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.     

九江市林业产权制度改革现状分析与建议

江西省是我国南方重要的集体林区之一,九江市作为江西省的林业大市,其林业在九江社会经济发展中占有重要地位。九江市林权制度改革时间较早,2004年在武宁县开始试点后推开,2007年主体改革结束,并通过江西省林权制度改革领导小组的全面检查验收。笔者通过对九江市林权制度改革现状进行分析,指出林权制度改革中出现的问题,从龙头企业...     

Alteration of glutathione S-transferase properties during the development of <Emphasis Type="Italic">Micromelalopha troglodyta</Emphasis> larvae (Lepidoptera: Notodontidae)

Micromelalopha troglodyta (Graeser) is an important pest of poplar in China. Glutathione S-transferases (GSTs) are known to be responsible for adaptation mechanisms of M. troglodyta. The activities and kinetic constants of glutathione S-transferases in M. troglodyta were studied. Significant differences in glutathione S-transferase activity and kinetic characteristics were observed among five instars of M. troglodyta larvae. Furthermore, the inhibition of glutathione S-transferase activity in five instars by 24 inhibitors was conducted. The results show the inhibition of GST activity of different instars by 24 inhibitors was different. For GST activity in the 1st instar, chlorpyrifos, lambda-cyhalothrin, endosulfan, abamectin, fipronil and pyridaben were the best inhibitors tested, and for GST activity in the 2nd instar, tannic acid and quercetin were the most potent inhibitors tested, and for GST activity in the 3rd instar, the inhibitory effects of quercetin, chlorpyrifos and lambda-cyhalothrin were the highest, and for GST activity in the 4th instar, quercetin and lambda-cyhalothrin were the best inhibitors, and the inhibitory effect of phoxim was the highest for GST activity in the 5th instar. Our results show that glutathione S-transferases in different instars are qualitatively different in isozyme composition and thus different in sensitivity to inhibitors.     

陕西省几种代表性土壤NH4+吸附、解吸动力学特征研究

采用连续液流法测定了五种土壤吸附、解吸ＮＨ＾＋４的动力学性质。研究表明：（１）ＮＨ＾＋４吸附、解吸平衡时间及反应速率，平衡时的吸附、解吸量及吸附平衡常数均随土壤粘粒和ＣＥＣ不同而变化；（２）不同动力学模型及同一模型对不同土壤的拟合性不同。     

进入21世纪中国畜牧业结构调整的思路与对策

进入21世纪中国将努力成为一个工业化的现代强国。面对经济全球一体化进程的加快趋势，中国畜牧业应充分认识到，进入21世纪我国畜牧业结构调整的现状、地位和战略；找准进入21世纪影响中国畜牧业结构调整与发展的原因以及制约因素；对进入21世纪中国畜牧业结构调整的发展，要加大力度，采取相应的对策，进一步提高中国畜牧业的整体利益和国际竞争力，增加农民收入，促进农业和农村经济再上新台阶。     

膨润土改善鸡粪厌氧消化产酸产甲烷特性

为探究膨润土对鸡粪厌氧消化过程中产甲烷特性和可溶性有机酸代谢特性的影响,采用L8(23)正交试验设计,以鸡粪添加量(有机负荷率)、膨润土添加量和接种量为三因素,每个因素设置2个水平,研究了中温条件下(35±1)℃膨润土添加对鸡粪厌氧消化过程中产酸和产甲烷特性的影响。结果表明:与对照组相比,低有机负荷条件下,膨润土添加能显著(P0.05)提高鸡粪挥发性固体(volatile solid,VS)产甲烷量,添加量为3.0%和1.5%时VS产甲烷量分别提升了22.72%、27.72%(膨润土添加量不同的组差异不显著(P0.05));高有机负荷条件下,膨润土添加能极显著(P0.01)提高鸡粪VS产甲烷量,添加量为3.0%和1.5%时VS产甲烷量分别提升了78.68%和55.41%(膨润土添加量不同的组差异显著(P0.05))。当鸡粪添加量为19.91 g挥发性固体,膨润土添加量为3.0%(占干基比)和接种量为80 m L(体积分数20%)时,单位挥发性固体产甲烷量最高为301.92 m L/g,比对照组高87.8%,此时可变成本也最低为2.43元/m~3,比两对照组分别低1.29和1.68元/m~3。方差分析表明:膨润土添加可提高鸡粪厌氧消化过程中挥发性脂肪酸,pH值,可溶性有机碳和可溶性无机碳的稳定性。膨润土可加强鸡粪厌氧消化系统的稳定性,降低产甲烷的可变成本,为膨润土强化鸡粪厌氧处理提供了试验验证据。     

