Laboratory of Molecular Pharmacology, School of Pharmacy, Yantai University, Yantai, Shandong Province 264005, China.
Curr Mol Med. 2012 Feb;12(2):163-76. doi: 10.2174/156652412798889063.
The purpose of this study was to test the hypothesis that administration of epigallocatechin-3-gallate (EGCG), a polyphenol present in abundance in widely consumed tea, inhibits cell proliferation, invasion, and angiogenesis in breast cancer patients. EGCG in 400 mg capsules was orally administered three times daily to breast cancer patients undergoing treatment with radiotherapy. Parameters related to cell proliferation, invasion, and angiogenesis were analyzed while blood samples were collected at different time points to determine efficacy of the EGCG treatment. Compared to patients who received radiotherapy alone, those given radiotherapy plus EGCG for an extended time period (two to eight weeks) showed significantly lower serum levels of vascular endothelial growth factor (VEGF), hepatocyte growth factor (HGF), and reduced activation of metalloproteinase-9 and metalloproteinase-2 (MMP9/MMP2). Addition of sera obtained from patients treated with combination of radiotherapy and EGCG feeding for 2-8 weeks to in vitro cultures of highly-metastatic human MDA-MB-231 breast cancer cells resulted in the following significant changes: (1) suppression of cell proliferation and invasion; (2) arrest of cell cycles at the G0/G1 phase; (3) reduction of activation of MMP9/MMP2, expressions of Bcl-2/Bax, c-Met receptor, NF-κB, and the phosphorylation of Akt. MDA-MB-231 cells exposed to 5-10 µM EGCG also showed significant augmentation of the apoptosis inducing effects of γ-radiation, concomitant with reduced NF-κB protein level and AKT phosphorylation. These results provide hitherto unreported evidence that EGCG potentiated efficacy of radiotherapy in breast cancer patients, and raise the possibility that this tea polyphenol has potential to be a therapeutic adjuvant against human metastatic breast cancer.
表没食子儿茶素没食子酸酯(EGCG),一种在广泛食用的茶中大量存在的多酚,可抑制乳腺癌患者的细胞增殖、侵袭和血管生成。将 400mg 胶囊形式的 EGCG 口服每日三次给予接受放射治疗的乳腺癌患者。在不同时间点采集血液样本以分析与细胞增殖、侵袭和血管生成相关的参数,以确定 EGCG 治疗的疗效。与单独接受放疗的患者相比,那些接受放疗加 EGCG 延长时间(2-8 周)治疗的患者,其血清血管内皮生长因子(VEGF)、肝细胞生长因子(HGF)水平明显降低,基质金属蛋白酶-9 和基质金属蛋白酶-2(MMP9/MMP2)的活性降低。将来自接受放疗和 EGCG 联合治疗 2-8 周的患者的血清添加到体外高转移性人 MDA-MB-231 乳腺癌细胞培养物中,导致以下显著变化:(1)抑制细胞增殖和侵袭;(2)细胞周期停滞在 G0/G1 期;(3)降低 MMP9/MMP2、Bcl-2/Bax、c-Met 受体、NF-κB 和 Akt 磷酸化的活性。暴露于 5-10μM EGCG 的 MDA-MB-231 细胞也显示出 γ 辐射诱导凋亡作用的显著增强,同时 NF-κB 蛋白水平和 AKT 磷酸化降低。这些结果提供了迄今为止未报道的证据,表明 EGCG 增强了乳腺癌患者放疗的疗效,并提出了这种茶多酚有可能成为治疗人类转移性乳腺癌的辅助药物的可能性。