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1.
J Med Microbiol ; 68(8): 1227-1232, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31215858

RESUMO

PURPOSE: Haemophilus influenzae strains with low susceptibility to quinolones have recently emerged in the paediatric field in Japan. These strains are judged as 'susceptible' in routine susceptibility tests, although they may survive after quinolone treatment. Therefore, we aimed to construct a simple and cost-effective identification method for low-susceptibility strains using disc diffusion assays. METHODOLOGY: A total of 33 H. influenzae clinical isolates and a control strain were used. For the disc diffusion assay, levofloxacin, norfloxacin, nalidixic acid and pipemidic acid were employed. Correlations between the inhibition zone diameter and amino acid substitutions were evaluated. RESULTS: All of the tested strains formed clear inhibition zones on both levofloxacin and norfloxacin discs. By contrast, none of the low-susceptibility strains showed inhibition zones against nalidixic acid, while the low-susceptibility strains with amino acid substitutions in both GyrA and ParC did not show inhibition zones against pipemidic acid discs, indicating that low-susceptibility strains can be detected with high sensitivity and specificity by the presence or absence of inhibition zones for earlier quinolones. CONCLUSION: A disc diffusion test combining results from nalidixic acid and pipemidic acid can detect low-susceptibility strains harbouring amino acid substitutions without the need for genetic analysis. This test can help reduce inappropriate and unnecessary fluoroquinolone use.


Assuntos
Antibacterianos/farmacologia , Farmacorresistência Bacteriana/efeitos dos fármacos , Infecções por Haemophilus/microbiologia , Haemophilus influenzae/efeitos dos fármacos , Quinolonas/farmacologia , Substituição de Aminoácidos , Proteínas de Bactérias/genética , Criança , DNA Girase/genética , DNA Topoisomerase IV/genética , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Farmacorresistência Bacteriana/genética , Haemophilus influenzae/genética , Haemophilus influenzae/isolamento & purificação , Humanos , Japão , Ácido Nalidíxico/farmacologia , Ácido Pipemídico/farmacologia , Sensibilidade e Especificidade
2.
Int J Mol Sci ; 20(2)2019 Jan 18.
Artigo em Inglês | MEDLINE | ID: mdl-30669399

RESUMO

Pipemidic acid (HPPA) is a quinolone antibacterial agent used mostly to treat gram-negative infections of the urinary tract, but its therapeutic use is limited because of its low solubility. Thus, to improve drug solubility, natural cyclodextrins (CDs) are used for their ability of including guest molecules within their cavities. The aim of this work was to evaluate the antibacterial activity and the preliminary anticancer activity of HPPA included into Heptakis (2,3,6-tri-O-methyl)-ß-cyclodextrin (TRIMEB) as a possible approach for a new innovative formulation. The inclusion complex of HPPA with TRIMEB was prepared in solid state by the kneading method and confirmed by FT-IR and powered X-ray diffraction. The association in aqueous solutions of pipemidic acid with TRIMEB was investigated by UV-Vis spectroscopy. Job's plots have been drawn by UV-visible spectroscopy to confirm the 1:1 stoichiometry of the host⁻guest assembly. The antibacterial activity of HPPA, TRIMEB and of their complex was tested on Escherichia coli, Pseudomonas aeruginosa, and Staphilococcus aureus. The complex was able to increase 47.36% of the median antibacterial activity of the free HPPA against E. coli (IC50 = 249 µM vs. 473 µM). Furthermore, these samples were tested on HepG-2 and MCF-7. After 72 h, the median tumoral cytotoxicity exerted by the complex was increased by 78.08% and 94.27% for HepG-2 and MCF-7 respectively, showing a stronger bioactivity of the complex than the single HAPPA.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Ácido Pipemídico/química , Ácido Pipemídico/farmacologia , beta-Ciclodextrinas/química , Bactérias/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
3.
Analyst ; 143(24): 5940-5949, 2018 Dec 03.
Artigo em Inglês | MEDLINE | ID: mdl-30345433

RESUMO

AFM-IR is a photothermal technique that combines AFM and infrared (IR) spectroscopy to unambiguously identify the chemical composition of a sample with tens of nanometer spatial resolution. So far, it has been successfully used in contact mode in a variety of applications. However, the contact mode is unsuitable for soft or loosely adhesive samples such as polymeric nanoparticles (NPs) of less than 200 nm of wide interest for biomedical applications. We describe here the theoretical basis of the innovative tapping AFMIR mode that can address novel challenges in imaging and chemical mapping. The new method enables gaining information not only on NP morphology and composition, but also reveals drug location and core-shell structures. Whereas up to now the locations of NP components could only be hypothesized, tapping AFM-IR allows accurately visualizing both the location of the NPs' shells and that of the incorporated drug, pipemidic acid. The preferential accumulation of the drug in the NPs' top layers was proved, despite its low concentration (<1 wt%). These studies pave the way towards the use of tapping AFM-IR as a powerful tool to control the quality of NP formulations based on individual NP detection and component quantification.


