天然产物Combretastatin B-1的合成

该文基于Perkin反应合成了具有血管阻断及抗肿瘤活性的天然产物Combretastatin B-1(CB1)。以异香兰素为起始原料,用二溴海因对其进行选择性溴代得到2-溴-3-羟基-4-甲氧基苯甲醛(Ⅱ),该化合物与3,4,5-三甲氧基苯乙酸(Ⅲ)发生Perkin反应得到(Z/E)-2-(3,4,5-三甲氧基苯基)-3-(2'-溴-3'-乙酰氧基-4'-甲氧基)丙烯酸(Z-4、E-4),再经羟化反应及脱羧-异构化反应制备得到E-Combretastatin A-1(E-CA1),最后经催化氢化反应得到CB1,总收率为53.4%。     

雷公藤红素的结构修饰及抗肿瘤活性研究进展

雷公藤红素是一种来源于药用植物雷公藤(Tripterygium wilfordii Hook.f.)的五环三萜类天然活性产物，具有显著而广泛的抗肿瘤活性，然而，水溶性差、毒副作用强等缺点限制了其转化成为临床抗肿瘤药物。为此，通过结构修饰，改善其临床应用的局限性成为该研究领域的热点。迄今，针对其进行的结构修饰主要集中于A环C-2、C-3位，B环的C-6位及E环的28位，主要有酯化、酰胺化及引入药效基团等修饰，此外，部分非常见的修饰位点同样对抗肿瘤活性有重要影响。综述了近年来雷公藤红素的结构修饰及其抗肿瘤活性研究进展，为深入研究雷公藤红素的临床应用提供参考。     

天然产物活性组分的糖基化修饰研究进展

天然产物广泛存在于自然界中,其数量种类繁多且结构复杂多样,具有许多生理与药理活性。糖基化修饰能增加天然产物结构和功能的多样性,已成为当今新药开发的研究热点。文章归纳了不同结构类型的天然产物糖基化修饰的国内外研究现状与特点,并从糖的连接位置、数量及种类等方面描述糖基化修饰对天然产物水溶性、药理活性和生物利用率等方面的影响,为天然产物糖基化的开发与应用提供参考。     

偶联尿苷二磷酸循环体系的天然产物体外糖基化修饰

糖基化是天然产物的一种重要基团修饰,主要通过尿苷二磷酸(UDP)-糖基转移酶催化实现,而UDP-糖基供体价格昂贵限制了其应用,构建UDP-糖基供体再生系统可以有效解决该问题。本文从天然产物的体外糖基化修饰入手,阐述了糖基化修饰对天然产物功能的调控作用,比较了目前的糖基化修饰方法,其中基于UDP-糖基转移酶的生物法具备了重要的产业化应用前景。接着总结了各种UDP-糖基供体的合成方式,概述了偶联蔗糖合酶或海藻糖合酶的基于UDP循环的UDP-糖基供体再生系统,重点描述了UDP循环体系在萜类、黄酮类及其他化合物体外糖基化修饰中的应用,从而高效合成具有高附加值的天然产物糖苷化合物。指出偶联蔗糖合酶和UDP-糖基转移酶的循环体系是今后天然产物糖苷化合物合成的重要方式。     

植物天然产物氧化与微生物制造

在植物天然产物合成过程中,氧化反应是其中的关键反应,氧化酶是催化氧化反应不可或缺的生物催化剂,也是利用微生物合成植物天然产物过程中不可或缺的关键酶。介绍了萜类、生物碱、黄酮等植物天然产物骨架的氧化修饰,按照辅基的差异对合成植物天然产物过程中的氧化酶进行分类介绍,阐释了不同辅基参与氧化反应的机理。此外,还介绍了植物天然产物氧化过程在微生物合成过程中的难点,以及提高氧化酶催化效率的方法。最后,对未来合成生物学中氧化酶在微生物合成植物天然产物领域的前景进行了展望。     

天然产物化学课程问卷调查与分析

本文对我校生命科学学院20102、011届应用化学专业天然产物化学课程的教学情况进行了问卷调查。通过调查分析,对其教学效果进行检测和评价,诊断了现行教学中所存在的问题,并提出改革相应措施,提高教学质量。     

高效抗癌天然产物OSW-1及其类似物的合成进展

OSW-1是一种高效的抗癌天然产物,也是当今抗癌药物研究的热点之一。本文简要概括了近年来该药物的主要合成方法,并初步探讨了其工业生产的可行性。     

植物天然产物氧化与微生物制造

在植物天然产物合成过程中,氧化反应是其中的关键反应,氧化酶是催化氧化反应不可或缺的生物催化剂,也是利用微生物合成植物天然产物过程中不可或缺的关键酶。介绍了萜类、生物碱、黄酮等植物天然产物骨架的氧化修饰,按照辅基的差异对合成植物天然产物过程中的氧化酶进行分类介绍,阐释了不同辅基参与氧化反应的机理。此外,还介绍了植物天然产物氧化过程在微生物合成过程中的难点,以及提高氧化酶催化效率的方法。最后,对未来合成生物学中氧化酶在微生物合成植物天然产物领域的前景进行了展望。     

