| Summary: | This study aimed to develop a comprehensive quantification of 20 bioactive compounds in Achillea millefolium L (A. millefolium) fractions obtained by different solvents (petroleum ether (pet-ether), ethyl acetate (EtOAc), methanol (MeOH) and water) using HPLC quantitative analysis. Additionally, total flavonoids (TF), total phenolics (TP), antioxidants (DPPH, ABTS) and cytotoxic activities of A. millefolium fractions on k562, HeLa, MCF7, A431 and A549 Cell Lines were evaluated using MTT assay [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] and compared to doxorubicin as a standard. According to the obtained results, TP ranged from 3.8 to 91.85 mg gallic acid equivalent (GAE)/g fraction, while TF ranged from 9.68 to 79.50 mg catechin equivalent (CE)/g generally. The lowest IC50 values were recorded for doxorubicin compared by all fractions except for EtOAc fraction against Hela cells, followed by water fraction, which showed the highest anticancer potential against MCF-7 cells. In contrast, the pet-ether fraction showed the lowest IC50 value against K562 cells. The cell cycle profile and apoptosis analysis of the EtOAc fraction was studied in HeLa cells. EtOAc fraction caused preG1 apoptosis and cell growth arrest in G2/M in HeLa cancer cells. Overall, this study heightens the importance of A. millefolium, which may be a promising and valuable source of natural antioxidant and anticancer agents to be used in the development of new functional and therapeutic compounds in the future.
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