Objective:To screen the anti-inflammatory monomeric compounds isolated from Berchemia lineata(L.)DC and explore the anti-inflammatory mechanism of some compounds based on NF-κB signaling pathway.Methods:LPS was used ...Objective:To screen the anti-inflammatory monomeric compounds isolated from Berchemia lineata(L.)DC and explore the anti-inflammatory mechanism of some compounds based on NF-κB signaling pathway.Methods:LPS was used to induce RAW264.7 to establish a model of cellular inflammatory reaction.CCK-8 method was used to detect the effect of monomer compounds on the activity of RAW264.7 cells.The release of nitric oxide(NO)in the superneant was measured by Griess method,and NO inhibition rate was calculated.The anti-inflammatory activity gradient of some monomeric compounds was also measured.The effects of monomer compound 21 on the secretion of IL-6,TNF-α,NF-κB,COX-2 and iNOS induced by LPS were detected by ELISA.Results:The concentration of monomer compound of Berchemia lineata(L.)DC.was 50μmol/L,and it was administered for 24 h.The results showed that anthraquinone compound No.19 had obvious drug toxicity,while other compounds had weak or no obvious drug toxicity.The concentration was 50μmol/L,and the drug was administered for 12 h.The results showed that all the monomer compounds could inhibit the release of NO to varying degrees,and the highest NO inhibition rate was over 90%,which showed obvious anti-inflammatory activity.NO inhibition rate of No.01 new skeleton compound can reach 70.81%.The results of anti-inflammatory activity gradient showed that the monomer compound of Berchemia lineata(L.)DC.could inhibit the release of NO in a dose-dependent manner.The results of ELISA showed that phenolic compound 21 could inhibit the secretion of IL-6,TNF-α,NF-κB,COX-2 and iNOS in RAW264.7 cells.Conclusion:The monomer compound of Berchemia lineata(L.)DC.has a certain anti-inflammatory activity,among which flavonoids and bibenzyl components isolated from this plant for the first time may be the material basis for its anti-inflammatory activity.The simple phenolic monomer compound 21 may play an anti-inflammatory role by regulating NF-κB signaling pathway.展开更多
[Objectives]To expose the plausible mechanism of Blumea balsamifera(L.)DC.against Alzheimer s disease via network pharmacology and HPLC-ESI-HRMS technology.[Methods]To begin with,HPLC-ESI-HRMS was employed to identify...[Objectives]To expose the plausible mechanism of Blumea balsamifera(L.)DC.against Alzheimer s disease via network pharmacology and HPLC-ESI-HRMS technology.[Methods]To begin with,HPLC-ESI-HRMS was employed to identify the components of B.balsamifera.Secondly,the potential targets of the components were identified and predicted based on chemical similarity and online databases.Thirdly,by way of topological analysis of a component-disease target interaction network,the primary candidate targets and potential active components were identified.Lastly,molecular docking analysis was used to confirm the interaction between active components and therapeutic targets.[Results]According to the final results,HPLC-ESI-HRMS identified 70 components.Out of these,20 components were potentially biologically active,and most of them were sesquiterpenoids.According to the molecular docking results,the primary active components were appropriately coordinated with the core targets,indicating a high level of pharmacodynamic activity.Thus,the sesquiterpenes present in B.balsamifera are considered potential active ingredients having multi-target and multi-pathway effects for treating Alzheimer s disease.[Conclusions]This research will provide a scientific reference for the future pharmacological activity and clinical application of B.balsamifera.展开更多
基金This study was supported by National Key Research and Development Program(No.2022YFC3502201)National Natural Science Foundation of China(No.81960762)+3 种基金Guangxi Key Discipline of Traditional Chinese Medicine(No.GZXK-Z-20-62)Guangxi Science and Technology Base and Talent Special Project(No.Guike AD19245183,AD22035052)Guangxi Demonstration Base of External Treatment of Traditional Chinese Medicine(No.14,2019)National Famous TCM Inheritance Studio,National Famous Old TCM Expert Inheritance Studio Construction Project,National Famous TCM Huang Hanru Academic Thinking and Clinical Experience Inheritance and Promotion Center(No.2022V004)。
文摘Objective:To screen the anti-inflammatory monomeric compounds isolated from Berchemia lineata(L.)DC and explore the anti-inflammatory mechanism of some compounds based on NF-κB signaling pathway.Methods:LPS was used to induce RAW264.7 to establish a model of cellular inflammatory reaction.CCK-8 method was used to detect the effect of monomer compounds on the activity of RAW264.7 cells.The release of nitric oxide(NO)in the superneant was measured by Griess method,and NO inhibition rate was calculated.The anti-inflammatory activity gradient of some monomeric compounds was also measured.The effects of monomer compound 21 on the secretion of IL-6,TNF-α,NF-κB,COX-2 and iNOS induced by LPS were detected by ELISA.Results:The concentration of monomer compound of Berchemia lineata(L.)DC.was 50μmol/L,and it was administered for 24 h.The results showed that anthraquinone compound No.19 had obvious drug toxicity,while other compounds had weak or no obvious drug toxicity.The concentration was 50μmol/L,and the drug was administered for 12 h.The results showed that all the monomer compounds could inhibit the release of NO to varying degrees,and the highest NO inhibition rate was over 90%,which showed obvious anti-inflammatory activity.NO inhibition rate of No.01 new skeleton compound can reach 70.81%.The results of anti-inflammatory activity gradient showed that the monomer compound of Berchemia lineata(L.)DC.could inhibit the release of NO in a dose-dependent manner.The results of ELISA showed that phenolic compound 21 could inhibit the secretion of IL-6,TNF-α,NF-κB,COX-2 and iNOS in RAW264.7 cells.Conclusion:The monomer compound of Berchemia lineata(L.)DC.has a certain anti-inflammatory activity,among which flavonoids and bibenzyl components isolated from this plant for the first time may be the material basis for its anti-inflammatory activity.The simple phenolic monomer compound 21 may play an anti-inflammatory role by regulating NF-κB signaling pathway.
基金Supported by Science and Technology Project of Guizhou Province of China(QKHPTRC[2021]259,QKH LH[2017]7146)Doctoral Research Initiation Fund(GYZYYFY-BS-2018[14])+2 种基金2018 Guizhou Provincial High Level Innovative Talent ProjectResearch Project on Traditional Chinese Medicine and Ethnic Medicine Science and Technology in Guizhou Province(QZYY2017-079,QZYY2017-087)Project of Key Laboratory Characteristic Forestry of Guizhou Province of China(QJHKY[2021]002).
文摘[Objectives]To expose the plausible mechanism of Blumea balsamifera(L.)DC.against Alzheimer s disease via network pharmacology and HPLC-ESI-HRMS technology.[Methods]To begin with,HPLC-ESI-HRMS was employed to identify the components of B.balsamifera.Secondly,the potential targets of the components were identified and predicted based on chemical similarity and online databases.Thirdly,by way of topological analysis of a component-disease target interaction network,the primary candidate targets and potential active components were identified.Lastly,molecular docking analysis was used to confirm the interaction between active components and therapeutic targets.[Results]According to the final results,HPLC-ESI-HRMS identified 70 components.Out of these,20 components were potentially biologically active,and most of them were sesquiterpenoids.According to the molecular docking results,the primary active components were appropriately coordinated with the core targets,indicating a high level of pharmacodynamic activity.Thus,the sesquiterpenes present in B.balsamifera are considered potential active ingredients having multi-target and multi-pathway effects for treating Alzheimer s disease.[Conclusions]This research will provide a scientific reference for the future pharmacological activity and clinical application of B.balsamifera.
