Cytotoxicity of flavonoids toward cultured normal human cells
Cytotoxicity of flavonoids toward cultured normal human cells
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DOI：
10.1248/bpb.28.253
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发表时间：
2005-02-01
影响因子：
2
通讯作者：
Kaneko, T
中科院分区：
文献类型：
--
作者：
Matsuo, M;Sasaki, N;Kaneko, T
类黄酮，包括芹菜素、圣草酚、3-羟基黄酮、山奈酚、木犀草素、柚皮素、槲皮素、芦丁和花旗松素，对培养的人正常细胞，即，人肺胚胎成纤维细胞（TIG-1）和人脐静脉内皮（HUVE）细胞。当这些正常的人类细胞与每种黄酮类化合物在培养基中孵育24小时时，一些黄酮类化合物在相对高的浓度下以剂量依赖的方式显示出相当大的细胞毒性。3-羟基黄酮、毛地黄黄酮和芹菜素对TIG-1细胞的毒性高于其他黄酮类化合物，毛地黄黄酮、3-羟基黄酮和槲皮素对HUVE细胞的毒性高于其他黄酮类化合物。HUVE细胞比TIG-1细胞更容易受到Havlastin细胞毒性的影响。用2 ′，7 ′-二氯荧光素二乙酸酯（DCF-DA）检测类黄酮处理的TIG-1细胞内活性氧（ROS）水平。活性氧水平显着增加的黄酮芹菜素或毛地黄黄酮或黄酮醇3-羟基黄酮，槲皮素，或山奈酚的存在下。这些结果表明，这些黄酮和黄酮醇通过增加细胞内ROS水平发挥细胞毒性。此外，检查了在24小时孵育期间更具毒性的芹菜素、3-羟基黄酮、毛地黄黄酮和槲皮素掺入到TIG-1细胞中。这些黄酮类化合物被掺入其中，其掺入效率的顺序与其细胞毒性的顺序相似。总之，一些Havavalanine在较高浓度下对人正常细胞具有细胞毒性。此外，有人建议，他们被纳入细胞，增加细胞内的ROS水平，然后发挥细胞毒性。
The cytotoxicity of flavonoids, including apigenin, eriodictyol, 3-hydroxyflavone, kaempherol, luteolin, naringenin, quercetin, rutin, and taxifolin, toward cultured human normal cells, i.e., human lung embryonic fibroblasts (TIG-1) and human umbilical vein endothelial (HUVE) cells, was examined. When these normal human cells were incubated with each flavonoid in culture medium for 24 h, some of the flavonoids showed considerable cytotoxicity at relatively high concentrations and in a dose-dependent manner. 3-Hydroxyflavone, luteolin, and apigenin were more toxic toward TIG-1 cells than the other flavonoids, and luteolin, 3-hydroxyflavone, and quercetin were more toxic toward HUVE cells. HUVE cells were more vulnerable to Havonoid cytotoxicity than TIG-1 cells. Using 2',7'-dichlorofluorescin diacetate (DCF-DA), the intracellular reactive oxygen species (ROS) level of flavonoid-treated TIG-1 cells was examined. The ROS level increased significantly in the presence of the flavone apigenin or luteolin or the flavonol 3-hydroxyflavone, quercetin, or kaempherol. These results suggest that these flavones and flavonols exert cytotoxicity through increasing intracellular ROS levels. Further, the incorporation of apigenin, 3-hydroxyflavone, luteolin, and quercetin, which are more toxic, into TIG-1 cells during 24-h incubation was examined. These flavonoids were incorporated into them and the order of their incorporation efficiency was similar to that of their cytotoxicity. In conclusion, some Havonoids are cytotoxic at higher concentrations toward human normal cells. Further, it is suggested that they are incorporated into cells, increase intracellular ROS levels, and then exert cytotoxicity.