杨梅醇 5-氟苯甲醚通过调节生存素通路抑制人肺腺癌细胞 A549 的体外生长。
Myricanol 5-fluorobenzyloxy ether regulation of survivin pathway inhibits human lung adenocarcinoma A549 cells growth in vitro.
机构信息
Zhejiang Academy of Traditional Chinese Medicine, Institute of Basic Medicine, Hangzhou, 310007, China.
Zhejiang University-University of Edinburgh Institute, Zhejiang University, Haining, 314400, China.
出版信息
BMC Complement Med Ther. 2020 Sep 3;20(1):269. doi: 10.1186/s12906-020-03062-8.
BACKGROUND
This study aimed to explore the growth inhibitory effect of myricanol 5-fluorobenzyloxy ether (5FEM) and its underlying mechanisms in human lung adenocarcinoma A549 cells in vitro.
METHODS
5FEM was obtained by the chemical modification of myricanol with fluorobenzyloxy ether at the OH(5) position. The cytotoxicity, cell apoptosis, cell cycle, mitochondrial membrane potential (ΔΨm), scratch test, colony formation, and the expression levels of the key survivin pathway-related genes in A549 were evaluated.
RESULTS
5FEM could significantly inhibit A549 cell growth; induce cell apoptosis; increase G0/G1 population; reduce ΔΨm; inhibit cell migration and colony formation; upregulate caspase-9, P21, and Bax expression levels; and downregulate PARP, survivin, and Bcl-2 expression level.
CONCLUSION
These results enhanced our understanding of 5FEM and aid the discovery of novel myricanol derivatives as potential antitumor agents.
背景
本研究旨在探讨 5-氟苯甲氧基醚(myricanol 5-fluorobenzyloxy ether，5FEM)对人肺腺癌细胞 A549 体外生长的抑制作用及其作用机制。
方法
用氟苯甲氧基醚对 myricanol 的 OH(5)位进行化学修饰得到 5FEM。评估 5FEM 对 A549 细胞的细胞毒性、细胞凋亡、细胞周期、线粒体膜电位（ΔΨm）、划痕实验、集落形成以及关键存活素途径相关基因的表达水平。
结果
5FEM 能显著抑制 A549 细胞生长；诱导细胞凋亡；增加 G0/G1 期细胞比例；降低 ΔΨm；抑制细胞迁移和集落形成；上调 caspase-9、P21 和 Bax 的表达水平；下调 PARP、存活素和 Bcl-2 的表达水平。
结论
这些结果加深了我们对 5FEM 的认识，并有助于发现新型 myricanol 衍生物作为潜在的抗肿瘤药物。
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