Quercetin inhibits okadaic acid-induced tau protein hyperphosphorylation through the Ca2+‑calpain‑p25‑CDK5 pathway in HT22 cells

Int J Mol Med. 2018 Feb;41(2):1138-1146. doi: 10.3892/ijmm.2017.3281. Epub 2017 Nov 22.

Abstract

Alzheimer's disease (AD) is a common neurodegenerative disorder characterized by aberrant tau protein hyperphosphorylation, which eventually leads to the formation of neurofibrillary tangles. Hyperphosphorylated tau protein is considered as a vital factor in the development of AD and is highly associated with cognitive impairment. Therefore, it is recognized to be a potential therapeutic target. Quercetin (QUE) is a naturally occurring flavonoid compound. In the present study, the inhibitory effect of QUE on okadaic acid (OA)-induced tau protein hyperphosphorylation in HT22 cells was explored. Western blotting results indicated that QUE significantly attenuated OA‑induced tau protein hyperphosphorylation at the Ser396, Ser199, Thr231 and Thr205 sites. Further experiments demonstrated that QUE inhibited the activity of cyclin‑dependent kinase 5 (CDK5), a key enzyme in the regulation of tau protein, and blocked the Ca2+‑calpain‑p25‑CDK5 signaling pathway. These observations indicate the ability of QUE to decrease tau protein hyperphosphorylation and thereby attenuate the associated neuropathology. In conclusion, these results support the potential of QUE as a therapeutic agent for AD and other neurodegenerative tauopathies.

MeSH terms

  • Alzheimer Disease / chemically induced
  • Alzheimer Disease / drug therapy*
  • Alzheimer Disease / genetics
  • Alzheimer Disease / metabolism
  • Calcium / metabolism
  • Calpain / genetics
  • Calpain / metabolism
  • Cognitive Dysfunction / chemically induced
  • Cognitive Dysfunction / drug therapy*
  • Cognitive Dysfunction / metabolism
  • Cyclin-Dependent Kinase 5 / genetics
  • Cyclin-Dependent Kinase 5 / metabolism
  • Hippocampus / drug effects
  • Hippocampus / metabolism
  • Hippocampus / pathology
  • Humans
  • Nerve Tissue Proteins / genetics
  • Nerve Tissue Proteins / metabolism
  • Neurons / drug effects
  • Neurons / metabolism
  • Neurons / pathology
  • Okadaic Acid / toxicity
  • Phosphorylation / drug effects
  • Quercetin / administration & dosage*
  • tau Proteins / genetics
  • tau Proteins / metabolism*

Substances

  • Nerve Tissue Proteins
  • TPPP protein, human
  • tau Proteins
  • Okadaic Acid
  • Quercetin
  • Cyclin-Dependent Kinase 5
  • CDK5 protein, human
  • Calpain
  • Calcium