Synthesis,Crystal Structure and Antitumor Activity of Mixed Ligand Coordination Compound of Copper with Norfloxacin and 1,10-Phen,[Cu(NFLX)(phen)(H2O)]NO3·3H2O

The mixed ligand coordination compound of copper with norfloxacin (NFLX) and 1, 10-phen has been synthesized and characterized by means of X-ray single crystal diffraction. The structure features of the coordination compound are described. Antibacterial activities of the coordination compound have been tested against different microorganisms. The antitumor activities of the coordination compound on leukemia HL-60 cell line and liver cancer BEL-7402 cell line have been measured, respectively. The results indicated that the coordination compound has strong inhibitory effect on HL-60 and BEL-7402 cell lines.

诺氟沙星(Norfloxacin)对蛋白核小球藻(Chlorella pyrenoidosa)生长及抗氧化酶活性的影响

以蛋白核小球藻(Chlorella pyrenoidosa)为实验材料,研究了喹诺酮类药物诺氟沙星(Norfloxacin,NFLX)对小球藻生长及抗氧化酶活性的影响.结果表明,NFLX对小球藻的96hEC50为30.78mg·L-1,属于低毒.NFLX暴露对小球藻谷胱甘肽硫转移酶(GST)和过氧化氢酶(CAT)具有显著影响,当NFLX浓度高于30mg·L-1时,小球藻GST活性受到显著诱导,并随NFLX浓度增加而显著升高,而小球藻CAT活性随NFLX暴露浓度的升高表现出先诱导后抑制现象.NFLX对谷胱甘肽(GSH)和7-乙氧基-异吩唑酮-脱乙基酶(EROD)的影响较弱.在低浓度NFLX暴露下,GST和CAT可作为NFLX暴露的生物标记物.

基于羧甲基纤维素包裹铜纳米颗粒复合材料电化学传感器检测牛奶中诺氟沙星

以羧甲基纤维素(carboxymethyl cellulose,CMC)包覆的铜纳米颗粒(copper nanoparticles,Cu NPs)和碳黑(carbon black,CB)为原料,制备CMC@Cu/CB复合材料,构建检测诺氟沙星(norfloxacin,NFX)的高灵敏度电化学传感器。基于扫描电子显微镜、X射线光电子能谱和X射线衍射等手段对CMC@Cu/CB结构和形貌进行表征,在玻碳电极(glassy carbon electrode,GCE)表面滴铸复合材料悬浮液,制备CMC@Cu/CB/GCE传感器。结果表明:CMC@Cu/CB/GCE呈均匀分散球状,传感器对NFX具有良好的电流响应,线性范围为0.4~100.0μmol/L,检出限为0.24μmol/L(R_(SN)=3),此外,该修饰电极对实际样品中NFX的测定具有良好的灵敏度和稳定性,对牛奶提取物中NFX的加标回收率为98.8%~112.5%。同时,由于实验过程中原材料价格低廉,传感器的制备成本极低,在实际检测中具有良好的应用前景。

SDS-Al^(3+)-NFLX体系的荧光特性及诺氟沙星的测定

研究了不同表面活性剂对Al3+-诺氟沙星(Norfloxacin,NFLX)体系荧光特性的影响,发现十二烷基硫酸钠(SDS)对该体系有显著的增敏作用;系统研究了SDS-Al3+-NFLX反应体系的荧光特性,利用这一反应体系,建立了简单、快速、灵敏的测定诺氟沙星的荧光方法,选择了最佳实验条件,并将此方法用于诺氟沙星滴眼液和胶囊的测定,结果满意.

Impacts of soil organic matter, pH and exogenous copper on sorption behavior of norfloxacin in three soils

Norfloxacin sorption and the factors （soil organic matter （SOM）, pH, and exogenous copper （Cu） influencing the sorption were investigated in a black soil （soil B）, a fluvo-aquic soil （soil F）, and a red soil （soil R）. With increasing norfloxacin concentrations, sorption amount of norfloxacin increased in both the bulk soils and their SOM-removed soils, but the sorption capacity of SOM-removed soils was higher than that of their corresponding bulk soils, indicating that the process of norfloxacin sorption in soil was influenced by the soil properties including SOM. The sorption data in all bulk soils and SOM-removed soils were fitted to Freundlich and Langmuir models. The correlation coefficients suggested that the experimental data fitted better to Freundlich equation than to Langmuir equation. Furthermore, the data from soil F and SOM-removed F could not be described by Langmuir equation. The norfloxacin sorption amount decreased in soil B and soil F, whereas it increased in soil R as solution pH increased. The maximum KD and Koc were achieved in soil R when the equilibrium solution pH was 6. The norfloxacin sorption was also influenced by the exogenous Cu^2＋, which depended on the soil types and Cu^2＋ concentrations. With increasing Cu^2＋ concentrations in solution, generally, sorption amount, KD and Koc for norfloxacin in soils increased and were up to a peak at 100 mg/L Cu^2＋, and then the sorption amount decreased regardless of norfloxacin levels.

