银松素类衍生物分子的几何结构和光谱性质

采用密度泛函理论(Density functional theory,DFT)方法研究了7个银松素衍生物分子的结构和光谱性质。在B3LYP/6-311G**理论级别上优化了它们的几何结构,通过频率计算拟合了分子的红外振动光谱:具有共轭芳烃特征的银松素衍生物体系在1650~1450cm-1具有高红外活性的苯环伸缩振动峰,而双键在1690cm-1附近的特征伸缩振动是偶级对称振动,不产生高强度红外光谱吸收峰;在高频区(3830cm-1)观察到羟基的O-H键伸缩振动谱带。采用含时密度泛函理论(Time-dependent Density functional theory,TD-DFT)方法和极化连续介质模型(Polarized Continuum Model,PCM)计算了上述分子在CHCl3溶液中的电子吸收光谱,计算揭示吸收谱带以π→π*跃迁为主,羟基和甲氧基的引入仅起修饰作用。     

米尔贝霉素类似物的合成及杀螨杀蚜活性

为寻找高活性的米尔贝霉素衍生物,以伊维菌素为原料,经脱糖、羟基保护、氧化、还原胺化、脱保护等将其转变为13-氨基米尔贝霉素类似物,通过三组分反应设计合成了一系列米尔贝霉素磺酰脒类化合物(7a~7i),并初步测定了其对朱砂叶螨Tetranychus cinnabarinus和豆蚜Aphis craccivora的室内活性。结果表明:各衍生物对朱砂叶螨和豆蚜均有较好的触杀活性,其中7f、7h和7i对朱砂叶螨24 h的LC50值分别为1.04×10–2、9.60×10–4和1.44×10–2 mg/L;7i对豆蚜24 h的LC50值为7.81 mg/L。米尔贝霉素13位氨基上磺酰化的结构修饰有助于提高米尔贝霉素类化合物的杀螨、杀蚜活性。     

绵阳系小麦抗条锈性变异的系统调查

 绵阳系小麦是我国重要的抗条锈育种资源,近10年来的田间调查和变异观察圃试验结果表明,绵阳系小麦已经开始丧失成株抗条锈性。田间标样中分离出两类能侵染绵阳系小麦成株的重要致病类群。新的毒性菌系与条中29号相比,毒性谱更宽,致病范围更广,它们是引起绵阳系小麦丧失抗病性的主要原因。新的毒性菌系的出现和发展及绵阳系小麦抗条锈性的丧失,将对我国小麦生产产生重要影响,建议加强绵阳系小麦抗条锈变异的系统监测及控制对策研究。     

天气衍生品的运作机制与精算定价

天气衍生品是为了规避天气风险给天气敏感行业带来收入的不稳定性而兴起的创新型风险管理工具，其实质是通过衍生合约对天气风险进行分割、重组和交易的证券化产品。不同于传统金融衍生品，天气衍生品的价值取决于温度、湿度或降雨量等天气指数。本文在分析天气衍生品市场发展的基础上，重点探讨了最常见的天气期货和天气期权的运作机制及其精算定价。     

Hemodynamic effects of incremental doses of acepromazine in isoflurane-anesthetized dogs

ObjectiveTo evaluate the effects of incremental doses of acepromazine on hemodynamics in isoflurane-anesthetized dogs.Study designProspective, experimental study.AnimalsHealthy, adult, mixed-breed dogs (two male and four female) weighing 16.8 ± 5.1 kg (mean ± standard deviation).MethodsDogs were anesthetized with propofol (7 mg kg^–1) intravenously (IV) and isoflurane. Thermodilution and arterial catheters were placed for hemodynamic monitoring and arterial blood sampling for blood gas analysis. Baseline measurements were performed with stable expired concentration of isoflurane (Fe′Iso) at 1.8%. Each dog was then administered four incremental acepromazine injections (10, 15, 25 and 50 μg kg^–1) IV, and measurements were repeated 20 minutes after each acepromazine injection with Fe′Iso decreased to 1.2%. The four acepromazine injections resulted in cumulative doses of 10, 25, 50 and 100 μg kg^–1 (time points ACP₁₀, ACP₂₅, ACP₅₀ and ACP₁₀₀, respectively).ResultsCompared with baseline, cardiac index (CI) increased significantly by 34%, whereas systemic vascular resistance index (SVRI) decreased by 25% at ACP₅₀ and ACP₁₀₀. Arterial oxygen content (CaO₂) was significantly lower than baseline after all acepromazine injections (maximum decreases of 11%) and was lower at ACP₅₀ and ACP₁₀₀ than at ACP₁₀. No significant change was found in heart rate, stroke index, oxygen delivery index and systolic, mean and diastolic blood pressures. Hypotension (mean arterial pressure < 60 mmHg) was observed in one dog at baseline, ACP₁₀, ACP₂₅ and ACP₁₀₀, and in two dogs at ACP₅₀.Conclusions and clinical relevanceCompared with isoflurane alone, anesthesia with acepromazine–isoflurane resulted in increased CI and decreased SVRI and CaO₂ values. These effects were dose-related, being more pronounced at ACP₅₀ and ACP₁₀₀. Under the conditions of this study, acepromazine administration did not change blood pressure.     

