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1.
Radiography (Lond) ; 27(1): 247-249, 2021 02.
Artigo em Inglês | MEDLINE | ID: mdl-32684331

RESUMO

A 61-year-old man presented with dysphagia, weight loss and shortness of breath. On examination, he had reduced lung sounds on the right, and obvious neck vein distention. Chest X-ray raised a suspicion of lung tumor with possible superior vena cava syndrome. Subsequent CT scan of chest confirmed the presence of markedly dilated and tortuous esophagus (sigmoid megaesophagus) extending to the right hemithorax and pressing on the trachea. The patient was referred for surgery.


Assuntos
Acalasia Esofágica , Síndrome da Veia Cava Superior , Humanos , Masculino , Pessoa de Meia-Idade , Radiografia , Síndrome da Veia Cava Superior/diagnóstico por imagem , Tórax , Tomografia Computadorizada por Raios X
2.
J Chromatogr A ; 1621: 461078, 2020 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-32312546

RESUMO

A new derivatization reagent, N-(naphthalen-1-yl)-2-oxopropanehydrazonoyl chloride (UOSA54), was prepared and coupled with four drugs, bearing primary amino, secondary amino or mercapto functional groups. Glucosamine sulfate (GLU), cysteine (CYS), captopril (CAP), and vildagliptin (VIL), were used as representative reactive analytes. The prepared reagent was successfully coupled with the targeted analytes in the presence of triethylamine (TEA) as hydrochloride acceptor and acetonitrile as solvent. The resulting reaction products were separated by high-performance liquid chromatography and monitored simultaneously by diode array and triple quad mass spectrometry detectors. Enhanced DAD and electrospray ionization-MS (ESI-MS) responses were observed for the derivatized products. Complete derivatization of VIL was achieved after heating at 65 ± 3 °C for 4 min, while other analytes were derivatized instantaneously at room temperature. Both, the ESI-ionization suppression, due to the excess reagent, and matrix effect, due to co-eluted biogenic plasma constituents, were negligible. The derivatized GLU, CYS, CAP, and VIL showed a maximum absorption wavelength at 376, 417, 340, and 376 nm, with MS-limit of quantification value of 250.0, 2.0, 2.5, and 3.0 pg/µL, respectively. The relative ESI-MS response of UOSA54 derivatization products was within the range of 0.6-4.1 compared with dansylated products. The method was optimized and validated for optimal reaction product stability, sensitivity, linearity, range, precision, and accuracy. The percentage recovery was exceeding 97.2%, with an RSD value of less than 4.0%. The limit of quantification of targeted analytes was ranged from 80.0 to 0.7 pg/µL.


Assuntos
Aminas/análise , Cromatografia Líquida/métodos , Iminas/análise , Espectrometria de Massas/métodos , Compostos de Sulfidrila/análise , Cromatografia Líquida de Alta Pressão , Compostos de Dansil/química , Fluorenos/síntese química , Fluorenos/química , Reprodutibilidade dos Testes , Compostos de Sulfidrila/síntese química , Compostos de Sulfidrila/química
3.
Acta Clin Belg ; 67(2): 137-9, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-22712172

RESUMO

Abdominal tuberculosis is a rare infectious disease that can involve the peritoneum and lead to portal vein thrombosis and mimic peritoneal carcinomatosis. We report on a 43-year-old male patient with fatigue and progressive weight loss for two years. Ascites was the only pathologic finding in his physical examination and laboratory findings revealed only a mild anaemia with Ca-125 elevation. The ascitic fluid Adenosine deaminase (ADA) level was also elevated. Computed tomography revealed splenomegaly, a mesenteric mass measuring 3.5 cm and intra-abdominal lymphadenopathies at the hepatic hilum. Oesophagogastroduodenoscopy (EGD) revealed oesophageal varices which was also consistent with portal hypertension. Diagnostic laparotomy and biopsies obtained from the omentum and the lymph nodes revealed acid-fast staining tuberculosis bacilli.


