Application of eupatilin in the treatment of osteosarcoma

Abstract

5,7‑dihydroxy‑3',4',6‑trimethoxyflavone, commonly known as eupatilin, is a traditional Asian medicinal plant, which is mainly used for the treatment of gastritis, as well as its use as an anti‑inflammatory agent. Eupatilin is a bioactive compound; however, its effects on osteosarcoma (OS) have remained to be elucidated. Therefore, the present study aimed to investigate the effects of eupatilin on this malignant bone tumor, using the U‑2 OS cell line. The experimental results revealed that eupatilin inhibited U‑2 OS cell growth in a concentration‑dependent manner and induced G2/M phase cell cycle arrest and apoptosis. Additionally, western blot analysis indicated that eupatilin was able to trigger the mitochondrial apoptotic pathway, demonstrated by the enhanced Bax/B cell lymphoma‑2 ratio, decrease in mitochondrial membrane potential, release of cytochrome c, caspase‑3 and ‑9 activation and poly(ADP‑ribose)polymerase cleavage detected in the U‑2 OS cells. These results indicated that eupatilin was able to inhibit U‑2 OS cancer cell proliferation by the induction of apoptosis via the mitochondrial intrinsic pathway. Eupatilin may therefore represent a novel anticancer drug for use in the treatment of osteosarcoma.