Morré D James, Morré Dorothy M, Sun Howard, Cooper Raymond, Chang Joseph, Janle Elsa M
Departments of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN 47907, USA.
Pharmacol Toxicol. 2003 May;92(5):234-41. doi: 10.1034/j.1600-0773.2003.920506.x.
The anticancer properties of tea catechins are most frequently attributed to the principal catechin (-)-epigallocatechin-3-gallate (EGCg). Efficacy was evaluated using growth of cultured HeLa cells and inhibition of the enzymatic activity of a putative cell surface tea target enzyme, a cancer-associated cell surface-located NADH oxidase (ECTO-NOX) designated tNOX. The amounts of EGCg required to inhibit by both criteria was reduced 10 times by combination with inactive catechins such as (-)-epicatechin (EC), (-)-epigallocatechin (EGC) or (-)-epicatechin-3-gallate (ECG). Various synthetic mixtures based on purified catechins and decaffeinated tea extracts treated enzymatically to reduce the ester bond-containing catechins varying in EGCg content from 0.065 to 40% were of comparable efficacy to decaffeinated green tea extracts as long as EGCg was present and the ratio of total catechins to EGCg + EGC was about 1.5. Such mixtures appear to offer potential cancer protection and therapeutic advantages over those of EGCg alone through lowered toxicity of the mixture to normal cells and for more efficient blood delivery of orally-administered catechins to a tumour site.
茶儿茶素的抗癌特性通常归因于主要儿茶素(-)-表没食子儿茶素-3-没食子酸酯(EGCg)。使用培养的HeLa细胞的生长以及对一种假定的细胞表面茶靶酶(一种与癌症相关的位于细胞表面的NADH氧化酶,称为tNOX)的酶活性的抑制来评估疗效。通过与无活性儿茶素如(-)-表儿茶素(EC)、(-)-表没食子儿茶素(EGC)或(-)-表儿茶素-3-没食子酸酯(ECG)联合使用,两种标准下抑制所需的EGCg量减少了10倍。基于纯化儿茶素和经过酶处理以减少含酯键儿茶素的脱咖啡因茶提取物的各种合成混合物,其EGCg含量从0.065%到40%不等,只要存在EGCg且总儿茶素与EGCg + EGC的比例约为1.5,其疗效与脱咖啡因绿茶提取物相当。与单独使用EGCg相比,此类混合物似乎具有潜在的癌症预防和治疗优势,因为混合物对正常细胞的毒性较低,并且口服儿茶素向肿瘤部位的血液输送更有效。