The present study aimed to establish a pharmacodynamic method using the py Solo software to explore the influence of freeze-dried powders of Shuangxia Decoction(SXD) on the sleep of normal Drosophila melanogaster and ...The present study aimed to establish a pharmacodynamic method using the py Solo software to explore the influence of freeze-dried powders of Shuangxia Decoction(SXD) on the sleep of normal Drosophila melanogaster and the Drosophila melanogaster whose sleep was divested by light. The dose-effect and the time-effect relationships of SXD on sleep were examined. The effect-onset concentration of SXD was 0.25%, the plateau appeared at the concentration of 2.5% and the total sleep time showed a downtrend when the concentration was greater than 2.5%. The sleep time was the longest on the fourth day after SXD was given. The fruit fly sleep deprivation model was repeated by light stimulation at night. The middle dosage group(2.5%) had the best insomnia-curing effect. In conclusion, using the py Solo software, an approach for the pharmacodynamics study was established with Drosophila melanogaster as a model organism to determine the insomnia-curing effects of the traditional Chinese medicine(TCM). Our results demonstrated the reliability of this method. The freeze-dried powders of SXD could effectively improve the sleep quality of Drosophila melanogaster.展开更多
目的:通过网络药理学和分子对接技术探讨双夏汤治疗不寐的主要活性成分及作用机制。方法:通过中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,TCMSP)数据库获取双...目的:通过网络药理学和分子对接技术探讨双夏汤治疗不寐的主要活性成分及作用机制。方法:通过中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,TCMSP)数据库获取双夏汤活性成分,通过Swiss Target Prediction数据库预测其成分的作用靶点,结合OMIM、Gencards、Drugbank数据库获取不寐的作用靶点,取二者共同作用的靶点制作韦恩图。运用Cytoscape 3.7.2软件筛选并构建“活性成分-核心靶点”网络,利用STRING数据库构建蛋白质-蛋白质相互作用网络图,筛选出核心靶点后对其进行基因本体论(GO)富集分析和京都基因与基因组学百科全书(KEGG)通路分析,最后将核心靶点与主要活性成分进行分子对接验证。结果:筛选得到双夏汤治疗不寐的22个活性成分和115个药物与疾病的共同靶点,推测丝氨酸/苏氨酸蛋白激酶1(Akt Serine/Threonine Kinase 1,AKT1)、白细胞介素(Interleukin,IL)-6、淀粉样蛋白前体(Beta Amyloid A4 Protein,APP)、肿瘤坏死因子(Tumor Necrosis Factor,TNF)等关键靶点主要作用于G蛋白偶联受体信号通路、神经递质水平的调节、神经活性配体-受体相互作用等信号通路。分子对接结果表明,主要活性成分能够分别与核心靶点对接良好。结论:双夏汤可能通过保护中枢神经细胞,下调炎性因子表达,影响神经递质的释放和传递来发挥治疗不寐的作用。展开更多
基金supported by National Natural Science Foundation of China(No.81173521)the Central University Basic Scientific Research Project of Ministry of Education,China(No.2015-JYB-XS068)
文摘The present study aimed to establish a pharmacodynamic method using the py Solo software to explore the influence of freeze-dried powders of Shuangxia Decoction(SXD) on the sleep of normal Drosophila melanogaster and the Drosophila melanogaster whose sleep was divested by light. The dose-effect and the time-effect relationships of SXD on sleep were examined. The effect-onset concentration of SXD was 0.25%, the plateau appeared at the concentration of 2.5% and the total sleep time showed a downtrend when the concentration was greater than 2.5%. The sleep time was the longest on the fourth day after SXD was given. The fruit fly sleep deprivation model was repeated by light stimulation at night. The middle dosage group(2.5%) had the best insomnia-curing effect. In conclusion, using the py Solo software, an approach for the pharmacodynamics study was established with Drosophila melanogaster as a model organism to determine the insomnia-curing effects of the traditional Chinese medicine(TCM). Our results demonstrated the reliability of this method. The freeze-dried powders of SXD could effectively improve the sleep quality of Drosophila melanogaster.
文摘目的:通过网络药理学和分子对接技术探讨双夏汤治疗不寐的主要活性成分及作用机制。方法:通过中药系统药理学数据库与分析平台(Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,TCMSP)数据库获取双夏汤活性成分,通过Swiss Target Prediction数据库预测其成分的作用靶点,结合OMIM、Gencards、Drugbank数据库获取不寐的作用靶点,取二者共同作用的靶点制作韦恩图。运用Cytoscape 3.7.2软件筛选并构建“活性成分-核心靶点”网络,利用STRING数据库构建蛋白质-蛋白质相互作用网络图,筛选出核心靶点后对其进行基因本体论(GO)富集分析和京都基因与基因组学百科全书(KEGG)通路分析,最后将核心靶点与主要活性成分进行分子对接验证。结果:筛选得到双夏汤治疗不寐的22个活性成分和115个药物与疾病的共同靶点,推测丝氨酸/苏氨酸蛋白激酶1(Akt Serine/Threonine Kinase 1,AKT1)、白细胞介素(Interleukin,IL)-6、淀粉样蛋白前体(Beta Amyloid A4 Protein,APP)、肿瘤坏死因子(Tumor Necrosis Factor,TNF)等关键靶点主要作用于G蛋白偶联受体信号通路、神经递质水平的调节、神经活性配体-受体相互作用等信号通路。分子对接结果表明,主要活性成分能够分别与核心靶点对接良好。结论:双夏汤可能通过保护中枢神经细胞,下调炎性因子表达,影响神经递质的释放和传递来发挥治疗不寐的作用。