Antitumor effects of vanillin based chalcone analogs in vitro

Abstract

© 2020 Polish Pharmaceutical Society. All rights reserved. Chalcones, as a large group of organic compounds, are widely implemented in various types of anticancer therapeutics. These plant metabolites are present in fruits, vegetables, spices, and have anti-tumor, antiinflammation, immunomodulation, antibacterial and anti-oxidative activities, as well as many other pharmacological and biological effects. The aim of the present study was to investigate cytotoxic effects, type of cell death and mechanism of action of the newly synthesized vanillin based chalcone analogs, (CH1) and (CH2) on human colon cancer HCT-116 and noncancerous (control) MRC-5 cell lines. In order to compare the effects of vanillin based chalcone analogs on investigated cell lines, as reference substances cisplatin (cisPt) and dehydrozingerone (DHZ) were used. Investigation of antitumor effect of chalcone analogs on HCT-116 cells was carried out by three methods MTT assay, flow cytometry and immunofluorescence analysis. The result of our investigation indicated that newly synthesized vanillin based chalcone analogs expressed powerful antitumor effect on cancer cells (HCT-116 cell line), while their effect on healthy cells (MRC-5 cell line) was not statistically significant. Vanillin based chalcone analogs caused overexpression and activation of mitochondrial Bax protein and caspase-3 in HCT-116 cells, indicating that their mechanism of antitumor action was mediated through activation of the inner apoptotic pathway. These results indicate possible usefulness of CH1 and CH2 in antitumor therapy whether through its direct cytotoxic effect or as adjuvant therapy. Our results indicate possible usefulness of CH1 and CH2 vanillin based chalcone analogs in antitumor therapy.