乙酰胆碱酯酶抑制剂酶法筛选的探索研究

用Ellman法建立了用于农药的乙酰胆碱酯酶(AChE)抑制剂的离体酶筛选方法.另外,本研究结果还表明：离体与活体等多种方法的对比研究是构效关系数据库资料积累的现阶段切实可行的方法.     

靶标酶在农药研发中的作用

靶标酶在农药研发中具有极其重要的作用,大多数新开发的超高活性农药的靶标都是各种重要的代谢酶系统,了解靶标酶的作用机理,将有助于开发新型高效、低毒、专一性好的农药.综述了除草剂和杀虫剂作用于靶标酶的机理、针对专一靶标酶开发的除草剂和杀虫剂品种、昆虫和杂草产生抗药性的机制,并对新型除草剂和杀虫剂的开发前景进行了展望.     

从植物中探寻杀虫、杀菌活性物质

前言研究、开发新农药时,最重要而且最困难的是如何探寻新母体化合物。以往寻找农药活性物质,主要是采用合成大量化合物进行筛选的方法,但是成功率逐年下降。而在(植物)天然产物中寻求母体化合物,并作种种结构改变,直到现在已开发许多拟除虫菊酯类、氨基甲酸酯类杀虫剂等。它们在农药中已占独特位置。作者在(植物)天然产物中广泛寻找农药活性物     

拟除虫菊酯类农药隐忧凸显

拟除虫菊酯类农药是20世纪70年代由国外公司开发的一类仿生杀虫剂,它的开发被称为是杀虫剂农药的新突破,被誉为杀虫剂历史上的第三个里程碑。据专家推测,手性农药将成为21世纪新农药开发的热点,而手性农药杀虫剂主要集中在拟除虫菊酯类杀虫剂,     

苜蓿蚜敏感品系的纯化

农药的生物筛选和毒力测定需要选用对杀虫剂敏感的昆虫虫种,并要求被测试对象对杀虫剂的反应尽量一致(即具有稳定的遗传因子).因此,获取具有稳定遗传因子的敏感品系是农药筛选的第一步,利用苜蓿蚜能孤雌生殖的特性,通过室内多次选育和药剂筛选,培育出相对较纯的、对药剂敏感的苜蓿蚜.     

《天然产物杀虫剂——原理·方法·实践》

为了保证对环境及非靶生物的安全,从天然物中开发农药已成为当今农药研究开发的热点,由西北农业大学吴文君教授等撰写的《天然产物杀虫剂——原理·方法·实践》一书正是从理论和实践上对此类杀虫剂的总结。     

哒嗪酮类杀虫剂的研究开发概况

从天然物质中开发新颖农药已成为当今农药开发的热点，来自鱼藤酮的哒嗪酮类杀虫剂将成为杀虫剂中的一个新类别。本文介绍了哒嗪酮类杀虫剂的研究开发概况，其中包括了已商品化的及即将商品化的产品以及近期研究开发的专利情况。     

我国有机磷杀虫剂的研究开发与技术进展

有机磷杀虫剂是我国杀虫剂产品的主体,1994年其产量占杀虫剂总产量的69％,有5个骨干品种的年产量超过万t以上,在我国病虫害防治工作中发挥了相当重要的作用。有机磷杀虫剂也是我国农药生产中的主体产品,1994年其产量占农药总产量的52.6％。 近年我国有机磷杀虫剂的新品种开发主要集中在乙烯型磷酸酯、含杂环磷酸酯和不对称结构磷酸酯杀虫剂等方面。     

农药的效构关系的估量 Ⅰ.某些磷酸酯类化合物

农药杀虫剂中大量使用者为有机磷、有机氯及氨基甲酸酯三大类。由于慢性毒性的关系,有机氯已渐趋于淘汰,有机磷因无慢性积累毒性并逐步低毒化,故产量逐步上升,成为杀虫剂的主要部分,并已进入杀菌剂和除草剂的领域。目前,新的有机磷农药还在不断出现,为提高筛选新农药的效率,并设计新的农     

