Department of Medical and Surgical Sciences, Clinica Medica 3, University of Padova, Italy,
Purinergic Signal. 2005 Dec;1(4):369-75. doi: 10.1007/s11302-005-1172-0. Epub 2005 Dec 3.
Steroid hormones, beside their classical genomic mechanism of action, exert rapid, non genomic effects in different cell types. These effects are mediated by still poorly characterized plasma membrane receptors that appear to be distinct from the classic intracellular receptors. In the present study we evaluated the non genomic effects of estradiol (17betaE(2)) in human sperm and its effects on sperm stimulation by extracellular ATP, a potent activator of sperm acrosome reaction. In human sperm 17betaE(2) induced a rapid increase of intracellular calcium (Ca(2+)) concentrations dependent on an influx of Ca(2+) from the extracellular medium. The monitoring of the plasma membrane potential variations induced by 17betaE(2) showed that this steroid induces a rapid plasma membrane hyperpolarization that was dependent on the presence of Ca(2+) in the extracellular medium since it was absent in Ca(2+) free-medium. When sperm were pre-incubated in the presence of the K(+) channel inhibitor tetra-ethylammonium, the 17betaE(2) induced plasma membrane hyperpolarization was blunted suggesting the involvement of K(+) channels in the hyperpolarizing effects of 17betaE(2). Extracellular ATP induced a rapid plasma membrane depolarization followed by acrosome reaction. Sperm pre-incubation with 17betaE(2) inhibited the effects of extracellular ATP on sperm plasma membrane potential variations and acrosome reaction. The effects of 17betaE(2) were specific since its inactive steroisomer 17alphaE(2) was inactive. Furthermore the effects of 17betaE(2) were not inhibited by tamoxifen, an antagonist of the classic 17betaE(2) intracellular receptor.
甾体激素除了经典的基因组作用机制外,还在不同的细胞类型中发挥快速的非基因组作用。这些作用是由仍然特征描述较差的质膜受体介导的,这些受体似乎与经典的细胞内受体不同。在本研究中,我们评估了雌二醇(17βE(2))对人精子的非基因组作用及其对细胞外 ATP 刺激精子顶体反应的作用,细胞外 ATP 是精子顶体反应的有效激活剂。在人精子中,17βE(2)诱导依赖于细胞外介质中 Ca(2+)内流的细胞内 Ca(2+)浓度的快速增加。监测 17βE(2)诱导的质膜电位变化表明,这种甾体诱导快速的质膜超极化,这依赖于细胞外介质中 Ca(2+)的存在,因为在无 Ca(2+)的介质中不存在。当精子在 K(+)通道抑制剂四乙铵存在下预孵育时,17βE(2)诱导的质膜超极化被削弱,表明 K(+)通道参与 17βE(2)的超极化作用。细胞外 ATP 诱导快速的质膜去极化,随后发生顶体反应。精子用 17βE(2)预孵育可抑制细胞外 ATP 对精子质膜电位变化和顶体反应的作用。17βE(2)的作用是特异性的,因为其无活性的甾体异构体 17αE(2)是无活性的。此外,17βE(2)的作用不受他莫昔芬的抑制,他莫昔芬是经典 17βE(2)细胞内受体的拮抗剂。