Synthesis of novel methyl jasmonate derivatives and evaluation of their biological activity in various cancer cell lines

Warburg hypothesized that the energy consumption of cancer cells is different than the normal cells. When compared to normal conditions, cancer cells do not undergo tricarboxylic acid (TCA) cycle therefore resulting in more lactate in the cells. Glycolysis pathway is a way of cancer cells to provide energy. The first step in glycolysis is the phosphorylation of glucose to glucose-6-phosphate. This reaction is catalyzed by the hexokinase-II enzyme (HK-II) which is known to be overexpressed in tumor cells. The feeding of cancer cells can be prevented by inhibiting the hexokinase-II enzyme in the first step of aerobic glycolysis. In literature, Methyl Jasmonate (MJ) is known as a Hexokinase-II inhibitor since it disposes VDAC and HK-II interaction on mitochondrial membrane. In our study, we aimed to increase the activity by synthesizing the novel MJ analogues with appropriate modifications. Here we report Hexokinase-2 enzyme and cell viability study results in different cancer cells. Based on the three different cancer cell lines we investigated, our novel MJ analogues proved to be more potent than the original molecule. Thus this research may provide more efficacious/novel HK-II inhibitors and may shed light to develop new anti-cancer agents.     

黄河三角洲滨海滩涂不同密度柽柳林的土壤盐碱与养分特征

为探讨黄河三角洲滨海滩涂不同密度柽柳林的土壤盐碱和养分特征，明确不同密度柽柳林的“盐谷”及“肥岛”效应，以黄河三角洲山东省滨州市北海新区滨海滩涂的低密度（1100 株/hm2）、中密度（4100 株/hm2）和高密度（7100 株/hm2）柽柳林为研究对象，测定分析不同密度柽柳林及柽柳植株周边不同位置的土壤pH、电导率、速效氮、速效磷、速效钾、有机碳等指标。结果表明：（1）土壤电导率随林分密度增大表现为逐渐减小，在中、高密度柽柳林，土壤电导率分别比低密度降低28.39%、55.74%；随距离柽柳植株远近不同，中、高密度柽柳林土壤电导率表现为根部<冠幅中心<冠幅边缘<株间空地，即中、高密度柽柳林出现“盐谷”效应，而低密度林分未出现。（2）土壤速效氮、速效磷和有机碳含量随林分密度增大表现出先增大后减小，在中、高密度柽柳林，柽柳植株周边不同位置的速效氮、速效磷和有机碳含量存在显著差异（P<0.05），表现为根部>冠幅中心>冠幅边缘>株间空地，而低密度柽柳林差异不显著（P>0.05）；即中、高密度柽柳林出现“肥岛”效应，而低密度林分未出现。（3）中密度柽柳林在养分含量、养分富集率方面高于高密度，在盐分富集率方面低于高密度，具有更强的“肥岛”、“盐谷”效应。（4）不同密度柽柳林以及柽柳植株周边不同位置的土壤pH差异均不显著（P>0.05）。林分密度显著影响土壤盐分及养分含量，中密度柽柳林具有显著提高土壤肥力的作用，高密度次之，而低密度较差。不同密度柽柳林的降盐作用表现为中、高密度较好，低密度较差。基于柽柳林改良土壤盐碱与养分的作用，建议黄河三角洲滨海滩涂柽柳合理的初植密度为4100 株/hm2。     

Salt effects on urea hydrolysis and nitrification during leaching through laboratory soil columns

Summary We studied the transport and transformation of urea under steady-state conditions in two soils and at three water salinities (1.0, 5.0, and 10.0 dS/m) using laboratory soil columns. A mathematical model that considers diffusion, convection, adsorption and first-order kinetic transformation of nitrogen was used to describe measured effluent concentration of the two nitrogen species. Increasing salt levels in the applied water decreased the hydrolysis of urea in the two soils studied with first-order rate coefficients decreasing from 0.015 to 0.009 h^–1 in the fine sandy loam, and from 0.075 to 0.015 h^–1 in a silty loam. Similarly, the nitrification rate decreased by 50% and 70% in the two soils as salinity increased. The rate coefficients measured in the leaching studies were much smaller than measured in incubation-type experiments. Calculated half-lives for urea and NH ₄ ⁺ provided a method interpreting the kinetic rate coefficients as a function of the experimental conditions.     

