Objective:To predict and analyze the potential Q-markers of Chuanxiong Chatiao Prescription,and the pharmacokinetic properties of pulvis and pills in vivo were studied,which provided a basis for the rational evaluatio...Objective:To predict and analyze the potential Q-markers of Chuanxiong Chatiao Prescription,and the pharmacokinetic properties of pulvis and pills in vivo were studied,which provided a basis for the rational evaluation of the phenomenon of“Different Dosage Forms of the Same Prescription”.Methods and Material:Q-markers analysis of Chuanxiong Chatiao Prescription based on the“Five Principles”(traceability and transmissibility,specificity,effectiveness,prescription compatibility and testability).The content determination method of Q-markers in Chuanxiong Chatiao Prescription was established by UPLC,and the content difference of Q-markers in the two dosage forms ware determined and compared.The Q-markers in rabbit plasma was determined by LC-MS/MS method,and the pharmacokinetic parameters of Q-markers in pulvis and pills were analyzed.Results:A total of 16 potential Q-markers from the“Five Principles”were used,nine components of tetramethylprazine,ferulic acid,glycyrrhizin,glycyrrhizic acid,luteolin,cimicifugoside,senkyunolideⅠ,isoimperatorin,nodakenin were identified as Q-markers of Chuanxiong Chatiao Presciption.The content of tetramethylprazine and other components in the pulvis form was found to be significantly higher than that in the pills,while the content of senkyunolideⅠwas lower than that in the pills,which may be related to the preparation process of the dosage form and the physicochemical properties of the components.Compared with pulvis,the Tmax and t_(1/2)of ferulic acid and other components in pills were significantly prolonged.To a certain extent,it can explain the classical theory of traditional Chinese medicine“Components in pulvis release quickly and take effect in fast-acting manner,while in pills release slowly and take effect in slow-acting”.Meanwhile,the Cmax and AUC0-t of tetramethylprazine and other components in pills were higher than those in pulvis,which showed unexpected pharmacokinetic characteristics,indicating the complexity of compounding and the importance of dosage form design.Conclusions:A method for the determination of Q-markers content was established by UPLC,which provide reference for the quality control of Chuanxiong Chatiao Prescription.In vivo studies have found the pharmacokinetic parameters indicate the absorption and distribution characteristics of pulvis and pills.However,it is also found that the release behavior of different components not only affected by the dosage form but also closely related to their own physical and chemical properties.展开更多
Lianqiao(Forsythia suspensa(Thunb.)Vahl,Abbreviated as“F.suspensa”below)is traditional Chinese medicine in China,widely distributed all over the country and also highly rich in resources.The Northwest Territories is...Lianqiao(Forsythia suspensa(Thunb.)Vahl,Abbreviated as“F.suspensa”below)is traditional Chinese medicine in China,widely distributed all over the country and also highly rich in resources.The Northwest Territories is a genuine producing area.There are many chemical components in F.suspensa,including lignans,phenylethanolic glycosides,flavonoids,C6-C2 natural alcohols and their glycosides,phenolic acids,terpenes and volatile oils.Among them,lignans and phenylethanolic glycosides are the main active components.Based on the review of chemical components or constituents and main pharmacological activities,according to the definition of quality marker,the components of quality marker of F.suspensa were predicted and analyzed from the aspects of plant genetics and chemical composition,traditional efficacy,traditional medicine,new efficacy,blood entering composition,measurable composition,effective composition in different compatibility,and the influence of storage conditions of extract.Further research on its medicinal active ingredients will provide scientific basis for the evaluation of F.suspensa quality.展开更多
Saposhnikovia divaricata(SD)has high medicinal and edible value,but relatively little research has been done on its qual-ity markers(Q-markers).To further clarify the Q-markers of SD with their corresponding pharmacod...Saposhnikovia divaricata(SD)has high medicinal and edible value,but relatively little research has been done on its qual-ity markers(Q-markers).To further clarify the Q-markers of SD with their corresponding pharmacodynamic targets.In this experiment,14 batches of SD were identified and screened for Q-marker candidate components using a combination of HPLC fingerprint with similarity analysis,principal component analysis,hierarchical cluster analysis,and partial least squares discriminant analysis.Then,network pharmacology was used to predict Q-markers and core targets.The results showed that 5-O-methylvisammioside,cimifugin,and prim-O-glucosylcimifugin could be used as Q-markers of SD;while,MAPK1,MAPK3,PIK3CA,JUN,and MAPK8 were the core targets of SD for drug efficacy.To further evaluate the bind-ing efficiency of Q-markers,molecular docking of the main active ingredients of SD to the core targets was performed.The results showed that the compounds bind well to their targets,and binding energies were all less than-5 kcal/mol.The Q-markers obtained from the screening were closely related to the core target genes,which could achieve therapeutic effects by modulating the relevant signaling pathways.This study offers a reference for the establishment of a set of quality control evaluation system for SD potential Q-markers prediction analysis,and lays the foundation for elucidating the mechanism of actionunderlying itspharmacodynamic substance.展开更多
基金supported by Chinese Medicine Pharmaceutical Key Discipline of Shaanxi province(No.303061107)National key Research and Development plan(No.2018-YFC1706904)+1 种基金Discipline Innovation team Project of Shaanxi University of Chinese Medicine(No.2019-YL11)Shaanxi Province Key subject of pharmacy engineering of Shaanxi Provincial Traditional Chinese Medicine administration(No.2017001).
