Each study patient was given 500 mg t.i.d. amoxicillin and 200 mg t.i.d. clarithromycin. In addition, three different treatment regimens were compared: a standard dose (20 mg q.d.) of the proton pump inhibitor omeprazole (OAC), a double dose (20 mg b.i.d.) of omeprazole (Ox2AC), and a standard dose of omeprazole and a standard dose (100 mg t.i.d.) of sofalcone (OACS). Thirty-one H. pylori-positive patients were treated with OAC, 37 with Ox2AC, and 41 with OACS therapy. With an intention-to-treat analysis, the eradication rates were 74.2% for OAC, 86.2% for Ox2AC, and 85.0% for OACS therapy. The incidence of side effects was 9.6% for patients given OAC therapy, 86.5% for Ox2AC, and only 7.5% for OACS-treated patients, which was significantly lower than the incidence in the Ox2AC group. High-quality peptic ulcer scars were observed after eradication therapy which included solfacone. Although it is necessary to conduct a randomized double-blind study to obtain definitive conclusions, our results indicate that this novel quadruple eradication therapy with solfacone is an efficacious regimen with a high eradication rate and positive effects on ulcer healing, combined with a low incidence of adverse events.

Topics: Adolescent; Adult; Aged; Amoxicillin; Anti-Bacterial Agents; Anti-Ulcer Agents; Chalcone; Chalcones; Clarithromycin; Drug Therapy, Combination; Endoscopy, Gastrointestinal; Female; Helicobacter Infections; Helicobacter pylori; Humans; Male; Middle Aged; Omeprazole; Penicillins; Peptic Ulcer; Treatment Outcome

Solon, a synthetic isoprenyl flavonoid derived from sophoradin isolated from the root of an ancient Chinese plant, administered orally to rats, prevented, dose-dependently, the formation of acute gastric lesions produced by absolute ethanol given orally. Solon also enhanced the healing of chronic gastric and duodenal ulcerations induced by the serosal application of acetic acid. The gastroprotective action of Solon was probably mediated by increased mucosal content of prostaglandins (PG) due mainly to the inhibition of 15-OH-prostaglandin dehydrogenase. The ulcer-healing action of Solon was probably related to the stimulation of mucus-alkaline secretion, increased mucosal blood flow and the formation of a protective barrier on the ulcer base.

Topics: Acetates; Acetic Acid; Animals; Anti-Ulcer Agents; Bicarbonates; Chalcone; Chalcones; Dinoprostone; Ethanol; Gastric Acid; Gastric Mucosa; Male; Pancreas; Peptic Ulcer; Propiophenones; Prostaglandins E; Rats; Rats, Inbred Strains; Regional Blood Flow; Stomach Ulcer

A study was made on changes in the gastric mucosal prostaglandin (PGE2) at the time of onset of stress ulcer in view of the association between those changes and the blood flow of the gastric mucosa, and further study was performed on the preventive effect of pGE2 and carboxymethoxy-4,4'-bis (3-methyl-2-butenyloxy) chalcone (hereinafter referred to as SU-88) administered to the enthetic cases. When the control rats were loaded with water immersion stress, a noticeable decline of as much as about 50% was seen in the blood flow of gastric mucosa in 2 hours, and simultaneously a decrease was recognized in the quantity of the gastric mucosal pGE2 approximately 32%. On the other hand, these changes are controlled in the vagotomized rats. In comparison with vagotomized rats, a decline was seen in the gastric mucosal PGE2 while an increase was observed in it in the rats with the vagus nerves stimulated by bethanechol. In the dehemotized (24 ml/kg) rats and the rats loaded with water immersion stress, a decline was seen in the synthesis of the gastric mucosal pGE2. Administration of PGE2 and SU-88 before the loading of stress suppressed an increase in the quantity of the gastric mucosal pGE2 and the blood flow of the gastric mucosa.

Topics: Animals; Chalcone; Chalcones; Dinoprostone; Gastric Mucosa; Immersion; Male; Peptic Ulcer; Prostaglandins E; Rats; Rats, Inbred Strains; Stomach; Stress, Physiological; Vagotomy

Effect of 2'-carboxymethoxy-4,4'-bis(3-methyl-2-butenyloxy)chalcone (SU-88), a new anti-ulcer drug, on gastric tissue blood flow was investigated by using an inhaled hydrogen gas clearance method in rats. As a result, following the intravenous infusions of 10,20 and 30 mg/kg/h of SU-88, the gastric blood flow increased with an increase rate of 38.1, 70.5 and 61.7% as compared with the control value, respectively. Following the intraperitoneal administrations of 50 and 100 mg/kg of SU-88, the gastric blood flow increased by 59.8 and 51.2%, respectively, immediately after the administration.

Topics: Animals; Anti-Ulcer Agents; Autonomic Nervous System; Chalcone; Chalcones; Injections, Intravenous; Male; Peptic Ulcer; Propiophenones; Rats; Rats, Inbred Strains; Regional Blood Flow; Stomach