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1.
Medicine (Baltimore) ; 103(18): e38012, 2024 May 03.
Artigo em Inglês | MEDLINE | ID: mdl-38701320

RESUMO

Success in eradication of H. pylori is decreasing due to increasing resistant strains. In particular, side-effects due to 4-agent treatment multiple drug use are observed and treatment compliance decreases. The aim of this study was to evaluate the efficacy, reliability, and side-effect profile of the combination of amoxicillin and rabeprazole with gemifloxacin, which is a new generation quinolone, in the treatment of H. pylori infection. This study was conducted on 71 naive patients who received H. pylori eradication. All the patients were administered treatment of Amoxicillin (1000 mg twice a day) + Gemifloxacin (320 mg once a day) + rabeprazole (20 mg twice a day) for 7 days. Drug compliance and treatment tolerance were evaluated after finishing the treatment. At 1 month after the end of the treatment, H. pylori eradication was evaluated in all the patients by examining H. pylori antigen in the feces. In the evaluation after treatment, H. pylori eradication was obtained in 63 (88.7%) patients and eradication was not obtained in 8 (11.3%) patients. The treatment was not completed by 2 patients because of side-effects and noncompliance, so after exclusion of these 2 patients, successful H. pylori eradication was obtained in 63 (91.3%) of 69 patients who completed the treatment. Side-effects were seen in a total of 9 (12.7%) patients. Diarrhea, bloating, abdominal pain, and nausea-vomiting were seen in some patients, but no reflux, constipation, skin rash, listlessness-fatigue, headache, dizziness, palpitations, dry mouth, or weight loss was seen in any patient. In regions with high resistance to clarithromycin and metronidazole in particular, the combination of gemifloxacin with amoxicillin and rabeprazole can be considered for use in first-stage treatment as both the efficacy and tolerability are high.


Assuntos
Amoxicilina , Antibacterianos , Quimioterapia Combinada , Fluoroquinolonas , Gemifloxacina , Infecções por Helicobacter , Helicobacter pylori , Rabeprazol , Humanos , Rabeprazol/administração & dosagem , Rabeprazol/uso terapêutico , Amoxicilina/administração & dosagem , Amoxicilina/uso terapêutico , Infecções por Helicobacter/tratamento farmacológico , Masculino , Feminino , Projetos Piloto , Helicobacter pylori/efeitos dos fármacos , Antibacterianos/uso terapêutico , Antibacterianos/administração & dosagem , Antibacterianos/efeitos adversos , Pessoa de Meia-Idade , Adulto , Fluoroquinolonas/uso terapêutico , Fluoroquinolonas/administração & dosagem , Resultado do Tratamento , Idoso
2.
Anal Methods ; 16(16): 2556-2568, 2024 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-38592494

RESUMO

A novel luminescence-based analytical methodology was established employing a europium(III) complex with 3-allyl-2-hydroxybenzohydrazide (HAZ) as the coordinating ligand for the quantification of gemifloxacin mesylate (GMF) in pharmaceutical preparations and human plasma samples spiked with the compound. The stoichiometry of the europium complex with HAZ was determined via the Job plot and exhibited a metal-to-ligand ratio of 1 : 2. The analytical procedure relies on a rapid and significant enhancement of luminescence by the Eu(AZ)2 complex when it interacts with gemifloxacin mesylate, which allowed for the rapid detection of 96 samples within approximately 2 minutes. The thermodynamic parameters of the complexation of GMF with Eu(AZ)2 were evaluated and showed that the complexation of GMF was spontaneous with a negative ΔG. The binding constant K was 4.27 × 105 L mol-1 and DFT calculations supported GMF binding and the formation of Eu(AZ)2-GMF without further ligand exchange. The calibration graph for the luminescence quantitation of GMF was linear over a wide concentration range of 0.11-16 µg mL-1 (2.26 × 10-7 to 3.30 × 10-5 mol L-1), with a limit of quantification (LOQ) of 110 ng mL-1 (230 nmol L-1) and a detection limit (LOD) of 40 ng mL-1 (82 nmol L-1). The proposed method showed good accuracy with an average recovery of 99% with relative standard deviations of less than 5% in spiking experiments, even in complex pharmaceutical dosage forms such as tablets and in human blood plasma. Herein, the ability of the suppression of the luminescence background by using the long lag times of the lanthanide probe in a time-resolved detection scheme provided reliable and precise results, which suggests its potential for use in further real or patient samples.


