目的 从网络视角出发,探讨枸骨叶抗肿瘤的的可能作用机制,为其临床使用提供依据.方法 通过中药系统药理学数据库与分析平台(TCMSP)、中医百科全书数据库(ETCM)及查阅相关文献,获取枸骨叶的有效成分及潜在靶点.利用人类基因组注释数据库(GeneCards)结果对比,获得枸骨叶与肿瘤重合的潜在靶点基因,并通过Cytoscape 3.6.0软件构建枸骨叶的"候选成分-作用靶点"网络.利用String数据库和Cytoscape 3.6.0软件构建药物抗肿瘤的蛋白质相互作用(PPI)网络;并通过分子对接验证和筛选潜在的核心化合物,利用DAVID生物信息资源数据库对核心靶点进行基因本体论(GO)功能和京都基因与基因组百科全书(KEGG)通路富集分析.结果 共筛选出枸骨叶抗肿瘤的作用的靶点137个,对应13种有效成分.关键靶点涉及TP53、MAPK1、STAT3等.主要通过调控肿瘤坏死因子(TNF)信号通路、缺氧诱导因子-1(HIF-1)信号通路、磷脂酰肌醇3-激酶(PI3K/AKT)信号通路、肿瘤抑制因子P53信号通路、T细胞受体信号通路等发挥抗癌作用.涉及的癌种包括前列腺癌、胰腺癌、非小细胞肺癌等.分子对接结果显示,长梗冬青苷与MAPK1能稳定地结合并通过蛋白氨基酸Gly32、Glu33、Gly34、Tyr36等发生相互作用.结论 枸骨叶抗肿瘤作用的主要机制涉及槲皮素、熊果酸、长梗冬青苷、芒柄花黄素为代表的多成分,以TP53、MAPK1及STAT3为代表的多靶点,以及细胞增殖、细胞凋亡、信号传导为代表的多通路.
目的 建立银杏叶片中萜类内酯的含量测定方法.方法 采用HPLC-CAD法测定白果内酯、银杏内酯A、银杏内酯B和银杏内酯C的含量.使用Agilent TC C18色谱柱(250 mmX4.6 mm,5 μm),以正丙醇-四氢呋喃-水(1∶15∶84)为流动相,流速1.0 mL·min-1,柱温40℃,采用电喷雾检测器进行检测.结果 各萜类内酯在线性范围内与峰面积线性关系良好,相关系数为0.9997~1.000,平均回收率(n=6)在97.3%~99.1%,RSD在1.6%~2.5%.结论 该方法灵敏度高,精密度、重复性、准确度均良好,可作为银杏叶片中萜类内酯的含量测定方法.
Objective To optimize the extraction process of Flos Lonicerae and Hawthorn with water for fresh breath effervescent tablets and to provide the basis for the development of new drug of traditional Chinese medicine.Methods The extraction process of Flos Lonicerae and Hawthorn was optimized by orthogonal test,using the extract ratio,organic acid and chlorogenic acid content as indice.Results The optimum water extraction of Flos Lonicerae and Hawthorn condition was:12 times and 10 times of water for 2 cycles,1.5 h and 1 h each time.Conclusion The extraction rate of active components in the drug is high by the selected technology,which is simple,economic,rational and feasible.
Objective To improve the quality standard of Kouqi Qingxin Paotengpian.Methods Hawthorn in the tables were identified by thin-layer chromatography,the content of chlorogenic acid was determined by HPLC,the separation was performed on an 100-5-C18(250 mm×4.6 mm,5 μm),the mobile phase consisted of 0.4% phosphoric acid-acetonitrile(87∶13),the detective wavelength was 327 nm,the flow rate was 1.0 mL·min-1,and the column temperature was 30℃.Results Hawthorn could be identified by thin-layer chromatography,and the identification was highly specific without interference.The linear range of chlorogenic acid was 0.122 4-0.367 2 μg.The average recovery was 100.4%,RSD=1.7%.Conclusion The method is simple,reliable,and accurate,and can be used for the quality control of Kouqi Qingxin Paotengpian.
Objective To study preparation technology of Fresh breath effervescent tablets.Methods The optimum molding technology was screened through single factor test such as disintegration time,quantity of producing foam,pH value and taste.Results The best preparation process was the optimum water extraction of Flos lonicerae and Hawthorn for 2 cycles,then inspissated and dried using lactose-mannitol(2∶1) and tea polyphenols,followed by pulverizing.Citric acid-tartaric acid(1.5∶1) and sodium bicarbonate were used as effervescent material,sodium bicarbonate as admixture,and CMS-Na was added by two steps.The effervescent tablets had good taste,suitable hardness,good hydros-copicity and valid disintegration time.Conclusion Our preparation procedure is stable and simple.