英语情侣网名Drug Discovery and Natural Products
It may be argued that drug discovery is a recent concept that evolved from modern science during the 20th century, but this concept in reality dates back many centuries, and has its origins in nature. On many occasions, humans have turned to Mother Nature for cures, and discovered unique drug molecules. Thus, the term natural product has become almost synonymous with the concept of drug discovery. In modem drug discovery and development process, natural products play an important role at the early stage of "lead" discovery, i.e. discovery of the active (determined by various bioassays) natural molecule, which itlf or its structural analogues could be an ideal drug candidate.
1.origin ['ɔridʒin] n.起点，端点; 来源；出身, 血统.
2.Synonymous [sɪ'nɔnəməs] adj.同义的，类义的.
3.i.e. [,aɪ'i:] <拉> abbr. (=id est) 即，换言之.
4.candidate ['kændidit] n.申请求职者, 候选人；报考者；候选物.
有人可能认为药物发现是一个20世纪才出现的、来源于现代科学的新概念，但是事实上这个概念是源于自然界的，可以追溯到许多个世纪以前。过去，人们常常向自然母亲寻求帮助，并且找到了分子结构独特的药物。在那时，天然产物几乎是药物发现的同义词。天然产物在现代药物发现和开发过程中也发挥着重要的作用，即作为天然活性化合物（通过各种生物检定方法）的来源，而天然活性化合物或者其结构类似物可能是很好的候选药物。
Natural products have been enormous source of drugs and drug leads. It is estimated that 61 percent of the 877 small-molecular new chemical entities introduced as drugs worldwide during 1981-2002 can be traced back to or were developed from natural products. The include natural products (6 percent), natural product derivatives (27 percent), and synthetic compounds with natural-product-derived pharmacophores (5 percent) and synthetic compounds designed on the basis of knowledge gained from a natural product, i.e. a natural product mimic (23 percent). In some therapeutic areas, the contribution of natural products is even greater, e.g. about 78 percent of antibacterials and 74 percent of anticancer drug candidates are natural products or structural analogues of natural products. In 2000, approximately 60 percent of all drugs in clinical tri
als for the multiplicity of cancers were of natural origins. In 2001, eight (simvastatin, pravastatin, amoxycillin, clavulanic acid, clarithromycin, azithromycin, ceftriaxone, cyclosporin and paclitaxel) of 30 top lling medicines were natural products or derived from natural products, and despite being neglected by the pharmaceutical companies, the eight drugs together totaled $16 billion in sales.
1. entity 部门英文['entiti] n.实体, 独立存在体, 实际存在物.
2. derivative [di'rivətiv]
n.派生物, 引出物，衍生物adj.模仿他人的; 衍生的; 派生的
3. pharmacophore ['fɑ:məkəfɔ:] n. 药效基团
4. multiplicity [,mʌlti'plisiti] n. 多样性
天然产物已经成为药物或先导化合物的重要来源。据统计，在1981年至2002年间新发现的、在全世界广泛应用的877种小分子药物中，有61%与天然产物有关或者源于天然产物。
其中直接来自于天然产物的占6%；天然产物的衍生物占27%；根据天然产物药效团合成的化合物占5%；基于对天然产物的认识设计、合成的化合物，即模拟天然产物的合成化合物，占23%。甚至于在某些治疗领域天然产物的贡献更大，例如78%的抗生素类候选药物和74%抗癌类候选药物是天然产物或其结构类似物。在2000年，进行到临床试验阶段的用于治疗多重癌的药物中，大约有60%是天然来源的。在2001年，药品销售额前30强中，源于天然产物的药物或天然产物类似物就占了8席（辛伐他汀、帕伐他汀、阿莫西林、克拉维酸、克拉霉素、阿奇霉素、头孢曲松、环孢菌素和紫杉醇）。尽管制药公司对这一点的认识尚有不足，但是这8种药物的销售总额已经达到了160亿美元。
Despite the impressive record and statistics regarding the success of natural products in drug discovery, "natural product drug discovery" has been neglected by many big pharmaceutical companies in the recent past. The declining popularity of natural products as a source of new drugs began in the 1990s, becau of some practical factors, e.g. the apparent lack of compatibility of natural products with the modern high throughput screening (HTS) programs, where significant degrees of automation, robotics and computers are ud, the complexity in the isolation and identification of natural products
and the cost and time involved in the natural product "lead" discovery process. Complexity in the chemistry of natural products, especially in the ca of novel structural types, also became the rate-determining step in drug discovery programs. Attempts to discover new drug "leads" from natural sources has never stopped, despite being neglected by the pharmaceutical companies, but continued in academia and some mi-academic rearch traditional approaches to natural product drug discovery have been applied.
