Brasil Edikarlos M, Canavieira Luciana M, Cardoso Érica T C, Silva Edilene O, Lameira Jerônimo, Nascimento José L M, Eifler-Lima Vera L, Macchi Barbarella M, Sriram Dharmarajan, Bernhardt Paul V, Silva José Rogério Araújo, Williams Craig M, Alves Cláudio N
Laboratório de Planejamento e Desenvolvimento de Fármacos, Instituto de Ciências Exatas e Naturais, Universidade Federal do Pará, Belém, PA, Brazil.
School of Chemistry and Molecular Biosciences, University of Queensland, Brisbane, Queensland, Australia.
Chem Biol Drug Des. 2017 Nov;90(5):804-810. doi: 10.1111/cbdd.13001. Epub 2017 Jun 12.
Inhibition of mushroom tyrosinase was observed with synthetic dihydropyrano[3,2-b]chromenediones. Among them, DHPC04 displayed the most potent tyrosinase inhibitory activity with a K value of 4 μm, comparable to the reference standard inhibitor kojic acid. A kinetic study suggested that these synthetic heterocyclic compounds behave as competitive inhibitors for the L-DOPA binding site of the enzyme. Furthermore, molecular modeling provided important insight into the mechanism of binding interactions with the tyrosinase copper active site.
合成的二氢吡喃并[3,2 - b]色烯二酮对蘑菇酪氨酸酶具有抑制作用。其中，DHPC04表现出最强的酪氨酸酶抑制活性，K值为4μm，与参考标准抑制剂曲酸相当。动力学研究表明，这些合成杂环化合物对该酶的L - 多巴结合位点起竞争性抑制剂的作用。此外，分子模拟为与酪氨酸酶铜活性位点的结合相互作用机制提供了重要见解。
