• Journal of Pharmaceutical Investigation
• /
• 제23권4호
• /
• pp.217-223
• /
• 1993

The combined products of antacid and anti-ulcer agent were prepared with antacid composed of aluminium hydroxide dried gel, magnesium hydroxide and simethicone with a ratio of 1:1:0.1 (M) and anti-ulcer agent, aceglutamide aluminium (AGA). The efficacy of antacid was evaluated in vitro with Fuchs, Johnson-Duncan and Rosset-Rice methods and in vivo using an aspiration method in rat. The addition of anti-ulcer agent did not affect the neutralizing capacity of M significantly. The combined products with the M/AGA ratios of 2.3:1 and 3.4:1 produced the maximum pH of $4.0{\sim}5.8$ and the duration time of $64{\sim}137$ min in vitro test. The in vivo neutralizing test in rats showed the rapid increase of gastric pH up to 3.5 within 30 min and the gastric pH of $4{\sim}6$ was kept for 5 hr.

• Archives of Pharmacal Research
• /
• 제22권2호
• /
• pp.137-142
• /
• 1999

Anti-ulcer activity of newly synthesized acylquinoline derivatives was investigated. For the in vitro screening, the effects of compounds on gastric $H^{+}/K^{+}$ ATPase isolated from hog and rabbit were examined. Among them, AU-090, AU-091, AU-254, AU-413 and AU-466 exhibited good in vitro activity on both enzymes. To correlate the in vitro activity with in vivo action, the effects of the compounds on the basal gastric acid secretion were studied. Some derivatives showed considerable anti-secretory activities, and AU-413 was selected for further studies. AU-413 protected gastric damage induced by either ethanol or NaOH dose dependently when given orally. $ED_{50}$ values of 12 mg/kg, p.o. (ethanol) and 41 mg/kg, p.o. (NaOH) were obtained. In addition, histamine-stimulated gastric secretion was reduced upon AU-413 administration. Taken together, newly synthesized acylquinoline derivatives, especially AU-413, is worthy of further investigation to be developed as an anti-ulcer agent.

• Biomolecules & Therapeutics
• /
• 제14권3호
• /
• pp.171-177
• /
• 2006

Gastritis and gastric ulcer were known to be induced by gastic acid, stress, ethanol, Helicobacter pylori and free radical, etc. This study was performed for the development of a new drug or nutraceutical from medicinal plants or natural products with anti-gastritis, anti-ulcerative and gastroprotective activities. The water extract of Scutellaria baicalensis was exhibited potent inhibition in HCl ethanol-induced gastric lesion, acetic acid-induced and Shay ulcers, indicating the effects on gastric lesion and ulcer in rats. The water extract of Scutellaria baicalensis significantly inhibited HCl ethanol-induced gastric lesions at the oral dose of 300, 500 mg/kg. In pylorus ligated rats, the treatments of the water extract from Scutellaria baicalensis showed decrease in the volume of gastric secretion and acid output and increase pH at oral dose of 300, 500 mg/kg. And significantly reduced acetic acid-induced ulcer at the oral dose of 500 mg/kg for 12 days. In this study, we have found that the water extract from Scutellaria baicalensis had significant improvement in acute gastritis and ulcer at the dose of 300, 500 mg/kg and in chronic gastritis and ulcer at the dose of 500 mg/kg. Also we evaluated the antibacterial activity against Helicobacter pylori treated with Scutellaria baicalensis. Scutellaria baicalensis had a equivalent antibacterial activity with ampicilin against H. pylori at the dose of $100\;{\mu}/ml$. In histological examination, the water extract of Scutellaria baicalensis drastically restored gastric damages induced by HCl ethanol solution, pylorus- ligature and acetic acid. Therefore, we may use the water extract from Scutellaria baicalensis as antigastritic and antiulcerative agent for the purpose of the improvement or treatment of gastritis and gastric ulcer.

• 한국식품영양과학회지
• /
• 제22권4호
• /
• pp.374-380
• /
• 1993

녹차추출액을 사용하여 Sprague Dawley 휜쥐를 63일간 사육한 뒤 십이지장궤양 유발제 cysteamineㆍHCI(400mg/1kg b.w.)을 투여하면 수도물에 의해 같은 기간 사육한 대조군 (TW군) 보다 cysteamine에 대한 감수성은 유의하게 저하되어 십이지장궤양 발병율이 TW군의 50%를 나타냈다. 또한 TW군은 cysteamine투여에 의해 십이지장점막 극재 효소인 alkaline phosphatase (ALP) 활성을 상부십이지장 점막에 있어서 현저하게 저하시켰으나 GT군은 유의하게 활성이 유지되고 ALP 분자종에 있어서도 TW군과 상이한 양상을 나타내 녹차 추출액이 cysteamine 궤양에 있어서 항 궤양적 생리활성을 발휘하고 있는 사실이 밝혀졌다.