实体水-虚拟水"二维三元"耦合流动理论基本框架

在变化环境下,区域水资源系统演变规律正在发生深刻变化。解决新形势下出现的水问题单单依靠传统的实体水资源规划、调度和调控手段还不够。虚拟水概念和理论的提出拓展了水文水资源的认知范畴,丰富了水问题的解决手段。然而,如何搭建虚拟水理论与传统水文水资源认知体系的统一框架,认识自然-经济-社会连续系统中水资源演化的新规律,目前学界还没有成熟统一的看法。该文首先提出了实体水-虚拟水耦合流动效应的基本理论框架,指出实体水-虚拟水耦合流动是现代环境下自然-经济-社会水资源系统呈现的新特征。其次,从文明进步和生产力发展角度,论述了人类社会水文水资源系统的演化历史,将水文水资源系统演进大体分为三个阶段:早期的实体水"一维一元"自然循环阶段,近现代的实体水"二元"水循环阶段和当前的实体水-虚拟水"二维三元"耦合流动阶段。最后,该文详细论述了实体水-虚拟水耦合流动过程的路径结构,并针对其流动过程和状态表征提出了定量表达方程,初步构建了实体水-虚拟水耦合流动基本理论框架。     

西藏高原土壤多元发生的微形态研究

自上新世末以来,随着西藏高原的隆起和多次冰川作用,作为成土因素的气候、植被、地形、水文等条件发生了剧烈的演变,从而对西藏高原土壤的发生、演化产生重要的影响.土壤大形态研究表明,西藏高原土壤广泛地显示有明显的组合剖面,突出表现在这些土壤剖面中存在有黄棕或棕带红色的、与其上下土层无发生上联系的、在暖湿气候条件下形成的土层;或者在某些现代陆成上壤剖面中存在有水成土的残遗特征等,这些形态特征在很大程度上说明了西藏高原土壤多元发生的客观存在.     

免耕播种机防堵技术研究现状与发展趋势

免耕播种机在残茬覆盖地作业是否具备良好的防堵性能,已成为影响免耕播种机生产效率和播种质量的关键因素之一.该文系统分析了免耕播种机防堵的必要性和防堵技术研究现状,提出了免耕播种机应着手找准防堵技术的切入点,加强免耕播种机防堵技术与作业工艺措施有机结合,加强作物残茬的几何特性和机械特性的基础研究,并降低防堵装置功率消耗和转速,提高定向抛撒能力和秸秆覆盖量适应性以及具有安全性能好和作业粉尘低等方面研究,同时加强利用高速摄影和虚拟仪器等现代先进测试仪器与技术开展秸秆抛撒运动规律研究,以探讨改善防堵性能的途径,提高免耕播种机播种质量和生产效率,加快旱地农业保护性耕作技术的推广应用.     

腐殖质对白浆土中Fe、Mn、Al形态转化及磷生物有效性的影响

在三江平原布置长期试验，研究连年施用有机肥后土壤腐殖质变化及其对白浆±Fe、Mn、Al形态转化及磷生物有效性的影响。结果表明，施用牛粪后土壤腐殖质含量升高，且以松结态腐殖质的增长为主；土壤的DTPA提取态和有机络合态Fe、Mn、Al含量上升，使土壤有效态磷含量上升。因此，生物措施是治理白浆土，促进土壤磷素养分有效性上升，增大土壤缓冲容量和抗逆性的有效措施。