民权农区林业与农牧业有机质流动的研究

建国后 ,我国农区林业迅速崛起 ,成为农业生态系统不可缺少的组成部分。关于农区林业的经济、生态和社会效益研究报告很多[1～ 3 ] ,尤其是农区生态系统农林牧之间的相互关系 ,但多为定性描述。河南省民权县是黄淮海地区典型的平原农业县 ,本文将民权县作为一个系统 ,定量分析农林牧之间的相互关系。1　材料与方法1.1　民权县基本概况民权县位于豫东平原 ,为黄河冲积扇组成 ,人口 71 4万人 ,耕地 8 0 13×10 4 ｈａ,1731个自然村。故黄河屡次改道经过民权 ,使大片土地沦为沙荒和盐碱。光、温、水、热资源充沛 ,但旱、涝、风、沙、碱等自然灾…     

An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: Emerging ‘Novel Psychoactive Drugs’

Novel Psychoactive Drugs (NPD) can be sold without restriction and are often synthetic analogues of controlled drugs. The tryptamines are an important class of NPD as they bind to the various serotonin (5-HT) receptor subtypes and cause psychosis and hallucinations that can lead to injury or death through misadventure. Here we report on the structure elucidation and receptor binding profiles of two widely marketed tryptamine-derived NPDs, namely alpha-methyl-tryptamine and 5-methoxy-N,N-diallyl-tryptamine.     

The potential role of pomegranate and its nano-formulations on cerebral neurons in aluminum chloride induced Alzheimer rat model

The oxidative stress leading to degenerative changes in the brain of Alzheimer’s disease (AD) is evident. Our aim was to evaluate the therapeutic and protective effects of pomegranate extract (PE) and pomegranate extract-loaded nanoparticles (PE nano) in an AlCl 3-induced AD rat model. Nanoparticles were synthesized with a PE load of 0.68% w/w, and 70 male Wistar rats were divided into 7 groups: Group I was the control, Group II received PE., Group III received PE nano for 2 weeks, Group IV received AlCl 3 (50 mg/kg) daily orally for 4 weeks, Group V received PE for 2 weeks, Group VI received PE nano for 2 weeks, and Groups V and VI were started after AlCl 3 administration was stopped. Group VII received PE for 2 weeks and was stopped before AlCl 3 was administered. The Results revealed that the discrimination index in the novel object recognition test was the least in AD rat model but increased in cases protected with PE treated with PE nano. Similar results were shown based on calculating the brain weight/body weight percent. The biomarkers of antioxidant activity (catalase, glutathione and total antioxidant activity) in brain homogenate were significantly increased in groups treated with either PE or PE nano. The thiobarbituric acid reactive substance measured to estimate lipid peroxidation was significantly increased in AD rat model and decreased in groups protected with PE or treated with PE nano. Histopathological studies using hematoxylin and eosin, cresyl violet, and silver stains revealed hyaline degeneration, chromatolysis, and hallmarks of AD; neurofibrillary tangles and the senile plaques in brains of AD rat model. Restoration of the histological architecture, Nissl granules, and minimal appearance of hallmarks of AD characterized brains treated with PE or PE nano. In conclusion, PE was more effective as a protectant than a therapeutic measure in alleviating the antioxidant, lipid peroxidative effects and histopathological hallmarks in AD brains. But, the therapeutic PE-loaded nanoparticles increased the efficacy of active components and produced similar results as the protective PE.     

Novel methods of genome shuffling in <Emphasis Type="Italic">Saccharomyces cerevisiae</Emphasis>

Genome shuffling can improve complex phenotypes; however, there are several obstacles towards its broader applicability due to increased complexity of eukaryotic cells. Here, we describe novel, efficient and reliable methods for genome shuffling to increase ethanol production of Saccharomyces cerevisiae. Using yeast sexual and asexual reproduction by itself, mutant diploid cells were shuffled through highly efficient sporulation and adequate cross among the haploid cells, followed by selection on the special plates. The selected strain obtained after three round genome shuffling not only distinctly improved the resistance to ethanol, but also, increased ethanol yield by up to 13% compared with the control.