1.compatibility [kəm,pætə'bɪlətɪ]
n. ① 适合，一致;互换性；通用性，兼容性②和睦相处；并存；相容
2. isolation [,aɪsə'leɪʃalthough和though的区别ən] n. 隔离, 与世隔绝
3. academia [,ækə'di:mjə] n. 学术界,学术环境
尽管统计数据表明从天然产物中发现药物这种方法非常成功，但是在刚刚过去的一些年里，这种方法还是没有引起制药业巨头的足够重视。受到一些现实原因的制约，例如天然
rip是什么意思产物的分离和鉴别是很复杂的过程，天然产物的生物活性筛选需要投入大量时间和资金，天然产物、特别是新发现的各类天然产物的化学结构的复杂性，这些显然无法与电脑程控的高度机械化、自动化的，快速的高通量筛选方式相适应，因而从20世纪90年代开始，天然来源的新药所占比例有所下降。尽管制药企业对从天然产物中发现新药的方法的重视不足，这项工作却从未停止过，科研院所和许多半学术研究团体仍在进行这项工作。
Neglected for years, natural product drug discovery appears to be drawing attention and immen interest again, and is on the verge of a comeback in the mainstream of drug discovery ventures. In recent years, a significant revival of interests in natural products as a potential source for new medicines has been obrved among academics as well as veral pharmaceutical companies. This extraordinary comeback of natural products in drug discovery rearch is mainly due to the following factors: combinatorial chemistry's promi to fill drug development pipelines with de novo synthetic small-molecular drug candidates is somewhat unsuccessful; the practical difficulties of natural product drug discovery are being overcome by advances in paration and identification technologies and in the speed and nsitivity of structure elucidation and, finally, the unique and incom
parable chemical diversity that natural products have to offer. Moreover, only a small fraction of the world's biodiversity has ever been investigated for bioactivity to date. For example, there are at least 250 000 species of higher plants that exist on this planet, but merely five to ten percent of the terrestrial plants have been investigated so far. In addition, re-investigation of previously investigated plants has continued to produce new bioactive compounds that have the potential for being developed as drugs. While veral biologically active compounds have been found in marine organisms, e.g. antimicrobial compound cephalosporin C from marine organisms (Cephalosporium acremonium and Streptomyces spp.) and antiviral compounds such as avarol and avarone from marine sponges, e.g. octopusDysidea avara, rearch in this area is still at the starting point. The following notes are the summary of the traditional as well as the modern drug discovery process involving natural products.
1. revival [rɪ'vaɪvəl] n. 复活, 再生;复兴, 再流行
2. extraordinary danee[iks'trɔ:dnəri]
adj.非常奇怪的；非同寻常的, 特别的；额外安排,临时的
基本英语单词
3. de novo [di: 'nəuvəu] n. 重新,更始
filetype4. terrestrial [tə'restri:əl]
adj. 地球的；陆地的;陆上的;陆栖的;陆生的；人间的;尘世的；
至死不渝的近义词n. 地球人;陆地生物
5. marine粗大的 [mə'ri:n]
adj. 海的, 海产的, 海生的；海军的；海事的, 海运的
n. 水兵; 海军陆战队士兵
6. organism ['ɔ:ɡənizəm] n. 有机物, 有机体; 生物；有机体系
7. cephalosporin C [,fələu'spɔ:rin] n. 头孢菌素 C
沉寂了数年之后，从天然产物中发现药物的方法重新得到了人们的极大重视，并且有了回归药物发现领域主流的趋势。近年来，从天然产物中发现新药的方法再一次得到了学术界以及许多制药企业的高度重视。天然产物在药物发现领域能够出人意料的重获重视主要有以下几个原因：人们曾对组合化学能给药物研发领域提供全合成的小分子候选药寄予厚望，但是结果不甚理想；天然产物的分离和鉴别技术的进步以及天然产物的结构确证速度和灵敏度的提升解决了天然产物中发现药物时遇到的难题；天然产物化学结构的独特性和多样性无以伦比。而且，迄今为止，在全世界的多种多样的生物中，科研人员仅对其中的一小部分进行了生物活性研究。例如，全球至少有25万中高等植物，但目前为止，仅对其中的5%－10%进行了研究。此外，对于已研究过的植物进行重新研究，往往也能发现可能被开发成药物的生物活性物质。尽管现已从海洋生物中发现了多种生物活性物质，例如从海洋生物中发现的抗生素，头孢菌素C，以及从海绵，例如贪婪倔海绵，中发现的诸如阿瓦醇和阿瓦醌这样的具有抗病毒活性的化合物，这方面的研究还处于起步阶段。下面简要介绍一下从天然产物中发现药物的传统方法和现代方法。
