• Advances in Traditional Medicine
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• 제9권3호
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• pp.238-244
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• 2009

Gymnosporia rothiana (walp) Lawson (celastraceae), commonly known as Maytenus rothiana, is used in Indian folk medicine as an antiulcerogenic agent. However, there have been no scientific reports regarding its antiulcer activity. Therefore, this study was intended to evaluate the antiulcer property of petroleum ether, chloroform, and methanolic extract of leaves of Gymnosporia rothiana at different dose levels in ethanol induced and indomethacin induced gastric ulcer models. It was observed that oral administration of all the extract of Gymnosporia rothiana produces significant reduction in ulcer lesion index as well as increase in volume and pH of gastric content in both experimental models, being petroleum ether extract the most effective at dose of 250 mg/kg; it significantly reduced gastric lesion index (70.06%), in comparison to omeprazole (71.20%) and methanolic extract at a dose of 500 mg/kg (67.22%). Increased gastric mucosal defense mechanism by petroleum ether extract is probably due to its high levels of terpenoids like $\beta$ amyrin, lupeol acetate. The present results clearly shows antiulcer effect of Gymnosporia rothiana against various irritants has been mainly due to cytoprotective effect mediated through prostaglandin and partly due to free radical scavenging activity.

• Biomolecules & Therapeutics
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• 제7권4호
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• pp.362-370
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• 1999

Propolis, a natural resinous compound collected from honey bees, contains many biochemical constituents(wax, flavonoids, phenolic compounds, etc.) and has been used in traditional medicines as early as 300 B.C. It was been demonstrated that ethanol, acetylsalicylic acid, ischemia reperfusion, non-steroidal antiin-flammatory drugs and stress induce gastric lesions by promoting the generation of reactive oxygen metabolites. Therefore, some drugs that are capable of scavenging or inhibiting the generation of reactive oxygen radicals might be expected to prevent the gastric mucosal injury. The aim of this study was 1) to examine the antiulcer effect of propolis, 2) to investigate the mechanism of action by determining gastric acid secretion, lipid per-oxidation, mucus content and proton pump ($H^+$/$K^+$-ATPase) activity on gastric mucus in varios experimental models, and finally, 3) to isolate and identify the pure compounds that exert antiulcer activity. Step 2-1 and 2-3 sub-sub fraction shoed a significant reduction of severity of gastirc damage at the dose of 25 mg/kg in various experimental models. We isolated 4 sub-sub-sub fractions by flash column chromatography of Step 2-1 sub-sub fraction and one sub-sub-sub fraction by recrystalization of Step 2-3 sub-sub fraction. The protective effects of propolis sub-sub-sub fraction manifested sifnificant effects in HCl-ethanol induced gastric erosion model and aspirin induced gastric ulcer model. These results showed that the gastric mucosal protective effect of propolis might result from the increase of mucus secretion, free radical scavenging effect as well as the reduction of acid secretion in accordance with the reduction of $H^+$/$K^+$-ATPase activitv. Three compounds were isolated and identified from sub-sub fraction of propolis which showed antiulcer effects. Subsequently, these compounds were identified as a flavonoid, namely, 2-acetoxy-5,7,-dihydroxy-flavanone, galangin and chrysin.

• Biomolecules & Therapeutics
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• 제4권3호
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• pp.285-290
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• 1996

This study was designed to determine the effect of newly synthesized antiulcer agent, 5-pyrrolyl-6-halo-2-(pyridyl-2-methylthio)benzimidazole derivatives (IY-81233), on various experimental ulcers and on the secretion of prostaglandin $E_2(PGE_2)$ into the gastric lumen of rat. IY-81233 was previously reported to have a strong inhibitory effect on $H^+/K^$-ATPase and on gastric acid secretion in rats. Oral administration of IY-81233 at concentrations of 0.2, 2.0, and 20 mg/kg inhibited gastric lesions and duodenal ulcer induced by indomethacin, HCI-ethanol, water-immersion stress, cysteamine, and acetic acid in a dose dependent manner. Their IC$IC_{50}$ values were 3.4, 1.4, 0.8, 1.3, and 1.2 mg/kg, respectively. These results indicate that IY-81233 is a potent antiulcer agent although it is slightly less potent than omeprazole in healing of gastritis and ulcers. The secretion of $PGE_2$ into gastric lumen was also investigated in relation to the cytoprotective effect by IY-81233 in rats. The $PGE_2$ level was not changed significantly by an oral administration of IY-81233, suggesting that IY-81233 has little effect on the gastric protection. Therefore, it can be concluded that IY-81233 exerts prominent antiulcer activity by suppressing gastric acid secretion via an inhibition of a proton pump and not by protecting the gastrointestinal mucosa against various ulcerative stimuli.

