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Mar. Drugs 2012, 10(4), 762-774; doi:10.3390/md10040762

Epigenetic Tailoring for the Production of Anti-Infective Cytosporones from the Marine Fungus Leucostoma persoonii

, 1
, 2
, 2
, 2
, 3
, 3
, 3
, 3
 and 1,*
1 Department of Chemistry and Center for Molecular Diversity in Drug Design, Discovery and Delivery, University of South Florida, Tampa, FL 33620, USA 2 Department of Cell Biology, Microbiology and Molecular Biology, University of South Florida, Tampa, FL 33620, USA 3 Department of Global Health, University of South Florida, Tampa, FL 33620, USA
* Author to whom correspondence should be addressed.
Received: 22 February 2012 / Revised: 13 March 2012 / Accepted: 20 March 2012 / Published: 28 March 2012
(This article belongs to the Special Issue Marine Anti-infective Agents)
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Recent genomic studies have demonstrated that fungi can possess gene clusters encoding for the production of previously unobserved secondary metabolites. Activation of these attenuated or silenced genes to obtain either improved titers of known compounds or new ones altogether has been a subject of considerable interest. In our efforts to discover new chemotypes that are effective against infectious diseases, including malaria and methicillin-resistant Staphylococcus aureus (MRSA), we have isolated a strain of marine fungus, Leucostoma persoonii, that produces bioactive cytosporones. Epigenetic modifiers employed to activate secondary metabolite genes resulted in enhanced production of known cytosporones B (1, 360%), C (2, 580%) and E (3, 890%), as well as the production of the previously undescribed cytosporone R (4). Cytosporone E was the most bioactive, displaying an IC90 of 13 µM toward Plasmodium falciparum, with A549 cytotoxicity IC90 of 437 µM, representing a 90% inhibition therapeutic index (TI90 = IC90 A459/IC90 P. falciparum) of 33. In addition, cytosporone E was active against MRSA with a minimal inhibitory concentration (MIC) of 72 µM and inhibition of MRSA biofilm at roughly half that value (minimum biofilm eradication counts, MBEC90, was found to be 39 µM).
Keywords: epigenetics; fungus; mangrove; MRSA; malaria epigenetics; fungus; mangrove; MRSA; malaria
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.

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Beau, J.; Mahid, N.; Burda, W.N.; Harrington, L.; Shaw, L.N.; Mutka, T.; Kyle, D.E.; Barisic, B.; van Olphen, A.; Baker, B.J. Epigenetic Tailoring for the Production of Anti-Infective Cytosporones from the Marine Fungus Leucostoma persoonii. Mar. Drugs 2012, 10, 762-774.

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