The screening toolbox of bioactive substances from natural products: a review

Hunting lead compounds from natural products plays a vital role in finding successful drug candidates. The efficiency of screening campaigns is mainly determined by the validity of selected screening models. To screen desired lead compounds, researchers have developed a plethora of experimental screening models. However, the considerable diversity of screening models from animal models, tissue models, to cell models and so on, may cause some trouble in choosing the suitable one. This review provides a toolbox of experimental screening models that have been used to discover new drug candidates from natural products. Two screening indexes are designed for different research directions in this screening toolbox. Index I is proposed from the direction of screening different objective substance populations, including plant extracts, active fractions and pure compounds; index Π is according to screening different drug properties, including pharmacological properties, pharmacokinetic properties and affinity binding properties. We hope that the abbreviated bibliographies will help readers to quickly retrieve useful information by two screening indexes and provide certain reference value for choosing more appropriate screening models. Finally, we discuss ways of improving model systems, as well as future directions.     

Two new chalcone glycosides from the stems of Entada phaseoloides

Two new chalcone glycosides 4′-O-(6″-O-galloyl-β-d-glucopyranosyl)-2′,4-dihydroxychalcone (1) and 4′-O-(6″-O-galloyl-β-d-glucopyranosyl)-2′-hydroxy-4-methoxychalcone (2) together with one known chalcone glycoside 4′-O-β-d-glucopyranosyl-2′-hydroxy-4-methoxychalcone (3) were isolated from the stems of Entada phaseoloides. The structures of the new compounds were elucidated on the basis of extensive spectroscopic analysis, including HSQC, HMBC, ¹H–¹H COSY, and chemical evidences. This is the first report of chalcone-type compounds isolated from the genus Entada.     

Berberine attenuates lipopolysaccharide-induced impairments of intestinal glutamine transport and glutaminase activity in rat

Berberine was reported to protect against the intestinal injury and improve the survival rate in sepsis, and glutamine deficiency was considered to be correlated with mortality in sepsis. We found that berberine pretreatment ameliorated lipopolysaccharide-induced direct intestinal injury and mucosal hypoplasia and attenuated impairments of intestinal glutamine transport and glutaminase activity, B⁰AT1 mRNA and protein expressions, and glutaminase protein expression. These findings showed the first time that berberine pretreatment could improve intestinal recovery and attenuate the impairment of glutamine transport and glutaminase activity in rat sepsis. This might be one of the mechanisms for the beneficial effect of berberine on sepsis.     

外源激素对油茶种子根系及轻基质嫁接容器苗生长的影响

以良种油茶种子和嫁接苗为试验材料,设计3种外源激素处理方式,探讨外源激素对油茶种子萌发、根系生长及油茶轻基质嫁接容器苗生长的影响。结果表明:适宜的激素处理对油茶种的根系生长、出芽和轻基质嫁接容器苗的生长具有促进作用。用50mg/L ABT处理过的油茶种子根系生长迅速、主根饱满健壮、须根浓密,发根质量好,Ⅱ级根出现早,须根出现和出芽时间比对照均提前7d左右。在轻基质嫁接容器苗株高生长和地径生长上具有显著的生长优势,可以在生产中推广使用。     

Characteristics of nucleotides and amino acids in cDNA sequence of xyloglucan endotransglycosylase cloned from <Emphasis Type="Italic">Anthocephalus chinensis</Emphasis>

Xyloglucan endotransglycosylase is an identified relaxation factor with functions of easing and extending of plant cell walls.Its activities are directly related to plant growth and elongation of organisms.Anthocephalus chinensis is a tall and fast growing evergreen tree species.We cloned the full cDNA sequence of AcEXT genes which is abundantly expressed in the cambium of A.chinensis.The sequence analysis of nucleotides and amino acids revealed the presence of a 1396 bp full cDNA sequence,including a 960 bp complete open reading frame(ORF) encoding a 320 amino acid protein.The deduced amino acid sequence of AcXET was homologous to the other known XET proteins and contained the conserved EIDFE catalytic site which was specific to all the XETs.Our data should serve as a foundation for further insight into AcXET gene molecular mechanisms during wood formation and cell wall engineering of woody plants.     