Assuntos
Európio , Gemifloxacina , Humanos , Gemifloxacina/química , Gemifloxacina/sangue , Európio/química , Medições Luminescentes/métodos , Limite de Detecção , Complexos de Coordenação/química , Complexos de Coordenação/sangue , Elementos da Série dos Lantanídeos/química , Naftiridinas/sangue , Naftiridinas/química
3.
Naunyn Schmiedebergs Arch Pharmacol ; 397(1): 599-616, 2024 01.
Artigo em Inglês | MEDLINE | ID: mdl-37490123

RESUMO

Psoriasis is a lifelong immune-driven skin condition characterized by excessive epidermal overgrowth and inflammatory cell infiltration. Gemifloxacin is a fourth-generation fluoroquinolone with improved immunomodulatory and anti-inflammatory properties that are believed to possess an attractive role in psoriasis via suppressing the production of cytokines, chemokines, and eosinophil and neutrophil chemotaxis. The aim of this research is to investigate the ameliorative effects of prolonged topical gemifloxacin (GMF) alone and combined with clobetasol propionate (CLO) on an imiquimod (IMQ)-induced mouse model of psoriasis. Forty-eight Swiss albino mice were divided into six groups of eight. All groups except the negative controls got 62.5 mg of IMQ 5% topically for 8 days. Mice in the control group (controls) got Vaseline instead. Following the induction in the IMQ 5% group, mice in treatment groups CLO 0.05, GMF 1%, GMF 3%, and CLO + GMF obtained clobetasol propionate 0.05%, GMF 1% and 3%, and a combination of both, respectively, for an additional 8 days, rendering the experiment 16 days long. Our results revealed that gemifloxacin alleviated erythematous, thickened, and scaly psoriatic lesions and inhibited the tissue level of inflammatory cytokines, including interleukin (IL)-8, IL-17A, IL-23, tumor necrosis factor-α (TNF-α), and transforming growth factor-ß1 (TGF-ß1). The anti-inflammatory effect also occurred by hindering nuclear factor-kappa B (NF-κB) signaling and reversing histopathological problems. Gemifloxacin acts effectively in mitigating psoriasis-associated lesions and restricting NF-κB-mediated inflammation, recommending gemifloxacin as a promising adjuvant candidate for additional studies on the long-term treatment of autoimmune and autoinflammatory dermatoses like psoriasis.


Assuntos
Clobetasol , Psoríase , Animais , Camundongos , Imiquimode/efeitos adversos , Clobetasol/uso terapêutico , Clobetasol/farmacologia , Gemifloxacina/efeitos adversos , NF-kappa B , Fator de Maturação da Glia/farmacologia , Psoríase/induzido quimicamente , Psoríase/tratamento farmacológico , Pele , Citocinas , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Modelos Animais de Doenças , Camundongos Endogâmicos BALB C
4.
Arq Gastroenterol ; 60(3): 350-355, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37792765

RESUMO

•In eradication treatment of H. pylori gemifloxacin containing triple treatment regimen was as effective as bismuth containing quadruple treatment. •Drug adverse effects were fewer and milder in the gemifloxacin group. •Since treatment period was shorter and pills to be taken were fewer compared to quadruple treatment, patient compliance was significantly higher in the gemifloxacin group. Background - After eradication of Helicobacter pylori (H. pylori) chronic gastritis will resolve, complications due to H. pylori infection and recurrence of infection will be prevented. Objective - To determine efficacy and safety of gemifloxacin containing treatment regimen in first line treatment of H. pylori with comparison to bismuth containing quadruple therapy. Methods - This retrospective study was conducted in a tertiary care university hospital between January 2018 and January 2021 with 410 participants who were diagnosed to have H. pylori infection with biopsies obtained during upper gastrointestinal system endoscopy. Patients were distributed into two groups according to their first-line treatment regimens. First group patients were treated with amoxicillin, gemifloxacin and pantoprazole and second group patients were treated with amoxicillin, metronidazole, bismuth subcitrate and pantoprazole for seven days. Results - Intention to treat and per protocol ratios for gemifloxacin containing regimen were 90.0% and 91.2%, while quadruple treatment has these ratios as 91.7% and 93.8% respectively. Treatment success rate in both regimens were similar. But adverse effects were lower and patient compliance were better in patients who had gemifloxacin containing treatment (P<0.001). Conclusion - Gemifloxacin containing treatment regimen is as effective as bismuth containing quadruple treatment regimen for H. pylori infection and patient compliance is better in this group. Gemifloxacin containing treatment regimens may be novel and effective alternatives for eradication of H. pylori infection.


Assuntos
Gastrite , Infecções por Helicobacter , Helicobacter pylori , Humanos , Gemifloxacina/farmacologia , Gemifloxacina/uso terapêutico , Bismuto/efeitos adversos , Pantoprazol/farmacologia , Pantoprazol/uso terapêutico , Estudos Retrospectivos , Quimioterapia Combinada , Infecções por Helicobacter/tratamento farmacológico , Infecções por Helicobacter/diagnóstico , Amoxicilina/farmacologia , Metronidazol/farmacologia , Resultado do Tratamento , Gastrite/tratamento farmacológico , Antibacterianos/efeitos adversos , Inibidores da Bomba de Prótons/uso terapêutico
5.
Molecules ; 28(13)2023 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-37446807

