Study On Antioxidation And Pharmacokinetics Of Flavonoids From Galium Verum L.

Objective:The oxidative damage model of rats was prepared by Dgalactose.To study the effect of FGVL on oxidative damage in rats induced by D-galactose and explore the antioxidative activity of total flavonoids in vivo.The increasing percentage of GSH-PX activity was taken as evaluation index of pharmacology effect.Pharmacokinetics parameters of total flavonoids from Galium Verum L.in rats were determined by pharmacology effect method.Methods:(1)Healthy male SD rats were randomly divided into the normal blank group,the control group,vitamin E positive control group and FGLV the low,medium and high dose groups.In addition to the normal group,the other five groups of rats were injected with D-galactose,once a day for 8 weeks.In addition to the control group,the other four groups were treated with vitamin E,low,medium,and high doses of FGLV in the gavage.At the beginning of the model administration,the weight change of the rats was recorded every week.The blood was taken after the last administration and the heart,kidney,spleen,liver and brain were removed and weighed.Meanwhile,the indexes of antioxidant in blood,liver and brain were detected:T-SOD,MDA,and GSH-Px.(2)The increasing percentage of GSH-PX activity was taken as evaluation index of pharmacology effect.The time-response curve and the time-biological inventory curve were plotted using the pharmacodynamics and efficacy method to calculate the main pharmacokinetic parameters.Results:D-galactose induced oxidative damage of rats showed poor general condition,slow response,sparse hair loss,frequent accumulation and increased reactive oxygen species and lipid peroxides,and decreased antioxidant capacity.After giving the FGLV,the general state of the rats in each dose group improved,the action was rapid,and the coat was gloss.There was no significant difference in weight between rats in each group(P>0.05),the weight of the rats was on the rise.The T-SOD and GSH-Px of the serum and liver tissues and the T-SOD activity of the brain tissue are elevated in varying degrees.The content of MDA in serum and liver and brain tissue was reduced.Low,medium and high-dose different doses of FGLV were orally administered in rats.It was best fitted to two compartment model.The main pharmacokinetic parameters obtained:t1/2α=1.23,0.93,0.97h;t1/2β=11.84,12.06,16.5 1h;AUC0-t=143.43,206.25,275.92mg·L-1·h-1;AUC0-∞=181.02,231.74,295.06mg·L-1·h-1.Peak time is 2h.Conclusions:FGLV can relive the model rats’ aging state,elevate the anti-oxidation capability,reduce the ROS and maintain normal function.It is suggested that the FGLV can resist oxidation and delay aging.The pharmacokinetic process of FGLV extracts is identical with that of first order dynamics and two-compartment mode,and the AUC value and dose had a good linear correlation.The linear pharmacokinetic characteristics of FGLV in dose range.Which the elimination speed of drug is slower than its absorption speed.It can be concluded that the drug may stay for long time in vivo.