Synthesis of genistein derivatives and determination of their protective effects against vascular endothelial cell damages caused by hydrogen peroxide
Synthesis of genistein derivatives and determination of their protective effects against vascular endothelial cell damages caused by hydrogen peroxide
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DOI：
10.1016/j.bmcl.2007.11.097
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发表时间：
2008-01-15
影响因子：
2.7
通讯作者：
Cao, Jian-Guo
中科院分区：
文献类型：
--
作者：
Fu, Xiao-Hua;Wang, Li;Cao, Jian-Guo
通过烷基化和二氟甲基化法制备了一系列染料木素衍生物，在体外研究了它们对过氧化氢诱导的人脐静脉内皮细胞损伤的抑制作用。用载体溶剂（DMSO）、染料木素或不同量的染料木素衍生物预处理HUVE-12细胞30分钟，然后暴露于1mm过氧化氢中24小时。用碘化丙啶（PI）染色的流式细胞术检测细胞凋亡。通过乳酸脱氢酶（LDH）的释放来评估细胞损伤。结果表明，染料木素衍生物对过氧化氢诱导的HUVE-12细胞凋亡和降低LDH释放具有保护作用。在这些衍生物中，7-二氟甲基-5,4'-二甲氧基染料木素对过氧化氢诱导的HUVE-12细胞凋亡表现出最强的活性。(c) 2007 Elsevier Ltd.版权所有。
A series of genistein derivatives, prepared by alkylation and difluoromethylation, were tested for their inhibitory effects on the hydrogen peroxide induced impairment in human umbilical vein endothelial (HUVE-12) cells in vitro. The HUVE-12 cells were pretreated with either the vehicle solvent (DMSO), genistein, or different amounts of the genistein derivatives for 30 min before exposed to 1 mM hydrogen peroxide for 24 h. Cell apoptosis was determined by flow cytometry with propidium iodide (PI) staining. Cellular injury was estimated by measuring the lactate dehydrogenase (LDH) release. Data suggested that the genistein derivatives possessed a protective effect on HUVE-12 cells from hydrogen peroxide induced apoptosis and reduced LDH release. Among these derivatives, 7-difluoromethyl-5,4'-dimethoxygenistein exhibited the strongest activity against hydrogen peroxide induced apoptosis of HUVE-12 cells. (c) 2007 Elsevier Ltd. All rights reserved.