RESUMO

Supramolecular gemifloxacin (GF) sensors have been developed. Supramolecular chemistry is primarily concerned with noncovalent intermolecular and intramolecular interactions, which are far weaker than covalent connections, but they can be exploited to develop sensors with remarkable affinity for a target analyte. In order to determine the dose form of the quinolone antibacterial drug gemifloxacin, the current study's goal is to adapt three polyvinylchloride (PVC) membrane sensors into an electrochemical technique. Three new potentiometric membrane sensors with cylindric form and responsive to gemifloxacin (GF) were developed. The sensors' setup is based on the usage of o-nitrophenyl octyl ether (o-NPOE) as a plasticizer in a PVC matrix, ß-cyclodextrin (ß-CD) (sensor 1), γ-cyclodextrin (γ-CD) (sensor 2), and 4-tert-butylcalix[8]arene (calixarene) (sensor 3) as an ionophore, potassium tetrakis (4-chlorophenyl) borate (KTpClPB) as an ion additive for determination of GF. The developed method was verified according to IUPAC guidelines. The sensors under examination have good selectivity for GF, according to their selectivity coefficients. The constructed sensors demonstrated a significant response towards to GF over a concentration range of 2.4 × 10-6, 2.7 × 10-6, and 2.42 × 10-6 mol L-1 for sensors 1, 2, and 3, respectively. The sensors showed near-Nernstian cationic response for GF at 55 mV, 56 mV, and 60 mV per decade for sensors 1, 2, and 3, respectively. Good recovery and relative standard deviations during the day and between days are displayed by the sensors. They demonstrated good stability, quick response times, long lives, rapid recovery, and precision while also exhibiting good selectivity for GF in various matrices. To determine GF in bulk and dose form, the developed sensors have been successfully deployed. The sensors were also employed as end-point indicators for titrating GF with sodium tetraphenyl borate.


Assuntos
Boratos , Plastificantes , Gemifloxacina , Plastificantes/química , Tetrafenilborato/química , Antibacterianos , Potenciometria/métodos
6.
Chemosphere ; 334: 139019, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37236274

RESUMO

A critical, challenging environmental issue is explored pollution of water supplies by discharging industrial/pharmaceutical/hospital/urban wastewaters into the aquatic environment. These needs introducing/developing novel photocatalysts/adsorbents/procedures for removing or mineralizing various pollutants in wastewater before discharging them into marine environments. Further, optimizing conditions to achieve the highest removal efficiency is an important issue. In this study, CaTiO3/g-C3N4 (CTCN) heterostructure was synthesized and characterized by some identification techniques. The simultaneous interaction effects of the experimental variables on the boosted photocatalytic activity of CTCN in the degradation of gemifloxcacin (GMF) were studied in RSM design. The optimal values for four parameters were: catalyst dosage: 0.63 g L-1, pH: 6.7, CGMF: 1 mg L-1, and irradiation time: 27.5 min, with approximately 78.2% of degradation efficiency. The quenching effects of the scavenging agents were studied to show the reactive species' relative importance in GMF photodegradation. The results illustrate that the reactive •OH plays a significant role, and the electron plays a minor role in the degradation process. The direct Z-scheme mechanism better described the photodegradation mechanism due to the great oxidative and reductive abilities of prepared composite photocatalysts. This mechanism is an approach to efficiently separating photogenerated charge carriers and improving the CaTiO3/g-C3N4 composite photocatalyst activity. The COD has been performed to study the details of the mineralization of GMF. The pseudo-first-order rat (from the Hinshelwood model) constants of 0.046 min-1 (t1/2 = 15.1 min) and 0.048 min-1 (t1/2 = 14.4 min) were respectively obtained from the GMF photodegradation data and COD results. The prepared photocatalyst retained its activity after five reusing runs.


Assuntos
Fator de Maturação da Glia , Projetos de Pesquisa , Animais , Ratos , Gemifloxacina , Cinética , Física , Águas Residuárias , Catálise
7.
Drug Deliv ; 30(1): 2185180, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36876464

RESUMO

Traditional eye drops used for topically administering drugs have poor ocular bioavailability due to the biological barriers of the eye. There is an interest to design and develop novel drug delivery systems that would extend the precorneal residence time, reduce the frequency of administration and decrease dose-related toxicity. This study aimed to prepare Nanoparticles of Gemifloxacin Mesylate and incorporate them into an in situ gel. The nanoparticles were prepared by ionic gelation technique, using 32 factorial design. Sodium tripolyphosphate (STPP) was used to crosslink Chitosan. The optimized formulation of the nanoparticles (GF4) contained 0.15% Gemifloxacin Mesylate, 0.15% Chitosan and 0.20% STPP, producing 71 nm particle size and 81.11% entrapment efficiency. The prepared nanoparticles showed biphasic release, with an initial burst release of 15% in 1.0 hr and a cumulative drug release of 90.53% at the end of 24 hrs. After that, the prepared nanoparticles were incorporated into an in situ gel, using Poloxamer 407, producing a sustained drug release with efficient antimicrobial activity against gram-positive and gram-negative bacteria as confirmed by the cup plate method.