Assuntos
Microscopia de Força Atômica/métodos , Nanopartículas/química , Poliésteres/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/química , Espectrofotometria Infravermelho/métodos , Ácido Pipemídico/química , Álcool de Polivinil/química , Tensoativos/química
4.
Arch Pharm Res ; 41(6): 633-645, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29619676

RESUMO

This article describes the synthesis and antimicrobial activity evaluation of new pipemidic acid derivatives. New compounds were obtained on the basis of Mannich reaction of 4,5-disubstituted 1,2,4-triazole-3-thiones with pipemidic acid. Antimicrobial tests revealed high antibacterial activity of obtained derivatives. Gram-negative rods belonging to Enterobacteriaceae family were particularly most sensitive to new pipemidic acid derivatives. Synthesized compounds exhibited very strong activity towards Proteus mirabilis ATCC 12453, Salmonella typhimurium ATCC 14028 and Escherichia coli ATCC 25922. The minimum inhibitory concentrations of new pipemidic acid derivatives which inhibited the growth of these bacteria were 0.98-7.81 µg/ml, 0.98-7.81 µg/ml and 0.98-3.91 µg/ml, respectively. The antibacterial activity of newly synthesized pipemidic acid derivatives in many cases was far better than the activity of substances used as positive controls (nitrofurantoin, cefuroxime, ampicillin and pipemidic acid).


Assuntos
Antibacterianos/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Ácido Pipemídico/farmacologia , Antibacterianos/síntese química , Testes de Sensibilidade Microbiana , Ácido Pipemídico/análogos & derivados , Ácido Pipemídico/síntese química , Tionas/química , Triazóis/química
5.
Mol Divers ; 22(1): 83-93, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29138963

RESUMO

A series of 1-substituted-1H-tetrazole-5-thiol building blocks were synthesized and introduced to the N-4 piperazinyl group at C-7 position of the quinolone core, and these novel compounds (5a-g and 8a-g) were screened for their antibacterial and antiproliferative activities. Bioactive assay studies manifested that most of new compounds exhibited significant antibacterial activity against the tested strains, including multi-drug-resistant MRSA in comparison with reference drugs ciprofloxacin, streptomycin B and pipemidic acid. Among the synthesized compounds, only ciprofloxacin (5a-g) derivatives displayed significant activity ([Formula: see text]) compared to reference drugs. In addition, these compounds were evaluated for their in vitro inhibition of human cancer cell lines viz human cervical carcinoma cell line (SiHA), breast adenocarcinoma (MDA-MB-235) and human pancreas carcinoma (PANC-1) cell lines by using the SRB assay method. Most of the target compounds showed broad potent growth inhibition activity ([Formula: see text]) against all the tested cancer cell lines compared with reference drug. The most promising active compounds in this series were 5c, 5d, 8c, 8d and 8f endowed with excellent antiproliferative activity. A new class of compounds was designed rationally by introducing tetrazole building block on N-4 piperazinyl group at C-7 position of quinolones core. The titled compounds were evaluated for their preliminary antibacterial and antiproliferative activities.


Assuntos
Antibacterianos/síntese química , Antibacterianos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Ciprofloxacino/química , Ácido Pipemídico/química , Tetrazóis/síntese química , Tetrazóis/farmacologia , Antibacterianos/química , Antineoplásicos/química , Bactérias/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade , Tetrazóis/química
6.
J Grad Med Educ ; 9(2): 255, 2017 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-28439366
7.
Acta Med Indones ; 48(3): 184-192, 2016 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-27840352

