Ferroverdins, inhibitors of cholesteryl ester transfer protein produced by Streptomyces sp. WK-5344. I. Production, isolation and biological properties.
Streptomyces sp. WK-5344, a soil isolate, was found to produce structurally related inhibitors of cholesteryl ester transfer protein (CETP). New active compounds, designated ferroverdins B and C, were isolated along with known ferroverdin A from the fermentation broth by solvent extraction, ODS column chromatography and silica gel column chromatography. All ferroverdins showed a dose-dependent inhibitory activity against human CETP. The IC50 values were 21, 0.62 and 2.2 microM for ferroverdins A, B and C, respectively, indicating that ferroverdin B is one of the most potent CETP inhibitors of microbial origin.
Tomoda
H
H
Research Center for Biological Function, The Kitasato Institute and Graduate School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
Tabata
N
N
Shinose
M
M
Takahashi
Y
Y
Woodruff
H B
HB
Omura
S
S
D001419:Bacteria / Q000187:drug effects; D002352:Carrier Proteins / Q000037:antagonists & inhibitors*; D053480:Cholesterol Ester Transfer Proteins; D004305:Dose-Response Relationship, Drug; D005285:Fermentation; D005296:Ferrous Compounds / Q000302:isolation & purification* / Q000494:pharmacology; D006023:Glycoproteins; D006801:Humans; D009603:Nitroso Compounds / Q000302:isolation & purification* / Q000494:pharmacology; D013302:Streptomyces / Q000145:classification / Q000378:metabolism*
C506642:CETP protein, human; D002352:Carrier Proteins; D053480:Cholesterol Ester Transfer Proteins; D005296:Ferrous Compounds; D006023:Glycoproteins; D009603:Nitroso Compounds; C405055:ferroverdin B; C405056:ferroverdin C; C033515:ferroverdin