目的：通过系统药理学方法探讨葛根芩连汤治疗2型糖尿病的作用机制及原理。方法：利用中药系统药理学分析平台（traditional Chinese medicine systems pharmacology database and analysis platform,TCMSP）数据库筛选葛根芩连汤有效...目的：通过系统药理学方法探讨葛根芩连汤治疗2型糖尿病的作用机制及原理。方法：利用中药系统药理学分析平台（traditional Chinese medicine systems pharmacology database and analysis platform,TCMSP）数据库筛选葛根芩连汤有效成分和相关靶标蛋白;运用网络可视化软件Cytoscape 3.5.1构建葛根芩连汤＂有效成分-靶标＂相互作用网络进行拓扑学分析;借助STRING 10.5在线数据库进行蛋白质与蛋白质相互作用（protein-protein interaction networks,PPI）网络的构建与分析;通过Uniprot数据库获取靶标蛋白的基因名称,借助David数据库进行基因通路功能富集分析京都基因和基因组百科全书（kyoto encyclopedia of genes and genomes,KEGG）,研究葛根芩连汤治疗2型糖尿病的作用机制及原理。结果：葛根芩连汤的核心化合物有槲皮素（quercetin）,山柰酚（kaempferol）,β-谷甾醇（beta-sitosteroll）等,核心靶标前列腺素G/H合成酶2（prostaglandin G/H synthase 2）等;PPI网络图显示葛根芩连汤有效成分中关键蛋白主要有c-Jun氨基末端激酶（JUN）,肿瘤坏死因子（TNF）,fos蛋白（FOS）,丝裂原活化蛋白激酶3（MAPK3）等;KEGG结果表明葛根芩连汤主要作用与肿瘤坏死因子信号通路（TNF signaling pathway）,丝裂原活化蛋白激酶信号通路（MAPK signaling pathway）等信号通路有关。结论：葛根芩连汤主要通过多种途径,多种信号通路作用于多种靶点发挥其药物功效,起到抗炎功效,治疗2型糖尿病的作用。展开更多
Thais luteostoma has been utilized as a crude drug whose shell and soft tissue have been widely used for the treatment of heat syndrome in China for thousands of years. The present study was designed to investigate th...Thais luteostoma has been utilized as a crude drug whose shell and soft tissue have been widely used for the treatment of heat syndrome in China for thousands of years. The present study was designed to investigate the antipyretic and anti-inflammatory activities of T. luteostoma. T. luteostoma was divided into shell （TLSH） and soft tissue （TLST） samples in the present study. The rat model of yeast-induced fever was used to investigate their antipyretic effects; and the rat model of hind paw edema induced by carrageenan was utilized to study their anti-inflammatory activities, and at the same time, the concentration variations of the central neurotransmitter [prostaglandin E2 （PGE2） and cyclic adenosine monophosphate （cAMP）], inflammatory mediators [tumor necrosis factor （TNFα）, interleukin-1β （IL-1）, interleukin-2 （IL-2） and interleukin-6 （IL-6）] and ion （Na^＋ and Ca^2＋） were also tested. The results showed that TLSH and TLST extracts significantly inhibited yeast-induced pyrexia in rats （P 〈 0.05）, and exhibited more lasting effects as compared to aspirin, and TLSH had the better antipyretic activity than TLST, and that TLSH and TLST could significantly prevent against carrageenan induced paw edema in rats （P 〈 0.05）; and markedly reduced levels of PGE2, cAMP, TNFα, IL-1β, IL-2, IL-6, and Na^＋/Ca^2＋. In fever model, TLST could significantly reduce the levels of PGE2 （P 〈 0.01） in rats＇ homogenate and TNF a （P 〈 0.05）, IL-113 （P 〈 0.01） in the plasma than TLSH, whereas TLSH could reduce the content of IL-2 （P 〈 0.01） and IL-6 （P 〈 0.01） in plasma and increase the content of Ca2＋ （P 〈 0.01） in plasma and homogenate more significantly than TLST. In conclusion, T. luteostoma extract has antipyretie and anti-inflammatory activities, which may be mediated through the suppression of production of PGE2, cAMP, Na^＋/Ca^2＋ , TNF a, IL-1β, IL-2, and IL-6.展开更多
