山楂酸减少L02细胞脂质累积作用的研究(英文)

非酒精性脂肪性肝在发达国家和发展中国家中是一种常见的肝脏疾病。引起非酒精性脂肪性肝病的最常见原因有肥胖、糖尿病和高胆固醇。尽管非酒精性脂肪性肝病的发病率日益升高,事实上至今尚未发现可以用于治疗的药物。山楂酸是一种五环三萜化合物,已报道具有多种药理特性,包括抗炎、抗氧化以及免疫调节作用。我们的前期研究表明,山楂酸能够抑制高脂饲料诱导大鼠非酒精性脂肪性肝病的生成。本研究中,我们将探讨山楂酸体外对肝细胞(LO2)脂质累积的抑制作用。结果表明,山楂酸可抑制游离脂肪酸(FFA)诱导的LO2细胞脂质累积,进一步研究表明,山楂酸可抑制LO2细胞的SCAP mRNA水平和蛋白水平的表达。     

Synthesis and biological evaluation of aminomethyl and alkoxymethyl derivatives as carbonic anhydrase,acetylcholinesterase and butyrylcholinesterase inhibitors

Compounds containing nitrogen and sulfur atoms can be widely used in various fields such as industry, medicine, biotechnology and chemical technology. Therefore, the reactions of aminomethylation and alkoxymethylation of mercaptobenzothiazole, mercaptobenzoxazole and 2-aminothiazole were developed. Additionally, the alkoxymethyl derivatives of mercaptobenzoxazole and 2-aminothiazole were synthesized by a reaction with hemiformals, which are prepared by the reaction of alcohols and formaldehyde. In this study, the inhibitory effects of these molecules were investigated against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) enzymes and carbonic anhydrase I, and II isoenzymes (hCA I and II). Both hCA isoenzymes were significantly inhibited by the recently synthesized molecules, with K_i values in the range of 58–157?nM for hCA I, and 81–215?nM for hCA II. Additionally, the K_i parameters of these molecules for BChE and AChE were calculated in the ranges 23–88 and 18–78?nM, respectively.     

Design,in Silico Studies and Biological Evaluation of New Chiral Thiourea and 1,3-Thiazolidine-4,5-dione Derivatives

In this study, new chiral thiourea and 1,3-thiazolidine-4,5-dione derivatives were synthesized, it was aimed to evaluate the various biological activities and molecular docking of these compounds. Firstly, the new thioureas ( 1 – 16 ) were obtained by reacting 1-naphthylisothiocyanate with different chiral amines. Then, the chiral thioureas were cyclized with oxalyl chloride to obtain 1,3-thiazolidine-4,5-dione derivatives ( 17 – 32 ). All compounds were evaluated with several in vitro antioxidant and enzyme inhibition activities. Compound 30 was the most active compound against AChE, with a value of IC₅₀=8.09±0.58 μM. On the other hand, all compounds were tested in silico absorption, distribution, metabolism, and excretion (ADME) assays to better understand their bioavailability. These physicochemical properties, pharmacokinetics, and drug-likeness of all compounds were calculated using SwissADME. Furthermore, according to molecular docking analyses compound 30 exhibited significant binding affinities for all enzymes. Based on our overall observations, compound 30 could be recommended as a potential lead for the therapuetic of Alzheimer's.     

Evaluation of the effectiveness of the FWS-DBL-1 solar insect killer and its safety with respect to predatory insects in the Turpan grape growing region

本文研究了FWS-DBL-1新型太阳能灭虫器在320～580、360、400、460和520nm 5种不同波长下对吐鲁番葡萄产区害虫的诱捕效果及对天敌安全性.结果表明:在5种波长下,灭虫器诱捕昆虫的种类相似,以鞘翅目、鳞翅目、半翅目、脉翅目、双翅目、直翅目和膜翅目等为主.诱捕的主要昆虫是蜉金龟Aphodius sp.、白云斑鳃金龟Polyphyyla alba vicaria Semenov、额喙丽金龟Adoretus nigriforns Steven、毛喙丽金龟Adoretus hirsutus Ohaus、绣罗夜蛾Leucanitis picta Christoph和淘赏夜蛾Catocala puerpera Gioma等.其中:灭虫器在400nm波长下的诱捕量最多,其次是320～580nm和360nm波长.综合分析比较:400nm波长对鞘翅目害虫的诱捕效果最好,360nm波长对鳞翅目和双翅目害虫的诱捕能力最强,520nm波长对半翅目害虫的诱捕效果最好.对天敌的安全性研究表明:FWS-DBL-1太阳能灭虫器对天敌有一定的诱捕作用,益害比为1:4～1:5.诱捕量较多的是步甲科和草蛉科的天敌,占天敌总诱捕量的85.82％.在这5个波长中,360nm波长下,灭虫器对天敌的诱捕作用最小,对天敌的安全性相对较高.     

Phytophthora gemini sp. nov., a new species isolated from the halophilic plant Zostera marina in the Netherlands

Eight strains belonging to the Oomycete genus Phytophthora were isolated from Zostera marina (seagrass) in The Netherlands over the past 25 y. Based on morphology, isozymes, temperature-growth relationships and ITS sequences, these strains were found to belong to two different Phytophthora species. Five strains, four of them isolated from rotting seeds and one isolated from decaying plants, could not be assigned to a known species and hence belong to a new species for which we propose the name Phytophthora gemini sp. nov. Three strains were isolated from decaying plants and were identified as Phytophthora inundata, thereby expanding the known habitat range of this species from fresh to brackish-saline areas. The possible role of both Phytophthora species in the decline of Z. marina in The Netherlands and the evolutionary significance of the presence of Phytophthora species in marine environments are discussed.     

JDV Tat反式激活LTR与HIV-1 Tat采用类似的细胞因子

为分析JDV Tat在反式激活JDV及HIV-1 LTR过程中是否采用与H1V-1 Tat类似的细胞因子,本文构建了包含完整激活域的jTat70和hTat47,同时构建了cyclin T1和CDK9真核表达及反义转译质粒。过量表达hTat47和jTat70对hTat反式激活HIV-1 LTR,jTat反式激活JDV和HIV-1 LTR均有明显的抑制作用推测jTat和hTat的反式激活作用可能涉及类似的细胞因子。通过cyclin T1和CDK9的反义转译质粒对jTat反式激活的抑制作用证实这两种细胞因子参与了jTat对JDV和HIV-1 LTR的反式激活。     

Tools for biotechnological production of useful phytochemicals from adventitious root cultures

Adventitious roots are natural roots which develop from the differentiated cells of any organ such as leaf, root or stem. These roots are attractive source of phytochemicals due to their genetic and biosynthetic stability. Their stability offers new scope for the in vitro production of valuable secondary metabolites. In the past two decades, adventitious roots have been induced from different plant systems and the suspension cultures have been established. However, the special morphology of adventitious roots hampers the scale-up processes, which needs modifications with the existing bioreactors to facilitate proper mixing, aeration and which can overcome shear stress. Various modifications have been done with the stirred tank and air-lift bioreactors and successfully used for the cultivation of adventitious roots. The progress made in this area is tremendous, in few cases adventitious root cultures are succeeded up to commercial scale with step-wise viz. small scale to large-scale by establishing the standards with various parameters which affect the biomass accumulation and metabolite productivity. This review addresses the recent progresses made in this area and discusses the potential applications and limitations.