Ampelopsis megalophylla has been found to demonstrate anticancer activities in human
cancer cells; however, the effect of total
flavone extract (
TFE), commonly used in
Traditional Chinese Medicine, remains unclear. Furthermore, there is limited information on its effects on
breast cancer cell lines. The present study aimed to investigate the inhibitory effects of
TFE in different human
cancer cell lines. In addition, the underlying mechanisms and the signaling pathways involved were also investigated by determining
tumor cell morphological changes, and differences in the cell cycle, apoptosis, mitochondrial transmembrane potential, and related
protein expression levels in a
breast cancer cell line. It was found that
TFE inhibited proliferation in seven
cancer cell lines (HeLa, A549, MCF‑7, HepG2, A2780, SW620 and MDA‑MB‑231 and demonstrated a strong inhibitory effect on MCF‑7 cell proliferation. Cell morphological changes were also observed and arrested at the G2/M phase following treatment with
TFE at different concentrations. In addition,
TFE disrupted the mitochondrial membrane potential and upregulated the expression level of apoptotic
proteins, including caspase‑3, ‑8 and ‑9, the Bax/Bcl‑2 ratio, and Apaf‑1 in time‑dependent manner. These results indicated that
TFE induced apoptosis of the MCF‑7 cells via a mitochondrial‑mediated apoptotic pathway. In conclusion,
TFE is potentially effective in treating
breast cancer.