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Mar. Drugs 2015, 13(8), 4949-4966; doi:10.3390/md13084949

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

1
Institute for Pharmaceutical Biology, University of Bonn, Nussallee 6, Bonn D-53115, Germany
2
Department of Pharmacy, College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Korea
3
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
Received: 18 May 2015 / Revised: 26 June 2015 / Accepted: 15 July 2015 / Published: 6 August 2015
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Abstract

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
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

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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