Nanbo T
Tokai Research Laboratories, Daiichi Pure Chemicals Co., Ltd., Ibaraki, Japan.
Chem Pharm Bull (Tokyo). 1991 Oct;39(10):2756-7. doi: 10.1248/cpb.39.2756.
The influence of 4-substituent of phenol on the sulfate conjugation was studied in the rat. 4-Substituents used were 4-ethyl, 4-tert-butyl and 4-phenyl. The in vivo and in vitro sulfations decreased in the order of phenol, 4-ethylphenol, 4-tert-butylphenol and 4-phenylphenol. The activity of sulfotransferase was correlated with the van der Waals volume of 4-substituent. The modification of thiol and arginyl residues of cytosol protein showed a similar degree of inactivation of sulfotransferase to all substituents used. Inactivation by the modification of histidyl residue of the protein increased with the increase of the van der Waals volume of 4-substituent. This result suggests that histidyl residue recognized van der Waals volume of 4-substituent.
在大鼠体内研究了苯酚4-位取代基对硫酸结合反应的影响。所用的4-位取代基为4-乙基、4-叔丁基和4-苯基。体内和体外的硫酸化反应活性按照苯酚、4-乙基苯酚、4-叔丁基苯酚和4-苯基苯酚的顺序依次降低。硫酸转移酶的活性与4-位取代基的范德华体积相关。对胞质溶胶蛋白的巯基和精氨酰残基进行修饰后，所有所用取代基的硫酸转移酶失活程度相似。通过修饰蛋白的组氨酰残基导致的失活随着4-位取代基范德华体积的增加而增加。该结果表明组氨酰残基能够识别4-位取代基的范德华体积。
