Abstract
Phytochemical investigation of EtOAc extracts of the aerial parts of Isodon wikstroemioides afforded 18 new ent-kaurane diterpenoids (wikstroemioidins E-V, 1-18), along with 17 known analogues (19-35). The absolute configurations of 1 and 16 were confirmed by single-crystal X-ray diffraction analysis. The isolates were screened against five human tumor cell lines; compounds 3, 4, 9, 11-13, 23, 25-28, and 33 exhibited significant cytotoxic activity against all five, with IC50 values ranging from 0.4 to 5.1 μM. In addition, 17 of the isolates strongly inhibited nitric oxide production in LPS-activated RAW264.7 macrophages.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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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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Crystallography, X-Ray
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Diterpenes, Kaurane* / chemistry
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Diterpenes, Kaurane* / isolation & purification
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Diterpenes, Kaurane* / pharmacology
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Drug Screening Assays, Antitumor
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Drugs, Chinese Herbal* / chemistry
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Drugs, Chinese Herbal* / isolation & purification
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Drugs, Chinese Herbal* / pharmacology
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HL-60 Cells
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Humans
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Isodon / chemistry*
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Lipopolysaccharides / pharmacology
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Macrophages / drug effects
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Mice
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Nitric Oxide / biosynthesis
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Nuclear Magnetic Resonance, Biomolecular
Substances
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Antineoplastic Agents, Phytogenic
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Diterpenes, Kaurane
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Drugs, Chinese Herbal
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Lipopolysaccharides
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Nitric Oxide