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抗溃疡药物2'-羧基甲氧基-4,4'-双(3-甲基-2-丁烯氧基)查耳酮(SU-88)对束缚及水浸大鼠胃硫酸化黏液物质生物合成的影响

Effect of an anti-ulcer agent, 2'-carboxymethoxy-4, 4'-bis (3-methyl-2-butenyloxy) chalcone (SU-88), on the biosynthesis of gastric sulfated mucosubstances in restrained and water-immersed rats.

作者信息

Suwa T, Fukushima K, Kyogoku K, Edo H, Mori Y

出版信息

Jpn J Pharmacol. 1984 Jan;34(1):89-94. doi: 10.1254/jjp.34.89.

Abstract

2'-Carboxymethoxy-4,4'-bis(3-methyl-2-butenyloxy) chalcone (SU-88) has an anti-ulcer effect which is considered to increase the resistant factors of the gastric mucosa. In order to clarify the mechanism of the action of SU-88, the biosynthesis of gastric sulfated mucosubstances (SMS) in vivo and in vitro was investigated in rats with gastric erosion induced by restraint and water-immersion. The incorporation of 35S-sulfate into gastric SMS was significantly reduced 18 hr after the onset of stress. Pretreatment with SU-88 (500 mg/kg, p.o., X 10 days) prevented a reduction in the incorporation of 35S-sulfate due to stress when 35S-sulfate was administered in vivo. On the contrary, the incorporating activity of 35S-sulfate into the SMS in the isolated rat gastric mucosa with erosion was significantly increased 12 hr after the onset of stress, as compared with that of the control group in vitro. The incorporation of 35S-sulfate into the SMS was still further increased by the oral administration of SU-88. The mode of action of SU-88 on the biosynthesis of SMS was discussed.

摘要

2'-羧甲氧基-4,4'-双(3-甲基-2-丁烯氧基)查耳酮(SU-88)具有抗溃疡作用,被认为可增强胃黏膜的抵抗因子。为阐明SU-88的作用机制,在通过束缚和水浸诱导胃糜烂的大鼠体内和体外研究了胃硫酸化黏液物质(SMS)的生物合成。应激开始18小时后,35S-硫酸盐掺入胃SMS的量显著减少。当在体内给予35S-硫酸盐时,用SU-88(500mg/kg,口服,共10天)预处理可防止因应激导致的35S-硫酸盐掺入量减少。相反,与体外对照组相比,应激开始12小时后,在离体的有糜烂的大鼠胃黏膜中,35S-硫酸盐掺入SMS的活性显著增加。口服SU-88可使35S-硫酸盐掺入SMS的量进一步增加。讨论了SU-88对SMS生物合成的作用方式。

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