抗骨质疏松药物作用靶位分子水平研究进展

随着全国人口老龄化进程的加快，骨质疏松症的防治对于全民身体素质的提高具有重要意义，分子生物学等技术的应用，使我们在细胞分子水平上对于骨质疏松症的形成机理有了更深入的理解，本文就近年来发现的成骨细胞和破骨细胞发育，分化，增殖以及发挥功能所涉及的新通路加以介绍，希望能为寻找新型有效治疗骨质疏松药物提供作用靶点。     

抗骨质疏松药物作用靶位分子水平研究进展

1成骨细胞上的药物作用靶位多功能骨髓基质干细胞或多功能骨髓间充质干细胞(p luripotent mesenchymal stem cell,MSC)分化形成纤维样系统细胞,包括前成骨细胞、成骨细胞、成软骨细胞、成纤维细胞和网织细胞。来源于MSC的骨髓基质成纤维样系统细胞的前体细胞,在成年的哺乳动物体内分为2种:定向成骨前体细胞和可诱导成骨前体细胞。不论是MSC,还是已形成的前体细胞都可在一定条件下继续分化或被诱导分化为成熟的成骨细胞。     

几种治疗银屑病的药物

银屑病又名牛皮癣,是皮肤科的常见病和疑难病,发病机制未明,临床治疗也无特效药物,现就近年来临床治疗银屑病药物介绍如下。一、鳞屑多肽谭氏等用鳞属多肽注射液治疗银屑病465例,该药每2ml含磷屑多肽样物1 mg。     

治疗银屑病药物的临床应用

治疗银屑病药物的临床应用杨君义，高淑香，李永法（山东省临沂地区沂水中心医院临沂２７６４００）银屑病是一种慢性、反复发作、以表皮细胞过度增殖为特点的皮肤病。其病因和发病机制至今仍不十分清楚。目前研究发现，该病在遗传、免疫、生化及内分泌等方面都有异常。银...     

以细胞因子为靶点的抗哮喘药物研究进展

许多细胞因子在哮喘患者的气道慢性炎症与重构过程中起到关键作用,是抗哮喘药物的重要靶点。本文主要介绍了近年来以细胞因子（白细胞介素类、肿瘤坏死因子、嗜酸性粒细胞活化趋化因子）为靶点的抗哮喘药物最新进展和发展趋势,并就近年来涌现出的一些新的抗哮喘药物的研究进展作一综述。     

细胞因子类抗糖尿病药物研究进展

细胞因子(cytokine,CK)是免疫原、丝裂原或其他刺激剂诱导多种细胞产生的低分子量可溶性蛋白质,具有多种生物功能,其重组产物在许多疾病治疗中得到广泛应用。近年来,成纤维细胞因子、脂肪细胞因子、肠道细胞因子和表皮细胞因子等相继被报道具有一定的糖尿病治疗作用,且较少产生低血糖和体重增加等不良反应,因此越来越受到广泛关注,为糖尿病治疗提供了更多药物选择。该文对细胞因子类抗糖尿病药物的研究情况进行综述。     

药物分子设计的模拟原理

药物分子设计的模拟原理郭宗儒（中国医学科学院、中国协和医科大学药物研究所，北京１０００５０）药物分子设计是人工预建可与机体重要功能成分（蛋白质、核酸、酶、受体、离子通道等）发生作用的化学物质的分子操作，以达到防治疾病、纠正失调的机体内环境的目的。药物...     

端粒/端粒酶--抗肿瘤药物设计的新靶点

端粒是染色体末端具有TTAGGG重复序列的特殊结构，它对维护染色体完整并在细胞老化和肿瘤中起着重要作用。端粒酶是一种带有内源RNA及蛋白组分的特殊逆转录酶，研究证实它在80％－90％的肿瘤细胞中呈高水平表达，而在正常体细胞中检测不到。因此端粒／端粒酶已成为抗肿瘤药物的新靶点，综述端粒／端粒酶的结构和功能、各种有效抑制端粒／端粒酶的途径及其研究现状。     

以科研能力培养为导向的药物设计学课程教学创新与实践

在课程教学中融入新的人才培养理念,培养学生创新精神和科研能力。对教学内容、教学方法、教学手段、学生学习效果评价方法等课程教学各环节进行全面改革。探索创新性人才培养新方式,使课程教学面向新知识传授和学生综合能力培养。     

Molecular Aspects of Drug Metabolism

Abstract: Drug oxidation is linked to a liver-microsomal electron transport system consisting of at least two components - cytochrome P-450 and the NADPH-cytochrome P-450 reductase. Cytochrome P-450 is also involved in the hydroxylation of lipid-soluble endogenous compounds, such as steroid hormones and fatty acids. Substrates capable of undergoing hydroxylation bind to cytochrome P-450 and the reduction of the cytochrome P-450-substrate complex so formed may well be the rate-limiting step in the over-all hydroxylation process. It is suggested that the competitive inhibition that various substrates exert on each other's hydroxylation is due to a competition for binding to a common cytochrome P-450 species in the liver microsomes.     

