Embellicines A and B: Absolute Configuration and NF-kappa B Transcriptional Inhibitory Activity

作者：Ebrahim Weaam; Aly Amal H; Wray Victor; Mandi Attila; Teiten Marie Helene; Gaascht Francois; Orlikova Barbora; Kassack Matthias U; Lin WenHan; Diederich Marc; Kurtan Tibor; Debbab Abdessamad^*; Proksch Peter

来源：Journal of Medicinal Chemistry, 2013, 56(7): 2991-2999.

DOI：10.1021/jm400034b

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.

• 出版日期2013-4-11
• 单位北京大学