Yu Hai-ning, Shen Sheng-rong, Xiong Yao-kang
Department of Tea Science, School of Agriculture and Biotechnology, Zhejiang University, Hangzhou 310009, China.
J Zhejiang Univ Sci B. 2005 Feb;6(2):125-31. doi: 10.1631/jzus.2005.B0125.
Epigallocatechin-3-gallate (EGCG) has shown remarkably anti-cancer activity, with its bioactivity being related to reactive conditions, such as pH and metal ions. The present study investigated the degradation of EGCG and its effect on prostate cancer cell in the presence of Cu2+. EGCG was incubated with prostate cancer cells, LNCaP, pretreated with or without Cu2+. EGCG in F-12 medium was quantified using HPLC and the viability of cells was assessed by gel electrophoresis, flow cytometry, and electron microscope. The results of HPLC showed that EGCG degraded completely within 12 h in F-12 medium with or without Cu2+. Gel electrophoresis and flow cytometry did not detect apoptosis of LNCaP cells when they were incubated with EGCG. Electron microscopy examination revealed that EGCG-Cu2+ complex led to damage of cytoplasm membrane in LNCaP cells. It was speculated that not EGCG, but its oxide and complex with Cu2+, are the bioactive components responsible for its cytotoxicity to LNCaP prostate cancer cells.
表没食子儿茶素-3-没食子酸酯(EGCG)已显示出显著的抗癌活性,其生物活性与反应条件有关,如pH值和金属离子。本研究调查了在Cu2+存在下EGCG的降解及其对前列腺癌细胞的影响。将EGCG与经或未经Cu2+预处理的前列腺癌细胞LNCaP一起孵育。使用高效液相色谱法(HPLC)对F-12培养基中的EGCG进行定量,并通过凝胶电泳、流式细胞术和电子显微镜评估细胞活力。HPLC结果表明,无论有无Cu2+,EGCG在F-12培养基中12小时内完全降解。当LNCaP细胞与EGCG孵育时,凝胶电泳和流式细胞术未检测到细胞凋亡。电子显微镜检查显示,EGCG-Cu2+复合物导致LNCaP细胞的细胞质膜损伤。据推测,对LNCaP前列腺癌细胞具有细胞毒性的生物活性成分不是EGCG,而是其氧化物以及与Cu2+形成的复合物。