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Study On The Pharmaceutical Chemistry Analysis And Pharmacokinetic Of Phyhalis Alkekeng In Vivo

Posted on:2017-01-13Degree:DoctorType:Dissertation
Country:ChinaCandidate:H X LiuFull Text:PDF
GTID:1484304838456324Subject:Natural medicinal chemistry
Abstract/Summary:PDF Full Text Request
The calyces of Physalis alkekengi var.franchetii are a well-known traditional Chinese medicine(Jindenglong,Chinese Lantern)for the treatment of sore throat,cough,eczema,and tumors.To explore the efficacy material basis of Jindenglong in vivo,in this study,the metabolites profile of Jindenglong were systematically analyzed and the pharmacokinetic of its major components were researched by using UPLC-MS technique.A workflow-interpretation strategy was established and introduced to identify the metabolites in vivo based on UPLC-Q/TOF-MS and MetabolynxTM data processing software.A total of 44 metabolites were identified in rat biological samples after oral administration of luteolin-7-O-glucopyranoside,including 35 metabolites in urine,17 metabolites in plasma,17 metabolites in bile and 5 metabolites in feces.The results showed that phase I metabolites are hydrolysis and reduction,and phase II metabolites include sulfation,glucuronidation and methylation.A total of 24 metabolites were identified in rat biological samples after oral administration of physalin A.including 15 metabolites in urine,5 metabolites in plasma,16 metabolites in bile and 22 metabolites in feces.The results showed that phase I are reduction and hydroxylation,and phase II include sulfonation.On the basis of analysis of the metabolic profile of luteolin-7-O-glucopyranoside and physalin A,Jindenglong-related metabolites in rat urine,feces and plasma were investigated by UPLC-MSE/MS2 in the similar manner.As a result,16 prototype compounds and 51 metabolites were detected in vivo.Accordingly,their possible metabolic pathway was proposed.The analysis of metabolites in different bio-samples suggested that the flavonol glycoside was hydrolyzed to the aglycone firstly,and then for further absorption,metabolism and excretion in vivo,and the typical metabolic reaction was sulfonation.This research provides scientific and reliable support for full understanding of the metabolic profiling of Jingdenglong and the results provide evidence that should help to elucidate the effective substance basis of Jingdenglong in vivo.A quantitative determination method was developed to study pharmacokinetic of the major compounds in this herb.It clarified the in vivo pharmacokinetic characteristics of this herb in rats,so as to provide a basis for revealing the material foundation and guiding rational clinical application of Jingdenglong.In summary,these outcomes may reveal the bioactive material basis of Jingdenglong in vivo to some extent.Additionally,it also provides valuable data for the pharmacokinetic study of this Traditional Chinese Medicine as well as it’s deeply development in further.
Keywords/Search Tags:Jindenglong, UPLC-Q/TOF-MS, Metabolate, Pharmacokinetic, Pharmaceutical chemistry in vivo
PDF Full Text Request
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