Further sesquiterpene lactones from Viguiera robusta and the potential anti-inflammatory activity of a heliangolide: inhibition of human neutrophil elastase release.
In addition to known heliangolides, a new eudesmanolide was isolated from the leaf rinse extract of Viguiera robusta (Asteraceae). Structural elucidation was based on spectral analysis. It is the first report on eudesmanolides in members of the subgenus Calanticaria of Viguiera. In this work, the main isolated compound, the furanoheliangolide budlein A, besides its previously reported in vitro and in vivo anti-inflammatory activities, inhibited human neutrophil elastase release. The inhibition was at the concentration of (16.83 +/- 1.96) microM for formylated bacterial tripeptide (fMLP) stimulation and (11.84 +/- 1.62) microM for platelet aggregation factor (PAF) stimulation, being slightly less active than the reference drug parthenolide. The results are important to demonstrate the potential anti-inflammatory activities of sesquiterpene lactones and corroborate the previous studies using other targets.
Arakawa
Nilton S
NS
Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Laboratório de Farmacognosia, Universidade de São Paulo (USP), Av. do Café s/no., 14040-903, Ribeirão Preto, SP, Brazil.
Schorr
Karin
K
Ambrósio
Sérgio R
SR
Merfort
Irmgard
I
Da Costa
Fernando B
FB
D000893:Anti-Inflammatory Agents / Q000302:isolation & purification / Q000494:pharmacology*; D019659:Asteraceae / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D007783:Lactones / Q000302:isolation & purification / Q000494:pharmacology*; D019272:Leukocyte Elastase / Q000037:antagonists & inhibitors*; D009682:Magnetic Resonance Spectroscopy; D012717:Sesquiterpenes / Q000302:isolation & purification / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization
D000893:Anti-Inflammatory Agents; D004791:Enzyme Inhibitors; D007783:Lactones; D012717:Sesquiterpenes; D019272:Leukocyte Elastase