Department of Pharmacology and Toxicology, School of Medicine, University of Puerto Rico, Medical Sciences Campus, P.O. Box 365067, San Juan, 00936-5067 Puerto Rico, USA.
Evid Based Complement Alternat Med. 2011;2011:891819. doi: 10.1155/2011/891819. Epub 2010 Dec 2.
The effects of two valerian extracts (aqueous and hydroalcoholic) were investigated through [(3)H]Glutamate ([(3)H]Glu) and [(3)H]Fluorowillardine ([(3)H]FW) receptor binding assays using rat synaptic membranes in presence of different receptor ligands. In addition, the extract stability was monitored spectrophotometrically. Both extracts demonstrated interaction with ionotropic glutamate receptors (iGluRs). However, the extracts displayed considerable differences in receptor selectivity. The hydroalcoholic extract selectively interacted with quisqualic acid (QA), group I metabotropic glutamate receptor (mGluR) ligand, while the aqueous extract did not alter the binding of QA. The stability of the extracts was examined during several weeks. Freshly prepared extract inhibited 38-60% of [(3)H]FW binding (AMPA). After 10 days, the aqueous extract inhibited 85% of [(3)H]FW binding while the hydroalcoholic extract markedly potentiated (200%) [(3)H]FW binding to AMPA receptors. Thus, our results showed that factors such as extraction solvent and extract stability determine the selectivity for glutamate receptor (GluR) interactions.
两种缬草根提取物（水提物和醇提物）的作用通过使用大鼠突触膜和不同受体配体的[(3)H]谷氨酸([(3)H]Glu)和[(3)H]氟威利定([(3)H]FW)受体结合测定进行了研究。此外，还通过分光光度法监测了提取物的稳定性。两种提取物均显示与离子型谷氨酸受体(iGluRs)相互作用。然而，提取物在受体选择性方面存在显著差异。醇提物选择性地与瓜氨酸(QA)，I 组代谢型谷氨酸受体(mGluR)配体相互作用，而水提物不改变 QA 的结合。在数周内检查了提取物的稳定性。新鲜制备的提取物抑制 38-60%的[(3)H]FW 结合(AMPA)。10 天后，水提物抑制了 85%的[(3)H]FW 结合，而醇提物则显著增强(200%)[(3)H]FW 与 AMPA 受体的结合。因此，我们的结果表明，提取溶剂和提取物稳定性等因素决定了对谷氨酸受体(GluR)相互作用的选择性。
