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目的:探讨中药臭灵丹中黄酮类化合物的体外抗肿瘤活性。方法:采用MTT法,检测分离自臭灵丹的6个黄酮类化合物对2种正常细胞的毒性和对2种肿瘤细胞的增殖抑制作用,并初步分析它们的构效关系;运用流式细胞仪,检测活性化合物对细胞凋亡率及细胞周期的影响。结果:6个黄酮化合物中,5,7,3,′4′-四甲氧基-3-羟基黄酮与金腰素乙显著抑制A549和HeLa 2种肿瘤细胞的增殖并呈浓度依赖性关系,且对正常细胞Vero和EVC304的毒性较小;这2个黄酮结构中均有邻位酚甲氧基。流式结果显示金腰素乙对HeLa细胞的G2/M期起阻滞作用并呈浓度依赖性关系。5,7,3,′4′-四甲氧基-3-羟基黄酮与金腰素乙对A549和HeLa细胞都有促凋亡作用并呈明显的量效关系。结论:5,7,3,′4′-四甲氧基-3-羟基黄酮与金腰素乙对肿瘤细胞的生长有显著的抑制增殖作用且细胞毒性小,并通过调节细胞周期及诱导凋亡发挥抗肿瘤作用。
Objective: To investigate the antitumor activity of Flavonoids in traditional Chinese medicine Silander. Methods: MTT assay was used to detect the cytotoxicity of 6 flavonoids isolated from stinky ganoderma on 2 kinds of normal cells and their effects on the proliferation of 2 kinds of tumor cells. The structure-activity relationship of them was analyzed preliminarily. Flow cytometry , The effect of the active compound on apoptosis rate and cell cycle was tested. Results: Among 6 flavonoids, 5,7,3 ’, 4’-tetramethoxy-3-hydroxyflavone and gold-rosiglitazone significantly inhibited the proliferation of A549 and HeLa tumor cells in a concentration-dependent manner, And less toxic to normal cells Vero and EVC304; ortho-phenolic methoxy is present in both flavonoids. The flow cytometry results showed that LBPB blocked G2 / M phase of HeLa cells in a concentration-dependent manner. 5,7,3, 4’-tetramethoxy-3-hydroxyflavone and gold waist hormone B on A549 and HeLa cells have a pro-apoptotic effect and showed a significant dose-effect relationship. CONCLUSION: 5, 7, 3 ’, 4’-Tetramethoxy-3-hydroxyflavone and gold waist progesterone significantly inhibit the proliferation of tumor cells and have less cytotoxicity. By regulating cell cycle and inducing apoptosis Death play anti-tumor effect.