Antifungal Activity of Natural Naphthoquinones and Anthraquinones against Madurella mycetomatis |
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| Authors: | Jingyi Ma Matthew Todd Wendy W. J. van de Sande Bernhard Biersack |
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| Affiliation: | 1. Department of Medical Microbiology and Infectious Diseases, Erasmus MC, University Medical Center Rotterdam, Dr. Molewaterplein 40, 3015 GD Rotterdam, The, Netherlands;2. School of Pharmacy, University College London, London, WC1N 1AX United Kingdom;3. Organic Chemistry Laboratory, University Bayreuth, Universitätsstrasse 30, 95440 Bayreuth, Germany |
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| Abstract: | Eumycetoma, the fungal form of the neglected tropical disease mycetoma, is a crippling infectious disease with low response rates to currently available antifungal drugs. In this study, a series of natural naphthoquinones and anthraquinones was evaluated for their activity against Madurella mycetomatis, which is the most common causative agent of eumycetoma. The metabolic activity of Madurella mycetomatis as well as the viability of Galleria mellonella larvae upon treatment with quinones was investigated. Several hydroxy-substituted naphthoquinones exhibited activity against Madurella mycetomatis. In particular, naphthazarin (5,8-dihydroxy-1,4-naphthoquinone) was identified as a considerably active antifungal compound against Madurella mycetomatis (IC50=1.4 μM), while it showed reduced toxicity to Galleria mellonella larvae, which is a well-established in vivo invertebrate model for mycetoma drug studies. |
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| Keywords: | antifungal eumycetoma naphthazarin naphthoquinone neglected tropical disease |
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