PYRIPYROPENES, NOVEL ACAT INHIBITORS PRODUCED BY ASPERGILLUS-FUMIGATUS .3. STRUCTURE ELUCIDATION OF PYRIPYROPENES E TO L

被引:58
作者
TOMODA, H [1 ]
TABATA, N [1 ]
YANG, DJ [1 ]
TAKAYANAGI, H [1 ]
NISHIDA, H [1 ]
OMURA, S [1 ]
KANEKO, T [1 ]
机构
[1] PFIZER INC,DIV CENT RES,GROTON,CT 06340
关键词
D O I
10.7164/antibiotics.48.495
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
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 mu M in rat liver microsomes.
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页码:495 / 503
页数:9
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