Tanii H, Huang J, Hashimoto K
Department of Hygiene, School of Medicine, Kanazawa University, Japan.
Toxicol Lett. 1995 Feb;76(1):27-31. doi: 10.1016/0378-4274(94)03189-4.
The structure-acute toxicity relationship of aromatic hydrocarbons was examined in mice. In all test compounds, the acute toxicity was determined under 2 conditions: control LD50 (LD50-cont) and carbon tetrachloride (CCl4)-pretreated LD50 (LD50-CCl4). The CCl4-pretreatment was done in order to evaluate the toxic potency of compound itself without the influence of metabolism. Both log (1/LD50-cont) and log (1/LD50-CCl4) were functions of the log P, n-octanol/water partition coefficient, i.e., log (1/LD50-cont) = 0.080 log P - 1.532 and log (1/LD50-CCl4) = -0.040(logP)2 + 0.157 log P - 1.373. Both equations were statistically significant (P < 0.01). The ratio of LD50-cont/LD50-CCl4 indicated that metabolic activation is more evident in hydrophobic compounds than in hydrophilic compounds. The results suggest that hydrophobicity of the aromatic hydrocarbons plays an important role in determining their acute toxicity.
在小鼠中研究了芳烃的结构-急性毒性关系。在所有测试化合物中，急性毒性在两种条件下测定：对照半数致死量（LD50-cont）和四氯化碳（CCl4）预处理后的半数致死量（LD50-CCl4）。进行CCl4预处理是为了评估化合物本身的毒效，而不受代谢的影响。log(1/LD50-cont)和log(1/LD50-CCl4)均为正辛醇/水分配系数log P的函数，即log(1/LD50-cont)=0.080 log P - 1.532，log(1/LD50-CCl4)= -0.040(logP)2 + 0.157 log P - 1.373。两个方程均具有统计学意义（P < 0.01）。LD50-cont/LD50-CCl4的比值表明，代谢活化在疏水性化合物中比在亲水性化合物中更明显。结果表明，芳烃的疏水性在决定其急性毒性方面起重要作用。
