Abstract
Biseokeaniamides A, B, and C (1-3), structurally novel sterol O-acyltransferase (SOAT) inhibitors, were isolated from an Okeania sp. marine cyanobacterium. Their structures were elucidated by spectroscopic analyses and degradation reactions. Biseokeaniamide B (2) exhibited moderate cytotoxicity against human HeLa cancer cells, and compounds 1-3 inhibited both SOAT1 and SOAT2, not only at an enzyme level but also at a cellular level. Biseokeaniamides (1-3) are the first linear lipopeptides that have been shown to exhibit SOAT-inhibitory activity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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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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Caspase 3 / metabolism
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Cyanobacteria / chemistry*
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HeLa Cells
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Humans
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Lipopeptides / chemistry
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Lipopeptides / isolation & purification*
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Lipopeptides / pharmacology*
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Marine Biology
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Molecular Structure
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Nuclear Magnetic Resonance, Biomolecular
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Sterol O-Acyltransferase / antagonists & inhibitors*
Substances
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Antineoplastic Agents
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Lipopeptides
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biseokeaniamide A
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biseokeaniamide B
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biseokeaniamide C
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Sterol O-Acyltransferase
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Caspase 3