药学英语Unit 6 Text A 注释及译文

药学英语Unit 6 Text A 注释及译文
药学英语Unit 6 Text A 注释及译文

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 processes, 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 itself or its structural analogues could be an ideal drug candidate.

1.origin ['?rid?in] n.起点,端点; 来源;出身, 血统.

2.Synonymous [s?'n?n?m?s]adj.同义的,类义的.

3.i.e. [,a?'i:] <拉> abbr. (=id est) 即,换言之.

4.candidate ['k?ndidit] 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. These 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 trials 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 selling medicines were natural products or derived from natural products, and despite being neglected by the pharmaceutical companies, these eight drugs together totaled $16 billion in sales.

1. entity ['entiti] n.实体, 独立存在体, 实际存在物.

2. derivative [di'riv?tiv]

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:m?k?f?:] n.药效基团

4. multiplicity [,m?lti'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, because 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 used, 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 case 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 semi-academic research traditional approaches to natural product drug discovery have been applied.

https://www.360docs.net/doc/5a17335943.html,patibility [k?m,p?t?'b?l?t?]

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 [,a?s?'le???n]n.隔离, 与世隔绝

3. academia [,?k?'di:mj?] 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 immense 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 observed among academics as well as several pharmaceutical companies. This extraordinary comeback of natural products in drug discovery research is mainly due to the following factors: combinatorial chemistry's promise 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 separation and identification technologies and in the speed and sensitivity of structure elucidation and, finally, the unique and incomparable 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 these 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 several 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. Dysidea avara,research 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 processes involving natural products.

1. revival [r?'va?v?l] n.复活, 再生;复兴, 再流行

2. extraordinary [iks'tr?:dn?ri]

adj.非常奇怪的;非同寻常的, 特别的;额外安排,临时的

3. de novo [di: 'n?uv?u] n.重新,更始

4. terrestrial [t?'restri:?l]

adj.地球的;陆地的;陆上的;陆栖的;陆生的;人间的;尘世的;

n.地球人;陆地生物

5. marine [m?'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 ['?:ɡ?niz?m] n.有机物, 有机体; 生物;有机体系

7. cephalosporin C [,sef?l?u'sp?: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。

Natural Product Drug Discovery: the Traditional Way

In the traditional, rather more academic, method of drug discovery from natural products, drug targets are exposed to crude extracts, and in the case of a hit 1 , i.e. any evidence of activity, the extract is fractionated and the active compound is isolated and identified. Every step of fractionation and isolation is usually guided by bioassays, and the process is called bioassay-guided isolation. The following scheme presents an overview of a bioassay-guided traditional natural product drug discovery process.

1. exposed [iks'p?uzd] adj.①裸露的,暴露的,无遮蔽的;②易受攻击(或批评)的;无保护的③风险高的;很可能遭受经济损失的

2. fractionate ['fr?k??neit]

vt.把…分成几部分; (用分馏法等)分解(混合物),分馏, 分级

3. scheme [ski:m] vt. & vi.策划; 图谋n.阴谋, 诡计;计划, 方案

从天然产物中寻找药物的传统的、学术界常用的方法是将药物靶点暴露在粗提物下,如果有所发现,即发现某种生物活性,则将该粗提物分段提取,再从中分离出和鉴别活性化合物。通常情况下,分段提取和分离的每一步都是在生物检定的指导下进行的,这种方法被称为生物检定指导下的分离。下面对这种方法进行简要的图解。

Sometimes, a straightforward natural product isolation route, irrespective of bioactivity, is also applied, which results in the isolation of a number of natural compounds (small compound library) suitable for undergoing any bioactivity screening. However, the process can be slow, ineffectual and labour intensive, and it does not guarantee that a "lead" from screening would be chemically workable or even patentable.

1. irrespective [,?ris'pektiv] adj.不考虑的,不问的,不顾的

2. ineffectual[,?n?'fekt?u:?l] adj.效果不佳的,无效果的,不起作用的

有时,科研人员也会采用在不考虑生物活性的情况下从天然产物中分离化合物的方法,通过这种方法会得到数个天然化合物(小型的化合物数据库),因而适合开展各种生物活性筛选试验。但是,这种方法可能费时、费力,效率不高,而且不能保障通过生物活性筛选一定可以得到活性化合物,更不用说得到可以申请专利的活性化合物。

Natural Product Drug Discovery: the Modern Processes

Modern drug discovery approaches involve HTS, where, applying full automation and robotics, hundreds of molecules can be screened using several assays within a short time, and with very little amounts of compounds. In order to incorporate natural products in the modern HTS programs, a natural product library (a collection of dereplicated natural products) needs to be built. Dereplication is the process by which one can eliminate recurrence or re-isolation of same or similar compounds from various extracts. A number of hyphenated techniques are used for dereplication, e.g. LC-PDA (liquid chromatography-photo-diode-array detector), LC-MS (liquid chromatography-mass detector) and LC-NMR (liquid chromatography-nuclear magnetic resonance spectroscopy).

