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[阿地比特(N-丁基双胍)对大鼠组织体外葡萄糖代谢及氧化的影响]

[Effect of adebit (N-butylbiguanide) on the metabolism and oxidation of glucose in rat tissues in vitro].

作者信息

Kosovskiĭ M I

出版信息

Probl Endokrinol (Mosk). 1984 Nov-Dec;30(6):52-6.

PMID:6514686
Abstract

The effect of adebit (N-butylbiguanide) on the rat tissues in vitro, namely, on sugar consumption and transport, glucose oxidation, as well as on gluconeogenesis in the rat organism, was studied. Glucose consumption and D-xylose transport in the diaphragms of intact animals and glucose consumption and oxidation in the epididymal fat of rats, given hydrocortisone, were determined. Gluconeogenesis intensity under adebit action was investigated according to the blood sugar level following adrenaline injections to rats after 24-hour fasting. It was established that the administration of adebit at concentrations of 0.2 to 0.5 mM results in intensified insulin-independent glucose consumption and xylose transport in the diaphragm, the maximum transport rate being augmented and the dissociation constant remaining unchanged. It is concluded that adebit does not change the properties of sugar transmitter, but influences the cell metabolism by inhibiting oxidative phosphorylation. The use of adebit in therapeutic concentrations (5 to 10 mcM) gave an insulin-dependent rise of glucose consumption and oxidation in the fatty tissue by 44%. A decrease in the blood sugar level in the presence of adrenaline hyperglycemia under the action of adebit therapeutic doses was not observed. It is concluded that biguanide hypoglycemizing action in diabetes mellitus is based on the biguanide potentiated insulin effectiveness.

摘要

研究了阿地比特(N-丁基双胍)对大鼠组织的体外作用,即对大鼠机体糖消耗与转运、葡萄糖氧化以及糖异生的影响。测定了完整动物膈肌中的葡萄糖消耗和D-木糖转运,以及给予氢化可的松的大鼠附睾脂肪中的葡萄糖消耗和氧化。根据禁食24小时后给大鼠注射肾上腺素后的血糖水平,研究了阿地比特作用下的糖异生强度。已确定,以0.2至0.5 mM的浓度给予阿地比特会导致膈肌中胰岛素非依赖性葡萄糖消耗和木糖转运增强,最大转运速率增加,解离常数保持不变。得出的结论是,阿地比特不会改变糖转运体的特性,但通过抑制氧化磷酸化影响细胞代谢。以治疗浓度(5至10 μM)使用阿地比特可使脂肪组织中葡萄糖消耗和氧化胰岛素依赖性增加44%。在阿地比特治疗剂量作用下,未观察到在肾上腺素性高血糖存在时血糖水平降低。得出的结论是,双胍类药物在糖尿病中的降血糖作用基于双胍类药物增强的胰岛素有效性。

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