临床试验中的天然产物：抗寄生虫、抗病毒和神经系统药物

本文综述了从1998年到2005年底进行临床试验或注册的抗寄生虫、抗病毒和作用于神经系统的天然产物、半合成天然产物及天然产物衍生药物。     

源于天然产物或其衍生物的分子靶向抗肿瘤药物研究进展

传统化疗药物、分子靶向药物和肿瘤免疫药物是目前用于肿瘤临床治疗的3类主要抗肿瘤药物。分子靶向抗肿瘤药物在分子水平上特异靶向在肿瘤细胞发生发展过程中的关键蛋白、基因或信号转导通路,从而选择性地杀伤肿瘤细胞或抑制其生长,具有选择性高、毒副作用小的特点,是目前抗肿瘤药物研究与开发的一个主流方向之一。天然产物是指动物、植物和微生物体内的化学成分或其代谢产物,其作为药物发现的一个重要来源,具有来源丰富和结构新颖多样的特点,目前已有多个来源于天然产物或其衍生物的分子靶向抗肿瘤药物用于肿瘤治疗或处于临床试验阶段。本文按照作用靶标分类对来源于天然产物或其衍生物的分子靶向抗肿瘤药物进行总结,并对各类药物的分子作用机制、研究进展和展望进行概述。     

用好资源 开发新药

纵观药物科学的发展进程,天然产物历来就是药物的重要来源。2000年最畅销的20个非蛋白质类药物中,有9个是从天然产物获得的先导化合物或先导化合物的衍生物研究开发而成。这9个药物的年总销售额超过160亿美元。目前,有一系列天然产物正在研究开发之中。天然产物不仅是药物的重要来源,而且在药物开发中被作为分子骨架受到关注。1995年曾作过统计,总共244个基本化学结构模型,其中83%来源于动物、植物、微生物或矿物质,仅17%出自化学合成。尽管如此,目前制药工业界在采用高通量筛选法寻找新药时,在化合物样品收集方面对天然产物仍缺乏足够重视…     

抗肿瘤植物药中同型药物的比较分析

从天然植物或生物中寻找具有抗肿瘤活性的药物组分是目前乃至今后抗肿瘤药物研究的主要途径.据报道,截止1994年,美国开发的81种新型抗肿瘤药物中,有2/3为天然植物提取物或半合成的衍生物.     

多靶点抗肿瘤天然产物研究进展

天然产物及其衍生物是抗肿瘤药物的重要组成部分.目前在临床上应用的天然产物来源的抗肿瘤药物以传统细胞毒类药物或靶向某一特定靶点的分子靶向药物为主,其应用受限于药物相关不良反应和肿瘤耐药.近年的研究表明,抗肿瘤活性天然产物往往能够靶向肿瘤细胞的多个靶点,影响肿瘤发生发展中的多个过程.由于肿瘤是一种多因素诱发的系统性疾病,多...     

抗肿瘤天然药物的研究概况

目的介绍近年来一些抗肿瘤天然药物的研究概况。方法综合最新国内外文献报道,总结抗肿瘤天然药物的研究近况。结果一些抗肿瘤天然药物及其衍生物的研究取得很大进展。结论从天然活性产物中寻找开发抗肿瘤新药具有重要意义。     

抗肿瘤天然药物的研究概况

目的介绍近年来一些抗肿瘤天然药物的研究概况。方法综合最新国内外文献报道,总结抗肿瘤天然药物的研究近况。结果一些抗肿瘤天然药物及其衍生物的研究取得很大进展。结论从天然活性产物中寻找开发抗肿瘤新药具有重要意义。     

香豆素衍生物及其抗结核活性

香豆素类化合物是一类极其重要的天然产物,广泛存在于自然界中.香豆素及其衍生物具有抗肿瘤、抗病毒、抗炎、抗氧化、抗菌和抗结核(TB)等多种生物活性,众多基于香豆素结构的药物在临床上广泛使用.近年来,香豆素及其衍生物在抗TB领域的研究引起了药物化学家的极大兴趣.药物化学家从天然产物中分离和设计合成了成千上万的香豆素衍生物,目前已从中筛选出了若干有潜力的化合物.特别值得一提的是,吡喃型香豆素类化合物(+)-Calanolide A不仅是抗HIV热点先导物,而且对药敏性和耐药性结核分枝杆菌(MTB)均显示出良好的体内外活性,无疑可用于治疗MTB/HIV双重感染患者.本文将着重探讨香豆素衍生物抗TB的构-效关系,为寻找疗效更高、毒副作用更小的香豆素类抗TB新药提供理论依据.     

