Topical anti-inflammatory activity of flavonoids and a new xanthone from Santolina insularis.
Bioactivity-guided fractionation of the methanol extract from the leaves of Santolina insularis led to the isolation of one new xanthone, (E)-3-(6-[(E)-3-hydroxy-3-oxo-1-propenyl]-9-oxo-9H-xanthen-2-yl)-2-propenoic acid, together with six known flavonoids: hispidulin, nepetin, cirsimaritin, rhamnocitrin, luteolin and luteolin 7-O-beta-D-glucopyranoside. The structures were elucidated by means of 1D-, 2D-NMR spectroscopy and mass spectrometry. The topical anti-inflammatory activity of all isolated compounds and extracts was investigated employing the croton oil-induced dermatitis in mouse ear. The most active compound, luteolin, showed an ID50 of 0.3 micromol/cm(2) and prevented ear oedema more effectively than an equimolar dose of indomethacin within 24 h.
Cottiglia
Filippo
F
Dipartimento Farmaco Chimico Tecnologico, Facoltà di Farmacia, Università di Cagliari, Via Ospedale 72, 09124 Cagliari, Italy. cottiglf@unica.it
Casu
Laura
L
Bonsignore
Leonardo
L
Casu
Mariano
M
Floris
Costantino
C
Sosa
Silvio
S
Altinier
Gianmario
G
Della Loggia
Roberto
R
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D019659:Asteraceae / Q000737:chemistry*; D004487:Edema / Q000188:drug therapy; D005419:Flavonoids / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D007213:Indomethacin / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D018515:Plant Leaves / Q000737:chemistry; D044004:Xanthones / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005419:Flavonoids; D044004:Xanthones; D007213:Indomethacin