Title :
Relationships between Inhibition Constants, Types of Inhibition and IC50: Calculation and Comparison on IC50 of Two Model Tyrosinase Inhibitors
Author :
Mao, Hairong ; Xie, Jiangang ; Zhang, Qimeng ; Lü, Xinyu ; Li, Shubai
Author_Institution :
Dept. of Chem., Zhengzhou Teachers Coll., Zhengzhou, China
Abstract :
Calculating methods for inhibitor concentration (IC50) leading to 50% activity lost (for diphenolase activity) of a novel parabolic competitive inhibitor (the trifluoromethyl-containing 1,2,3-triazole, TF-TA) and a novel mixed inhibitor ([E]-4-(1-imidazoylmethyl) cinnamic acid (ozagrel) were derived on the basis of kinetics of tyrosinase inhibition. These methods were applied to calculate IC50 values of the two tyrosinase inhibiting compounds. The experimental IC50 values of TF-TA and ozagrel were 41.9 μM and 3.45 mM, respectively. Moreover, the calculated IC50 value of TF-TA and ozagrel were 82.8 μM and 3.15 mM, respectively. The calculation result of ozagrel is closer to experimental data.
Keywords :
biochemistry; biotechnology; enzymes; inhibitors; IC50; TF-TA; [E]-4-(1-imidazoylmethyl) cinnamic acid; diphenolase activity; inhibition constants; inhibitor concentration; mixed inhibitor; ozagrel; parabolic competitive inhibitor; trifluoromethyl-containing 1,2,3-triazole; tyrosinase inhibitors; Biochemistry; Biological system modeling; Chemical engineering; Chemical technology; Chemistry; Drugs; Inhibitors; Kinetic theory; Particle measurements; Pharmaceutical technology;
Conference_Titel :
Bioinformatics and Biomedical Engineering (iCBBE), 2010 4th International Conference on
Conference_Location :
Chengdu
Print_ISBN :
978-1-4244-4712-1
Electronic_ISBN :
2151-7614
DOI :
10.1109/ICBBE.2010.5515848