Assuntos
Quitosana , Nanopartículas , Antibacterianos , Gemifloxacina , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Soluções Oftálmicas
8.
Environ Sci Pollut Res Int ; 30(22): 61710-61725, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-36933133

RESUMO

Appropriate material selection and proper understanding of bandgap modification are key factors for the development of efficient photocatalysts. Herein, we developed an efficient, well-organized visible light oriented photocatalyst based on g-C3N4 in association with polymeric network of chitosan (CTSN) and platinum (Pt) nanoparticles utilizing a straightforward chemical approach. Modern techniques like XRD, XPS, TEM, FESEM, UV-Vis, and FTIR spectroscopy were exploited for characterization of synthesized materials. XRD results confirmed the involvement of α-polymorphic form of CTSN in graphitic carbon nitride. XPS investigation confirmed the establishment of trio photocatalytic structure among Pt, CTSN, and g-C3N4. TEM examination showed that the synthesized g-C3N4 possesses fine fluffy sheets like structure (100 to 500 nm in size) intermingled with a dense layered framework of CTSN with good dispersion of Pt nanoparticles on g-C3N4 and CTSN composite structure. The bandgap energies for g-C3N4, CTSN/g-C3N4, and Pt@ CTSN/g-C3N4 photocatalysts were found to be 2.94, 2.73, and 2.72 eV, respectively. The photodegradation skills of each created structure have been examined on antibiotic gemifloxacin mesylate and methylene blue (MB) dye. The newly developed Pt@CTSN/g-C3N4 ternary photocatalyst was found to be efficacious for the elimination of gemifloxacin mesylate (93.3%) in 25 min and MB (95.2%) just in 18 min under visible light. Designed Pt@CTSN/g-C3N4 ternary photocatalytic framework exhibited ⁓ 2.20 times more effective than bare g-C3N4 for the destruction of antibiotic drug. This study provides a simple route towards the designing of rapid, effective visible light oriented photocatalyts for the existing environmental issues.


Assuntos
Quitosana , Nanopartículas , Antibacterianos/química , Gemifloxacina , Azul de Metileno/química , Platina , Catálise , Luz
9.
BMJ ; 379: e069931, 2022 10 04.
Artigo em Inglês | MEDLINE | ID: mdl-36195324

RESUMO

OBJECTIVE: To evaluate the association between initiation of fluoroquinolones and hospital admission or emergency department visit for suicidality. DESIGN: Population based cohort study. SETTING: IBM MarketScan database, USA. PARTICIPANTS: 2 756 268 adults (≥18 years) who initiated an oral fluoroquinolone (ciprofloxacin, levofloxacin, moxifloxacin, gemifloxacin, ofloxacin, gatifloxacin, norfloxacin, lomefloxacin, besifloxacin) or comparator antibiotic (January 2003 to September 2015) and had at least six months of continuous health plan enrollment and a diagnosis of pneumonia or urinary tract infection (UTI) three days or less before the drug initiation date. Comparator antibiotics were azithromycin in the pneumonia cohort and trimethoprim-sulfamethoxazole in the UTI cohort. Participants were matched 1:1 within each cohort on a propensity score, calculated from a multivariable logistic regression model that included 57 baseline covariates. MAIN OUTCOMES MEASURE: Primary outcome was hospital admission or emergency department visit for suicidal ideation or self-harm within 60 days after treatment initiation. Cox proportional hazard models were used to estimate hazard ratios and 95% confidence intervals. RESULTS: The pneumonia cohort included 551 042 individuals, and the UTI cohort included 2 205 526 individuals. During the 60 day follow-up, 181 events were observed in the pneumonia cohort and 966 in the UTI cohort. The adjusted hazard ratios for fluoroquinolones were 1.01 (95% confidence interval 0.76 to 1.36) versus azithromycin in the pneumonia cohort and 1.03 (0.91 to 1.17) versus trimethoprim-sulfamethoxazole in the UTI cohort. Results were consistent across sensitivity analyses and subgroups of sex, age, or history of mental illnesses. CONCLUSION: Initiation of fluoroquinolones was not associated with a substantially increased risk of admission to hospital or emergency department visits for suicidality compared with azithromycin or trimethoprim-sulfamethoxazole.


Assuntos
Suicídio , Infecções Urinárias , Adulto , Antibacterianos/uso terapêutico , Azitromicina/uso terapêutico , Ciprofloxacina/uso terapêutico , Estudos de Coortes , Serviço Hospitalar de Emergência , Fluoroquinolonas/uso terapêutico , Gatifloxacina/uso terapêutico , Gemifloxacina , Hospitais , Humanos , Levofloxacino/efeitos adversos , Moxifloxacina/uso terapêutico , Norfloxacino/uso terapêutico , Estudos Retrospectivos , Ideação Suicida , Combinação Trimetoprima e Sulfametoxazol , Infecções Urinárias/tratamento farmacológico
10.
Environ Sci Pollut Res Int ; 29(59): 89255-89272, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-35843973

