Abstract
A screening study for TRAIL resistance-overcoming activity was carried out, and activity-guided fractionations of Thevetia peruviana and Sapindus emarginatus led to the isolation of four cardenolide glycosides (1-4) and four triterpenoid saponins (5-8), respectively. In particular, cardenolide glycosides (1 and 2) from T. peruviana were shown to have a significant reversal effect on TRAIL resistance in human gastric adenocarcinoma cells, and real-time PCR showed that thevefolin (2) enhanced mRNA expression of death receptor 4 (DR4) and DR5. In addition, 1H and 13C NMR characterizations are shown for thevefolin (2) for the first time.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Base Sequence
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Cardenolides / chemistry
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Cardenolides / isolation & purification*
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Cardenolides / pharmacology*
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Humans
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Molecular Structure
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Nuclear Magnetic Resonance, Biomolecular
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Plants, Medicinal / chemistry*
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Receptors, TNF-Related Apoptosis-Inducing Ligand / genetics
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Sapindus / chemistry*
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Saponins / chemistry
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Saponins / isolation & purification*
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Saponins / pharmacology*
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Stomach Neoplasms / metabolism
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TNF-Related Apoptosis-Inducing Ligand / drug effects*
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Thailand
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Thevetia / chemistry*
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Tumor Cells, Cultured
Substances
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Cardenolides
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Receptors, TNF-Related Apoptosis-Inducing Ligand
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Saponins
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TNF-Related Apoptosis-Inducing Ligand