Lung cancer has been threatening human health worldwide for a long time. However, the clinic
therapies remain unsatisfactory. In this study, the anti-
adenocarcinoma lung cancer A549 cell line abilities of Tetrastigma hemsleyanum tuber
flavonoids (THTF) were evaluated in vivo, and isobaric tags for relative and absolute quantification (iTRAQ)-based proteomic analysis was conducted to detect the
protein alterations in THTF-treated solid
tumors. The differentially expressed
proteins were related to the cytoskeleton and mostly accumulated in the calcium signaling pathway. The in vitro study illustrated that 80 μg mL-1 THTF significantly suppressed cellular viability to approximately 75% of the control. Further results suggested that
kaempferol-3-O-rutinoside (K3R), the major component of THTF, effectively triggered cytoskeleton collapse,
mitochondrial dysfunction and consequent
calcium overload to achieve apoptosis, which remained consistent with proteomic results. This study uncovers a new mechanism for THTF anti-
tumor ability, and suggests THTF and K3R as promising anti-
cancer agents, providing new ideas and possible strategies for future anti-
lung cancer prevention and
therapy.