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山奈酚对活性氧诱导的溶血的保护作用及其对人癌细胞的抗增殖活性。

Protective effects of kaempferol against reactive oxygen species-induced hemolysis and its antiproliferative activity on human cancer cells.

机构信息

Department of Food Science and Engineering, Jinan University, 601 West, Huangpu Road, Guangzhou, 510632, China; College of Light Industry and Food Sciences, South China University of Technology, Guangzhou, 510640, China.

College of Light Industry and Food Sciences, South China University of Technology, Guangzhou, 510640, China.

出版信息

Eur J Med Chem. 2016 May 23;114:24-32. doi: 10.1016/j.ejmech.2016.02.045. Epub 2016 Feb 27.

DOI:10.1016/j.ejmech.2016.02.045
PMID:26974372
Abstract

The protective effects of kaempferol against reactive oxygen species (ROS)-induced hemolysis and its antiproliferative activity on human cancer cells were evaluated in this study. Kaempferol exhibited strong cellular antioxidant ability (CAA) with a CAA value of 59.80 ± 0.379 μM of quercetin (QE)/100 μM (EC50 = 7.74 ± 0.049 μM). Pretreatment with kaempferol significantly attenuated the ROS-induced hemolysis of human erythrocyte (87.4% hemolysis suppressed at 100 μg/mL) and reduced the accumulation of toxic lipid peroxidation product malondialdehyde (MDA). The anti-hemolytic activity of kaempferol was mainly through scavenging excessive ROS and preserving the intrinsic antioxidant enzymes (superoxide dismutase, SOD; catalase, CAT; and glutathione peroxidase, GPx) activities in normal levels. Additionally, kaempferol showed significant antiproliferative activity on a panel of human cancer cell lines including human breast carcinoma (MCF-7) cells, human stomach carcinoma (SGC-7901) cells, human cervical carcinoma (Hela) cells and human lung carcinoma (A549) cells. Kaemperol induced apoptosis of MCF-7 cells accompanied with nuclear condensation and mitochondria dysfunction.

摘要

本研究评估了山柰酚对活性氧(ROS)诱导的溶血的保护作用及其对人癌细胞的抗增殖活性。山柰酚具有很强的细胞抗氧化能力(CAA),CAA 值为 59.80±0.379μM 槲皮素(QE)/100μM(EC50=7.74±0.049μM)。山柰酚预处理可显著减轻人红细胞的 ROS 诱导溶血(100μg/mL 时抑制 87.4%溶血),并减少毒性脂质过氧化产物丙二醛(MDA)的积累。山柰酚的抗溶血活性主要是通过清除过量的 ROS 并保持正常水平的内在抗氧化酶(超氧化物歧化酶、SOD;过氧化氢酶、CAT;和谷胱甘肽过氧化物酶、GPx)活性。此外,山柰酚对一系列人癌细胞系表现出显著的抗增殖活性,包括人乳腺癌(MCF-7)细胞、人胃癌(SGC-7901)细胞、人宫颈癌(Hela)细胞和人肺癌(A549)细胞。山奈酚诱导 MCF-7 细胞凋亡,伴有核浓缩和线粒体功能障碍。

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