Takahashi O, Hiraga K
Acta Pharmacol Toxicol (Copenh). 1985 Jan;56(1):6-13. doi: 10.1111/j.1600-0773.1985.tb01246.x.
Rats and mice were fed a diet containing aspirin at levels of 0, 0.3, 0.6 and 1.2% for 1 and 4 weeks. Haemorrhagic death and/or haemorrhagic anaemia occurred in rats in a dose-dependent manner. Prothrombin and kaolin-activated partial thromboplastin time indices were also decreased depending on the daily doses. However, no conspicuous haemorrhagic signs were found in mice given aspirin. These results suggest marked differences in haemorrhagic effects of aspirin between rats and mice. From results of supplementary experiments with two metabolites of aspirin, salicylic acid and gentisic acid, and from the fact of close relationship between hepatic concentration of salicylic acid and haemorrhagic effects of aspirin, it is inferred that salicylic acid may be a precursor for the active metabolite(s) to cause haemorrhage. The mechanism of species differences of aspirin is discussed.
给大鼠和小鼠喂食含有0%、0.3%、0.6%和1.2%阿司匹林的饲料,持续1周和4周。大鼠出现出血性死亡和/或出血性贫血,且呈剂量依赖性。凝血酶原和高岭土活化部分凝血活酶时间指标也随每日剂量的增加而降低。然而,给予阿司匹林的小鼠未出现明显的出血迹象。这些结果表明,阿司匹林对大鼠和小鼠的出血作用存在显著差异。从阿司匹林的两种代谢产物水杨酸和龙胆酸的补充实验结果,以及水杨酸在肝脏中的浓度与阿司匹林出血作用之间的密切关系来看,推测水杨酸可能是导致出血的活性代谢产物的前体。本文还讨论了阿司匹林种属差异的机制。