Chalcone Derivative 15 Induces Apoptosis in Human HOS, HCT116, and MCF-7 Cancer Cells

Abdelhalim, Esraa M.; Fahmi, Abdelgawad; El-Manawaty, May; Abdur-Rahman, Mariam

doi:10.21608/ejchem.2024.326942.10616

Chalcone Derivative 15 Induces Apoptosis in Human HOS, HCT116, and MCF-7 Cancer Cells

Document Type : Original Article

Authors

¹ Biotechnology Department, Faculty of Science, Cairo University, Egypt

² Chemistry Department, Faculty of Science, Cairo University, Egypt

³ Drug Bioassay-Cell Culture Laboratory, Pharmacognosy Department, National Research Centre, Dokki, Giza, Egypt

10.21608/ejchem.2024.326942.10616

Abstract

Cancer is one of the most life threating diseases requiring the search of novel treatment strategies. Our study aims to investigate the anticancer effect of new chalcone derivatives on human cancer HOS, HCT116, and MCF-7 lines. Both 2- and 3-D spheroid cell culture models were constructed, MTT / acid phosphatase cytotoxic assays were applied, and GraphPad PRISM was used to for IC50 values estimation. RT-qPCR analysis for apoptotic genes was conducted and followed by analysing of the cell cycle via flow cytometry. Screening results showed that exceeding Doxorubicin, a concentration of 200 µM of the Compound 15 exerted a significant in vitro cytotoxic activity of 96.50, 90.56, and 81.43 % with IC50 values of 32.73, 25.60, 22.65 µM on MCF-7, HCT116, and HOS cell lines, respectively. Compound 15 indicated a very high selectivity against tested lines of cancer relative to the normal one (hTERT RPE-1). Data from RT-qPCR reported that Compound 15 induces apoptosis in MCF-7 through upregulating P53 & BAX proapoptotic genes while simultaneously downregulating BCL-2 antiapoptotic gene. It also arrests the cellular cycle at the G0/G1 phase (85.36 %). Applied on 3-D spheroid culture model of MCF-7, Compound 15 induced an anti-cancer effect reaching 69.30 % with an IC50 value of 59.86 µM ±8.97. Hence, Compound 15 represents a potential synthetic chalcone-based drug against MCF-7 breast cancer, HCT116 colorectal carcinoma and HOS osteosarcoma human cancer cell lines.

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