Abstract
Ten new indole alkaloids of the aspidofractinine type, in addition to several recently reported indole alkaloids and 20 other known alkaloids, were obtained from the leaf and stem-bark extract of the Malayan Kopsia singapurensis, viz., kopsimalines A-E (1-5), kopsinicine (6), kopsofinone (7), and kopsiloscines H-J (8-10). The structures of these alkaloids were determined using NMR and MS analysis. Kopsimalines A (1), B (2), C (3), D (4), and E (5) and kopsiloscine J (10) were found to reverse multidrug-resistance in vincristine-resistant KB cells, with 1 showing the highest potency.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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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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Apocynaceae / chemistry*
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Drug Resistance, Neoplasm / drug effects
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Drug Screening Assays, Antitumor
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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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KB Cells
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Malaysia
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Molecular Structure
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Plant Bark / chemistry
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Plant Leaves / chemistry
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Plants, Medicinal / chemistry*
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Vincristine / pharmacology*
Substances
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Antineoplastic Agents, Phytogenic
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Indole Alkaloids
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Vincristine