CYP3A4酶对土茯苓黄酮类成分代谢的影响

Effect of CYP3A4 enzyme on the metabolism of flavonoids in Smilax glabra

以土茯苓6种黄酮类成分为底物,研究了不同孵育时间、不同CYP3A4酶浓度对6种成分代谢的影响。通过土茯苓6种黄酮类成分的酶促动力学,得到米氏常数(Km)、最大反应速度(Vmax)和代谢清除率(Clint)。结果表明,以表儿茶素、新落新妇苷、落新妇苷、异落新妇苷、黄杞苷、白藜芦醇为底物时,Km分别为1.39,1.38,2.37,1.59,0.79,2.01μmol/L;Vmax分别为0.02,0.01,0.02,0.02,0.01,0.02μmol/(L·min);Clint分别为(1.14,0.96,0.90,0.99,1.42,0.97)×10^-2min^-1。

Six flavonoids of Smilax glabra were used as substrates to study the effects of different incubation time and different concentrations of CYP3 A4 on the metabolism of six components.The Michaelis constant(Km),the maximum reaction rate(Vmax) and the metabolic clearance rate (Clint) were obtained from the enzymatic kinetics of six flavonoids from Smilax glabra.The results showed that Kmwere 1.39,1.38,2.37,1.59,0.79, 2.01μmol/L,Vmax were 0.02,0.01,0.02,0.02,0.01,0.02 μmol/(L·min),and Clintwere(1.14,0.96,0.90, 0.99,1.42,0.97)×10^-2 min^-1 for epicatechin,neoastilbin,astilbin,isoastilbin,engeletin and resveratrol as substrates,respectively.