Investigation on the interaction of letrozole with herring sperm DNA through spectroscopic and modeling methods

The interaction of letrozole, an efficient and safe aromatase inhibitor, with herring sperm DNA (hsDNA) was investigated in vitro through spectroscopy analysis and molecular modeling to elucidate the binding mechanism of anticancer drugs and DNA. The binding constant and the number of binding sites were 2.13 × 10⁴ M^?1 and 1.09, respectively, at 298 K. Thermodynamic parameters (ΔG, ΔH and ΔS) exhibited negative values, which indicated that binding was spontaneous and Van der Waals forces and hydrogen bond were the main interaction forces. Fourier transform infrared spectroscopy and other spectroscopy analysis methods illustrated that letrozole could intercalate into the phosphate backbone of hsDNA and interact with the nitrogenous bases. Consistent with the experimental findings, molecular modeling results demonstrated that the interaction was dominated by intercalation and hydrogen bonding. Copyright © 2015 John Wiley & Sons, Ltd.     

Fluorescence spectroscopy and docking study in two flavonoids,isolated tectoridin and its aglycone tectorigenin,interacting with human serum albumin: a comparison study

Two flavonoids, tectoridin (TD) isolated from rhizomes of Iris tectorum and hydrolyzed aglycone tectorigenin (TG) were prepared and characterized to compare their different interaction ability with human serum albumin (HSA). Based on the results, the affinity of TG–HSA was stronger than that of TD–HAS, and TG combined more closely with HSA than did TD. HSA fluorescence was quenched by TD/TG. The interactions between TD/TG and HSA involved static quenching. The thermodynamic parameters indicated that both binding processes were spontaneous; hydrogen binding and van der Waals force were the main forces between TD and HSA, whereas a hydrophobic interaction was the main binding force between TG and HSA. Synchronous and 3D fluorescence spectra showed that the binding of TD/TG to HSA induced conformational changes. Moreover, a docking study confirmed the experimental results. Copyright © 2015 John Wiley & Sons, Ltd.     

Construction of photodynamic‐effect immunofluorescence probes by a complex of quantum dots,immunoglobulin G and chlorin e6 and their application in HepG2 cell killing

In this study, tri‐functional immunofluorescent probes (Ce6–IgG–QDs) based on covalent combinations of quantum dots (QDs), immunoglobulin G (IgG) and chlorin e6 (Ce6) were developed and their photodynamic ability to induce the death of cancer cells was demonstrated. Strategically, one type of second‐generation photosensitizer, Ce6, was first coupled with anti‐IgG antibody using the EDC/NHS cross‐linking method to construct the photosensitive immunoconjugate Ce6–IgG. Then, a complex of Ce6–IgG–QDs immunofluorescent probes was obtained in succession by covalently coupling Ce6–IgG to water soluble CdTe QDs. The as‐manufactured Ce6–IgG–QDs maintained the bio‐activities of both the antigen–antibody‐based tumour targeting effects of IgG and the photodynamic‐related anticancer activities of Ce6. By way of polyclonal antibody interaction with rabbit anti‐human epidermal growth factor receptor (anti‐EGFR antibody, N‐terminus), Ce6–IgG–QDs were labelled indirectly onto the surface of human hepatocarcinoma (HepG2) cells in cell recognition and killing experiments. The results indicated that the Ce6–IgG–QDs probes have excellent tumour cell selectivity and higher photosensitivity in photodynamic therapy (PDT) compared with Ce6 alone, due to their antibody‐based specific recognition and location of HepG2 cells and the photodynamic effects of Ce6 killed cells based on efficient fluorescence resonance energy transfer between QDs and Ce6. Copyright © 2015 John Wiley & Sons, Ltd.     

Effect of high fibre diets formulated with different fibrous ingredients on performance,nutrient digestibility and faecal microbiota of weaned piglets

The aim of the experiment on 180 weaned piglets (8.9 kg body weight) was to investigate the influence of high fibre diets formulated with different fibrous ingredients on performance, nutrient digestibility, diarrhoea incidence and numbers of faecal microbiota. The dietary treatments included a Control diet and five high fibre diets formulated with different fibre sources including wheat bran, soybean hulls, naked oat hulls, palm kernel expeller and bamboo fibre. The high fibre diets averaged 14.6% neutral detergent fibre with different non-starch polysaccharides (NSP) components and were fed ad libitum for 28 d. Faecal samples were collected during the last 3 d of the experiment and the apparent total tract digestibility of nutrients and fibre components were determined. Pigs fed the Control and wheat bran diets had a higher (p ≤ 0.05) average daily gain (ADG) than pigs fed the palm kernel expeller and bamboo meal diets. The reduced ADG for pigs appeared to be related to reductions in the digestibility of gross energy and dry matter, respectively. The feed-to-gain ratio was significantly higher (p ≤ 0.05) for pigs fed the fibre diets. The digestibility of NSP components was different among the treatments. The diarrhoea incidence was not affected by treatments. The abundance of faecal bifidobacteria was significantly higher (p ≤ 0.05) for pigs fed the wheat bran diet than for pigs fed the bamboo meal diet. It was concluded that the diets formulated with different fibre sources when fed to weaned piglets have different effects on pig performance, nutrient digestibility and numbers of faecal microbiota. The wheat bran diet rich in arabinoxylans enabled a better performance than the other tested diets with fibre addition.     

