Abstract
Bioassay-guided fractionation of a non-polar extract of Lyngbya cf. polychroa resulted in the isolation of the cytotoxic desacetylmicrocolin B (1) as well as the known compounds microcolins A (2) and B (3). Compound 1 was found to inhibit the growth of HT-29 colorectal adenocarcinoma and IMR-32 neuroblastoma cells with half maximal inhibitory concentration (IC(50)) values of 14 nM for both cancer cell types. Microcolins A and B were found to have little activity against two strains of the marine fungus Dendryphiella salina with LD(50) values above 200 microg/mL. Compounds 1, 2, and 3 were obtained by reverse-phase chromatography and their structures were determined by NMR and MS. In this paper we report the isolation, identification, and biological activity of 1.
Georg Thieme Verlag KG Stuttgart-New York.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Adenocarcinoma / drug therapy
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Antineoplastic Agents, Phytogenic / isolation & purification
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Antineoplastic Agents, Phytogenic / pharmacology
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Antineoplastic Agents, Phytogenic / therapeutic use*
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Biological Assay
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Cell Line, Tumor
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Colonic Neoplasms / drug therapy
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Cyanobacteria / chemistry*
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Fungi / drug effects
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Humans
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Inhibitory Concentration 50
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Lyngbya Toxins / isolation & purification
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Lyngbya Toxins / pharmacology
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Lyngbya Toxins / therapeutic use*
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Molecular Structure
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Neoplasms / drug therapy*
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Neuroblastoma / drug therapy
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Oligopeptides / isolation & purification
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Oligopeptides / pharmacology
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Oligopeptides / therapeutic use*
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Pyrrolidines / isolation & purification
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Pyrrolidines / pharmacology
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Pyrrolidines / therapeutic use*
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Rectal Neoplasms / drug therapy
Substances
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Antineoplastic Agents, Phytogenic
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Lyngbya Toxins
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Oligopeptides
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Pyrrolidines
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desacetylmicrocolin B