Inhibition of epidermal growth factor receptor by ferulic acid and 4-vinylguaiacol in human breast cancer cells
To examine the potential of ferulic acid and 4-vinylguaiacol for inhibiting epidermal growth factor receptor (EGFR) in human breast cancer cells in vitro.
Ferulic acid and 4-vinylguaiacol limit the EGF (epidermal growth factor)-induced breast cancer proliferation and new DNA synthesis. Western blot analysis revealed both ferulic acid and 4-vinylguaiacol exhibit sustained inhibition of EGFR activation through down-regulation of Tyr 1068 autophosphorylation. Molecular docking analysis shows ferulic acid forming hydrogen bond interaction with Lys 745 and Met 793 whereas, 4-vinylguaiacol forms two hydrogen bonds with Phe 856 and exhibits stronger hydrophobic interactions with multiple amino acid residues at the EGFR kinase domain.
Ferulic acid and 4-vinylguaiacol could serve as a potential structure for the development of new small molecule therapeutics against EGFR.
KeywordsBreast cancer Epidermal growth factor receptor Ferulic acid 4-Vinylguaiacol
The Authors thank University Grants Commission, Government of India for the major research grant (F.No. 40-182/2011 (SR)). We thank departmental level assistance programmes UGC-SAP-DSA-I (No.F.5-6/2015/DSA-I (SAP-II), DST-PURSE, and DBT-BUILDER (BT/PR12153/INF/22/200/2014), Government of India for their support.
Biotransformation of ferulic acid to 4-vinylguaiacol.
Identification of 4-vinylguaiacol.
Supplementary Fig. 1—13C NMR analysis of ferulic acid and 4-vinylguaiacol.
Compliance with ethical standards
Conflict of interest
The authors declare that there are no conflicts of interest.
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