Studies on the anti-inflammatory activity of phytopharmaceuticals prepared from Arnica flowers.
Phytopharmaceuticals prepared from flowerheads of Arnica montana of Spanish origin and of the new type "Arbo", which can be easily and economically cultivated, were studied for their capability to impair activation of the transcription factors NF-kappa B and NF-AT. Both proteins are responsible for the transcription of genes encoding various inflammatory mediators. Additionally, their influence on the release of the cytokines IL-1 and TNF-alpha were examined. The inhibitory activities correlate with their quantitative and qualitative content of sesquiterpene lactones (Sls). Moreover, it was shown that the inhibitory potency of 11 alpha,13-dihydrohelenalin derivatives being the main Sls in the Spanish flowers depend on their esterfication. Compounds with unsaturated acyl moieties, such as methacrylate and tiglinate, exhibited a stronger activity in the NF-kappa B EMSA as well as in the croton oil ear test in mice than the acetate derivative.
Klaas
Christoph A
CA
Institute of Pharmaceutical Biology, University of Freiburg, Freiburg, Germany.
Wagner
Gerd
G
Laufer
Stefan
S
Sosa
Silvio
S
Della Loggia
Roberto
R
Bomme
Ulrich
U
Pahl
Heike L
HL
Merfort
Irmgard
I
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D018650:Arnica; D002470:Cell Survival / Q000187:drug effects; D003436:Croton Oil / Q000494:pharmacology; D004268:DNA-Binding Proteins / Q000187:drug effects / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D006801:Humans; D007213:Indomethacin / Q000494:pharmacology; D007375:Interleukin-1 / Q000378:metabolism; D019169:Jurkat Cells / Q000187:drug effects; D007783:Lactones / Q000302:isolation & purification / Q000494:pharmacology; D007963:Leukocytes, Mononuclear / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D008297:Male; D051379:Mice; D015394:Molecular Structure; D016328:NF-kappa B / Q000187:drug effects / Q000378:metabolism; D050778:NFATC Transcription Factors; D009687:Nuclear Proteins; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology*; D018547:Plant Stems / Q000737:chemistry; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D014157:Transcription Factors / Q000187:drug effects / Q000378:metabolism; D014409:Tumor Necrosis Factor-alpha / Q000187:drug effects / Q000378:metabolism
D000893:Anti-Inflammatory Agents; D004268:DNA-Binding Proteins; D007375:Interleukin-1; D007783:Lactones; D016328:NF-kappa B; D050778:NFATC Transcription Factors; D009687:Nuclear Proteins; D010936:Plant Extracts; D012717:Sesquiterpenes; D014157:Transcription Factors; D014409:Tumor Necrosis Factor-alpha; C026745:plenolin; D003436:Croton Oil; D007213:Indomethacin