Assuntos
Cirrose Hepática/diagnóstico , Neoplasias Peritoneais/diagnóstico , Veia Porta , Tuberculose/complicações , Trombose Venosa/etiologia , Adulto , Humanos , Linfonodos/microbiologia , Masculino , Mycobacterium tuberculosis/isolamento & purificação , Omento/microbiologia
5.
Clin Exp Rheumatol ; 26(4 Suppl 50): S114-6, 2008.
Artigo em Inglês | MEDLINE | ID: mdl-19026128

RESUMO

OBJECTIVE: Serum levels of tumor markers can be elevated in several benign diseases affecting the serosal surfaces. Familial Mediterranean fever (FMF) is a genetic disease characterized by acute attacks of fever and inflammation of the serosal membranes. The aim of this study was to examine the levels of tumor markers in FMF patients and their correlation with the frequency of attacks. METHODS: Serum levels of CA 125, CA 19-9, CA 15-3, CA 72-4, CEA, and AFP were measured by ELISA in 36 patients with a definitive diagnosis of FMF (21 males, 15 females, mean age 36.4+/-10.3 yrs) and in 19 healthy controls. RESULTS: Serum levels of all tumor markers were normal in the controls. In FMF patients serum levels of CA 125, CA 19.9, CA 15.3, CEA and AFP were within normal ranges, whereas CA 72.4 was significantly higher than in the controls (p=0.001). Half of the FMF patients showed increased levels of CA 72.4; the mean level was lower in those in complete remission. However, no statistically significant correlation was found between FMF attacks and acute phase reactant levels. CONCLUSION: With the exception of Ca 72.4, serum levels of tumor markers are not affected by changes in inflammatory cytokines levels during FMF attacks.


Assuntos
Biomarcadores Tumorais/sangue , Febre Familiar do Mediterrâneo/sangue , Proteínas de Fase Aguda/análise , Adulto , Estudos de Casos e Controles , Feminino , Humanos , Masculino
6.
Acta Gastroenterol Belg ; 69(1): 5-11, 2006.
Artigo em Inglês | MEDLINE | ID: mdl-16673555

RESUMO

BACKGROUND: Oxidative stress and free oxygen radicals play an important role in the progression from simple fatty liver to steatohepatitis. Deficiency of antioxidants like vitamin-E has been reported to trigger this progression. The main aims of our study were to measure plasma vitamin-E levels in nonalcoholic fatty liver disease (NAFLD), to explain its relationship with biochemical parameters and to examine the possible therapeutic and prophylactic role of vitamin-E. METHODS: 52 patients with NAFLD and elevated liver function tests were enrolled. After 6 months of follow-up with a standard low-fat, low-calorie diet, changes in liver enzymes were evaluated. RESULTS: Deficiency of vitamin-E was detected in 16 patients with NAFLD. Homogenous echo pattern of the liver and attenuation was found to be significantly higher in the low vitamin-E group (p = 0.03). The low vitamin-E group had significantly higher levels of triglyceride (p = 0.02). After 6 months, patients in the low vitamin-E group did not respond to the diet and no decrease in ALT levels was detected (p = 0.04). CONCLUSION: This is the first study measuring the serum vitamin-E levels in nonalcoholic fatty liver disease. A correlation was found between low vitamin-E levels, high triglyceride levels, as well as sonographic findings, both of which are negative prognostic factors causing progression of fatty liver to steatohepatitis. Patients with low vitamin-E levels did not respond to a classical diet for fatty liver disease. Based on the data, we suggest that diet alone is not adequate for patients with fatty liver, and vitamin-E supplementation should be added.


Assuntos
Alanina Transaminase/sangue , Fígado Gorduroso/sangue , Fígado Gorduroso/diagnóstico , Vitamina E/sangue , Adulto , Fatores Etários , Idoso , Análise de Variância , Biomarcadores/sangue , Distribuição de Qui-Quadrado , Estudos de Coortes , Progressão da Doença , Feminino , Seguimentos , Humanos , Testes de Função Hepática , Masculino , Pessoa de Meia-Idade , Probabilidade , Medição de Risco , Sensibilidade e Especificidade , Índice de Gravidade de Doença , Fatores Sexuais
7.
Postgrad Med J ; 81(959): e12, 2005 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-16143676

RESUMO

POEMS syndrome (polyneuropathy, organomegaly, endocrinopathy, monoclonal gammopathy, and skin changes) is characterised by a rare multisystem disorder of unknown pathogenesis. Although its pathophysiology is not well understood, overexpression of proinflammatory cytokines has been implicated. Gastrointestinal system disorders have not been reported among the components of the syndrome. A case is reported of POEMS syndrome with gastrointestinal involvement shown by gastrointestinal endoscopy.


