Discovery of halogenated eurypamide B analogues as inhibitors of lipid droplet accumulation in macrophages.
Halogenated cyclic isodityrosine-tripeptides were synthesized as analogues of a marine natural product, eurypamide B. Although the original eurypamides showed no inhibitory activity, the new analogues were found to inhibit lipid droplet accumulation in macrophages with a low micromolar IC50 value.
Obata
Rika
R
Department of Chemistry, Faculty of Science and Technology, Keio University, Hiyoshi 3-14-1, Kohoku-ku, Yokohama 223-8522, Japan.
Ohshiro
Taichi
T
Tomoda
Hiroshi
H
Nishiyama
Shigeru
S
D000818:Animals; D001688:Biological Products / Q000494:pharmacology*; D006219:Halogens; D020128:Inhibitory Concentration 50; D050356:Lipid Metabolism; D008055:Lipids / Q000037:antagonists & inhibitors*; D017737:Macrophages, Peritoneal / Q000187:drug effects / Q000378:metabolism*; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D001688:Biological Products; D006219:Halogens; D008055:Lipids; D009842:Oligopeptides; D010456:Peptides, Cyclic