• Biomolecules & Therapeutics
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• 제4권4호
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• pp.354-363
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• 1996

This study was conducted to investigate the repeated dose toxicity of DA-9601, an antiulcer agent of Artemisia app. extract, in rats. DA-9601 was administered orally once a day for 4 weeks to 10 males and 10 females per group at doses of 0(vehicle control), 125, 500 or 2000 mg/kg/day. Throughout the study, no treatment-related deaths and clinical signs were observed. In female rats receiving 125 mg/kg of DA-9601, water consumption increased slightly on day 4, 11 and 25. Hematological examination showed a decrease of MCV and an increase of PLT in male rats at the doses of 500 and 2000 mg/kg groups. Blood biochemistry revealed slight decreases of cholesterol, BUN and Na in male rats and decreases of total bilirubin and creatinine and slight increases of globulin and Cl in female rats. The organ weights at the end of 4 weeks showed slight changes in some organs of treated groups. But, all these changes were not considered to be of toxicological importance, because they did not show dose-response relationship and relevance to gross and microscopic findings. Histopathologically, abnormal treatment-related changes were not observed in any organ and target organs were not detected. On the basis of these results, the NOAEL(no-observed-adverse-effect level) of DA-9601 was estimated to be more than 2000 mg/kg/day under the conditions tested.

• Biomolecules & Therapeutics
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• 제4권2호
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• pp.111-121
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• 1996

Antiulcer effects of Artemisia herba extract (DA-9601) were evaluated in various types of experimental gastric ulcer induced in rats. And the effects of DA-9601 on mucus, basal and stimulated gastric acid secretion were also investigated in rats. DA-9601 (12.5∼400 mg/kg, p.o.) prevented the formation of gastric ulcers induced by 60% EtOH in 150 mM HC1, restraint water immersion stress, platelet activating factor (PAF), aspirin in 150 mM HCI with Pylorus-ligation and indomethacin. DA-9601 (4∼400 mg/kg, p.o.) significantly accelerated the healing rate of acetic acid-induced gastric ulcer and significantly stimulated mucus secretion in a dose-dependent manner. DA-9601 (20∼200 mg/kg, i.d.), however, did not inhibit basal gastric acid secretion in pylorus ligated rats and DA-9601 (200 mg/kg, i.d.) failed to influence histamine-, pentagastrin- and carbachol- stimulated gastric acid secretion. These results suggest that DA-9601 has inhibitory action on gastric lesion and ulceration through increasing mucus secretion in the stomach of rats without influencing basal and stimulated gastric acid secretion.

• Biomolecules & Therapeutics
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• 제5권3호
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• pp.246-252
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• 1997

This study was performed to evaluate antiulcer effects of traditional folk medicines such as heat-treated acumen, halloysitum rubrum and os sepiae against stomach ulcer induced by acetic acid in Sprague-Dawley rats. Various pharmacological parameters were utilized to compare the antiulcer effects of aforementioned drugs based on the size of ulcer lesion, pepsin activity, free and total acidity, gastric secretory volume, and 5-HT (hydxoytrytamine) content. All folk medicines and ranitidine as control drus were shown to decrease ulcer lesion size after 5-day treatments, with the order of halloysitum rubrum, os sepiae, heat-treated acumen and ranitidine. All treated drugs except os sepiae inhibited the gastric volume as compared with that in the control group. Ranitidine most significantly inhibited the gastric volume. All the experimented drugs in this study lowered the gastric acidity. Halloysitum rubrum decreased it most remarkably, followed by ranitidine, os sepiae and heat-treated alumen after 5-day treatments. All used drugs alleviated the pepsin activity as compared with the control group, os sepiae being the highest then halloysitum rubrum, heat-treated alumen and ranitidine in turn. Heat-treated alumen and halloysitum rubrum showed mucin production to the great extent, and ranitidine had slight increasing effect thereon. At the end of observation period, all drugs except ranitidine increased 5-HT contents as compared to the normal group. From the above results, we could confirm the folk medicines such as heat-treated alumen, halloysitum rubrum and os sepiae have not only remarkable antiulcer effects but also preventing effects for the stomach ulcer recurrence, which suggest the experimented folk medicines could be developed as new antiulcer agents.

