Synthesis and lipid-lowering activities of preussin derivatives. (PubMed, Bioorg Med Chem)
All analogues at 5 μg/mL statistically reduced cholesterol absorption comparable to 40 μg/mL of a positive drug, ezetimibe, without cytotoxic effect to the Caco-2 cells...Remarkably, preussin B significantly modulated hepatic lipid metabolism genes by down-regulating HMGR and up-regulating PPARα, rendering preussin B a new and promising candidate for hypolipidemic and hepatic lipid-lowering agent. Nevertheless, the parent compound, preussin, exhibited the most potent antioxidative effect by markedly scavenging intracellular reactive oxygen species in H2O2-induced oxidative stress condition in both Caco-2 and HepG2 cell lines.