Evaluation of Endocrine Disrupting Activities of Monohydroxylated Derivatives of 1-nitropyrene by Yeast Two-hybrid Assay

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Endocrine disrupting activities of three isomers of monohydroxylated 1-nitropyrene (1-NP) [3-, 6-, and 8-hydroxy-1-nitropyrenes (OHNPs)] were evaluated for the first time by yeast two-hybrid assay. OHNPs, which are not only metabolites of 1-NP but are also found in airborne particles, did not exhibit androgenic activity but exhibited estrogenic, antiestrogenic, and antiandrogenic activities. 6-OHNP showed the strongest estrogenic activity among the three OHNP isomers examined in this study. Concentrations of the OHNP isomers that gave 10% of activity of 1.0 × 10^<-6>M 17β-estradiol (E_2) were as follows: 3-OHNP, 6.0 × 10^<-7>M; 6-OHNP, 6.0 × 10^<-8>M; 8-OHNP, 9.0 × 10^<-7>M. On the contrary, 8-OHNP exhibited the strongest antiestrogenic and antiandrogenic activities of the three isomers. 1.0 × 10^<-6>M of 8-OHNP inhibited 32 and 90% of β-galactosidase activity induced by 1.0 × 10^<-9>M of E_2 and 1.0 × 10^<-8>M of 5a-dihydrotestosterone (DHT), respectively. These findings point out the necessity for detailed investigation of environmental sources and distributions of OHNPs as well as the parent 1-NP.
公益社団法人日本薬学会の論文
2008-02-01