A simple and selective ultra performance liquid chromatography--electrospray ionization tandem mass spectrometry （UPLC-ESI-MS/MS） assay was developed for the determination of the human plasma protein binding of four...A simple and selective ultra performance liquid chromatography--electrospray ionization tandem mass spectrometry （UPLC-ESI-MS/MS） assay was developed for the determination of the human plasma protein binding of four bioactive ftavonoids （such as orientin and vitexin） in Polygonum orientale. Protein precipitation was used for sample preparation. Equilibrium dialysis technique was applied to determine the plasma protein binding under physiological conditions. The separation was achieved through a Waters C i s column with a mobile phase composed of 0.1% formic acid in acetonitrile and 0.1% aqueous formic acid using step gradient elution at a flow rate of 0.35 mL/min. A Waters ACQUITYTM TQD system was operated under the multiple reaction monitoring （MRM） mode of positive electrospray ionization. All of the recovery, precision, accuracy and stability of the method met the requirements. Good correlations （r 〉 0.99） of the four compounds were found, which suggested that these compounds can be simultaneously determined with acceptable accuracy. Results showed that the plasma protein bindings of the four bioactive flavonoids were in the range of 74-89% over the six concentrations studied. The binding parameters containing protein binding affinity, protein binding dissociation constant, and protein binding site were studied. The maximum ability to bind with protein was also determined in the assay in order to understand the drug-protein binding of each compound better.展开更多
OBJECTIVE To investigate the antihyperlipidemic effect of methanol and aqueous extracts of the leaves of Polygonum minus in acute hyperlipidemic rat model.METHODS Acute hyperlipidemia was chemically induced in Sprague...OBJECTIVE To investigate the antihyperlipidemic effect of methanol and aqueous extracts of the leaves of Polygonum minus in acute hyperlipidemic rat model.METHODS Acute hyperlipidemia was chemically induced in Sprague Dawley rats by using poloxamer 407(500mg·kg-1 of body weight;intraperitoneal).Increase in total cholesterol was confirmed after six hours of induction.The normal and hyperlipidemic control groups were administered with 1mL carboxymethylcellulose(CMC),the two test groups received aqueous and methanol extract of leaves of P.minus respectively(1000mg·kg-1;orally;suspended in 1% CMC)whereas reference standard treated group received atorvastatin(60mg·kg-1;orally;suspended in 1% CMC)once daily for 3consecutive days.Blood samples were collected at 10 th and 24 th hour of the study for total cholesterol and triglycerides determination,while terminal blood samples were collected at58 th hour for full lipids profile analysis.RESULTS In the present study,both methanol and aqueous extracts lowered the serum total cholesterol and triglycerides significantly(P<0.001 and P<0.05,respectively)when compared with the hyperlipidemic control,similar to the standard drug atorvastatin.Varying effects were observed for both extracts on the other lipid parameter studied.Methanol extract showed significant reduction in LDL(P<0.05),VLDL(P<0.01)and atherogenic index(AI;P<0.001)and it showed a significant elevation in HDL levels(P<0.05).On the other hand,the aqueous extract showed significant reduction only in VLDL and AI(P<0.05)but no increase in HDL levels.CONCLUSION Present study confirmed the antihyperlipidemic effect of leaves of P.minus in acute hyperlipidemic rat model.The study also suggested that the methanol extract possess higher antihyperlipidemic effect than aqueous extract.Currently a study is ongoing to evaluate the antihyperlipidemic effect of the methanol extract in high-fat diet-induced chronic hyperlipidemic rat model.展开更多
