Protosappanin B protects PC12 cells against oxygen-glucose deprivation-induced neuronal death by maintaining mitochondrial homeostasis via induction of ubiquitin-dependent p53 protein degradation

Eur J Pharmacol. 2015 Mar 15:751:13-23. doi: 10.1016/j.ejphar.2015.01.039. Epub 2015 Feb 2.

Abstract

Protosappanin B (PTB) is a bioactive dibenzoxocin derivative isolated from Caesalpinia sappan L. Here, we investigated the neuroprotective effects and the potential mechanisms of PTB on oxygen-glucose deprivation (OGD)-injured PC12 cells. Results showed that PTB significantly increased cell viability, inhibited cell apoptosis and up-regulated the expression of growth-associated protein 43 (a marker of neural outgrowth). Moreover, our study revealed that PTB effectively maintained mitochondrial homeostasis by up-regulation of mitochondrial membrane potential (MMP), inhibition of cytochrome c release from mitochondria and inactivation of mitochondrial caspase-9/3 apoptosis pathway. Further study showed that PTB significantly promoted cytoplasmic component degradation of p53 protein, a key negative regulator for mitochondrial function, resulting in a release of Bcl-2 from p53-Bcl-2 complex and an enhancing translocation of Bcl-2 to mitochondrial outer membrane. Finally, we found the degradation of p53 protein was induced by PTB via activation of a MDM2-dependent ubiquitination process. Taken together, our findings provided a new viewpoint of neuronal protection strategy for anoxia and ischemic injury with natural small molecular dibenzoxocin derivative by activating ubiquitin-dependent p53 protein degradation as well as increasing mitochondrial function.

Keywords: Mitochondrial dysfunction; Protosappanin B (PubChem CID: 102036-29-3); Ubiquition-dependent degradation; p53.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Caspase 3 / metabolism
  • Caspase 9 / metabolism
  • Cell Death / drug effects
  • Cytochromes c / metabolism
  • Glucose / deficiency*
  • Homeostasis / drug effects*
  • Mitochondria / drug effects*
  • Mitochondria / metabolism
  • Neurons / cytology
  • Neurons / drug effects*
  • Neurons / metabolism
  • Neuroprotective Agents / pharmacology
  • Oxocins / pharmacology*
  • Oxygen / metabolism*
  • PC12 Cells
  • Protein Transport / drug effects
  • Proto-Oncogene Proteins c-bcl-2 / metabolism
  • Proto-Oncogene Proteins c-mdm2 / metabolism
  • Rats
  • Tumor Suppressor Protein p53 / metabolism*
  • Ubiquitination / drug effects
  • Ubiquitins / metabolism*

Substances

  • Neuroprotective Agents
  • Oxocins
  • Proto-Oncogene Proteins c-bcl-2
  • Tumor Suppressor Protein p53
  • Ubiquitins
  • protosappanin B
  • Cytochromes c
  • Proto-Oncogene Proteins c-mdm2
  • Caspase 3
  • Caspase 9
  • Glucose
  • Oxygen