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1.
Arch Rheumatol ; 39(1): 89-98, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-38774707

RESUMEN

Objectives: This study aimed to evaluate choroidal thickness (CT) in patients with rheumatoid arthritis (RA) and healthy controls and to determine its relationship with RA-associated interstitial lung disease (RA-ILD). Patients and methods: A total of 63 patients with RA and 36 age- and sex-matched healthy controls were recruited in the cross-sectional study. Serological findings, Disease Activity Score-28, disease duration, and medical treatment of patients were recorded. Patients with RA were subdivided into two groups: patients with RA-ILD (Group 1) and patients with RA but without ILD (RA-noILD; Group 2). CTs were measured using enhanced depth imaging optical coherence tomography. CT was measured at five points: the subfoveal region, 750 µm nasal and temporal to the fovea, 1500 µm nasal and temporal to the fovea. Patients with RA-ILD were evaluated with delta high-resolution computed tomography (ΔHRCT) and pulmonary function test to determine the severity of interstitial lung disease. Results: Four of 63 RA patients were excluded due to comorbidities. Thus, 59 RA patients, 20 in the RA-ILD group and 39 in the RA-noILD group, were included in the analyses. The RA groups were similar in terms of clinical characteristics and laboratory findings. There were statistically significant differences between Group 1, Group 2 and healthy controls (Group 3) compared to all CT values (p<0.05). The mean CT measured at 750 µm and 1500 µm nasal to the fovea was lowest in the RA-ILD group, followed by the RA-noILD and healthy groups (p<0.05). CT measurements did not correlate with the pulmonary function test and ΔHRCT. Conclusion: RA-ILD patients had a thinner CT measured at nasal points. However, there was no association between CT measurements and the severity of ILD.

2.
Arch Rheumatol ; 38(4): 556-565, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-38125066

RESUMEN

Objectives: The study aimed to evaluate stiffness and the cross-sectional area (CSA) of the tibial nerve (TN) using shear wave elastography (SWE) and ultrasound (US) and investigate the relationship of these with disease activity, quality of life, and severity of neuropathic pain in patients with systemic sclerosis (SSc). Patients and methods: This cross-sectional study included 28 SSc patients (1 male, 27 females; mean age: 50±11 years; range, 28 to 67 years) and 22 age- and sex-matched healthy controls (4 males, 18 females; mean age: 48±6 years; range, 37 to 66 years) between March and April 2022. US and SWE were performed on the TN, and CSA and nerve stiffness were measured. The TN was examined by a radiologist, 4 cm proximal to the medial malleolus. A few days later, an evaluation was performed in the second session by a second observer to investigate inter-and intraobserver agreement. Interobserver agreement was evaluated using the intraclass correlation coefficient (ICC). The Scleroderma Health Assessment Questionnaire, European League Against Rheumatism European Scleroderma Trial and Research (EUSTAR) group activity index, and Douleur-Neuropathique 4 scores of the patients were evaluated. Correlations between the questionnaires and measurements of nerve stiffness and CSA were assessed. Results: Patients with SSc had significantly higher stiffness and CSA values of the right TN compared to healthy controls (p<0.001 and p=0.015, respectively). The nerve stiffness values of the right TN were positively correlated with the EUSTAR activity index (p=0.004, r=0.552). The CSA of the left TN was larger in patients with SSc (21.3±4.9 mm2 ) than in controls (12.8±3.4 mm2 ), and the nerve elasticity was positively correlated with the EUSTAR activity index (p=0.001, r=0.618). The interobserver agreement was moderate to good for measuring stiffness and CSA of the TN (ICC were 0.660 and 0.818, respectively). There was a good to excellent intraobserver agreement for measuring stiffness and CSA of TN (ICC were 0.843 and 0.940, respectively). Conclusion: The increased disease activity in patients with SSc is associated with TN involvement, which can be demonstrated by US and SWE.

