Department of Applied Chemistry, Dongduk Women's University, Seoul, Republic of Korea.
Rappeler Company (4F) 39, Gyeonggi-do, Republic of Korea.
Anticancer Res. 2024 Mar;44(3):1109-1120. doi: 10.21873/anticanres.16906.
BACKGROUND/AIM: Phloretin is a natural flavonoid compound found in some plants, such as apples and pears, as well as in the bark of apple trees. Phloretin has been shown to have inhibitory effects on glucose transporters in cells and can potentially inhibit the growth of cancer cells. However, the mechanism by which phloretin regulates the expression of estrogen receptor alpha (ERα), a key transcription factor in breast cancer, is still unclear. This study investigated how phloretin affects the growth of ERα positive human breast cancer cells.
The growth of breast cancer cell lines, including MCF7 and T47D, was examined using cell proliferation and colony formation assays. Western blotting and semi-quantitative RT-PCR were used to examine protein and mRNA levels, respectively. Localization of cellular proteins was analyzed using subcellular fractionation. Transient transfection and reported gene assays were used to elucidate the impact of phloretin on cell proliferation and ERα transactivation.
Phloretin decreased ERα expression at the mRNA and protein levels in MCF7 and T47D cells. It also inhibited the binding of ERα to the estrogen response element present in the promoter of target genes. Moreover, treatment with phloretin inhibited the expression of cyclin D1 and breast cancer marker gene pS, which are known ERα target genes. Consequently, it inhibited the growth of ERα-positive human breast cancer cells. Furthermore, inhibition of breast cancer growth by phloretin was found to be mediated through both the ERα and ERK1/ERK2 pathways.
Phloretin, a dihydrochalcone extracted from natural sources, exhibits the ability to regulate ERα function and suppress breast cancer cell proliferation.
背景/目的：根皮苷是一种天然类黄酮化合物，存在于一些植物中，如苹果和梨，以及苹果树的树皮中。根皮苷已被证明对细胞中的葡萄糖转运蛋白具有抑制作用，并可能抑制癌细胞的生长。然而，根皮苷调节雌激素受体α（ERα）表达的机制，ERα 是乳腺癌中的关键转录因子，仍不清楚。本研究探讨了根皮苷如何影响 ERα 阳性人乳腺癌细胞的生长。
使用细胞增殖和集落形成测定法检查乳腺癌细胞系 MCF7 和 T47D 的生长情况。使用 Western blot 和半定量 RT-PCR 分别检测蛋白质和 mRNA 水平。使用亚细胞分级分离分析细胞内蛋白质的定位。瞬时转染和报告基因测定用于阐明根皮苷对细胞增殖和 ERα 反式激活的影响。
根皮苷降低 MCF7 和 T47D 细胞中 ERα 的 mRNA 和蛋白水平。它还抑制 ERα 与靶基因启动子中存在的雌激素反应元件的结合。此外，用根皮苷处理抑制了已知的 ERα 靶基因 cyclin D1 和乳腺癌标志物基因 pS 的表达。因此，它抑制了 ERα 阳性人乳腺癌细胞的生长。此外，发现根皮苷通过 ERα 和 ERK1/ERK2 途径抑制乳腺癌的生长。
根皮苷，一种从天然来源提取的二氢查尔酮，具有调节 ERα 功能和抑制乳腺癌细胞增殖的能力。
