天然抗肿瘤药物的研究进展

在天然抗肿瘤药物方面,医药专家从植物学、植物化学、药效学到毒理学等方面做了大量研究,本文就一些天然药物抗肿瘤的新研究进展作一综述.     

全球新型抗肿瘤药物研发进展及趋势

新型抗肿瘤药物已成功用于规避常规策略的某些局限性,同时提供更高的敏感性和特异性、更高的生物利用度和改善的综合治疗效果。本文总结了过去70年的抗肿瘤药物开发里程碑,综述了基于肿瘤标志性特征的14类抗肿瘤药物开发路径,并且从多学科交叉融合的视角探索了抗肿瘤药物开发中的前景。     

抗肿瘤药物的研发及市场前景

目前正在研发中的抗肿瘤药物大致可分为以下八类：     

天然抗肿瘤药物的发展趋势

通过查阅文献，回顾喜树碱和紫杉醇的开发历程，总结目前天然抗肿瘤药物的研究现状，发现天然抗肿瘤药物的发展方向可以归纳为以下几个方面。1）对现有药物进行结构改造以改善其药理学特性；2）以新的作用机理或作用靶点为指导寻找新的活性物质作为先导化合物；3）发现新的作用靶点；4）加强构效关系研究。     

抗肿瘤天然药物新剂型的研究进展

癌症是危害人类健康及生命的常见病,化疗是癌症治疗的有效手段之一,抗肿瘤天然药物是化疗药物中一个重要组成部分.近年来,随着科学技术的迅速发展,现代药剂学进入了药物传递系统(drug delivery system, DDS)时代;同样,随着越来越多的中药抗肿瘤新药的发现,对中药制剂的研究也日益深入与广泛,利用药物制剂新技术、新辅料开发中药新剂型已成为中药现代化的一个重要内容.现将近年来抗肿瘤天然药物新剂型的研究进展作一概括.     

抗肿瘤海洋生物的研究进展

海洋是人类赖以生存的资源宝库,海洋生物的多样性和特殊性,为人类提供了许多结构新颖、功能独特的生理活性物质。本文就具有抗肿瘤作用的海洋生物作一概述。     

天然药物多聚糖类抗肿瘤研究进展

天然药物中多聚糖作为具有多种生物活性的一类天然大分子化合物药理作用广泛,其抗肿瘤作用已得到各界肯定.本文通过植物多糖影响肿瘤细胞基因表达,直接抑制肿瘤细胞信号转导,诱导细胞凋亡、分化,破坏细胞结构、改变肿瘤细胞膜特性,抗氧化、清除自由基,增强免疫功能等方面对其作用机理进行综述.     

抗肿瘤药物的时辰药理学进展

目的综述抗肿瘤药物时辰药理学的相关进展,为临床合理用药提供参考。方法通过查阅国内外相关文献对肿瘤细胞生物节律及不同抗肿瘤药物的时辰药理学进行综述和分析。结果与结论肿瘤细胞生长有着节律性,因此合理应用时间治疗学的原则和方法,采取节律性给药,从而达到降低化疗药物毒性、提高疗效的目的。     

Drug discovery from natural sources

Organic compounds from terrestrial and marine organisms have extensive past and present use in the treatment of many diseases and serve as compounds of interest both in their natural form and as templates for synthetic modification. Over 20 new drugs launched on the market between 2000 and 2005, originating from terrestrial plants, terrestrial microorganisms, marine organisms, and terrestrial vertebrates and invertebrates, are described. These approved substances, representative of very wide chemical diversity, together with several other natural products or their analogs undergoing clinical trials, continue to demonstrate the importance of compounds from natural sources in modern drug discovery efforts.     

