• 대한한방내과학회지
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• 제15권2호
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• pp.27-36
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• 1994

In order to investigate the effect of BODUOPAE-SAN(BOS), experiments were performed on analgesic effect induced by acetic acid, duration of hypnosis induced by pentobarbital-Na in mice and gastric ucler in Shay rats and indomethacin induced gastric ulcer, HCI-ethanol induced gastrci lesion in rats and gastric juice secretion in Shay rats. The results are as followings. 1. BOS showed significantly an analgesic effect induced by acetic acid. 2. BOS prolonged the duration of hypnosis induced by pentobarbital-Na in rats 3. BOS rised the spontaneous motility of isolatied ileum of mice temporarily. 4. BOS depressed the gastric motility of rats significantly. 5. BOS showed an anti-ulcer effect in Shay rats and indometacine-induced ulcer rats significantly. 6. BOS reduced the ulcer index of the HCl-ethanol induced gastric lesion in rats. 7. BOS reduced the gastric juice secretion in Shay rats. From above results think BOS is more effective in comparison to the OPAESAN alone on gastrointestinal disorder.

• The Korean Journal of Physiology and Pharmacology
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• 제1권3호
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• pp.337-343
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• 1997

Antiulcer effects of YH1238 and YH1885 were determined in the isolated gastric cells from human and rabbit stomach. Intracellular accumulation of $[^{14}C]-aminopyrine\;and\;[^{14}C]-glucose$ oxidation were used as indicators of acid secretory ability of the gastric cells. Unstimulated and stimulated gastric cells with dibutyryl cAMP$(10^{-3}M)$ were used and the inhibitory effects of YH1238 and VH1885 on acid secretion were compared with known proton pump inhibitors such as omerrazole and SK&F 96067. Dibutyryl cAMP stimulated the $[^{14}C]-aminopyrine$ accumulation and $[^{14}C]-glucose$ oxidation, which were inhibited by YH1238, YH1885, SK&F 96067 and omeprazole. Inhibitory effects of YH1238, YH1885 and omeprazole on $[^{14}C]-aminopyrine$ accumulation in stimulated gastric cells were more potent than that of SK&F 96067 at the concentration of $10^{-5}M$. It is suggested that the reversible proton pump inhibitors YH1238 and YH1885 would be effective antiulcer agents.

• Biomolecules & Therapeutics
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• 제3권3호
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• pp.205-209
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• 1995

The novel compound KH 3218 was synthesized and evaluated for its ability to inhibit the gastric H$^{＋}$＋ $K^{＋}$ ATPase activity in vitro as well as to lessen gastric acid secretion in vivo. KH 3218 inhibited rabbit gastric H$^{＋}$＋ $K^{＋}$ ATPase in a concentration and time dependent manner. $IC_{50}$/ value was estimated to be about 15 $\mu$M. The inhibition of the H$^{＋}$＋ $K^{＋}$ ATPase by KH 3218 was blocked by sulfhydryl reducing agents, dithiothreitol or $\beta$-mercaptoethanol. The inhibition of the enzyme was not reversible by 50 fold dilution of the incubation mixtures, suggesting the irreversible nature of the inactivation. In the pylorus-ligated rift, KH 3218 reduced the total acid output as compared with the control. In addition, KH 3218 was capable of inhibiting H. pylori urease activity. These data suggest that KH 3218 is a potent inhibitor for H$^{＋}$＋ $K^{＋}$ ATPase activity as well as for gastric acid secretion, and has a potential to be developed as a novel antiulcer agent.

• 대한한방내과학회지
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• 제21권1호
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• pp.87-99
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• 2000

Objectives : This is the experimetal paper to evaluate and compare the effects of Bosimgunbitang(補心健脾湯) with those of Jungjungamiyijintang(正傳加味二陳湯) on contraction of isolated organs, anti-ulcer, secretion of gastric juice, secretion of gastrin in serum, transport ability of intestine, analgesic effect and sedative effect Methods : We used mice and rats administered with the extract of the above herbs. Results: Bosimgunbitang and jungjungamiijintang showed the inhibitory effect on the smooth muscle contraction of the isolated ileum induced by acethylcholine chloride and barium chloride in mice. transport ability of intestine. Bosimgunbitang and jungjungamiijintang showed the inhibitory effect on the contraction of the fundus-strip induced by acethylcholine chloride and barium chloride in rats. The preventive effect on pyloric ulcer, indomethacin induced ulcer and ethanol-HCl induced ulcer bf mice was significant. The inhibitory effect of Bosimgunbitang on gastric free acidity, total acidity in Shay rats was significant. The inhibitory effect of on gastrin secretion in serum was significant after only 1 hour when the Bosimgunbitang and jungjungamiijintang was administered. The promoting effect of the jungjungamiijintang on the transport ability of small intestine was significant in the high concentration. The promoting effect of the Bosimgunbitang and jungjungamiijintang on the transport ability of large intestine was significant. The analgesic and the sedative effect were recognized. It meaned that Bosimgunbitang and jungjungamiijintang effected on the C.N.S.. Conclusion : Bosimgunbitang and jungjungamiijintang have the inhibitory effect on the smooth muscle abnormal contraction of the isolated ileum and the anti-ulcer effect to prevent, secretion of gastric juice and gastrin in serum. And they also have to increase a transport ability of intestine, analgesic effect and sedative effect. Jungjungamiijintang especially is eminent for analgesic effect while Bosimgunbitang has excellent sedative effect.

