Lipid reducing activity and toxicity profiles of a library of polyphenol derivatives

摘要: Abstract Obesity is an increasing epidemic worldwide and novel treatments are urgently needed. Polyphenols natural compounds derived from plants, which known in particular for their antioxidant properties. However, some polyphenols were described to possess anti-obesity activities in vitro in vivo. In this study, we aimed screen a library of 85 polyphenol derivatives lipid reducing activity toxicity. Compounds analyzed at 5 μM with the zebrafish Nile red fluorescence fat metabolism assay general toxicity To improve safety profile, screened 50 μM murine preadipocytes cytotoxicity. Obtained data used create 2D-QSAR (quantitative structure relationship) model. 38 showed strong activity. Toxicity analysis revealed that 18 them did not show any or QSAR importance number rings, fractional partial positively charged surface area, relative positive charge, oxygen atoms, negative area lipid-reducing The five most potent EC50 values nanomolar range without toxic effects candidates future research development into drugs. Molecular profiling fasn, sirt1, mtp ppary one compound reduced significantly fasn mRNA expression.