Abstract
Inhibiting interleukin-6 (IL-6) has been postulated as an effective therapy in the pathogenesis of several inflammatory diseases. In this study, seven flavonoids were isolated from the methanol extracts of Psoralea corylifolia by bioactivity-guided fractionation. The structures of bakuchiol (1), bavachinin (2), neobavaisoflavone (3), corylifol A (4), corylin (5), isobavachalcon (6), and bavachin (7) were determined by spectroscopic analysis (1H-, 13C- NMR and MS). We demonstrated that compounds 1-7 showed an inhibitory effect on IL-6-induced STAT3 promoter activity in Hep3B cells with IC50 values of 4.57 ± 0.45, 3.02 ± 0.53, 2.77 ± 0.02, 0.81 ± 0.15, 1.37 ± 0.45, 2.45 ± 0.13, and 4.89 ± 0.05 µΜ, respectively. These compounds also inhibited STAT3 phosphorylation induced by IL-6 in Hep3B cells. Overall, several flavonoids from P. corylifolia might be useful remedies for treating inflammatory diseases by inhibiting IL-6-induced STAT3 activation and phosphorylation.
Georg Thieme Verlag KG Stuttgart · New York.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Inflammatory Agents / chemistry
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Anti-Inflammatory Agents / pharmacology*
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Cell Line
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Drug Evaluation, Preclinical / methods
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Flavones / chemistry
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Flavones / isolation & purification
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Flavones / pharmacology
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Flavonoids / chemistry*
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Flavonoids / isolation & purification
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Flavonoids / pharmacology*
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Humans
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Inhibitory Concentration 50
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Interleukin-6 / pharmacology*
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Isoflavones / chemistry
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Isoflavones / isolation & purification
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Isoflavones / pharmacology
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Molecular Structure
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Phenols / chemistry
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Phenols / isolation & purification
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Phenols / pharmacology
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Phosphorylation / drug effects
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Plant Extracts / pharmacology
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Plants, Medicinal / chemistry
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Promoter Regions, Genetic
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Psoralea / chemistry*
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STAT3 Transcription Factor / genetics
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STAT3 Transcription Factor / metabolism*
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Structure-Activity Relationship
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Tyrosine / metabolism
Substances
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Anti-Inflammatory Agents
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Flavones
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Flavonoids
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Interleukin-6
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Isoflavones
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Phenols
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Plant Extracts
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STAT3 Transcription Factor
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STAT3 protein, human
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bavachin
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corylifol A
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corylin
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neobavaisoflavone
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Tyrosine
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bakuchiol
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bavachinin