“十二五”国家重点图书出版规划项目《植物药活性成分大辞典》已经出版

植物中的活性成分是植物药发挥疗效的物质基础,植物活性成分研究是阐释植物药的生物活性、临床疗效和毒性的必要手段,也是新药发现和创制的可行途径,更是中药药效物质基础研究、质量控制以     

“十二五”国家重点图书出版规划项目《植物药活性成分大辞典》已经出版

植物中的活性成分是植物药发挥疗效的物质基础,植物活性成分研究是阐释植物药的生物活性、临床疗效和毒性的必要手段,也是新药发现和创制的可行途径,更是中药药效物质基础研究、质量控制以及配伍合理性及作用规律研究的前提和基础。     

甘草次酸及其衍生物TY501对小鼠巨噬细胞RAW264.7增殖的影响

植物中的活性成分是植物药发挥疗效的物质基础,植物活性成分研究是阐释植物药的生物活性、临床疗效和毒性的必要手段,也是新药发现和创制的可行途径,更是中药药效物质基础研究、质量控制以及配伍合理性及作用规律研究的前提和基础。近些年来,随着国际上     

“十二五”国家重点图书出版规划项目《植物药活性成分大辞典》（上、中、下册）

植物中的活性成分是植物药发挥疗效的物质基础,植物活性成分研究是阐释植物药的生物活性、临床疗效和毒性的必要手段,也是新药发现和创制的可行途径,更是中药药效物质基础研究、质量控制以及配伍合理性及作用规律研究的前提和基础。近些年来,随着国际上植物化学以及天然药物化学学科的迅速发展,大量的植物活性成分被研究和报道,形成大量、丰富的植物活性成分研究的信息源。但是,     

“十二五”国家重点图书出版规划项目《植物药活性成分大辞典》即将出版

植物中的活性成分是植物药发挥疗效的物质基础,植物活性成分研究是阐释植物药的生物活性、临床疗效和毒性的必要手段,也是新药发现和创制的可行途径,更是中药药效物质基础研究、质量控制以及配伍合理性及作用规律研究的前提和基础。近些年来,随着国际上     

药用植物的质量要求

本文根据德国目前植物药情况,分析了植物药质量标准的具体特点及决定植物药质量标准的因素,如:药用植物原料的质量.药用植物所含活性成分,药用植物变异性,植物栽培控制以及纯度试验等。指出了建立药用植物质量标准的条件、步骤及可行性,并设想了未来药用植物质量研究的方向和前景。     

建立植物活性成分数据库—为新药研究服务、为中药现代化服务

自古以来 ,植物药是人类防治疾病的主要天然药物。植物中的活性成分是植物产生疗效的物质基础。回顾药物的发展史和现代药物的生产 ,可以看到世界上通过植物来源的药物约占全部药物的 1 /3;全世界 3/4人口的医药保健依靠植物 ;美国 1 /3处方药来自植物。近 50年来 ,我国新化学实体的发现大多来源于植物。世界上自从长春花碱、青蒿素、紫杉醇等植物活性成分的开发成功 ,为植物新药研究展示了光明的前景。当前从植物中寻找新的活性分子或先导化合物已成为世界大制药公司竞争的新目标。进入二十一世纪 ,我国创新药物研究和中药现代化研究都将面…     

超临界二氧化碳流体萃取植物药活性成分的研究进展

目的 对超临界二氧化碳流体(SC-CO2)萃取植物药活性成分的研究进展进行综述.方法 通过检索近10年相关文献,将SC-CO2萃取植物药活性成分的研究按香豆素与木脂素、挥发油、多糖、黄酮、生物碱和单体成分进行归纳总结和讨论.结果 SC-CO2对于植物药中脂溶性活性成分具有较好的萃取效果,萃取率优于传统方法;对于植物药中...     

以DNA为作用靶追踪分离天然植物药活性成分

目的:从天然植物药中分离活性成分。方法:综述DNA与其靶向分子的作用方式以及DNA为作用靶的生物活性筛选系统跟踪分离天然植物药活性成分的情况。结果:应用DNA为作用靶的生物活性筛选系统跟踪分离天然植物药成分可快速有效地得到活性化合物。结论:DNA与其靶向分子相互作用的研究对阐述抗肿瘤、抗病毒药物及致癌物的作用机理和筛选新的药物活性成分具有重要的意义     

以DNA为作用靶追踪分离天然植物药活性成分

目的：从天然植物药中分离活性成分。方法：综述DNA与其靶向分子的作用方式以及DNA为作用靶的生物活性筛选系统跟踪分离天然植物药活性成分的情况。结果：应用DNA为作用靶的生物活性筛选系统跟踪分离天然植物药成分可快速有效地得到活性化合物。结论：DNA与其靶向分子相互作用的研究对阐述抗肿瘤，抗病毒药物及致癌物的作用机理和筛选新的药物活性成分具有重要的意义。     

