Phytochemical Investigation and Cytotoxic Profile of Genistein Isolated from the Cytisus scoparius Linn. on Topoisomerase II

Abstract

Background: Genistein is one of many new cytotoxic drug leads that have been discovered recently. It is a well-studied chemopreventive drug that has attracted the attention of the scientific community due to its favourable effects on grave illnesses in humans such as cancer. Objective: The present study focuses on the methanolic extraction, isolation, and characterization of an isoflavone, genistein, from the weed plant of Cytisus scoparius Linn. (family: Fabaceae). Methods: The phytochemical structure of genistein was confirmed by its spectral and chromatography analysis through IR, HPTLC, LCMS, NMR, etc. The total flavonoid fraction of methanolic extracts containing genistein was evaluated for in-vitro cytotoxic activity on cervical cancer HeLa cells using MTT assay, cell cycle analysis, and topoisomerase II inhibitory activity. Results: The result of the in-vitro cytotoxicity study showed the IC50 value of 4.5 μg/ml, which shows that the isolated compound is cytotoxic. The result of cell cycle analysis revealed the cell arrest at a sub-G phase, which shows that the isolated compound was apoptotic. Moreover, the human topoisomerase II assay proved that it is an excellent human topoisomerase II inhibitor at 10 μg/ml. Conclusion: These findings revealed that genistein increased cytotoxicity and cell arrest owing to human topoisomerase II inhibitory activity and thus it may be an anti-cancer component. The relationship between the phytochemical structural analysis of this compound and its bioactivities is discussed.