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通过给予带有四唑硫醇基团的β-内酰胺抗生素来减轻大鼠乙醇诱导的高血糖症。

Diminution of ethanol-induced hyperglycaemia in the rat by administration of beta-lactam antibiotics with a tetrazole thiol group.

作者信息

Römer K G, Alanis O T, de Torres G G, Freundt K J

出版信息

Pharmacol Res Commun. 1983 Jun;15(6):631-40. doi: 10.1016/s0031-6989(83)80034-4.

Abstract

The acute-onset hyperglycaemia produced by i.p. injection of 2 g of ethanol/kg body weight in adult female SPF Sprague-Dawley rats (200-220 g) was considerably less pronounced when 100 mumol/kg b.w. of one of the following tetrazole thiol-containing beta-lactam antibiotics (BLAs) was given i.p. 3 hours in advance: cephamandole (CMD), moxalactam (MOX), cephoperazone (CPZ) or cephothiam (CTM). An equimolar dose of cephazolin (CEZ), a thiadiazole thiol-containing cephalosporin, did not affect the ethanol-induced hyperglycaemia. Administration of an equimolar oral dose of disulfiram, which has an NCS structure similar to that of the tetrazole thiol-containing BLAs, produced an additional increase of the ethanol-induced hyperglycaemia. The diminution of the ethanol-induced hyperglycaemia by BLAs with a tetrazole thiol group appears to be linked to their NCS structure. It is conceivable that this effect which might be important for human therapy, is causally related to an inhibition of the glycolytic or gluconeogenetic enzyme system.

摘要

在成年雌性无特定病原体(SPF)斯普拉格-道利大鼠(体重200 - 220克)中,腹腔注射2克乙醇/千克体重会引发急性高血糖症。若提前3小时腹腔注射下列含四氮唑硫醇的β-内酰胺抗生素(BLAs)之一,剂量为100微摩尔/千克体重,则这种急性高血糖症的表现会明显减轻,这些抗生素包括头孢孟多(CMD)、拉氧头孢(MOX)、头孢哌酮(CPZ)或头孢硫脒(CTM)。等摩尔剂量的含噻二唑硫醇的头孢菌素头孢唑林(CEZ),对乙醇诱导的高血糖症没有影响。口服等摩尔剂量的双硫仑,其具有与含四氮唑硫醇的BLAs相似的NCS结构,会使乙醇诱导的高血糖症进一步加剧。含四氮唑硫醇基团的BLAs对乙醇诱导的高血糖症的减轻作用似乎与其NCS结构有关。可以想象,这种可能对人类治疗很重要的效应,与糖酵解或糖异生酶系统的抑制存在因果关系。

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