Assuntos
Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico , Gastroenteropatias/complicações , Síndrome POEMS/complicações , Adulto , Ciclofosfamida/uso terapêutico , Doxorrubicina/uso terapêutico , Feminino , Gastroenteropatias/tratamento farmacológico , Gastroenteropatias/patologia , Humanos , Mucosa Intestinal/patologia , Síndrome POEMS/tratamento farmacológico , Síndrome POEMS/patologia , Prednisona/uso terapêutico , Vincristina/uso terapêutico
8.
Biophys Chem ; 97(2-3): 113-20, 2002 Jun 19.
Artigo em Inglês | MEDLINE | ID: mdl-12050003

RESUMO

Kinetics of solid state stability of seven derivatives of 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazine-2-thione (THTT) of glycine as a model for amino acids and peptide drugs were studied using differential scanning calorimetry (DSC). Each DSC curve for each derivative showed an endothermic peak followed by an exothermic one, which could be attributed to the melting and decomposition, respectively. The decomposition activation energy of each derivative was calculated using the Augis and Bennet, Kissinger equations and Mahadevan approximation. Also, the melting activation energies as well as the thermodynamic parameter (enthalpy) for the investigated derivatives were evaluated. The relative stability of the derivatives in the solid state according to the calculated values of the decomposition activation energy, frequency factors and half-life for each derivative could be determined.


Assuntos
Varredura Diferencial de Calorimetria/métodos , Glicina/metabolismo , Peptídeos/metabolismo , Tiadiazinas/metabolismo , Estabilidade de Medicamentos , Cinética , Modelos Químicos
9.
Arch Pharm (Weinheim) ; 334(10): 305-8, 2001 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-11759168

RESUMO

In a search for promising antifungal compounds, nine new 3,3'-ethylenebis(5-alkyl-1,3,5-thiadiazine-2-thiones) were synthesized by the reaction of ethylene diamine, carbon disulfide, formaldehyde, and the appropriate alkyl amine. The title compounds were tested for their antifungal activity in vitro against pathogenic (Trichophyton rubrum and Candida albicans), phytopathogenic (Penicillum expansum, Trichoderma hazianum, and Fasarium oxysporum), and aflatoxin producing (Aspergillus flavus) fungi. These compounds exhibited varied inhibitory effects on growth or sporulation of some tested fungal species.


Assuntos
Antifúngicos/síntese química , Tiadiazinas/síntese química , Tiadiazinas/farmacologia , Antifúngicos/farmacologia , Fungos/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Espectrofotometria Infravermelho
10.
Arch Pharm (Weinheim) ; 333(9): 281-6, 2000 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-11039183

RESUMO

The deacylated chloramphenicol amine D-(-)-threo-2-amino-1-(4-nitrophenyl)-1,3-diol (D-amine, 1a), and its enantiomer, the L-(+)-threo-form (L-amine, 1b), were introduced into a tetrahydro-2H-1,3,5-thiadiazine-2-thione (THTT) skeleton. They are incorporated in three ways (Chart 1, types I-III) at N3 (type I), N5 (type II) or both N3 and N5 (type III) of the THTT system. These selections were made in order to investigate the effect of combining the structural features of the THTT and the D-amine on the antimicrobial activity, if any.


Assuntos
Anti-Infecciosos/síntese química , Bactérias/efeitos dos fármacos , Fungos/efeitos dos fármacos , Tiadiazinas/síntese química , Tionas/síntese química , Antibacterianos , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antifúngicos/síntese química , Antifúngicos/química , Antifúngicos/farmacologia , Cloranfenicol/farmacologia , Indicadores e Reagentes , Testes de Sensibilidade Microbiana , Relação Estrutura-Atividade , Tiadiazinas/química , Tiadiazinas/farmacologia , Tionas/química , Tionas/farmacologia
11.
Boll Chim Farm ; 139(5): 228-34, 2000.
Artigo em Inglês | MEDLINE | ID: mdl-11213444

