目的:研究瑶族药用植物中黄酮化合物的体外抗肿瘤活性,并初步分析它们的构效关系。方法:采用四甲基偶氮唑盐(MTT)吸收减少实验,测定6个黄酮化合物对2种正常细胞的毒性和对7种肿瘤细胞的增殖抑制作用。结果:6种化合物中,圣草苷、柚皮苷、槲皮素和槲皮苷对2种正常细胞非洲绿猴肾细胞Vero和人黑色素细胞MC基本不显示出毒性,柚皮素对这2种细胞的毒性都较大,而圣草酚对Vero细胞毒性很小,对MC细胞的毒性非常大。柚皮素有较广谱的抗肿瘤活性,它对7个受试肿瘤细胞都显示出较强的增殖抑制,尤其对乳腺癌细胞MCF-7的半数抑制浓度达到了50μg/ml。在7种肿瘤细胞中,MCF-7和肝癌细胞HepG2对受试黄酮化合物最为敏感,两者都被圣草酚、柚皮素和槲皮素以较低浓度有效地抑制。这些化合物对肿瘤细胞的抑制作用都显示出浓度依赖性。结论:圣草酚、柚皮素和槲皮素对肿瘤细胞的生长有较好的抑制作用.而官们的葡萄糖苷的细胞毒性较小.
Objective: To detect the cytotoxicity and in vitro antiproliferative effects of the flavones compounds isolated from some Yao herbal medicines, and analyze the basic structure-activity relationship. Methods: The cytotoxieity on normal cells and antiproliferative effect on tumor cells were tested by MTF reduction assay respectively. Results: Among the 6 flavones, the Eriodietyol-7-O-a-D- glueoside, Naringenin-7-O-β-D-glucoside, quercetin and quercetin-3-O-β-D-glueoside showed very low cytotoxicity to the two normal cells, Vero and MC cells, while the naringenin was high toxic to both of them. The eriodictyol was no toxic to Vero Cell but could affect MC cell at low concentration. The naringenin exhibited a wide-spectrum antiproliferative effect on all of the 7 tested cancer cell lines especially on the MCF-7 with low IC50 about 50 μg/ml. Among these cancer cells, the MCF-7 and HepG2 were more sensitive to the flavones compounds than the others. Both of them were inhibited by eriodietyol, quercetin and naringenin even at low test concentration. Furthermore, the antiproliferative effects of these compounds were concentration-related. Conclusion: Some of flavones compounds isolated from some Yao herb medicines showed high antiproliferative effect on cancer cells with low eytotoxieity on normal cells.