Abstract
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. © 2013 by the authors; licensee MDPI.
| Original language | English |
|---|---|
| Pages (from-to) | 5036-5050 |
| Journal | Marine Drugs |
| Volume | 11 |
| Issue number | 12 |
| DOIs | |
| Publication status | Published - Dec 2013 |
Bibliographical note
Publication details (e.g. title, author(s), publication statuses and dates) are captured on an “AS IS” and “AS AVAILABLE” basis at the time of record harvesting from the data source. Suggestions for further amendments or supplementary information can be sent to <a href="mailto:[email protected]">[email protected]</a>.Funding
This research was supported by Medicines for Malaria Venture, MMV08/0105. NMR and mass spectrometric facilities in the Center for Drug Discovery and Innovation were supported by a State of Florida Center of Excellence award.
UN SDGs
This output contributes to the following UN Sustainable Development Goals (SDGs)
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SDG 3 Good Health and Well-being
Research Keywords
- Cytotoxicity
- Endophytes
- Fungi
- High-throughput
- Malaria
- Mangroves
Publisher's Copyright Statement
- This full text is made available under CC-BY 3.0. https://creativecommons.org/licenses/by/3.0/
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