海洋药物研究开发进展

新颖结构和重要生物活性天然产物的发现是创新药物开发的关键要素。海洋生物资源以其多样性、复杂性、特殊性成为新药研发中先导化合物的重要来源,截止目前基于海洋天然产物或其衍生物开发而成功上市的药物有16种,进入III期、II期、I期临床研究的活性物质分别有8、14、7种,而折戟于临床阶段的有4种;本文对其生物来源、作用机理、临床研究进展作了简要概述,期待海洋药物学科能更快、更好地发展,产生更多新药,为人类重大疾病的治疗做出重大贡献。     

海洋药物—生态功能及其应用于海洋生物药研究的展望

海洋存在大量的生物多样性品种,以往人类主要从海洋生物资源中获得蛋白质,近年来,天然产物化学家开始从大量的海洋无脊椎动物如海绵,被囊动物,苔藓虫类及其其它如海藻等发现生物活性次生代谢产物,多种该类化合物具有强生物活性如抗肿瘤并已应用于临床研究,部分化合物则具有保护植物,（如天然杀虫剂）和作为天然化妆品配方的功能,本报告将报道具有新药开发前景的海洋天然产物的发展动态。在海洋中,生物活性分子通常作为化学保护以对抗环境的不利因素如被鱼软体动物吞噬,或竞争生存空间,本文将讨论从海绵中分到的天然产物的对鱼类的强拒食活性,众所周知,海洋无脊椎动物通常于各种海洋微生物包括细胞菌,真菌或微藻共生,这些微生物可能存在于细胞外,细胞内或存在于宿主细胞的核内,从结构特征看,海洋微生物可能参加了海洋无脊椎动物的代谢过程,因此,海洋天然产物化学家开始热衷于微生物天然产物－新药研究先导化合物的新资源的研究。     

Antineoplastic agents from natural sources: achievements and future directions

The influence of natural products upon anticancer drug discovery and design cannot be overestimated. Approximately 60% of all drugs now in clinical trials for the multiplicity of cancers are either natural products, compounds derived from natural products, contain pharmacophores derived from active natural products or are 'old drugs in new clothes', where (modified) natural products are attached to targeting systems. This review covers those materials that the authors are aware of as being in clinical trials through early 2000 and demonstrates how, even today, in the presence of massive numbers of agents from combinatorial libraries, the compounds produced by 'Mother Nature' are still in the forefront of cancer chemotherapeutics as sources of active chemotypes.     

Antineoplastic agents from natural sources: achievements and future directions

The influence of natural products upon anticancer drug discovery and design cannot be overestimated. Approximately 60% of all drugs now in clinical trials for the multiplicity of cancers are either natural products, compounds derived from natural products, contain pharmacophores derived from active natural products or are ‘old drugs in new clothes’, where (modified) natural products are attached to targeting systems. This review covers those materials that the authors are aware of as being in clinical trials through early 2000 and demonstrates how, even today, in the presence of massive numbers of agents from combinatorial libraries, the compounds produced by ‘Mother Nature’ are still in the forefront of cancer chemotherapeutics as sources of active chemotypes.     

The role of pharmacognosy in modern medicine and pharmacy

This review details the contribution to modern medicine and pharmacy made by natural products and drugs derived from natural products, with an emphasis on essential medicines and new introductions to the market. Areas covered include recent advances in the development of drugs derived from marine organisms, microbes, terrestrial animals, and vascular plants, and current issues regarding botanical medicines. The role of natural products in drug discovery and development is evaluated, particularly with regard to their value as sources of drug leads with "drug-like" properties. A rationale for the success of natural products research in providing new drugs and drug prototypes is presented, drawing on lines of evidence from chemical informatics and chemical ecology. Several innovative strategies for natural products drug discovery and evaluation of botanical medicines are also reviewed.     