RESUMO

AIM: to evaluate the analgesic effect, the side effects and the safety of analgesics following endoscopic urological procedure. METHODS: eighty patients who underwent endoscopic urological surgery at Kardinah Hospital, Tegal from June to July 2015 were divided into four groups. The experimental group was administered analgesic for 4 days pipemidic acid (A) 400 mg bid, or phenazopyridine (B) 200 mg tid, or sodium diclofenac (C) 50 mg bid and the control (D) group was administered placebo tid for 4 days. The analgesic effects were assessed using Visual Analog Scale (VAS). Association between variables was assessed using Cramers V and Kruskall Wallis. RESULTS: the endoscopic urological procedures consisted of 30 patients for URS, 6 patients for lithotripsy, 17 patients for TURP, 24 patients for removal JJ stent and 3 patients for cystoscopy. The mean age of group A, B, C and D (control) was 50.1 (13.7), 50.7 (14.8), 49.1 (13.4), and 49.6 (14.3) years, respectively, and follow-up period was 7 days. The VAS score in all experimental groups was less than control group on day 1 to 7 following endoscopic urological procedures (p<0.05). In the experimental group, there was no difference between groups B and C (p>0.05). Group A demonstrated a more favourable analgesic effect than B and C (p<0.05). No serious side effects were detected in any of the cases. CONCLUSION: we conclude that oral analgesics are effective for pain relief following endoscopic urological surgery. Pipemidic acid was found to have a superior analgesic effect than phenazopyridine HCl and sodium diclofenac.


Assuntos
Anestésicos Locais/uso terapêutico , Anti-Infecciosos Urinários/uso terapêutico , Anti-Inflamatórios não Esteroides/uso terapêutico , Diclofenaco/uso terapêutico , Percepção da Dor , Fenazopiridina/uso terapêutico , Ácido Pipemídico/uso terapêutico , Procedimentos Cirúrgicos Urológicos , Método Duplo-Cego , Endoscopia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Estudos Prospectivos
8.
J Inorg Biochem ; 162: 280-285, 2016 09.
Artigo em Inglês | MEDLINE | ID: mdl-26979255

RESUMO

The antimicrobial properties of copper have been known to mankind since the ancient times. In a coordination chemistry approach to develop novel antimicrobial agents, the quinolone antimicrobial agents ciprofloxacin (Hcipro) and pipemidic acid (Hpia), as well as dimers thereof (piperazinyl-linked with a p-xylenyl moiety) were complexed with copper(II). The synthesis and antimicrobial evaluation of bis(ciprofloxacino)copper(II) [Cu(cipro)2], bis(pipemido)copper(II) [Cu(pia)2], and the corresponding dimer complexes, [Cu2(ciproXcipro)2] and [Cu2(piaXpia)2], are reported. No combinational or synergistic effect between copper(II) and the respective quinolone ligands was observed in vitro.


Assuntos
Antibacterianos/síntese química , Ciprofloxacino/química , Complexos de Coordenação/síntese química , Cobre/química , Ácido Pipemídico/química , Antibacterianos/farmacologia , Complexos de Coordenação/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Negativas/crescimento & desenvolvimento , Bactérias Gram-Positivas/efeitos dos fármacos , Bactérias Gram-Positivas/crescimento & desenvolvimento , Ligantes , Viabilidade Microbiana/efeitos dos fármacos
9.
Urologiia ; (1): 4-7, 2015.
Artigo em Russo | MEDLINE | ID: mdl-26094378

RESUMO

This paper presents evaluation of rehabilitation effectiveness of 113 patients aged 19-78 years diagnosed as having mixed and uric acid stones. 88 patients with uric acid stones 0,5-2,5 cm were assigned to group 1 and treated with Trometamol N parenteral litholis and a complex metaprophilaxis by dietary supplements Prolit and Urisan. 25 patients with mixed stones 1-3,5 cm were allocated to group 2 and treated with external shock wave lithotripsy and complex metaprophilaxis by dietary supplements Prolit Super Septo and Urisan. Positive results were achieved in all the patients. In the patients of group 1 the stones were completely dissolved. In group 2 treatment resulted in stone disintegration and clearance of small fragments 0,4 cm after partial dissolution.


