Gatifloxacin-铕荧光探针测定DNA

在pH 7.0±0.1的Tris-HCl缓冲溶液中,Eu3+与加替沙星形成的络合物受270 nm紫外光激发发出Eu3+的特征荧光峰,加入脱氧核糖核酸(DNA)能大大增强体系的荧光强度,由此建立GFLX-Eu3+络合物探针测定核酸的方法。与GFLX-Eu3+二元络合物相比,GFLX-Eu3+-DNA三元体系荧光强度显著增强,且最大吸收波长紫移5 nm,表明形成三元络合物。研究了反应的最佳条件,并初步探讨了GFLX-Eu3+络合物探针和DNA结合机制。

氟喹诺酮类抗菌剂Gatifloxacin

喹诺酮类抗菌剂对革兰阳性和阴性菌均有较强药效,被广泛用于治疗各种细菌感染。但目前临床使用的喹诺酮类药物常具有光毒性,并对胚胎和婴幼儿的生长发育有一定不良影响。Ｇａｔｉｆｌｏｘａｃｉｎ虽然也是氟喹诺酮类抗菌药,但其具有光毒性较小的特点,而且因其对细菌的拓扑...

Potential Antimicrobial Effects of Gatifloxacin on Periodontopathic Bacteria in Vitro

The aim of this study was to identify the potential antibacterial effects of gatifloxacin on periodontal pathogens including Aggregatibacter actinomycetemcomitans, Porphyromonas gingi-valis, and Prevotella intermedia. The minimum inhibitory concentrations (MIC) of gatifloxacin and its bactericidal effects were investigated. Gatifloxacin inhibited the growth of all three kinds of periodontopathic bacteria tested in broth. The MIC value of 2.5 nM was found to be the most effective in inhibiting A. actinomycetemcomitans. An adenosine triphosphate biolumi-nescence assay revealed that gatifloxacin exhibited bactericidal effects on the tested bacteria in a time-dependent manner. The safety of gatifloxacin in mammalian cells was evaluated by assessing the viability of normal human dermal fibroblast (NHDF) cells treated with gatifloxacin. Almost all NHDF cells survived after 2-d culture, while 81% of the cells survived after 4-d culture when treated with 1.0 × 103 nM gatifloxacin. These results indicate that gatifloxacin is a possible drug for local administration to prevent periodontal infection.

Gatifloxacin inducing apoptosis of stromal fibroblasts through cross-talk between caspase-dependent extrinsic and intrinsic pathways

AIM: To reveal the cytotoxicity and related mechanisms of gatifloxacin(GFX) to stromal fibroblasts(SFs) in vitro.METHODS: SFs were treated with GFX at different concentrations(0.009375%-0.3%), and their viability was detected by MTT method. The cell morphology was observed using light/transmission electron microscope. The plasma membrane permeability was measured by AO/EB double-staining. Then cell cycle, phosphatidylserine(PS) externalization, and mitochondrial transmembrane potential(MTP) were analyzed by flow cytometry. DNA damage was analyzed by electrophoresis and immunostaining. ELISA was used to evaluate the caspase-3/-8/-9 activation. Finally, Western blotting was applied for detecting the expressions of apoptosis-related proteins.RESULTS: Morphological changes and reduced viability of GFX-treated SFs demonstrated that GFX above 0.009375% had cytotoxicity to SFs with dependence of concentration and time. GFX-treating cells also showed G1 phase arrest, increased membrane permeability, PS externalization and DNA damage, which indicated that GFX induced apoptosis of SFs. Additionally, GFX could activate the caspase-8, caspase-9, and caspase-3, induce MTP disruption, downregulate B-cell leukemia-2(Bcl-2) and B-cell leukemiaXL(Bcl-XL), and upregulate Bcl-2 assaciated X protein(Bax), Bcl-2-associated death promoter(Bad), Bcl-2 interacting domain(Bid) and cytoplasmic cytochrome C in SFs, suggesting that caspase-dependent extrinsic and intrinsic pathways were related to GFX-contributed apoptosis of SFs.CONCLUSION: The cytotoxicity of GFX induces apoptosis of SFs through triggering the caspase-dependent extrinsic and intrinsic pathways.

表面gatifloxacin和环丙沙星、阿米卡星和克拉霉素对于实验性治疗 chelonae海龟属分支杆菌角膜炎的效果比较

目的：在动物模型上测定局部gatifloxacin和环丙沙星、阿米卡星和克拉霉素对于治疗海龟属分支杆菌chelonae角膜炎的效果。

A NOVEL MOLECULARLY IMPRINTED POLYMER:SYNTHESIS AND ADSORPTION BEHAVIOR OF GATIFLOXACIN

A kind of molecularly imprinted polymer (MIPs) with high selectivity was prepared using methacrylic acid (MAA) as functional monomer, ethylene glycol dimethacrylate (EDMA) as crosslinker and Gatifloxacin as template. The effect of various parameters such as volume of solvent, functional monomer dosage, crosslinker dosage and polymerization time were investigated. The selective binding experiment for substrates show that the affinity and selectivity for Gatifloxacin were higher than that for blank polymer. Scatchard analysis show that the MIPs recognized template with two kinds of binding sites. The dissociation constant Kd and maximum adsorption quantity Qmax of these two kinds of binding sites were calculated: Kd1 and Qmax1 of the binding sites with high affinity were 8.67×10-4 mol/L and 28.19μmol/g, while Kd2 and Qmax2 of the binding sites with low affinity were1.05×10-3 mol/L and 33.20μmol/g respectively.

