Abstract
Eight new pseudoguaianolides (1-8), two new guaianolides (9 and 10), and 14 known sesquiterpenes were isolated from the aerial parts of Inula hupehensis. The structures were elucidated using spectroscopic methods and circular dichroism analysis. All compounds were tested for inhibitory activities against LPS-induced nitric oxide production in RAW264.7 macrophages. Compounds 13 and 22 were found to inhibit nitric oxide production potently, with IC50 values of 0.9 and 0.6 μM, respectively. Preliminary structure-activity relationships for these compounds are proposed.
MeSH terms
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / isolation & purification*
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Cell Survival / drug effects
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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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Inhibitory Concentration 50
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Inula / chemistry*
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Lipopolysaccharides / pharmacology
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Macrophages / drug effects
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Mice
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Molecular Structure
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Nitric Oxide / antagonists & inhibitors
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Nitric Oxide / biosynthesis
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Sesquiterpenes, Guaiane / chemistry
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Sesquiterpenes, Guaiane / isolation & purification*
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Sesquiterpenes, Guaiane / pharmacology*
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Structure-Activity Relationship
Substances
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2alpha-acetoxy-4alpha,6alpha-dihydroxy-1beta,5alphaH-guai-9(10),11(13)-dien-12,8alpha-olide
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4beta,10alpha-dihydroxy-5alphaH-guai-1(2),11(13)-dien-12,8alpha-olide
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Anti-Inflammatory Agents, Non-Steroidal
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Drugs, Chinese Herbal
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Lipopolysaccharides
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Sesquiterpenes, Guaiane
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Nitric Oxide