[Objectives]This study was conducted to investigate the volatile components of Polygonum chinense L.[Methods]The volatile components of the methanol extract,ethyl acetate extract,chloroform extract and petroleum ether...[Objectives]This study was conducted to investigate the volatile components of Polygonum chinense L.[Methods]The volatile components of the methanol extract,ethyl acetate extract,chloroform extract and petroleum ether extract of P.chinense were analyzed and determined by gas chromatography.[Results]The volatile components of the methanol extract from P.chinense were the most,and phenolic acids and ketones accounted for a relatively high proportion,among which pyrogallic acid had the highest content.The ethyl acetate extract contained the second most volatile components,mostly acids and esters,of whichβ-sitosterol had the highest content;the chloroform and petroleum ether extracts had relatively few types of volatile components,most of which were alkanes,and the content ofγ-sitosterol shared by the two was the highest.The common substances of the four extracts were palmitic acid and phytol.[Conclusions]This study provides a theoretical basis for the quality evaluation of P.chinense and a scientific basis for its resource development.展开更多
[Objectives]To explore the pharmacodynamic material basis of Sijicao granules for the treatment of eczema through chemical composition-network pharmacology.[Methods]First of all,the chemical constituents of Polygonum ...[Objectives]To explore the pharmacodynamic material basis of Sijicao granules for the treatment of eczema through chemical composition-network pharmacology.[Methods]First of all,the chemical constituents of Polygonum capitatum and Plantago asiatica from Sijicao granules were collected,and the relevant target information of the constituents was collected by TCMSP,PubChem,DisGeNET,GeneCards and STRING databases.Furthermore,Cytoscape 3.8.2 software was used to construct the chemical compounds-target network map of Sijicao granules.Finally,STRING database was used for PPI protein network analysis,GO functional enrichment analysis and KEGG pathway enrichment analysis of core targets,and molecular docking between core constituents and protein targets was also performed.[Results]30 constituents,including quercetin,kaempferol,luteolin,ellagic acid and gallic acid,were discovered to be the key effective compounds of Sijicao granules in the treatment of eczema.And its core action protein targets were PTGS2,NOS2,AKT1,TP53,IL6,HMOX1.What s more,through GO functional enrichment analysis of biological process(BP),cell component(CC),molecular function(MF)analysis and KEGG pathway enrichment analysis,the main pathways of action of Sijicao granules for the treatment of eczema including IL-17 signaling pathway,T cell receptor signaling pathway,cancer signaling pathway,TNF signaling pathway and Relaxin signaling pathway.In addition,molecular docking results displayed that the primary active constituents quercetin,kaempferol and luteolin were well combined with the core protein targets AKT1 and IL6.[Conclusions]Sijicao granules could play an important role for the treatment of eczema through multi-component,multi-target,multi-pathway and their interaction.展开更多
基金This work was supported by the National Science Foundation of China （No. 30860366） Guizhou Province Municipal Science and Technology Project （No. 2007-6010）.
文摘A simple and selective ultra performance liquid chromatography--electrospray ionization tandem mass spectrometry （UPLC-ESI-MS/MS） assay was developed for the determination of the human plasma protein binding of four bioactive ftavonoids （such as orientin and vitexin） in Polygonum orientale. Protein precipitation was used for sample preparation. Equilibrium dialysis technique was applied to determine the plasma protein binding under physiological conditions. The separation was achieved through a Waters C i s column with a mobile phase composed of 0.1% formic acid in acetonitrile and 0.1% aqueous formic acid using step gradient elution at a flow rate of 0.35 mL/min. A Waters ACQUITYTM TQD system was operated under the multiple reaction monitoring （MRM） mode of positive electrospray ionization. All of the recovery, precision, accuracy and stability of the method met the requirements. Good correlations （r 〉 0.99） of the four compounds were found, which suggested that these compounds can be simultaneously determined with acceptable accuracy. Results showed that the plasma protein bindings of the four bioactive flavonoids were in the range of 74-89% over the six concentrations studied. The binding parameters containing protein binding affinity, protein binding dissociation constant, and protein binding site were studied. The maximum ability to bind with protein was also determined in the assay in order to understand the drug-protein binding of each compound better.
