Pyripyropenes, Novel ACAT inhibitors produced by Aspergillus fumigatus. III. Structure elucidation of pyripyropenes E to L.
Eight new pyripyropenes, E to L, were isolated from the culture broth of Aspergillus fumigatus FO-1289-2501 selected as a higher producer by NTG mutation. Structural elucidation indicated that all the pyripyropenes have the same pyridino-alpha-pyrone sesquiterpene core as pyripyropenes A to D. Among them, pyripyropene L showed the most potent inhibition against acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 value of 0.27 microM in rat liver microsomes.
Tomoda
H
H
Research Center for Biological Function, Kitasato Institute, Tokyo, Japan.
Tabata
N
N
Yang
D J
DJ
Takayanagi
H
H
Nishida
H
H
Omura
S
S
Kaneko
T
T
D000818:Animals; D001232:Aspergillus fumigatus; D018360:Crystallography, X-Ray; D005285:Fermentation; D008826:Microbial Sensitivity Tests; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D015394:Molecular Structure; D011725:Pyridines / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D051381:Rats; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D011725:Pyridines; D012717:Sesquiterpenes; D002785:Sterol O-Acyltransferase