Embellicines A and B: Absolute Configuration and NF-魏B Transcriptional Inhibitory Activity
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- 作者：Weaam Ebrahim ; Amal H. Aly ; Victor Wray ; Attila M谩ndi ; Marie-H茅l猫ne Teiten ; Fran莽ois Gaascht ; Barbora Orlikova ; Matthias U. Kassack ; WenHan Lin ; Marc Diederich ; Tibor Kurt谩n ; Abdessamad Debbab ; Peter Proksch
- 刊名：Journal of Medicinal Chemistry
- 出版年：2013
- 出版时间：April 11, 2013
- 年：2013
- 卷：56
- 期：7
- 页码：2991-2999
- 全文大小：488K
- 年卷期：v.56,no.7(April 11, 2013)
- ISSN：1520-4804
文摘
Two new metabolites, embellicines A and B (1 and 2), were isolated from the EtOAc extract of the fungus Embellisia eureka, an endophyte of the Moroccan plant Cladanthus arabicus (Asteraceae). The structures of these new compounds were determined on the basis of extensive one- and two-dimensional NMR spectroscopy as well as by high-resolution mass spectrometry. The absolute configuration of embellicine A (1) was determined by TDDFT ECD calculations of solution conformers, whereas that of embellicine B (2) was deduced based on ROESY correlations and on biogenetic considerations in comparison to 1. Both embellicines (1 and 2) are cytostatic, cytotoxic, and inhibit NF-魏B transcriptional activity, indicating that inhibition of NF-魏B may be a possible mechanism of action of these compounds. Embellicine B (2) was the most active compound encountered in this study and acts at nanomolar concentrations without affecting tumor microenvironment.