基于网络药理学分析防风-乌梅药对治疗荨麻疹的作用机制

目的 基于网络药理学分析防风-乌梅药对治疗荨麻疹的物质基础及分子机制。方法 根据文献报道,结合口服利用度≥ 30%和类药性分析≥ 0.18,在TCMSP数据库、BATMAN-TCM数据库筛选防风-乌梅药对活性成分及靶点,GeneCards数据库筛选荨麻疹靶点,通过靶点映射确定药对活性成分作用的荨麻疹靶点;借助Cytoscape 3.5.1软件构建活性成分-靶点网络图,STRING平台构建靶蛋白互作网络,应用DAVID数据库对靶点进行KEGG通路分析,利用Cytoscape软件中BiNGO和MCODE插件对靶基因进行GO生物过程富集和聚类分析。结果 从防风-乌梅药对中筛选得到槲皮素、山奈酚、汉黄芩素、欧前胡素、升麻素等16个活性成分,作用于IL-6、TNF、SRC、EGFR、IL-8、PTGS2等62个荨麻疹相关靶点,调控TNF信号通路、PI3K/Akt信号通路、NF-kB信号通路、低氧诱导因子1信号通路、NOD样受体信号通路等8条信号通路,参与调节炎症反应、肽-酪氨酸磷酸化、蛋白质分解代谢等生物过程。结论 充分揭示了防风-乌梅药对多成分、多靶点、多通路治疗荨麻疹的科学内涵。     

增液汤的网络靶标预测及作用机制研究

目的 采用网络药理学方法对增液汤中活性成分的作用机制进行分析,探讨其成分、靶点及通路间的相关关系。方法 运用中药系统药理学成分分析平台（BAT-MAN）数据库获取增液汤的作用靶标基因,采用Cytoscape 3.5.1软件构建活性成分-靶点网络,STRING平台构建靶蛋白互作网络,利用BiNGO和MCODE插件对相互作用的靶基因进行GO生物过程富集和聚类分析,借助生物学信息注释数据库对靶点进行KEGG信号通路分析。结果 增液汤中23个药效成分作用于268个潜在靶点,聚类分析862个GO生物过程得到物质合成代谢、氧化应激、细胞离子平衡、炎症反应、凝血调节等23个子簇。KEGG信号通路富集主要涉及代谢、神经递质、氨基酸合成、信号转导、心血管和其他等6大类22条信号通路。结论 本研究揭示了增液汤活性成分、靶点及多维药理作用机制,为其临床治疗价值拓展提供新的线索。     

基于网络药理学和分子对接探讨三七治疗腰椎间盘突出症的作用机制

目的 运用网络药理学方法和分子对接技术预测三七治疗腰椎间盘突出症的潜在靶点及作用机制。方法 在TCMSP数据库筛选三七有效活性成分及作用靶点，构建三七“活性成分–靶点”网络。在GeneCards、OMIM数据库检索腰椎间盘突出症相关靶点，取药物与疾病交集靶点，利用String数据库构建蛋白互作（PPI）网络，通过Cytoscape 3.8.2软件构建“成分–靶点–疾病”网络图，并使用R软件进行GO富集分析和KEGG信号通路富集分析。MOE软件对有效成分与潜在靶点作分子对接验证。结果 共筛选三七治疗腰椎间盘突出症的有效活性成分8个、有效药物靶点33个，其中前列腺素内过氧化物合酶、半胱氨酸蛋白酶-3、基质金属蛋白酶9、细胞趋化因子2等靶点基因可能起着关键作用。GO富集分析选取43个条目，主要包括对脂多糖的反应、对细菌来源分子的反应等生物过程；膜筏、膜微区等细胞组分；内肽酶活性、细胞因子受体结合等分子功能。KEGG通路富集分析获得了涉及炎症、细胞凋亡、代谢、免疫、肿瘤等102个条目，其中IL-17信号通路起着关键作用。分子对接结果表明三七主要有效活性成分与核心靶点有较强的结合能力。结论 三七通过多途径、多靶点发挥治疗腰椎间盘突出症的作用。     

