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1.
《中国药房》2019,(11):1529-1534
目的:分析、预测甘草中黄酮类化合物的潜在药理作用及可能作用机制。方法:采用网络药理学方法,依据中药整合药理学计算平台(TCMSP)等数据库,以化合物的口服药物生物利用度(OB)>30%和类药性(DL)>0.18为标准,筛选甘草中的黄酮类化合物。采用药效团匹配与PharmMapper数据库预测其潜在的作用靶点,随后借助生物学信息注释数据库V 6.8(DAVID V 6.8)分析工具对获得的靶点蛋白进行京都基因与基因组数据库(KEGG)信号通路分析和基因本体(GO)生物过程富集分析(以P<0.05为标准判断相关),并运用Cytoscape 3.5.1软件构建甘草中黄酮类化合物-靶点蛋白-信号通路网络图。结果:共从甘草中筛选出了19个黄酮类化合物(如甘草苷、异甘草苷、甘草素等),涉及细胞视黄酸结合蛋白2、脑啡肽酶等78个靶点蛋白(共188次),以及胰岛素信号通路、磷脂酰肌醇3激酶-丝氨酸/苏氨酸激酶(PI3K-Akt)等40条信号通路(其中与癌症相关的通路8条、与内分泌系统相关的通路7条、与信号转导相关的通路6条、与传染病相关的通路5条、与代谢相关的通路3条等);所建黄酮类化合物-靶点蛋白-信号通路网络图显示,甘草中黄酮类化合物可通过多个靶点作用于不同的疾病代谢通路。结论:甘草中黄酮类化合物对癌症、内分泌系统、传染病、代谢系统等方面疾病可能具有治疗作用,且可能有潜在的抗帕金森症作用。  相似文献   

2.
目的 研究黄酮类化合物对三阴性乳腺癌(TNBC)肿瘤微环境(TME)的改善作用。方法 查阅国内外相关文献并归纳总结,综述黄酮类化合物通过影响TME对TNBC产生的作用。结果 黄酮类化合物通过不同机制,使TNBC细胞与TME相互作用,阻滞细胞周期、抑制癌细胞侵袭、转移、新血管生成和诱导细胞凋亡。结论 黄酮类化合物在TME中具有不同的抗TNBC活性,将TME作为治疗靶点的进一步研究具有重要意义。  相似文献   

3.
目的:观察10种黄酮类化合物对糖尿病致病机制中4条重要通路的多靶点抑制作用,发挥中药多靶点、综合治疗的优势。方法:从正常大鼠脑组织中提取半纯化的蛋白激酶C(PKC)、肾脏组织中提取醛糖还原酶(AR)粗酶,Fenton试剂体外激发正常大鼠脑组织脂质过氧化生成丙二醛(MDA)及体外合成高级糖化终产物(AGEs),将上述酶或合成物与10种黄酮类化合物(终浓度为1 mg.mL-1)作用,观察黄酮类化合物对上述酶或合成物的抑制作用。结果:黄芩苷和灯盏花素对AR,PKC,AGEs及MDA均有不同程度的抑制作用。结论:上述结果提示此两种黄酮类化合物可以通过抑制上述4条通路来预防糖尿病及其并发症的发生,为进一步的机制研究及临床应用提供良好的实验依据。  相似文献   

4.
《中国药房》2018,(1):58-62
目的:从黑沙蒿所含黄酮类化合物中筛选过氧化物酶体增殖物激活受体γ(PPAR-γ)的激动活性成分,为发现黑沙蒿中抗糖尿病药效物质提供参考。方法:以已知PPAR-γ激动药罗格列酮为阳性对照,采用分子对接技术对黑沙蒿中已分离得到的18个黄酮类化合物与PPAR-γ靶点进行一一分子对接,并对化合物与PPAR-γ靶点的对接亲和力、对接构象等进行分析比较,筛选黑沙蒿中可能的PPAR-γ激动活性成分。结果:有5个黄酮类化合物呈现了较好的对接亲和力,其中以化合物3(5,3′,4′-三羟基-7-甲氧基黄酮)亲和力最高(-8.3 kcal/mol);对接构象分析发现,黄酮类化合物A环与B环上的氧原子易与PPAR-γ配体结合域活性位点形成1个(Tyr327)或2个(Tyr327、Arg288)氢键结合,这对于黄酮类化合物与PPAR-γ的结合以及PPAR-γ构象的稳定起着重要作用。结论:采用分子对接技术进行的虚拟筛选结果表明,黑沙蒿中的黄酮类化合物(大多含有多个自由酚羟基)易与PPAR-γ形成较好的对接模式与较高亲和力,具有潜在抗糖尿病活性;本研究可为黑沙蒿治疗2型糖尿病的化学成分研究提供参考。  相似文献   

5.
目的研究黄酮类化合物对钙调素的拮抗作用。方法用化学实验证实并比较三种黄酮类化合物杨酶素、槲皮素、蛇葡萄素对钙调素的拮抗作用。结果三种黄酮类化合物皆对CaM-PDE激活系统有拮抗作用。结论表明三种黄酮类化合物可通过抑制钙调素而影响PDE。从以上实验表明三种黄酮类化合物皆为特异的钙调素拮抗剂。  相似文献   

