Study On Hepatoprotective Effect And Organization Distribution Of Baicalin Magnesium Salt

Scutellaria baicalensis Georgi,a dry root medicine,comes from labidae plant.It has a bitter cold and goes to lungs,gallbladder,spleen,large intestine,and small intestine.It has the effects of antipyretic and dampness,purging and detoxification,hemostasis,and tocolysis.It is used in wet temperatures,Shushi,chest tightness,vomiting,dampness,fever,fullness,diarrhea,jaundice,hyperactivity and cough,high fever,polydipsia,blood spit,phlegm,soreness,fetal movement anxiety and so on.Modern pharmacological research found that its main active ingredients are baicalein,baicalin,wogonin,glycosides and other flavonoids.The content of baicalin is the highest,widely used in clinical treatments.At present,there are many studies on the hepatoprotective effect of baicalin,but its poor water solubility and low bioavailability limit its clinical application.However,the solubility of baicalin in the decoction is larger.The research group found that baicalin was present in the form of magnesium salt in medicinal materials,and the water solubility of baicalin magnesium salt was excellent.Then a synthetic method was found to prepare baicalin magnesium salt.According to reports in the literature,magnesium ion has a certain protective effect on liver injury,but whether it can play a synergistic effect with baicalin and enhance the liver protection efficacy of baicalin magnesium salt remains to be studied,and the distribution of magnesium salt in the body is not clear.Therefore,in this study,after intravenously administered baicalin magnesium salt to rats,we explored its liver protection efficacy in the liver damage rats and its organization distribution to provide the basis for the research and development of baicalin magnesium preparations.Objective:1.To study the effect of baicalin and its magnesium salt on the hepatoprotective after intravenous injection of baicalin and its magnesium salt,then to explore whether the baicalin and magnesium ions in the baicalin magnesium salt structure have synergistic hepatoprotective effects.2.Determine the organization distribution of injecting baicalin magnesium in rats by HPLC method,to provide reference for the pharmacological effects and toxicity studies of the injection of baicalin magnesium salt.Methods:1.Rats were injected intravenously with magnesium glycyrrhizinate,magnesium sulphate,baicalin,and its magnesium salts and then injected with50%carbon tetrachloride intraperitoneally to establish a liver injury rat model.After 24 hours,we collect plasma and liver tissues and tested for the activity of ALT and AST in serum,MDA concentration in liver tissue,liver index and liver pathological sections.2.We anaesthetized and draw heart,liver,spleen,lung and kidney from rats at 0.25,0.75,1,2,4 and 8 h after tail vein injection of baicalin magnesium(50 mg·kg^-1),and determined the concentration of the target component in each tissue by HPLC.Results:1.Compared with the model group,the serological,histological,and hepatic indexes of the administration group were all decreased,with statistical significance?P<0.05?.There was no significant difference in the indicators of the baicalin magnesium group and the magnesium isoglycyrrhizinate group.The activity of ALT,AST in the serum and MDA content of liver in the baicalin magnesium group was lower than that in the baicalin group and magnesium sulfuric group,with statistical differences?P<0.05?.The disease degree of liver in the baicalin magnesium salt group and magnesium isoglycyrrhizinate group was lighter,while the baicalin group and magnesium sulfate group was more serious.2.After intravenous administration of 50 mg·kg^-1 baicalin magnesium salt,the test results showed that the target component was mostly distributed in the kidney,followed by lung tissue,and the distribution in the heart,liver,and spleen was very small.At the time of 0.25 h,the concentration of the drug reached a maximum value.The concentration of the baicalin magnesium rapidly decreased at the time of 0.75 h.With the prolongation of time,the target component could not be detected quickly.At the 8 h time,the target component only could be detected in the kidney.Conclusion:1.Pharmacodynamic study found that the hepatoprotective effect difference of baicalin magnesium salt and the positive drug isoglycyrrhizic group is not obvious.The pharmacological activity of baicalin magnesium salt is better than baicalin and magnesium sulfate.The results show that the baicalin magnesium salt has good pharmacological effects on liver injury.Baicalin and magnesium ions in the baicalin magnesium salt structure may act synergistically to exert hepatoprotective effects.2.Distribution experiments showed that the baicalin magnesium in the heart,liver,spleen,lung,and kidney distributed rapidly and eliminated quickly.Among them,there are more distributions in the lungs and kidneys,and less distribution in the livers.It can provide reference for the development of new pharmacological effects and of baicalin magnesium.