Assuntos
Anti-Infecciosos Urinários/administração & dosagem , Suplementos Nutricionais , Ácido Pipemídico/administração & dosagem , Ácido Úrico , Urolitíase/reabilitação , Adulto , Idoso , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Urolitíase/diagnóstico , Urolitíase/metabolismo
10.
Pak J Pharm Sci ; 28(2): 557-9, 2015 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-25730788

RESUMO

Urinary Tract Infections are the largest group of infections after the respiratory tract infections. In 85% of the cases the causative organism is E. Coli. A clinical trial was conducted to evaluate the efficacy of coded herbal formulation "Cranoff" (Test drug) for the treatment of Urinary tract infection comparing with Urixin (Control). One hundred and thirty patients suffering from Urinary tract infection from both groups (Males: 45, mean age: 34±14 and females: 85, mean age: 33±13 year, range: 15-55) were enrolled in the trial and divided in to two groups according to treatment regimens. Cranoff (Test drug) 500mg two capsules and Urixin (Pipemidic Acid Trihydrate JP15) (Control) 400mg capsules twice daily were prescribed for 2-3 weeks. Urinary tract infection was improved in 23 (35.38%) patients out of 65 patients by the use of Cranoff (Test drug), and in 15 (23.07%) patients out of 65 by the use of Urixin (Control drug). Furthermore, there was a significant improvement in Urinary tract infection associated clinical features as compared to Urixin. It is concluded that Cranoff possesses a therapeutic value for the improvement of urinary tract infection and its associated symptoms as compared to Urixin.


Assuntos
Anti-Infecciosos Urinários/uso terapêutico , Fitoterapia , Ácido Pipemídico/uso terapêutico , Infecções Urinárias/tratamento farmacológico , Adolescente , Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade
11.
Int J Mol Sci ; 14(7): 13022-41, 2013 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-23799358

RESUMO

The aptitude of cyclodextrins (CDs) to form host-guest complexes has prompted an increase in the development of new drug formulations. In this study, the inclusion complexes of pipemidic acid (HPPA), a therapeutic agent for urinary tract infections, with native ß-CD were prepared in solid state by kneading method and confirmed by FT-IR and 1H NMR. The inclusion complex formation was also characterized in aqueous solution at different pH via UV-Vis titration and phase solubility studies obtaining the stability constant. The 1:1 stoichiometry was established by a Job plot and the inclusion mechanism was clarified using docking experiments. Finally, the antibacterial activity of HPPA and its inclusion complex was tested on P. aeruginosa, E. coli and S. aureus to determine the respective EC50s and EC90s. The results showed that the antibacterial activity of HPPA:ß-CD against E. coli and S. aureus is higher than that of HPPA. Furthermore, HPPA and HPPA:ß-CD, tested on human hepatoblastoma HepG2 and MCF-7 cell lines by MTT assay, exhibited, for the first time, antitumor activities, and the complex revealed a higher activity than that of HPPA. The use of ß-CD allows an increase in the aqueous solubility of the drug, its bioavailability and then its bioactivity.


Assuntos
Ácido Pipemídico , beta-Ciclodextrinas , Varredura Diferencial de Calorimetria , Ciclodextrinas/química , Escherichia coli , Humanos , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Staphylococcus aureus , beta-Ciclodextrinas/química
12.
Cell Physiol Biochem ; 32(7): 96-110, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24429818

RESUMO

BACKGROUND: With the rise of antibiotic resistance, new alternatives are being sought to effectively modulate the characteristics of gut microbiota to obtain pathogen resistance without the use of antibiotics. In the past, an oligosaccharide derivative of carrots, galursan HF 7K (GHF7K), has been used clinically in Austria and recently in the fowl-industry to promote health. This study examined the potential role of GHF7K as a prebiotic to alter the gut microbiota in mice. METHODS: Mice were fed either a control diet (CT) or a diet containing 2% GHF7K in the water and chow for 2 weeks, and weight, food and water consumption, gut microbiota and ion composition of the intestinal fluid were examined. RESULTS: Dietary supplement of GHF7K did not alter mouse weight or daily food consumption. Additionally, no changes were observed in the total number of luminal or mucosa-associated bacteria populations in GHF7K-fed mice. GHF7K supplementation significantly altered the composition of luminal, and to a less extent, mucosa-associated bacterial populations at the level of the phyla, with region-specific differences. Similar to antibiotic use, Proteobacteria number was increased in the ileum and colon of GHF7K-fed mice, with no changes in the number of beneficial Lactobacillus and Bifidobacterium genera of phylum Firmicutes. Corresponding with the altered gut microbiota, changes in the ion composition of the intestinal fluid were observed. An increased Cl(-) concentration was observed in the duodenum and jejunum, while the Na(+) concentration was increased in the cecum of GHF7K-fed mice. Decreases were observed in the K(+) concentration in the cecum and distal colon. CONCLUSIONS: Dietary supplement of GHF7K is capable of altering the gut microbiota, which correlates to changes in the intestinal environment. These data suggest that GHF7K dietary supplement can purposefully be used to alter the gut microbiota, and thus could potentially represent an alternative approach to prophylactic antibiotic use.