基于网络药理学研究白芍治疗肝纤维化的作用机制

目的 基于网络药理学方法探讨白芍治疗肝纤维化的可能作用机制。方法 使用TCMSP数据库筛选出白芍的活性成分。借助PubChem和Swiss Target Prediction数据库预测白芍有效成分的潜在作用靶点。运用GeneCards及OMIM数据库筛选肝纤维化对应靶点,利用Venn2.1.0获得白芍与肝纤维化疾病的共同靶点。使用Cytoscape3.9.0软件构建“白芍-有效成分-交集靶点-肝纤维化”网络图,预测主要活性部位,使用String数据库绘制PPI网络。利用DAVID数据库对有效作用靶点进行GO分析及Pathway中的KEGG进行富集分析。结果 筛选得到白芍有效成分6个,作用靶点213个;肝纤维化靶点155个;白芍治疗肝纤维化的靶点49个;主要活性成分是山萘酚、芍药苷、白桦脂酸及β-谷甾醇。GO富集分析显示269个生物过程、30个细胞组成、64个分子功能,KEGG通路富集分析共67条通路。结论 通过网络药理学方法初步研究白芍抗肝纤维化的作用机制,表明白芍具有多成分、多通路、多靶点等的作用特点,为进一步相关实验研究提供参考。     

基于网络药理学、分子对接及分子动力学模拟探讨黄连治疗溃疡性结肠炎的作用机制

目的 通过网络药理学、分子对接和分子动力学模拟（MD）探讨黄连治疗溃疡性结肠炎的作用机制。方法 利用TCMSP和UniProt数据库获取黄连活性成分及其对应靶点，经GeneCards、OMIM、Drugbank、TTD、DisGeNET数据库筛选溃疡性结肠炎相关靶点，利用Venny 2.1.0获取黄连和溃疡性结肠炎的交集靶点，并上传String 11.0数据库绘制蛋白相互作用（PPI）网络图。通过Cytoscape3.9.0的Cyto Hubb插件和“药物活性成分–靶点–通路网络图”筛选核心靶点。借助Metascape数据库对交集靶点进行基因本体功能注释（GO）及京都基因与基因组百科全书（KEGG）通路富集分析。通过Autodock Tools 1.5.6软件将活性成分与核心靶点进行分子对接。用分子动力学模拟法验证最佳结合模型的稳定性。结果 共筛选出黄连7个活性成分及其137个靶点，溃疡性结肠炎1 258个相关靶点和81个交集靶点。核心靶点包括蛋白激酶B1（Akt1）、B淋巴细胞2（BCL2）、有丝分裂原活化蛋白激酶1（MAPK1）等。生物过程包括无机物的反应、细胞因子受体结合等。KEGG通路富集主要包括MAPK信号通路等。分子对接结果显示，黄连的核心活性成分能够很好地与关键靶点结合。MD进一步验证了能量结合最好的小檗碱与白细胞介素（IL）-1β的结合能为−36.19 kJ/mol。结论 黄连可能通过多成分、多靶点及多通路参与溃疡性结肠炎的治疗。     

