Abstract
Two novel quinomycin derivatives, RK-1355A (1) and B (2), and one known quinomycin derivative, UK-63,598 (3), were isolated from a microbial metabolites fraction library of Streptomyces sp. RK88-1355 based on Natural Products Plot screening. The structural elucidation of 1 and 2 was established through two-dimensional NMR and mass spectrometric measurements. They belong to a class of quinomycin antibiotics family having 3-hydroxyquinaldic acid and a sulfoxide moiety. They are the first examples for natural products as a quinoline type quinomycin having a sulfoxide on the intramolecular cross-linkage. They showed potent antiproliferative activities against various cancer cell lines and they were also found to exhibit moderate antibacterial activity.
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 / metabolism
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Anti-Bacterial Agents / pharmacology
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / isolation & purification*
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Antineoplastic Agents / metabolism
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Drug Discovery*
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Echinomycin / analogs & derivatives*
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Echinomycin / chemistry
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Echinomycin / isolation & purification
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Echinomycin / metabolism
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Echinomycin / pharmacology
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Escherichia coli / drug effects*
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Escherichia coli / growth & development
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Humans
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Inhibitory Concentration 50
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Mice
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Microbial Sensitivity Tests
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Molecular Structure
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Neoplasms / drug therapy*
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Small Molecule Libraries
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Staphylococcus aureus / drug effects*
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Staphylococcus aureus / growth & development
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Streptomyces / metabolism*
Substances
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Anti-Bacterial Agents
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Antineoplastic Agents
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RK-1355A
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Small Molecule Libraries
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UK 63598
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Echinomycin