Relative inhibitory activity of berberine-type alkaloids against 12-O-tetradecanoylphorbol-13-acetate-induced inflammation in mice.

Forty eight derivatives of berberine-type alkaloids were examined for their inhibition activity against the induction of edema on mouse ear by application of 12-O-tetradecanoylphorbol-13-acetate (TPA). Berberine had an inhibitory effect against TPA-induced ear edema at a grade corresponding to those of quercetin, caffeine and cepharanthine. Berberine derivatives had stronger inhibitory activity than palmatine derivatives. 9-N,N-Diphenylcarbamoyl derivatives of both 9-demethylberberine and 9-demethylpalmatine had rather strong activity. These inhibitory activities are about ten times the activity of the respective mother compounds. Furthermore, 9-N-monophenylcarbamoyl derivatives and N,N-diphenylcarbamoyl chloride are found to have no effect.