• 대한약리학회지
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• 제31권3호
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• pp.313-321
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• 1995

위점막 손상에 미치는 영향에 관한 nicotine의 효과는 아직 정설이 없는 형편이다. 본 연구에서는 nicotine이 위점막 손상에 미치는 영향을 보기 위하여 nicotine (5 mg/kg, 10mg/kg)을 9일간 하루에 두번씩 위내 투여하였다. 위점막 손상은 gastrin (1.2 mg/kg)을 피하 주사함과 동시에 유문부결찰을 6시간 동안 시행하므로 야기시켰다. 그 결과 nicotine 투여군에서 현저한 위점막 손상의 감소를 보였다 (대조군의 50%). 이러한 nicotine의 위점막 보호 효과에 대한 기전을 추구하기 위하여 위관류 실험을 시행하였다. Nicotine은 기초 위산 분비에는 영향이 없었으나 gastrin으로 자극된 위산 분비를 현저히 감소시켰고, 이러한 반응은 nicotine 용량에 비례하였다. 이상의 결과로 보아 nicotine의 장기간 간헐적 투여는 gastrin 투여로 인한 위점막 손상에 보호 효과가 있으며, 이러한 효과는 gastrin으로 자극된 위산 분비를 억압하는 nicotine의 효과가 관련될 것으로 생각된다. 또한 nicotine의 위점막 손상 악화 효과를 관찰한 보고들을 고려하면 nicotine의 위점막 손상에 관한 효과는 nicotine의 투여 방법에 따라 전혀 다르게 나타날 수 있을 것으로 생각된다.

• 생약학회지
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• 제33권4호통권131호
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• pp.389-394
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• 2002

Present study was carried out for development of a new supplementary product with gastroprotective effect. Natural Products mentioned that have GI protective property in Dongeuibogam and reports were evaluated anti-bacterial activity against Helicobacter pylori, then five heres were selected. The material used for the test were water extract of Alpinia oxyphlla (AO), Astragalus membranaceus (AM), Cinnamomum loureirii(CL), Citrus aurantium(CA), Amomum villosum(AV). They were tested individually on HCI ethanol-induced gastric lesion in rats, AV CL, AO showed the most significant effectiveness, respectively. Then two mixture different in their content ratio (P020701-1,-2) and complex with P020701-1 (CP) were made, and tested on HCI·ethanol, indomethacin-induced gastric lesion, aspirin-ligature, Shay ulcer and gastric secretion. P020701-1, -2 and CP showed significant effect on HCI ethanol, indomethacin-induced gastric lesion, and Shay ulcer. It can be regarded that the antigasuitic and anti-ulcerative effects of P020701- 1, -2 and CP are originated from reduction of total acid output identified by gastric secretion test.

• 동의생리병리학회지
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• 제22권1호
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• pp.108-114
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• 2008

Present study was carried out for development of a new herb product with gastroprotective effect. Natural herbs mentioned that have gastrointenstial protective property in Donggeuibogam and reports were evaluated anti-bacterial activity against Helicobacter pylori, then Ulmus davidiana var. japonica Nakai (YGP) were selected. The material used for the test were water extract of Ulmus davidiana var. japonica Nakai. They were tested individually on HCl ethanol-induced gastric lesion in rats showed the most significant effectiveness, respectively. Then YGP was made, and tested on HCl ethanol, indomethacin-induced gastric lesion, shay ulcer and gastric secretion. Conclusions : YGP showed significant effect on HCl ethanol, indomethacin-induced gastric lesion, and Shay ulcer. It can be regarded that the antigastritic and anti-ulcerative effects of YGP is originated from reduction of total acid output identified by gastric secretion test.

• Archives of Pharmacal Research
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• 제19권2호
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• pp.126-131
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• 1996

The effects of various synthetic benzimidazole derivatives on gastric H^+/K^+$ATPase activity in vitro were examined. The results showed that the effects of substituents on the benzimidazole ring were not significant. However, replacement of sulfoxide connecting two ring systems to sulfide resulted in a completely inactive compound in vitro, suggesting the essential role of sulfoxide group in the inhibition. In addition, compounds with 5 or 6-membered oxacyclic substituents attached to the pyridine ring displayed the most effective inhibitory activity. Among these derivatives, AU-47 was the most potent, and detailed mechanistic studies with the compound were carried out. AU-47 inhibited gastricH^+/K^+$ATPase in a concentration and time dependent manner with 50% inhibition at $6\muM$. The presence of sulfhydryl reducing agents or substrate analogue protected H^+/K^+$ATPase from the inactivation. The inhibition by AU-47 was potentiated by acid pretreatment of the compound, suggesting the structural conversion of AU-47 into a more active intermediate which was favored in acidic condition. Consistent with in vitro results, AU-47 inhibited in vivo gastric acid secretion. The results suggest that AU47 is a relevant candidate for the development of new antiulcer agent.

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

• 생약학회지
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• 제21권4호
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• pp.300-306
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• 1990

Chichul-Tang, a combined preparation of crude drug, which was composed of Atractylodis Rhizoma alba and Ponciri Fructus, has been used widely for digestive disorder. Each herb extract of Atractylodis Rhizoma and Ponciri Fructus, the mixture of both herb extracts were examined for the effects on isolated smooth muscle, intestinal propulsion, anti-cathartic action and gastric secretion. The results were summarized as follows: Chichul-Tang showed the inhibitory effects of the convulsion of smooth muscle. Anti-cathartic effect was shown and gastric secretion was inhibited.