Resolution of Rac‐Bambuterol via Diastereoisomeric Salt Formation with o‐Chloromandelic Acid and Differences in the Enantiomers' Pharmacodynamical Effects in Guinea Pigs and Beagles

In this study an enantioseparation method for rac‐bambuterol (5‐(2‐(tert‐butylamino)‐1‐hydroxyethyl)‐1,3‐phenylene bis(dimethylcarbamate)) via diastereoisomeric salt formation with o‐chloromandelic acid was developed. The enantiomeric excess (ee) values and chemical purities of the desired products were confirmed by high‐performance liquid chromatography (HPLC) using chiral stationary phase and reverse‐phase HPLC analyses, respectively. The ee values and the chemical purities both exceeded 99%. Animal experiments showed that (R)‐bambuterol was a potent inhibitor for histamine‐induced asthma reactions. (S)‐bambuterol was ineffective in relaxing the airways. Both enantiomers increased heart rates in beagles. Therefore, replacing rac‐bambuterol with (R)‐bambuterol could be beneficial for asthma patients. Chirality 28:306–312, 2016. © 2016 Wiley Periodicals, Inc.     

燕麦属颖果微形态特征及其分类学意义

为探讨燕麦属颖果微形态特征的分类学意义,采用体视显微镜和扫描电子显微镜观察燕麦属27种颖果的微形态特征,结合分子系统发育证据分析其分类学意义。燕麦属颖果有纺锤形、倒披针形、椭圆形3种形状,条纹、棱纹、网纹3种纹饰。燕麦属颖果形状、纹饰和花柱基宿存模式具有有限的属下分类学意义,颖果大小和表面大毛密度具有种间鉴定价值,而颖果腹面形态、压扁方式、胚比不具有种间鉴定价值。大穗燕麦(Avena macrostachya Balansa ex Coss.Durieu)颖果纺锤形,条纹纹饰,隶属于燕麦属颖果微形态特征的变异范围。大粒裸燕麦(A.nuda L.)与普通栽培燕麦(A.sativa L.)颖果大小、形状及纹饰特征的差异支持将大粒裸燕麦作为独立种处理。燕麦属颖果大小、表面大毛密度、胚比变异幅度大,推测与分布区广幅的气候变异相适应,凹腹面颖果体积相对缩减,有利于颖果快速发育、成熟,推测与燕麦属植物在温带、寒带分布区适生期较短相适应。     

气候波动和土地覆盖变化对广东省植被净初级生产力的相对影响

为深入理解人类活动对陆地生态系统的影响,采用CASA(Carnegie-Ames-Stanford Approach)模型估算广东省2000、2005和2010年实际植被净初级生产力(Net primary productivity,NPP),并基于情景模拟法估算气候和土地覆盖类型稳定条件下的植被NPP,对气候波动和土地覆盖变化在植被NPP变化中的相对贡献进行了研究。结果表明:太阳辐射对植被NPP具有显著的正向控制作用,气温与植被NPP表现为显著负相关,降水不是该区域植被生长的限制性因子;各气候因子与植被NPP的相关性具有季节和区域差异性。在气候不变条件下,土地覆盖变化整体上增加了NPP,对NPP变化的相对贡献与城市扩张格局相类似,不同生态区存在差异性,以珠三角区的贡献最大。总之,气候波动对NPP变化的相对贡献较为复杂,取决于气候因子的波动特征以及与NPP的相关性;其它因子(城市热岛、农耕活动和园林管理等)对NPP变化的相对贡献存在很多不确定性,整体上增加了NPP。     

四合木根部及茎部导管分子比较解剖学研究

采用显微照相技术对四合木根、茎部导管分子形态特征及数量特征进行比较研究,并运用SMA分析导管分子长度与直径之间的异速生长关系,探讨四合木的次生木质部导管分子对草原化荒漠地区的适应特性。结果表明:(1)四合木根部与茎部导管分子均以孔纹、网纹和两端无尾类型为主,具单穿孔板。(2)四合木根部与茎部导管分子在长度上均为短级水平,直径上均为小级水平,且宽窄导管并存;茎部导管分子较根部导管分子更加"小型化"。(3)不论根部或茎部,其导管分子的长度与直径之间均表现出异速生长的关系,且导管分子长度的增长速率大于直径的增长速率。这些结果有助于从细胞学尺度上了解荒漠区木本植物对草原化荒漠地区的适应策略。