Active Components From Gouteng Danshen And Huangqin Target At NMDA Receptor And Its Complex

Object: Identification of active component from traditional Chinese medicine (TCM) targeting at N-methyl-D-aspartate receptors (NMDARs) and its complex. Methods: The whole-cell patch clamp technique and cytotoxicityexperiments were applied parallelly for detection of TCMs effectthrough NMDARs. Nuclear magnetic resonance (NMR) was used for detection of the binging of active component in TCMs with the postsynaptic density (PSD) through its second PDZ domain (PDZ2). Results: The presence of Mg2+ in the extracts of Scutellaria baicalensis, Stephania tetrandra, and Salvia miltiorrhiza was the blocker of NMDARs of these TCMs. The active compound "enp" isolated from the extracts of U. rhynchophylla revealed to have the NMDAR antagonist activity and blocked NMDA-induced neuronal death in vitro. Four flavones were isolated and found to account for the PDZ-binding activity of the extract of Scutellaria baicalensis. Conclusion: Some of TCMs effect by blocking of NMDARs. The blockage might be the channel blocker, interaction with NMDAR subunits or binding with the NMDAR complex protein.