Ginsenoside Rb3(G-Rb3)is one of the primary active compounds isolated from Panax ginseng Meyer,which belongs to protopanaxadiol ginsenosides(PPD).Based on the structure-activity relationship(SAR)of ginsenosides,the pe...Ginsenoside Rb3(G-Rb3)is one of the primary active compounds isolated from Panax ginseng Meyer,which belongs to protopanaxadiol ginsenosides(PPD).Based on the structure-activity relationship(SAR)of ginsenosides,the pentose structure of G-Rb3 limited itself to possess more pharmacological activity to a certain extent.However,pharmacokinetics show that G-Rb3 is processed through deglycosylation in the intestinal tract and converted into more active rare saponins,such as Compound K,F2,etc.A series of studies focused on neuroprotection and the cardiovascular system demonstrating its therapeutic potentials,which was achieved by diminishing oxidative stress and apoptosis.Therefore,more systematic and in-depth studies are needed to complete the pharmaceutical value and to promote its clinical applications.This article highlights the multiple pharmacological effects and mechanisms of G-Rb3 and prospects for its development.展开更多
目的运用网络药理学方法探索地稔治疗宫颈癌的潜在作用机制。方法通过检索相关文献得到地稔化学成分并筛选出地稔的活性成分,利用SwissTargetPrediction平台预测活性成分的潜在靶点。利用Genecards数据库检索宫颈癌相关靶点。利用Cytosc...目的运用网络药理学方法探索地稔治疗宫颈癌的潜在作用机制。方法通过检索相关文献得到地稔化学成分并筛选出地稔的活性成分,利用SwissTargetPrediction平台预测活性成分的潜在靶点。利用Genecards数据库检索宫颈癌相关靶点。利用Cytoscape3.7.2软件构建"地稔-活性成分-宫颈癌靶点"网络,并运用String数据库构建蛋白互作网络(protein-protein interaction,PPI)。使用OmicShare Tools数据库进行基因本体(Gene Ontology,GO)分析和京东基因与基因组百科全书(Kyoto Encyclopedia of Genes and Genomes,KEGG)富集分析。结果得到地稔中活性成分25个、活性成分靶点420个、宫颈癌靶点150个,最后获得关键靶点7个,与地稔治疗宫颈癌显著相关的信号通路20条。地稔的主要活性成分为3-甲氧基鞣花酸、柚皮素、芹菜素等。地稔治疗宫颈癌关键靶点为STAT3、PIK3CA、AKT1、ESR1等;关键的生物进程和通路可能包括免疫系统过程、转录调节活性、内分泌与代谢相关信号通路、细胞周期信号转导通路等。另外,3-甲氧基鞣花酸成剂量依赖性地抑制人宫颈癌细胞Hela细胞的增殖。结论本研究通过筛选发现地稔治疗宫颈癌的关键靶点及通路与细胞信号转导、细胞的增殖、分化、凋亡以及免疫调节等过程密切相关。因此,3-甲氧基鞣花酸可能主要通过影响宫颈癌细胞增殖和凋亡,从而达到治疗宫颈癌的目的。展开更多
基金This work was funded by the grant of Jilin Science&Technology Development Plan(No.20200301037RQ).
文摘Ginsenoside Rb3(G-Rb3)is one of the primary active compounds isolated from Panax ginseng Meyer,which belongs to protopanaxadiol ginsenosides(PPD).Based on the structure-activity relationship(SAR)of ginsenosides,the pentose structure of G-Rb3 limited itself to possess more pharmacological activity to a certain extent.However,pharmacokinetics show that G-Rb3 is processed through deglycosylation in the intestinal tract and converted into more active rare saponins,such as Compound K,F2,etc.A series of studies focused on neuroprotection and the cardiovascular system demonstrating its therapeutic potentials,which was achieved by diminishing oxidative stress and apoptosis.Therefore,more systematic and in-depth studies are needed to complete the pharmaceutical value and to promote its clinical applications.This article highlights the multiple pharmacological effects and mechanisms of G-Rb3 and prospects for its development.
文摘目的运用网络药理学方法探索地稔治疗宫颈癌的潜在作用机制。方法通过检索相关文献得到地稔化学成分并筛选出地稔的活性成分,利用SwissTargetPrediction平台预测活性成分的潜在靶点。利用Genecards数据库检索宫颈癌相关靶点。利用Cytoscape3.7.2软件构建"地稔-活性成分-宫颈癌靶点"网络,并运用String数据库构建蛋白互作网络(protein-protein interaction,PPI)。使用OmicShare Tools数据库进行基因本体(Gene Ontology,GO)分析和京东基因与基因组百科全书(Kyoto Encyclopedia of Genes and Genomes,KEGG)富集分析。结果得到地稔中活性成分25个、活性成分靶点420个、宫颈癌靶点150个,最后获得关键靶点7个,与地稔治疗宫颈癌显著相关的信号通路20条。地稔的主要活性成分为3-甲氧基鞣花酸、柚皮素、芹菜素等。地稔治疗宫颈癌关键靶点为STAT3、PIK3CA、AKT1、ESR1等;关键的生物进程和通路可能包括免疫系统过程、转录调节活性、内分泌与代谢相关信号通路、细胞周期信号转导通路等。另外,3-甲氧基鞣花酸成剂量依赖性地抑制人宫颈癌细胞Hela细胞的增殖。结论本研究通过筛选发现地稔治疗宫颈癌的关键靶点及通路与细胞信号转导、细胞的增殖、分化、凋亡以及免疫调节等过程密切相关。因此,3-甲氧基鞣花酸可能主要通过影响宫颈癌细胞增殖和凋亡,从而达到治疗宫颈癌的目的。
