Studying The Effects Of Some Oxadiazole Derivatives On Transaminases Activities in Serum and Tissue Homogenate of Hepatocellular Cancer Patients

Abstract

This study conducted to evaluate the effect of some oxadiazole derivatives 1-(4-ethoxy benzylidene amino)-4-(2-n- butyl thio-1,3,4-oxadiazole-5yl) benzene[I] and 1-(4-pentoxy benzylidene amino)-4-(2-n- butyl thio-1,3,4-oxadiazole-5yl) benzene[II], on the activities of alanine transaminase (ALT) and aspartate transaminase (AST) in serum and tissue's homogenate of hepatocellular cancer patients (HCC). The results revealed that compound I and compound II showed activation effect on ALT enzyme in serum of HCC patients, while they were competitive inhibitors on ALT enzyme in the tissue's homogenate of the same patients with Vmax values (105.26)U/L and (102.04)U/L respectively, and Km values (38.76 and 100)mmol/L and (38.46 and 105.26)mmol/L for compounds I and II for uninhibited and inhibited enzyme respectively. The effect of compound I on SAST enzyme was found to be noncompetitive inhibitor with Vmax values (142.86 and 105.26)U/L for uninhibited and inhibited enzyme and Km value (33.33)mmol/L, while it showed activitory effect on the same enzyme in tissue's homogenate of HCC patients. Compound II was found to be competitive inhibitor on SAST enzyme with Vmax value (121.95)U/L and Km values (66.67 and 125)mmol/L for uninhibited and inhibited enzyme, and it was noncompetitive inhibitor on AST in tissue's homogenate of HCC patients with Vmax values (138.9 and 105.26)U/L for uninhibited and inhibited enzyme and Km value (33.9)mmol/L. In conclusion oxadiazole derivatives I and II showed inhibitory and activatory effects on ALP and AST enzymes in serum and tissue's homogenate of HCC patients.