Plant-derived leading compounds for chemotherapy of human immunodeficiency virus (HIV) infection - an update (1998 - 2007)

The high number of citations of the previous review on anti-HIV compounds from plants published in 1998 in Planta Medica indicates the importance of natural products research in the battle against HIV. Therefore, we have decided to write an update of our previous review paper, this time covering the time span 1998 - 2007. The following antiviral chemical classes are discussed in detail: alkaloids, carbohydrates, coumarins, flavonoids, lignans, phenolics, proteins, quinones/xanthones, tannins and terpenes. If available, chemical structures, antiviral activity and selectivity, mechanism of action, and structure-activity relationship are presented.     

以非洲猪瘟病毒DNA聚合酶X为靶点的海洋药物计算机虚拟筛选

摘 要：目的 从天然产物中高效快速的筛选出一批有效针对非洲猪瘟病毒的药物苗头化合物,为寻找能抑制猪瘟蔓延的生物饲料提供线索。方法 利用计算机辅助药物设计技术,以非洲猪瘟病毒。DNA聚合酶X的DNA结合区为靶点,进行虚拟筛选,在陆生和海洋天然产物中,化合物通过文献搜索和数据库查询明确部分天然产物的来源。结果 从陆生天然产物库中筛选出16个苗头化合物,其中有5个源自中国;在海洋化合物数据库MarineChem3D中得到了59个苗头化合物,其中有8个源自中国。结论 我国境内分布有13种潜在的具抑制非洲猪瘟效果的天然产物,其中大部分来源于海洋生物。     

Cancer prevention and treatment using combination therapy with natural compounds

ABSTRACT

Introduction: Naturally occurring compounds play an essential role in the prevention and treatment of various cancers. There are more than 100 plant and animal based natural compounds currently in clinical use.

Areas covered: 1) The importance of natural products combinations in the prevention and treatment of cancer, 2) the need to maximize efficacy while minimizing side effects when using natural product combinations, and 3) specifics related to plant and animal derived natural products, as well as agents derived from natural products. Therapies using natural compounds that have been investigated, their rationale, mechanism of action and findings are reviewed. When the data warrant it, combined interventions that appear to increase efficacy (compared with monotherapy) while minimizing toxicity have been highlighted. Pubmed was used to search for relevant publications.

Expert opinion: Combination therapy with natural compounds has the potential to be more effective than single agent therapy. Similar to pharmacologic agents, the goal is to maximize efficacy while mimimizing potential side effects. There is an increasing research focus on the development of agents derived from natural products, with notable successes already achieved from the effort.     

天然产物促进药物发现（英文）

Natural products or natural product derived drugs comprised 32% of small molecule approved drugs between 1981 and 2010.In the same period of time,16% of small molecule approved drugs were synthetic or natural mimics based on the study of pharmacophores related to natural products.Indisputably,natural products provide diverse structural diversity and intricate carboskeletal frameworks.As it is believed that nature has evolved optimized biologically active compounds-the secondary metabolites-to ensure survival of the species that produce them,natural products are perceived by some to be more′drug-like′than totally synthetic compounds.As such,natural products may provide us with the′best′lead compounds yet for drug discovery,giving rise to natural product inspired drug design.This talk will provide an overview of some of my research in this area.Specifically,I will outline the challenges and some of the lessons learnt in this quest to develop natural products as leads to potential drugs.     

Potential of microalgal compounds in trending natural cosmetics: A review

Microalgae are photosynthetic organisms that produce valuable metabolites as a result of being constantly exposed to stress conditions such as high or low temperature, high salinity, osmotic pressure, photo-oxidation, and ultraviolet radiation. These valuable metabolites drew attention from cosmetic and cosmeceutical industries to be used in anti-aging, sunscreen, and skin whitening products. Microalgal secondary metabolites can have anti-blemish or anti-microbial effect; can also repair and heal skin, protect skin from UV damage, and prevent inflammation. Existing cosmetic products can be replaced by microalgae derived cosmetic products which are environment-friendly and safe which make them publicly important since people want to have products as natural as possible. Currently some microalgal derived products are commercially available and biotechnology of microalgae is getting more and more developed every day which will be resulted in more commercial products in short period of time. This review highlights the potential of microalgae species and, bioactive molecules derived by them in trending natural cosmetics with a special emphasis on application areas and production steps.