Abstract
Aigialomycins A-E (2-6), new 14-membered resorcylic macrolides, were isolated together with a known hypothemycin (1) from the mangrove fungus, Aigialus parvus BCC 5311. Structures of these compounds, including absolute configuration, were elucidated by spectroscopic methods, chemical conversions, and X-ray crystallographic analysis. Hypothemycin and aigialomycin D (5) exhibited in vitro antimalarial activity with IC(50) values of 2.2 and 6.6 microg/mL, respectively, while other analogues were inactive. Cytotoxicities of these compounds were also evaluated.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / isolation & purification*
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Anti-Bacterial Agents / pharmacology
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Antimalarials / chemistry
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Antimalarials / isolation & purification*
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Antimalarials / pharmacology
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / isolation & purification
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Antineoplastic Agents / pharmacology
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Antiprotozoal Agents / chemistry
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Antiprotozoal Agents / isolation & purification*
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Antiprotozoal Agents / pharmacology
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Ascomycota / chemistry*
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Botrytis / drug effects
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Breast Neoplasms
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Chlorocebus aethiops
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Chromatography, High Pressure Liquid
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Colonic Neoplasms
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Crystallography, X-Ray
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Drug Screening Assays, Antitumor
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Female
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Humans
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Inhibitory Concentration 50
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KB Cells / drug effects
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Kidney / cytology
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Leukemia
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Leukemia P388
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Macrolides*
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Molecular Conformation
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Molecular Structure
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Nuclear Magnetic Resonance, Biomolecular
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Plasmodium falciparum / drug effects
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Tetrahymena / drug effects
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Thailand
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Ustilago / drug effects
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Vero Cells / drug effects
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Zearalenone / analogs & derivatives
Substances
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Anti-Bacterial Agents
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Antimalarials
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Antineoplastic Agents
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Antiprotozoal Agents
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Macrolides
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aigialomycin D
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hypothemycin
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Zearalenone