基于网络药理学的升麻治疗乳腺癌作用机制研究

目的 通过构建升麻Cimicifugae Rhizoma化学成分-靶点-代谢信号通路网络，探讨其治疗乳腺癌的作用机制。方法 利用中药系统药理学数据库与分析平台（TCMSP）和PharmMapper获取升麻化学成分与作用靶点，将其与乳腺癌疾病靶点取交集得到升麻治疗乳腺癌的作用靶点，进一步利用靶点-成分反向筛选得到治疗乳腺癌的升麻潜在活性成分；通过GeneMANIA数据库获取间接靶标和“蛋白-靶点”互作网络，并通过蛋白-蛋白相互作用筛选关键靶标；采用Cytoscape构建“成分-靶点”网络图，使用分子对接将潜在活性成分和关键靶标配对，以证实前期靶标筛选和反向药效团匹配的可靠性；通过DAVID网站对作用靶点进行基因本体论（GO）分析和京都基因与基因组百科全书（KEGG）分析，利用R语言和在线绘图网站（omishare tools）将结果可视化。结果 获得升麻潜在活性成分共68个，与乳腺癌相关疾病靶点48个，关键靶点为ESR1、SRC和HRAS。GO功能富集分析得到生物过程（BP）条目484条，细胞组成（CC）条目7条，分子功能（MF）条目75条。KEGG通路富集筛选获得到21条信号通路。分子对接结果显示关键靶标与升麻潜在活性成分匹配性较好。结论 升麻主要通过作用于ESR1、SRC、HRAS等靶点，调节癌症通路、蛋白多糖通路和雌激素信号通路等起到治疗乳腺癌的作用。     

猪肺磷脂注射液联合高频振荡通气治疗新生儿呼吸衰竭的临床研究

目的 基于网络药理学方法探讨麻杏石甘汤的主要活性成分及治疗支气管哮喘的作用机制。方法 在中药系统药理学分析平台（TCMSP）数据库中检索麻杏石甘汤的化学成分及靶点,采用Cytoscape 3.7.2软件构建活性成分-预测靶点网络图。在Genecards数据库中获取支气管哮喘疾病靶点,与药物靶点映射获得麻杏石甘汤作用于支气管哮喘的预测靶点。通过STRING数据库构建靶点相互作用网络,导入Cytoscape 3.7.2中筛选麻杏石甘汤的核心靶点。利用DAVID数据库及Cytoscape3.7.2对麻杏石甘汤的核心靶点进行KEGG信号通路和GO生物过程富集分析,并构建麻杏石甘汤活性成分-核心靶点-信号通路网络图。结果 预测结果显示,麻杏石甘汤中136个主成分可靶向98个哮喘相关靶点,关键有效成分包括麻黄碱、槲皮素、木犀草素、山柰酚等,核心靶点包括IL-6、MAPK3、TNF、TP53、VEGFA、JUN、EGFR、EGF、NOS3、CAT,涉及HIF-1、PI3K-Akt、MAPK、雌激素等71个信号通路和RNA聚合酶II启动子转录、细胞凋亡过程、ERK1和ERK2级联的正调控、上皮细胞增殖、平滑肌细胞增殖等20个生物过程。结论 初步揭示了麻杏石甘汤的药效物质基础及治疗支气管哮喘的机制,为麻杏石甘汤治疗支气管哮喘的研究提供参考。     

枸杞子治疗代谢相关脂肪性肝病机制的网络药理学研究

目的 基于网络药理学方法研究枸杞子治疗代谢相关脂肪性肝病（MAFLD,曾用名非酒精性脂肪肝）主要活性成分的作用靶点及机制。方法 通过中药系统药理学数据库（TCMSP）获取枸杞子的活性成分,设定口服生物利用度（OB）≥30%和类药性（DL）≥0.18,并筛选出枸杞子作用靶点,构建成分-靶点网络。通过GenCards数据库筛选出枸杞子治疗MAFLD的潜在作用靶点,利用Cytoscape软件构建疾病-成分-靶点可视化网络图,进行基因本体论（GO）功能分析和京都基因和基因组百科全书（KEGG）通路富集分析。结果 获得枸杞子活性成分45个,MAFLD差异基因1 656个,交集靶点87个,涉及60条通路,可能通过AKT1、IL6、IL1B等关键靶蛋白,参与DNA结合转录激活因子活性表达、RNA聚合酶Ⅱ特异性转录、肽链内切酶活性等生物学过程,枸杞子可能通过作用于IL-17信号通路、AGE-RAGE信号通路、MAFLD信号通路等发挥治疗MAFLD的作用。结论 枸杞子通过多成分、多靶点、多通路治疗MAFLD。     

