Phytochemicals are natural products which extracted from vegetables, fruits or plant roots by chemical methods. The interest in phytochemicals as anticancer agents were progressively developed in the last decades as they are safer than chemotherapy on human health. Breast safeguard (BSG), the drug under study, is a commercial product consisted of seven phytochemical compounds. This study aims to assess the impact of two different extraction approaches in increasing the efficacy of BSG in sensitizing the HepG2 cells for Docetaxel. The extraction of BSG was conducted by either 20% DMSO or 100% DMSO then diluted to 20% concentration using a complete media of cell culture. The phenolics and flavonoids contents and the antioxidant activity using DPPH assay was evaluated in both extracts. The effect of the two extracts on HepG2 cell proliferation and migration was tested using MTT assay and wound healing assay, respectively. The data revealed a significant effect of the second approach (100% DMSO) in increasing the antioxidant activity of BSG indicated by the significant increase at phenolic, flavonoid content confirmed by the marked decrease at IC50 compared to ascorbic acid as a reference standard. MTT assay indicated a significant effect of the second approach in inhibiting HepG2 cell proliferation in a dose dependent manner compared to the first approach (20% DMSO). Estimation of the wound size of the treated cells revealed a marked effect of second approach in inhibiting cell migration in comparison with the first approach. We concluded that the extraction of phytochemicals content using 100% DMSO not the 20% pre-diluted DMSO would provide a significant increase at the phenolic and flavonoid content which in turn lead to a significant increase at antioxidant activity and significant inhibition at HepG2 cell proliferation and migration pointing out BSG as a potent anticancer agent.