Cytotoxic Potential and Apoptotic Mechanism of Digigrandifloroside: A Cardioactive Glycoside Targeting Caspase 3/7

Authors : Vahap Murat Kutluay, İclal Saraçoğlu
Pages : 283-292
Doi:10.55262/fabadeczacilik.1569373
View : 29 | Download : 30
Publication Date : 2025-08-26
Article Type : Research Paper
Abstract :Cardioactive glycosides (CGs) have been used mainly for their positive inotropic effects. However, recent studies on CGs showed their antitumor potential in several cancers. Cytotoxicity of a CG digigrandifloroside was tested against MCF-7 and HeLa cancer cells by MTT method. Lanatoside A-C, and digitonin were also tested for comparison. To determine the role of apoptosis via caspase 3 and 7, Caspase-Glo 3/7 test was used. The predicted biological activities of the compounds were also evaluated via PASSONLINE database. IC50 values for cytotoxic activity of digigrandifloroside against MCF-7 and HeLa cells were found as<100 nM and 252.1 nM, respectively. Digigrandifloroside at 100 nM increased enzyme levels, 1.29 and 2.35 fold, compared to the control cells for MCF-7 and HeLa cells, respectively. These findings suggest the role of apoptosis. Digitonin, a steroidal saponin, showed relatively lower cytotoxicity when compared to CGs on both cells. According to the results obtained from PASSONLINE database, the potential biological activities of the compounds were reported as, anticarcinogenic activity, antineoplastic activity in lung and breast cancer, caspase 3 and 8 stimulant activity, tp53 expression enhancer activity, together with anti-inflammatory activity, and chemopreventive potential. Digigrandifloroside has an activating effect on caspase 3; this has been proved with the help of the biological activity testing. Digigrandifloroside IC50 found for MCF-7 cells is higher than for HeLa cells. It is a well-known fact that MCF-7 cells do not have caspase 3. That is why the higher IC50 found for MCF-7 cells can be connected with the tend to caspase 3 stimulation of digigrandifloroside.
Keywords : Kardiyoaktif glikozit, Digitalis, Sitotoksisite, Hela hücresi, MCF-7 hücresi

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