喹诺酮类抗菌药的耐药性机制及研究进展

喹诺酮类抗菌药抗菌谱广,在临床上广泛应用于各种感染的治疗。喹诺酮类药物可通过阻断拓扑酶的生理功能继而干扰细菌的复制,从而起到抗菌的作用。也正是由于其广泛应用,近年来此类药物的耐药现象严重,且机制多样。综述了喹诺酮类药物的作用机制、耐药机制及其研究进展。     

武汉地区7家医院连续5年喹诺酮类药用药频度与细菌耐药性分析

目的：研究喹诺酮类抗菌药的用量与细菌耐药率之间的关系,促进临床合理用药。方法：回顾性调查武汉地区7家医院2005～2009年喹诺酮类抗菌药的用量,并与监测菌的耐药率做相关分析。结果：大多数监测菌种对喹诺酮类药的耐药率均超过30%;鲍曼不动杆菌对喹诺酮类药的耐药率随喹诺酮类药用量的变化而变化,与喹诺酮类药总用药频度高度相关。结论：喹诺酮类药对多数常见菌种的耐药率较高,其用药频度对细菌耐药性变异也有一定影响。应严格把握喹诺酮类药的临床适应证,加强对喹诺酮类药的管理,以减少或延缓细菌耐药性的发生。     

Fluorinated quinolones

Quinolones, chemically related to nalidixic acid, have a strong and rapid bactericidal action against Gram-negative bacteria, includingPs. aeruginosa, someMycobacteria, Legionella andStaphylococci. Streptococci and anaerobic bacteria are usually less sensitive. The quinolones exert their bactericidal action through inhibition of the enzyme DNA gyrase. Quinolones are absorbed for 50–100% from the gastro-intestinal tract, their volume of distribution is generally high (2 l/kg) and high concentrations are reached in almost all organs. The elimination half-lives range from 4 to 14 h. The efficacy of quinolones in urinary tract infections has been shown in many studies. They also seem to be effective in many serious infections. In animal studies their efficacy was generally equal or superior to aminoglycosides. Until now only mild and infrequent side effects have been reported.     

某教学医院肛肠疾病术后感染的病原菌特征及其耐药性分析

目的 了解肛肠疾病术后感染的病原菌分布和耐药性特征，为术后细菌性感染的诊断与治疗提供预防措施。方法 收集2016-2018年肛肠科手术患者的临床资料，分析肛肠疾病术后感染的病原菌分布特征和耐药性；应用SPSS 18.0软件进行数据分析。结果 在2714例肛肠疾病手术患者中，186例发生术后感染(6.85%)，其中痔疮92例、肛周脓肿57例、肛裂18例、肛瘘15例、肛乳头肥大3例和直肠息肉1例。从切口部位组织或分泌物中分离194株病原菌，其中革兰阴性菌121株(62.37%)，革兰阳性菌68株(35.05%)和真菌5株(2.58%)。不同肛肠疾病术后感染的病原菌种类和分离率存在较大差异。大肠埃希菌等革兰阴性菌对阿米卡星敏感，对头孢吡肟和氨苄西林/舒巴坦较敏感，对左氧氟沙星耐药率较低，对第一、二代头孢类菌素和第二代喹诺酮类抗菌药物均存在较高耐药性，但未发现亚胺培南耐药株。耐3种以上抗菌药物的革兰阴性菌47株，占革兰阴性菌38.8%。表皮葡萄球菌和金黄色葡萄球菌对利福平敏感；粪肠球菌对利福平和利奈唑胺较敏感；表皮葡萄球菌等革兰阳性菌对氨基糖苷类、喹诺酮类和青霉素类抗菌药物均有较高的耐药性，但未发现万古霉素耐药株以及利奈唑胺耐药的表皮葡萄球菌和金黄色葡萄球菌。耐3种以上抗菌药物的革兰阳性菌22株，占革兰阳性菌32.4%。 结论 肛肠疾病术后感染的病原菌主要为革兰阴性菌，临床应根据病原菌分布特征和耐药性分析，采取积极有效的针对性干预措施，降低肛肠疾病术后感染率和耐药菌的产生。     