文摘Objective:To predict and analyze the potential Q-markers of Chuanxiong Chatiao Prescription,and the pharmacokinetic properties of pulvis and pills in vivo were studied,which provided a basis for the rational evaluation of the phenomenon of“Different Dosage Forms of the Same Prescription”.Methods and Material:Q-markers analysis of Chuanxiong Chatiao Prescription based on the“Five Principles”(traceability and transmissibility,specificity,effectiveness,prescription compatibility and testability).The content determination method of Q-markers in Chuanxiong Chatiao Prescription was established by UPLC,and the content difference of Q-markers in the two dosage forms ware determined and compared.The Q-markers in rabbit plasma was determined by LC-MS/MS method,and the pharmacokinetic parameters of Q-markers in pulvis and pills were analyzed.Results:A total of 16 potential Q-markers from the“Five Principles”were used,nine components of tetramethylprazine,ferulic acid,glycyrrhizin,glycyrrhizic acid,luteolin,cimicifugoside,senkyunolideⅠ,isoimperatorin,nodakenin were identified as Q-markers of Chuanxiong Chatiao Presciption.The content of tetramethylprazine and other components in the pulvis form was found to be significantly higher than that in the pills,while the content of senkyunolideⅠwas lower than that in the pills,which may be related to the preparation process of the dosage form and the physicochemical properties of the components.Compared with pulvis,the Tmax and t_(1/2)of ferulic acid and other components in pills were significantly prolonged.To a certain extent,it can explain the classical theory of traditional Chinese medicine“Components in pulvis release quickly and take effect in fast-acting manner,while in pills release slowly and take effect in slow-acting”.Meanwhile,the Cmax and AUC0-t of tetramethylprazine and other components in pills were higher than those in pulvis,which showed unexpected pharmacokinetic characteristics,indicating the complexity of compounding and the importance of dosage form design.Conclusions:A method for the determination of Q-markers content was established by UPLC,which provide reference for the quality control of Chuanxiong Chatiao Prescription.In vivo studies have found the pharmacokinetic parameters indicate the absorption and distribution characteristics of pulvis and pills.However,it is also found that the release behavior of different components not only affected by the dosage form but also closely related to their own physical and chemical properties.
文摘Lianqiao(Forsythia suspensa(Thunb.)Vahl,Abbreviated as“F.suspensa”below)is traditional Chinese medicine in China,widely distributed all over the country and also highly rich in resources.The Northwest Territories is a genuine producing area.There are many chemical components in F.suspensa,including lignans,phenylethanolic glycosides,flavonoids,C6-C2 natural alcohols and their glycosides,phenolic acids,terpenes and volatile oils.Among them,lignans and phenylethanolic glycosides are the main active components.Based on the review of chemical components or constituents and main pharmacological activities,according to the definition of quality marker,the components of quality marker of F.suspensa were predicted and analyzed from the aspects of plant genetics and chemical composition,traditional efficacy,traditional medicine,new efficacy,blood entering composition,measurable composition,effective composition in different compatibility,and the influence of storage conditions of extract.Further research on its medicinal active ingredients will provide scientific basis for the evaluation of F.suspensa quality.
基金funded by Fundamental Research Funds for the Central Universities(2572022DJ01)Natural Science Foundation of Heilongjiang Province(LH2022B004)+1 种基金111 Project(B20088)Heilongjiang Touyan Innovation Team Program(Tree Genetics and Breeding Innovation Team).
文摘Saposhnikovia divaricata(SD)has high medicinal and edible value,but relatively little research has been done on its qual-ity markers(Q-markers).To further clarify the Q-markers of SD with their corresponding pharmacodynamic targets.In this experiment,14 batches of SD were identified and screened for Q-marker candidate components using a combination of HPLC fingerprint with similarity analysis,principal component analysis,hierarchical cluster analysis,and partial least squares discriminant analysis.Then,network pharmacology was used to predict Q-markers and core targets.The results showed that 5-O-methylvisammioside,cimifugin,and prim-O-glucosylcimifugin could be used as Q-markers of SD;while,MAPK1,MAPK3,PIK3CA,JUN,and MAPK8 were the core targets of SD for drug efficacy.To further evaluate the bind-ing efficiency of Q-markers,molecular docking of the main active ingredients of SD to the core targets was performed.The results showed that the compounds bind well to their targets,and binding energies were all less than-5 kcal/mol.The Q-markers obtained from the screening were closely related to the core target genes,which could achieve therapeutic effects by modulating the relevant signaling pathways.This study offers a reference for the establishment of a set of quality control evaluation system for SD potential Q-markers prediction analysis,and lays the foundation for elucidating the mechanism of actionunderlying itspharmacodynamic substance.