基于网络药理学与分子对接技术新疆阿魏抗癌作用机制探讨

目的 采用网络药理学与分子对接技术探讨新疆阿魏Ferula sinkiangensisk抗癌的作用机制。方法 通过SymMap和SwissTargetPrediction 数据库筛选新疆阿魏的成分和靶点信息。利用 Genecards 数据库输入“cancer”关键词检索疾病的靶点;利用韦恩图获取药物-疾病的交集靶点,并借助STRING平台获取蛋白质-蛋白质相互作用（PPI）网络;利用DAVID数据库对药物-疾病的交集靶点进行基因本体（GO）富集分析和京都基因与基因组百科全书（KEGG）通路富集分析;利用Cytoscape 3.9.0软件绘制“活性成分-靶点-通路”网络图。利用 AutoDock软件对筛选出的主要活性成分及关键靶点进行分子对接实验,验证其结合活性。结果 获取新疆阿魏化学成分34个,对应靶点537个,通过筛选获得癌症靶点1 155个,药物-疾病的交集靶点134个。GO功能富集分析共获取331条条目（P＜0.05）,其中生物过程（BP）249条,细胞组成（CC）31条,分子功能（MF）51条。KEGG通路 133条,并建立活性成分-靶点-通路网络,分子对接实验表明活性物质阿魏酸、法尼斯淝醇 A、法尼斯淝醇 C、柠檬烯和 β -蒎烯与关键靶点 CCND1、JUN、CXCL8、PIK3CA 均具有较好的结合能 力 。 结论 新疆阿魏中阿魏酸、法尼斯淝醇 A、法尼斯淝醇 C、柠檬烯和 β-蒎烯等化学物质,通过 CCND1、JUN、CXCL8和PIK3CA等靶点,调节PDL-1表达和PD-1免疫检查点通路、IL-17信号通路、雌激素信号通路和PI3K-Akt信号通路等发挥抗癌作用。     

三七主要活性成分作用机制的网络药理学研究

目的 通过网络药理学研究三七的主要活性成分、作用靶点、相关信号通路和疾病等几方面的关联性，揭示其发挥药效的作用机制。方法 从中药系统药理学分析平台（TCMSP）数据库中获得三七的化学成分，并把口服生物利用度（OB）≥ 30%和类药性（DL）≥ 0.15作为筛选条件，获得三七的主要活性成分和相关作用靶点。通过UniProt数据库提取作用靶点的基因名称，并用CTD网络在线分析平台获得与靶点相关的疾病和信号通路。最后用Cytoscape 3.6.1构建"活性成分-靶点""靶点-信号通路"和"靶点-疾病"网络图，采用Cytoscape 3.6.1的Network Analyzer插件分析网络图，探讨三七的多重药理作用机制。结果 共获得槲皮素、β-谷甾醇、豆甾醇、人参皂苷rh2等9个主要活性成分；这些成分可作用于176个靶点，其主要靶点有PTGS2、PTGS1、HSP90AB1、ER、PDE3A等，这些靶点与肿瘤、高血压、中枢神经系统障碍、自身免疫疾病等45种疾病相关，涵盖癌症、心血管系统、神经系统、免疫系统等几大类疾病。三七的主要活性成分通过作用于靶点而影响相关的信号通路发挥治疗疾病的作用，其影响的信号通路主要包括信号转导通路、免疫通路、Cytokine信号通路、癌症通路等，其中肿瘤、免疫相关的占绝大部分。结论 三七是通过多成分、多靶点、多信号通路的协调作用发挥治疗疾病的作用，其中在治疗肿瘤疾病和增强人体免疫力方面具有潜在的优势。     

Synthesis and evaluation of 2,6-piperidinedione derivatives as potentially novel compounds with analgesic and other CNS activities