基金The project supported in part by AIMST University Internal Grant(AURGC/18/FOP/2013)
文摘OBJECTIVE To investigate the antihyperlipidemic effect of methanol and aqueous extracts of the leaves of Polygonum minus in acute hyperlipidemic rat model.METHODS Acute hyperlipidemia was chemically induced in Sprague Dawley rats by using poloxamer 407(500mg·kg-1 of body weight;intraperitoneal).Increase in total cholesterol was confirmed after six hours of induction.The normal and hyperlipidemic control groups were administered with 1mL carboxymethylcellulose(CMC),the two test groups received aqueous and methanol extract of leaves of P.minus respectively(1000mg·kg-1;orally;suspended in 1% CMC)whereas reference standard treated group received atorvastatin(60mg·kg-1;orally;suspended in 1% CMC)once daily for 3consecutive days.Blood samples were collected at 10 th and 24 th hour of the study for total cholesterol and triglycerides determination,while terminal blood samples were collected at58 th hour for full lipids profile analysis.RESULTS In the present study,both methanol and aqueous extracts lowered the serum total cholesterol and triglycerides significantly(P<0.001 and P<0.05,respectively)when compared with the hyperlipidemic control,similar to the standard drug atorvastatin.Varying effects were observed for both extracts on the other lipid parameter studied.Methanol extract showed significant reduction in LDL(P<0.05),VLDL(P<0.01)and atherogenic index(AI;P<0.001)and it showed a significant elevation in HDL levels(P<0.05).On the other hand,the aqueous extract showed significant reduction only in VLDL and AI(P<0.05)but no increase in HDL levels.CONCLUSION Present study confirmed the antihyperlipidemic effect of leaves of P.minus in acute hyperlipidemic rat model.The study also suggested that the methanol extract possess higher antihyperlipidemic effect than aqueous extract.Currently a study is ongoing to evaluate the antihyperlipidemic effect of the methanol extract in high-fat diet-induced chronic hyperlipidemic rat model.
基金Supported by Development of Huotanmu Capsules,a New Drug for Hepatitis B Treatment(20183046-1)Collaborative Innovation Center for Zhuang and Yao Medicines(GJKY[2013]20)+2 种基金Guangxi Key Laboratory of Zhuang and Yao Medicines(GKJZ[2014]32)Guangxi Key Discipline:Zhuang Medicine(GJKY[2013]16)First-class Discipline in Guangxi of Traditional Chinese Pharmacology(GJKY[2018]12)。
文摘[Objectives]This study was conducted to investigate the volatile components of Polygonum chinense L.[Methods]The volatile components of the methanol extract,ethyl acetate extract,chloroform extract and petroleum ether extract of P.chinense were analyzed and determined by gas chromatography.[Results]The volatile components of the methanol extract from P.chinense were the most,and phenolic acids and ketones accounted for a relatively high proportion,among which pyrogallic acid had the highest content.The ethyl acetate extract contained the second most volatile components,mostly acids and esters,of whichβ-sitosterol had the highest content;the chloroform and petroleum ether extracts had relatively few types of volatile components,most of which were alkanes,and the content ofγ-sitosterol shared by the two was the highest.The common substances of the four extracts were palmitic acid and phytol.[Conclusions]This study provides a theoretical basis for the quality evaluation of P.chinense and a scientific basis for its resource development.
基金Supported by Science and Technology Planning Project of Guizhou Province[QKHJC-ZK(2022)362]Science and Technology Achievements Transfer and Transformation Project of Guizhou Provincial Department of Education[(2022)064]+1 种基金Higher Education Institution Engineering Research Center of Guizhou Provincial Department of Education[(2023)035,No.(2023)zk01]National Undergraduate Innovation Training Project(202210660131,202310660082).
文摘[Objectives]To explore the pharmacodynamic material basis of Sijicao granules for the treatment of eczema through chemical composition-network pharmacology.[Methods]First of all,the chemical constituents of Polygonum capitatum and Plantago asiatica from Sijicao granules were collected,and the relevant target information of the constituents was collected by TCMSP,PubChem,DisGeNET,GeneCards and STRING databases.Furthermore,Cytoscape 3.8.2 software was used to construct the chemical compounds-target network map of Sijicao granules.Finally,STRING database was used for PPI protein network analysis,GO functional enrichment analysis and KEGG pathway enrichment analysis of core targets,and molecular docking between core constituents and protein targets was also performed.[Results]30 constituents,including quercetin,kaempferol,luteolin,ellagic acid and gallic acid,were discovered to be the key effective compounds of Sijicao granules in the treatment of eczema.And its core action protein targets were PTGS2,NOS2,AKT1,TP53,IL6,HMOX1.What s more,through GO functional enrichment analysis of biological process(BP),cell component(CC),molecular function(MF)analysis and KEGG pathway enrichment analysis,the main pathways of action of Sijicao granules for the treatment of eczema including IL-17 signaling pathway,T cell receptor signaling pathway,cancer signaling pathway,TNF signaling pathway and Relaxin signaling pathway.In addition,molecular docking results displayed that the primary active constituents quercetin,kaempferol and luteolin were well combined with the core protein targets AKT1 and IL6.[Conclusions]Sijicao granules could play an important role for the treatment of eczema through multi-component,multi-target,multi-pathway and their interaction.
