Title:Anti-Metastatic Effects of Lupeol via the Inhibition of MAPK/ERK Pathway in Lung Cancer
VOLUME: 21 ISSUE: 2
Author(s):Mital Bhatt, Mitesh Patel*, Mohd Adnan and Mandadi N. Reddy
Affiliation:Bapalal Vaidya Botanical Research Centre, Department of Biosciences, Veer Narmad South Gujarat University, Surat, Gujarat, Bapalal Vaidya Botanical Research Centre, Department of Biosciences, Veer Narmad South Gujarat University, Surat, Gujarat, Department of Biology, College of Science, University of Ha’il, Ha’il, P O Box 2440, Bapalal Vaidya Botanical Research Centre, Department of Biosciences, Veer Narmad South Gujarat University, Surat, Gujarat
Keywords:Cancer, ERK, lupeol, metastasis, reverse docking, Epithelial-Mesenchymal Transition (EMT) marker genes.
Abstract:Background and Objective: ERK pathway is one of the most crucial pathways in lung cancer
metastasis. Targeting its pathway is decisive in lung cancer research. Thus, this study demonstrated for the first
time for significant and selective anti-metastatic effects of lupeol against lung cancer A549 cells via perturbations in
the ERK signaling pathway.
Materials and Methods: Human protein targets of lupeol were predicted in silico. Migration and cytotoxicity
assays were carried out in vitro. Expression levels of proteins Erk1/2 and pErk1/2 were ensured using Enzyme-
Linked Immunosorbent Assay (ELISA). Semi-quantitative RT-PCR technique was used to estimate changes in
crucial mesenchymal marker gene expression levels of N-cadherin and vimentin.
Results: Lupeol was found to target ERK and MEK proteins effectively. Despite having no cytotoxic effects,
lupeol also significantly inhibited cell migration in A549 cells with decreased expression of the pErk1/2 protein
along with N-cadherin and vimentin genes.
Conclusion: Lupeol inhibits cell migration, showed no cytotoxic effects on A549 cells, decreased pErk1/2 and
EMT gene expression. Thus, it can serve as a potential ERK pathway inhibitor in lung cancer therapeutics.
