Anti-inflammatory effects of a bioavailable compound, Artepillin C, in Brazilian propolis

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• 作者：Niraldo Paulino ; Sheila Rago Lemos Abreu ; Yoshihiro Uto ; Daisuke Koyama ; Hideko Nagasawa ; Hitoshi Hori ; Verena M. Dirsch ; Angelika M. Vollmar ; Amarilis Scremin ; Walter A. Bretz
• 关键词：Artepillin C ; Propolis ; Inflammation ; NF-κ ; B ; Prostaglandin E₂ ; Nitric oxide
• 刊名：European Journal of Pharmacology
• 出版年：2008
• 出版时间：10 June 2008
• 年：2008
• 卷：587
• 期：1-3
• 页码：296-301
• 全文大小：409 K

文摘

Artepillin C is the major compound in the Brazilian green propolis from Baccharis dracunculifolia. Our aim in this study was to investigate the anti-inflammatory effects, absorption, and bioavailability of Artepillin C in mice. The animals used were male Swiss mice subjected to: paw oedema by carrageenan (300 ;c;g/paw), carrageenan-induced peritonitis, and prostaglandin E₂ determination. We also measured in vitro nitric oxide production by RAW 264.7 cells and NF-κB activity in HEK 293 cells. Finally, we measured the absorption and bioavailability of Artepillin C in plasma from mice by means of GC-MS after a single oral dose (10 mg/kg). In vivo, Artepillin C produced a maximal inhibition of 38 % after 360 min on paw oedema. Artepillin C also decreased the number of neutrophils during peritonitis (IC₅₀: 0.9 (0.5–1.4) mg/kg). Treatment with Artepillin C decreased prostaglandin E₂ by 29 ± 3 % and 58 ± 5 % at 1 and 10 mg/kg, respectively, with a mean ID₅₀ of 8.5 (8.0–8.7)mg/kg). Similarly, in in vitro models, Artepillin C (3, 10, or 100 ;c;M) decreased nitric oxide production by RAW 264.7 cells with a mean IC₅₀ of 8.5 (7.8–9.2) ;c;M. In HEK 293 cells, Artepillin C reduced NF-κB activity with a mean IC₅₀ of 26 (22–30) ;c;g/ml), suggesting anti-inflammatory activity, particularly during acute inflammation. Lastly, Artepillin C was absorbed after an oral dose (10 mg/kg) with maximal peaks found at 1 h (22 ;c;g/ml). Collectively, Artepillin C showed anti-inflammatory effects mediated, at least in part, by prostaglandin E₂ and nitric oxide inhibition through NF-κB modulation, and exhibited bioavailability by oral administration.