Phytochemical screening and biological activities of the oil components of Prunus domestica Linn

Phytochemical screening of three different oil fractions, obtained from n-hexane extract of Prunus domestica shoots were analyzed by GC and GC–MS. It resulted in the identification of 9, 16 and 24 compounds which representing 92.56%, 90.6% and 90.69% of these oil fractions, respectively. The main components identified from fraction 1, 2 and 3 were hentricontane (35.7%), ethyl hexadecanoate (21.7%) and linoleic acid (16.16%), respectively. Bioassay screening of oil showed moderate antibacterial activity against Salmonella group (Gram +ve and ?ve) by agar well diffusion method, moderate antifungal activity against Microsporum canis by agar tube dilution method and good antioxidant activity by DPPH radical scavenging method.     

Synthesis of CuS and ZnO/Zn(OH)2 nanoparticles and their evaluation for in vitro antibacterial and antifungal activities

In this study, the copper sulfide nanoparticles (CuS‐NPs) and the zinc oxide/zinc hydroxide nanoparticles ((ZnO/Zn(OH)₂‐NPs) were synthesized by a simple and low‐cost method, and the synthesized nanoparticles were characterized and identified by UV–Vis, field emission scanning electron microscopy (FE‐SEM), transmission electron microscopy (TEM) and X‐ray diffraction (XRD). The antimicrobial activity of the CuS‐NPs and the ZnO/Zn(OH)₂‐NPs were examined by broth dilution to determine the minimal inhibitory concentration (MIC) of antibacterial agent required to inhibit the growth of a pathogen and the minimum bactericidal concentration (MBC) required to kill a particular bacterium. Agar disc diffusion method was used to determine the zone of inhibition. The nanoparticles demonstrated potent antibacterial activity against Klebsiella pneumonia (ATCC 1827), Acinetobacter baumannii (ATCC 150504), Escherichia coli (ATCC 33218) and Staphylococcus aureus (ATCC 25293). Antifungal activity against Aspergillus oryzae (PTCC 5164) was also obtained. The data obtained from antimicrobial activities by broth dilution and agar disc diffusion methods exhibited the CuS‐NPs were more effective than the ZnO/Zn(OH)₂‐NPs. A good correlation was observed between the data obtained by both methods.     

Syntheses and Biological Activities of Novel 3-Bromo-1-（3-chloropy- ridin-2-yl）-N-hydroxy-N-aryl- 1H-pyrazole-5-carboxamides

A series of novel 3-bromo-1-（3-chloropyridin-2-yl）-N-hydroxy-N-aryl-lH-pyrazole-5-carboxamides was synthesized by the reaction of pyrazole carbonyl chloride with each of substituted phenylhydroxyamines. The latter ones were prepared in good yields by reducing substituted nitrobenzene compounds with Zn/NH4CI reductant system in alcohol. Structures of the title compounds were determined by IR, 1H NMR, and HRMS. Their insecticidal and fungicidal activities were evaluated by larvicidal test against oriental armyworm and the mycelium growth rate method, respectively.     

Isolation and bioactivities of organic acids and phenols from walnut shell pyroligneous acid

Based on differences in acidity, organic acids and phenols were enriched by pH gradient extraction method from walnut shell pyroligneous acid. Contents of organic acids and phenols were measured by acid-base titration method and Folin colorimetric assay, respectively to assess the effectiveness of the extraction. In addition, the antimicrobial activity of the organic acids and antioxidant activity of phenols extracted were investigated. Chemical components of the extracts that were from the optimal concentrations of NaHCO₃ and NaOH were measured by GC-MS. The results showed that 5% NaHCO₃ could enrich the highest amount of organic acids, whereas 4% NaOH could enrich the highest amount of phenols. The enriched organic acids exhibited high antimicrobial activity, and the enriched phenols exhibited antioxidant activity under low concentrations, and demonstrated dosage dependency.     