抗真菌微生物天然产物的研究进展

真菌感染疾病近年在增加．能有效治疗这种疾病的药物不多．因此．开发新的抗真菌药物成为当务之急。天然产物在新药及新药先导化合物的发现中起着重要作用。本文主要综述微生物来源的天然抗真菌药物的发展，并根据化合物作用机制将其分为细胞壁成分合成抑制剂、鞘脂类合成抑制剂、蛋白质合成抑制剂和作用于新靶点的抑制剂四类。     

长春碱类抗肿瘤药的研究进展

长春碱类抗肿瘤药已广泛应用于临床并显示出很好的疗效。综述其发现、提取分离、药理作用以及在使用过程中对其进行的结构修饰和近年来出现的新剂型,为进一步开发利用提供参考依据。     

Antimicrobial discovery from natural and unusual sources

Objectives

Whether vertebrates/invertebrates living in polluted environments are an additional source of antimicrobials.

Key findings

Majority of antimicrobials have been discovered from prokaryotes and those which are of eukaryotic origin are derived mainly from fungal and plant sources. With this in mind, it is important to note that pests, such as cockroaches come across pathogenic bacteria routinely, yet thrive in polluted environments. Other animals, such as snakes thrive from feeding on germ‐infested rodents. Logically, such species must have developed an approach to protect themselves from these pathogens, yet they have largely been ignored as a potential source of antimicrobials despite their remarkable capability to fight disease‐causing organisms.

Summary

Animals living in polluted environments are an underutilized source for potential antimicrobials, hence it is believed that several novel bioactive molecule(s) will be identified from these sources to counter increasingly resistant bacterial infections. Further research will be necessary in the development of novel antimicrobial(s) from these unusual sources which will have huge clinical impact worldwide.

     

天然产物中抗HIV生物碱类化合物的研究进展

近年来,从天然产物中寻找高效低毒的先导化合物已成筛选抗HIV药物的重要研究方向。生物碱类化合物作为一类重要的天然产物,数量众多,结构类型复杂,其中有多种抑制和阻断HIV感染的有效成分,通过实验室研究工作和临床用药观察,有望从中获得抗HIV的有效药物。以生物碱类化合物的化学结构为基础,将生物碱类化合物分为异喹啉类、喹啉类、大环类、哌啶类、莨菪烷类、吲哚类、咔唑类、海洋多环胍类、萜类、manzamine型生物碱等10类,对其抗HIV活性进行综述。     

异硫氰酸酯化合物的抗癌作用及其机制研究进展

异硫氰酸酯化合物具有不同程度的防癌、抗癌作用,其作用机制既与抑制Ⅰ相代谢酶细胞色素氧化酶P450和(或)诱导Ⅱ相代谢酶相关,也与诱导肿瘤细胞周期阻滞及细胞凋亡密切相关。     

抗肿瘤药物伊马替尼酶代谢相关的研究进展

伊马替尼是治疗慢性粒细胞白血病的一线药物,它在体内经多种CYP450酶广泛代谢,由此导致的显著个体差异以及药物相互作用,对临床治疗带来影响。从伊马替尼的代谢途径、主要代谢酶、基因多态性和药物相互作用影响进行综述,为进一步了解体内处置过程以及临床用药提供了理论依据,促进伊马替尼的临床安全、有效用药。     

Photodegradation of natural organic matter from diverse freshwater sources

Natural organic matter (NOM) is significant in determining fate, transport and toxicity of metals in aqueous systems but NOM is not a static component; NOM can undergo photochemical changes in chemical structure. These changes will modify NOM quality and in turn influence how metals are transported in the environment, as well as their toxicity to aquatic organisms. Natural organic matter was collected from five freshwater sources using a portable reverse osmosis unit, diluted to about 10 mg CL(-1), then exposed for 13 days to summer temperatures either in the dark or exposed to sunlight. Light exposed NOM had decreases in total organic carbon (TOC) of 8-35% compared to samples kept in a refrigerator (dark, 4 degrees C), and the NOM became optically lighter, as shown by specific absorbance coefficients (SAC) taken at 340 nm (55-76% decreases in SAC(340)). In contrast, dark exposed NOM showed much smaller decreases in TOC (< or = 3%) or SAC(340) (相似文献