Abstract
The inhibition of human and rat 11ß-hydroxysteroid dehydrogenase 2 by perfluoroalkylated substances (HTML)
Zhao,Binghai; Lian,Qing-Quan; Chu,Yanhui; Hardy,Dianne O.; Li,Xiao-Kun; Ge,Renshan
Journal of Steroid Biochemistry and Molecular Biology 125(1-2): 143-147
Publication date: 2011
11ß-Hydroxysteroid dehydrogenase 2 (11ß-HSD2) regulates active glucocorticoid access to glucocorticoid and mineralocorticoid receptors by metabolizing it to an inactive form. Perfluoroalkylated substances (PFASs) are man-made polyfluorinated compounds that are widely used and persistent in the environment. We tested the inhibitory potencies of four PFASs including perfluorooctanoic acid (PFOA), perfluorooctane sulfonate (PFOS), perfluorohexanesulfonate (PFHxS) and perfluorobutane sulfonate (PFBS) on human and rat 11ß-HSD2. PFOS was a potent inhibitor of both human (IC = 48 nM) and rat (IC = 293 nM) 11ß-HSD2 activities. The potencies for the inhibition of human and rat 11ß-HSD2 activities were PFOS > PFOA > PFHxS > PFBS. PFASs showed competitive inhibition of both human and rat 11ß-HSD2 activities. This observation indicates that PFOS is a potent endocrine disruptor for glucocorticoid metabolism.
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