Abietane Diterpenoids Isolated from Clerodendrum bracteatum and Their Antioxidant and Cytotoxic Activities

Two new abietane diterpenoids (1,2), along with five known diterpenoids (3–7), were first isolated and purified from the stems of Clerodendrum bracteatum. The structures of the new compounds were established by extensive analysis of mass spectrometric and 1-D, 2-D NMR spectroscopic data. Their antioxidant activities were determined on DPPH radical scavenging and ABTS. The in vitro cytotoxic activities of the compounds were evaluated against the HL-60 and A549 cell lines by the MTT method.     

Synthesis and Biological Activity of Novel Anthranilic Diamides Containing N-Substituted Arylmethylene Moieties

A series of novel anthranilic diamides containing N-substituted arylmethyl moieties was designed and synthesized, in which the bond distance and conjugation pattern between pyrazole and pyridine rings contained in Chlorantraniliprole were changed. Their structures were confirmed by JH NMR, IR, elemental analysis or high resolution mass spectromentry{HRMS）, and the conformation of compound 4d was confirmed by X-ray diffraction. The preliminary bioassay results indicate that all the target compounds exhibited moderate insecticidal activity against oriental armyworm at 200 mg/L and some of them presented favorable antitumor activities against human lung cancer cells（A549）, liver cancer cells（BelT402） and colon cancer celIs（HCT-8） in vitro by microculture tetrazolium（MTT） method, among which compound 6j afforded the best anti-proliferative activity at 5μg/mL.     

Synthesis,antibacterial, anticancer and molecular docking studies of macrocyclic metal complexes of dihydrazide and diketone

The complexes of Co(II), Ni(II), Cu(II) and Zn(II) metal ions has been synthesized through template method by the condensation of succinic acid dihydrazide with 5-chloroisatin in alcoholic medium. Complexes were characterized by C H N analysis, molar conductance, thermal analysis, magnetic susceptibility, mass spectrometry, FTIR, EPR, ¹H NMR, UV–Visible spectroscopy. These studies suggest an octahedral geometry for all the complexes. The compounds were found active against B. subtilis and S. aureus and P. aeruginosa and E. coli bacteria. The Zn(II) complex showed significant anticancer activity against Squamous Cell Carcinoma cells tested by the MTT assay method. Molecular docking studies with EGFR tyrosine kinase were also carried out. All these results show that some of the synthesized compounds have remarkable antibacterial and anticancer property.     

马来酰亚胺类GSK-3β抑制剂的QSAR研究及分子设计

为了研究马来酰亚胺类化合物抑制活性与分子结构的定量构效关系,在分子理论的基础上计算了67个马来酰亚胺类化合物的电性距离矢量,通过最佳变量子集回归的方法,建立了抑制活性的五元线性回归模型,模型的传统相关系数(R2)和交叉验证相关系数(RCV2)分别为0.864和0.825.该模型经过Jackknife法检验、交叉验证、F检验及外部检验法证明具有良好的稳健性和预测能力.根据进入模型的5个变量分析,影响马来酰亚胺类GSK-3β抑制剂抑制活性的主要结构基团是-NH-,=O(或-OH),≡CH,Cl-及-O-(或-S-).同时基于QSAR模型设计了6个抑制活性显著提高的马来酰亚胺类分子,并预测了它们的抑制活性.     

化学发光法测定几种怀山药的抗自由基活性

用不同溶剂将三种怀山药分成极性不同的部位 ,并用鲁米诺—H2 O2 —CuSO4 化学发光体系测定天然产物抗自由基活性的方法检测了这些部位的抗自由基活性 ,比较了不同品种怀山药的质量差异 ,所得结果与传统经验相吻合。     

A New and Efficient Synthetic Method and Antibacterial Activities of Oxazolidinone Analogues

A series of novel oxazolidinone analogues were prepared by a new and efficient synthetic method and their antibacterial activities were determined. These compounds wer echaracterized by LC-MS and ^1H NMR.     

