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6-Methoxyflavone induces S-phase arrest through the CCNA2/CDK2/p21CIP1 signaling pathway in HeLa cells

Chaihong Zhang1,2, Yuchong Quan3, Lijuan Yang1,2

  • 1The First Clinical Medical College of Lanzhou University, Lanzhou, Gansu, China.

Bioengineered
|March 5, 2022
PubMed

Insights

6-Methoxyflavone inhibits cervical cancer cell proliferation by inducing S-phase arrest. This anticancer effect is mediated through the cyclin A2/cyclin-dependent kinase 2/p21CIP1 pathway, impacting cell cycle progression.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Cervical cancer remains a significant global health concern, necessitating novel therapeutic strategies.
  • Understanding the molecular mechanisms underlying cancer progression is crucial for developing targeted treatments.
  • Flavonoids, like 6-methoxyflavone, are being investigated for their potential anticancer properties.

Purpose of the Study:

  • To elucidate the specific anticancer mechanism of 6-methoxyflavone in HeLa cervical cancer cells.
  • To identify the molecular targets and pathways affected by 6-methoxyflavone.
  • To investigate the interaction of 6-methoxyflavone with key cell cycle regulatory proteins.

Main Methods:

  • Utilized PharmMapper database for target identification, followed by microarray and transcriptome sequencing.
  • Performed functional and gene set enrichment analyses to explore target roles in cervical cancer.
  • Employed cell proliferation assays, cell cycle analysis, PCR, and Western blotting to confirm mechanisms.
  • Conducted molecular docking and noncovalent interaction analyses for structural validation.

Main Results:

  • Identified 178 putative targets for 6-methoxyflavone, with high mRNA expression of cyclin A2 (CCNA2) and cyclin-dependent kinase 2 (CDK2) linked to cervical cancer cell cycle progression.
  • 6-Methoxyflavone significantly inhibited HeLa cell proliferation and induced S-phase arrest.
  • The mechanism involves the CCNA2/CDK2/cyclin-dependent kinase inhibitor 1A (p21CIP1) pathway.
  • Molecular docking revealed strong affinity and inhibitory effects of 6-methoxyflavone on CDK2, enhanced by CCNA2 interaction.

Conclusions:

  • 6-Methoxyflavone exhibits anticancer activity in HeLa cells by inducing S-phase arrest.
  • The primary mechanism involves the modulation of the CCNA2/CDK2/p21CIP1 pathway, crucial for cell cycle regulation.
  • 6-Methoxyflavone demonstrates potential as a therapeutic agent for cervical cancer, warranting further investigation into its clinical relevance.
Keywords:
6-methoxyflavonecell cyclecervical cancermolecular dockingnetwork pharmacology

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