Inhibitory effects of cefotaxime on the activity of mushroom tyrosinase

Journal of Bioscience and Bioengineering
Yong-Hua HuQing-Xi Chen

Abstract

Tyrosinase (EC 1.14.18.1) catalyzes both the hydroxylation of tyrosine into o-diphenols and the oxidation of o-diphenols into o-quinones that form brown or black pigments. In the present paper, cefotaxime, a cephalosporin antibacterial drug, was tested as an inhibitor of tyrosinase. The results show that cefotaxime inhibits both the monophenolase and diphenolase activities of tyrosinase. For the monophenolase activity, cefotaxime increased the lag time and decreased the steady-state activity with an IC50 of 3.2 mM. For the diphenolase activity, the inhibition by cefotaxime is reversible and mix-I type with an IC50 of 0.14 mM. The inhibition constants (K(I) and K(IS)) were determined to be 0.14 and 0.36 mM, respectively. The molecular mechanism of inhibition of tyrosinase by cefotaxime was determined by fluorescence quenching and molecular docking. The results demonstrated that cefotaxime was a static quencher of tyrosinase and that cefotaxime could dock favorably in the active site of tyrosinase. This research may offer a lead for designing and synthesizing novel and effective tyrosinase inhibitors in the future.

References

Jan 27, 2004·Bioorganic & Medicinal Chemistry Letters·Ken-ichi NiheiIsao Kubo
May 14, 2004·The Journal of Investigative Dermatology·Behrooz KasraeeJean-Hilaire Saurat
Feb 18, 2005·Biochimica Et Biophysica Acta·Ying LiXingguo Chen
Oct 3, 2008·Journal of Enzyme Inhibition and Medicinal Chemistry·Jiang-Xing ZhuangQing-Xi Chen
Nov 11, 2010·Journal of Agricultural and Food Chemistry·Zhi-Cong LiQing-Xi Chen
Jan 19, 2012·Journal of Agricultural and Food Chemistry·Liang-Hua ChenQing-Xi Chen
Aug 21, 2013·Journal of Bioscience and Bioengineering·Yong-Hua HuQing-Xi Chen
Jan 16, 2014·Journal of the Science of Food and Agriculture·Elena IoniţăGabriela Bahrim
Apr 2, 2014·Bioinorganic Chemistry and Applications·Aurora ReissCezar Ionuţ Spînu
Apr 8, 2014·Bioorganic & Medicinal Chemistry·Chin-Feng ChanMing-Jen Chen
Jun 19, 2014·Journal of Agricultural and Food Chemistry·Wei-Ming ChaiQing-Xi Chen
Sep 27, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Chin-Feng ChanYung-Sheng Lin

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