6.
黄酮类化合物是一类母核为苯并吡喃酮的多酚化合物的总称,具有抗氧化、抗炎、抗肿瘤、心脑血管保护等多种生物活性。近年来研究显示,黄酮类化合物在防治良性前列腺增生中具有一定的作用。综述了黄酮类化合物防治良性前列腺增生作用机制的研究进展。  相似文献   

7.
中药黄酮类化合物药理作用及作用机制研究进展   总被引:1,自引:0,他引:1  
目的对黄酮类化合物的药理作用及其作用机制进行综述和分析。方法对近年来有关黄酮类化合物的药理作用及其作用机制的文献进行总结与分析。结果黄酮类化合物具有抗氧化、抗炎、镇痛、调节免疫、抗衰老、降血脂、抗肿瘤等药理作用,其作用机制可能与其抗自由基或抗氧化有关。结论黄酮类化合物是许多中草药的有效成分,具有广泛的生物活性,其产生生物活性的作用机制有待于进一步深入的研究。  相似文献   

8.
黄酮类化合物抗肿瘤作用及其相关机制研究进展   总被引:1,自引:0,他引:1  
赵梅  周淑琴 《中国药业》2011,20(23):1-3
黄酮类化合物种类繁多并广泛分布于自然界中,具有丰富的药理学活性。近年来,关于黄酮类化合物抗肿瘤作用的药理学研究日趋深入。大量研究结果表明,多种黄酮类化合物具有良好的体内外抗肿瘤活性,具有广阔的开发前景。该文综述了近年来国内外关于黄酮类化合物抗肿瘤作用及其相关机制的研究进展。  相似文献   

9.
黄酮类化合物抗氧化和抑菌生物活性研究进展   总被引:3,自引:0,他引:3  
陈丛瑾  王琪  李欣 《中国药房》2011,(35):3346-3348
目的:综述黄酮类化合物的抗氧化和抑菌生物活性研究进展。方法:查阅近年来公开发表的论文、专著等资料,对黄酮类化合物的抗氧化和抑菌生物活性的研究进展进行概述。结果:黄酮类化合物具有抗氧化、清除自由基和抑制细菌和真菌的作用。结论:黄酮类化合物可作为植物药开发。  相似文献   

10.
黄酮类化合物对动物实验性肝损伤保护作用的研究进展   总被引:5,自引:1,他引:5  
各种黄酮类化合物如黄酮类、黄酮醇类、二氢黄酮类、异黄酮类、黄烷酮类等对化学性肝损伤、药物性肝损伤、免疫性肝损伤、酒精性肝损伤、缺血/再灌注性肝损伤等实验性肝损伤均有不同程度的保护作用。这种保护作用与黄酮化合物清除自由基、抗氧化、抗脂质过氧化反应、调节免疫功能等有关。研究各种黄酮类化合物对动物实验性肝损伤的作用对于开发防治肝脏疾病的药物有重要意义。该文就近年来黄酮类化合物对动物实验性肝损伤作用的研究进展作一综述。  相似文献   

11.
Zhu MY  Wang RB  Zhou W  Li SS 《药学学报》2012,47(5):588-593
紫草的主要有效成分紫草素及其衍生物已被证实具有良好的抗肿瘤作用,其抗肿瘤作用机制涉及多个靶点。本文在文献报道的基础上,对紫草素及其衍生物的抗肿瘤作用及其机制进行综述。重点阐述紫草素及其衍生物在诱导细胞凋亡、诱导细胞坏死、以基质金属蛋白酶为作用靶点、作用于蛋白酪氨酸激酶、抗肿瘤血管再生等方面的抗肿瘤作用及其机制。最后对紫草素类衍生物抗肿瘤活性的研究现状进行概述,并对以紫草素为先导的抗肿瘤药物研究加以展望。  相似文献   

12.
蛋白酪氨酸激酶(PTK)抑制剂是一类作用于细胞信号转导通路的分子靶向药物,针对特定靶点发挥抗肿瘤作用。目前已有十余种蛋白酪氨酸激酶抑制剂上市,且它们在多种实体瘤的治疗中显示出较好的疗效。该文对近年来蛋白酪氨酸激酶抑制剂的研究进展做简要综述。  相似文献   

13.
《Drug discovery today》2021,26(10):2431-2438
Matching biological data sequences is one of the most interesting ways to discover new bioactive compounds. In particular, matching cell chemosensitivity with a protein expression profile can be a useful approach to predict the activity of compounds against definite biological targets. In this review, we discuss this correlation. First, we analyze case studies in which some known drugs, acting on known targets, show a good correlation between their antiproliferative activities and protein expression when a large panel of tumor cells is considered. Then, we highlight how the application of in silico methods based on the correlation between cell line chemosensitivity and gene/protein expression patterns might be a quick, cheap, and interesting approach to predict the biological activity of investigated molecules.  相似文献   