NFLX抗原模拟表位的淘选及鉴定

从噬菌体随机肽库中淘选模拟NFLX（Norfloxacin）表位的噬菌体粒子并进行性质鉴定。以抗NFLX单克隆抗体为靶分子，对噬菌体环七肽库和十二肽库进行生物亲和淘选，以ELISA鉴定阳性克隆，进行DNA测序，采用生物信息学方法对淘选得到的模拟表位进行分析。分别得到了9个（环七肽）和8个（十二肽）能与靶分子特异性结合且能被NFLX标准品阻断的阳性克隆，其特有序列为（环七肽）：X-X-X-X-X-脯氨酸-苯丙氨酸（X为任意氨基酸），以阻断效果最好的抗原模拟表位H3建立了竞争ELISA标准曲线，IC50为：（48．07±6）ng·mL^-1，检测线性范围为10-200ng·mL^-1。噬菌体展示技术可淘选得到NFLX模拟表位，淘选到的噬菌体粒子可作为NFLX的替代品建立免疫学检测方法。

Exploring a broadened operating pH range for norfloxacin removal via simulated solar-light-mediated Bi_2WO_6 process

Semiconductor photocatalysis can be operated over a narrow pH range for wastewater treatment. In this study, a simulated solar-light-mediated bismuth tungstate (SSL/Bi2WO6) process is found to be effective for norfloxacin degradation over a narrow pH range. To broaden the operating pH range of the SSL/Bi2WO6 process, an NH4+ buffer system and an Fe3+ salt were introduced under extremely basic and acidic pH conditions, respectively. The NH4+ buffer system continuously supplied hydroxyl ions to generate ·OH radicals and prevented acidification of the solution, resulting in improved norfloxacin removal and mineralization removal under alkaline conditions. In contrast, the Fe3+ salt offered an additional homogeneous photo-sensitization pathway. The former treatment assisted in norfloxacin decay and the latter increased the collision frequency between the photo-generated hole and hydroxyl ions. Moreover, the effect of parameters such as pH and Fe3+ dosage was optimized.

Enhancement of norfloxacin solubility via inclusion complexation with β-cyclodextrin and its derivative hydroxypropyl-β-cyclodextrin

The objectives of the study were to investigate the effects of β-cyclodextrin(βCD) and hydroxypropyl-β-cyclodextrin(HPβCD) on the solubility and dissolution rate of norfloxacin prepared using three different methods, at drug to cyclodextrin weight ratios of 1:1, 1:2, 1:4 and 1:8. All the methods increased the solubility and dissolution rate of norfloxacin via inclusion complexation with βCD and HPβCD. Norfloxacin was converted from crystalline to amorphous form through inclusion complexation. Solvent evaporation method was the most effective method in terms of norfloxacin solubilisation, while inclusion complex of HPβCD has higher solubility than βCD complex when prepared using the same procedure.

Effect of bismuth tungstate with different hierarchical architectures on photocatalytic degradation of norfloxacin under visible light

The photocatalytic degradation of norfloxacin by bismuth tungstate(Bi2WO6)with different hierarchical architectures wasinvestigated under visible light irradiation.Bi2WO6was prepared by hydrothermal method with the reaction solution pH rangingfrom4to11.The relatively ultrathin Bi2WO6nanoflakes prepared at pH4showed excellent adsorption and photodegradationefficiency towards norfloxacin.The characterization results showed that Bi2WO6prepared at pH4had a larger specific area andfaster photo-generated carrier separation rate.The decay rate reached the maximum in weak alkaline reaction solution,which couldbe attributed to the presence of moderate OH-anions.The present study demonstrated that the smaller size of Bi2WO6could be anefficient photocatalyst on the degradation of norfloxacin in the aquatic environment.

