Yamasaki Kanji, Noda Shuji, Imatanaka Nobuya, Yakabe Yoshikuni
Chemicals Assessment Center, Chemicals Evaluation and Research Institute, 3-822 Ishii, Hita, 877-0061 Oita, Japan.
Toxicol Lett. 2004 Jan 15;146(2):111-20. doi: 10.1016/j.toxlet.2003.07.003.
We performed an immature rat uterotrophic assay of 14 chemicals having various receptor-binding affinities in order to assess the relationship between their uterotrophic potency and receptor-binding affinity. The chemicals tested were phthalic acid di-n-hexyl ester, phthalic acid di-n-amyl ester, phthalic acid di-n-propyl ester, 2-ethylhexyl-p-hydroxybenzoate, 4,4'-biphenol, 4,4'-sulfonyldiphenol, 4,4'-dihydroxydiphenylmethane, 2,4-dihydroxybenzophenone, 4,4'-cyclohexylidenebisphenol, 4-t-butylpyrocatechol, clomiphene citrate, 4,4'-(1,3-phenylenediisopropylidene)bisphenol, p-t-butylphenol, and diallylterephthlate. Two of the 14 chemicals, phthalic acid di-n-propyl ester and diallylterephthlate, exhibited no receptor-binding affinity, and the receptor-binding affinity of phthalic acid di-n-hexyl ester and phthalic acid di-n-amyl ester was lower than that of the other chemicals. Ten of the chemicals showed uterotrophic potency, the exceptions being phthalic acid di-n-propyl ester, diallylterephthlate, phthalic acid di-n-hexyl ester, and phthalic acid di-n-amyl ester. The results of the present study demonstrate that the affinity of the chemicals in the receptor-binding assay correlated well with their potency in the uterotrophic assay except for a few chemicals with very low receptor-binding affinity.
我们对14种具有不同受体结合亲和力的化学物质进行了未成熟大鼠子宫增重试验，以评估它们的子宫增重效力与受体结合亲和力之间的关系。所测试的化学物质有邻苯二甲酸二正己酯、邻苯二甲酸二正戊酯、邻苯二甲酸二正丙酯、对羟基苯甲酸2-乙基己酯、4,4'-联苯酚、4,4'-磺酰基二苯酚、4,4'-二羟基二苯甲烷、2,4-二羟基二苯甲酮、4,4'-环己叉双酚、4-叔丁基邻苯二酚、枸橼酸氯米芬、4,4'-(1,3-亚苯基二异亚丙基)双酚、对叔丁基苯酚和对苯二甲酸二烯丙酯。14种化学物质中的两种，即邻苯二甲酸二正丙酯和对苯二甲酸二烯丙酯，没有表现出受体结合亲和力，邻苯二甲酸二正己酯和邻苯二甲酸二正戊酯的受体结合亲和力低于其他化学物质。其中10种化学物质显示出子宫增重效力，例外的是邻苯二甲酸二正丙酯、对苯二甲酸二烯丙酯、邻苯二甲酸二正己酯和邻苯二甲酸二正戊酯。本研究结果表明，除了少数受体结合亲和力非常低的化学物质外，受体结合试验中化学物质的亲和力与其子宫增重试验中的效力具有良好的相关性。
