Abstract
Compounds BM2419-1 and -2 were isolated from a culture broth of a fungus Paecilomyces sp. BM2419. It was shown that these novel compounds were artifacts derived from saintopin, a dual inhibitor of topoisomerase I and II by independent processes. In the human topoisomerase I inhibition assay using the recombinant Saccharomyces cerevisiae, BM2419-1 and -2 inhibited selectively the yeast growth dependent on human topoisomerase I induction with IC50 values of 0.3 ng/ml and 6.0 ng/ml, respectively.
MeSH terms
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Animals
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Anthracyclines*
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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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Benz(a)Anthracenes / chemistry
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Benz(a)Anthracenes / isolation & purification
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Benz(a)Anthracenes / pharmacology
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Camptothecin / pharmacology
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Chemical Phenomena
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Chemistry, Physical
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DNA Topoisomerases, Type I / genetics
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Drug Screening Assays, Antitumor
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / isolation & purification
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Enzyme Inhibitors / pharmacology*
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Humans
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In Vitro Techniques
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Magnetic Resonance Spectroscopy
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Molecular Structure
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Paecilomyces / chemistry
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Recombinant Proteins / antagonists & inhibitors
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Recombinant Proteins / genetics
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Saccharomyces cerevisiae / enzymology
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Saccharomyces cerevisiae / genetics
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Topoisomerase I Inhibitors*
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Tumor Cells, Cultured
Substances
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Anthracyclines
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Antibiotics, Antineoplastic
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BM 2419-1
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BM 2419-2
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Benz(a)Anthracenes
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Enzyme Inhibitors
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Recombinant Proteins
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Topoisomerase I Inhibitors
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saintopin
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DNA Topoisomerases, Type I
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Camptothecin