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Diosmetin Induces Cell Apoptosis by Regulating CYP1A1/CYP1A2 Due to p53 Activation in HepG2 Cells

Bin Liu1, Kaiqiao Jia1, Yu Yang2

  • 1Laboratory of Hepatobiliary Surgery, Zhanjiang Key Laboratory of Hepatobiliary Diseases, Guangdong Medical University, Zhanjiang 524001. China.

Protein and Peptide Letters
|March 2, 2017
PubMed

Insights

Diosmetin, a natural flavonoid, shows anti-cancer effects by inducing apoptosis in HepG2 cells. This activity involves the p53 enzyme regulating Cytochrome P450 CYP1A, crucial for diosmetin

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Cytochrome P450 (CYP) enzymes, particularly the CYP1 family, are often overexpressed in various cancers.
  • Natural compounds like flavonoids are being investigated for their potential anti-cancer properties.

Purpose of the Study:

  • To investigate the anti-proliferative effects and metabolism of the flavonoid diosmetin in human hepatoma HepG2 cells.
  • To explore the role of p53 and Cytochrome P450 CYP1A1/CYP1A2 in diosmetin's anti-cancer activity.

Main Methods:

  • Utilized human hepatoma HepG2 cells expressing CYP1 family enzymes.
  • Administered diosmetin and PFT-α (p53 blockade) to cells, examining protein levels of p53 and CYP1A1/CYP1A2.
  • Assessed diosmetin-induced apoptosis and its modulation by p53 blockade.

Main Results:

  • Diosmetin treatment upregulated both p53 and CYP1A1/CYP1A2 protein levels in HepG2 cells.
  • PFT-α treatment downregulated p53 while upregulating CYP1A1/CYP1A2.
  • Co-treatment with diosmetin and PFT-α resulted in downregulated p53 and upregulated CYP1A1/CYP1A2, similar to diosmetin alone.

Conclusions:

  • Diosmetin induces apoptosis in HepG2 cells, an effect that can be reversed by blocking p53.
  • The p53 enzyme plays a significant role in regulating Cytochrome P450 CYP1A, mediating diosmetin's anti-cancer effects in HepG2 cells.
Keywords:
ApoptosisCYP1A1/CYP1A2DiosmetinHepG2P53PFT-α

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