Anti-estrogenic activity of fifty chemicals evaluated by in vitro assays.
We examined the anti-estrogenic activity of 50 chemicals by the yeast two-hybrid assay and detected the activity of hexachlorophene, pentachlorophenol, and vitamin K3 (menadione), in that order. These chemicals were also observed to inhibit the transcriptional activity of 17beta-estradiol in a reporter gene assay system using MCF-7 cells, estrogen receptor-positive breast cancer cells, and to bind directly to estrogen receptor alpha in a competitive binding assay system, although the order of the activity was slightly different among the 3 assays. These findings suggested that three of fifty chemicals could inhibit estrogen activity by competitive binding with 17beta-estradiol to the estrogen receptor.
Jung
Joohee
J
Laboratory of Environmental Biochemistry, Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan.
Ishida
Kunie
K
Nishihara
Tsutomu
T
D001667:Binding, Competitive / Q000187:drug effects; D001943:Breast Neoplasms / Q000378:metabolism* / Q000473:pathology; D004958:Estradiol / Q000378:metabolism* / Q000494:pharmacology; D004965:Estrogen Antagonists / Q000494:pharmacology*; D047628:Estrogen Receptor alpha; D005260:Female; D006582:Hexachlorophene / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D008156:Luciferases / Q000378:metabolism; D010416:Pentachlorophenol / Q000494:pharmacology; D011960:Receptors, Estrogen / Q000187:drug effects / Q000378:metabolism*; D012441:Saccharomyces cerevisiae / Q000187:drug effects; D014158:Transcription, Genetic; D014407:Tumor Cells, Cultured; D020798:Two-Hybrid System Techniques; D024483:Vitamin K 3 / Q000494:pharmacology
D004965:Estrogen Antagonists; D047628:Estrogen Receptor alpha; D011960:Receptors, Estrogen; D004958:Estradiol; D024483:Vitamin K 3; D010416:Pentachlorophenol; D008156:Luciferases; D006582:Hexachlorophene