目的:研究核桃分心木的化学成分。方法:采用硅胶、ODS等柱色谱结合HPLC技术对核桃分心木70%乙醇提取物进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。结果:从核桃分心木中分离得到6个化合物,分别鉴定为:juglandisde A(1)、...目的:研究核桃分心木的化学成分。方法:采用硅胶、ODS等柱色谱结合HPLC技术对核桃分心木70%乙醇提取物进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。结果:从核桃分心木中分离得到6个化合物,分别鉴定为:juglandisde A(1)、salviaplebeiaside(2)、3′-O-β-D-glucopyranoside of 4-(3′,4′-dihydroxyphenyl)butan-2-one(3)、benzyl-β-D-glucopyranoside(4)、phenylethyl-β-D-glucopyranoside(5)和methyl(6-O-p-hydroxy-benzoyl)-β-D-glucopyranoside(6)。结论:其中,化合物1为新的苯基丁酮苷类化合物,化合物2和3为首次从核桃分心木中分离得到。展开更多
This study aimed to investigate the anti-inflammatory properties and underlying molecular mechanisms of 2,4',5'-trihydroxyl-5,2'-dibromo diphenylmethanone(LM49)using a carrageenan-induced paw edema model i...This study aimed to investigate the anti-inflammatory properties and underlying molecular mechanisms of 2,4',5'-trihydroxyl-5,2'-dibromo diphenylmethanone(LM49)using a carrageenan-induced paw edema model in mice,which serves as a well-established model for acute inflammation.Mice were randomly assigned into six groups,and acute inflammation was induced by injecting 1%carrageenan solution into the paw.To elucidate the anti-inflammatory effects and mechanisms of LM49,a comprehensive approach was employed,including pathology,transcriptomics,flow cytometry,RT-qPCR,Western blotting analysis,and molecular docking analysis.The results demonstrated that LM49 exerted a significant protective effect by reducing paw edema and lowering serum levels of pro-inflammatory cytokines IL-1βand TNF-a,while concurrently elevating anti-inflammatory cytokine IL-10 levels.Transcriptomic analysis identified 453 differentially expressed genes in the LM49-treated group.KEGG and GO enrichment analyses indicated that LM49 suppressed the NF-kB signaling pathway and modulated several other immuneinflammatory pathways.Molecular docking studies identified eight key targets of LM49 within the NF-kB signaling pathway.Furthermore,Western blotting analysis confirmed that LM49 inhibited the phosphorylation of p65 and IB-αand downregulated the expression of MYD88 and TLR4 in mouse paw tissues.These findings provided a foundational understanding of the anti-inflammatory effects and molecular mechanisms of LM49,paving the way for further in-depth studies in this field.展开更多
文摘目的:揭示活血化瘀药对丹参-川芎反向调节血管新生作用药效物质基础及作用机制。方法:在中药系统药理学数据库(TCMSP)中搜索出冠心宁注射液中丹参和川芎两种中药的有效成分,并在Swiss Target Prediction数据库中检索药物作用靶点;在疾病-基因数据库(DisGeNET)中检索促进血管新生靶点和抑制血管新生靶点;使用蛋白质相互作用数据库(STRING)数据库和Cytoscape软件分析网络核心靶点;使用DAVID数据库对药物-疾病靶点交集进行基因本体(gene ontology,GO)功能富集分析与京都基因与基因组百科全书(Kyoto Encyclopedia of Genes and Genomes,KEGG)通路富集分析;使用SYBYL-X 2.0软件进行分子对接分析;RT-qPCR实验验证木犀草素对MMP9基因表达的影响;体外小管形成实验分析木犀草素对内皮细胞新血管生成的作用。结果:经分析得出丹参有10个有效成分,50个血管新生作用靶点;川芎有2个有效成分,4个血管新生作用靶点。取药靶交集得出9个作用靶点,包括AR、PARP1、MMP9、MMP2、MMP12、AKR1B10、ABCC1、CDK6、STAT3。经过丹参/川芎活性成分-靶点网络图分析,经分析得出木犀草素是关键化学成分。经蛋白相互作用分析,结果显示MMP9是核心靶点。KEGG通路主要富集在5条信号通路,最主要的通路是癌症相关通路。GO生物学过程主要有22条,主要涉及胶原分解代谢过程、蛋白质细胞外基质、金属内肽酶活性等,经小管形成实验分析初步得出木犀草素抑制血管新生并下调MMP9基因的表达。结论:丹参-川芎药对的关键化学成分木犀草素通过调节MMP9靶点抑制血管新生作用,为活血化瘀中药在已知治疗缺血性疾的基础上开拓了反向调节血管新生作用,进而为丹参-川芎药对在临床癌症病人的使用提供新的视角和理论依据。
文摘目的:研究核桃分心木的化学成分。方法:采用硅胶、ODS等柱色谱结合HPLC技术对核桃分心木70%乙醇提取物进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。结果:从核桃分心木中分离得到6个化合物,分别鉴定为:juglandisde A(1)、salviaplebeiaside(2)、3′-O-β-D-glucopyranoside of 4-(3′,4′-dihydroxyphenyl)butan-2-one(3)、benzyl-β-D-glucopyranoside(4)、phenylethyl-β-D-glucopyranoside(5)和methyl(6-O-p-hydroxy-benzoyl)-β-D-glucopyranoside(6)。结论:其中,化合物1为新的苯基丁酮苷类化合物,化合物2和3为首次从核桃分心木中分离得到。
基金The National Natural Science Foundation of China(Grant No.82003770)the National Science and Technology Major Project of China(Grant No.2018ZX09711001-001-017)the Key Research and Development Plan of Shanxi Province(Grant No.202102130501005)。
文摘This study aimed to investigate the anti-inflammatory properties and underlying molecular mechanisms of 2,4',5'-trihydroxyl-5,2'-dibromo diphenylmethanone(LM49)using a carrageenan-induced paw edema model in mice,which serves as a well-established model for acute inflammation.Mice were randomly assigned into six groups,and acute inflammation was induced by injecting 1%carrageenan solution into the paw.To elucidate the anti-inflammatory effects and mechanisms of LM49,a comprehensive approach was employed,including pathology,transcriptomics,flow cytometry,RT-qPCR,Western blotting analysis,and molecular docking analysis.The results demonstrated that LM49 exerted a significant protective effect by reducing paw edema and lowering serum levels of pro-inflammatory cytokines IL-1βand TNF-a,while concurrently elevating anti-inflammatory cytokine IL-10 levels.Transcriptomic analysis identified 453 differentially expressed genes in the LM49-treated group.KEGG and GO enrichment analyses indicated that LM49 suppressed the NF-kB signaling pathway and modulated several other immuneinflammatory pathways.Molecular docking studies identified eight key targets of LM49 within the NF-kB signaling pathway.Furthermore,Western blotting analysis confirmed that LM49 inhibited the phosphorylation of p65 and IB-αand downregulated the expression of MYD88 and TLR4 in mouse paw tissues.These findings provided a foundational understanding of the anti-inflammatory effects and molecular mechanisms of LM49,paving the way for further in-depth studies in this field.