Crystal Structure of Norfloxacin Methanol Solvate: C_(16)H_(18)FN_3O_3·CH_3OH·H_2O

Norfloxacin methanol solvate （ 1 -ethyl-6-fluoro- 1,4-dihydro-4-oxo-7-（ 1 -piperazinyl）-3- quinoline carboxylic acid methanol solvate） has been prepared. The crystal and molecular structures of the title compound, C16H18FN3O3·CH3OH·H2O, were determined by X-ray diffraction method. The compound crystallizes in monoclinic, space group P21/c with a = 7.8660（16）, b = 22.525 （5）, c = 10.253（2）A, β= 108.31°, Mr = 369.39, V = 1724.7（6）A^3, Z = 4, Dc= 1.423 g/cm^3, F（000） = 784, R = 0.0557 and wR = 0.1224. The TGA analysis indicates that it decomposes completely at 723.75℃.

Adsorption and degradation of norfloxacin by a novel molecular imprinting magnetic Fenton-like catalyst

In this study,a novel magnetically separable adsorbent,molecular imprinting magnetic γ-Fe_2O_3/crosslinked chitosan composites(MIPs),were prepared by a microemulsion process.Adsorption and Fenton-like oxidative degradation of a model pharmaceutical pollutant norfloxacin(NOR) by using MIPs were investigated.Various characterization methods were used to study the properties of MIPs,and it is suggested that the hydroxyl groups are the main adsorption sites for NOR.MIPs present better selective adsorption for NOR than its reference antibiotic sulfadiazine.The NOR adsorption data can be well fitted by Langmuir isotherm model and pseudosecond-order kinetic model.The optimum pH range for NOR adsorption is 7-10.In addition,the MIP-catalyzed Fenton-like system(MIPs/H_2O_2) exhibits remarkably faster removal rate for NOR than the case of γ-Fe_2O_3/H_2O_2.The result indicates that MIPs will be a good functional material in decontamination of pharmaceutical wastewaters since MIPs can be magnetically recycled after the treatment.

Minor Groove Binding between Norfloxacin and DNA Duplexes in Solution: A Molecular Dynamics Study

Molecular dynamics were used to investigate the interaction between norfloxacin and DNA duplex. The results showed that norfloxacin was situated in the minor groove of DNA, binding to the TCGA region of d [ATATCGATAT] 2- Specific hydrogen bonds were formed between norfloxacin and guanine base of DNA during the 2 ns MD, which may be the reason for the preferentiality of quinolone antibacterial towards the guanine base of DNA duplex.

Molecularly Imprinted Polymers with Bi-functional Monomers of Polymerizable Cyclodextrin Derivatives and 2-(Diethylamino)-ethyl Methacrylate for Recognition of Norfloxacin in Aqueous Media

A molecularly imprinted polymer was synthesized using 2-（diethylamino）ethylmethacry -late（DEM） and bismethacryloyl-β-cyclodextrin（BMA-β-CD） as bi-functional monomers and norfloxacin（NOF） as a template. The results of equilibrium binding experiments indicated that the polymer has affinity and specificity for NOF in aqueous media, and that its selective recognition ability for the template was higher than that of the imprinted polymers synthesized with a single functional monomer （BMA-β-CD or DEM）.

Thermal Decomposition Kinetics of Ni(Ⅱ)Complex with Norfloxacin

The thermal decomposition of the 2H2O (NFA=C16H18FN3O3, norfloxacin) and its kinetics were studied under the nonisothermal condition in nitrogen by TGDTG and DTA methods. The intermediate and residue for each decomposition were identified from TG curve. The Achar method and the MadhusudananKrishnanNinan (MKN) method were used to analyze the nonisothermal kinetic data. The possible reaction mechanisms were investigated by comparing the kinetic parameters. The kinetic equation for the third stage and the mathematical expressions for the kinetic compensation effects of the third stage were obtained.

Effects of Norfloxacin on the Superoxide Dismutase Activities of 2 Sturgeon Species