Synthesis and Anticancer Effect of gem-Difluoromethylenated Chrysin Derivatives

Ten gem-difluoromethylenated chrysin derivatives were prepared and their anticancer activities in vitro were evaluated by the standard MTT method. The results of biological test showed that some of gem-difluoromethylenated chrysin derivatives had higher anticancer activity than chrysin.     

Synthesis,antimicrobial and anti-inflammatory activities of some novel 5-substituted imidazolone analogs

In view of potent antimicrobial and anti-inflammatory activities exhibited by 5-substituted imidazolones, a variety of novel imidazolone analogs 3a-l were synthesized by the condensation of different substituted oxazolones 1 with various aromatic amines 2. All the synthesized compounds were screened for in vitro activities against a panel of Gram-positive and Gram-negative bacteria and the yeast-like pathogenic fungus Candida albicans. Several analogs produced good or moderate activities particularly against the tested Gram-positive bacteria Micrococcus luteus and Gram-negative bacteria Pseudomonas aeruginosa and. Meanwhile, compounds 3b and 3c displayed marked antifungal activity against C. albicans. In addition, the in vivo anti-inflammatory activity of the synthesized compounds was determined using the carrageenin-induced paw oedema method in rats. Two of 5-substituted imidazolone derivatives, 3k and 3d show good anti-inflammatory activity. The structures of all the newly synthesized compounds were elucidated using IR, ¹H NMR and ¹³C NMR.     

二茂铁基1,3,4-三唑席夫碱衍生物合成及生物活性和电化学性质

首次合成了二茂铁基-1,3,4-三唑Schiff碱衍生物（5a~5e）,利用IR、1H NMR和HRMS等手段对其进行了结构表征。 用黄瓜子叶生根法以及小麦芽鞘法,分别测试化合物的细胞分裂素活性和生长素活性。 结果表明,在10 mg/L浓度下,有4个化合物的子叶生根促进作用为46.9%~73.6％,比对参照物的细胞分裂活性更高,但生长素活性不明显,化合物5c仅提高25％;化合物的除草活性在68%~72%之间。 以石墨烯修饰的玻碳电极为工作电极,在Britton-Robison缓冲溶液中,研究了目标化合物电化学行为。 结果表明,在pH值为2或3的溶液中,合成目标化合物具有良好的氧化还原可逆性,氧化峰电流对数（lg Ipc）与扫描速度对数(lg v)、浓度对数(lg c)均呈现良好线性关系,目标化合物(5a~5d)的电子转移过程均受吸附-扩散混合控制,该类化合物的循环伏安法最低检出限为10-5 mol/L。     

Catalytic properties of Cu/Co/Zn/Zr oxides prepared by various methods

The new Cu-Co based （Cu/Co/Zn/Zr） catalysts for higher-alcohol synthesis were prepared using coprecipitation method, plasma enhanced method and reverse coprecipitation method under ultrasound irradiation. The catalysts were investigated by the means of BET, SEM, XRD, H2-TPR and XPS. Catalytic properties of the catalysts prepared by various methods were examined using CO hydrogenation reaction. It was found that plasma enhanced method and reverse coprecipitation method under ultrasound irradiation were both effective in enhancing the catalytic properties of Cu/Co/Zn/Zr mixed oxides. The small particle size, high dispersion of active components, the improvement of specific surface area and surface contents of active phases could account for the excellent performance of the experimental Cu/Co/Zn/Zr catalysts.     

