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Controlling non small cell lung cancer progression by blocking focal adhesion kinase-c-Src active site with

Hyacinth N Highland1, Monica B Thakur2, Linz-Buoy George1

  • 1Department of Zoology, Biomedical Technology and Human Genetics, School of Sciences, Gujarat University, Ahmedabad, Gujarat, India.

Journal of Cancer Research and Therapeutics
|November 22, 2022
PubMed
Abstract

Insights

Rosmarinus officinalis L. extract shows potential as an alternative therapy for non-small cell lung cancer (NSCLC). Its phytocomponents inhibit key proteins (c-Src, FAK) involved in cancer progression and exhibit significant antioxidant and antiproliferative effects.

Area of Science:

  • Phytochemistry
  • Molecular Biology
  • Oncology

Background:

  • Non-small cell lung cancer (NSCLC) presents significant therapeutic challenges with conventional treatments.
  • Proto-oncogene tyrosine kinase Src (c-Src) and focal adhesion kinase (FAK) overexpression drives NSCLC proliferation and invasion.
  • Phytocomponents offer a promising avenue for novel cancer interventions due to their potential efficacy and reduced side effects.

Purpose of the Study:

  • To investigate the in silico and in vitro efficacy of Rosmarinus officinalis L. (rosemary) hydroalcoholic extract against NSCLC.
  • To identify specific phytocomponents that can inhibit the activity of c-Src and FAK kinases.
  • To evaluate the antiproliferative and antioxidant potential of rosemary extract in NSCLC models.

Main Methods:

  • In silico molecular docking was performed to assess ligand-protein interactions with FAK and c-Src.
  • Phytochemical analysis and antioxidant activity assays (DPPH) were conducted on the rosemary extract.
  • In vitro antiproliferative effects were evaluated using MTT assays on A549 NSCLC cell lines.

Main Results:

  • In silico analysis revealed rosmarinic acid effectively binds to and inhibits FAK and c-Src.
  • The hydroalcoholic extract demonstrated potent, dose-dependent antiproliferative activity against NSCLC cells.
  • The extract exhibited high antioxidant activity (94.9%), indicating free radical scavenging capabilities.

Conclusions:

  • Phytocomponents in R. officinalis L. extract can inhibit FAK and c-Src, crucial targets in NSCLC.
  • The extract possesses significant antiproliferative and antioxidant properties, making it a viable candidate for NSCLC treatment.
  • Rosmarinus officinalis L. extract shows promise as an effective alternative or complementary therapy for NSCLC.
Keywords:
AntiproliferativeRosmarinus officinalis L.focal adhesion kinasenon small cell lung cancerproto-oncogene tyrosine kinase

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