双酚 A 对人和大鼠 11β-羟甾脱氢酶活性的抑制作用。
Inhibition of human and rat 11β-hydroxysteroid dehydrogenases activities by bisphenol A.
机构信息
The 2nd Affiliated Hospital, Wenzhou Medical College, Wenzhou, Zhejiang 325000, PR China.
出版信息
Toxicol Lett. 2012 Nov 30;215(2):126-30. doi: 10.1016/j.toxlet.2012.10.002. Epub 2012 Oct 13.
Bisphenol A (BPA) is a potential endocrine disruptor. It has been shown that it can interfere with steroid biosynthesis and metabolism. However, the mechanism is unclear. The objective of the present study is to investigate the effects of BPA on two isoforms of 11β-hydroxysteroid dehydrogenases (11β-HSD1 and 11β-HSD2) in human and rat tissues. Human liver, rat testis microsomes as well as rat adult Leydig cells were used for measurement of 11β-HSD1 activity, and human and rat kidney microsomes for 11β-HSD2 activity. BPA inhibited human and rat 11β-HSD1 activities with the half maximal inhibitory concentrations (IC50s) of 14.81 ± 0.06 μM (mean ± SEM) for human and 19.39 ± 0.09 μM for rat enzyme, respectively. BPA inhibited rat 11β-HSD1 activity in intact rat Leydig cells. BPA also weakly inhibited both human and rat 11β-HSD2 activities. At 100 μM, BPA inhibited human and rat enzymes by 51.16% and 41.61%, respectively. In conclusion, BPA is an inhibitor for both 11β-HSD1 and 11β-HSD2, with selectivity against the type I enzyme.
双酚 A（BPA）是一种潜在的内分泌干扰物。已经表明，它可以干扰甾体生物合成和代谢。然而，其机制尚不清楚。本研究的目的是研究 BPA 对人及大鼠组织中两种 11β-羟甾脱氢酶（11β-HSD1 和 11β-HSD2）同工酶的影响。用人肝、大鼠睾丸微粒体以及大鼠成年莱迪希细胞测定 11β-HSD1 活性，用人及大鼠肾微粒体测定 11β-HSD2 活性。BPA 抑制人及大鼠 11β-HSD1 活性，其半数最大抑制浓度（IC50）分别为人酶 14.81±0.06 μM（均值±SEM）和大鼠酶 19.39±0.09 μM。BPA 抑制完整大鼠莱迪希细胞中的大鼠 11β-HSD1 活性。BPA 还轻度抑制人及大鼠 11β-HSD2 活性。在 100 μM 时，BPA 抑制人及大鼠酶的活性分别为 51.16%和 41.61%。总之，BPA 是 11β-HSD1 和 11β-HSD2 的抑制剂，对 1 型酶具有选择性。
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