Abstract
Bioassay guided separation of Sida acuta whole plants led to the isolation of an alkaloid, cryptolepine (1), along with two kaempferol glycosides (2-3). Compound 1 showed strong activity in overcoming TRAIL-resistance in human gastric adenocarcinoma (AGS) cells at 1.25, 2.5 and 5 μm. Combined treatment of 1 and TRAIL sensitized AGS cells to TRAIL-induced apoptosis at the aforementioned concentrations.
Copyright © 2010 John Wiley & Sons, Ltd.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenocarcinoma / pathology
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Antineoplastic Agents, Phytogenic / chemistry
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Antineoplastic Agents, Phytogenic / isolation & purification
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Antineoplastic Agents, Phytogenic / pharmacology*
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Apoptosis / drug effects*
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Caspase 3 / metabolism
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Caspase 7 / metabolism
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Cell Line, Tumor
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Drug Resistance, Neoplasm
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Enzyme Activation / drug effects
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Glycosides / chemistry
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Glycosides / isolation & purification
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Glycosides / pharmacology
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Humans
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Indole Alkaloids / chemistry
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Indole Alkaloids / isolation & purification
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Indole Alkaloids / pharmacology*
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Malvaceae / chemistry*
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Quinolines / chemistry
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Quinolines / isolation & purification
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Quinolines / pharmacology*
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Stomach Neoplasms / pathology
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TNF-Related Apoptosis-Inducing Ligand / pharmacology*
Substances
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Antineoplastic Agents, Phytogenic
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Glycosides
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Indole Alkaloids
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Quinolines
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TNF-Related Apoptosis-Inducing Ligand
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cryptolepine
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Caspase 3
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Caspase 7