Assuntos
Intestinos/efeitos dos fármacos , Microbiota/efeitos dos fármacos , Ácido Pipemídico/administração & dosagem , Prebióticos , Animais , Antibacterianos/administração & dosagem , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Peso Corporal , Suplementos Nutricionais , Intestinos/microbiologia , Camundongos
13.
ScientificWorldJournal ; 2013: 452107, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24453852

RESUMO

We retrospectively evaluated the efficacy of prophylaxis with pipemidic acid and levofloxacin in transrectal ultrasound guided prostate biopsy (TRUSP-Bx). From January 2002 to December 2004, patients receiving oral pipemidic acid 500 mg twice daily for three days with or without a preoperative intravenous cefazolin 1 gm injection comprised group A. Between January 2005 and December 2009, patients receiving oral levofloxacin 500 mg one hour before biopsy comprised group B. We calculated the annual febrile urinary tract infection (fUTI) rates. Patients' characteristics, including age, prophylactic antibiotics, biopsy core numbers, pathologic results, PSA, and the spectrums and susceptibility of pathogens, were also evaluated. A total of 1313 (35.5%) patients belonged to group A, while 2381 (64.5%) patients belonged to group B. Seventy-three patients experienced postoperative infectious complications. There was a significant difference in the fUTI rate between groups A and B (3.7% versus 1.0%, P < 0.001). The yearly fUTI rates varied from 0.6 to 3.9% between 2002 and 2009. Of the 73 patients with fUTI, those receiving levofloxacin prophylaxis were more likely to harbor fluoroquinolone-resistant pathogens (P < 0.001). E. coli was the most common pathogen in both groups. Levofloxacin remains effective and appears superior to pipemidic acid based prophylaxis.


Assuntos
Antibioticoprofilaxia/métodos , Biópsia/métodos , Levofloxacino/uso terapêutico , Ácido Pipemídico/uso terapêutico , Próstata/patologia , Ultrassom Focalizado Transretal de Alta Intensidade/métodos , Infecções Urinárias/prevenção & controle , Biópsia/efeitos adversos , Cefazolina/uso terapêutico , Humanos , Masculino , Estudos Retrospectivos , Taiwan , Ultrassom Focalizado Transretal de Alta Intensidade/efeitos adversos , Infecções Urinárias/patologia
14.
Urologiia ; (3): 7-8, 10, 2012.
Artigo em Russo | MEDLINE | ID: mdl-23074924

RESUMO

We estimated the efficacy of combined treatment and metaphylaxis of urate and mixed urolithiasis in 87 patients aged 18-87 years. The patients were divided into two groups: 68 patients of group 1 (the size of the concrements between 5-25 mm) have undergone parenteral litholysis of the drug trometamol N and metaphylaxis with biologically active additives prolit and urisan; 19 patients of group 2 have undergone extracorporeal shock-wave lithotripsy with parenteral litholysis and metaphylaxis by using biologically active additives prolit septo and urisan. Positive results were achieved in all the patients. In group 1 the concrements dissolved completely. In group 2 small fragments up to 4 mm eliminated after partial solution.


Assuntos
Anti-Infecciosos Urinários/administração & dosagem , Excipientes/administração & dosagem , Litotripsia , Ácido Pipemídico/administração & dosagem , Trometamina/administração & dosagem , Ácido Úrico/metabolismo , Urolitíase , Adulto , Idoso , Idoso de 80 Anos ou mais , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Urolitíase/metabolismo , Urolitíase/patologia , Urolitíase/terapia
15.
Urologiia ; (5): 18-20, 2012.
Artigo em Russo | MEDLINE | ID: mdl-23342610

