Baicalein reduces E46K alpha-synuclein aggregation in vitro and protects cells against E46K alpha-synuclein toxicity in cell models of familiar Parkinsonism

J Neurochem. 2010 Jul;114(2):419-29. doi: 10.1111/j.1471-4159.2010.06752.x. Epub 2010 Apr 19.

Abstract

The E46K is a point mutation in alpha-synuclein (alpha-syn) that causes familial Parkinsonism with Lewy body dementia. We have now generated a cell model of Parkinsonism/Parkinson's disease (PD) and demonstrated cell toxicity after expression of E46K in the differentiated PC12 cells. E46K alpha-syn inhibited proteasome activity and induced mitochondrial depolarization in the cell model. Baicalein has been reported to inhibit fibrillation of wild type alpha-syn in vitro, and to protect neurons against several chemical-induced models of PD. We now report that baicalein significantly attenuated E46K-induced mitochondrial depolarization and proteasome inhibition, and protected cells against E46K-induced toxicity in a cell model of PD. Baicalein also reduced E46K fibrilization in vitro, with a concentration-dependent decrease in beta sheet conformation, though it increased some oligomeric species, and decreased formation of E46K alpha-syn-induced aggregates and rescued toxicity in N2A cells. Taken together, these data indicate that mitochondrial dysfunction, proteasome inhibition and specific aspects of abnormal E46K aggregation accompany E46K alpha-syn-induced cell toxicity, and baicalein can protect as well as altering aggregation properties. Baicalein has potential as a tool to understand the relation between different aggregation species and toxicity, and might be a candidate compound for further validation by using in vivo alpha-syn genetic PD models.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Cell Death
  • Cell Differentiation
  • Flavanones / pharmacology*
  • Membrane Potential, Mitochondrial / drug effects
  • Mutation
  • Neurons / metabolism
  • Neurons / ultrastructure
  • PC12 Cells
  • Parkinsonian Disorders / genetics
  • Parkinsonian Disorders / metabolism*
  • Proteasome Inhibitors
  • Rats
  • alpha-Synuclein / biosynthesis
  • alpha-Synuclein / genetics*

Substances

  • Flavanones
  • Proteasome Inhibitors
  • alpha-Synuclein
  • baicalein