《天然产物化学》教学方法初步探讨

《天然产物化学》是林产化工专业一门重要的专业课程,对学生的专业知识积累和未来职业发展具有重要作用。文章对该课程的教学方法进行了初步的分析探讨,以提高学生学习兴趣和主动性,改善学习效果,培养学生创新意识。     

生物转化在天然产物化学中的研究进展

随着生物科学的不断发展,生物转化逐渐应用于天然产物化学的研究中。简介了生物转化中的几种主要的化学反应,对生物转化在天然产物化学中的应用进行了综述,并对其发展前景进行了展望。     

Impact of Histone Modifications and Their Therapeutic Targeting in Hematological Malignancies

Hematologic malignancies are a large and heterogeneous group of neoplasms characterized by complex pathogenetic mechanisms. The abnormal regulation of epigenetic mechanisms and specifically, histone modifications, has been demonstrated to play a central role in hematological cancer pathogenesis and progression. A variety of epigenetic enzymes that affect the state of histones have been detected as deregulated, being either over- or underexpressed, which induces changes in chromatin compaction and, subsequently, affects gene expression. Recent advances in the field of epigenetics have revealed novel therapeutic targets, with many epigenetic drugs being investigated in clinical trials. The present review focuses on the biological impact of histone modifications in the pathogenesis of hematologic malignancies, describing a wide range of therapeutic agents that have been discovered to target these alterations and are currently under investigation in clinical trials.     

Natural Products Targeting Amyloid Beta in Alzheimer’s Disease

Alzheimer’s disease (AD) is a neurodegenerative disease characterized by severe brain damage and dementia. There are currently few therapeutics to treat this disease, and they can only temporarily alleviate some of the symptoms. The pathogenesis of AD is mainly preceded by accumulation of abnormal amyloid beta (Aβ) aggregates, which are toxic to neurons. Therefore, modulation of the formation of these abnormal aggregates is strongly suggested as the most effective approach to treat AD. In particular, numerous studies on natural products associated with AD, aiming to downregulate Aβ peptides and suppress the formation of abnormal Aβ aggregates, thus reducing neural cell death, are being conducted. Generation of Aβ peptides can be prevented by targeting the secretases involved in Aβ-peptide formation (secretase-dependent). Additionally, blocking the intra- and intermolecular interactions of Aβ peptides can induce conformational changes in abnormal Aβ aggregates, whereby the toxicity can be ameliorated (structure-dependent). In this review, AD-associated natural products which can reduce the accumulation of Aβ peptides via secretase- or structure-dependent pathways, and the current clinical trial states of these products are discussed.     

天然气化工发展趋势及深加工产品

介绍了当代天然气化工的技术现状和发展趋势及一些天然气精细化工产品。     

天然气化工发展趋势及深加工产品（续）

介绍了当代天然气化工的现状和发展趋势及天然气精细精细化工产品。     

Chemical Genetic Screen Identifies Natural Products that Modulate Centriole Number

Centrioles are microtubule‐based organelles found in most eukaryotic cells and that are critical for the formation of cilia and flagella, as well as of centrosomes in animal cells. The number of centrioles must be strictly regulated in proliferating cells in order to ensure genome integrity upon cell division. Despite their importance, however, the mechanisms governing centriole assembly and number control remain incompletely understood, owing in part to a paucity of available small‐molecule compounds for dissection and alteration of the underlying processes. Here we have developed a chemical genetic approach to identify small‐molecule compounds capable of modulating centriole numbers in human cells. High‐throughput screening of ≈2600 natural compounds identified 14 candidate molecules that either diminish (ten compounds) or augment (four compounds) the number of centrioles per cell. We investigated the mechanisms of action of four of these compounds and discovered that two of them potentially reduce centriole number through effects on NF‐κB signalling. Moreover, we established that one further compound blocks cell cycle progression and probably indirectly causes an augmentation of centriole number. The last compound analysed induces, in addition to excess centrioles, exceptionally long primary cilia‐like structures. Overall, our analysis demonstrates that natural products constitute a rich source of tool compounds useful for unravelling and manipulating the mechanisms governing centriole assembly and number control.     

天然气化工的应用研究进展

根据天然气化工利用的两条技术路线,综述了合成气的制备方法,重点介绍了催化部分氧化制气的研究现状以及天然气直接转化为产品甲醇、乙烯与乙炔等的研究情况.     

化学筛选在微生物天然产物研究中的应用

介绍了一种在我国鲜有应用的微生物天然产物研究的系统筛选途径:化学筛选。并简要介绍了化学筛选样品的制备、数据库的建立、数据库的使用的基本知识。