Abstract
In our search for bioactive metabolites from a marine sponge-associated bacterium Psychrobacter sp., a new bile acid derivative (1), which was assumed to be an artifact, were isolated along with six known (2-7) compounds by bioactivity-guided fractionation. Elucidation of the structure of the new compound was done using a combination of NMR ((1)H, (13)C, HMBC, HSQC, and COSY) and MS spectroscopy. Compound 1 exhibited moderate suppressive effects on both NO and IL-6 production at a concentration of 200 microM (87.3 microg/mL) without significant cytotoxicity against cells. Compounds 2-5 and 7 showed selective inhibitory activity against several human pathogenic bacterial strains at the low concentration of 30 microg/well. In a cytotoxicity evaluation, only compound 7 showed mild cytotoxicity against five human solid tumor cell lines (A-549, SK-OV-3, SK-MEL-2, XF-498, and HCT-15) with ED(50) values in the range of 11-14 microg/mL.
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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Anti-Inflammatory Agents / chemistry
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Anti-Inflammatory Agents / isolation & purification
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Anti-Inflammatory Agents / 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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Bile Acids and Salts* / chemistry
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Bile Acids and Salts* / isolation & purification
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Bile Acids and Salts* / pharmacology
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Cell Line
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Cell Line, Tumor
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Cholic Acids / chemistry
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Cholic Acids / isolation & purification
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Cholic Acids / pharmacology
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Drug Screening Assays, Antitumor
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Humans
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Interleukin-6 / metabolism
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Macrophages / drug effects
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Macrophages / metabolism
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Mice
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Models, Chemical
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Molecular Structure
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Nitric Oxide / metabolism
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Porifera / microbiology*
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Psychrobacter / chemistry*
Substances
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3-dimethoxy-12alpha-hydroxycholanic acid
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Anti-Bacterial Agents
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Anti-Inflammatory Agents
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Antineoplastic Agents
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Bile Acids and Salts
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Cholic Acids
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Interleukin-6
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Nitric Oxide