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代表性论文

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Inhibitory kinetics of DABT and DABPT as novel tyrosinase inhibitors

发布时间:2014-01-01

Mei-Hua Yang, Chih-Min Chen, Yong-Hua Hu,

Cheng-Yi Zheng, Zhi-Cong Li, Lian-Lian Ni, Li Sun, Qing-Xi Chen.Journal

of Bioscience and Bioengineering, 2013. 115: 514-517.

4-Dimethylaminobenzaldehyde-thiosemicarbazone (DABT) and

4-dimethylaminobenzaldehyde-N-phenyl-thiosemicarbazone (DABPT) were synthesized

and established by1H and13C NMR and mass spectrum. Both

compounds wereevaluated for their inhibition activities on mushroom tyrosinase

and their anti-tyrosinase kinetics was investigated. Theresults 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 mM and 1.78 mM as their IC50 values respectively. Theinhibitory

effects of diphenolase activity exhibited sharp in a dose-dependent manner and

their IC50 values were estimatedas 2.01 mM and 0.80 mM, respectively. Kinetic

analysis showed that their inhibition mechanism was reversible. Theinhibition

type of DABT was mix-type with inhibition constants KI [ 1.77 mM and KIS [ 6.49

mM, while that of DABPTdisplays non-competitive with the inhibition constant KI

[ 0.77 mM].

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