Tsui Ko-Chung, Chiang Tzu-Hsuan, Wang Jinn-Shyan, Lin Li-Ju, Chao Wei-Chih, Chen Bing-Huei, Lu Jyh-Feng
School of Medicine, Fu Jen Catholic University, New Taipei City 24205, Taiwan.
Graduate Institute of Medicine, Fu Jen Catholic University, New Taipei City 24205, Taiwan.
Molecules. 2014 Oct 31;19(11):17663-81. doi: 10.3390/molecules191117663.
Flavonoids, containing mainly kaempferol rhamnohexoside derivatives, were extracted from Gynostemma pentaphyllum (G. pentaphyllum) and their potential growth inhibition effects against H460 non-small cell lung cancer cells was explored and compared to that on A549 cells. The extracted flavonoids were found to exhibit antiproliferation effects against H460 cells (IC50 = 50.2 μg/mL), although the IC50 of H460 is 2.5-fold that of A549 cells (IC50 = 19.8 μg/mL). Further investigation revealed that H460 cells are more susceptible to kaempferol than A549, whereas A549 cell growth is better inhibited by kaempferol rhamnohexoside derivatives as compared with H460. In addition, flavonoids from G. pentaphyllum induced cell cycle arrest at both S and G2/M phases with concurrent modulated expression of the cellular proteins cyclin A, B, p53 and p21 in A549 cells, but not H460. On the contrary, apoptosis and concomitant alteration in balance of BCL-2 and BAX expression as well as activation of caspase-3 were equally affected between both cells by flavonoid treatment. These observations strongly suggest the growth inhibition discrepancy between H460 and A549 following flavonoid treatment can be attributed to the lack of cell cycle arrest in H460 cells and the differences between H460 and A549 cells may serve as contrasting models for further mechanistic investigations.
从绞股蓝中提取了主要含有山柰酚鼠李糖己糖苷衍生物的黄酮类化合物，并探讨了它们对H460非小细胞肺癌细胞的潜在生长抑制作用，并与对A549细胞的作用进行了比较。结果发现，提取的黄酮类化合物对H460细胞具有抗增殖作用（IC50 = 50.2 μg/mL），尽管H460的IC50是A549细胞（IC50 = 19.8 μg/mL）的2.5倍。进一步研究表明，H460细胞比A549细胞对山柰酚更敏感，而与H460相比，山柰酚鼠李糖己糖苷衍生物对A549细胞生长的抑制作用更好。此外，绞股蓝中的黄酮类化合物使A549细胞的细胞周期在S期和G2/M期均发生阻滞，同时细胞蛋白周期蛋白A、B、p53和p21的表达受到调节，但对H460细胞无此作用。相反，黄酮类化合物处理对两种细胞的凋亡以及BCL-2和BAX表达平衡的伴随改变以及caspase-3的激活均有同等影响。这些观察结果强烈表明，黄酮类化合物处理后H460和A549之间生长抑制的差异可归因于H460细胞缺乏细胞周期阻滞，H460和A549细胞之间的差异可能作为进一步机制研究的对比模型。