不同季节断根对滇润楠根系发育的影响

滇润楠（Machilus yunnanensis）不同季节断根对比试验结果表明:滇润楠新根的萌发与断根季节的气候因素有较大关系,新根萌发时间与温度紧密相关而与湿度关系不大,根系萌发状况与断根季节的温度和降水量紧密相关,而与相对湿度和蒸发量关系不大.断根时的温度愈高,新根的萌发时间愈早;断根时的温度、降水量愈高,根系的发...     

松材线虫病综合治理技术及成效

采取专业公司3年承包机制对广东省龙眼洞林场松材线虫病进行治理,由监理单位监理,治理公司实施防治.技术措施采用综合防治法,进行检疫封锁、清除病死树、应用引诱剂和诱木剂诱杀天牛成虫、林间喷洒虫线清等,通过6年来的综合治理,发生面积逐年减少,病死树逐年下降,病死树率由2005年的25.79‰下降到2010年的0.86‰,疫情...     

Cd胁迫对灰木莲幼苗生长及某些生理特性的影响

通过对灰木莲幼苗在重金属镉(Cd)胁迫下生长与生理特征的分析,研究在镉胁迫下生长和生理特征的变化情况.结果表明,灰木莲幼苗的苗高和地径的增长率随着Cd2+浓度的增加而减少,Cd2+对苗高增长的影响较为显著;叶片的保护酶活性在低浓度下升高,在高浓度下保护酶的活性受到抑制;丙二醛浓度、游离脯氨酸含量随着镉胁迫的增加而缓慢上...     

发酵床垫料翻耙结合网床养殖改善鸭舍空气质量与鸭生产性能

为解决规模化肉鸭生产中粪污影响鸭健康和污染环境的问题,研发了一种发酵床结合网床架养新技术及其配套的可移动式网床下发酵床垫料翻耙系统,并研究了该模式在控制舍内气载微生物数量和提高鸭生产性能中的优势。结果显示:1)可移动式发酵床垫料翻耙系统实现不同发酵床体共用一台翻耙机。2)与发酵床平养相比,鸭26日龄之前未翻耙垫料时,发酵床网养舍内需氧菌总数(1.531×105 CFU/m3)和大肠杆菌数量(1.298×104 CFU/m3)显著升高(P0.05);鸭27~34日龄时每4 d翻耙垫料,发酵床网养舍内需氧菌总数(2.304×105 CFU/m3)和金黄色葡萄球菌数量(1.353×105 CFU/m3)显著降低(P0.05);鸭35~39日龄时每天翻耙垫料,发酵床网养舍内需氧菌总数(1.255×105 CFU/m3)和"沙门+志贺"氏菌数量(14.13 CFU/m3)显著降低(P0.05)。3)在发酵床平养舍内,与每4 d翻耙1次垫料相比,每天翻耙1次垫料舍内需氧菌总数(2.688×105 CFU/m3)、大肠杆菌(2.038×104 CFU/m3)、金黄色葡萄球菌(8.90×104 CFU/m3)和"沙门+志贺"氏菌(47.11 CFU/m3)数量显著(P0.05)降低,而在发酵床网养舍内,每天翻耙1次垫料舍内需氧菌总数(1.255×105 CFU/m3)和"沙门+志贺"氏菌(14.13 CFU/m3)数量显著降低(P0.05)。4)与发酵床平养相比,发酵床网养增加鸭体质量(P0.05),降低死亡率和上市淘汰率(P0.05)。结果表明研发的肉鸭养殖新模式能更好地减少舍内空气中病原菌浓度,改善鸭舍内空气环境,提高鸭生产性能。该研究为发酵床结合网床架养新模式在规模企业中推广应用提供技术支持。     

基于多目标粒子群的土地整理项目选址模型

土地整理项目选址实质上是一个多目标空间优化问题,将传统选址方法用于解决多目标土地整理项目选址存在明显不足。该文提出了一种基于多目标粒子群的土地整理项目选址模型,归纳了土地整理项目选址的选址规则,提取3个能够体现土地整理项目选址目的及意义的目标函数,即新增耕地潜力最高、空间分区集中连片、土地适宜性评价指数最高,同时考虑了土地整理项目最小新增耕地率、实施规模2类约束条件,并详细阐述了算法的核心思想、矢量编码策略、状态更新机制等内容,最后选取湖北省嘉鱼县为试验区,验证了模型的可行性和有效性,结果表明通过对目标的权重调控可以得到不同目标偏好的土地整理项目选址方案,该文所构建模型在土地整理实践中具有可操作性,提供的选址方案科学合理,为土地利用规划和土地利用调控管理提供支持。