Watanabe, Hiroaki; Yamaori, Satoshi; Kamijo, Shinobu; Aikawa, Kaori; Ohmori, Shigeru published the artcile< In vitro inhibitory effects of sesamin on CYP4F2 activity>, Formula: C11H8N2O3S2, the main research area is microsome CYP4F2 enzyme inhibition sesamin NADPH; CYP4F2; inactivation; inhibition; sesamin.
Sesamin is a major lignan in sesame seeds, and a recent meta-anal. of controlled trials indicated that sesamin intake decreases blood pressure. The antihypertensive effect of sesamin has been suggested to be due to sesamin-mediated suppression of 20-hydroxyeicosatetraenoic acid production catalyzed by CYP4F2. However, the detailed mechanism underlying inhibition of CYP4F2 function by sesamin remains unclear. In this study, the effects of sesamin on catalytic activity of CYP4F2 were investigated in vitro. Sesamin inhibited luciferin-4F2/3 O-dealkylase activity of recombinant human CYP4F2 with an IC50 value of 0.381μM. When preincubated in the presence of reduced NADP (NADPH) for 20 min, sesamin potentiated the inhibition of CYP4F2 activity. Moreover, kinetic anal. of the inactivation revealed that sesamin showed a preincubation time- and concentration-dependent inhibition of CYP4F2 activity yielding a maximal inactivation rate constant (kinact) value of 0.354 min-1 and half-maximal inhibitory concentration (KI) value of 1.12μM. The inactivation of CYP4F2 by sesamin required NADPH. These results indicated that sesamin is a mechanism-based inactivator of human CYP4F2.
Biological & Pharmaceutical Bulletin published new progress about Enzyme inhibition kinetics. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Formula: C11H8N2O3S2.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica