Terasaki Masanori, Kazama Takeshi, Shiraishi Fujio, Makino Masakazu
Institute for Environmental Sciences, University of Shizuoka, 52-1 Yada, Shizuoka, Japan.
Chemosphere. 2006 Oct;65(5):873-80. doi: 10.1016/j.chemosphere.2006.03.015. Epub 2006 May 2.
A sample of commercial BADGE was fractioned by HPLC and eight impurities including novel propyl derivatives (2), (5) and (6) were identified by NMR spectrometry, FAB-MS and GC-MS. The estrogenicity, both agonist and antagonist, of fractions containing these impurities was measured with a yeast two-hybrid assay incorporating the human (hER alpha) and a competitive binding assay for hER alpha (ELISA). In the yeast two-hybrid assay, estrogenic antagonist activity was found in two fractions, while estrogenic agonist activity was not found in any. In the ELISA method, the binding affinity to hER alpha was found in three fractions. It is probable that a comprehensive assessment of the estrogenic properties of commercial BADGE, and their implications for human health, will require examination of all its components as described here.
将市售BADGE样品通过高效液相色谱法进行分离,并通过核磁共振光谱法、快原子轰击质谱法和气相色谱-质谱法鉴定出包括新型丙基衍生物(2)、(5)和(6)在内的8种杂质。采用包含人雌激素受体α(hERα)的酵母双杂交试验和hERα竞争性结合试验(酶联免疫吸附测定法)测定含有这些杂质的馏分的雌激素激动剂和拮抗剂活性。在酵母双杂交试验中,在两个馏分中发现了雌激素拮抗剂活性,而在任何馏分中均未发现雌激素激动剂活性。在酶联免疫吸附测定法中,在三个馏分中发现了与hERα的结合亲和力。正如这里所描述的,对市售BADGE的雌激素特性及其对人类健康的影响进行全面评估可能需要检查其所有成分。