A novel gatifloxacin-loaded intraocular lens for prophylaxis of postoperative endophthalmitis

Postoperative endophthalmitis(POE)has been the most threatening complication after cataract surgery,which perhaps can be solved by the antibiotic-loaded intraocular lens(IOL).However,most drug-loaded IOLs demonstrate insufficient drug quantity,short release time,increased implantation-related difficulties or other noticeable drawbacks.To prevent POE and to address these deficiencies,a drug-loaded copolymer IOL,prepared from poly(urethane acrylate)prepolymer,isobornyl methacrylate(IBOMA),N-vinyl-2-pyrrolidone(NVP),Irgacure 819,RUVA-93,and gatifloxacin(GAT),was rapidly fabricated via photocuring and by using a 3D-printed mold.This composite displayed an outstanding and controllable GAT release behavior in vitro,a high light transmittance,and a moderate refractive index.Also,it demonstrated improved strain stress and elongation compared with the reference commercial acrylic IOL material.In vivo tests demonstrated satisfying released drug concentration at the early treatment stage.In vitro and in vivo studies further confirmed the remarkable bacterial inhibition and prevention of POE by the proposed IOL,which also displayed good biocompatibility.These findings suggested that the GAT-loaded IOL could be a promising implant to prevent and cure POE,also the proposed methods could inspire more designs for various medical applications.

改性沼渣生物炭活化过硫酸盐去除加替沙星研究

为探究生物炭(BC)活化过硫酸氢钾(PMS)去除加替沙星(GAT)的机制,本实验以厨余沼渣为原料,制备沼渣生物炭,并进行改性处理得到钴炭复合材料(Co-BC)。探索了Co-BC活化PMS降解GAT的机理,研究了催化剂投加量、PMS溶液浓度、初始pH和反应温度对GAT去除率的影响,同时探究了Co-BC活化PMS的反应机制及其作为催化剂的可再生性。结果表明,改性后生物炭的孔隙结构得到改善,Co元素以CoO晶体形式存在于材料表面,且含有丰富羧基羟基等含氧官能团;Co-BC活化PMS体系对GAT的降解效果最佳,材料投加量和PMS浓度越大反应速率越快,高温碱性条件有利于反应进行;Co-BC活化PMS体系过程中存在自由基和非自由基两种机制协同降解机制;所制备的材料具备良好的再生性能,研究结论为水体中GAT的污染治理提供了新的思路。

Development of an electrochemical immunoassay for detection of gatifloxacin in swine urine

To detect gatifloxacin(GAT)residue in swine urine,an electrochemical immunoassay was established.An indirect competitive immunoassay was developed,in which the coating antigen is immobilized in an enzyme-linked immunosorbent assay(ELISA)plate and GAT residue from the sample competes with the limited binding sites in added anti-GAT antibody.Horseradish peroxidase(HRP)conjugated to goat anti-rabbit IgG was used as the enzymatic label.A carbon fiber working electrode was constructed and current signals were detected by using hydrogen peroxide as a substrate and hydroquinone as an electrochemical mediator.The electrochemical immunoassay was evaluated by analysis of GAT in buffer or swine urine and an average value of half inhibition concentration(IC50)of 8.9 ng/ml was obtained.Excellent specificity of the antibody was achieved with little cross-reaction with lomefloxacin(3.0%),ciprofloxacin(3.0%),and ofloxacin(1.9%)among commonly used(fluoro)quinolones.In conclusion,the immunoassay system developed in this research can be used as a rapid,powerful and on-site analytical tool to detect GAT residue in foods and food products.

Photodegradation of fluoroquinolone antibiotic gatifloxacin in aqueous solutions

Fluoroquinolone antibiotics (FQs) are frequently detected as emerging pollutants in aqueous environments.In this study,kinetics,influencing factors and mechanisms on the photodegradation of gatifloxacin,a representative FQ,were investigated.The photodegradation follows the pseudo-first-order kinetics.Gatifloxacin photodegrades with a quantum yield of (5.94 ± 0.95) × 10 3 in pure water and undergoes direct photolysis as well as self-sensitized photodegradation.The FQ photodegrades slower in freshwater and seawater than in pure water,which is attributed to the integrative effects of pH and the aqueous dissolved matter (e.g.,humic acids and NO 3-) on the photodegradation.A toxicity test using Vibrio fischeri revealed the formation of hazardous photoproducts.

