Anti-inflammatory activity of flavonoids from Cayaponia tayuya roots.
BACKGROUND
Taiuiá or tayuya (Cayaponia tayuya, Cucurbitaceae) is a climbing, lignified plant with a large swollen root that has traditionally been used as an anti-inflammatory and anti-rheumatic agent in the folk medicine of Brazil, Peru, and Colombia.


OBJECTIVE
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.


METHODS
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.


RESULTS
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 0.5mg/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 0.5mg/ear x 7 applications (7.5+/-0.6 mg vs. 11.9+/-1.3mg, P<0.05). When assayed in vitro, the flavonoid showed no toxicity at 33.45 microg/mL on RAW 264.7 macrophages. Although the nitric oxide production in these cells was moderately reduced (42%) at 33.45 microg/mL, the flavonoid-enriched fraction had no effect on TNF-alpha production. In addition, at 22.30 microg/mL, the test sample inhibited both iNOS and COX-2 expression by 98% and 49%, respectively.


CONCLUSIONS
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.
Aquila
Silvia
S
Departament de Farmacologia, Facultat de Farmàcia, Universitat de València, Spain.
Giner
Rosa M
RM
Recio
María C
MC
Spegazzini
Etile D
ED
Ríos
José Luis
JL
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000302:isolation & purification / Q000494:pharmacology*; D001938:Brazil; D002460:Cell Line; D003105:Colombia; D019662:Cucurbitaceae / Q000737:chemistry*; D051546:Cyclooxygenase 2 / Q000187:drug effects / Q000378:metabolism; D004195:Disease Models, Animal; D005260:Female; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology*; D007249:Inflammation / Q000188:drug therapy / Q000503:physiopathology; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D008519:Medicine, Traditional; D051379:Mice; D052247:Nitric Oxide Synthase Type II / Q000187:drug effects / Q000378:metabolism; D010568:Peru; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D018517:Plant Roots
D000893:Anti-Inflammatory Agents; D005419:Flavonoids; D010936:Plant Extracts; D052247:Nitric Oxide Synthase Type II; D051546:Cyclooxygenase 2