Sulfation of estradiol in human epidermal keratinocyte.
Sulfation of estradiol in human epidermal keratinocyte.
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DOI：
10.1248/bpb.34.1147
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发表时间：
2011-07
影响因子：
2
通讯作者：
Akira Kushida;K. Hattori;N. Yamaguchi;Tetsuyuki Kobayashi;A. Date;H. Tamura
中科院分区：
文献类型：
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作者：
Akira Kushida;K. Hattori;N. Yamaguchi;Tetsuyuki Kobayashi;A. Date;H. Tamura
表皮是众所周知的雌激素靶组织之一。与雌激素作用的信息相比，有关表皮雌激素代谢的信息仍然非常有限。乳腺癌组织中，17β-雌二醇（E(2)）因硫酸化而失活，雌激素磺基转移酶（SULT1E1）的表达水平与其恶性程度呈负相关。然而，关于雌二醇在皮肤中失活的数据很少。为了同时检测和测定E(2)及其代谢物，我们建立了放射性高效液相色谱法的测定方法。在正常人表皮角质形成细胞 (NHEK) 细胞中，大部分 [(3)H] 标记的 E(2) 转化为 E(2) 硫酸盐。 20 nM 时磺基转移酶对 E(2) 的估计活性为 0.11±0.01（pmol/min/mg 蛋白质）。在钙分化的 NHEK 细胞中观察到雌激素磺基转移酶活性的显着诱导（0.58±0.07（pmol/min/mg 蛋白质））。 SULT1E1的基因表达在分化的角质形成细胞中比在增殖的角质形成细胞中高15倍，而类固醇硫酸酯酶的基因表达降低。这些结果表明 E(2) 失活主要由角质形成细胞中的 SULT1E1 介导，并且 E(2) 作用可能在表皮分化中受到抑制。
Epidermis is one of the well-known estrogen target tissues. Information regarding estrogen metabolism in epidermis is still very limited compared to that of estrogen action. In the breast cancer tissue, 17β-estradiol (E(2)) is inactivated by sulfation and the expression level of estrogen sulfotransferase (SULT1E1) is inversely correlated with its malignancy. However, there is little datum about inactivation of estradiol in skin. In order to detect and measure E(2) and its metabolites simultaneously, we established an assay method with radio HPLC. A majority of [(3)H] labeled E(2) was converted to E(2) sulfate in normal human epidermal keratinocyte (NHEK) cells. The estimated activity of sulfotransferase toward E(2) at 20 nM was 0.11±0.01 (pmol/min/mg protein). Significant induction of estrogen sulfotransferase activity was observed in calcium-differentiated NHEK cells (0.58±0.07 (pmol/min/mg protein)). The gene expression of SULT1E1 was fifteen-fold higher in differentiated keratinocyte than in proliferating keratinocyte, whereas that of steroid sulfatase was reduced. These results suggest that E(2) inactivation is primarily mediated by SULT1E1 in keratinocyte and E(2) action is likely suppressed in epidermal differentiation.