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NF kappa B inhibitors and antitrypanosomal metabolites from endophytic fungus Penicillium sp. isolated from Limonium tubiflorum |
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| Authors: | Aly Amal H Debbab Abdessamad Clements Carol Edrada-Ebel Ruangelie Orlikova Barbora Diederich Marc Wray Victor Lin Wenhan Proksch Peter |
| Affiliation: | a Heinrich-Heine-Universität, Institut für Pharmazeutische Biologie und Biotechnologie, Universitätsstrasse 1, Geb. 26.23, D-40225 Düsseldorf, Germany b Strathclyde Institute of Pharmacy and Biomedical Science, University of Strathclyde, The John Arbuthnott Building, 27 Taylor Street, Glasgow G4 0NR, UK c Laboratoire de Biologie Moléculaire et Cellulaire du Cancer, Hôpital Kirchberg 9, rue Steichen L-2540, Luxembourg d Helmholtz Centre for Infection Research, Inhoffenstraße 7, D-38124 Braunschweig, Germany e National Research Laboratories of Natural and Biomimetic Drugs, Peking University, Health Science Center, 100083 Beijing, People’s Republic of China |
| Abstract: | Chemical investigation of the endophytic fungus Penicillium sp. isolated from Limonium tubiflorum growing in Egypt afforded four new compounds of polyketide origin, including two macrolides, penilactone (1) and 10,11-epoxycurvularin (2), a dianthrone, neobulgarone G (7), and a sulfinylcoumarin, sulfimarin (14), along with twelve known metabolites (3-6, 8-13, 15 and 16). The structures of all compounds were assigned by comprehensive spectral analysis (1D and 2D NMR) and mass spectrometry. Compounds 3, 4, 13 and 16 showed pronounced antitrypanosomal activity with mean MIC values ranging from 4.96 to 9.75 ??M. Moreover, when tested against a panel of three human tumor cell lines compounds 3, 4, 6 and 12 showed selective growth inhibition against Jurkat and U937 cell lines with IC50 values ranging from 1.8 to 13.3 ??M. The latter compounds also inhibited TNF??-induced NF-??B activity in K562 cells with IC50 values ranging from 1.6 to 10.1 ??M, respectively. |
| Keywords: | Penicillium Limonium tubiflorum Endophytic fungi Natural products Trypanosoma Antitrypanosomal activity Cytotoxic activity NF kappa B |
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