Inhibition of Lipid Droplet Accumulation in Mouse Macrophages by Stemphone Derivatives

Abstract

From a study on the biological activity of fungal stemphones and their derivatives, five derivatives having an O-alkyl moiety at C-11 of stemphone C were found to inhibit lipid droplet accumulation in macrophages without any cytotoxic effect. Among the derivatives, those having O-isopropyl and O-isobutyl were the most potent inhibitors by blocking the synthesis of both cholesteryl ester (CE) and triacylglycerol (TG), the main constituents of lipid droplets in macrophages.

Relative and Absolute Stereochemistry of Quinadoline B, an Inhibitor of Lipid Droplet Synthesis in Macrophages

“…No cytotoxic effects on macrophages were observed even at 300 μΜ. An assay for the synthesis of cholesteryl ester (CE) and triacylglycerol (TG), the main constituents of lipid droplets in macrophages, was then carried out by the method described previously . Compound 1 inhibited CE synthesis with an IC 50 value of 93 μM but had almost no effect on TG synthesis even at the highest dose (192 μM).…”

New Chlorinated Metabolites and Antiproliferative Polyketone from the Mangrove Sediments-Derived Fungus Mollisia sp. SCSIO41409

“…Stemphone C ( 4 ) had been reported from an Aspergillus strain as a potentiator of imipenem activity against methicillin-resistant Staphylococcus aureus , with other stemphone derivatives [ 21 , 29 ]. Stemphone was found to inhibit over contraction of portal vein, induced by high glucose levels [ 30 ], and its derivatives were also revealed to inhibit lipid droplet accumulation in macrophages [ 31 ]. In our study, stemphone C ( 4 ) exhibited obvious antimicrobial activity against the bacteria Erysipelothrix rhusiopathiae WH13013, with the MIC value of 1.56 μg/mL.…”