Department of Medicine, University of Virginia, Charlottesville, Virginia 22908, USA.
Endocrinology. 2010 Nov;151(11):5349-58. doi: 10.1210/en.2010-0385. Epub 2010 Aug 25.
GnRH neurons are central regulators of fertility, and their activity is modulated by steroid feedback. In normal females, GnRH secretion is regulated by estradiol and progesterone (P). Excess androgens present in hyperandrogenemic fertility disorders may disrupt communication of negative feedback signals from P and/or independently stimulate GnRH release. Voltage-gated calcium channels (VGCCs) are important in regulating excitability and hormone release. Estradiol alters VGCCs in a time-of-day-dependent manner. To further elucidate ovarian steroid modulation of GnRH neuron VGCCs, we studied the effects of dihydrotestosterone (DHT) and P. Adult mice were ovariectomized (OVX) or OVX and treated with implants containing DHT (OVXD), estradiol (OVXE), estradiol and DHT (OVXED), estradiol and P (OVXEP), or estradiol, DHT, and P (OVXEDP). Macroscopic calcium current (I(Ca)) was recorded in the morning or afternoon 8-12 d after surgery using whole-cell voltage-clamp. I(Ca) was increased in afternoon vs. morning in GnRH neurons from OVXE mice but this increase was abolished in cells from OVXEP mice. I(Ca) in cells from OVXD mice was increased regardless of time of day; there was no additional effect in OVXED mice. P reduced N-type and DHT potentiated N- and R-type VGCCs; P blocked the DHT potentiation of N-type-mediated current. These data suggest P and DHT have opposing actions on VGCCs in GnRH neurons, but in the presence of both steroids, P dominates. VGCCs are targets of ovarian steroid feedback modulation of GnRH neuron activity and, more specifically, a potential mechanism whereby androgens could activate GnRH neuronal function.
GnRH 神经元是生育能力的中枢调节剂,其活性受类固醇反馈的调节。在正常女性中,GnRH 的分泌受雌二醇和孕酮(P)的调节。在高雄激素血症等生殖障碍中,过多的雄激素可能会破坏 P 的负反馈信号的传递,或者独立地刺激 GnRH 的释放。电压门控钙通道(VGCCs)在调节兴奋性和激素释放方面起着重要作用。雌二醇以时间依赖的方式改变 VGCCs。为了进一步阐明卵巢类固醇对 GnRH 神经元 VGCCs 的调节作用,我们研究了二氢睾酮(DHT)和 P 的作用。成年小鼠接受卵巢切除术(OVX)或 OVX 并接受含有 DHT(OVXD)、雌二醇(OVXE)、雌二醇和 DHT(OVXED)、雌二醇和 P(OVXEP)或雌二醇、DHT 和 P(OVXEDP)的植入物治疗。手术后 8-12 天,使用全细胞膜片钳技术在上午或下午记录宏观钙电流(I(Ca))。与 OVXE 小鼠相比,OVXE 小鼠的 GnRH 神经元中 I(Ca)在下午增加,但在 OVXEP 小鼠中这种增加被消除。OVXD 小鼠的 I(Ca)无论何时都增加;OVXED 小鼠没有额外的作用。P 减少 N 型,DHT 增强 N 型和 R 型 VGCC;P 阻断 DHT 对 N 型介导电流的增强作用。这些数据表明 P 和 DHT 对 GnRH 神经元中的 VGCCs 具有相反的作用,但在两种类固醇存在的情况下,P 占主导地位。VGCCs 是卵巢类固醇反馈调节 GnRH 神经元活动的靶点,更具体地说,是雄激素激活 GnRH 神经元功能的潜在机制。