• Journal of Microbiology and Biotechnology
• /
• 제21권4호
• /
• pp.400-404
• /
• 2011

Indomethacin is a nonsteroid anti-inflammatory agent that is known to induce severe gastric mucosal lesions. In this study, we investigated the effect of selenium on gastric mucosal lesions in rats. To confirm the curative effect of selenium against indomethacin-induced gastric ulcers, gastric ulcers were induced by oral administration of 25 mg/kg indomethacin, and then different doses (10, 50, and 100 ${\mu}g$/kg of body weight) of selenium or vehicle were treated by oral gavage for 3 days. Oral administration of indomethacin clearly increased the gastric ulcer area in the stomach, whereas selenium applied for 3 days significantly decreased the gastric ulcer area in a dose-dependent manner. In addition, selenium markedly reduced the increase of lipid peroxidation induced by indomethacin in the gastric mucosa and increased activities of radical scavenging enzymes such as superoxide dismutase, catalase, and glutathione peroxidase in a dose-dependent manner. These results reveal that selenium can heal indomethacin-induced gastric ulcers through elimination of the lipid peroxides and activation of radical scavenging enzymes.

• International Journal of Industrial Entomology and Biomaterials
• /
• 제35권1호
• /
• pp.14-21
• /
• 2017

Gastric ulcer is a clinical symptom characterized by inflammation of the gastric mucosa. Stress and alcohol consumption have been identified as the major cause of gastric ulcer. However, the effects of silkworms on ethanol-induced gastric ulcer have not been studied yet. The mature silkworms that are difficult to eat have become easier to ingest due to recent technological development to make steaming and freeze-drying mature silkworm larval powder (SMSP). In this study, we investigated whether three silkworm varieties, Baekokjam, Golden-silk and Yeonnokjam could alleviate ethanol-induced gastric mucosal damage in vivo. Sprague-Dawley rats pretreated with 3 SMSPs (0.1 or 1 g/kg BW) or normal diet (AIN-76A) were exposed to absolute ethanol (3 g/kg BW, 3 h) by oral gavage. Morphological examination included ulcer index as a measurement of hemorrhages and hematoxylin and eosin staining was performed to analyze the severity of gastric ulcer. Results of macroscopic examination suggested that all 3 SMSPs pretreatment significantly protected gastric mucosa against ethanol-induced damage. Microscopic observations demonstrated significant mucosal erosion and inflammation in ethanol-treated rats, which was abrogated in rats pretreated with 3 SMSPs. In addition, pretreatment with all 3 SMSPs showed significant decreases the expression of pro-inflammatory mediators, IL-6 and cyclooxygenase-2. Among SMSP from 3 varieties of silkworm, preadministration of 1 g/kg Baekokjam SMSP showed the most effective protective effect against ethanol-induced gastric ulcer. These results suggest that Baekokjam SMSP can be a potential gastroprotective agent against ethanol-induced gastric ulcer.

• 한국수산과학회지
• /
• 제33권6호
• /
• pp.520-523
• /
• 2000

Alginate를 가열에 의해 저분자화하여 저분자화에 따른 위점막 보호작용을 검토하기 위해 랫드에 있어서 저분자 alginate인 HAG-10, HAG-50, HAG-100 및 alginate의 투여 가 $HCl{\cdot}ethanol$ 용액과 침수스트레스에 의해 유발되는 위손상과 위궤양의 억제효과에 미치는 영향을 광학현미경으로 점막의 형태를 관찰하면서 그 억제율과 조직학적 변화를 측정하였다. $HCl{\cdot}ethanol$ 용액과 침수스트레스에 의해 유발되는 위손상과 위궤양에 대한 억제효과에 미치는 저분자 alginate의 영향을 검토한 결과, 그 억제효과는 alginate에서 가장 높았고, 다음으로 HAG-50과 HAG-100 및 HAG-10의 순으로 HAG-50, HAG-100 및 alginate에서 현저한 효과를 보였으나, HAG-10은 아무런 효과를 나타내지 않았다. 위손상과 위궤양점막을 광학현미경으로 관찰해 볼 때, 대조군과 HAG-10에서는 위점막 전체에 걸친 출혈과 부식에 의한 응고괴사가 진행되었고 점막 (粘膜)과 점막근판 (粘膜筋板) 및 근육층 (筋肉層)에 부종의 발생과 조직의 파괴가 일어났으나 HAG-50, HAG-100 및 alginate에서는 가벼운 병변이 진행되어 위점막층에 약간의 출혈만 관찰되어 위손상억제 및 위궤양 억제효과를 뚜렷히 나타내었다.

