Inhibitory effects of Cefazolin and Cefodizime on the activity of mushroom tyrosinase

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, the effects of Cefazolin and Cefodizime on the activity of mushroom tyrosniase have been studied. The results showed that the Cephalosporin antibacterial drugs (Cefazolin and Cefodizime) could inhibit both monophenolase activity and diphenolase activity of the enzyme. For the monophenolase activity, Both Cefazolin and Cefodizime could lengthen the lag time and decrease the steady-state activities, and the IC 50 values were estimated as 7.0 mM and 0.13 mM for monophenolase activity, respectively. For the diphenolase activity, the inhibitory capacity of Cefodizime was obviously stronger than that of Cefazolin, and the IC 50 values were estimated as 0.02 mM and 0.21 mM, respectively. Kinetic analyses showed that inhibition by both compounds was reversible and their mechanisms were competitive and mixed-type, respectively. Their inhibition constants were also determined and compared. The research may offer a lead for designing and synthesizing novel and effective tyrosinase inhibitors and also under the application field of Cephalosporins.

Discrimination between Alternative Substrates and Inhibitors of Tyrosinase

“…When an inhibitor is added to the reaction medium, the reaction rate of the enzyme decreases and so does the rate of accumulation of o -diphenol in the medium, and this means an increase in the lag period and the steady state is reached later, which therefore entails a longer measuring period. This has not usually been taken into account when studying the inhibition of the monophenolase activity, meaning that inexact values have been obtained for many studied inhibitors. − …”

Synthesis and Antityrosinase Mechanism of Benzaldehyde Thiosemicarbazones: Novel Tyrosinase Inhibitors

“…In our pervious research, a great many tyrosinase inhibitors were screened from natural materials and synthetic methods. We have reported some tyrosinase inhibitors, such as hinokitiol; fatty acids; 2-phenylethanol, 2-phenylacetaldehyde, and 2-phenylacetic acid; α-cyano-4-hydroxycinnamic acid; cefazolin and cefodizime; methyl trans -cinnamate; trans -cinnamaldehyde thiosemicarbazone; and alkyl-3,4-dihydrobenzoates . The inhibitory effect of thiosemicarbazone derivatives on tyrosinase exhibited potent inhibitory activity, the reason being that the sulfur atom of the thiosemicarbazide moiety was able to chelate the two copper ions in the active site of tyrosinase .…”

Inhibitory Effects of Fatty Acids on the Activity of Mushroom Tyrosinase

“…It is well-known that tyrosinase can be inhibited by aromatic aldehydes [7], aromatic acids [8], tropolone [9], and kojic acid [10], α-cyano-4-hydroxycinnamic acid [11], 4-chlorosalicylic acid [12], phloridzin dihydrate [13], cefazolin and cefodizime [14], azelaic acid [15], and so on. Some inhibitors of tyrosinase were also found in the antimicrobial activities [16,17].…”