Ximenynic acid is a conjugated enyne
fatty acid, which is currently of interest due to its anti-inflammatory activity. Due to the association between
inflammation and
cancer, the present study was designed to investigate the anti‑cancer activity of
ximenynic acid in the HepG2 human
hepatoma cell line and the underlying mechanisms. The current study demonstrated the anti‑proliferation and pro‑apoptosis activities of
ximenynic acid by cell viability assay and flow cytometry analysis. The expression of anti‑apoptosis
protein silent information regulator T1 (
SIRT1) was significantly suppressed by
ximenynic acid. Furthermore,
ximenynic acid blocked G1/S phase transition by inhibiting the
protein expression of the cell cycle‑associated
protein general control of
amino acid synthesis yeast homolog like 2 (GCN5L2), and the
mRNA expression of cyclin D3 and
cyclin E1. Furthermore,
ximenynic acid suppressed the expression of angiogenesis‑associated genes, including
vascular endothelial growth factor (
VEGF)‑B and VEGF‑C. Finally,
ximenynic acid significantly inhibited the expression of cyclooxygenase‑1 (COX‑1)
mRNA and
protein, however COX‑2 expression was not reduced. The results of the present study suggested that
ximenynic acid may inhibit growth of HepG2 cells by selective inhibition of COX‑1 expression, which leads to cell cycle arrest, and alters the apoptosis pathway and expression of angiogenic factors. The current study aimed to investigate whether
ximenynic acid might be developed as novel
anticancer agent.