• 약학회지
• /
• 제17권1호
• /
• pp.1-8
• /
• 1973

The pharmacological activities of paeoniflorin abtained from paeony roots, F$_M$100 from glycyrrhiza roots, crude saikosides from bupleurum roots, crude platycodin from platycodon roots, and bothj of ginsenoside Rb and ginsenoside Rg series from ginseng roots were investigated. Paeoniflorin, F$_M$ 100, crude saikosides, and crude platycodin exhibited sedative antipyretic, anlagesic and anti-ulcerative actions. In addition, crude saidosides and crude platycodin showed antitusaive and the potent anti-inflammatory action. An expectorant action was also observed with crude platycodin. These results coincided with the clinical applications of the aforementioned oriental medicinals. It also should be noted that crude saikosides nad crude platycodin are preferable to the other steroidal nad nonsteroidal drugs as an anti-inflammatory agent, because the drugs aggravate the digestive ulcer. In ginseng, G No3. and GNS frctions out of ginsenoside Rb series hsowed stimulant and antifatigue actions. The synergistic effects identified between paeoniflorin and F$_M$ 100 on the various pharmacological activities, have verified the reasonability of combined uses of two oriental drugs as Jakyak Gaqmcho-Tang.

• 약학회지
• /
• 제39권2호
• /
• pp.153-160
• /
• 1995

Receptor binding study was carried out as an in vitro assay to test the anti-ulcer effect for newly synthesized test compounds(IY-80843 and IY-80845) which were reported to have a strong anti-secretory effect in Shay-ligated rats. The histamine H$_{2}$-receptor fraction was prepared from the membranes of the isolated gastric glands in guinea pigs and $^{3}$H-cimetidine was used as a radioligand. The binding of $^{3}$H-cimetidine to the membranes of the isolated gastric glands was found to be time dependent, saturable and confined to a single population of binding sites with $K_{D}$ value of 0.13$\pm$0.03 $\mu{M}$ and B$_{max}$ value of 52.5$\pm$1.5 pmol/mg. From the competition experiments, both IY-80843 and IY-80845 were shown to have a strong blocking effect against binding of $^{3}$H-cimetidine to the histamine H$_{2}$-receptor. The IC$_{50}$, Ki, and Hill coefficient(nH) values for IY-80843 were 0.18$\pm$0.02 $\mu{M}$, 0.16$\pm$0.02 $\mu{M}$, and 0.97$\pm$0.15, respectively and those values for IY-80845 were 0.27$\pm$0.02 $\mu{M}$, 0.24$\pm$0.02 $\mu{M}$, and 0.82$\pm$0.13, respectively. The results demonstrated that the blocking effects of IY-80843 and IY-80845 were 7 and 5 times stronger than that of cimetidine, respectively. Therefore, the newly synthesized compounds, IY-80843 and IY-80845, appeared to be the highly potent competitive inhibitors of histamine on the H$_{2}$-receptor.

• 사상체질의학회지
• /
• 제9권2호
• /
• pp.227-243
• /
• 1997

The experimental study used in this paper was done to examine the clinical effects of Taeumchowetang for the gastric ulcer and the function of gastrointestinal tract using rats and mice which were administered orally the water extraction from Taeumchowetang. Then, the counter-action of the water extraction on the isolated ileum and gastric fundus, the inhibitory effects of pylorus-ligated ulcer and indomethacin-induced ulcer, the associations with gastric juice secretion, total acidity, pepsin output, the transportability in the small and large intestine, were studied with administering acetylcholine chloride and barium chloride. In addition, it was investigated whether the central nervous system related to pain control and sleeping time was influenced by Taeumchowetang. The following results have been obtained; 1. As resulting from injection of acetylcholine chloride and barium chloride into the isolated ileum of rats and mice, Taeumchowetang led to have an inhibitory effect on the muscle contraction of the ileum. Then, acetylcholine chloride was measured as lower effect than barium chloride 2. For the inhibitory effect on contraction for the gastric fundus strip in rats by either acetylcholine chloride or barium chloride, the one showed low inhibitory effect, on the other hand the other showed density-dependent effect. 3. The water extraction was given on the pylorus ligated ulcer with using two different administration groups of 1,300mg/kg and 2,600mg/kg, each result was measured as 22.9% and 36.5% for an ulcerous inhibitory effect (p<0.05). 4. According to the two administration groups, the preventive effect was tabulated 18.1% and 29.3% for indomethacin-induced ulcer (p<0.05, P<0.01). 5. For associations with gastric juice secretion, total acidity, pepsin output in the administration group 2,600mg/kg, Taeumchowetang was recognized as having an inhibitory effects related to suppressive actions involving gastric juice secretion(p<0.05), and free acidity(p<0.01), but there was no significant association with total acidity and pepsin output. 6. To know the transportability in the intestine, BaSO4 solution was used. The transportability of the small intestine in the administration group 2,600mg/kg was 22.2% which was statistically significant compared with the large intestine's transportability(P<0.01). 7. In the administration group 1,300mg/kg and 2,600mg/kg, analgesic effect with against acetic acid was measured as being 16.8% and 24.4% which was shown as statistically siginificant(p<0.01). 8. No statistically significant association between Taeumchowetang and sleeping time was found in both 1,300mg/kg and 2,600mg/kg by administering phenobarbital-Na. According to the results of this study, Taeumchowetang has agreed with the effects of literature review. Further more in this study, Taeumchowetang also has preventive effects on pylorus-ligated ulcer. Hence, Teaumchowetang can be significant effect such as both anti ulcer agent and increasing gastric activity for the patients who suffer from gastric ulcer.