In Vitro Effect of Some Chemical Compositions in Wuzhuyu on Berberine Metabolism in Rat Liver Microsomes

OBJECTIVE To investigate the metabolic kinetics of berberine in rat liver microsome and the effects of some chemical compositions in Wuzhuyu on berberine metabolism.METHODS By developing an in vitro system of rat liver microsomes,the factors including incubation time,microsomal protein concentration and original concentration of berberine were surveyed and the effect on berberine metabolism rate from diverse concentration of evodiamine,rutaecarpine and evodin was investigated.RESULTS Berberine was metabolized in rat liver microsomes.Berberine metabolism showed time(0-60 min) and microsomes protein concentration(0.5-2.0 mg·mL-1) dependented characteristics.The Michaelis-Menten parameters of Km and Vmax in rat microsomes were initially estimated by analyzing Lineweave-Brurk plot.The Km and Vmax of berberine were(2.41±0.617) mg·mL-1 and(6.88 ±1.89) ng·mg-1·min-1.All those three components from Wuzhuyu significantly inhibited the metabolism of berberine,moreover the inhibition effect of rutaecarpine and evodin were higher than that of evodiamine(P0.001).CONCLUSION Berberine was rapidly metabolized in rat liver microsomes.Chemical compositions in Wuzhuyu can significantly inhibit the metabolism of berberine.This might be one significant mechanism of Huanglian and Wuzhuyu compatibility.