RESUMO

The evaluation of clinical efficacy of combined treatment and metaphylaxis in 58 patients with gout complicated by nephropathy and urolithiasis was performed. The study included 41 (71%) men and 27 (29%) women aged 44 to 88 years (mean age - 58 +/- 7 years). All patients received parenteral therapy with trometamol H, 5 -10 infusion for the course, an average of 7 infusions. For the metaphylaxis, all patients received biologically active supplement urisan 2 tablets 2 times a day during next three months against the background of drug therapy. Findings indicate a high clinical efficacy of the trometamol H in the combined treatment of patients with gout, complicated by nephropathy and urolithiasis, considering that improvement of renal function, microcirculation in the renal parenchyma, increased glomerular filtration rate, normalization of nitrogenous wastes levels, partial or complete dissolution of concretions of the kidneys, a significant decrease in the tophs size, an increase in motor activity were observed, which ultimately improves the quality of life for these patients. Metaphylaxis using urisan for 3 months on a background of traditional therapy contributed to a stable normalization of blood uric acid levels, which prevented the exacerbation of underlying disease and recurrent stone formation. These data allow to recommend reducing the dose of traditional anti-gout drugs and conducting repeated course of metaphylaxis with the urisan after 5-6 months during 3 months.


Assuntos
Anti-Infecciosos Urinários/administração & dosagem , Excipientes/administração & dosagem , Gota , Nefropatias , Ácido Pipemídico/administração & dosagem , Trometamina/administração & dosagem , Urolitíase , Adulto , Idoso , Idoso de 80 Anos ou mais , Feminino , Taxa de Filtração Glomerular/efeitos dos fármacos , Gota/sangue , Gota/complicações , Gota/fisiopatologia , Gota/prevenção & controle , Humanos , Nefropatias/sangue , Nefropatias/etiologia , Nefropatias/fisiopatologia , Nefropatias/prevenção & controle , Masculino , Pessoa de Meia-Idade , Fatores de Tempo , Ácido Úrico/sangue , Urolitíase/sangue , Urolitíase/etiologia , Urolitíase/fisiopatologia , Urolitíase/prevenção & controle
16.
J Chromatogr A ; 1218(42): 7608-14, 2011 Oct 21.
Artigo em Inglês | MEDLINE | ID: mdl-21683365

RESUMO

The present work describes a method based on solid-phase extraction (SPE) and ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) for the simultaneous determination of three quinolones (pipemidic acid, oxolinic acid and flumequine) and twelve fluoroquinolones (marbofloxacin, fleroxacin, pefloxacin, levofloxacin, norfloxacin, ciprofloxacin, enrofloxacin, danofloxacin, lomefloxacin, difloxacin, sarafloxacin, and moxifloxacin) in different infant and young children powdered milks. After suitable deproteination of the reconstituted powdered samples, a SPE procedure was developed providing recovery values higher than 84% (RSDs lower than 13%) for all the analytes, with limits of detection between 0.04 and 0.52 µg/kg. UPLC-MS/MS analyses were carried out in less than 10 min. Sixteen infant and young children powdered milk samples of different origin, type and composition bought at Spanish markets were analyzed. Residues of the selected antibiotics were not detected in any of the analyzed samples.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Resíduos de Drogas/análise , Fluoroquinolonas/análise , Fórmulas Infantis/química , Extração em Fase Sólida/métodos , Acetonitrilos , Antibacterianos/análise , Humanos , Lactente , Ácido Oxolínico/análise , Ácido Pipemídico/análise , Análise de Regressão , Reprodutibilidade dos Testes , Sensibilidade e Especificidade , Espectrometria de Massas em Tandem/métodos
18.
J Clin Lab Anal ; 24(5): 327-33, 2010.
Artigo em Inglês | MEDLINE | ID: mdl-20872568

RESUMO

Pipemidic acid is extensively used in the treatment of Gram-negative urinary tract infections, and the contents of proline in human urine vary in association with chronic uremia. The simultaneous determination of pipemidic acid and proline in human urine is of significance for quality control of the dosage and clinical study. The coupling of Ru(bpy)(3)(2+)-based electrochemiluminescence detection with capillary electrophoresis was developed for the simultaneous determination of proline and pipemidic acid in human urine. Parameters related to the separation and detection were investigated and optimized. The standard curves were linear between 0.1 and 90 µg mL(-1) for proline and between 0.4 and 100 µg mL(-1) for pipemidic acid. Underoptimized conditions, the detection limits (3σ) were 0.02 µg mL(-1) for proline and 0.06 µg mL(-1) for pipemidic acid. Relative standard derivations for the electrochemiluminescence intensity and the migration time were 3.2 and 0.9% for proline and 3.7 and 1.2% for pipemidic acid, respectively. The developed method was successfully applied to determine proline and pipemidic acid in human urine. The result showed that the content and decreasing rates of proline in urine for male were higher than that for female, and the content and decreasing rate of pipemidic acid in urine for male and female were consistent, respectively.


