7-Difluoromethyl-5,4'-dimethoxygenistein inhibits oxidative stress induced adhesion between endothelial cells and monocytes via NF-kappaB.
7-Difluoromethyl-5,4'-dimethoxygenistein (dFMGEN), prepared by the difluoromethylation and alkylation of genistein, is an active new chemical entity. The effects of dFMGEN on cell adhesion and inflammation were investigated in human umbilical vein endothelial cells, and whether its role involved regulation of NF-kappaB expression was also studied. Results demonstrated that pretreatment with dFMGEN decreased the adhesion between vascular endothelial cells and monocytes, reduced the release of E-Selectin, ICAM-1, IL-6 and TNF-alpha in vascular endothelial cells, and down-regulated the expression of NF-kappaB. Therefore, data suggested that dFMGEN can effectually inhibit the adhesion between vascular endothelial cells and monocytes induced by oxidative stress and inflammatory reaction, and its role is connected with the downregulation of NF-kappaB.
Wang
Li
L
College of Medicine, University of South China, Hengyang, Hunan, China.
Zheng
Xing
X
Xiang
Hong-lin
HL
Fu
Xiao-hua
XH
Cao
Jian-guo
JG
D002448:Cell Adhesion / Q000187:drug effects*; D002460:Cell Line; D015536:Down-Regulation / Q000187:drug effects; D019040:E-Selectin / Q000187:drug effects / Q000378:metabolism; D042783:Endothelial Cells / Q000187:drug effects* / Q000378:metabolism; D019833:Genistein / Q000031:analogs & derivatives* / Q000494:pharmacology; D006801:Humans; D018799:Intercellular Adhesion Molecule-1 / Q000187:drug effects / Q000378:metabolism; D015850:Interleukin-6 / Q000378:metabolism; D009000:Monocytes / Q000187:drug effects / Q000378:metabolism; D016328:NF-kappa B / Q000235:genetics / Q000378:metabolism*; D018384:Oxidative Stress / Q000187:drug effects*; D014409:Tumor Necrosis Factor-alpha / Q000187:drug effects / Q000378:metabolism; D014470:Umbilical Cord / Q000166:cytology
C541079:7-difluoromethyl-5,4'-dimethoxygenistein; D019040:E-Selectin; D015850:Interleukin-6; D016328:NF-kappa B; D014409:Tumor Necrosis Factor-alpha; D018799:Intercellular Adhesion Molecule-1; D019833:Genistein