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Topical anti-inflammatory activity of boropinic acid and of its natural and semi-synthetic derivatives
Boropinic acid (R=OCH3) is an isopentenyloxycinnamic acid isolated from the roots of Boronia pinnata Sm., an Australian shrub belonging to the family of Rutaceae . In a recent study we have shown that this natural compound exerts a significant in vitro inhibitory activity on soybean 5-lipoxygenase and, by means of molecular techniques, put in evidence its ability to strongly bind to the active site of this enzyme .
Basing on these findings, we verified the topical anti-inflammatory activity of boropinic acid and of its eight natural and semi-synthetic derivatives, resulting from the substitution of the methoxy group in position 8, following the environmental friendly route that we already reported . Each compound was evaluated for its ability to inhibit the Croton oil induced-ear oedema in mice , in comparison to equimolar doses of nordihydroguaiaretic acid, a known lipoxygenase inhibitor, and of the non steroidal anti-inflammatory drug indomethacin. Almost all the compounds (0.3µmol/cm2) provoked significant oedema inhibition (from 19 to 78%), comparable or higher than that of nordihydroguaiaretic acid (36% oedema inhibition) and of indomethacin (62% inhibition).
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