title: Membrane permeability-guided identification of neuroprotective components from Polygonum cuspidatun.
abstract: BACKGROUND
  Polygonum cuspidatum Sieb et Zucc. (Polygonaceae) possesses various pharmacological activities and has been widely using as one of the most popular and valuable Chinese herbal medicines in clinics. Its usage has increasingly attracted much of our attention and urges investigation on its bioactive components.
  
  
  OBJECTIVE
  To establish a rapid and valid approach for screening potential neuroprotective components from P. cuspidatum.
  
  
  METHODS
  Potential neuroprotective components from P. cuspidatum were screened utilizing liposome equilibrium dialysis followed by high-performance liquid chromatography (HPLC) analysis. Their neuroprotective effects on modulation of protein expression of α7 nAChR, α3 nAChR and synaptophysin (SPY) on SH-SY5Y human neuroblastoma cell line (SH-SY5Y) were evaluated by means of Western blotting.
  
  
  RESULTS
  Two potential compounds, polydatin (C1) and emodin-8-O-β-D-glucoside (C2), were detected and identified in our study. The biological tests showed that both compounds C1 and C2, respectively, at concentrations of 0.1 and 0.25 mg/mL significantly increased protein expression of α7 and α3 nicotinic acetylcholine receptors (nAChRs) in SH-SY5Y cells. Moreover, C1 and C2 at 0.1 mg/mL significantly reversed the Aβ₁₋₄₂-induced decrease of α7 and α3 nAChRs protein expression in SH-SY5Y cells. In addition, C2 at 0.1 mg/mL significantly increased protein expression of SPY in SH-SY5Y cells and Aβ1₁₋₄₂-induced SH-SY5Y cells whereas C1 did not provide any positive effects.
  
  
  CONCLUSIONS
  In conclusion, our approach utilizing liposome equilibrium dialysis combined with HPLC analysis and cell-based assays is a prompt and useful method for screening neuroprotective agents.
authors.affiliation: School of Pharmacy and.
authors.forename: Hai-tao
authors.initials: HT
authors.lastname: Xiao
authors.forename: Xiao-lan
authors.initials: XL
authors.lastname: Qi
authors.forename: Yan
authors.initials: Y
authors.lastname: Liang
authors.forename: Cheng-yuan
authors.initials: CY
authors.lastname: Lin
authors.forename: Xia
authors.initials: X
authors.lastname: Wang
authors.forename: Zhi-zhong
authors.initials: ZZ
authors.lastname: Guan
authors.forename: Xiao-yan
authors.initials: XY
authors.lastname: Hao
mesh_terms: D000880:Anthraquinones / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology; D015153:Blotting, Western; D045744:Cell Line, Tumor; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D003956:Dialysis / Q000379:methods; D004305:Dose-Response Relationship, Drug; D045468:Fallopia japonica / Q000737:chemistry*; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D005960:Glucosides / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D008081:Liposomes; D009447:Neuroblastoma / Q000473:pathology; D018696:Neuroprotective Agents / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D010539:Permeability; D010936:Plant Extracts / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D011978:Receptors, Nicotinic / Q000235:genetics; D013267:Stilbenes / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology; D064569:alpha7 Nicotinic Acetylcholine Receptor / Q000235:genetics
chemical_list: D000880:Anthraquinones; D005960:Glucosides; D008081:Liposomes; D018696:Neuroprotective Agents; D010936:Plant Extracts; D011978:Receptors, Nicotinic; D013267:Stilbenes; D064569:alpha7 Nicotinic Acetylcholine Receptor; C526172:emodin-8-O-beta-D-glucoside; C058229:polydatin