Tyrosinase inhibition studies of diterpenoid alkaloids and their derivatives: structure–activity relationships
M. N. Sultankhodzhaeva S. Yunusov Institute of the Chemistry of Plant Substances , Academy of Sciences Republic of Uzbekistan , Tashkent, UzbekistanMahmud Tareq Hassan Khanb H.E.J. Research Institute of Chemistry , International Center for Chemical Sciences, University of Karachi , Karachi-75270, PakistanMahera Moinb H.E.J. Research Institute of Chemistry , International Center for Chemical Sciences, University of Karachi , Karachi-75270, PakistanM. Iqbal Choudharyb H.E.J. Research Institute of Chemistry , International Center for Chemical Sciences, University of Karachi , Karachi-75270, PakistanAtta‐ur Rahmanb H.E.J. Research Institute of Chemistry , International Center for Chemical Sciences, University of Karachi , Karachi-75270, Pakistan
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Abstract
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).
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