We have assayed the pharmacological properties of a flavonoid fraction obtained from the butanol extract of Cayaponia tayuya roots using two models of topical mouse ear oedema, paying special attention to its influence on the induction on pro-inflammatory enzymes and peptidic mediators.
The in vivo experiments involved both the acute oedema induced by a single application of TPA and the subchronic inflammation brought on by repeated applications of TPA. The effects on the induction of pro-inflammatory enzymes and peptidic mediators in RAW 264.7 macrophages were analyzed with the aid of Western blot analysis.
The extract was identified as a mixture of flavonoids in which vicenin-2, spinosin, isovitexin, and a mixture of swertisin and isoswertisin were found. In acute TPA-induced oedema in mouse ears, the flavonoid-enriched fraction (at a dose of 0.5 mg/ear) inhibited the oedema by 66 % (4.2 ± 0.6 mg vs. 12.3 ± 1.4 mg, P < 0.01) while in the subchronic model, the inhibition reached 37 % at a dose of 0.5 mg/ear × 7 applications (7.5 ± 0.6 mg vs. 11.9 ± 1.3 mg, P < 0.05). When assayed in vitro, the flavonoid showed no toxicity at 33.45 μg/mL on RAW 264.7 macrophages. Although the nitric oxide production in these cells was moderately reduced (42 % ) at 33.45 μg/mL, the flavonoid-enriched fraction had no effect on TNF-α production. In addition, at 22.30 μg/mL, the test sample inhibited both iNOS and COX-2 expression by 98 % and 49 % , respectively.
These results indicate that the anti-inflammatory activity of flavonoids from tayuya roots most likely stems from their inhibition of the induction of the enzymes COX-2 and iNOS.