反毒为药：精准控制河鲀毒素用作局部麻醉药的新进展

钠离子通道阻断剂河鲀毒素(TTX)是致命的毒素之一,却是极具价值的神经生物学和生理学等生命科学研究领域的工具药.近年来,越来越多的研究指出,TTX具有强大的局部麻醉潜能,有望成为替代氨基酯类和氨基酰胺类局部麻醉药、避免阿片类药物滥用的新型麻醉药物.本文综述TTX局部麻醉应用的辅助药物、TTX缓释及控释给药系统等相关研究,旨在为局部麻醉新药研发提供参考并探讨新的思路.     

城市近郊型乡镇农业生态经济系统生态潜力及产业空间布局——以延安市河庄坪镇为例

生态脆弱区抗干扰能力弱，明确其系统的生态潜力，在潜力的基础上开发利用资源对区域的可持续发展具有重要的意义。研究基于生态系统服务价值视角，尝试测度农业生态经济系统生态潜力，同时以三产融合典型代表乡镇为研究对象，对其农业生态经济系统生态潜力和主导产业进行时空分析，最后对生态系统加以功能分区。结果显示：（1）气体调节、气候调节、水源涵养和土壤形成与保护是生态系统提供的主要服务功能。随退耕还林工程实施，林地面积的增加使生态系统服务价值量随之上升，在空间上呈现"中间低两翼高"的格局。（2）农业生态经济系统生态潜力受服务价值与资源开发过程影响，与生态系统服务价值在空间上相对一致，呈现出"两翼高中间低，北高南低"的分布格局，其中，退耕还林工程的推进直接导致林地的生态潜力增加，耕地的生态潜力减少。（3）研究区在退耕过程中形成以大棚种植为主的设施农业、以农林特色销售为主的商品型种植农业，以山地苹果为主的林果产业以及以酒店商贸为主的服务行业。并随城镇一体化的推进，主导产业呈现出由传统粗放型大田种植向集约型设施农业方向发展。在空间上形成了以镇区分布为主的第三产业、依托拐沟坡地的林果产业和沿川道展开的设施农业的产业布局。（4）基于生态系统服务价值，研究区农业生态经济系统功能区划分为城镇生态环境维护区（第Ⅰ类型区）、农业生态保护区（第Ⅱ类型区）、生态安全屏障区（第Ⅲ类区）3个区域。     

基于可持续发展目标的资源型城市可持续发展评价技术及应用——以湖南省郴州市为例

资源型城市作为我国重要战略保障基地，面临较为突出的不可持续问题，定量化开展可持续发展水平监测评估是推动其绿色转型发展、激活再生动力的重要途径。基于联合国可持续发展目标体系(SDGs),结合行星边界理论，从资源型城市可持续发展特征出发，建立了由2个系统、4个支柱、12个领域和48项指标组成的资源型城市可持续发展评价指标体系。借鉴全球SDGs监测评估实践经验，考虑指标属性，综合确定各指标的阈值，并采用改进的离差标准化、障碍度分析及耦合协调度分析等方法建立综合评价技术体系。以拥有“有色金属之乡”称号的郴州市国家可持续发展议程创新示范区为评价对象，对其2005—2019年连续15年的可持续发展水平进行实证分析。结果表明：(1)郴州市可持续发展水平整体上呈现稳步上升趋势，得分由0.398上升到0.610。(2)4个支柱中，自然资源支柱的得分进步幅度最大，高达71.3%,说明郴州市已经逐步提高对资源利用效率的重视，同时意识到挖掘替代资源的重要性，资源保障与利用能力不断提升；而发展动力支柱得分始终处于较弱或中等水平，已成为制约郴州市可持续发展和绿色转型的主要因素，其中科技创新驱动是该支柱发展关键障碍...     

Using some growth stimuli,a comparative study of salt tolerance in two tomatoes cultivars and a related wild line with special reference to superoxide dismutases and related micronutrients

Salinity is a major global problem that threatens the agricultural sector, especially in areas that suffer from a shortage of water. It motivates ionic toxicity, osmotic and oxidative stresses, which greatly inhibits plant performances and crop productivites. However, micronutrients (MNs) or plant extracts, like germinated maize grain extract (gMGE), have been reported to minimize the effects of salt stress on plant growth and returns. Therefore, this study aimed at evaluating the influences of MNs or gMGE applied as foliar sprays on growth, physio-biochemical indices, and antioxidative system components in three genotypes of tomato plants stressed by 9 dS m⁻¹ NaCl. This salinity level markedly increased Na⁺ content, lipid peroxidation, ion leakage, and markers related to oxidative stress (superoxide; O₂⁻ and hydrogen peroxide; H₂O₂). Besides, marked increases in activities of enzymatic (especially different forms of superoxide dismutase; SODs) and non-enzymatic antioxidants and osmoprotectant compounds were also observed. In contrast, growth, photosynthetic capacity including hill reaction activity (HRA), K⁺/Na⁺ ratio, tissue cell integrity (e.g., cell water content and membrane stability), and K⁺ and MNs contents decreased significantly under stress. However, compared to MNs, gMGE significantly improved the activities of the antioxidative system components (particularly SODs) and osmoprotectants, which were reflected in reduced Na⁺ accumulation, lipid peroxidation, ion leakage, and oxidative stress. These results were coupled with remarkable elevations in photosynthetic capacity including HRA, K⁺/Na⁺ ratio, tissue cell integrity, K⁺ content, and MNs contents, all of which were reflected in the enhancement of plant growth. Compared to local tomato cultivars (e.g., Castle Rock and C10), the wild line “0043-1” had better results. The interaction of three factors; salt stress, promoters, and tomato genotypes was significant. The wild tomato line “0043-1” as the best salt-tolerant is a good candidate for implication in breeding programs for tolerance to salinity to produce salt-tolerant cultivars for use to maximize tomato growth and productivity in saline environments.     