[Objective]This study was to investigate the effect of different concentrations of Norfloxacin on the superoxide dismutase （ SOD） activities in the blood plasma and liver tissues of Amur sturgeon （ Acipenser schrencki Brandt） and sterlet （ Acipenser ruthenus Linnaeus） . [Method] Using pharmaco-toxicological evaluation method,Norfloxacin with the concentrations of 0,20,40,60,80 and 100 mg /kg,was orally delivered to the Amur sturgeon and sterlet for 5 d,respectively. The SOD activities in the blood plasma and liver tissues were measured after drug withdrawal for 2 d to explore the optimal dosing concentration of Norfloxacin during sturgeon culture,as well as the effect of Norfloxacin on liver injury. [Result] SOD existed in both two sturgeons but with different amounts,and the SOD activities were higher in the livers than in the blood plasma no matter in the control and all drug delivered groups. Under different drug delivery concentrations,the SOD activities first increased and then decreased in the 2 tissues of the 2 sturgeon species,and the SOD activities reached the maximum when the drug delivery concentration was 40 mg /kg. The drug de- livery concentration had little effect on the SOD activities in the blood plasma,which showed stable changes. When the drug delivery concentration was 40 mg /kg,the SOD activities in the blood plasma of Amur sturgeon were higher than that of sterlet,while for the other concentrations,the SOD activities in the plasma of sterlet showed higher performance. However,the SOD activities changed significantly through drug delivery in the liver tis- sues,and the SOD activities were higher in the sterlet than in the Amur sturgeon when the drug delivery concentrations were 0,40 and 100 mg /kg. The SOD activity in the sterlet was the highest under 40 mg /kg,presenting a sharp peak value. The optimal drug delivery concentration of Norfloxa- cin was 30 -50 mg /kg,under which the Norfloxacin presented best effect and had no injury effect on livers. [Conclusion]This study provides theo- retical basis for the reasonable application of Norfloxacin in aquaculture.

Distribution and Elimination of Norfloxacin in Fenneropenaeus chinensis Larvae

This study examined the distribution and elimination of Norfloxacin （NFLX） in Fenneropenaeus chinensis ovary and egg and newly hatched larvae. Mature parental shrimp were exposed to 4 or 10mgL-1 NFLX for 2 or 5d. Ovary and eggs of the shrimp were sampled after spawning in order to detect NFLX residue using high-performance liquid chromatography （HPLC）. Re- suits showed that NFLX residue accumulated in F. chinensis eggs after the parental exposure, with the highest residue detected in ovary. To examine the fate of NFLX residue in larvae, we further determined the concentration of NFLX residue in F. chinensis eggs and larvae at 4 different developmental stages after 24-h exposure. From the newly metamorphosed larvae （Oh post-metamorphosis, h.p.m）, samples were taken at different time intervals to 72 h,p.m. HPLC assay showed that the concentrations of NFLX residue in zoea exposed to 4 and 10mgL-1 NFLX were the highest at 1.5h, i.e., 0.332 and 0.454μgg-1, respectively. At the two NFLX expo- sure levels, the elimination time of half NFLX （half life） in nauplius was 45.36 and 49.85h, respectively, followed by that in zoea （31.68 and 33.13 h）, mysis larvae （42.24 and 47.28 h） and postlarvae （24.48 and 30.96 h）. Both NFLX exposure levels had a germi- cidal effect. The distribution and elimination of NFLX residue in F. chinensis tissue, eggs and larvae correlated well with the drug exposure level. The disappearance of NFLX residue coincided with the larval growth, and the half-life of NFLX decreased with the larval development.

Enhanced adsorption of target branched compounds including antibiotic norfloxacin frameworks on mild steel surface for efficient protection: An experimental and molecular modelling study

In this study, an approach was proposed to employ new target branched compounds(TBCs) including multiple antibiotic norfloxacin frameworks for intensified adsorption films to achieve super protection of mild steel in HCl medium. Thus, the TBCs containing bis/tri norfloxacin skeletons were synthesized by multi-step preparation route. In addition, the reference linear compound(RLC) including a single norfloxacin part was also synthesized. The chemical structures of these compounds were confirmed by various means. It was demonstrated that the TBCs could form the tough adsorption films on the surface of mild steel, which could be processed mainly through chemisorption effect. The electrochemical analysis suggested that the TBCs displayed superior corrosion inhibition performance for low carbon steel in1.0 mol·L^(-1) HCl solution over the RLC(RLC, 87.80%;TBC1, 97.63%;TBC2, 98.35%), which was further understood by the molecular modelling. The isotherm adsorption plots were employed to analyze the spontaneous adsorption process of the TBCs on low carbon steel surface, and a prominent chemisorption could be inferred by the standard Gibbs free energy changes of the adsorption.

HPLC法优选NFLX和PFLX混合物的分离条件

目的:用高效液相色谱法优选 NFLX 和 PFLX 的分离条件。方法:ODS 柱,以甲醇—乙酸钠(0.25M)为流动相,于275nm 波长处检测,流速为1.0ml/min。结果:NFLX 和 PFLX 混合物的分离条件为,甲醇:乙酸钠缓冲液=70:30,缓冲液 PH 值为5.7。结论:此方法简便,快速,重现性好。

探讨金属离子Norfloxacin缩环反应收率的影响

作者通过一系列实验证实了原料中锌离子含量的高低直接影响缩环收率。