Abstract
A new bafilomycin-type macrolide, named hygrobafilomycin (6), was isolated by a bioassay-guided selection and fractionation from a terrestrial actinomycete, Streptomyces varsoviensis, along with three known derivatives, bafilomycin D (3), C1 (4) and C2 (5). The structure of hygrobafilomycin was fully established by MS and NMR analyses, revealing a hygrolidin-bafilomycin hybrid with an unusual monoalkylmaleic anhydride moiety. Hygrobafilomycin (6) shows strong antifungal, antiproliferative and cytotoxic activities. In a panel of 40 tumor cell lines, compound 6 shows high cytotoxic potency (mean IC(50)=5.3 n).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antibiotics, Antineoplastic / chemistry
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Antibiotics, Antineoplastic / isolation & purification*
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Antibiotics, Antineoplastic / pharmacology*
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Antifungal Agents / chemistry
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Antifungal Agents / isolation & purification*
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Antifungal Agents / pharmacology*
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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Humans
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Macrolides / chemistry
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Macrolides / isolation & purification*
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Macrolides / metabolism
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Macrolides / pharmacology*
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Magnetic Resonance Spectroscopy
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Maleates / chemistry
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Maleates / isolation & purification*
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Maleates / metabolism
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Maleates / pharmacology*
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Mass Spectrometry
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Molecular Structure
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Streptomyces / chemistry*
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Streptomyces / metabolism
Substances
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Antibiotics, Antineoplastic
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Antifungal Agents
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Macrolides
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Maleates
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hygrobafilomycin
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hygrolidin
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bafilomycin A1