文摘
Human CYP2J2 isoform, the only member of the human CYP2J subfamily, is also over-expressed in human liver carcinoma tissues and hepatocarcinoma cells, and promotes tumor growth and proliferation. 4-(p-Toluenesulfonylamide)-4-hydroxychalcone (TSAHC) is a synthetic sulfonylamino chalcone compound, which has anti-cancer effect. Inhibitory potential of a promising anti-cancer agent TSAHC against CYP2J2 activity was evaluated using human liver microsomes. TSAHC inhibited CYP2J2-mediated astemizole O-demethylation activity with K i value of 2.03±0.40 μM in a competitive mode, suggesting that TSAHC is a potential candidate for further evaluation for its CYP2J2 targeting anti-cancer activities. Studies are presently underway to estimate TSAHC as potential therapeutic agent for cancer.