Structurally related cytotoxic effects of flavonoids on human cancer cells in vitro
Structurally related cytotoxic effects of flavonoids on human cancer cells in vitro
复制标题
黄酮类化合物对体外人类癌细胞的结构相关细胞毒作用
DOI：
10.1007/s12272-001-1280-8
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发表时间：
2008-09-01
影响因子：
6.7
通讯作者：
Yuan, Jialin
中科院分区：
文献类型：
--
作者：
Chang, Hui;Mi, Mantian;Yuan, Jialin
黄酮类化合物广泛存在于人类饮食中，对健康有多种影响。研究了23类黄酮对乳腺癌细胞（MDA-MB-231和MCF-7）、结直肠癌细胞（LoVo和DLD-1）和前列腺癌细胞（PC3）的细胞毒作用。通过比较只有一个结构元素不同的选定分子的细胞毒性（EC(50)），我们确定了与增强的细胞毒性相关的几种结构特性，包括2,3-双键的存在、适当的羟基数、3-OH、6-OH和b环上的邻羟基化。结果表明，3,6-二羟基黄酮对肿瘤细胞的杀伤作用最强。在3,6-二羟黄酮作用下，肿瘤细胞DAPI染色观察到凋亡细胞的出现，流式细胞术细胞凋亡分析也显示3,6-二羟黄酮诱导肿瘤细胞凋亡。这些结果揭示了黄酮类化合物对人类癌细胞的结构相关毒性，表明3,6-二羟基黄酮是一种值得开发的肿瘤化疗活性化合物。
Flavonoids exist extensively in the human diet, and a variety of health effects have been ascribed to them. The cytotoxic effects of 23 flavonoids on breast cancer cells (MDA-MB-231 and MCF-7), colorectal carcinoma cells (LoVo and DLD-1) and prostatic cancer cells (PC3) were investigated. By comparing the cytotoxicity (EC(50)) of selected molecules that differ in only one structure element, we identified several structural properties associated with enhanced cytotoxicity, including the presence of the 2,3-double bond, appropriate hydroxyl numbers, 3-OH, 6-OH and ortho-hydroxylation in ring B. Flavonoids with a 5-OH exhibited lower cytotoxicity than their non-hydroxylated counterparts. Results indicated that 3,6-dihydroxylflavone showed the most potent cytotoxic effect on these cancer cells. The appearance of apoptotic cells with DAPI staining was observed in cancer cells under 3,6-dihydroxylflavone treatment, and the apoptosis analysis by flow cytometry also showed that 3,6-dihydroxylflavone induced apoptotic cell death in these cancer cells. These results revealed the structurally related toxicity of flavonoids on human cancer cells, and indicates that 3,6-dihydroxylflavone is an active compound worthy of development for cancer chemotherapy.