RESUMO

Laccase was successfully hybridized with polyamidoamine (PAMAM) dendrimer-grafted silica-coated hercynite-copper phosphate magnetic hybrid nanoflowers (MHNFs) to increase the catalytic performance of the enzyme and apply in an effective bioremoval of gemifloxacin. For this purpose, the magnetic nanoparticles (MNPs) of hercynite were covered with a silica layer, and the core-shell SiO2@hercynite was then modified with PAMAM dendrimer to increase the surface area of the carrier for the enzyme attachment. Subsequently, the whole complex was hybridized with laccase and copper phosphate to attain a large surface area (104.3 m2 g-1). The fabricated MHNFs acquired the entrapment yield and efficiency of 90 ± 3% and 66 ± 5%, respectively. The catalytic activity of the fabricated biocatalyst was remained up to 50% after 13 reusability cycles. Approximately 90% of gemifloxacin was removed by the constructed MHNFs after 3 h incubation by adsorption and degradation mechanisms. The biotransformation products were then identified, and degradation pathways were proposed as defluorination, decarboxylation, elimination of a cyclopropyl group, and cleavage of the pyrrolidine moiety. Furthermore, the toxicity of gemifloxacin was effectively diminished against some bacterial strains.


Assuntos
Dendrímeros , Lacase , Lacase/metabolismo , Dióxido de Silício , Cobre , Gemifloxacina , Fosfatos , Fenômenos Magnéticos , Enzimas Imobilizadas
11.
Int J Mol Sci ; 23(4)2022 Feb 14.
Artigo em Inglês | MEDLINE | ID: mdl-35216223

RESUMO

Four novel ligand-metal complexes were synthesized through the reaction of Fe(III), pleaseCo(II), Zn(II), and Zr(IV) with Schiff base gemifloxacin reacted with ortho-phenylenediamine (GMFX-o-phdn) to investigate their biological activities. Elemental analysis, FT-IR, 1H NMR, UV-visible, molar conductance, melting points, magnetic susceptibility, and thermal analyses have been carried out for insuring the chelation process. The antimicrobial activity was carried out against Monilinia fructicola, Aspergillus flavus, Penicillium italicum, Botrytis cinerea, Escherichia coli, Bacillus cereus, Pseudomonas fluorescens, and P. aeruginosa. The radical scavenging activity (RSA%) was in vitro evaluated using ABTS method. FT-IR spectra indicated that GMFX-o-phdn chelated with metal ions as a tetradentate through oxygen of carboxylate group and nitrogen of azomethine group. The data of infrared, 1H NMR, and molar conductivity indicate that GMFX-o-phdn reacted as neutral tetra dentate ligand (N2O2) with metal ions through the two oxygen atoms of the carboxylic group (oxygen containing negative charge) and two nitrogen atoms of azomethine group (each nitrogen containing a lone pair of electrons) (the absent of peak corresponding to ν(COOH) at 1715 cm-1, the shift of azomethine group peak from 1633 cm-1 to around 1570 cm-1, the signal at 11 ppm of COOH and the presence of the chloride ions outside the complex sphere). Thermal analyses (TG-DTG/DTA) exhibited that the decaying of the metal complexes exists in three steps with the final residue metal oxide. The obtained data from DTA curves reflect that the degradation processes were exothermic or endothermic. Results showed that some of the studied complexes exhibited promising antifungal activity against most of the tested fungal pathogens, whereas they showed higher antibacterial activity against E. coli and B. cereus and low activity against P. fluorescens and P. aeruginosa. In addition, GMFX-o-phdn and its metal complexes showed strong antioxidant effect. In particular, the parent ligand and Fe(III) complex showed greater antioxidant capacity at low tested concentrations than that of other metal complexes where their IC50 were 169.7 and 164.6 µg/mL, respectively.


Assuntos
Anti-Infecciosos/farmacologia , Compostos Férricos/farmacologia , Gemifloxacina/farmacologia , Metais/farmacologia , Bases de Schiff/farmacologia , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Complexos de Coordenação/farmacologia , Humanos , Ligantes , Testes de Sensibilidade Microbiana/métodos
12.
J Exp Psychol Gen ; 151(9): 2173-2194, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35157482

RESUMO

It is well established that the processing of hand-, mouth-, and foot-related action terms can activate areas of the motor cortex that are involved in the planning and execution of the described actions. In the present study, the sensitivity of these motor structures to language processes was exploited to test linguistic theories on information layering. Human languages possess a variety of linguistic devices, so-called presupposition triggers, that allow us to convey background information without asserting it. A statement such as "Marie stopped smoking" presupposes, without asserting it, that Marie used to smoke. How such presupposed information is represented in the brain is not yet understood. Using a grip-force sensor that allows capturing motor brain activity during language processing, we investigated effects of information layering by comparing asserted information that is known to trigger motor activity ("In the living room, Peter irons his shirt") with information embedded under a presuppositional factive verb construction ("Louis knows that Peter irons his shirt"; Experiment 1) and a nonfactive verb construction ("Louis believes that Peter irons his shirt"; Experiment 2). Furthermore, we examined whether the projection behavior of a factive verb construction modulates grip force under negation ("Louis does not know that Peter irons his shirt"; Experiment 3). The data show that only the presupposed action verb in affirmative contexts (Experiment 1) triggers an increase in grip force comparable to the one of asserted action verbs, whereas the nonfactive complement and projection structure show a weaker response (Experiments 2 and 3). While the first two experiments seem to confirm the sensitivity of the grip-force response to the construction of a plausible situation or event model, in which the motor action is represented as taking place, the third one raises the question of how robust this hypothesis is and how it can take the specificity of projection into account. (PsycInfo Database Record (c) 2022 APA, all rights reserved).


