Synthesis and spectroscopic characterization of 4-butoxyethoxy-N-octadecyl-1,8-naphthalimide as a new fluorescent probe for the determination of proteins

A novel 4-butoxyethoxy-N-octadecyl-1,8-naphthalimide (BON) was synthesized as a fluorescent probe for the determination of proteins. The interactions between BON and bovine serum albumin (BSA) were studied by fluorescence spectroscopy and UV-vis absorption spectroscopy. Fluorescence data revealed that the fluorescence quenching of BSA by BON was likely the result of the formation of the BON-BSA complex. According to the modified Stern-Volmer equation, the binding constants of BON with BSA at four different temperatures were obtained. The thermodynamic parameters, enthalpy change (ΔH) and entropy change (ΔS) for the reaction were calculated to be −23.27 kJ mol⁻¹ and 10.40 J mol⁻¹ K⁻¹ according to van’t Hoff equation, indicating that the hydrogen bonds and hydrophobic interactions played a dominant role in the binding of BON to BSA. Furthermore, displacement experiments using warfarin indicated that BON could bind to site I of BSA. The effect of BON on the conformation of BSA was also analyzed by synchronous fluorescence and three-dimensional fluorescence spectra. A new fluorescence quenching assay of the proteins BSA using BON in the HCl-Tris (pH 7.4) buffer solution was developed with maximum excitation and emission wavelengths of 373 and 489 nm, respectively. The linear range was 0.1-10.0 × 10⁻⁵ mol L⁻¹ with detection limits were determined to be 1.76 × 10⁻⁸ mol L⁻¹. The effect of metal cations on the fluorescence spectra of BON in ethanol was also investigated. Determination of protein in human serum by this method gave results which were very close to those obtained by using Coomassie Brilliant Blue G-250 colorimetry.     

Design and synthesis of potent HIV-1 protease inhibitors incorporating hydroxyprolinamides as novel P2 ligands

A series of new HIV-1 protease inhibitors with the hydroxyethylamine core and different hydroxyprolinamide P2 ligands were designed and synthesized. Variation of substitutions at the P2 significantly affected the enzyme inhibitory potency of the inhibitors. Compounds 2a and 2d showed excellent enzyme inhibitory activity with IC₅₀ values in the nanomolar range. An active site binding model for inhibitors 2a and 2d was suggested based upon the computational-docking results of the ligand with HIV-1 protease. This model offers molecular insights regarding ligand-binding site interactions of the hydroxyprolinamide-derived novel P2-ligand.     

四川天南星属(天南星科)一新种——川西南星

描述了四川西部天南星属(天南星科)植物一新种,即川西天南星.     

Discovery of vinylogous carbamates as a novel class of β-ketoacyl-acyl carrier protein synthase III (FabH) inhibitors

β-ketoacyl-acyl carrier protein synthase III (FabH) catalyzes the initial step of fatty acid biosynthesis via a type II fatty acid synthase in most bacteria. The important role of this essential enzyme combined with its unique structural features and ubiquitous occurrence in bacteria has made it an attractive new target for the development of new FabH inhibitors. We first used a structure-based approach to develop 24 new vinylogous carbamates (4a-15a, 4b-15b) that target FabH for the development of new antibiotics in this paper. Potent FabH inhibitory and selective anti- Gram-negative bacteria activities were observed in most of these vinylogous carbamates. Especially, compound 6a and 7a showed the most potent FabH inhibitory activity with IC?? of 2.6 and 3.3 μM, respectively. Docking simulation was performed to position compound 6a into the Escherichia coli FabH active site and the possible binding conformation of compounds has been proposed. The biological data and molecular docking indicated that compounds 6a and 7a were potent inhibitors of E. coli FabH as antibiotics deserving further research.     

Synthesis, biological evaluation, and molecular modeling of cinnamic acyl sulfonamide derivatives as novel antitubulin agents

A series of novel cinnamic acyl sulfonamide derivatives (9a-16e) have been designed and synthesized and their biological activities were also evaluated as potential tubulin polymerization inhibitors. Among all the compounds, 10c showed the most potent growth inhibitory activity against B16-F10 cancer cell line in vitro, with an IC(50) value of 0.8μg/mL. Docking simulation was performed to insert compound 10c into the crystal structure of tubulin at colchicine binding site to determine the probable binding model. Based on the preliminary results, compound 10c with potent inhibitory activity in tumor growth may be a potential anticancer agent.     

