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

PYRIPYROPENES, NOVEL ACAT INHIBITORS PRODUCED BY ASPERGILLUS-FUMIGATUS .3. STRUCTURE ELUCIDATION OF PYRIPYROPENES E TO L
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DOI:
10.7164/antibiotics.48.495
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发表时间:
1995-06-01
影响因子:
3.3
通讯作者:
KANEKO, T
KANEKO, T
中科院分区:
医学4区
文献类型:
--
作者:
TOMODA, H;TABATA, N;KANEKO, T

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从烟曲霉(Aspergillus fumigatus) FO-1289-2501高产菌株培养液中分离到8个新的pyripypypenes,从E到L。结构分析表明,所有的pyripyropenes与pyripyropenes A ~ d具有相同的pyridino- α - pyroone倍半萜核心,其中pyripyropenes L对大鼠肝微粒体中酰基辅酶A:胆固醇酰基转移酶(ACAT)活性的抑制作用最强,IC50值为0.27 μ M。
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.