14.
Despite considerable progress in the analysis of microbial genomes, the number of validated targets suitable for the development of drugs acting on agents causing infectious diseases remains modest. The diversity of new chemical entities specific for such targets has almost not increased over the last years, while resistance to anti-infectious drugs has, in contrast, become a real threat in certain surroundings. New strategies are thus needed for selecting novel validated targets. We discuss here a combined approach which uses protein interaction mapping as the basic strategy to identify interacting domains which then serve to validate newly identified targets. The interactome of Helicobacter pylori is used as model to successively describe high-throughput protein interaction mapping, use of the H. pylori data to predict the interactome from other bacteria, analysis of interacting domains, and evaluation of the capacity of one such domain to block synthesis of flagella. The general applicability of this approach to target identification and validation, and to development of novel compounds is also discussed.  相似文献   

15.
Modern drug discovery is primarily based on the search and subsequent testing of drug candidates acting on a preselected therapeutic target. Progress in genomics, protein structure, proteomics, and disease mechanisms has led to a growing interest in and effort for finding new targets and more effective exploration of existing targets. The number of reported targets of marketed and investigational drugs has significantly increased in the past 8 years. There are 1535 targets collected in the therapeutic target database compared with approximately 500 targets reported in a 1996 review. Knowledge of these targets is helpful for molecular dissection of the mechanism of action of drugs and for predicting features that guide new drug design and the search for new targets. This article summarizes the progress of target exploration and investigates the characteristics of the currently explored targets to analyze their sequence, structure, family representation, pathway association, tissue distribution, and genome location features for finding clues useful for searching for new targets. Possible "rules" to guide the search for druggable proteins and the feasibility of using a statistical learning method for predicting druggable proteins directly from their sequences are discussed.  相似文献   

16.
17.
High density lipoprotein (HDL) has proven its role in reverse cholesterol transport and cellular cholesterol efflux thus acting as a protective factor against atherogenic cardiovascular diseases. The article focuses primarily on structure and function of genes influencing HDL metabolism. Various novel targets involve liver X receptor, retinoid X receptor, peroxisome proliferators activated receptor agonists and apoA-I mimetics. New molecules targeting these nuclear receptors are described. Phospholipid transfer protein and scavenger receptor B1 are also attractive targets in HDL metabolism. ATP-Binding Cassette transporter A1 and several lipases also play a crucial role in HDL metabolism and are very useful target for atherogenic dyslipidemia. Cholesteryl ester transfer protein inhibitors have shown great promise as possible drug candidates of future. Notably, JTT-705 (Japan Tobacco, Roche) is of great interest in spite of withdrawal of torcetrapib. Considering modest effect of currently available therapeutic options on HDL, these novel HDL elevating targets are doubtlessly the target for future atherosclerotic intervention.  相似文献   

18.
Pharmaceutical research on new anticancer drugs continues in two directions: a ‘prospective’ one involving the selection of compounds acting on ‘new’ biological targets; and a ‘conservative’ one involving the selection of chemotherapeutic agents acting on ‘validated’ targets. Clinical interest in paclitaxel (Taxol?) and docetaxel (Taxotere?) has led to a reactivation of research on agents that bind tubulin/microtubules. Several new antimitotic compounds were presented at the American Association for Cancer Research meeting in Toronto, last April.  相似文献   

19.
目的: 利用网络药理学研究泽泻汤治疗高血压的作用机制。方法: 根据ADME计算方法,利用中药系统药理学技术平台(TCMSP)等数据库、反向分子对接服务器(DRAR-CPI)、人类基因组注释数据库(Gene Cards)预测和筛选泽泻汤的活性成分及其降血压作用靶点。借助Cytoscape 3.5.1软件构建泽泻汤活性成分-作用靶点网络,借助STRING平台构建靶蛋白互作网络,通过生物学信息注释数据库(DAVID)对靶点GO生物过程及KEGG信号通路进行分析。结果: 从泽泻汤中筛选出10个活性成分,作用于136个高血压相关靶点,涉及7个主要信号通路,参与10个主要生物过程。结论: 泽泻汤通过作用于醛固酮调节钠吸收、肾素血管紧张素(RAS)系统,NO信号转导等信号通路及生物过程发挥降压作用。  相似文献   

20.
AMP-activated protein kinase AMP-activated protein kinase (AMPK AMPK ), a phylogenetically conserved serine/threonine protein kinase, is a major regulator of cellular and whole-body energy homeostasis that coordinates metabolic pathways in order to balance nutrient supply with energy demand. It is now recognized that pharmacological activation of AMPK improves blood glucose homeostasis, lipid profile, and blood pressure in insulin-resistant rodents. Indeed, AMPK activation mimics the beneficial effects of physical activity or those of calorie restriction calorie restriction by acting on multiple cellular targets. In addition, it is now demonstrated that AMPK is one of the probable (albeit indirect) targets of major antidiabetic drugs drugs including the biguanides (metformin metformin ) and thiazolidinedione thiazolidinedione s, as well as of insulin-sensitizing adipokines (e.g., adiponectin adiponectin ). Taken together, such findings highlight the logic underlying the concept of targeting the AMPK pathway for the treatment of metabolic syndrome and type 2 diabetes.  相似文献   

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