From the whole plant of Euphorbia peplus L., a new diterpene based on a rare pepluane skeleton, named pepluanone (1), was isolated together with a known pepluane diterpene (2). The stereostructure of pepluanone was determined on the basis of an extensive NMR study, MS data, and chemical reaction. The ability of these compounds to act as antiinflammatory agents has been evaluated for the first time by in vivo tests on carrageenin-induced rat paw edema, an experimental model of acute inflammation. Comparison of the bioactivity of pepluanone and compound 2 in terms of chemical structure, evidenced the high efficiency of pepluanone and the absence of appreciable activity for compound 2, thus giving a first insight into the structure-activity relationship. Further in vitro experiments performed on pepluanone let us hypothesize that its activity could be explained in reducing the production of nitric oxide, prostaglandin E-2, and TNF-alpha by inhibiting the expression of inducible nitric oxide synthase, cyclooxygenase-2, and TNF-alpha mRNA through the down-regulation of NF-kappa B binding activity.
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Univ London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, EnglandUniv London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, England
Andreakos, ET
Foxwell, BM
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Univ London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, EnglandUniv London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, England
Foxwell, BM
Brennan, FM
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Univ London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, EnglandUniv London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, England
Brennan, FM
Maini, RN
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Univ London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, EnglandUniv London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, England
Maini, RN
Feldmann, M
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Univ London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, EnglandUniv London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, England
机构:
UNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USAUNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USA
AUPHAN, N
DIDONATO, JA
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UNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USAUNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USA
DIDONATO, JA
ROSETTE, C
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UNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USAUNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USA
ROSETTE, C
HELMBERG, A
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UNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USAUNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USA
HELMBERG, A
KARIN, M
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UNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USAUNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USA
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Univ London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, EnglandUniv London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, England
Andreakos, ET
Foxwell, BM
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h-index: 0
机构:
Univ London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, EnglandUniv London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, England
Foxwell, BM
Brennan, FM
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Univ London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, EnglandUniv London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, England
Brennan, FM
Maini, RN
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Univ London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, EnglandUniv London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, England
Maini, RN
Feldmann, M
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h-index: 0
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Univ London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, EnglandUniv London Imperial Coll Sci Technol & Med, Fac Med, Div Rheumatol, Kennedy Inst, London W6 8LH, England
机构:
UNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USAUNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USA
AUPHAN, N
DIDONATO, JA
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h-index: 0
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UNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USAUNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USA
DIDONATO, JA
ROSETTE, C
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h-index: 0
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UNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USAUNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USA
ROSETTE, C
HELMBERG, A
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h-index: 0
机构:
UNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USAUNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USA
HELMBERG, A
KARIN, M
论文数: 0引用数: 0
h-index: 0
机构:
UNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USAUNIV CALIF SAN DIEGO, SCH MED,CTR GENET MOLEC,DEPT PHARMACOL, PROGRAM BIOMED SCI, LA JOLLA, CA 92093 USA