Assuntos
Encéfalo , Idioma , Encéfalo/fisiologia , Gemifloxacina , Mãos , Força da Mão , Humanos
13.
J Pharm Sci ; 111(5): 1497-1508, 2022 05.
Artigo em Inglês | MEDLINE | ID: mdl-34929155

RESUMO

Ocular infections are classified into superficial keratitis, conjunctivitis or deep infections such as corneal abscesses and blepharitis. Herein, we focused on the development of formulation approaches that could prolong the residence time of gemifloxacin (GM) and enhance its corneal penetration to facilitate GM effects both superficially and at the deep tissues. Ionic gelation method was used to prepare eight forms of GM nanoparticles (NPs) formulated from chitosan polymer using sodium tripolyphosphate (TPP)-induced precipitation method. Differential scanning colorimetry (DSC) and X-ray diffraction (XRD) demonstrated the interaction between the chitosan and GM. Particle size, entrapment efficiency and cumulative in vitro release were used to select the optimal formula using Design Expert® software. The mean diameter of the selected NPs was 158. 4 nm. The average entrapment efficiency and cumulative release exhibited by the formulated NPs were 46.6% and 74.9%, respectively. Pharmacokinetics studies carried out on rabbits revealed that the ocularly-administered NPs significantly increased the loaded GM concentration in the tear and aqueous humour samples that suggested enhancement of precorneal retention and transcorneal permeation, respectively. Furthermore, ocular pharmacodynamic studies conducted on rabbits following ocular infection with Staphylococcus aureus or Pseudomonas aeruginosa showed that the administered NPs augmented the antibacterial activity of the delivered GM. This was demonstrated via the histopathological examination of the dissected corneas that showed preserved histological features and reduced bacterial keratitis on using the GM NPs rather than GM solution. Moreover, the GM NPs-treated corneas showed lower viable bacterial counts than the GM solution-treated corneas. Accordingly, our study illustrated the capability of the chitosan NPs to promote the antibacterial activity of GM against eye infections via ocular administration.


Assuntos
Quitosana , Nanopartículas , Animais , Antibacterianos/farmacologia , Quitosana/farmacologia , Córnea , Portadores de Fármacos/farmacologia , Gemifloxacina/farmacologia , Tamanho da Partícula , Coelhos
14.
Pak J Pharm Sci ; 34(5(Supplementary)): 1983-1988, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34836870

RESUMO

Moxifloxacin and gemifloxacin were tested on isolated rabbits' jejunal preparations as little is known about its effects on gastrointestinal tissues. Moxifloxacin and gemifloxacin were tested in concentrations 0.01-10µg/mL for possible effect(s) on isolated rabbits' jejunal preparations. The drugs were applied on spontaneous, on low K+ (20mM)-induced contractions and on high K+ (80mM)-induced contractions. Response was plotted as % of its respective controls. EC50 for Moxifloxacin and Gemifloxacin on spontaneous (without Glibenclamide) contractions are 2.83±0.5µg/mL and 1.11±0.2µg/mL, respectively. Moxifloxacin and Gemifloxacin relaxed the low K+ (20mM) -induced contractions, which were inhibited in presence of Glibenclamide (3µM). Our result indicates that the relaxant activity of Moxifloxacin and Gemifloxacin is mediated possibly through activation of ATP-sensitive potassium channels (KATP). The relaxant effect of Moxifloxacin and Gemifloxacin is predominantly mediated by activation of ATP-Sensitive potassium channels (KATP), which could be cause of one of relaxing mechanisms.