文摘目的：通过系统药理学方法探讨葛根芩连汤治疗2型糖尿病的作用机制及原理。方法：利用中药系统药理学分析平台（traditional Chinese medicine systems pharmacology database and analysis platform,TCMSP）数据库筛选葛根芩连汤有效成分和相关靶标蛋白;运用网络可视化软件Cytoscape 3.5.1构建葛根芩连汤＂有效成分-靶标＂相互作用网络进行拓扑学分析;借助STRING 10.5在线数据库进行蛋白质与蛋白质相互作用（protein-protein interaction networks,PPI）网络的构建与分析;通过Uniprot数据库获取靶标蛋白的基因名称,借助David数据库进行基因通路功能富集分析京都基因和基因组百科全书（kyoto encyclopedia of genes and genomes,KEGG）,研究葛根芩连汤治疗2型糖尿病的作用机制及原理。结果：葛根芩连汤的核心化合物有槲皮素（quercetin）,山柰酚（kaempferol）,β-谷甾醇（beta-sitosteroll）等,核心靶标前列腺素G/H合成酶2（prostaglandin G/H synthase 2）等;PPI网络图显示葛根芩连汤有效成分中关键蛋白主要有c-Jun氨基末端激酶（JUN）,肿瘤坏死因子（TNF）,fos蛋白（FOS）,丝裂原活化蛋白激酶3（MAPK3）等;KEGG结果表明葛根芩连汤主要作用与肿瘤坏死因子信号通路（TNF signaling pathway）,丝裂原活化蛋白激酶信号通路（MAPK signaling pathway）等信号通路有关。结论：葛根芩连汤主要通过多种途径,多种信号通路作用于多种靶点发挥其药物功效,起到抗炎功效,治疗2型糖尿病的作用。
基金supported by Marine Industry Research Special Funds for Public Welfare Projects(201205024–1)The Project Funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions(ysxk-2010)
文摘Thais luteostoma has been utilized as a crude drug whose shell and soft tissue have been widely used for the treatment of heat syndrome in China for thousands of years. The present study was designed to investigate the antipyretic and anti-inflammatory activities of T. luteostoma. T. luteostoma was divided into shell （TLSH） and soft tissue （TLST） samples in the present study. The rat model of yeast-induced fever was used to investigate their antipyretic effects; and the rat model of hind paw edema induced by carrageenan was utilized to study their anti-inflammatory activities, and at the same time, the concentration variations of the central neurotransmitter [prostaglandin E2 （PGE2） and cyclic adenosine monophosphate （cAMP）], inflammatory mediators [tumor necrosis factor （TNFα）, interleukin-1β （IL-1）, interleukin-2 （IL-2） and interleukin-6 （IL-6）] and ion （Na^＋ and Ca^2＋） were also tested. The results showed that TLSH and TLST extracts significantly inhibited yeast-induced pyrexia in rats （P 〈 0.05）, and exhibited more lasting effects as compared to aspirin, and TLSH had the better antipyretic activity than TLST, and that TLSH and TLST could significantly prevent against carrageenan induced paw edema in rats （P 〈 0.05）; and markedly reduced levels of PGE2, cAMP, TNFα, IL-1β, IL-2, IL-6, and Na^＋/Ca^2＋. In fever model, TLST could significantly reduce the levels of PGE2 （P 〈 0.01） in rats＇ homogenate and TNF a （P 〈 0.05）, IL-113 （P 〈 0.01） in the plasma than TLSH, whereas TLSH could reduce the content of IL-2 （P 〈 0.01） and IL-6 （P 〈 0.01） in plasma and increase the content of Ca2＋ （P 〈 0.01） in plasma and homogenate more significantly than TLST. In conclusion, T. luteostoma extract has antipyretie and anti-inflammatory activities, which may be mediated through the suppression of production of PGE2, cAMP, Na^＋/Ca^2＋ , TNF a, IL-1β, IL-2, and IL-6.