• 동의생리병리학회지
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• 제16권3호
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• pp.572-576
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• 2002

Banhasasim-tang(半夏瀉心湯), oriental medicine, has been used for the treatment of the gastric diseases and cimetidine, H2-receptor blocker, has been also used as the gastric ulcer remedy but has some side action. Therefore the concurrent administration of these two drugs may increase antiulcer activities and also decrease cimetidine's side action more than administrating one by one. In order to investigate antiulcer activities, some experiments were conducted. The concurrent administration of Banhasasim-tang extract(BS) and cimetidine(CM) given intraperitoneally (CM 50mg/kg + BS 300mg/kg and CM 50mg/kg + BS 500 mg/kg), significantly inhibited Shay, aspirin and indomethacin ulcers in rats.

• 한국식품위생안전성학회지
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• 제14권4호
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• pp.358-364
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• 1999

벌집으로부터 채취한 수지상의 물질인 propolis는 다양한 생화학적 성분을 함유하며 기원전 300년부터 사용되어 온 전통약물이다. 최근 항균, 항 바이러스, 항진균, 국소마취, 면역 활성, 항염, 항산화 작용등의 생물학적 활성이 보고된 바 있다. 본 연구에서는 위염과 위궤양에 미치는 propolis추출물과 분획물의 약조학적 효과를 평가하고자 에탄올 추출물을 hexane, toluene, ethyl acetate로 분획하여 항위염 및 항위궤양 활성을 조사하였다. Propolis 에탄을 추출물은 염산·에탄을 위손상, Shay의 위액 분비 실험에서 용량 의존적인 보호효과를 나타내었고 hexnae과 toluene 분획물은 염산·에탄을 위손상, aspirin에 의한 위손상, Shay의 위액 분비 실험에서 위손상과 위액분비를 감소시켰다. propolis 추출물과 분획물의 위염 및 위궤양에 대한 보호효과는 H+/K+ATPase activity의 억제에 의한 위액분비의 감소에 의한 것으로 생각된다.

• 대한한의학회지
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• 제15권2호
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• pp.184-197
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• 1994

In order to investigate the effects of Kamikwakjeongtang by using the experimental animals. the action on gastrointestinal smooth muscles. the action of gastric juice secretion, the action of antiulcer. the transport ability of intestinal contents. the action of anticatharsis and the actions on the central nervous system were studied. The results were as follow: 1. Spontaneous motility of the isolated ileum of mice was suppressed and antiacetylcho-line chloride action was recognized. 2. Anti-action on barium chloride of fundus-strip of white rat was recognized. 3. Supression effects on gastric juice secretion. free acidity was recognized. 4. Preventive effect on the ulcer induced by pylorus-ligated was recognized. 5. Supression effects of large intestinal transport ability was recognized. 6. Anti-carthartic action was shown but was not recognized. 7. Analgesic effect by the acetic-acid method and prolonged effect of the total sleep time by pentobarbital-Na were recognized. According to the above results, effects based on oriental medical reference were consistent with the actual experimental effects.

• 한국산학기술학회:학술대회논문집
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• 한국산학기술학회 2009년도 춘계학술발표논문집
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• pp.607-611
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• 2009

Stomach ulcer is the sickness with high frequency of occurrence at the digestive organs and is usually induced by a disproportion of an aggressive factor and a defense factor. To find the medicines having comparative effect to $Stillen^{(R)}$ currently on sale, we screened SHI-7004 and carried out following experiments; Effects of HCl-EtOH induced gastric lesions measuring test, Acid-Neutralizing Capacity, DPPH antioxidation activity, effect of stomach glands secrection. We can suggest that this herbal medicines could be a promising drug for the treatment of gastrc ulcers.