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 a
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 geneexpression levels of Ncadherin 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.