Palau'amine and Related Oroidin Alkaloids Dibromophakellin and Dibromophakellstatin Inhibit the Human 20S Proteasome

被引：44
作者：
Lansdell, Theresa A. [1 ]
Hewlett, Nicole M. [1 ]
Skoumbourdis, Amanda P. [2 ]
Fodor, Matthew D. [2 ]
Seiple, Ian B. [3 ]
Su, Shun [3 ]
Baran, Phil S. [3 ]
Feldman, Ken S. [2 ]
Tepe, Jetze J. [1 ]
机构：
[1] Michigan State Univ, Dept Chem, E Lansing, MI 48823 USA
[2] Penn State Univ, Dept Chem, University Pk, PA 16802 USA
[3] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
来源：
JOURNAL OF NATURAL PRODUCTS | 2012年 / 75卷 / 05期
基金：
美国国家科学基金会; 美国国家卫生研究院;
关键词：
NF-KAPPA-B; NATURAL-PRODUCT DIBROMOPHAKELLSTATIN; PUMMERER REACTION CHEMISTRY; OXIDATIVE CYCLIZATION; MARINE SPONGE; IL-6;
D O I：
10.1021/np300231f
中图分类号：
Q94 [植物学];
学科分类号：
071001 ;
摘要：
We report herein that the oroidin-derived alkaloids palau'amine (1), dibromophakellin (2), and dibromophakellstatin (3) inhibit the proteolytic activity of the human 20S proteasome as well as the (i)20S immunoproteasome catalytic core. Palau'amine is found to prevent the degradation of ubiquitinylated proteins, including I kappa B alpha, in cell culture, which may be indicative of the potential mechanism by which these agents exhibit their exciting cytotoxic and immunosuppressive properties.
引用
收藏
页码：980 / 985
页数：6
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