广谱、高效农药——噻虫嗪综述

正天然烟碱(Nicotinods)也称尼古丁,是一种存在于烟草内的一种生物碱。它具有显著的杀虫活性,在作用方式上具有触杀、胃毒、熏蒸的作用,且既能杀虫,也能杀卵。然而天然烟碱对哺乳动物、鸟类和水生动物有较高的毒性,因此它不可能成为一种高效、安全和低毒的农药产品使用。新烟碱类杀虫剂实际上是在烟碱结构研究的基础上经过开发、筛选和合成出来的一类新型的农药杀虫剂。     

核酸适配体在光生化检测中的应用

核酸适配体是一小段经体外筛选得到的寡核苷酸序列,能与相应的配体进行高亲和力和强特异性的结合。本文根据核酸适配体在检测靶物质时获得光信号的机理,将核酸适配体在光生化的检测方法进行分类,并评述了‘这些检测方法的优缺点及核酸适配体在生物检测中的发展前景。     

No time to lose--high throughput screening to assess nanomaterial safety

Nanomaterials hold great promise for medical, technological and economical benefits. Knowledge concerning the toxicological properties of these novel materials is typically lacking. At the same time, it is becoming evident that some nanomaterials could have a toxic potential in humans and the environment. Animal based systems lack the needed capacity to cope with the abundance of novel nanomaterials being produced, and thus we have to employ in vitro methods with high throughput to manage the rush logistically and use high content readouts wherever needed in order to gain more depth of information. Towards this end, high throughput screening (HTS) and high content screening (HCS) approaches can be used to speed up the safety analysis on a scale that commensurate with the rate of expansion of new materials and new properties. The insights gained from HTS/HCS should aid in our understanding of the tenets of nanomaterial hazard at biological level as well as assist the development of safe-by-design approaches. This review aims to provide a comprehensive introduction to the HTS/HCS methodology employed for safety assessment of engineered nanomaterials (ENMs), including data analysis and prediction of potentially hazardous material properties. Given the current pace of nanomaterial development, HTS/HCS is a potentially effective means of keeping up with the rapid progress in this field--we have literally no time to lose.     

纳米粒子新型诊断试剂平台开发的必要性

文章是将成熟的纳米技术与现代生物医药技术结合起来,开发新型纳米诊断试剂研究平台。这是纳米生物技术在体外诊断检测领域中的最新应用,是对体外诊断检测系统的更新换代,对提升国家生物医药科技发展水平,增强行业国际竞争力,促进检验医学的快速发展具有重要意义,在重大传染病的预防及控制、生物反恐、食品安全检测、药物高通量筛选、农牧水产检测、环保及公安等领域的生物检测中,具有迫切的市场需求和形成产业产品技术升级的巨大商机。     

化妆品功效评价(XI)——体外试验技术在发用化妆品功效评价中的应用

综述了针对头发纤维的生物物理学仪器分析技术和针对头皮的体外生物学模型在发用化妆品功效评价中的应用,为发用化妆品进行功效评价时体外方法的选择提供了参考和指导,并对目前发用化妆品体外评价技术的现状和发展趋势进行了总结和展望。     

组合催化的原理、策略与发展

介绍了组合催化的基本原理和催化剂库的高通量筛选方法;讨论了组合催化技术的2个关键因素———催化剂库的合成方法和相应的高通量检测技术在催化研究中的重要作用。综述了组合催化技术在无机、有机以及生物催化领域中的应用进展,指出进一步与计算机相结合,研究新的催化剂体系、开发新的催化剂合成技术和新的筛选技术是今后组合催化的发展方向和趋势。     

Activity‐Fed Translation (AFT) Assay: A New High‐Throughput Screening Strategy for Enzymes in Droplets