Section Review Anti-infectives: The future role of quinolones

Quinolones, such as ciprofloxacin and ofloxacin, have gained wide acceptance for the treatment of bacterial infections of the respiratory tract, urinary tract, skin and soft tissues, as well as sexually transmitted diseases. Good pharmacokinetic profiles and potent activities against a wide range of Gram-negative and Gram-positive pathogens result in the use of these antibacterials in both hospital and community settings. Although recently developed clinical quinolones dominate in the chemotherapy of various bacterial infections, their use is restricted by limited activities against a number of clinically-important Gram-positive bacteria such as Streptococcus pneumoniae, Streptococcus pyogenes, Staphylococcus aureus, and enterococci. Ciprofloxacin, the market leader, also has low potency against anaerobes. Bacterial resistance (such as in Pseudomonas aeruginosa and methicillin-resistant Staphylococcus aureus) to ciprofloxacin is increasing rapidly. Many quinolone compounds are being synthesised to address these drawbacks. The new quinolones currently under development are characterised by enhanced activities against streptococci, staphylococci, enterococci and anaerobes. Although the treatment of traditional bacterial infections is at present the focus of quinolone research, the future role of quinolones will extend current applications to include new indications of bacterial infections and other non-bacterial diseases. This review will concentrate on the more recently developed quinolones which possess significantly more therapeutic value than existing quinolones, and will provide information on those compounds under commercial development with major therapeutic potential. Recent developments in research into the identification of quinolones for the treatment of tuberculous, cancer, viral, fungal infections and parasitic diseases will also be discussed.     

Type II topoisomerases as targets for quinolone antibacterials: turning Dr. Jekyll into Mr. Hyde

Quinolones are a very important family of antibacterial agents that are widely prescribed for the treatment of infections in humans. Although the founding members of this drug class had little clinical impact, successive generations include the most active and broad spectrum oral antibacterials currently in use. In contrast to most other anti-infective drugs, quinolones do not kill bacteria by inhibiting a critical cellular process. Rather, they corrupt the activities of two essential enzymes, DNA gyrase and topoisomerase IV, and induce them to kill cells by generating high levels of double-stranded DNA breaks. A second unique aspect of quinolones is their differential ability to target these two enzymes in different bacteria. Depending upon the bacterial species and quinolone employed, either DNA gyrase or topoisomerase IV serves as the primary cytotoxic target of drug action. While this unusual feature initially stymied development of quinolones with high activity against Gram-positive bacteria, it ultimately opened new vistas for the clinical use of this drug class. In addition to the antibacterial quinolones, specific members of this drug family display high activity against eukaryotic type II topoisomerases, as well as cultured mammalian cells and in vivo tumor models. These antineoplastic quinolones represent a potentially important source of new anticancer agents and provide an opportunity to examine drug mechanism across divergent species. Because of the clinical importance of quinolones, this review will discuss the mechanistic basis for drug efficacy and interactions between these compounds and their topoisomerase targets.     

Place of quinolones in the therapeutic armoury

On the basis of antimicrobial activity, resistance development, pharmacokinetics, side effects and pre-clinical results, the applicability of the quinolones ciprofloxacin, enoxacin, norfloxacin, ofloxacin and pefloxacin is assessed. These quinolones seem especially useful in infections in hospitalized patients, in gonococcal infections and in urinary tract infections. Also salmonellosis and shigellosis might be indications for quinolones.     

Quinolones in vitro

The first quinolone compound, nalidixic acid, showed activity against a limited number of Gram-negative micro-organisms. One step resistance developed hiin vitro and during treatment. Resistance was not mediated by transfer of R-plasmids, which is a characteristic of all quinolones. Newer quinolones like oxolinic acid, piromidic acid, cinoxacin and pipemidic acid exhibit an extended spectrum of activity against Gram-negative bacteria at lower MIC values. In recent years fluorinated quinolones were introduced like ciprofloxacin, norfloxacin, pefloxacin, ofloxacin, enoxacin and amifloxacin. These compounds exhibitin vitro a broad spectrum of activity against Gram-negative and Gram-positive bacteria at MIC values seventy to four hundred times less than those for nalidixic acid. Thein vitro activity of these compounds has been investigated in a large study of uncomplicated urinary tract infections in general practice (PINISU). No resistance was found. The fluorinated quinolones are very promising antimicrobial agents for a limited number of indications.     

辽宁锦州地区尿路感染致病菌分布及耐药性分析

目的 了解锦州地区尿路感染患者的致病菌分布及耐药性，指导临床合理用药。方法 分析2005年6月～2006年6月确诊为尿路感染的住院患者尿细菌培养及其对抗生素的耐药性。结果 分离前4位的细菌依次为大肠埃希菌（43．75％）、凝固酶阴性葡萄球菌（9．03％）、肠球菌（6．94％）、肺炎克雷伯菌（5．56％）；超广谱β-内酰胺酶（ESBLs）检出率21．43％；革兰阴性杆菌对头孢西丁、头孢哌酮、头孢他啶、头孢吡肟和亚胺培南的敏感性较好，对哌拉西林、氨苄西林、磺胺类、喹诺酮类抗生素耐药率高；革兰阳性球菌对万古霉素、利福平、呋喃妥因敏感，对头孢菌素类、青霉素类、红霉素等抗生素耐药率高。结论 分离菌株对常用抗生素耐药严重，临床应结合药敏试验和耐药菌株的报告结果，合理选择抗生素。