运用网络药理学方法探究黄连解毒汤调节巨噬细胞炎症反应、糖酵解、鞘脂代谢和谷氨酰胺代谢等方面的多成分、多靶点、多通路的相互作用规律和调控网络,为创新药物研究奠定基础。通过TCMSP数据库筛选黄连解毒汤活性成分, PharmMapper数...运用网络药理学方法探究黄连解毒汤调节巨噬细胞炎症反应、糖酵解、鞘脂代谢和谷氨酰胺代谢等方面的多成分、多靶点、多通路的相互作用规律和调控网络,为创新药物研究奠定基础。通过TCMSP数据库筛选黄连解毒汤活性成分, PharmMapper数据库预测靶点蛋白, DAVID数据库进行通路注释和分析, Cytoscape 3.2.1软件构建"活性成分-靶点-通路"网络图, GENEMANIA数据库进行蛋白相互作用分析, Systems Dock Web Site数据库进行分子对接验证。预测结果表明,黄连解毒汤中共筛选出84个活性成分,作用靶点111个,其中与巨噬细胞炎症相关的靶点蛋白13个,涉及代谢通路14条;与糖酵解、鞘脂代谢、谷氨酰胺代谢相关的靶点蛋白34个,涉及代谢通路8条。炎症相关蛋白和代谢相关蛋白通过物理相关性、蛋白共表达等方式互相作用,小檗碱、黄芩苷和栀子苷与5个重要靶点均能较好结合。黄连解毒汤可能通过作用于糖酵解、鞘脂代谢和谷氨酰胺代谢的相关靶点,影响其代谢过程中的代谢产物和酶,从而调节巨噬细胞炎症反应。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
The present study aimed at exploring different roles of the same compound in different environment, using preparative HPLC, and the significance to investigating bio-active constituents in traditional Chinese medicine...The present study aimed at exploring different roles of the same compound in different environment, using preparative HPLC, and the significance to investigating bio-active constituents in traditional Chinese medicine （TCM） on the basis of holism. In this study, the depletion of target component ferulic acid （FA） by using preparative HPLC followed by antioxidant activity testing was applied to investigate the roles of FA in Angelicae Sinansis Radix （DG）, Chuanxiong Rhizoma （CX） and their combination （GX）. The antioxidant activity was performed by 1, 1-diphenyl-2-picrylhydrazyl （DPPH） radical-scavenging activity testing. FA was successfully and exclusively depleted from DG, CX, and GX, respectively. By comparing the effects of the samples, it was found that FA was one of the main antioxidant constituents in DG, CX and GX, and the roles of FA were DG 〉 CX 〉 GX. Furthermore, the effects of FA varied at different doses in these herbs. This study provided a reliable and effective approach to clarifying the contribution of same compound in different TCMs to their bio-activities. The role of a constituent in different TCMs might be different, and a component with the same content might have different effects in different chemical environments. Furthermore, this study also suggested the potential utilization of preparative HPLC in the characterization of the roles of multi-ingredients in TCM.展开更多
文摘运用网络药理学方法探究黄连解毒汤调节巨噬细胞炎症反应、糖酵解、鞘脂代谢和谷氨酰胺代谢等方面的多成分、多靶点、多通路的相互作用规律和调控网络,为创新药物研究奠定基础。通过TCMSP数据库筛选黄连解毒汤活性成分, PharmMapper数据库预测靶点蛋白, DAVID数据库进行通路注释和分析, Cytoscape 3.2.1软件构建"活性成分-靶点-通路"网络图, GENEMANIA数据库进行蛋白相互作用分析, Systems Dock Web Site数据库进行分子对接验证。预测结果表明,黄连解毒汤中共筛选出84个活性成分,作用靶点111个,其中与巨噬细胞炎症相关的靶点蛋白13个,涉及代谢通路14条;与糖酵解、鞘脂代谢、谷氨酰胺代谢相关的靶点蛋白34个,涉及代谢通路8条。炎症相关蛋白和代谢相关蛋白通过物理相关性、蛋白共表达等方式互相作用,小檗碱、黄芩苷和栀子苷与5个重要靶点均能较好结合。黄连解毒汤可能通过作用于糖酵解、鞘脂代谢和谷氨酰胺代谢的相关靶点,影响其代谢过程中的代谢产物和酶,从而调节巨噬细胞炎症反应。
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.
基金supported by National Key Technology R&D Program(No.2008BAI51B01)the Specialized Research Fund for the Doctoral Program of Higher Education of China(No.20113237110010)A Project Funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions(PAPD)
文摘The present study aimed at exploring different roles of the same compound in different environment, using preparative HPLC, and the significance to investigating bio-active constituents in traditional Chinese medicine （TCM） on the basis of holism. In this study, the depletion of target component ferulic acid （FA） by using preparative HPLC followed by antioxidant activity testing was applied to investigate the roles of FA in Angelicae Sinansis Radix （DG）, Chuanxiong Rhizoma （CX） and their combination （GX）. The antioxidant activity was performed by 1, 1-diphenyl-2-picrylhydrazyl （DPPH） radical-scavenging activity testing. FA was successfully and exclusively depleted from DG, CX, and GX, respectively. By comparing the effects of the samples, it was found that FA was one of the main antioxidant constituents in DG, CX and GX, and the roles of FA were DG 〉 CX 〉 GX. Furthermore, the effects of FA varied at different doses in these herbs. This study provided a reliable and effective approach to clarifying the contribution of same compound in different TCMs to their bio-activities. The role of a constituent in different TCMs might be different, and a component with the same content might have different effects in different chemical environments. Furthermore, this study also suggested the potential utilization of preparative HPLC in the characterization of the roles of multi-ingredients in TCM.