New 2,6-piperidinediones 2_a–g and 4_a–d were prepared by initial condensation of aromatic aldehydes or cycloalkanones with cyanoacetamide to give α-cyanocinnamides l_a–g or cycloalkylidenes 3_a,b which underwent Michae1 addition with ethyl cyanoacetate or diethylmalonate. Compounds 4_a–d were alkylated by various alkyl halides to produce the N-alkylated 2,6-piperidinedione derivatives 5_a–m. Some new selected compounds 2_a–c,f, 4_a–d & 5_e,h,j were pharmacologically evaluated for potential anticonvulsant, sedative and analgesic activities. These compounds exhibited significant anticonvulsant and analgesic effects after a single I.P. administration 100 mg/kg b.wt. . On the other hand all the investigated compounds induced hypnotic activity and prolonged the phenobarbital sodium- induced sleep as compared with the control group and the most potent compound was found to be 2_f.     

鼻渊净胶囊的HPLC指纹图谱研究

目的 建立鼻渊净胶囊的高效液相色谱(HPLC)指纹图谱.方法 采用Agilent SB-C18(4.6 mm×250 mm,5μm)色谱柱,乙腈-水为流动相、以1.0 ml/min流速行梯度洗脱,检测波长210 nm,柱温30℃,洗脱时间为80 min.采用中药色谱指纹图谱相似度评价系统(2004A版)对检测出色谱进行...     

NEURAMIDE STIMULATES ADRENOCORTICOTROPIN BUT NOT PROLACTIN RELEASE FROM RAT PITUITARY

Neuramide (NMD), a substance found in crude preparations of porcine stomach extract, is a viral inhibitor that also has putative immunostimulatory effects. The effects of NMD on stress-hormone (ACTH and prolactin—PRL) release were assessed inin vivoandin vitrostudies. In the former, blood levels of corticosterone and PRL were measured in NMD-treated male rats.In vitroexperiments were performed to evaluate the effects of NMD and three of its fractions (obtained with high performance liquid chromatography) on ACTH and PRL release from perfused rat pituitary slices. NMD increased plasma corticosterone levelsin vivoand produced dose-dependent increases inin vitropituitary release of ACTH. No effects on PRL secretion were observedin vivoorin vitro. The stimulatory effects on ACTH release were caused by the NMD fraction with a molecular weight of >5000<10000Da.     

EFFECT OF POLICOSANOL SUCCESSIVE DOSE INCREASES ON PLATELET AGGREGATION IN HEALTHY VOLUNTEERS

Policosanol is a cholesterol-lowering drug with hypocholesterolemic effects demonstrated in experimental models, healthy volunteers and type II hypercholesterolemic patients. In addition, antiplatelet effects of policosanol have been shown in experimental models and healthy volunteers. The effect of successively increasing doses of policosanol on platelet aggregation was investigated in a randomized, placebo-controlled, double-blind study conducted in 37 healthy volunteers. The volunteers were on a placebo-baseline period (two tablets per day) for 7 days and thereafter they received randomly, under double-blind conditions, placebo or policosanol (10mgday⁻¹) for 7 days. After this period dosage was doubled to 20mgday⁻¹for the next 7 days and then again doubled to 40mgday⁻¹, while the control group received placebo tablets all the time. Platelet aggregation as well as coagulation time was measured at baseline and after each dosing step. Results showed that antiplatelet effects of policosanol were successfully enhanced throughout the study, thus suggesting a dose-dependent relationship. No significant effect was reached during the first dosing period, but significant reductions of epinephrine and ADP-induced platelet aggregation were observed after the second one. Finally, a significant inhibition of platelet aggregation induced by all the agonists was observed at the last dosing step. Coagulation time remained unchanged during the trial.     

