研究开发中的海洋抗癌活性物质

海洋天然产物现已成为临床抗癌药物的重要来源，从didenmline B开始，进入临床研究的抗癌活性物质已经有二十多种。根据海洋来源抗癌活性物质的作用靶点不同，系统综述了正在研究中的十几种来源于海洋的天然抗癌活性物质的作用机制和研究开发情况等。     

佐米曲普坦的合成及工艺改进

目的:改进佐米曲普坦的合成工艺.方法:以(L)-苯丙氨酸为原料,经硝化,酯化,还原(酯基),环合,还原(硝基),重氮化,还原(重氮盐)和费歇尔吲哚合成共八步反应制得佐米曲普坦.结果:改进了佐米曲普坦的合成工艺,总收率提高至16%.结论:改进后的合成工艺操作简便,成本低,收率高,适于工业化生产.     

大豆异黄酮片对正常小鼠生长和免疫功能的影响

目的研究大豆异黄酮片对正常小鼠生长和免疫功能的影响。方法正常小鼠分别ig大豆异黄酮片1.5、0.5 g.kg-1或等体积空白溶剂,连续给药21 d。观察小鼠的体重及体增重,并检测其网状内皮系统(RES)的吞噬功能、ConA诱导的小鼠脾淋巴细胞的增值能力和小鼠脾脏自然杀伤细胞(NK)的活性。结果大豆异黄酮片高、低剂量组均可显著促进小鼠T淋巴细胞的增殖和NK细胞的活性,与对照组比较有显著性差异(P<0.05);而高、低剂量组小鼠的体重、体增重、吞噬指数和吞噬系数等虽高于对照组,但无统计学意义(P>0.05)。结论大豆异黄酮片具有剂量依赖性提高细胞免疫功能和NK细胞活性的作用;但对小鼠的生长和非特异性免疫功能的影响均不明显。     

参麦注射液细菌内毒素检查法的建立

目的建立参麦注射液细菌内毒素检测的方法。方法用两个生产厂家的鲎试剂对6个批号的参麦注射液分别进行干扰实验,考察确立该品种细菌内毒素的检测方法。结果参麦注射液对细菌内毒素检查有干扰作用,但稀释20倍以上可消除。结论可以用细菌内毒素检查法(凝胶法)代替家兔热原检查法控制其热原。     

Microbubbles in ultrasound-triggered drug and gene delivery

Ultrasound contrast agents, in the form of gas-filled microbubbles, are becoming popular in perfusion monitoring; they are employed as molecular imaging agents. Microbubbles are manufactured from biocompatible materials, they can be injected intravenously, and some are approved for clinical use. Microbubbles can be destroyed by ultrasound irradiation. This destruction phenomenon can be applied to targeted drug delivery and enhancement of drug action. The ultrasonic field can be focused at the target tissues and organs; thus, selectivity of the treatment can be improved, reducing undesirable side effects. Microbubbles enhance ultrasound energy deposition in the tissues and serve as cavitation nuclei, increasing intracellular drug delivery. DNA delivery and successful tissue transfection are observed in the areas of the body where ultrasound is applied after intravascular administration of microbubbles and plasmid DNA. Accelerated blood clot dissolution in the areas of insonation by cooperative action of thrombolytic agents and microbubbles is demonstrated in several clinical trials.     

Magnetic nanoparticles in MR imaging and drug delivery

Magnetic nanoparticles (MNPs) possess unique magnetic properties and the ability to function at the cellular and molecular level of biological interactions making them an attractive platform as contrast agents for magnetic resonance imaging (MRI) and as carriers for drug delivery. Recent advances in nanotechnology have improved the ability to specifically tailor the features and properties of MNPs for these biomedical applications. To better address specific clinical needs, MNPs with higher magnetic moments, non-fouling surfaces, and increased functionalities are now being developed for applications in the detection, diagnosis, and treatment of malignant tumors, cardiovascular disease, and neurological disease. Through the incorporation of highly specific targeting agents and other functional ligands, such as fluorophores and permeation enhancers, the applicability and efficacy of these MNPs have greatly increased. This review provides a background on applications of MNPs as MR imaging contrast agents and as carriers for drug delivery and an overview of the recent developments in this area of research.     

天然药物概论课程的授课规划

天然药物化学是药学专业中比较重要的专业课，该课程的内容和方法在相关领域也有一些重要的应用，所以在相关专业进行天然药物概论的教学有越来越大的需求，本文对在生物工程专业中开展天然药物概论教学所涉及的教学内容和教学方法进行了讨论。     

成人药学教育中天然药物化学的教学改革

天然药物化学课程是药学专业中一门重要的基础课程。如何针对成人药学教育对象的特殊性和学习的阶段性来优化课程讲解内容，把握教学的深度和广度，最大程度地利用有限的课堂教学时间提高学生的专业理论水平和实践能力，是天然药物化学教学工作者需要思考和实践的课题。     

胰岛素口腔黏膜喷雾剂在四氧嘧啶致糖尿病兔体内的药动学研究

目的:考察胰岛素口腔黏膜喷雾剂在糖尿病模型兔体内的药动学。方法:将36只家兔以四氧嘧啶造模成功后分为生理盐水组、胰岛素舌下喷雾给药组(低、中、高剂量)、中性胰岛素组和胰岛素皮下给药组,单剂量给药后,放免法测定胰岛素血清浓度,并计算药动学参数。结果:与生理盐水组比较,低、中、高剂量胰岛素舌下喷雾给药组的tmax和Cmax值均明显升高(P<0·01),AUC值明显增加(P<0·05或P<0·01),平均生物利用度为6·6%。胰岛素给药剂量与血中胰岛素AUC值间均呈显著线性相关(P<0·01)。结论:口腔黏膜喷雾剂可作为胰岛素皮下给药的有效替代给药途径。     

“十五”期间NSFC资助的药物代谢与药物动力学研究项目简析

该文总结了"十五"期间国家自然科学基金对药物代谢与药物动力学领域研究项目的资助情况,分析了这些项目的主要研究内容和特点,简单地总结了不足,并进行了展望。