Estrogenic and anti-androgenic activity of nitrophenols in diesel exhaust particles (DEP)

Estrogenic and anti-androgenic activity of nitrophenols in diesel exhaust particles (DEP)
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DOI:
10.1248/bpb.27.835
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发表时间:
2004-06-01
影响因子:
2
通讯作者:
Suzuki, AK
Suzuki, AK
中科院分区:
医学4区
文献类型:
--
作者:
Taneda, S;Mori, Y;Suzuki, AK

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我们最近从柴油机排气微粒(DEP)中分离出4-硝基苯酚、2-甲基-4-硝基苯酚、3-甲基-4-硝基苯酚和4-硝基-3-苯基苯酚,并鉴定它们为血管扩张剂。由于这些化合物是可能模拟激素的烷基酚衍生物,我们通过人雌激素受体(hER)-酵母筛选试验评价了它们的雌激素活性。除2-甲基-4-硝基苯酚外,所有硝基苯酚衍生物均具有雌激素活性。有些雌激素类化合物也具有抗雄激素活性,因此我们采用人雄激素受体(hAR)-酵母筛选法测定了这些化合物的抗雄激素活性。我们发现在所有四个硝基酚抗雄激素。DEP中的硝基酚类化合物不仅具有扩血管活性,还具有雌激素活性和抗雄激素活性。
We recently isolated 4-nitrophenol, 2-methyl-4-nitrophenol, 3-methyl-4-nitrophenol, and 4-nitro-3-phenylphenol from diesel exhaust particles (DEP) and identified them as vasodilators. Because these compounds are alkylphenollic derivatives that might mimic hormones, we evaluated their estrogenic activity by human estrogen receptor (hER)-yeast screen assay. All of these nitrophenol derivatives except 2-methyl-4-nitrophenol exhibited estrogenic activity. Some estrogenic compounds are also anti-androgenic, so we measured the anti-androgenic activity of the same compounds by human androgen receptor (hAR)-yeast screen assay. We found anti-androgenicity in all four nitrophenols. Nitrophenols in DEP possess not only vasodilatory activity but also estrogenic and anti-androgenic activity.