ABSTRACT
Objective To investigate the metabolic profile of chrysin in SULT1A3 and human small intestine S9.Methods After incubation of chrysin using in vitro SULT1A3 and human small intestine S9 system, high-performance liquid chromatography was utilized to determine the sulfates of chrysin.Mass spectrum(MS) were employed to elucidate the structures of metabolite.Results In the SULT1A3 with PAPS, Km were (3.06 ±1.04) and (0.41±0.06) μM, Vmax were (12.13 ±1.30) and (6.72 ±1.61) nmol/(min· mg), Vmax/Km were 3.96 and 16.39 mL/(min· mg), respectively.In the human small intestine S9 with PAPS, Km were (1.92 ±0.35) and (0.01 ±0.00) μM, Vmax were (0.52 ±0.02) and (0.08 ± 0.02) nmol/(min· mg), Vmax/Km were 0.27 and 8.00 mL/(min· mg).The metabolic behavior of chrysin in SULT1A3 and human small intestine S9 both were followed biphasic kinetics.The sulfation of chrysin in SULT1A3 showed a significant correlation with that in human small intestine S9(R2 =0.985).Conclusion The result indicates that SULT1A3 is the major enzyme to the metabolism of chrysin, human small intestine may be the main metabolic organs of chrysin.
ABSTRACT
Purpose To compare pharmacokineics of puerarin and crude extract in rats.Methods Rats received 500 mg/kg puerarin and puerarin crude extract by oral administration respectively.Hydroxybenzoic acid was selected as internal standard and the plasma concentration of the puerarin and crude extract was analyzed by HPLC.The pharmacokinetics parameters were calculated with DAS2.0.Results The pharmacokinetics of puerarin and puerarin crude extract was both best fitted with two-compartment models in rats after oral administration,and the pharmacokinetics main parameters of the two formulations were different:the AUC_(0-t) and C_(max) of puerarin were much greater than those of puerarin crude extract,but T_(max),t_(1/(2z)),CL/F and V_z/F were much lesser than those of puerarin crude extract.Conclusion The complex components in pueraria crude extract can affect the pharmacokinetics of puerarin in rat in vivo.