In vivo and in vitro anti-inflammatory activities of alpha-linolenic acid isolated from Actinidia polygama fruits.
The fruit of Actinidia polygama (AP) has long been used as a folk medicine in Korea for the treatment of pain, rheumatoid arthritis and inflammation. In the present study, bioassay-guided fractionation of AP led to the separation and identification of a polyunsaturated fatty acid, alpha-linolenic acid (ALA), which was found to show anti-inflammatory activity. The anti-inflammatory effects of ALA, using acetic acid or carrageenan-induced inflammation models, were investi gated in mice or rats, respectively. ALA significantly inhibited the acetic acid-induced vascular permeability in a dose dependent manner (34.2 and 37.7% inhibition at doses of 5 and 10 mg/ kg, respectively). ALA also significantly reduced a rat paw edema induced by a single treatment of carrageenan. To investigate the mechanism of the anti-inflammatory action of ALA, the effects of ALA on lipopolysaccharide (LPS)-induced responses in the murine mac rophages cell line, RAW 264.7, were examined. Exposure of LPS-stimulated cells to ALA inhibited the accumulation of nitrite and prostaglandin E2 (PGE2) in the culture medium. Consistent with these observations, the protein and mRNA expression levels of iNOS and COX-2 enzyme were markedly inhibited by ALA in a dose dependent manner. These results suggest that the anti-inflammatory activity of ALA might be due to the suppression of the expressions of iNOS and COX-2 mRNA.
Department of Pharmacology and Clinical Pharmacy, College of Pharmacy, Kyung Hee University, Dongdaemun-gu, Seoul 130-701, Korea.
Jie
J
Ren
Eun Jung
EJ
Han
Sung Hyun
SH
Chung
D019342:Acetic Acid; D029042:Actinidia / Q000737:chemistry*; D000622:Aminolevulinic Acid / Q000378:metabolism; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000302:isolation & purification* / Q000494:pharmacology*; D015153:Blotting, Western; D002199:Capillary Permeability / Q000187:drug effects; D002351:Carrageenan; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D051546:Cyclooxygenase 2 / Q000378:metabolism; D052246:Cyclooxygenase 2 Inhibitors / Q000494:pharmacology; D015232:Dinoprostone / Q000032:analysis / Q000096:biosynthesis; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005638:Fruit / Q000737:chemistry*; D006586:Hexanes; D007202:Indicators and Reagents; D008070:Lipopolysaccharides / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D052247:Nitric Oxide Synthase Type II / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D010936:Plant Extracts / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D020133:Reverse Transcriptase Polymerase Chain Reaction; D012997:Solvents; D013778:Tetrazolium Salts; D013844:Thiazoles; D017962:alpha-Linolenic Acid / Q000302:isolation & purification* / Q000494:pharmacology*
D000893:Anti-Inflammatory Agents; D052246:Cyclooxygenase 2 Inhibitors; D004791:Enzyme Inhibitors; D006586:Hexanes; D007202:Indicators and Reagents; D008070:Lipopolysaccharides; D010936:Plant Extracts; D012997:Solvents; D013778:Tetrazolium Salts; D013844:Thiazoles; D017962:alpha-Linolenic Acid; D000622:Aminolevulinic Acid; D002351:Carrageenan; D052247:Nitric Oxide Synthase Type II; D051546:Cyclooxygenase 2; C022616:thiazolyl blue; D015232:Dinoprostone; D019342:Acetic Acid