Synthesis and Antitumor Activity of 7-Substituted Derivatives of Homocamptothecin

Camptotecin is the parent of an important class of anticancer agents which, can selectively poison the ubiquitous nuclear enzyme topoisomerase. Water soluble camptothecin analogues such as topotecan and irinotecan are already approved for clinical uses in…     

Essential oil extracted from leaf of Phoebe bournei (Hemsl.) yang: chemical constituents,antitumor, antibacterial,hypoglycemic activities

Abstract

The essential oil were extracted from the leaf of Phoebe bournei (Hemsl.) Yang by a hydrothermal method and then analyzed by gas chromatography–mass spectrometry. The leaf oil mainly included α-copaene (5.44%), α-muurolene (7.32%), δ-cadinene (11.44%), 1s-calamenene (5.18%). Phoebe bournei (Hemsl.) Yang leaf essential oil had significant inhibitory activity against Epidermophyton floccosum and Microsporum gypseum, the potential antitumor activity towards leukemia, breast, and colon cancer cell lines was good. Phoebe bournei (Hemsl.) Yang leaf essential oil had weaker activity on the four tested bacteria, it exhibited a certain role in promoting glucose uptake by adipocytes.     

Nine New Norlabdane Diterpenoids from the Leaves of Austroeupatorium inulifolium

Nine new norlabdane diterpenoids were isolated from the leaves of Austroeupatorium inulifolium collected in Indonesia. All of them have an acyl‐furan unit connected to C(11), and oxygenated functions at C(2) and C(3). The structure elucidations and the assignment of the absolute configurations of the isolated natural products were carried out by extensive spectroscopic analysis and the extended Mosher method, as well as chemical correlations. Antimicrobial activities and cytotoxicity against HL‐60 cells were determined using bioassays.     

A new method for determination of hyaluronidase activity in biological samples using capillary zone electrophoresis

The aim of the study was to develop a new capillary zone electrophoresis (CZE) method for determination of enzymatic activity of hyaluronidase. The method permits monitoring of the process of hyaluronic acid digestion by hyaluronidase. Studies were performed using CZE instrument equipped with capillary of 64.5 cm total length, 56 cm effective length and internal diameter 75 µm. Separation was performed in the phosphate buffer (pH 8.10) in the electric field of 20 kV, λ = 220 nm. The procedure was based on mixing a known quantity of hyaluronic acid and an aliquot of hyaluronidase solution, followed by obtaining CZE profiles after a known period of incubation (0.5 h). The activity of hyaluronidase was calculated using multiple regression analysis in which sizes of the peaks of the main degradation products were used. The newly developed method was fully validated and it is appropriate to evaluate the activity of hyaluronidase originating from different sources with high precision and accuracy. t‐Tests showed that there were no significant differences between results obtained using turbidimetric, viscosimetric and the new CZE method. The developed method is characterized by a short duration of analysis, low volume of analyzed sample, small amount of buffers used and low cost of analysis. Copyright © 2013 John Wiley & Sons, Ltd.     

依诺沙星与铁配合物的合成、表征及其生物活性

由水热法合成了依诺沙星铁配合物,用固体培养基平板药敏试验方法测定了配合物的体外抗菌活性。结果表明,合成的依诺沙星铁配合物对金黄色葡萄球菌、肺炎链球菌、绿脓杆菌、白色念珠菌都具有抗菌活性,但只有对金黄色葡萄球菌和绿脓杆菌的抗菌活性强于配体本身。     

The Use of Isothermal Heat-Conduction Calorimetry in Direct Measurements of Solvent Vapor Pressure

Principles for applying isothermal heat-conduction calorimetry for direct studies of vapor/liquid equilibria are presented. The ideas have been tested by measurements of the vapor pressure of water over aqueous NaCl(aq) solutions at 25°C. Seven different stock solutions were used with a composition ranging from 0.0879 mol-kg^–1 to saturated solution. The imprecision and inaccuracy were not dependent on the composition and were found to be about ±2 Pa over the entire composition range. The sample solution was placed in a container separated from the pure solvent which was kept in the calorimetric cell. Solvent vapor was transported isothermally between the container and the cell by means of an inert carrier gas. The vapor pressure was evaluated by measuring the heat-flow rate associated with the process where the vapor equilibrated with a NaCl(aq) solution is fully saturated by passing through pure solvent. Corrections for treating vapor phase imperfections are presented. The method was found to be fast, accurate, and easy to use. The concept developed here can easily be applied in any commercial heat-conduction calorimeter of modular design.