• Archives of Pharmacal Research
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• 제21권3호
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• pp.241-247
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• 1998

This study was designed to determine biochemical and pharmacological properties of a newly synthesized benzimidazole derivative, 2-amino-4, 5-dihydropyrido [1, 2-a] thiazolo [5, 4-g] benzimidazole (YJA20379-5) in vitro and in vivo. In the leaky membrane vesicles of pig gastric mucosa, YJA20379-5 inhibited the $K^+$-stimulated $H^+$, $K^+$-ATPase activity in a concentration- and time-dependent manner, with $IC_{50}$ values being $43{\mu}\textrm{M}$ and $43{\mu}\textrm{M}$ at pH 6.4 and 7.4, respectively. YJA20379-5, given intraduodenally, had a potent inhibitory effect on the gastric acid secretion in pylorus-ligated rats. The $ED_{50}$ value for acid secretion was 15.4 mg/kg. YJA20379-5, administered orally, also suppressed gastric damages induced by water-immersion stress, indomethacin and ethanol, and duodenal damage induced by mepirizole in rats; the $ED_{50}$ values were 17.6, 4.7, 3.0 and 18.7 mg/kg, respectively. Furthermore, repeated oral administration of YJA20379-5 accelerated the spontaneous healing of acetic acid-induced gastric ulcers in rats. It is concluded that the a-ntisecretory activity of YJA20379-5 appears to be associated with inhibition of $H^+$, $K^+$-ATPase, while its antigastric and antiduodenal lesion activities are primarily related to the antisecretory effect.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1995년도 춘계학술대회
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• pp.93-93
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• 1995

The three combined products were prepared as suspended solutions composed of various ratio of Sucralfate, Hydrotalcite and Neusilin, into which 30% ethanol extracts of Machili cortex, and of Atractylodis rhizoma were added. The efficacy for these products was examined in vivo using a pyrous ligation method in rats. The influence of these products on the intestinal motility was also examined in mice. In all experimental setting, the antisecretory effect of the combined treatment was more pronounced than that of each drug alone. The combined treatment consisted of Sucralfate, Hydrotalcite, Neusilin ratios of 2:2:1 produced the highest inhibitory effect for the gastric secretion. The intestinal motility was not influenced significantly by the treatment of all experimental setting. The above results revealed that the therapeutic dose of Sucralfate, Hydrotalcite, Neusilin given in combination showed a synergistic effect for the inhibition of gastric secretion and little side effect on the intestinal motility. Therefore, the combined product with Sucralfate, Hydrotalcite, Neusilin ratio of 2:2:1 is recommended for the useful drug to heal the gastrointestinal diseases with no side effect on the intestinal motility.

• 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.