Erabulenols, inhibitors of cholesteryl ester transfer protein produced by Penicillium sp. FO-5637. I.Production, isolation and biological properties.
Penicillium sp. FO-5637, a soil isolate, was found to produce a series of inhibitors of cholesteryl ester transfer protein (CETP). Novel active compounds, designated erabulenols A and B, were isolated from the fermentation broth of the producing strain by solvent extraction, ODS column chromatography and HPLC. Erabulenols A and B inhibit human CETP activity with IC50 values of 47.7 and 58.2 microM in an in vitro assay system containing 200 microM BSA, respectively.
Tomoda
H
H
Research Center for Biological Function, The Kitasato Institute and Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
Tabata
N
N
Masuma
R
R
Si
S Y
SY
Omura
S
S
D000900:Anti-Bacterial Agents / Q000096:biosynthesis / Q000302:isolation & purification / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D002352:Carrier Proteins / Q000037:antagonists & inhibitors*; D053480:Cholesterol Ester Transfer Proteins; D002788:Cholesterol Esters / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D004224:Diterpenes / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology; D005658:Fungi / Q000187:drug effects; D005663:Furans / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology; D006023:Glycoproteins; D006801:Humans; D010407:Penicillium / Q000737:chemistry* / Q000145:classification / Q000254:growth & development / Q000378:metabolism; D014280:Triglycerides / Q000378:metabolism*; D014315:Triterpenes / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology
D000900:Anti-Bacterial Agents; C506642:CETP protein, human; D002352:Carrier Proteins; D053480:Cholesterol Ester Transfer Proteins; D002788:Cholesterol Esters; D004224:Diterpenes; D005663:Furans; D006023:Glycoproteins; D014280:Triglycerides; D014315:Triterpenes; C114131:erabulenol B; C114130:erabulenol A