浅析我院药物咨询的规范化设计与服务模式

目的:浅析我院药物咨询工作的特点,供同行交流。方法:介绍我院药物咨询工作开展规范化设计和服务模式,总结了咨询中的常见问题与解决办法。结果与结论:设计了药物咨询记录表格,统一了记录格式,规范了记录内容。咨询服务模式包括开设药物咨询门诊、电话咨询、病区用药咨询指导等。药物咨询中遇到的咨询窗口冷清问题,可通过提高宣传力度、固定时间和人员坐诊、提高药师自身技能和业务水平的方式改进;对现场不能及时回答的问题,可通过了解患者更多的用药情况和病情,在查阅相关资料后以电话回复的形式告之。     

计算机在药物研究中的综合实践课程设计与实施

作为本科生理论综合应用能力和创新能力的拓展课程,《计算机在药物研究中的综合实践》设置了复合型目标,由理论讲授-验证实验-开放式探索型实验阶段过渡,内容在理论方面注重经典、探索型实验选择方面注重前沿,采用全班集中学习和分组实验教师指导两种方式,取得较理想的教学效果。     

The Apoptosome: Emerging Insights and New Potential Targets for Drug Design

Apoptosis plays a crucial role in tissue homeostasis, development and many diseases. The relevance of Apaf1, the molecular core of apoptosome, has been underlined in mitochondria-dependent apoptosis, which according to a growing body of evidence, is involved in various pathologies where the equilibrium of life-and-death is dysregulated, such as heart attack, stroke, liver failure, cancer and autoimmune diseases. Consequently, great interest has emerged in devising therapeutic strategies for regulating the key molecules involved in the life-and-death decision. Here we review recent progress in apoptosis-based pharmacological therapies and, in particular, we point out a possible role of the apoptosome as an emerging and promising pharmacological target. Marcello D’Amelio and Elisa Tino equally contributed to this work.     

计算机辅助药物设计在药物合成中的应用

计算机辅助药物设计方法(CADD)是药物分子设计的基础。从20世纪60年代构效关系方法(QSAR)提出以后,经过40多年的努力和探索,CADD方法已经发展成为一门完善和新兴的研究领域。计算机辅助药物设计是应用量子力学、分子动力学、构效关系等基础理论数据研究药物对酶、受体等作用的药效模型,从而达到药物设计之目的。计算机辅助药物设计方法(CADD)大体可以分为三类:基于小分子的药物分子设计方法;基于受体结构的药物分子设计方法;计算组合方法。计算机辅助药物设计是研究与开发新药的一种崭新技术,它大大加快了新药设计的速度,节省了创制新药工作的人力和物力,使药物学家能够以理论作指导,有目的地开发新药。     

Liposomal Formulation of a Cytokine Restraining Agent, (CRA)-HP 228: Encapsulation, Stability, and Release Characteristics

Cytokine restraining agents (CRAs) are a family of compounds having profound anti-inflammatory properties. Among them, HP 228 is a heptapeptide, containing some unnatural amino acids, with the unique ability to restrain the pathological effects of cytokines without interfering with their essential immune functions. A liposomal formulation of HP 228 was developed to protect the drug from proteolytic enzymes and to provide controlled release of the drug. The liposomes were prepared using either dimyristoyl phosphatidylcholine or dipalmitoyl phosphatidylcholine and cholesterol by the thin-film hydration method. Dicetyl phosphate was added to the lipids to provide negative charge to the liposomes. Homogeneous size distribution of multilamellar vesicles (MLVs) was achieved by extruding them through the 800-nm polycarbonate membranes. The size distribution was characterized using a submicrometer particle size analyzer. Encapsulation efficiency of HP 228 was determined by adding protamine to MLVs and separating the supernatant from the liposome protamine aggregate. Enzymatic stability of the drug was evaluated in phosphate-buffered saline, pH 7.0 and 37°C. The studies were conducted in the presence of trypsin and chymotrypsin. The encapsulation of HP 228 increased with the increase in fatty acid chain length. Encapsulation was further increased in negatively charged liposomes compared with neutral liposomes. The encapsulation efficiency was over 50%. Also, the negative charge helped in preventing the aggregation of the liposomes and promoted the electrostatic interaction between the lipid and the drug. Encapsulating the drug in the aqueous compartment of the liposomes completely protected HP 228 from trypsin and chymotrypsin. The rate of release of HP 228 was measured using a side-by-side diffusion chamber and was found to be drastically lower from the liposomes, as compared with the drug solution, making the formulation suitable for controlled release of HP 228.     

药物制剂研究与开发研究生课程设计与实践

在新药研究开发过程中,药物制剂的设计、研究、注册及专利申请等十分重要。为了使药剂学硕士研究生毕业后能更快适应制药企业工作的需要,在药剂学硕士研究生课程体系中开设“药物制剂研究与开发”课程。结合教学实践,对该门课程的设计依据、教学内容、相关知识结构、难点重点作一简单介绍。