A Comparative Study of Novel Chalcone Derivatives and Ethanolic Extract of Nerium Oleander as an Anticancer Agent Using Different Cancer Cell Lines

Abstract

Background: Cancer is major global health concern. Some methods of cancer treatment are available, such as chemotherapy which has many side effects and shows drug resistance. Alternative treatments using herbal medicine or synthetic compound has been known as new therapeutic approaches which act as anticancer drugs with less or no toxic issue. Chalcone derivatives that exhibit a variety of physiological bioactivities and target multiple biological receptors. On the other hand, N.Olender a Mediterranean herb is well known for its cytotoxic effect. Objectives: 1. This project aimed to screen and compare the cytotoxic effect of new chalcones derivatives in comparison with the ethanolic extract of leaves of N.Olender using different human cancer cell lines with parallel to normal cell lines. 2. Molecular docking of the chalcones with some cellular protein markers. Methods: MTT assay was conducted using different concentration of CH4 and CH6 chalcones and the percentage of viability was calculated. The dose respond curve (IC50) was calculated using graphpad prism software, in addition, Molecular docking was conducted using Autodock Vina software. Results: Chalcones CH6 significantly decreased A549 cells viability in vitro. After 48 hours treatment, the IC50 value was 46 µg/ml that displayed the highest cytotoxic activity from all the tested compounds. Moreover As for N.olender, the colorectal (HCT116) has shown to be the most sensitive cell line to the crude with IC50 = 46 µg/ml versus other cancer cell line. While CH4 has a high cytotoxicity effect on prostate cell line (PC3) more than CH6 does with IC50 123.9 µg/ml and 375.3 µg/ml respectively. CH4 and CH6 has shown their high binding affinity towards C-MET and NOS protein receptors. Conclusion: The observed data indicate the validity of using N.Olender in colorectal cancer while CH6 for lung cancer treatments. Collected date have been discussed in view of previous literature. Sensitivity 12 might be the matter of deference in cell surface receptors on different cancer cell lines but interact differently with tested compounds.