Sharaf A A, Khayyal M T, Kheir-el-Din A, Sharaf A A, Kassem F
Egypt J Bilharz. 1978;5(1-2):49-57.
The effects of the antischistosomal drug, niridazole, on the rate of gluconeogenesis in kidney cortex slices and on the rate of oxidation of pyruvate and some Krebs cycle intermediates in liver homogenate of non infected mice were determined. In vitro, niridazole was found to inhibit the succinate and pyruvate oxidation at the high concentration tested (10(-3)M). The rate of gluconeogenesis from alpha-ketoglutarate was unaffected. In vivo, niridazole showed a stimulatory effect on the rate of gluconeogenesis from alpha-ketoglutarate and on the rate of oxidation of pyruvate at a dosage level of 100 mg/kg for 5 days. The observed changes were discussed and the differences observed between the in vivo and in vitro work were assumed to be due to exposure of the tissues to the unmetabolized drug in vitro and to the drug and its metabolites in vivo.
研究了抗血吸虫药物硝唑咪对未感染小鼠肾皮质切片中糖异生速率以及肝匀浆中丙酮酸和一些三羧酸循环中间产物氧化速率的影响。在体外，发现硝唑咪在高测试浓度（10⁻³M）下可抑制琥珀酸和丙酮酸的氧化。α-酮戊二酸的糖异生速率未受影响。在体内，硝唑咪在剂量为100mg/kg、持续5天的情况下，对α-酮戊二酸的糖异生速率和丙酮酸的氧化速率显示出刺激作用。对观察到的变化进行了讨论，并且认为体内和体外实验结果的差异是由于体外组织暴露于未代谢的药物，而体内则暴露于药物及其代谢产物。