Assuntos
Gemifloxacina/farmacologia , Canais KATP/efeitos dos fármacos , Moxifloxacina/farmacologia , Parassimpatolíticos/farmacologia , Animais , Bioensaio , Feminino , Glibureto/farmacologia , Jejuno/efeitos dos fármacos , Masculino , Contração Muscular/efeitos dos fármacos , Relaxantes Musculares Centrais/farmacologia , Relaxamento Muscular/efeitos dos fármacos , Coelhos
15.
Artif Cells Nanomed Biotechnol ; 49(1): 661-671, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34818127

RESUMO

Drug-loaded nanoparticles (NPs) allow specific accumulation and controlled release of drugs to infected tissues with minimal cytotoxicity. In this study, gemifloxacin conjugated silver nanoparticles (Gemi-AgNPs) were synthesized, and the amplification of their antibacterial potential against the human pathogen as well as their stability was monitored under physiological conditions. Fourier transform infrared spectroscopy (FTIR) analysis demonstrated the interaction between -NH2 and -OH functional moiety and the metal surface. The morphological analyses via transmission electron microscopy revealed that Gemi-AgNPs has a round oval shape and average particle size of 22.23 ± 2 nm. The antibacterial and antibiofilm activities of these NPS showed that Gemi-AgNPs exhibit excellent antimicrobial and biofilm inhibition activity against human pathogens, namely, Proteus mirabilis (P. mirabilis) and methicillin-resistant Staphylococcus aureus (MRSA). A significant increase in the antibiofilm activity of Gemi-AgNPs was confirmed by crystal violet, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) staining, and microscopic analysis. Gemi-AgNPs exhibited the ability to inhibit urease with an IC50 value of 57.4 ± 0.72 µg/mL. The changes in the bacterial cell morphology were analyzed via TEM, which revealed that cell membranes disrupted and completely destroyed the cell morphology by the treatment of Gemi-AgNPs.


Assuntos
Nanopartículas Metálicas , Staphylococcus aureus Resistente à Meticilina , Antibacterianos/química , Gemifloxacina , Humanos , Nanopartículas Metálicas/química , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Prata/química , Prata/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier
16.
Chem Biodivers ; 18(9): e2100365, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34288421

RESUMO

String of Fe(III), Cu(II), Zn(II) and Zr(IV) complexes were synthesized with tetradentateamino Schiff base ligand derived by condensation of ethylene diamine with gemifloxacin. The novel Schiff base (4E,4'E)-4,4'-(ethane-1,2-diyldiazanylylidene)bis{7-[(4Z)-3-(aminomethyl)-4-(methoxyimino)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid} (GMFX-en) and its metal complexes were identified and confirmed by elemental analyses, FT-IR, UV/VIS, 1 H-NMR spectra, magnetic susceptibility, conductometric measurements and thermal analyses. The FT-IR spectral data showed the chelation behavior of GMFX-en toward the metal ions through oxygen of carboxylate group and nitrogen of azomethine group. In the light of all spectral data, these complexes presumably have octahedral geometry configurations. Thermal analysis specified that the decaying of the metal complexes exist in two or three steps with the final residue metal oxides. Antimicrobial activity of the new prepared metal complexes was screened against some common phytopathogens and their mode of action has been also discussed. The potential phytotoxic effectiveness of the new complexes was furthermore inspected on two commonly experimental plants. The complexes showed significant antimicrobial and phytotoxic effects against the majority of tested phytopathogens and the two tested plants, respectively. The potential antimicrobial activity of the complexes proved their possibility to be used successfully in agropharmacutical industry to control many serious phytopathogens. The phytotoxicity of the studied complexes also indicated their possibility as potential bio-based herbicides alternatives to weed control in crop fields.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Complexos de Coordenação/farmacologia , Gemifloxacina/farmacologia , Metais Pesados/farmacologia , Bases de Schiff/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Bactérias/efeitos dos fármacos , Complexos de Coordenação/síntese química , Complexos de Coordenação/química , Fungos/efeitos dos fármacos , Gemifloxacina/química , Lepidium sativum/efeitos dos fármacos , Solanum lycopersicum/efeitos dos fármacos , Metais Pesados/química , Testes de Sensibilidade Microbiana , Bases de Schiff/química
17.
Mini Rev Med Chem ; 21(5): 586-601, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33038911

RESUMO

1, 8- Naphthyridine nucleus belongs to significant nitrogen-containing heterocyclic compounds which has garnered the interest of researchers due to its versatile biological activities. It is known to be used as an antimicrobial, anti-psychotic, anti-depressant, anti-convulsant, anti- Alzheimer's, anti-cancer, analgesic, anti-inflammatory, antioxidant, anti-viral, anti-hypertensive, antimalarial, pesticides, anti-platelets, and CB2 receptor agonist, etc. The present review highlights the framework of biological properties of synthesized 1, 8-naphthyridine derivatives developed by various research groups across the globe.


Assuntos
Naftiridinas/farmacologia , Nitrogênio/química , Animais , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/química , Anticonvulsivantes/farmacologia , Antidepressivos/farmacologia , Antipsicóticos/farmacologia , Enoxacino/farmacologia , Fluoroquinolonas/farmacologia , Gemifloxacina/farmacologia , Humanos , Ácido Nalidíxico/farmacologia , Naftiridinas/síntese química , Polimedicação , Tiazóis/farmacologia
18.
Tuberk Toraks ; 68(2): 184-187, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-32755119

RESUMO

We present a case of tendon rupture and subcutaneous bleeding after administration of gemifloxacin for the treatment of lower respiratory tract infection. Fluoroquinolone-induced tendinopathy is a rare but increasingly acknowledged adverse effect of this group of antibiotics. Most of the cases occur in the Achilles tendon and can lead to tendon rupture. Possible predisposing risk factors include steroid use, patients with renal failure or kidney transplantation, old age and being an athlete.


