Abstract
Investigation of whole plants of Euphorbia fischeriana afforded three new tigliane-diterpenoid glycosides, fischerosides A-C (1-3), together with 11 known diterpenoids. Fischerosides A-C (1-3) are the first tigliane-type diterpenoid glucosides. Their structures were determined by a combination of 1D and 2D NMR, MS, and acid hydrolysis. Inhibitory activity against HIV-1 was assessed for compounds 1-5. The new compound 3 showed an EC₅₀ value of 0.02 μM and a therapeutic index (TI) of 17.50, while prostratin (4) and 12-deoxyphorbol-13,20-diacetate (5) showed significantly greater anti-HIV-1 activity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / isolation & purification*
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Anti-HIV Agents / pharmacology
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Diterpenes / chemistry
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Diterpenes / isolation & purification*
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Diterpenes / pharmacology
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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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Euphorbia / chemistry*
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Glucosides / chemistry
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Glucosides / isolation & purification*
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Glucosides / pharmacology
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HIV-1 / drug effects*
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Molecular Structure
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Nuclear Magnetic Resonance, Biomolecular
Substances
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Anti-HIV Agents
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Diterpenes
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Drugs, Chinese Herbal
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Glucosides
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fischeroside A
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fischeroside B
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fischeroside C