Investigation of the prevalence of tetQ, tetX and tetX1 genes in Bacteroides strains with elevated tigecycline minimum inhibitory concentrations

In this study, the antibiotic susceptibilities to tigecycline and tetracycline of 35 selected Bacteroides fragilis group strains were determined by Etest, and the presence of tetQ, tetX, tetX1 and ermF genes was investigated by polymerase chain reaction (PCR). tetQ was detected in all 12 B. fragilis group isolates (100%) exhibiting elevated tigecycline minimum inhibitory concentrations (MICs) (≥8 μg/mL) as well as the 8 strains (100%) with a tigecycline MIC of 4 μg/mL, whilst tetX and tetX1 were present in 15% and 75% of these strains, respectively. All of these strains were fully resistant to tetracycline (MIC ≥ 16 μg/mL). On the other hand, amongst the group of strains with tigecycline MICs < 4 μg/mL (15 isolates), tetQ, tetX and tetX1 were found less frequently (73.3%, 13.3% and 46.7%, respectively). All but two strains harbouring the tetQ gene in this group were non-susceptible to tetracycline, with a MIC > 4 μg/mL. These data suggest that in most cases tigecycline overcomes the tetracycline resistance mechanisms frequently observed in Bacteroides strains. However, the presence of tetX and tetX1 genes in some of the strains exhibiting elevated MICs for tigecycline draws attention to the possible development and spread of resistance to this antibiotic agent amongst Bacteroides strains. The common occurrence of ermF, tetX, tetX1 and tetQ genes together predicted the presence of the CTnDOT-like Bacteroides conjugative transposon in this collection of Bacteroides strains.     

INDIRECT PARASYMPATHOMIMETIC ACTIVITY OF THE CLASS III ANTIARRHYTHMIC SUBSTANCE / -SOTALOLIN VITRO: REVERSIBLE INHIBITION OF CHOLINESTERASE ISOENZYMES FROM BLOOD AND THE HUMAN CENTRAL NERVOUS SYSTEM

Inhibitory effects of the class III antiarrhythmic compound / -sotalol on acetylcholinesterase (AChE; EC 3.1.1.7) isoenzymes of both erythrocytes and the human caudate nucleus and on serum cholinesterase (ChE; EC 3.1.1.8) were studiedin vitrousing a spectrophotometric kinetic assay with acetylthiocholine (ASCh) as substrate. Sotalol concentrations in the assays varied from 0.32 to 3.2m . All isoenzymes studied were inhibited by / -sotalol in a reversible and concentration-dependent manner. Double reciprocal plots of the reaction velocity against varying ASCh concentrations revealed that / -sotalol reduced substrate affinity (apparent Michaelis constant, KM, increased) of serum ChE, but did not change the enzyme's maximal rate of ASCh hydrolysis (V_max). Thus, / -sotalol inhibition of serum ChE was of the competitive type (rate constant for reversible competitive inhibition: K_i=0.51m ). In contrast, / sotalol reduced the maximal reaction velocity of the AChE isoenzyme from the central nervous system (caudate nucleus), but had no influence on substrate affinity of the enzyme (K_Mwith ASCh unchanged) indicating purely non-competitive inhibition kinetics (rate constant of reversible non-competitive inhibition: K_i′=0.44m ). / -sotalol inhibition of erythrocyte AChE was of mixed competitive/non-competitive type (K_i=0.31m , K_i′=0.49m ). Non-competitive / -sotalol inhibition of caudate nucleus AChE and the non-competitive component of erythrocyte AChE inhibition cannot be overcome by increased concentrations of the cholinergic transmitter acetylcholine (ACh). Peak / -sotalol plasma levels as described in the literature for both humans (15μ ) and experimental animals (dogs: 18μ ; rats: 260μ ) as well as maximal myocardial concentrations of the substance (dogs: 46μ ; rats: 478μ ) are in the range of about 2% to 100% of the sotalol inhibition rate constants determined in the present paper for cholinesterase isoenzymesin vitro. Thus, / -sotalol inhibition of ACh hydrolysisin vivomay contribute to both the well known antiarrhythmic potential and proarrhythmic side effects of the compound.     

