
Description | Diethylmaleate is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NF-kB. | |
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Targets |
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In vitro | DEM induces upregulation of GSH(L-c-glutamyl-L-cysteinyl-glycine) metabolism, and the downregulation of pathways of cancer, chemokine signaling, cytokine-cytokine receptor, and focal adhesion in transformed cells. DEM appears to modify microenvironment of transformed cells thereby restraining tumor cell growth. DEM is cytotoxic to the transformed cells in a concentration dependent manner. DEM at 0.25 mM decreases cell viability to 75%. The co-exposure of cells to DEM+GSHe inhibits DEM induced cytotoxicity. DEM exposure increases the ROS generation by multiple orders of magnitude in transformed cells. This is evident from the dose and time dependent increase in fluorescence intensity of CMH2DCFDA. Moreover, DEM activates MAPK pathway and DEM induced activation of ERK is found to be due to phosphorylation at Thr 202/204[1]. | |
In vivo | Sperm motility and epididymal sperm count are significantly reduced in the DEM treated animals. Fertility status is also affected by DEM exposure as is evident from the percent fertility and the litter size. consequences of the oxidative stress produced by the DEM induces glutathione depletion, on the reproductive ability of male mice and modulation of the various components of the antioxidant defense system at the transcriptional level[4]. |
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