3.
Aquac Int ; : 1-18, 2023 May 30.
Artículo en Inglés | MEDLINE | ID: mdl-37361883

RESUMEN

The production period for salmon farming in the Black Sea comprises the winter period and is limited to seven months, due to high water temperatures during the summer time. As an alternative strategy, temporary cage submersion during the summer season might be a solution for salmon grow-out throughout the year. Therefore, this study was conducted for comparative evaluation of economic performance of submerged and surface cages, by analyzing structural costs and returns for Turkish salmon farming in the Black Sea. As a result of the temporary cage submersion strategy, economic profits increased by nearly 70%, granting higher values of financial indicators with increased net profit (685,652.5 $ year-1) and margin of safety (89.6%), compared to the traditional surface cage (397,058.5 $ year-1 net profit and 88.4% margin of safety). The "What-if" analysis showed that profits from both cage systems were sensitive to variations in sale price, and the simulation by 10% reduced export market value may decrease revenues, with less financial profit loss for the submerged cage over the surface once. Hence, temporary cage submersion seems to be an alternative farm management strategy with extended production cycle and higher profits for the sustainable development of Turkish salmon farming in the Black Sea.

4.
Arch Pharm (Weinheim) ; 355(12): e2200348, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-36153848

RESUMEN

A series of new imidazolium salts were prepared in good yield by the reaction between 1-alkylimidazole and a variety of alkyl halides. The structures of the compounds were identified by FT-IR, 1 H NMR, and 13 C NMR spectroscopy, elemental analysis, and mass spectrometry. The crystal structure of 1b was determined by the single-crystal X-ray diffraction method. The phthalimide-tethered imidazolium salts exhibited inhibition abilities toward acetylcholinesterase (AChE) and human carbonic anhydrases (hCAs) I and II, with Ki values in the range of 24.63 ± 3.45 to 305.51 ± 35.98 nM for AChE, 33.56 ± 3.71 to 218.01 ± 25.21 nM for hCA I and 17.75 ± 0.96 to 308.67 ± 13.73 nM for hCA II. The results showed that the new imidazolium salts can play a key role in the treatment of Alzheimer's disease, epilepsy, glaucoma, and leukemia, which is related to their inhibition abilities of hCA I, hCA II, and AChE. Molecular docking and in silico absorption, distribution, metabolism, excretion and toxicity studies were used to look into how the imidazolium salts interacted with the specific protein targets. To better visualize and understand the binding positions and the influence of the imidazolium salts on hCA I, hCA II, and AChE conformations, each one was subjected to molecular docking simulations.


Asunto(s)
Acetilcolinesterasa , Anhidrasa Carbónica II , Humanos , Acetilcolinesterasa/metabolismo , Inhibidores de Anhidrasa Carbónica , Sales (Química)/farmacología , Inhibidores de la Colinesterasa/química , Simulación del Acoplamiento Molecular , Espectroscopía Infrarroja por Transformada de Fourier , Relación Estructura-Actividad , Anhidrasa Carbónica I , Ftalimidas/farmacología , Estructura Molecular
5.
Bioorg Chem ; 120: 105566, 2022 03.
Artículo en Inglés | MEDLINE | ID: mdl-34974209

RESUMEN

A series of chiral and achiral cyclic seleno- and thiourea compounds bearing benzyl groups on N-atoms were prepared from enetetramines and appropriate Group VI elements in good yields. All the synthesized compounds were characterized by elemental analysis, FT-IR, 1H NMR and 13C NMR spectroscopy, and the molecular and crystal structures of (R,R)-4b and (R,R)-5b were confirmed by the single-crystal X-ray diffraction method. These assayed for their activities against metabolic enzymes acetylcholinesterase, butyrylcholinesterase, and α-glycosidase. These selenourea and thiourea derivatives of chiral and achiral enetetramines effectively inhibit AChE and BChE with IC50 values in the range of 3.32-11.36 and 1.47-9.73 µM, respectively. Also, these compounds inhibited α-glycosidase enzyme with IC50 values varying between 1.37 and 8.53 µM. The results indicated that all the synthesized compounds exhibited excellent inhibitory activities against mentioned enzymes as compared with standard inhibitors. Representatively, the most potent compound against α-glycosidase enzyme, (S,S)-5b, was 12-times more potent than standard inhibitor acarbose; 7b and 8a as most potent compounds against cholinesterase enzymes, were around 5 and 13-times more potent than standard inhibitor tacrine against achethylcholinesterase (AChE) and butyrylcholinesterase (BChE), respectively.


