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Epipolythiodiketopiperazines from the Marine Derived Fungus Dichotomomyces cejpii with NF-κB Inhibitory Potential

Institute for Pharmaceutical Biology, University of Bonn, Nussallee 6, Bonn D-53115, Germany
Department of Pharmacy, College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Korea
Laboratoire de Biologie Moléculaire et Cellulaire du Cancer (LBMCC), Hôpital Kirchberg, 9 rue Edward Steichen, Luxembourg L-2540, Luxembourg
Authors to whom correspondence should be addressed.
Academic Editor: Vassilios Roussis
Mar. Drugs 2015, 13(8), 4949-4966;
Received: 18 May 2015 / Revised: 26 June 2015 / Accepted: 15 July 2015 / Published: 6 August 2015
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The Ascomycota Dichotomomyces cejpii was isolated from the marine sponge Callyspongia cf. C. flammea. A new gliotoxin derivative, 6-acetylmonodethiogliotoxin (1) was obtained from fungal extracts. Compounds 2 and 3, methylthio-gliotoxin derivatives were formerly only known as semi-synthetic compounds and are here described as natural products. Additionally the polyketide heveadride (4) was isolated. Compounds 1, 2 and 4 dose-dependently down-regulated TNFα-induced NF-κB activity in human chronic myeloid leukemia cells with IC50s of 38.5 ± 1.2 µM, 65.7 ± 2.0 µM and 82.7 ± 11.3 µM, respectively. The molecular mechanism was studied with the most potent compound 1 and results indicate downstream inhibitory effects targeting binding of NF-κB to DNA. Compound 1 thus demonstrates potential of epimonothiodiketopiperazine-derived compounds for the development of NF-κB inhibitors. View Full-Text
Keywords: Ascomycete; Dichotomomyces; gliotoxin; NF-κB; leukemia Ascomycete; Dichotomomyces; gliotoxin; NF-κB; leukemia

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Harms, H.; Orlikova, B.; Ji, S.; Nesaei-Mosaferan, D.; König, G.M.; Diederich, M. Epipolythiodiketopiperazines from the Marine Derived Fungus Dichotomomyces cejpii with NF-κB Inhibitory Potential. Mar. Drugs 2015, 13, 4949-4966.

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