A novel stilbene derivative (GMQ3) suppressed proliferation and induced apoptosis in lung cancer via the p38-MAPK/SIRT1 pathway

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
出处
期刊:Biochemical Pharmacology [Elsevier BV]
卷期号:193: 114808-114808 被引量:1
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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