几种二氮氧化喹恶啉甲醛新衍生物的合成及其抑菌活性的研究

合成了5种二氮氧化喹恶啉甲醛的新衍生物并用HNMR谱和元素分析对其结构进行了表征。用新的化合物对5种常见的植物病菌进行了抑菌活性并进行了抑菌活性和结构关系的初步探讨。     

Characterization of Bioactivities and Biosynthesis of Angucycline/Angucyclinone Derivatives Derived from Gephyromycinifex aptenodytis gen. nov., sp. nov.

Strain NJES-13^T is the type strain and currently the only species of the newly established actinobacteria genera Aptenodytes in the family Dermatophilaceae isolated from the gut microbiota of the Antarctic emperor penguin. This strain demonstrated excellent bioflocculation activity with bacteria-derived exopolysaccharides (EPSs). Moreover, it produced bioactive angucycline/angucyclinone derivatives (ADs) and contained one type III polyketide synthase (T3PKS), thus demonstrating great potential to produce novel bioactive compounds. However, the low productivity of the potential new AD metabolite was the main obstacle for its chemical structure elucidation. In this study, to increase the concentration of targeted metabolites, the influence of cellular morphology on AD metabolism in strain NJES-13^T was determined using glass bead-enhanced fermentation. Based on the cellular ultra-structural observation driven by bacterial EPSs, and quantitative analysis of the targeted metabolites, the successful increasing of the productivity of three AD metabolites was achieved. Afterward, a new frigocyclinone analogue was isolated and then identified as 2-hydroxy-frigocyclinone, as well as two other known ADs named 2-hydroxy-tetrangomycin (2-HT) and gephyromycin (GPM). Three AD metabolites were found to demonstrate different bioactivities. Both C-2 hydroxyl substitutes, 2-hydroxy-tetrangomycin and 2-hydroxy-frigocyclinone, exhibited variable inhibitory activities against Staphylococcus aureus, Bacillus subtilis and Candida albicans. Moreover, the newly identified 2-hydroxy-frigocyclinone also showed significant cytotoxicity against three tested human-derived cancerous cell lines (HL-60, Bel-7402 and A549), with all obtained IC₅₀ values less than 10 µM. Based on the genetic analysis after genomic mining, the plausible biogenetic pathway of the three bioactive ADs in strain NJES-13^T was also proposed.     

The Microstructure,Antibacterial and Antitumor Activities of Chitosan Oligosaccharides and Derivatives

Chitosan obtained from abundant marine resources has been proven to have a variety of biological activities. However, due to its poor water solubility, chitosan application is limited, and the degradation products of chitosan oligosaccharides are better than chitosan regarding performance. Chitosan oligosaccharides have two kinds of active groups, amino and hydroxyl groups, which can form a variety of derivatives, and the properties of these derivatives can be further improved. In this review, the key structures of chitosan oligosaccharides and recent studies on chitosan oligosaccharide derivatives, including their synthesis methods, are described. Finally, the antimicrobial and antitumor applications of chitosan oligosaccharides and their derivatives are discussed.     

天维菌素酰化衍生物的合成及杀虫杀螨活性

以天维菌素B、天维菌素B单糖苷和天维菌素B苷元为原料,经选择性C-5羟基保护,在C-13、C-4′和C-4″位引入不同酰基基团,合成了3个系列共23个天维菌素B酰化衍生物,并通过1H NMR、13C NMR和高分辨质谱对所有目标化合物的结构进行了表征。生物活性测定结果表明,所有衍生物对小菜蛾Plutella xylostella、朱砂叶螨Tetranychus cinnabarinus以及松材线虫Bursaphelenchus xylophilus均表现出不同程度的毒杀活性,其中天维菌素B C-4″位衍生物的活性优于C-4′位衍生物及13位衍生物。化合物8e对小菜蛾和松材线虫的毒杀活性最优,LC50值分别为9.2 mg/L和0.42 mg/L,化合物8b对朱砂叶螨的毒性最高,LC50值为0.0019 mg/L,均优于对照药天维菌素B。     

EGCG甲基化衍生物酶促合成的反应条件研究

以EGCG-O-甲基转移酶催化EGCG生成EGCG3′′Me、EGCG4′′Me和EGCG3′Me等3种主要的EGCG甲基化衍生物的生成量为主要指标,考察了EGCG甲基化衍生物酶促合成的反应条件。结果表明,EGCG甲基化衍生物的酶促合成最佳反应条件为：温度35℃,pH7.5,DTT和Mg²⁺的浓度为2mmol/L;在该反应条件下,反应体系中EGCG3′′Me、EGCG4′′Me以及EGCG3′Me的生成量分别可达到386.39μg/mL、23.40μg/mL和107.01μg/mL。