Abstract
Six new 6,7-seco-ent-kaurane diterpenoids, sculponeatins N-S (1-6, resp.), together with eleven known analogues, 7-17, were isolated from the aerial parts of Isodon sculponeatus. The structures of compounds 1-6 were elucidated by spectroscopic methods including extensive 1D- and 2D-NMR experiments, as well as HR-ESI-MS analysis. All diterpenoids obtained were assayed for their cytotoxic activity against K562 and HepG2 human tumor cell lines. Among them, compound 1 showed the most significant cytotoxicity with the IC₅₀ values of 0.21 and 0.29 μM, respectively. The structure-activity relationships are discussed.
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 / toxicity
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Cell Line, Tumor
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Diterpenes, Kaurane / chemistry*
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Diterpenes, Kaurane / isolation & purification
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Diterpenes, Kaurane / toxicity
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Humans
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Isodon / chemistry*
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Magnetic Resonance Spectroscopy
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Molecular Conformation
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Plant Extracts / chemistry
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Plant Extracts / toxicity
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Spectrometry, Mass, Electrospray Ionization
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Structure-Activity Relationship
Substances
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Antineoplastic Agents, Phytogenic
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Diterpenes, Kaurane
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Plant Extracts