Palau鈥檃mine and Related Oroidin Alkaloids Dibromophakellin and Dibromophakellstatin Inhibit the Human 20S Proteasome

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• 作者：Theresa A. Lansdell ; Nicole M. Hewlett ; Amanda P. Skoumbourdis ; Matthew D. Fodor ; Ian B. Seiple ; Shun Su ; Phil. S. Baran ; Ken S. Feldman ; Jetze J. Tepe
• 刊名：Journal of Natural Products
• 出版年：2012
• 出版时间：May 25, 2012
• 年：2012
• 卷：75
• 期：5
• 页码：980-985
• 全文大小：311K
• 年卷期：v.75,no.5(May 25, 2012)
• ISSN：1520-6025

文摘

We report herein that the oroidin-derived alkaloids palau鈥檃mine (1), dibromophakellin (2), and dibromophakellstatin (3) inhibit the proteolytic activity of the human 20S proteasome as well as the ⁱ20S immunoproteasome catalytic core. Palau鈥檃mine is found to prevent the degradation of ubiquitinylated proteins, including I魏B伪, in cell culture, which may be indicative of the potential mechanism by which these agents exhibit their exciting cytotoxic and immunosuppressive properties.