Research Institute of Life Science and College of Veterinary Medicine, Gyeongsang National University, Gazwa, Jinju 660-701, Republic of Korea.
Food Chem. 2012 Dec 15;135(4):2728-35. doi: 10.1016/j.foodchem.2012.06.097. Epub 2012 Jul 6.
This study investigated the anti-proliferative and apoptotic effect of flavonoids isolated from Korean Citrus aurantium L. using A549 lung cancer cells. Flavonoids potently inhibited of A549 cells in a dose-dependent manner, whereas flavonoids had a weak inhibitory effect on proliferation of WI-38 cells. Flow cytometry and Western blot analysis showed that flavonoids induced cell cycle arrest at the G2/M checkpoint by controlling the proteins expression level of cyclin B1, cdc2, cdc25c and p21(WAF1/CIP1). Also, flavonoids induced apoptosis through the regulation of the expression of caspases, cleaved PARP and Bax/Bcl-xL ratio. The activity of caspase-3 on A549 cells increased in a dose-dependent manner. These results clearly indicated that the anti-cancer effect of flavonoids on A549 cells follows multiple cellular pathways through G2/M arrest and the induction of apoptosis.
本研究使用 A549 肺癌细胞，考察了从韩国枳椇中分离得到的类黄酮的抗增殖和促凋亡作用。类黄酮能以剂量依赖的方式强烈抑制 A549 细胞，而对 WI-38 细胞的增殖仅有微弱的抑制作用。流式细胞术和 Western blot 分析表明，类黄酮通过调控细胞周期蛋白 B1、cdc2、cdc25c 和 p21(WAF1/CIP1)的蛋白表达水平，诱导细胞周期阻滞于 G2/M 期检查点。此外，类黄酮通过调节 caspase、裂解 PARP 和 Bax/Bcl-xL 比值诱导细胞凋亡。A549 细胞中 caspase-3 的活性呈剂量依赖性增加。这些结果清楚地表明，类黄酮对 A549 细胞的抗癌作用通过 G2/M 期阻滞和诱导凋亡等多种细胞途径发挥作用。
