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1.
Radiography (Lond) ; 27(1): 247-249, 2021 02.
Article in English | MEDLINE | ID: mdl-32684331

ABSTRACT

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.


Subject(s)
Esophageal Achalasia , Superior Vena Cava Syndrome , Humans , Male , Middle Aged , Radiography , Superior Vena Cava Syndrome/diagnostic imaging , Thorax , Tomography, X-Ray Computed
2.
J Chromatogr A ; 1621: 461078, 2020 Jun 21.
Article in English | MEDLINE | ID: mdl-32312546

ABSTRACT

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.


Subject(s)
Amines/analysis , Chromatography, Liquid/methods , Imines/analysis , Mass Spectrometry/methods , Sulfhydryl Compounds/analysis , Chromatography, High Pressure Liquid , Dansyl Compounds/chemistry , Fluorenes/chemical synthesis , Fluorenes/chemistry , Reproducibility of Results , Sulfhydryl Compounds/chemical synthesis , Sulfhydryl Compounds/chemistry
3.
Acta Clin Belg ; 67(2): 137-9, 2012.
Article in English | MEDLINE | ID: mdl-22712172

ABSTRACT

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.


Subject(s)
Liver Cirrhosis/diagnosis , Peritoneal Neoplasms/diagnosis , Portal Vein , Tuberculosis/complications , Venous Thrombosis/etiology , Adult , Humans , Lymph Nodes/microbiology , Male , Mycobacterium tuberculosis/isolation & purification , Omentum/microbiology
5.
Clin Exp Rheumatol ; 26(4 Suppl 50): S114-6, 2008.
Article in English | MEDLINE | ID: mdl-19026128

ABSTRACT

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.


Subject(s)
Biomarkers, Tumor/blood , Familial Mediterranean Fever/blood , Acute-Phase Proteins/analysis , Adult , Case-Control Studies , Female , Humans , Male
6.
Acta Gastroenterol Belg ; 69(1): 5-11, 2006.
Article in English | MEDLINE | ID: mdl-16673555

ABSTRACT

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.


Subject(s)
Alanine Transaminase/blood , Fatty Liver/blood , Fatty Liver/diagnosis , Vitamin E/blood , Adult , Age Factors , Aged , Analysis of Variance , Biomarkers/blood , Chi-Square Distribution , Cohort Studies , Disease Progression , Female , Follow-Up Studies , Humans , Liver Function Tests , Male , Middle Aged , Probability , Risk Assessment , Sensitivity and Specificity , Severity of Illness Index , Sex Factors
7.
Postgrad Med J ; 81(959): e12, 2005 Sep.
Article in English | MEDLINE | ID: mdl-16143676

ABSTRACT

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.


Subject(s)
Antineoplastic Combined Chemotherapy Protocols/therapeutic use , Gastrointestinal Diseases/complications , POEMS Syndrome/complications , Adult , Cyclophosphamide/therapeutic use , Doxorubicin/therapeutic use , Female , Gastrointestinal Diseases/drug therapy , Gastrointestinal Diseases/pathology , Humans , Intestinal Mucosa/pathology , POEMS Syndrome/drug therapy , POEMS Syndrome/pathology , Prednisone/therapeutic use , Vincristine/therapeutic use
8.
Biophys Chem ; 97(2-3): 113-20, 2002 Jun 19.
Article in English | MEDLINE | ID: mdl-12050003

ABSTRACT

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.


Subject(s)
Calorimetry, Differential Scanning/methods , Glycine/metabolism , Peptides/metabolism , Thiadiazines/metabolism , Drug Stability , Kinetics , Models, Chemical
9.
Arch Pharm (Weinheim) ; 334(10): 305-8, 2001 Oct.
Article in English | MEDLINE | ID: mdl-11759168

ABSTRACT

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.


Subject(s)
Antifungal Agents/chemical synthesis , Thiadiazines/chemical synthesis , Thiadiazines/pharmacology , Antifungal Agents/pharmacology , Fungi/drug effects , Microbial Sensitivity Tests , Spectrophotometry, Infrared
10.
Arch Pharm (Weinheim) ; 333(9): 281-6, 2000 Sep.
Article in English | MEDLINE | ID: mdl-11039183

ABSTRACT

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.


Subject(s)
Anti-Infective Agents/chemical synthesis , Bacteria/drug effects , Fungi/drug effects , Thiadiazines/chemical synthesis , Thiones/chemical synthesis , Anti-Bacterial Agents , Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Chloramphenicol/pharmacology , Indicators and Reagents , Microbial Sensitivity Tests , Structure-Activity Relationship , Thiadiazines/chemistry , Thiadiazines/pharmacology , Thiones/chemistry , Thiones/pharmacology
11.
Boll Chim Farm ; 139(5): 228-34, 2000.
Article in English | MEDLINE | ID: mdl-11213444

ABSTRACT

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.


Subject(s)
Anti-HIV Agents/chemical synthesis , Antineoplastic Agents, Alkylating/chemical synthesis , Benzimidazoles/chemical synthesis , Chalcone/chemical synthesis , Anti-HIV Agents/pharmacology , Antineoplastic Agents, Alkylating/pharmacology , Benzimidazoles/pharmacology , Chalcone/pharmacology , Chromatography, High Pressure Liquid , Drug Screening Assays, Antitumor , Humans , Magnetic Resonance Spectroscopy , Methylation , Models, Molecular , Tumor Cells, Cultured
12.
Arch Pharm (Weinheim) ; 330(11): 327-32, 1997 Nov.
Article in English | MEDLINE | ID: mdl-9431024

ABSTRACT

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.


Subject(s)
Drug Carriers/chemical synthesis , Peptides/administration & dosage , Prodrugs/chemical synthesis , Thiadiazines/chemical synthesis , Thiones/chemical synthesis , Chemical Phenomena , Chemistry, Physical , Drug Carriers/pharmacokinetics , Humans , Kinetics , Peptides/pharmacokinetics , Prodrugs/pharmacokinetics , Thiadiazines/administration & dosage , Thiadiazines/pharmacokinetics , Thiones/administration & dosage , Thiones/pharmacokinetics
13.
Chem Pharm Bull (Tokyo) ; 37(11): 2971-5, 1989 Nov.
Article in English | MEDLINE | ID: mdl-2632041

ABSTRACT

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.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Imidazoles/chemical synthesis , Thiazoles/chemical synthesis , Animals , Chemical Phenomena , Chemistry , Imidazoles/pharmacology , Mice , Rats , Thiazoles/pharmacology
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