Pulse radiolysis study on gatifloxacin——A fluoroquinolone antibiotic

The reactions between gatifloxacin(GFX) and various one-electron oxidants,such as ˙OH,N3˙,Br2˙ˉ,and SO4˙ˉ,have been studied by pulse radiolysis techniques.The GFX radical anion formed in the reaction of GFX with eaqˉ could either be protonated or deprotonated,and the absorption of GFX radical anion was located at 390 nm.The transient species produced by the reaction of GFX with ˙OH radical shows a broad band in the 380?600 nm region with a shoulder,while the oxidation by N3˙,SO4˙ˉ,and Br2˙ˉ results in an absorption band with λmax = 370 nm.At neutral condition(pH 7),the rate constants of GFX reacting with ˙OH,N3˙,Br2˙ˉ,SO4˙ˉ and eaqˉ are estimated to be 1.0 × 1010,3.1 × 109,2.8 × 109,3.0 × 109,and 1.8 × 1010 dm3 mol?1 s?1,respectively.From the pH dependence on the formation of electron adducts and on the rate constant of GFX with eaqˉ,the pKa of GFX radical anion is estimated to be 5.5 and 9.3.

Determination of drug concentration in aqueous humor of cataract patients administered gatifloxacin ophthalmic gel

背景眼的胶化被开发了在水的幽默增加药集中并且延迟从研究是在奔流病人的水的幽默比较药集中的结膜 sac.The 的药的损失管理了在病人的有那的眼的胶化管理了的0.3% gatifloxacin 0.3% gatifloxacin 眼的 solution.Methods 有奔流的 96 个病人( 96 只眼睛)随机在组 1-4received 被分到 8 个 groups.The 病人热门 gatifloxacin 0.3%

Studies on Interaction between Gatifloxacin and Bovine Serum Albumin by Spectroscopy

有在 15 和 37 污慫楬敮猠汯瑵潩的牛的浆液白朊(BSA ) 的 gatifloxacin (HGA ) 的相互作用？

Distribution and Transfer of Gatifloxacin Between Two Microemulsion Phases with Different Structures in SDS/n-C5H11 OH/H2O System

在 n-C5H11OH/H2O=50/50 的重量比率，当钠 dodecyl 硫酸盐(SDS ) 的全部的内容是不到 6.0% 时， SDS/n-C5H11OH/H2O 的第三的混合在二不能混合的微乳液共存了。在二个阶段之间的 gatifloxacin (GTFX ) 的分发和转移被学习用紫外力并且电气化学交流阻抗系列。结果证明 GTFX 从上面的阶段( W/O )转了到更低的阶段( O/W 或 bicontinuous 微乳液)，吗但是 SDS 的小数量在 1.0 畲獧的全部的 GTFX 集中随全部的 SDS 内容的增加相应地从更低的阶段转了到上面的阶段？

泪小管结石刮除联合加替沙星眼用凝胶注入治疗泪小管炎的效果

目的探讨泪小管结石刮除联合加替沙星眼用凝胶注入治疗泪小管炎的效果。方法选择2021年1月至2022年6月九江市第一人民医院收治的泪小管炎患者60例(60只眼),按随机数字表法分为A组和B组,每组30例(30只眼)。A组给予泪小管结石刮除+0.9%氯化钠注射液冲洗治疗,B组给予泪小管结石刮除+0.9%氯化钠注射液冲洗+加替沙星眼用凝胶注入治疗,术后随访3个月,比较两组疗效,观察并发症情况。结果A组总有效率为80%,B组总有效率为100%,B组患者的临床治疗效果、复发率优于A组患者,差异有统计学意义(P<0.05),随访过程中未见不良并发症。结论采用泪小管结石刮除联合加替沙星眼用凝胶注入治疗泪小管炎,疗效确切,无不良并发症,复发率更低,值得临床推广。

加替沙星兔眼内组织分布及其药动学研究

目的 :研究加替沙星滴兔眼后在眼内组织的分布及药动学。方法 :经兔眼局部给以加替沙星 ,以高效液相色谱法测定眼内各组织中药物浓度 ,用3p97程序计算药动学参数。结果 :给药后0 .125h～1 .0h ,加替沙星在泪液、角膜、房水、虹膜 -睫状体、晶状体和玻璃体组织中最高药物浓度分别为 (1115. 75±151. 04) μg/ml、(17. 90±1. 39) μg/g、(2. 26±0 .18) μg/ml、(9. 12±0 .33) μg/g、(1. 07±0 .13) μg/g、(0 .77±0. 04) μg/g;各组织中t1/2β 分别为 (2 .14±0. 33)、(2.82±0. 54)、(3. 33±0 .43)、(3. 88±1 .21)、(3. 89±1. 43)、(3. 14±0. 43)h ;AUC0～t 分别为 (541 .77±69 .73) (μg·h)/ml、(51. 31±3 .04) (μg·h)/g、(6 .55±0.45) (μg·h)/ml、(51 .99±25. 66) (μg·h)/g、(4 19±0 .41) (μg·h)/g、(3 .25±0 .13) (μg·h)/g。结论 :加替沙星滴兔眼后在眼内各组织中渗透性好 ,浓度较高。