Roselipins, inhibitors of diacylglycerol acyltransferase, produced by Gliocladium roseum KF-1040.
Gliocladium roseum KF-1040, a marine isolate, was found to produce a series of new inhibitors of diacylglycerol acyltransferase (DGAT). Four active compounds, designated roselipins 1A, 1B, 2A and 2B, were isolated from the fermentation broth of the producing strain by solvent extraction, ODS column chromatography and preparative HPLC. The highest production of roselipins was observed when cultured in the medium containing natural sea water. Roselipins inhibit DGAT activity with IC50 values of 15 approximately 22 microM in an enzyme assay system using rat liver microsomes.
Tomoda
H
H
Research Center for Biological Function, The Kitasato Institute and Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
Ohyama
Y
Y
Abe
T
T
Tabata
N
N
Namikoshi
M
M
Yamaguchi
Y
Y
Masuma
R
R
Omura
S
S
D000217:Acyltransferases / Q000037:antagonists & inhibitors*; D000818:Animals; D051048:Diacylglycerol O-Acyltransferase; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000302:isolation & purification* / Q000378:metabolism / Q000494:pharmacology*; D005227:Fatty Acids / Q000302:isolation & purification* / Q000378:metabolism / Q000494:pharmacology*; D005285:Fermentation; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D008855:Microscopy, Electron, Scanning; D003904:Mitosporic Fungi / Q000145:classification / Q000378:metabolism* / Q000648:ultrastructure; D009005:Monosaccharides / Q000302:isolation & purification* / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats
D004791:Enzyme Inhibitors; D005227:Fatty Acids; D009005:Monosaccharides; C401212:roselipin 1A; C401213:roselipin 2A; D000217:Acyltransferases; D051048:Diacylglycerol O-Acyltransferase