Sorrenti, Valeria; Vanella, Luca; Platania, Chiara Bianca Maria; Greish, Khaled; Bucolo, Claudio; Pittala, Valeria; Salerno, Loredana published the artcile< Novel heme oxygenase-1 (HO-1) inducers based on dimethyl fumarate structure>, Application of C19H34O2, the main research area is unsaturated dicarbonyl compound preparation heme oxygenase docking; HO-1 inducers; LX-2 cells; dimethyl fumarate (DMF); heme oxygenase (HO); hepatic fibrosis.
Novel heme oxygenase-1 (HO-1) inducers based on di-Me fumarate (DMF) structure I [R = H, 4-Me, 2-CO2H, etc.; R1 = Me, Ph, 4-ClC6H4, etc.; X = O, NH; Y = a bond, CH2, CH2CH2, CH2CH2CH2] were reported in this paper. These compounds were obtained by modification of the DMF backbone. Particularly, maintaining the α, β-unsaturated dicarbonyl function as the central chain crucial for HO-1 induction, different substituted or unsubstituted Ph rings are introduced by means of an ester or amide linkage. Sym. and asym. derivatives were synthesized. All compounds were tested on a human hepatic stellate cell line LX-2 to assay their capacity for modifying HO-1 expression. Compounds I [R = H, R1 = Ph, X = O, Y = null; R = 4-Cl, R1 = 4-ClC6H4, X = O, Y = null; R = H, R1 = Ph, X = NH, Y = CH2] stand out for their potency as HO-1 inducers, being 2-3 fold more active than DMF, and for their ability to reverse reactive oxygen species (ROS) production mediated using palmitic acid (PA). These properties, coupled with a low toxicity toward LX-2 cell lines, made these compounds potentially useful for treatment of diseases in which HO-1 overexpression may counteract inflammation, such as hepatic fibrosis. Docking studies showed a correlation between predicted binding free energy and exptl. HO-1 expression data. These preliminary results might support the development of new approaches in the management of liver fibrosis.
International Journal of Molecular Sciences published new progress about Anilines Role: RCT (Reactant), RACT (Reactant or Reagent). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application of C19H34O2.
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