体内
细胞凋亡
p38丝裂原活化蛋白激酶
MAPK/ERK通路
化学
癌症研究
细胞
癌症
细胞周期检查点
细胞生长
细胞生物学
生物
细胞周期
癌细胞
肺癌
信号转导
医学
内科学
生物化学
生物技术
作者
Mengling Xia,He Cao,Jing Zheng,Yinan Yao,Fei Xu,Guohua Lü,Yongmin Ma,Jianying Zhou
标识
DOI:10.1016/j.bcp.2021.114808
摘要
Lung cancer is the primary cause of cancer-related mortality worldwide. The anticancer effect of stilbene has been noted in various tumor types. GMQ3, which has a stilbene-mimicking skeleton, is a novel small-molecule compound with promising antitumor activity. Our results revealed that GMQ3 not only suppressed cell proliferation and cell migration of lung cancer cells but also led to G1 phase cell cycle arrest and triggered caspase-dependent apoptosis. Furthermore, investigation of the molecular mechanism showed that GMQ3 could inhibited proliferation and induced apoptosis via the p38-MAPK/SIRT1 pathway both in vitro and in vivo. Xenograft tumor mouse models showed that GMQ3 significantly inhibited tumor growth in vivo without affecting body weight. Our findings indicated that GMQ3 exerts a strong anticancer action by suppressing cell proliferation, inhibiting cell migration and inducing cell apoptosis. Moreover, the efficacy of GMQ3 was enhanced in the presence of CDK4/6 inhibitor Abemaciclib. We conclude that GMQ3 is a promising agent with potential for lung cancer.
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