杨树试管苗嫩茎生根过程中内源IAA的免疫金银定位

生长素类物质在木本植物生根过程中发挥重要作用。杨树生根与生长素的关系及生根过程中内源激素的变化已有大量报道,而生根过程中生长素的组织定位分析则尚未见报道。该文应用免疫化学分析方法对741杨（Populus alba×（P.davidiana×P.simonii）×P.tomentosa）嫩茎生根过程中内源IAA在组织中的分布进行了研究。结果显示,741杨的嫩茎在无外源激素的1/2MS培养基上诱导10天后可生根,14天后生根率达100%。诱导前,嫩茎基部组织中几乎没有IAA信号;诱导8天后,嫩茎基部维管组织中有大量的IAA积累,而且中部的维管组织中也有明显的IAA信号（主要分布在韧皮部和维管形成层）;10天后,形成不定根原基,此时IAA主要分布在根原基;12天后,根原基分化成不定根并突破表皮,IAA在不定根中的分布主要集中在根尖和中柱。该文对741杨的嫩茎生根过程中IAA的组织分布特点及运输途径进行了讨论。     

高质量浓度IBA和插条木质化程度对兔眼蓝浆果扦插生根的影响

采用速蘸法研究了高质量浓度(3 000、5 000、7 000和9 000 mg.L-1)IBA对兔眼蓝浆果(Vaccinium asheiReade)品种‘粉蓝’(‘Powderblue’)、‘梯芙蓝’(‘Tifblue’)和‘芭尔德温’(‘Baldwin’)插条生根率和开始生根时间的影响,并对木质化程度不同的‘顶峰’(‘Climax’)和‘雾达德’(‘Woodard’)插条的生根率和开始生根时间进行了比较。结果表明:经3 000~9 000 mg.L-1IBA溶液速蘸3 s,3个品种插条的生根率均高于或显著高于对照(P<0.05),开始生根时间则较对照明显提前,但不同品种有明显差异;随IBA质量浓度的提高,‘粉蓝’和‘芭尔德温’的生根率逐渐增加,开始生根时间逐渐提早,以9 000 mg.L-1IBA处理组的生根率最高(分别为93.98%和86.46%),开始生根时间最早(分别为15和21 d);品种‘梯芙蓝’插条的生根率则以5 000 mg.L-1IBA处理组最高(88.02%),开始生根时间最早(18 d)。木质化程度不同的插条生根率有显著差异(P<0.05),木质化程度越低,插条的生根率越高且开始生根时间越早;采用木质化程度低的插条,品种‘顶峰’和‘雾达德’插条的生根率分别达到88.54%和77.60%,开始生根时间分别为25和29 d。研究结果显示:高浓度IBA速蘸法是兔眼蓝浆果扦插生根的有效方法,在实际生产中应根据不同品种的特性选择适宜的IBA浓度;从木质化程度及插条可取数量两方面考虑宜选用半木质化枝条作为插条。     

Predicting disease-associated substitution of a single amino acid by analyzing residue interactions

Background  

The rapid accumulation of data on non-synonymous single nucleotide polymorphisms (nsSNPs, also called SAPs) should allow us to further our understanding of the underlying disease-associated mechanisms. Here, we use complex networks to study the role of an amino acid in both local and global structures and determine the extent to which disease-associated and polymorphic SAPs differ in terms of their interactions to other residues.     

Total phosphorus removal from domestic wastewater with Cyperus alternifolius in vertical-flow constructed wetlands at the microcosm level

Vertical-flow constructed wetland (VFCW) is an effective alternative for removal of nutrients, heavy metals, and organic pollutants from wastewaters. This study investigated the uptake and removal of total phosphorus (TP) by Cyperus alternifolius from domestic wastewaters in the simulated VFCWs, The total of eight simulated VFCW treatments, including two different substrates, two different wet-to-dry ratios, and with and without C. alternifolius species (2 x 2 x 2 = 8), were utilized for an operation period of two years in this study. Results show that about 1.1 to 1.4 times more TP was removed from the influent with the presence of C. alternifolius as compared to without this plant species. A linear correlation existed between the aboveground biomass and its TP content. An increase in total biomass by 1000 g would result in an increase in TP accumulation in the aboveground biomass by 4.9 g. Large amounts of TP were removed by the substrate adsorption as compared to those by the aboveground biomass. Results suggest that, although substrate adsorption played a major role in TP removal, C. alternifolius uptake was an alternative pathway for further removal of TP from wastewaters in the VFCWs.