hispidulin and Edema

Topics: Animals; Anti-Inflammatory Agents; Baccharis; Disease Models, Animal; Ear Diseases; Edema; Flavones; Male; Mice; Mice, Inbred ICR; Terpenes; Tetradecanoylphorbol Acetate

Three anti-inflammatory compounds: nepetin, jaceosidin and hispidulin have been isolated and identified from Eupatorium arnottianum Griseb. dichloromethane extract. Nepetin reduced the TPA mouse ear edema by 46.9% and jaceosidin by 23.2% (1mg/ear). Both compounds inhibited the NF kappaB induction by 91 and 77%, respectively. Furthermore phytochemical analysis of the ethanol extract has led to the identification of eriodictyol, hyperoside, rutin, caffeic and chlorogenic acids. All these compounds are reported for the first time in this species. The finding of topical antiinflammatory activity exerted by Eupatorium arnottianum extract and the identification of active principles could support the use of this plant for the treatment of inflammatory affections.

Topics: Animals; Anti-Inflammatory Agents; Caffeic Acids; Carrageenan; Cell Survival; Dose-Response Relationship, Drug; Ear, External; Edema; Eupatorium; Female; Flavanones; Flavones; Flavonoids; HeLa Cells; Humans; Jurkat Cells; Mice; Molecular Structure; Plant Extracts; Quercetin; Rats; Rats, Sprague-Dawley; Tetradecanoylphorbol Acetate

Six flavonoid derivatives were tested for their influence on Naja naja and human recombinant synovial phospholipase A2. They showed a selectivity for the last enzyme with IC50 = 14.3, 17.6, 12.2 and 28.2 microM for quercetagetin, kaempferol-3-O-galactoside, scutellarein and scutellarein-7-O-glucuronide, respectively, while reduced effects were observed for hispidulin and hibifolin. After topical application all the flavonoids inhibited 12-O-tetradecanoylphorbol-13-acetate-induced ear oedema in mice with a potency comparable to that of indomethacin and they were also able to inhibit carrageenan-induced mouse paw oedema at a dose of 150 mg/kg p.o. The blockade of the free hydroxyl at C-7 or C-6 reduced the anti-inflammatory activity and also the inhibitory effect on human recombinant synovial phospholipase A2. These results are in accordance with the notion that group II phospholipases A2 may play a role in experimental inflammation, although several mechanisms seems to be involved in the anti-inflammatory effect of this group of flavonoids.

Topics: Animals; Chromones; Edema; Flavanones; Flavones; Flavonoids; Galactosides; Humans; Inflammation; Kaempferols; Male; Mice; Phospholipases A; Phospholipases A2; Quercetin; Recombinant Proteins; Snakes; Tetradecanoylphorbol Acetate