Lee Byung-Hwan, Hwang Sung-Hee, Choi Sun-Hye, Kim Hyeon-Joong, Jung Seok-Won, Kim Hyun-Sook, Lee Joon-Hee, Kim Hyung-Chun, Rhim Hyewhon, Nah Seung-Yeol
Department of Physiology, College of Veterinary Medicine and Bio/Molecular Informatics Center, Konkuk University.
Biol Pharm Bull. 2014;37(4):576-80. doi: 10.1248/bpb.b13-00808.
Resveratrol is found in grapes, red wine, and berries. Resveratrol has been known to have many beneficial health effects, such as anti-cancer, neuroprotective, anti-nociceptive, and life-prolonging effects. However, the single cellular mechanisms by which resveratrol acts are relatively unknown, especially in terms of possible regulation of receptors involved in synaptic transmission. The glycine receptor is an inhibitory ligand-gated ion channel involved in fast synaptic transmission in spinal cord. In the present study, we investigated the effect of resveratrol on human glycine receptor channel activity. Glycine α1 receptors were expressed in Xenopus oocytes and glycine receptor channel activity was measured using a two-electrode voltage clamp technique. Treatment with resveratrol alone had no effect on oocytes injected with H2O or on oocytes injected with glycine α1 receptor cRNA. In the oocytes injected with glycine α1 receptor cRNA, co- or pre-treatment of resveratrol with glycine inhibited the glycine-induced inward peak current (IGly) in a reversible manner. The inhibitory effect of resveratrol on IGly was also concentration dependent, voltage independent, and non-competitive. These results indicate that resveratrol regulates glycine receptor channel activity and that resveratrol-mediated regulation of glycine receptor channel activity is one of several cellular action mechanisms of resveratrol for pain regulation.
白藜芦醇存在于葡萄、红酒和浆果中。已知白藜芦醇具有许多有益的健康功效，如抗癌、神经保护、抗伤害感受和延长寿命等作用。然而，白藜芦醇发挥作用的单细胞机制相对未知，尤其是在涉及突触传递的受体可能的调节方面。甘氨酸受体是一种抑制性配体门控离子通道，参与脊髓中的快速突触传递。在本研究中，我们研究了白藜芦醇对人甘氨酸受体通道活性的影响。甘氨酸α1受体在非洲爪蟾卵母细胞中表达，并使用双电极电压钳技术测量甘氨酸受体通道活性。单独用白藜芦醇处理对注射水的卵母细胞或注射甘氨酸α1受体cRNA的卵母细胞均无影响。在注射甘氨酸α1受体cRNA的卵母细胞中，白藜芦醇与甘氨酸共同处理或预处理以可逆方式抑制了甘氨酸诱导的内向峰值电流（IGly）。白藜芦醇对IGly的抑制作用也是浓度依赖性、电压非依赖性和非竞争性的。这些结果表明，白藜芦醇调节甘氨酸受体通道活性，并且白藜芦醇介导的甘氨酸受体通道活性调节是白藜芦醇调节疼痛的几种细胞作用机制之一。
