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Anticancer activity of THMPP: Downregulation of PI3K/ S6K1 in breast cancer cell line

Suresh Palanivel1,2, Akshaya Murugesan1,2,3, Olli Yli-Harja2,4,5

  • 1Molecular Signaling Lab, Faculty of Medicine and Health Technology, Tampere University and BioMediTech, Tays Cancer Center, Tampere University Hospital, P.O. Box 553, 33101 Tampere, Finland.

Saudi Pharmaceutical Journal : SPJ : the Official Publication of the Saudi Pharmaceutical Society
|April 11, 2020
PubMed

Insights

This study reveals that 2-((1, 2, 3, 4-Tetrahydroquinolin-1-yl) (4 methoxyphenyl) methyl) phenol (THMPP) induces breast cancer cell death by activating apoptosis and downregulating the EGFR signaling pathway. THMPP shows potential as an effective anti-breast cancer drug candidate.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Breast cancer is a prevalent malignancy in women, necessitating novel therapeutic strategies.
  • The anticancer potential of 2-((1, 2, 3, 4-Tetrahydroquinolin-1-yl) (4 methoxyphenyl) methyl) phenol (THMPP) against human breast cancer requires elucidation.
  • Understanding THMPP's mechanism of action, signaling pathways, and drug-likeness is crucial for its development.

Purpose of the Study:

  • To investigate the anticancer activity of THMPP against human breast cancer cell lines.
  • To elucidate the molecular mechanisms underlying THMPP-induced apoptosis.
  • To assess the drug-likeness and potential therapeutic efficacy of THMPP.

Main Methods:

  • Cell viability and proliferation assays (MTT) were performed on MCF-7, SkBr3, and H9C2 cell lines.
  • Apoptosis was evaluated through caspase activity assays, DNA fragmentation, Annexin V staining, and AO/EtBr staining.
  • Gene expression analysis (RT-PCR), quantitative structure-activity relationship (QSAR), ADME analysis, and molecular docking were employed.

Main Results:

  • THMPP demonstrated significant cytotoxicity against MCF-7 and SkBr3 breast cancer cells at specific IC50 concentrations.
  • THMPP induced apoptosis, evidenced by increased caspase-3 and -9 levels, DNA fragmentation, and phosphatidylserine translocation.
  • THMPP downregulated PI3K/S6K1 gene expression via the EGFR signaling pathway, with molecular docking confirming THMPP-EGFR binding.

Conclusions:

  • THMPP effectively induces apoptosis in human breast cancer cells.
  • The EGFR signaling pathway plays a key role in mediating THMPP's anticancer effects.
  • THMPP exhibits favorable drug-likeness properties, positioning it as a promising candidate for breast cancer therapy.
Keywords:
ADMEADME-Absorption, Distribution, Metabolism, and ExcretionAO/EtBr, Acridine orange/ethidium bromideApoptosisDockingEGFREGFR, Epidermal Growth Factor ReceptorER, Estrogen ReceptorFACS, Fluorescence-activated cell sortingFITC, Fluorescein isothiocyanateGene expressionIC50, The half maximal inhibitory concentrationMCF-7, Michigan Cancer Foundation-7PI3K, Phosphoinositide 3-kinasePR, Progesterone ReceptorQSARQSAR, Quantitative structure activity relationshipRTPCR, Reverse Transcriptase PCRSkBr3, Sloan–Kettering Cancer CenterTHMPP, 2-((1, 2, 3, 4-Tetrahydroquinolin-1-yl) (4 methoxyphenyl) methyl) phenolTetrahydroquinoline

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