Zhou Langhua, Lu Sen, Gao Xiong, Chen Zhongzheng, Zhang Yuanyuan, Zhong Weixia, Zhu Fuming, Li Bin, Lin Xiaorong
College of Food Science, Scientific Research Base of Tea Comprehensive Utilization Technology Integration of Ministry of Agriculture and Rural Affairs, South China Agricultural University, Guangzhou 510642, China.
Institute of Food Microstructure, College of Food and Bioengineering, Fujian Polytechnic Normal University, Fuqing 350300, China.
Molecules. 2025 Apr 25;30(9):1919. doi: 10.3390/molecules30091919.
Chang (), a unique low-caffeine tea species, is valued for its bioactive properties, especially antioxidant and anticancer activities, due to its distinct phytochemical profile. However, its precise constituents and mechanisms remain poorly understood. This study employs an integrated approach combining chromatographic separation, bioinformatic analysis, and cellular assays to systematically investigate the antioxidant and anticancer properties of and elucidate its underlying molecular mechanisms. Quantitative analysis revealed that in addition to -catechins, the unique polyphenolic compounds, gallocatechin-3,5-di-O-gallate (GC-3,5-diGA) and 1,2,4,6-tetra-O-galloyl-β-D-glucopyranose (1,2,4,6-GA-glc), constituted significant proportions of extracts, with concentrations of 10.25 ± 0.29% and 6.60 ± 0.14%, respectively. Monomeric activity assessment demonstrated that both GC-3,5-diGA and 1,2,4,6-GA-glc exhibited pronounced antiproliferative effects against three cancer cell lines including the Lymph Node Carcinoma of the Prostate cell, human colon cancer cell, and human breast cancer cell. Notably, these compounds demonstrated potent antioxidant capacity, with 62.5 μM of GC-3,5-diGA and 15.63 μM of 1,2,4,6-GA-glc protecting against tBHP-induced oxidative stress in NIH3T3 cells comparable to 125 μM of epigallocatechin gallate and gallocatechin gallate in half-maximal inhibitory concentration. Mechanistic studies revealed that these polyphenols modulated antioxidant defenses and reactive oxygen species homeostasis via targets like fibroblast growth factor 2, telomerase reverse transcriptase, matrix metalloproteinase 9, and ATP-binding cassette subfamily G member 2, inducing oxidative stress and mitochondrial apoptosis to inhibit carcinogenesis. These findings enhance our understanding of the bioactive components responsible for the anticancer and antioxidant properties of and provide a scientific basis for the development of this dual-purpose plant for food and medicinal applications.
漳平水仙茶（Chang）是一种独特的低咖啡因茶品种，因其独特的植物化学特征，具有生物活性特性，尤其是抗氧化和抗癌活性，而备受重视。然而，其确切成分和作用机制仍知之甚少。本研究采用色谱分离、生物信息学分析和细胞实验相结合的综合方法，系统地研究了漳平水仙茶的抗氧化和抗癌特性，并阐明其潜在的分子机制。定量分析表明，除了儿茶素外，独特的多酚化合物，没食子儿茶素-3,5-二-O-没食子酸酯（GC-3,5-diGA）和1,2,4,6-四-O-没食子酰基-β-D-吡喃葡萄糖（1,2,4,6-GA-glc），在漳平水仙茶提取物中占相当大的比例，浓度分别为10.25±0.29%和6.60±0.14%。单体活性评估表明，GC-3,5-diGA和1,2,4,6-GA-glc对三种癌细胞系，包括前列腺淋巴结癌细胞、人结肠癌细胞和人乳腺癌细胞，均表现出显著的抗增殖作用。值得注意的是，这些化合物表现出强大的抗氧化能力，62.5μM的GC-3,5-diGA和15.63μM的1,2,4,6-GA-glc在NIH3T3细胞中对叔丁基过氧化氢（tBHP）诱导的氧化应激的保护作用，在半数抑制浓度下与125μM的表没食子儿茶素没食子酸酯和没食子儿茶素没食子酸酯相当。机制研究表明，这些多酚通过成纤维细胞生长因子2、端粒酶逆转录酶、基质金属蛋白酶9和ATP结合盒亚家族G成员2等靶点调节抗氧化防御和活性氧稳态，诱导氧化应激和线粒体凋亡以抑制致癌作用。这些发现加深了我们对漳平水仙茶抗癌和抗氧化特性的生物活性成分的理解，并为开发这种兼具食品和药用双重用途的植物提供了科学依据。