AMELIORIATION OF CHEMICALLY-INDUCED HEPATOCYTE INJURY BY CYCLOSPORINE A

Cyclosporine A, beside its current applications, possesses potential hepatoprotective effects. This study was directed to investigate the effect of Cyclosporine A pretreatment on hepatic injury due to carbon tetrachloride (CCl₄) and -galactosamine. Rats were injected by two successive doses of Cyclosporine A (5mgkg⁻¹day⁻¹). Six hours after the second dose, 1mlkg⁻¹of CCl₄was administered i.p. Effects associated with Cyclosporine A pretreatment were examined by using isolated hepatocytes and hepatocytes that were immobilized and continuously perfused. -Galactosamine (5m ) was added directly to the perfusion medium. After isolation, hepatocytes were examined histologically by light and electron microscopy, immobilized and perfused for further metabolic functional activity evaluation. Cyclosporine A pretreatmentin vivoproduced hepatoameliorative effects of various degrees which were statistically significant as manifested by: (1) an increased trypan blue exclusion after CCl₄; (2) an improved ureagenesis after CCl₄; (3) a reduction in the lipid droplets accumulation in the cytoplasm produced by CCl₄administration; (4) well preserved cytoplasmic organelles as mitochondria, endoplasmic reticulum ER, nuclear chromatin structures that were altered by CCl₄; and (5) an increased hepatocytes survival in the agarose gel matrix, reduction of LD leakage and improvement of ureagenesis after -galactosamine addition to the perfusion medium. The beneficial effect of Cyclosporine A pretreatment in modifying hepatotoxicity of chemical insults merits further studies.     

喙果黑面神化学成分研究

目的研究大戟科植物喙果黑面神(Breynia rostrata Merr.)的化学成分。方法利用硅胶、凝胶等色谱技术分离纯化化学成分,根据化合物的理化性质和光谱数据进行结构鉴定。结果从喙果黑面神的正丁醇萃取部分分离得到4个化合物,分别鉴定为6-O-甲基丙酰基-α-D-吡喃葡糖(6-O-methylpropanoyl-α-D-glucopyranose,1);4″-苯酚基-6-O-甲基丙酰基-β-D-吡喃葡糖苷(4″-phenolic-6-O-methylpropanoyl-β-D-glucopyranoside,2);1-O-没食子酰基-β-D-吡喃葡糖苷(1-O-galloyl-β-D-glucopyranoside,3);熊果苷(arbutin,4)。结论化合物1和2为新化合物,3和4均为首次从该种植物分离得到。     

EFFECTS OF 2-GUANIDINE-4-METHYLQUINAZOLINE ON GASTRIC ACID SECRETION IN RATS

In this study 2-guanidine-4-methylquinazoline (2-GMQ) appeared to decrease basal and stimulated gastric acid secretion, while structurally related compounds as dimethyl- biguanide, cyanoguanidine and 2-cyanoamino-4-methylpyrymidine did not. Thus, there is an antisecretory effect when the biguanide group is associated with a lipophilic structure. The antisecretive effects exerted by 2-GMQ are associated with anti H₂-histamine activity.The anti H₂-histamine nature of the effects of 2-GMQ was confirmed by the capacity of this compound of depressing the chronotropic activity of the isolated guinea pig auricle increased by histamine, as well as relaxant activity in rat uterus contracted by histamine, since both preparations are rich in H₂-histamine receptors.     

栝楼不同药用部位质量控制的研究进展

瓜蒌子、瓜蒌皮、瓜蒌、天花粉来源于栝楼的不同药用部位,4味药材均为常用的大宗药材,现行版《中国药典》对其制定的质量标准过于简单,无法科学合理地控制其质量。本文对瓜蒌子、瓜蒌皮、瓜蒌、天花粉安全性和有效组分的研究进行综述,明确了相关研究存在的问题并针对问题提出建议,为科学全面的药材及饮片标准的制定提供参考依据。