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Screening Mangrove Endophytic Fungi for Antimalarial Natural Products

Department of Chemistry, University of South Florida, 4202 E. Fowler, CHE 205, Tampa, FL 33620, USA
Department of Global Health, University of South Florida, 3720 Spectrum Blvd., Suite 304,Tampa, FL 33612, USA
Department of Biology and Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Hong Kong, China
Institute of Marine Biology and Center of Excellence for the Oceans, National Taiwan Ocean University, 2 Pei-Ning Road, Keelung 20224, Taiwan
Mycosynthetix, Inc., 505 Meadowlands Drive, Suite 103, Hillsborough, NC 27278, USA
Center for Drug Discovery and Innovation, University of South Florida, 3720 Spectrum Blvd., Suite 303, Tampa, FL 33612, USA
Author to whom correspondence should be addressed.
Mar. Drugs 2013, 11(12), 5036-5050;
Received: 12 September 2013 / Revised: 27 November 2013 / Accepted: 28 November 2013 / Published: 12 December 2013
(This article belongs to the Special Issue Antiprotozoal Marine Natural Products)
PDF [583 KB, uploaded 24 February 2015]


We conducted a screening campaign to investigate fungi as a source for new antimalarial compounds. A subset of our fungal collection comprising Chinese mangrove endophytes provided over 5000 lipophilic extracts. We developed an accelerated discovery program based on small-scale cultivation for crude extract screening and a high-throughput malaria assay. Criteria for hits were developed and high priority hits were subjected to scale-up cultivation. Extracts from large scale cultivation were fractionated and these fractions subjected to both in vitro malaria and cytotoxicity screening. Criteria for advancing fractions to purification were developed, including the introduction of a selectivity index and by dereplication of known metabolites. From the Chinese mangrove endophytes, four new compounds (1416, 18) were isolated including a new dimeric tetrahydroxanthone, dicerandrol D (14), which was found to display the most favorable bioactivity profile. View Full-Text
Keywords: fungi; endophytes; mangroves; malaria; cytotoxicity; high-throughput fungi; endophytes; mangroves; malaria; cytotoxicity; high-throughput

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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Calcul, L.; Waterman, C.; Ma, W.S.; Lebar, M.D.; Harter, C.; Mutka, T.; Morton, L.; Maignan, P.; Olphen, A.V.; Kyle, D.E.; Vrijmoed, L.; Pang, K.-L.; Pearce, C.; Baker, B.J. Screening Mangrove Endophytic Fungi for Antimalarial Natural Products. Mar. Drugs 2013, 11, 5036-5050.

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