RESUMO

A series of 2-(3-Arylpropenoyl)benzimidazole, 3a-d, and their corresponding N1-methyl analogues, 3e-h, were synthesized from p-substituted benzaldehyde and 2-acetylbenzimidazole or 2-acetyl-1-methylbenzimidazole, respectively. The in vitro alkylating activities of these alpha-beta-unsaturated ketones were investigated using L-cysteine as a model of cellular thioles at pH 7.4 and 37 degrees C. No significant difference between the alkylating activities of 3a-d and 3e-h as expressed from the pseudo first-order rate constants of the reactions of these derivatives with L-cysteine monitored by HPLC. However, significant variations in the rates of alkylation among these derivatives relative to the p-substituted group on the aryl moiety were observed, which is attributable to the electronic parameters of the substituted groups. The in vitro cytotoxic activity provided that the p-nitro derivative; 3d has some selectivity for cell lines of leukemia, renal cancer and breast cancer. The compounds were completely inactive as anti-HIV agents. Molecular modeling for all derivatives was undertaken.


Assuntos
Fármacos Anti-HIV/síntese química , Antineoplásicos Alquilantes/síntese química , Benzimidazóis/síntese química , Chalcona/síntese química , Fármacos Anti-HIV/farmacologia , Antineoplásicos Alquilantes/farmacologia , Benzimidazóis/farmacologia , Chalcona/farmacologia , Cromatografia Líquida de Alta Pressão , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Metilação , Modelos Moleculares , Células Tumorais Cultivadas
12.
Arch Pharm (Weinheim) ; 330(11): 327-32, 1997 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-9431024

RESUMO

3,5-Disubstituted tetrahydro-2H-1,3,5-thiadiazine-2-thione (THTT) derivatives; 4a-g were prepared and found to be a promising prodrug approach for peptide drugs. The pH profile for their degradation in aqueous buffer solutions was determined using HPLC technique and accounted for, in terms of specific base-catalyzed reactions. All of the compounds however, showed high acid-stability. Enzymatic (human serum) hydrolysis of the different derivatives offered an advantageous range of t1/2's, the property that permits controlling onset and duration of actions of drugs.


Assuntos
Portadores de Fármacos/síntese química , Peptídeos/administração & dosagem , Pró-Fármacos/síntese química , Tiadiazinas/síntese química , Tionas/síntese química , Fenômenos Químicos , Físico-Química , Portadores de Fármacos/farmacocinética , Humanos , Cinética , Peptídeos/farmacocinética , Pró-Fármacos/farmacocinética , Tiadiazinas/administração & dosagem , Tiadiazinas/farmacocinética , Tionas/administração & dosagem , Tionas/farmacocinética
13.
Chem Pharm Bull (Tokyo) ; 37(11): 2971-5, 1989 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-2632041

RESUMO

3-[2-[p-(Un)substituted phenyl]imidazo [2,1-b]benzothiazol-3- yl]propionic acid derivatives (2a--e) were prepared via the interaction of the corresponding 2-[p-(un)substituted phenyl]imidazo[2,1-b]benzothiazoles (1a--e) with acrylic acid in the presence of acetic anhydride and acetic acid. Esterification of 2a--e produced methyl esters (3a--e). Upon the interaction of 3a with m-chloroperbenzoic acid, the S-dioxide (4a) was obtained. Compound 5a was prepared from 4a by alkaline hydrolysis. Vilsmeier formylation for 1a--e produced novel [2-[p-(un)substituted phenyl]imidazo[2,1-b]benzothiazol-3- yl]formaldehyde derivatives (6a--e). Derivatives 6a--e reacted with ethyl bromoacetate to give ethyl 3-hydroxy-3-[2-[p-(un)substituted phenyl]imidazo[2,1-b]benzothiazol- 3-yl]propionate esters (7a--e). Compound dl-7a was resolved with l-(+)-tartaric acid. Compounds 2a--e showed weak or no activity in the carrageein-induced paw edema assay. Compound 4a significantly inhibited the leakage of pontamine-sky blue dye into the peritoneal cavity of mice, in the capillary permeability inhibition assay. Compound 5a inhibited the writhing by 62% in the acetic acid-induced writhing assay.


Assuntos
Anti-Inflamatórios não Esteroides/síntese química , Imidazóis/síntese química , Tiazóis/síntese química , Animais , Fenômenos Químicos , Química , Imidazóis/farmacologia , Camundongos , Ratos , Tiazóis/farmacologia
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