1.dereplication [di'repli'kei?n] n.去重复化

2.hyphenated ['haif?neitid] adj.带有连字符的

现代的药物发现过程要用到高通量筛选法,这种高度自动化、机械化的方法可以在短时间内完成针对百上千的化合物的多种生物活性的筛选工作,并且进行筛选仅需极少量的化合物。为使从天然产物中发现药物的方法与高通量筛选程序相适应,需要建立天然产物分子结构数据库(收集各种互不重复的天然产物结构信息的数据库)。去重复化的目的就是为了避免从各种提取物中重复的分离同一结构或者结构类似的天然化合物。去复杂化过程中要用到几种联用技术,例如液相-二极管阵列检测器联用,液相-质谱联用和液相-核磁共振联用技术。

While in the recent past it was extremely difficult, time consuming and labour intensive to build such a library from purified natural products, the situation has improved greatly with the advent of newer and improved technologies related to separation, isolation and identification of natural products. Now, it is possible to build a "high quality" and "chemically diverse" natural product library that can be suitable for any modern HTS programs. Natural product libraries can also be of crude extracts, chromatographic fractions or semi-purified compounds. However, the best result can be obtained from a fully identified pure natural product library as it provides scientists with the opportunity to handle the `lead' rapidly for further developmental work , e.g. total or partial synthesis, dealing with formulation factors, in vivo assays and clinical trials.

1.advent ['?dv?nt] n.出现, 到来

2.chromatographic[kr?um?t?'ɡr?fik] adj.色析法的,层离法的

尽管在刚刚过去的几年中,想要建立一个这样的天然产物分子结构数据库还是一项极为困难的、费时耗力的工作,随着原有的分离、纯化和鉴别技术的进步和新技术的出现,这种情况已大有改观。现在,已有可能建立高质量的、具有化学多样性的、能适应现代高通量筛选需求的数据库。天然产物的数据库也可以是粗提物,不同极性溶剂洗脱得到的色谱分段产物或半纯化化合物的数据库。当然,建立天然单体化合物的数据库对于科学家而言更有价值,因为他们可以更快的对先导化合物开展进一步的研究,例如全合成和半合成,处方研究,体内分析和临床研究。

To continue to exploit natural sources for drug candidates, the focus must be on exploiting newer approaches for natural product drug discovery. These approaches include the application of genomic tools, seeking novel sources of organisms from the environment ,new screening technologies and improved processes of sample preparation for screening samples. In addition, the recent focus on the synthesis of diversity-oriented combinatorial libraries based on natural –product-like compounds is an attempt to enhance the productivity of synthetic chemical libraries.

1.genomic[d??'n?um?k] adj.染色体组的,基因组的

2.productivity[,pr?d?k'tiviti] n.生产率,生产力

继续从自然界中发现候选药物的关键在于探索新的研究方法。这些新方法包括基因组学技术的运用,寻找自然界存在的新颖的、可作为候选药物来源的有机体,新的筛选技术应用和制备供筛选用样品的技术的改进。此外,该领域最近的研究热点是通过采用合成与天然产物结构类似的、具有结构多样性的化合物的方法提高合成法建立数据库的效率。