GLUT2 in pancreatic and extra-pancreatic gluco-detection

Detection of variations in blood glucose concentrations by pancreatic &#103 -cells and a subsequent appropriate secretion of insulin are key events in the control of glucose homeostasis. Because a decreased capability to sense glycemic changes is a hallmark of type 2 diabetes, the glucose signalling pathway leading to insulin secretion in pancreatic &#103 -cells has been extensively studied. This signalling mechanism depends on glucose metabolism and requires the presence of specific molecules such as GLUT2, glucokinase and the K ATP channel subunits Kir6.2 and SUR1. Other cells are also able to sense variations in glycemia or in local glucose concentrations and to modulate different physiological functions participating in the general control of glucose and energy homeostasis. These include cells forming the hepatoportal vein glucose sensor, which controls glucose storage in the liver, counterregulation, food intake and glucose utilization by peripheral tissues and neurons in the hypothalamus and brainstem whose firing rates are modulated by local variations in glucose concentrations or, when not protected by a blood-brain barrier, directly by changes in blood glucose levels. These glucose-sensing neurons are involved in the control of insulin and glucagon secretion, food intake and energy expenditure. Here, recent physiological studies performed with GLUT2 -/- mice will be described, which indicate that this transporter is ess ential for glucose sensing by pancreatic &#103 -cells, by the hepatoportal sensor and by sensors, probably located centrally, which control activity of the autonomic nervous system and stimulate glucagon secretion. These studies may pave the way to a fine dissection of the molecular and cellular components of extra-pancreatic glucose sensors involved in the control of glucose and energy homeostasis.     

Nutrient and chemical sensing by intestinal pathogens

Pathogenic gut bacteria, such as those comprising the Enterobacteriaceae family, have evolved sophisticated virulence mechanisms, including nutrient and chemical sensing, to escape host defense strategies and produce disease. In this review we describe the mechanisms utilized by the enteric pathogen enterohemorrhagic Escherichia coli (EHEC) O157:H7 to achieve successful colonization of its mammalian host.     

Glycine neurotransmitter transporters: an update

Glycine accomplishes several functions as a transmitter in the central nervous system(CNS). As an inhibitory neurotransmitter, it participates in the processing of motor and sensory information that permits movement, vision, and audition. This action of glycine is mediated by the strychnine-sensitive glycine receptor, whose activation produces inhibitory post-synaptic potentials. In some areas of the CNS, glycine seems to be co-released with GABA, the main inhibitory amino acid neurotransmitter. In addition, glycine modulates excitatory neurotransmission by potentiating the action of glutamate at N-methyl-D-aspartate (NMDA) receptors. It is believed that the termination of the different synaptic actions of glycine is produced by rapid reuptake through two sodium-and-chloride-coupled transporters, GLYT1 and GLYT2, located in the plasma membrane of glial cells or pre-synaptic terminals, respectively. Glycine transporters may become major targets for therapeutic of pathological alterations in synaptic function. This article reviews recent progress on the study of the molecular heterogeneity, localization, function, structure, regulation and pharmacology of the glycine transporter     

Dissipative particle dynamics simulation of a gold nanoparticle system

Dissipative particle dynamics (DPD) was carried out to study systems containing gold atoms, organic ether (oligohydroquinonyl ether terminated with a thiol group) and organic solvents. The components in the simulated system are very different in size and chemical nature. Our simulation showed that the reproduction of the macroscopic experimental phase separation, properly dividing the polymeric molecule into beads, selecting the size of gold bead, and choosing the appropriate interaction parameters between beads are crucial. In addition, the solvent effect was the dominant factor for the formation of spherical aggregates of Au atoms and organic ether molecules. We report the interaction strengths between the solvent and gold clusters. Our work has demonstrated that DPD methods can be applied to the study of complex meso-scale systems.     

The relationship between excitotoxicity and oxidative stress in the central nervous system

Excitotoxicity and oxidative stress are two phenomena that have been repeatedly described as being implicated in a wide range of disorders of the nervous system. Such disorders include several common idiopathic neurological diseases, traumatic brain injury, and the consequences of exposure to certain neurotoxic agents. While there is evidence that metabolic derangements can laed to these adverse processes, and that these processes may synergize in their damaging effects, the degree of interdependence, and the causal relation between them is not clear. The intent of this review is to delineate potential mechanisms which may unit hyperexcitation to the excessive generation of reactive oxygen species. The degree of linkage between these events appears rather strong. It is likely that excitoxicity frequency leads to a pro-oxidant condition but that high rates of generation of reactive oxygen species are not invariably accompanied by a hyperexcited neuronal state Both excitoxic and ‘oxidotoxic’ states result from the failure of normal compensatory anti excitatory and antioxidant mechanisms to maintain cellular homeostatis.     

An oxygenase enzyme system for Trametes versicolor

Abstract An oxygenase enzyme was isolated from the basidiomycete fungus Trametes versicolor , that is capable of attacking lignin and a large number of di- and tri-substituted benzene rings containing at least one hydroxy group. This enzyme system was produced late in the growth cycle without the requirement for any inducer. This non-selective enzyme system is thermophilic and operates at pH 3–5 in the presence of air or oxygen. The action of this enzyme system caused the loss of UV absorption in ferulic acid solution, the formation of hydroxy muconic semialdehyde from catechol, and transformation with the production of CO₂ from a number of hydroxy aromatics as well as lignin.