期刊
BIOLOGICAL & PHARMACEUTICAL BULLETIN
卷 31, 期 3, 页码 375-379出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/bpb.31.375
关键词
4,4'-butylidenebis(6-t-butyl-m-cresol); androgen antagonist; endocrine disruption; anti-androgenic effect; estrogen antagonist; 4,4'-thiobis(6-t-butyl-m-cresol)
Disposable gloves made of nitrite-butadiene rubber (NBR) are used for contact with foodstuffs rather than polyvinyl chloride gloves containing di(2-ethylhexyl)phthalate (DEHP), because endocrine-disruptive effects are suspected for phthalate diesters including DEHR However, 4,4'-butylidenebis(6-t-butyl-m-cresol) (BBBC), 2,4-di-t-butylphenol, and 2,2,4-trimetyl-1,3-pentanediol diisobutyrate can be eluted from NBR gloves, and possibly also detected in food. In this study, we examined the endocrine-disrupting effects of these chemicals via androgen receptor (AR) and estrogen receptor (ER)-mediated pathways using stably transfected reporter gene cell lines expressing AR (AR-EcoScreen system) and ER (MVLN cells), respectively. We also examined the binding activities. of these chemicals to AR and ER. The IC50 value of BBBC for antagonistic androgen was in the range of 10(-6) M. The strength of inhibition was about 5 times that of a known androgen antagonist, 1,1'-(2,2-dichloroethylidene)-bis[4-chlorobenzene](p,p'-DDE), and similar to that of bisphenol A. The IC50 value of BBBC for antagonistic estrogen was in the range of 10(-6) M. These results suggest that BBBC and its structural homologue, 4,4'-thiobis(6-t-butyl-m-cresol) are androgen and estrogen antagonists. It is therefore necessary to study these chemicals in vivo, and clarify their effect on the endocrine system.
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