黄酮类化合物抑制肿瘤细胞增殖活性及构效关系

Antiproliferation and SARs of Flavonoids on Human Cancers

通过MTT法分析比较了12种黄酮类化合物对乳腺癌细胞(MCF-7L,MDA-MB-231)、肝癌细胞(SMCC-7721)、结肠癌细胞(HCT-15)增殖抑制和细胞形态变化。根据12种化合物对癌细胞增殖抑制作用及其构效关系发现化合物FB4的A环6位羟基化能显著提高黄酮苷元化合物对癌细胞的增殖抑制作用。这些结果为改造黄酮化合物的结构,从而增强其抑制癌细胞增殖活性提供了重要依据。

The authors evaluate 12 flavonoids（including flavonoid aglycones and their glycosides） on cell proliferation by MTT assay,cell lines include breast cancer MCF-7L,MDA-MB-231,liver cancer SMCC-7721,colon cancer HCT-15.Meaning while,the cellular morphology changes are observed by optical microscopy.The authors compare the structure and activity relationships（SARs） based on the different activities of 12 flavonoids,6-hydroxylation on ring A significantly increases the inhibitory activity,the results provide a clue for us to modulate the structure of flavonoids and to inhibit the proliferation of cancer cells more efficiently.