Assuntos
Anti-Infecciosos/efeitos adversos , Gemifloxacina/efeitos adversos , Tendinopatia/induzido quimicamente , Tendão do Calcâneo , Antibacterianos/efeitos adversos , Fluoroquinolonas/efeitos adversos , Humanos , Masculino , Pessoa de Meia-Idade , Infecções Respiratórias/induzido quimicamente , Fatores de Risco , Tendinopatia/complicações , Tendinopatia/terapia
19.
J Hazard Mater ; 382: 121070, 2020 01 15.
Artigo em Inglês | MEDLINE | ID: mdl-31470301

RESUMO

The aim of the present study was to investigate the photocatalytic performance of biochar (BC)-incorporated Zn-Co-layered double hydroxide (LDH) nanostructures in gemifloxacin (GMF) degradation as a model pharmaceutical pollutant. The as-prepared Zn-Co-LDH@BC showed high photocatalytic efficiency due to the enhanced separation of photo-generated charge carriers using cobalt hydroxide as well as inhibiting the agglomeration of LDH nanostructures by incorporation of BC. According to the results, 92.7% of GMF was degraded through photocatalysis in the presence of Zn-Co-LDH catalyst. The photocatalytic performance of BC-incorporated Zn-Co-LDH was highly dependent on the solute concentration and photocatalyst dosage. The addition of ethanol caused more inhibiting effect than that of benzoquinone (BQ), indicating the major role of •OH in decomposition of GMF compared to the negligible role of O2•-. A greater enhancement in the photocatalytic degradation of GMF was obtained when the photoreactor containing Zn-Co-LDH@BC nanostructures was oxygenated. Less than 10% drop in the removal efficiency of GMF was observed within five successive operational runs. The results of chemical oxygen demand (COD) analysis indicated the COD removal efficiency of about 80% within 200 min, indicating the acceptable mineralization of GMF. The reaction pathways were also proposed for the photocatalytic conversion of GMF under UV light irradiation.


Assuntos
Antibacterianos/química , Carvão Vegetal/química , Cobalto/química , Gemifloxacina/química , Hidróxidos/química , Nanocompostos/química , Zinco/química , Catálise , Carvão Vegetal/efeitos da radiação , Cobalto/efeitos da radiação , Hidróxidos/efeitos da radiação , Nanocompostos/efeitos da radiação , Processos Fotoquímicos , Raios Ultravioleta , Zinco/efeitos da radiação
20.
J Formos Med Assoc ; 119(1 Pt 2): 367-376, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31262613

RESUMO

BACKGROUND/PURPOSE: Little remains known regarding whether newer FQ with less anti-mycobacterial activity (gemifloxacin) would reduce treatment delay. METHODS: We identified one hospital-based cohort (HBC) and one population-based cohort (PBC) including patients receiving amoxicillin/clavulanate acid (Beta-lactam), gemifloxacin (Gemi), and fluoroquinolones other than gemifloxacin (Non-Gemi FQ) prior to TB treatment. RESULTS: A total of 201 patients in the HBC and 3544 patients in the PBC were recruited. After 1:1 propensity score matching, TB treatment delay was statistically insignificant between Beta-lactam, Gemi group, and Non-Gemi FQ group in HBC (Beta-lactam vs Gemi: 22.3 ± 21.4 d vs 28.6 ± 27.9 d, p = 0.292; Beta-lactam vs Non-Gemi FQ: 33.3 ± 26.5 d vs 50.3 ± 47.3 d, p = 0.135) and PBC (Beta-lactam vs Gemi: 26.4 ± 29.1 vs 25.0 ± 28.1, p = 0.638; Beta-lactam vs Non-Gemi FQ: 29.4 ± 36.0 d vs 32.7 ± 35.0 d, p = 0.124, Non-Gemi FQ vs Gemi: 28.4 ± 33.0 d vs 25.0 ± 28.1 d, p = 0.29). CONCLUSION: While limited by relatively low case number, our study showed that use of gemifloxacin neither results in nor reduces delay in TB treatment. The issue of FQ use on TB treatment delay was also not observed in our study. Early survey and maintaining high clinical alertness remains the key to reducing TB treatment delay.


Assuntos
Antibacterianos/uso terapêutico , Fluoroquinolonas/uso terapêutico , Tempo para o Tratamento/estatística & dados numéricos , Tuberculose/tratamento farmacológico , Adulto , Idoso , Idoso de 80 Anos ou mais , Antituberculosos/uso terapêutico , Estudos de Coortes , Bases de Dados Factuais , Feminino , Gemifloxacina/uso terapêutico , Hospitais/estatística & dados numéricos , Humanos , Masculino , Pessoa de Meia-Idade , Pontuação de Propensão , Taiwan
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