There is an increasing demand for the development of sensitive enzymatic assays compatible with droplet‐based microfluidics. Here we describe an original strategy, activity‐fed translation (AFT), based on the coupling of enzymatic activity to in vitro translation of a fluorescent protein. We show that methionine release upon the hydrolysis of phenylacetylmethionine by penicillin acylase enabled in vitro expression of green fluorescent protein. An autocatalytic setup where both proteins are expressed makes the assay highly sensitive, as fluorescence was detected in droplets containing single PAC genes. Adding a PCR step in the droplets prior to the assay increased the sensitivity further. The strategy is potentially applicable for any activity that can be coupled to the production of an amino acid, and as the microdroplet volume is small the use of costly reagents such as in vitro expression mixtures is not limiting for high‐throughput screening projects.     

化妆品功效评价(Ⅶ)——细胞生物学在化妆品功效评价中的应用

概述了细胞生物学在化妆品功效评价中的应用,对当下细胞生物学中主流研究技术在化妆品的保湿、美白、延缓衰老以及抵御污染等方面的评价应用进行了介绍,为化妆品安全与功效评价的体外替代方法提供了新思路,并展望了基于体外细胞的评价方法发展新趋势。     

Drug Screening with Genetically Encoded Fluorescent Sensors: Today and Tomorrow

Genetically-encoded fluorescent sensors have been actively developed over the last few decades and used in live imaging and drug screening. Real-time monitoring of drug action in a specific cellular compartment, organ, or tissue type; the ability to screen at the single-cell resolution; and the elimination of false-positive results caused by low drug bioavailability that is not detected by in vitro testing methods are a few of the obvious benefits of using genetically-encoded fluorescent sensors in drug screening. In combination with high-throughput screening (HTS), some genetically-encoded fluorescent sensors may provide high reproducibility and robustness to assays. We provide a brief overview of successful, perspective, and hopeful attempts at using genetically encoded fluorescent sensors in HTS of modulators of ion channels, Ca²⁺ homeostasis, GPCR activity, and for screening cytotoxic, anticancer, and anti-parasitic compounds. We discuss the advantages of sensors in whole organism drug screening models and the perspectives of the combination of human disease modeling by CRISPR techniques with genetically encoded fluorescent sensors for drug screening.     

Combinatorial chemistry methods for coating development: VI. Correlation of high throughput screening methods with conventional measurement techniques

Combinatorial chemistry has proven to be a valuable tool for the development of new compounds. In the pharmaceutical industry, where combinatorial chemistry began, the approach has been instrumental in the high-speed development of new drugs. Due to the overwhelming success of the combinatorial methodology in the pharmaceutical industry, it has been recently applied to materials development. We have recently developed a combinatorial factory capable of preparing and evaluating on the order of 100 organic clear coatings in a day.

One of the most challenging aspects of the creation of the combinatorial factory was the development of the high throughput screening (HTS) methods for the primary coating properties of interest such as optical clarity, abrasion resistance, adhesion, and weatherability. For each property, an entirely new method was developed that allowed for rapid measurement of these properties on very small samples. This paper describes various aspects of the development of these novel measurement systems including the correlation of the HTS methods with conventional, industry standard measurement methods.     

植物系统获得抗性激活剂筛选方法探讨

在植物系统获得抗性(SAR)激活剂筛选中,可采用离体测定和活体盆栽测定相结合的方法进行。在离体测定时,不同植物病原细菌和病原真菌,用平板稀释法测定药物对病原物的抑菌活体;活体盆栽测定可在待测试作物水稻、黄瓜、玉米、番茄等作物上叶面喷雾药液,并于喷药当天及3 d、1周、2周后接种植物病原细菌、真菌和病毒,置适宜条件下培养至空白对照明显发病,考察药物对各病害的防治效果。通过离体活性与盆栽效果综合分析,若无离体活性或离体活性较弱,但盆栽药效持久且有广谱效果的药物,即有可能具有SAR激活剂作用。