Screening Mangrove Endophytic Fungi for Antimalarial Natural Products

Marine Drugs

Laurent Calcul⁴  Carrie Waterman⁴  Wai Sheung Ma⁴  Matthew D. Lebar⁴  Charles Harter⁴  Tina Mutka³  Lindsay Morton³  Patrick Maignan³  Alberto Van Olphen³  Dennis E. Kyle³  Lilian Vrijmoed²  Ka-Lai Pang¹  Cedric Pearce⁵ 

[1] Institute of Marine Biology and Center of Excellence for the Oceans, National Taiwan Ocean University, 2 Pei-Ning Road, Keelung 20224, Taiwan; E-Mail:;Department of Biology and Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Hong Kong, China; E-Mail:;Department of Global Health, University of South Florida, 3720 Spectrum Blvd., Suite 304, Tampa, FL 33612, USA; E-Mails:;Department of Chemistry, University of South Florida, 4202 E. Fowler, CHE 205, Tampa, FL 33620, USA; E-Mails:;Mycosynthetix, Inc., 505 Meadowlands Drive, Suite 103, Hillsborough, NC 27278, USA; E-Mail:

关键词: fungi;    endophytes;    mangroves;    malaria;    cytotoxicity;    high-throughput;   

DOI  :  10.3390/md11125036

来源: mdpi

【 摘 要 】

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 (14–16, 18) were isolated including a new dimeric tetrahydroxanthone, dicerandrol D (14), which was found to display the most favorable bioactivity profile.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.