期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 56, 期 7, 页码 2991-2999出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm400034b
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资金
- BMBF
- MOST
- Egyptian Government (Ministry of High Education) [10/6/117]
- National Information Infrastructure Development Institute [NIIFI 10038]
- Fonds National de la Recherche Scientifique, Belgium
- Recherche Cancer et Sang Foundation, by Recherches Scientifiques Luxembourg asbl
- Een Haerz fir Kriibskrank Kanner Association
- Action Lions Vaincre be Cancer Luxembourg
- Fonds National de la Recherche Luxembourg, Televie Luxembourg
- Foundation for Scientific Cooperation between Germany and Luxemburg
- European Union [ITN RedCat 215009]
- [HURO/0901/274/2.2.2]
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-kappa B transcriptional activity, indicating that inhibition of NF-kappa 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.
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