Anti-inflammatory Activity of Pectolinarigenin and Pectolinarin Isolated from Cirsium chanroenicum(Pharmacology)

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概要

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• In order to identify the active anti-inflammatory ingredient(s) in Cirsium chanroenicum (Compositae), its methanol extract and several solvent fractions were prepared; the methanol extract and the ethylacetate fraction inhibited cyclooxygenase-2 (COX-2)-mediated prostaglandin E_2 (PGE_2) and 5-lipoxygenase (5-LOX)-mediated leukotriene (LT) production in lipopolysaccharide-treated RAW 264.7 cells and A23187-treated rat basophilic leukemia (RBL-1) cells, respectively. Further bioactivity-guided fractionation of the ethylacetate fraction using column chromatography led to the isolation of pectolinarigenin (5,7-dihydroxy-4',6-dimethoxyflavone), along with pectolinarin [pectolinarigenin 7-rhamnosyl-(1→6)-glucosidel]. Pectolinarigenin strongly inhibited COX-2-mediated PGE_2 and 5-LOX-mediated LT production at>1μM, indicating that it is a dual inhibitor of COX-2/5-LOX. However, pectolinarigenin did not affect COX-2 expression or nuclear transcription factor (NF-κB) activation. In addition, in vivo studies demonstrated that oral administration of these two compounds at 20-100mg/kg resulted in similar inhibitory activities against several animal models of inflammation/allergy: arachidonic acid-induced mouse ear edema, carrageenan-induced mouse paw edema and passive cutaneous anaphylaxis. All of these results suggest that pectolinarigenin and pectolinarin possess anti-inflammatory activity and that they may inhibit eicosanoid formation in inflammatory lesions. These activities certainly contribute to the anti-inflammatory mechanism of C. chanroenicum.

• 2008-11-01

著者

• CHANG Hyeun

  College of Pharmacy, Yeungnam University

• BAE KiHwan

  College of Pharmacy, Chungnam National University

• Kim Hyun

  College Of Pharmacy Kangwon National University

• SON Kun

  Department of Food Nutrition, Andong National University

• KANG Sam

  College of Pharmacy, Seoul National University

• LIM Hyun

  College of Pharmacy, Kangwon National University

• BAE Ki

  College of Pharmacy, Chungnam National University

• Bae Ki

  College Of Pharmacy Chungnam National University

• Bae Kihwan

  韓国

• Son K

  Department Food & Nutriton Andong National University

• Chang Hyeun

  College Of Pharmacy Yeungnam University

• Kang Sam

  韓国

• Kang Sam

  Natural Products Research Institute And College Of Pharmacy Seoul National University

• Kang Sam

  College Of Pharmacy Seoul National University

• Bae Kihwan

  College Of Pharmacy Chungnam National University

• Chang Hyeun

  Coll. Of Pharmacy Yeungnam Univ.

• Son Kun

  Department Food & Nutriton Andong National University

• Kang S

  Natural Products Research Institute And College Of Pharmacy Seoul National University

• Lim Hyun

  College Of Pharmacy Kangwon National University

• Chang H

  College Of Pharmacy Yeungnam University

• Kim Hyun

  College Of Pharmacy And Research Institute Of Drug Development Chonnam National University

• Bae K

  College Of Pharmacy Chungnam National University

• Kim Hyun

  College Of Electrical & Computer Engineering Chungbuk National University

• Lim Hyun

  Coll. Of Pharmacy Kangwon National Univ. Kor

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