Novel lactone compounds from Mortierella verticillata that induce the human low density lipoprotein receptor gene:: Fermentation, isolation, structural elucidation and biological activities

被引:59
作者
Dekker, KA
Aiello, RJ
Hirai, H
Inagaki, T
Sakakibara, T
Suzuki, Y
Thompson, JF
Yamauchi, Y
Kojima, N
机构
[1] Pfizer Pharmaceut Inc, Div Cent Res, Aichi 47023, Japan
[2] Pfizer Inc, Div Cent Res, Groton, CT 06340 USA
关键词
D O I
10.7164/antibiotics.51.14
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
Among methods of controlling hypercholesterolemia and hyperlipidemia is the direct stimulation of hepatic low density lipoprotein (LDL) receptors. Two novel lactone compounds, CJ-12,950 and CJ-13,357, containing an unusual oxime moiety, were isolated from a zygomycete Mortierella verticillata. These lactones are potent inducers of the LDL receptor gene in vitro, that enhanced LDL receptor expression in human hepatocytes 2-fold at 100 nM.
引用
收藏
页码:14 / 20
页数:7
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