Abstract
The methanol-soluble extracts of the roots of Cynanchum wilfordii showed a significant multidrug-resistance-reversing activity, and four known pregnane glycosides were isolated by bioassay-directed fractionation and separation. Their structures were identified as gagaminin 3-O-beta-D-cymaropyranosyl-(1-->4)-beta-D-oleandropyranosyl- (1-->4)-b eta-D-cymaropyranosyl-(1-->4)-beta-D-cymaropyranoside (1), wilfoside K1N (2), wilfoside C1N (3), and cynauricuoside A (4). In particular, compound 1, at a concentration level of 1 microM, was found to completely reverse the multidrug-resistance of KB-V1 and MCF7/ADR cells to adriamycin, vinblastine, and colchicine.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / pharmacology
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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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Carbohydrate Sequence
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Colchicine / pharmacology
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Doxorubicin / pharmacology
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Drug Resistance, Multiple
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Drug Resistance, Neoplasm
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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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Inhibitory Concentration 50
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KB Cells
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Molecular Sequence Data
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Plant Roots / chemistry
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Plants, Medicinal / chemistry*
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Pregnanes / chemistry
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Pregnanes / isolation & purification*
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Pregnanes / pharmacology
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Tumor Cells, Cultured
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Vinblastine / pharmacology
Substances
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Antineoplastic Agents
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Antineoplastic Agents, Phytogenic
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Glycosides
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Pregnanes
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Vinblastine
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Doxorubicin
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Colchicine