药学专业英语简历

个人履历 教育背景: 2002-9---2006-02 在医学院药学系学习了所有药学专业的课程。 在医院中药房、西药房、住院药房、门诊药房、药库实习。熟 悉了医院工作环境和规章制度,及相关药事管理方面的工作。 在针剂,片剂和中药车间实习。熟悉了药品生产流程,质量控 制程序等相关方面的工作。使得在销售工作中对客户提出的相 关问题能够给出专业的答案。 2006-3---2006-6 在中药室学习。增加了对药品检验,鉴定等相关实验室知识。 并在此期间完成了毕业论文的设计,获得毕业答辩“优秀论 文”评定。 证书及技能 2004.9全国计算机等级三级证书 2005.12大学英语六级证书 能够熟练使用word,excel,PPT等各种办公软件,有良好的英语基础,但是口语欠佳,平时一直在努力学习spoken english 业务经验: 2007.5 在北京丰台区组织举行产品终端宣传会议 邀请终端药店,诊所及小医院共60多家参加,宣传公司的产品, 销售政策及未来市场规划,加强客户对公司品牌的认知以及对我公 司产品市场情况反馈。 2007.7在北京顺义区组织举行产品终端宣传订货会议 邀请终端药店,诊所及小医院共88家加,对公司各主要产品进行展 示,并举行了现场订货签单。进一步加强公司产品在北京地区的宣传 和推广。 2007.8 在石家庄和保定组织二级客户终端分销工作,进行了礼品促销;加

强了同二级客户的关系,加深了二级客户对我们的信任。 2007年,全年销量做到2700多万,居普药部门首位。 2008年,开始团队建设,负责北京,唐山,保定和石家庄区域团队协作。加强管理各区域业务员的二级客户分销工作,将分销工作做得更细致,更 深入。 2009.5,在北京平谷区组织举行产品终端宣传订货会议;6月在石家庄组织二级客户终端分销工作。 2010年—至今,依然负责北京及其周边地区的销售工作。 自我评价: ◆乐观、自信、积极向上 ◆很强的学习能力,能快速接受新事物 ◆较强的执行能力、沟通能力和良好的团队合作精神 求职意向:山西运城,西安或北京地区商务代表 Resume . Certifications and Skills 2004/09 National Computer Rank Examination Certificate. 3 2005/12 College English Test-6 2008/05-2008/07 The purchases/sales License of pharmaceuticals. Skillful in Microsoft Office(Word, Excel, PowerPoint, etc); Fluently in oral English and skillful in listening、reading、writing. Assignment experience

四种翻译方法,十种翻译技巧

四种翻译方法 1.直译和意译 所谓直译,就是在译文语言条件许可时,在译文中既保持原文的内容,又保持原文的形式——特别指保持原文的比喻、形象和民族、地方色彩等。 每一个民族语言都有它自己的词汇、句法结构和表达方法。当原文的思想内容与译文的表达形式有矛盾不宜采用直译法处理时,就应采用意译法。意译要求译文能正确表达原文的内容,但可以不拘泥与原文的形式。(张培基) 应当指出,在再能确切的表达原作思想内容和不违背译文语言规范的条件下,直译有其可取之处,一方面有助于保存原著的格调,另一方面可以进新鲜的表达方法。 Literal translation refers to an adequate representation of the original. When the original coincides or almost tallies with the Chinese language in the sequence of vocabulary, in grammatical structure and rhetorical device, literal translation must be used. Free translation is also called liberal translation, which does not adhere strictly to the form or word order of the original.(郭著章) 直译法是指在不违背英语文化的前提下,在英译文中完全保留汉语词语的指称意义,求得内容和形式相符的方法。

药学英语第五版第三单元

Biochemistry Seeks to Explain Life in Chemical Terms The molecules of which living organisms are composed conform to all the familiar laws of chemistry, but they also interact with each other in accordance with another set of principles, which we shall refer to collectively as the molecular logic of life. These principles do not involve new or yet undiscovered physical laws or forces. Instead, they are a set of relationships characterizing the nature, function, and interactions of biomolecules. If living organisms are composed of molecules that are intrinsically inanimate, how do these molecules confer the remarkable combination of characteristics we call life? How is it that a living organism appears to be more than the sum of its inanimate parts? Philosophers once answered that living organisms are endowed with a mysterious and divine life force, but this doctrine (vitalism) has been firmly rejected by modern science. The basic goal of the science of biochemistry is to determine how the collections of inanimate molecules that constitute living organisms interact with each other to maintain and perpetuate life. Although biochemistry yields important insights and practical applications in medicine, agriculture, nutrition, and industry, it is ultimately concerned with the wonder of life itself. All Macromolecules Are Constructed from a Few Simple Compounds Most of the molecular constituents of living systems are composed of carbon atoms covalently joined with other carbon atoms and with hydrogen, oxygen, or nitrogen. The special bonding properties of carbon permit the formation of a great variety of molecules. Organic compounds of molecular weight less than about 500, such as amino acids, nucleotidase, and monosaccharide, serve as monomeric subunits of proteins, nucleic acids, and polysaccharides,

药学英语

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