Assuntos
Eletroquímica , Eletroforese Capilar , Medições Luminescentes , Ácido Pipemídico/urina , Prolina/urina , Feminino , Humanos , Concentração de Íons de Hidrogênio , Limite de Detecção , Masculino
19.
J Med Chem ; 53(3): 1056-66, 2010 Feb 11.
Artigo em Inglês | MEDLINE | ID: mdl-20041668

RESUMO

Autotaxin (ATX, NPP2) has recently been shown to be the lysophospholipase D responsible for synthesis of the bioactive lipid lysophosphatidic acid (LPA). LPA has a well-established role in cancer, and the production of LPA is consistent with the cancer-promoting actions of ATX. Increased ATX and LPA receptor expression have been found in numerous cancer cell types. The current study has combined ligand-based computational approaches (binary quantitative structure-activity relationship), medicinal chemistry, and experimental enzymatic assays to optimize a previously identified small molecule ATX inhibitor, H2L 7905958 (1). Seventy prospective analogs were analyzed via computational screening, from which 30 promising compounds were synthesized and screened to assess efficacy, potency, and mechanism of inhibition. This approach has identified four analogs as potent as or more potent than the lead. The most potent analog displayed an IC(50) of 900 nM with respect to ATX-mediated FS-3 hydrolysis with a K(i) of 700 nM, making this compound approximately 3-fold more potent than the previously described lead.


Assuntos
Inibidores Enzimáticos/farmacologia , Lisofosfolipídeos/metabolismo , Complexos Multienzimáticos/química , Complexos Multienzimáticos/metabolismo , Fosfodiesterase I/química , Fosfodiesterase I/metabolismo , Ácido Pipemídico/química , Pirofosfatases/química , Pirofosfatases/metabolismo , Neoplasias da Mama/metabolismo , Neoplasias da Mama/patologia , Desenho Assistido por Computador , Avaliação Pré-Clínica de Medicamentos , Ensaios Enzimáticos , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Feminino , Humanos , Lisofosfatidilcolinas/metabolismo , Diester Fosfórico Hidrolases/química , Diester Fosfórico Hidrolases/metabolismo , Relação Quantitativa Estrutura-Atividade , Células Tumorais Cultivadas
20.
J AOAC Int ; 92(5): 1382-9, 2009.
Artigo em Inglês | MEDLINE | ID: mdl-19916376

RESUMO

A simple, sensitive, and novel method has been developed and validated for the separation and simultaneous quantitation of seven structurally different drugs-pipemidic acid and ofloxacin quinolone antibiotics, pseudoephedrine decongestant, piroxicam anti-inflammatory, thiamin, pyridoxine, and cobalamin-in a mixture by capillary zone electrophoresis. Factors affecting the separation were pH, concentration of buffer, and applied voltage. Separation was carried out in < 9 min with a 50 mM sodium tetraborate buffer, pH 10, and an applied voltage of 30 kV in an uncoated silica capillary tube. The carrier electrolyte gave baseline separation with good resolution, reproducibility, and accuracy. Calibration plots were linear over at least three orders of magnitude of analyte concentrations, and the lower LODs were within the range of 1-5 microg/mL. Detection was performed by UV absorbance at 230 nm. The method was validated for the analysis of drugs in pharmaceutical preparations and in urine samples with RSD of 0.5-2.4% and recovery of > 99%.


Assuntos
Antibacterianos/análise , Anti-Inflamatórios/análise , Eletroforese Capilar/métodos , Ofloxacino/análise , Ácido Pipemídico/análise , Quinolonas/análise , Urinálise/métodos , Antibacterianos/urina , Anti-Inflamatórios/urina , Boratos/análise , Boratos/urina , Tampões (Química) , Humanos , Concentração de Íons de Hidrogênio , Modelos Químicos , Ofloxacino/urina , Ácido Pipemídico/urina , Piridoxina/análise , Piridoxina/urina , Quinolonas/urina , Tiamina/análise , Tiamina/urina , Fatores de Tempo , Urinálise/instrumentação , Urina , Vitamina B 12/análise , Vitamina B 12/urina
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