Tyrosinase inhibition studies of diterpenoid alkaloids and their derivatives: structure-activity relationships

In the present article, tyrosinase inhibition studies on fifteen diterpenoid alkaloids, with lycoctonine skeleton, and their semisynthetic derivatives 1-15 and six napelline-type compounds 16-21 are discussed. Their structure-activity relationship for tyrosinase inhibition is also discussed. These activities were compared with two referenced tyrosinase inhibitors, kojic acid and L-mimosine. The study showed that lappaconitine HBr (1) is the most potent member of the series (IC50 = 13.30 microM).