Gastric mucosal protection by OPC-12759, a novel antiulcer compound, in the rat

Yamasaki, K.; Kanbe, Toshimi; Chijiwa, Takashi; Ishiyama, H.; Morita, Seiji

doi:10.1016/0014-2999(87)90649-2

Cited by 134 publications

(23 citation statements)

References 26 publications

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“…Thirty minutes after administration of the rice extract, rats were orally administered 30 mg/kg indomethacin dissolved in 3% NaHCO 3 to induce gastric lesions 6. Five hours after the indomethacin treatment, the rats were killed and gastric mucosal lesions were determined as described above.…”

Section: Methodsmentioning

confidence: 99%

“…The aggressive factors, such as increased gastric secretion, increased generation of reactive oxygen species and pro-inflammatory cytokines, and infection with Helicobacter pylori , can cause mucosal damage. Researchers have developed many in vivo gastric ulcer models with different gastropathic mechanisms 6. Among them, the ethanol-, indomethacin-, and water immersion restraint stress (WIRS)-induced models have been used in many studies to screen antiulcer substances,7,8,9 because alcohol, nonsteroidal anti-inflammatory drugs, and stress are major risk factors in human life for peptic ulcers and other gastrointestinal diseases.…”

Section: Introductionmentioning

confidence: 99%

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Gastroprotective Effects of Glutinous Rice Extract against Ethanol-, Indomethacin-, and Stress-induced Ulcers in Rats

et al. 2014

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This study was designed to evaluate the efficacy of an orally administered aqueous extract of glutinous rice (GRE) to protect against acute gastric mucosal lesions induced by ethanol, indomethacin, and water immersion restraint stress in rats and to characterize the active substances responsible for the protection. GRE was shown to dose-dependently prevent the gastric lesions induced by the above ulcerogenic treatments at doses of 30 to 300 mg/kg. GRE treatment increased the gastric mucin content and partially blocked the ethanol-induced depletion of the gastric mucus layer. Also, it increased the nonprotein sulfhydryl concentration in the gastric mucosa. The gastroprotective action of GRE was markedly enhanced by co-treatment with 4-8 mg/kg tea extracts. The activity of GRE was completely lost by heat treatment at 80℃ for 3 min or treatment with 0.01% pepsin at 37℃ for 1 h. Protein extraction studies indicated that prolamins are involved in the gastroprotective activity of GRE. Our results suggest that glutinous rice proteins are useful for the prevention and treatment of gastritis and peptic ulcer.

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Gastroprotective Effects of Glutinous Rice Extract against Ethanol-, Indomethacin-, and Stress-induced Ulcers in Rats

et al. 2014

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“…After its initial discovery, it was used as an agent that promoted the healing of lesions in an experimental rat gastric ulcer model 1,2. Subsequently, in 1990, it was marketed as the Mucosta ® tablet (Otsuka Pharmaceutical Company, Limited) for gastric ulcer therapy 3.…”

Section: Historymentioning

confidence: 99%

Rebamipide ophthalmic suspension for the treatment of dry eye syndrome: a critical appraisal

Kashima¹,

Itakura²,

Akiyama³

et al. 2014

OPTH

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Rebamipide was initially developed and approved for use in treating gastric ulcers and lesions associated with gastritis. Discovery of its ability to increase gastric mucin led to investigations of its effect on ocular surface mucin and the subsequent development for use in dry eye patients. Investigations have confirmed that rebamipide increases corneal and conjunctival mucin-like substances along with improving corneal and conjunctival injury. Clinically, rebamipide ophthalmic suspensions can effectively treat tear deficiency and mucin-caused corneal epithelial damage, and can restore the microstructure responsible for tear stability. Topical rebamipide has also been shown to be effective in treating other ocular surface disorders such as lagophthalmos, lid wiper epitheliopathy, and persistent corneal erosion. Rebamipide’s ability to modify epithelial cell function, improve tear stability, and suppress inflammation in the absence of any known major side effects suggest that it may be a beneficial first drug of choice for severe dry eye treatment and other ocular surface disorders. This review summarizes the history and development of this innovative dry eye treatment from its initial use as an effective stomach medication to its current use in the treatment of dry eye in Japan.

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“…Pre-clinical studies have indicated that rebamipide contributes to the enhancement of the defense mechanism in gastric mucosa, which results from increasing gastric mucus [10,11] and the stimulation of the production of endogenous prostaglandins without gastric acid suppression [12,13]. Rebamipide is known to suppress gastric mucosal inflammation, which is thought to be related to its activity in the inhibition of superoxide anion production from neutrophils [14,15] and scavenging hydroxyl radicals [16,17], and in inhibiting interleukin-8 production [18].…”

Section: Introductionmentioning

confidence: 99%

An Open-Labeled Study of Rebamipide Treatment in Chronic Gastritis Patients with Dyspeptic Symptoms Refractory to Proton Pump Inhibitors

2008

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To assess the efficacy of rebamipide therapy in chronic gastritis patients with refractory dyspeptic symptoms, we enrolled 30 patients with chronic gastritis nonresponsive to the antisecretory medications, proton pump inhibitors. Upper gastrointestinal endoscopy was performed in all patients to confirm and evaluate the severity of gastritis by gastric mucosal injury score and the histology by the updated Sydney system before and after treatment with rebamipide 300 mg daily for 8 weeks. At the end of the study, significant improvement in the scores for symptoms (epigastralgia, stomach heaviness, and abdominal fullness) and endoscopic mucosal injury were observed for all patients. The degrees of neutrophil activity in antrum and mononuclear cell inflammation in both body and antrum significantly decreased from baseline. Improvement of gastritis might be the mechanism by which rebamipide prevents gastric mucosal inflammation. In conclusion, rebamipide treatment improved symptom, endoscopic, and histologic features of chronic gastritis in patients with refractory dyspeptic symptoms.

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Gastric mucosal protection by OPC-12759, a novel antiulcer compound, in the rat

Cited by 134 publications

References 26 publications

Gastroprotective Effects of Glutinous Rice Extract against Ethanol-, Indomethacin-, and Stress-induced Ulcers in Rats

Gastroprotective Effects of Glutinous Rice Extract against Ethanol-, Indomethacin-, and Stress-induced Ulcers in Rats

Rebamipide ophthalmic suspension for the treatment of dry eye syndrome: a critical appraisal

An Open-Labeled Study of Rebamipide Treatment in Chronic Gastritis Patients with Dyspeptic Symptoms Refractory to Proton Pump Inhibitors

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