Abstract
A novel macrolide, apicularen A, was produced by several species of the genus Chondromyces. Initially it was discovered by bioassay-guided RP-HPLC-fractionation of culture extracts of Chondromyces robustus, strain Cm a13. Apicularen A showed no antimicrobial activity, but was highly cytotoxic for cultivated human and animal cells, with IC50 values ranging between 0.1 and 3 ng/ml. A cometabolite of apicularen A, the N-acetylglucosamine glycoside apicularen B, was distinctly less cytotoxic with IC50 values between 0.2 and 1.2 microg/ml, and showed weak activity against a few Gram-positive bacteria. Apicularen A is chemically closely related to the salicylihalamides A and B from the marine sponge Haliclona sp.
MeSH terms
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Animals
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Anti-Bacterial Agents / biosynthesis
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology*
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Antibiotics, Antineoplastic / biosynthesis
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Antibiotics, Antineoplastic / chemistry
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Antibiotics, Antineoplastic / pharmacology*
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Bridged Bicyclo Compounds, Heterocyclic / chemistry
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Bridged Bicyclo Compounds, Heterocyclic / metabolism
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Bridged Bicyclo Compounds, Heterocyclic / pharmacology*
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Chemical Phenomena
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Chemistry, Physical
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Drug Screening Assays, Antitumor
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Gram-Positive Bacteria / drug effects
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Humans
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Macrolides*
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Microbial Sensitivity Tests
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Molecular Structure
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Myxococcales / metabolism*
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Porifera / chemistry
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Tumor Cells, Cultured
Substances
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Anti-Bacterial Agents
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Antibiotics, Antineoplastic
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Bridged Bicyclo Compounds, Heterocyclic
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Macrolides
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apicularen A
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apicularen B