Natural products for human health: an historical overview of the drug discovery approaches

Natural products (NPs) are secondary metabolites produced and used by organisms for defending or adapting purposes. These molecules were naturally selected during thousands of years to improve the specificity and cover a very wide range of functions, depending on the origin, the habitat and the specific activity carried out in the organism of origin. Due to these intrinsic features, NPs have been used as healing agents since thousands of years and still today continue to be the most important source of new potential therapeutic preparations.The purpose of this review is to provide information about the historical evolution of the NPs investigation methods, focusing attention on the relative benefit/problems emerged after the improvement of the scientific investigations about them, especially over the last two centuries. Taken together, the reported information lead to the central role of NPs in the future of drug development for human needs.     

Two new phenylpropanoids from the Chinese mangrove Ceriops tagal

Two new phenylpropanoids, tagalphenylpropanoidins A-B (1–2), together with a known analogue, 2,3,6-trimethoxy-5-(1-propenyl)phenol (3), were isolated from the ethanolic extract of the Chinese mangrove Ceriops tagal. The structures of these compounds were determined by extensive spectroscopic analysis, including 1D and 2D NMR and HR-ESI-MS, as well as the comparison with data in the literature. Compound 3 was discovered from this plant for the first time. Cytotoxicities of the three compounds against MCF-7 and HL-60 cancer cell lines were also evaluated.     

Evaluation of eco-friendly compounds in the manufacturing of antibacterial papers

The papers have a porous structure which can be a suitable medium for the growth of bacteria. Therefore, in the sanitary papers, creation of a suitable antibacterial property is necessary. In this way, the plant extracts were prepared using solid–liquid extraction method from the Rosmarinus officinalis, Olea europaea, Mentha spicata and Punica granatum. Relatively, the total phenol and flavonoid contents were determined according to colorimetric method. Their antioxidant activity was evaluated using DPPH method. The extracts were sprayed on the surface of the handsheets, and then their antibacterial activity was investigated. The results showed that extracts from the P. granatum has the highest phenol (5.82%) and antioxidant activity (71.13%), while the extract from the R. officinalis had the highest flavonoid (4.23%) and antibacterial activity (90.43%). Hence, it can be concluded that these two extracts could be the suitable combinations to create desirable antibacterial properties in the manufacture of papers with sanitary purposes.     

转录物组学解析植物生长发育的生物钟调控模

基于拟南芥的时间序列的基因组芯片数据,分析了植物生长的昼夜调节模式相关的基因表达规律,发现有2.4%的基因的日振幅达到了显著差异水平.从整体基因转录组水平分析,白天诱导表达的基因主要参与调控植物与环境之间的相互作用,而夜晚表达上调的基因主要参与调节植物的生长发育.此外,植物叶绿素和血红素的生物合成也受到了生物钟的调控.对整个基因组水平上生物钟核心震荡调节子CCA1/LHY和TOC1的共表达基因做了基因组水平上的扫描鉴定,得到了一些新的潜在的生物节律调节因子.这些结果为今后更为系统地完善植物的生物节律的调控网络提供了参考.     

计及深度调峰辅助服务与多典型日的年度发电计划优化模型

在调峰市场背景下,机组调峰成本与辅助服务费用对发电企业影响较大,据此,提出了计及深度调峰辅助服务与多典型日的年度发电计划优化模型。在场景获取方面,提出了考虑负荷与风电耦合的典型场景聚类方法,有效解决了月内多个典型日场景的模拟问题。在模型方面,考虑了深度调峰成本、辅助服务补偿费用、售电利益与碳交易成本,建立了发电企业参与深度调峰辅助服务市场的收益约束,确保市场各主体能从中获利。考虑到该模型属于非线性混合整数规划模型,结合线性化策略和CPLEX求解器实现了高效求解。最后,基于修正算例系统进行了仿真分析,验证了所提模型的有效性。     

响应面法优化大比例厂拌热再生混合料参数

为对大比例厂拌热再生沥青混合料的工艺参数进行优化设计,选取再生料(reclaimed asphalt pavement, RAP)掺量,再生料预热温度,以及再生剂掺量为试验变量,选取动稳定度,低温小梁弯曲最大弯拉应变,以及冻融劈裂强度比为响应变量。使用Design-Expert软件中的Box-Behnken响应面优化设计方法,进行三因素三水平优化设计。其中,动稳定度,最大弯拉应变和冻融劈裂强度比分别作为混合料高温稳定性,低温抗裂性和水稳定性的衡量指标。再生料掺量选取20%～40%,再生料预热温度选取100～140℃,再生剂掺量选取6%～10%,响应变量均以最大值为优进行优化设计。结果表明：再生料掺量对于3个响应变量都有显著影响,而再生料预热温度和再生剂掺量对动稳定度和低温小梁弯曲最大弯拉应变有较大影响,对冻融劈裂强度比影响较小。优化得到最优解的再生料掺量为25.69%,再生料预热温度为131.59℃,再生剂掺量为8.29%。此时动稳定度为3 224.35次/mm,最大弯拉应变为2 870.37με,冻融劈裂强度比为89.230 1%。且使用优化后的工艺参数进行试验,得到的结果与预测结果...     

三氮唑类席夫碱的合成及其生物活性（Ⅱ）

合成了５种５－氨基－１Ｈ－１，２，４－三氮唑－３－羧酸的席夫碱和５种３－氨基－１Ｈ－１，２，４－三氮唑－３－羧酸的席夫碱，其中６种为新化合物，采用紫外可见光谱、红外光谱、核磁共振氢谱和元素分析对其进行了表征和分析，并对它们进行了生物活性测试，结果表明，氨基三氮唑羧酸的席夫的植物生长调节活性比氨基三氮唑席夫碱的活怀要好，杂环化合物中，含吲哚环的夫碱有较高的活性。     

河北植物区系的六新记录植物

报道了采自河北省青龙县老岭的５种和１变种河北新记录植物。它们是榛属的长苞榛ＣｏｒｙｌｕｓｈｅｔｅｒｏｐｈｙｌａＦｉｓｃｈ．ｅｘＴｒａｕｔｖ．ｖａｒ．ｓｈｅｎｙａｎｇｅｎｓｉｓＬ．ＺｈａｏｅｔＤ．Ｃｈｅｎ，缬草属的黑水缬草ＶａｌｅｒｉａｎａａｍｕｒｅｎｓｉｓＳｍｉｒ．ｅｘＫｏｍａｒｏｖ，马兰属的马兰Ｋａｌｉｍｅｒｉｓｉｎｄｉｃａ（Ｌ．）ｓｃｈ．－Ｂｉｐ．和裂叶马兰Ｋａｌｉｍｅｒｉｓｉｎｃｉｓａ（Ｆｉｓｃｈ．）ＤＣ．，灯心草属的乳头灯心草ＪｕｎｃｕｓｐａｐｉｌｏｓｕｓＦｒａｎｃｈ．ｅｔＳａｖ．以及鸢尾属的玉蝉花ＩｒｉｓｅｎｓａｔａＴｈｕｎｂ．     

植物分类学工具软件（PTT）的设计

给出了一个计算机辅助植物分类学研究的工具软件的设计方法，该软件可以帮助完成植物检索和资料查找工作，准确迅速方便，为植物分类学及其相关领域的研究提供了一种新的实用手段。