Inhibition of acute and chronic inflammatory responses by the hydroxybenzoquinonic derivative rapanone

• Published in: Planta medica Vol. 67; no. 9; p. 791
• Main Authors: Ospina, L F, Calle, J, Arteaga, L, Pinzón, R, Alcaraz, M J, Payá, M
• Format: Journal Article
• Language: English
• Published: Germany 01.12.2001
• Subjects: Animals; Anti-Inflammatory Agents, Non-Steroidal - therapeutic use; Antioxidants - therapeutic use; Benzoquinones - chemistry; Benzoquinones - pharmacology; Benzoquinones - therapeutic use; Cell Survival - drug effects; Cyclooxygenase 1; Cyclooxygenase 2; Female; Humans; Inflammation - drug therapy; Isoenzymes - metabolism; Lipid Peroxidation - drug effects; Membrane Proteins; Mice; Microsomes, Liver - drug effects; Mitochondria - drug effects; Myrsinaceae; Neutrophils - drug effects; Phytotherapy; Plant Extracts - chemistry; Plant Extracts - pharmacology; Plant Extracts - therapeutic use; Prostaglandin-Endoperoxide Synthases - metabolism; Rats
• ISSN: 0032-0943; 1439-0221
• DOI: 10.1055/s-2001-18839

Rapanone (2,5-dihydroxy-3-tridecyl-1,4-benzoquinone), a natural compound isolated from Myrsine guianensis growing in the Andean highlands of Colombia, was studied in different in vitro and in vivo models as a potential antioxidant and anti-inflammatory drug. Rapanone showed a mild anti-lipoperoxidative profile in rat liver microsomes and inhibited potently degranulation (IC(50) of 9.8 microM) and superoxide chemiluminescence (IC(50) of 3.0 microM) in human neutrophils. In addition, rapanone is a selective and potent human synovial PLA(2) inhibitor (IC(50) of 2.6 microM). In vivo experiments using the carrageenan paw oedema and the zymosan air pouch model in mice as well as the adjuvant arthritis model in rats have proved that rapanone is very efficient in controlling the inflammatory process by different administration routes.