Inhibitory kinetics of DABT and DABPT as novel tyrosinase inhibitors(ENZYMOLOGY, PROTEIN ENGINEERING, AND ENZYME TECHNOLOGY)

概要

論文の詳細を見る
4-Dimethylaminobenzaldehyde-thiosemicarbazone (DABT) and 4-dimethylaminobenzaldehyde-N-phenyl-thiosemicarbazone (DABPT) were synthesized and established by ^1H and ^<13>C NMR and mass spectrum. Both compounds were evaluated for their inhibition activities on mushroom tyrosinase and their anti-tyrosinase kinetics was investigated. The results showed that both compounds exhibited significant inhibitory effects on activity of monophenolase and diphenolase; DABT and DABPT decreased the steady-state rate with 1.54 μM and 1.78 μM as their IC_<50> values respectively. The inhibitory effects of diphenolase activity exhibited sharp in a dose-dependent manner and their IC_<50> values were estimated as 2.01 μM and 0.80 μM, respectively. Kinetic analysis showed that their inhibition mechanism was reversible. The inhibition type of DABT was mix-type with inhibition constants K_I = 1.77 μM and K_<IS> = 6.49 μM, while that of DABPT displays non-competitive with the inhibition constant K_I = 0.77 μM.
2013-05-00