Asunto(s)
Acetilcolinesterasa , Butirilcolinesterasa , Acetilcolinesterasa/metabolismo , Butirilcolinesterasa/metabolismo , Inhibidores de la Colinesterasa/química , Glicósido Hidrolasas/metabolismo , Simulación del Acoplamiento Molecular , Estructura Molecular , Compuestos de Organoselenio , Espectroscopía Infrarroja por Transformada de Fourier , Relación Estructura-Actividad , Tiourea/farmacología , Urea/análogos & derivados
6.
J Pediatr Hematol Oncol ; 44(1): e296-e298, 2022 01 01.
Artículo en Inglés | MEDLINE | ID: mdl-33828033

RESUMEN

INTRODUCTION: Roseola infantum is always considered to be among the differential diagnosis of young patients with fever and leukopenia whom to be strictly isolated with the preliminary diagnosis of COVID-19 until otherwise proven during the pandemic. RESULTS: Human herpes virus-6 (HHV-6) polymerase chain reaction (PCR) blood test was performed in 4 of 7 patients with a clinical diagnosis of roseola infantum and all found to be HHV-6 PCR positive. The most striking laboratory finding in all patients was leukopenia. HHV-6 PCR tests were found to be positive. Severe acute respiratory syndrome coronavirus-2 testing were found to be negative in all patients. CONCLUSION: During the peak of the pandemic, children continued to present with fever because of viral infections other than COVID-19.


Asunto(s)
Exantema Súbito/diagnóstico , Herpesvirus Humano 6/aislamiento & purificación , COVID-19/diagnóstico , Preescolar , Femenino , Humanos , Lactante , Leucopenia/diagnóstico , Masculino , SARS-CoV-2/aislamiento & purificación
7.
Clin Rheumatol ; 41(1): 177-186, 2022 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-34368908

RESUMEN

OBJECTIVE: To compare the clinical features, laboratory findings, and prognosis of Behçet's disease (BD) patients with and without Budd-Chiari syndrome (BCS). METHODS: This multicenter retrospective study investigated 61 (M/F: 41/20) patients with BD, having coexistent BCS, and 169 (M/F:100/69) BD patients as the control group without BCS from 22 different centers of Turkey diagnosed between 1990 and 2017. RESULTS: Of the total 61 BD patients with BCS, the onset of the first symptom and the median age of diagnosis were earlier in contrast to BD patients without BCS (p = 0.005 and p = 0.007). Lower extremity deep vein and inferior vena cava (IVC) thrombosis were more common in patients with BCS (all; p < 0.01) compared to the control group. Mortality was significantly higher in BD-BCS patients with IVC thrombosis than in the controls (p = 0.004). Since most of the cases in our cohort had chronic and silent form of BCS, mortality rate was 14.8%, which was on the lower range of mortality rate reported in literature (14-47%). While all BD-BCS patients received immunosuppressive (IS) agents, only half of them received additional anticoagulant treatments. Among IS agents, interferon treatment was more frequently used in this cohort (19%), compared to other series reported in literature (2.3%). CONCLUSION: To our knowledge, this is the largest series of BD patients with BCS. Our patients had earlier disease onset and diagnosis, higher frequency of IVC thrombosis, and higher mortality rate, compared to BD patients without BCS. Mortality was significantly higher in BD-BCS patients with IVC thrombosis compared to controls. Key Points • Mortality rate is higher in BD-associated BCS patients with IVC involvement. • Chronic and silent form of BD-associated BCS has a better prognosis. • The main treatment options are corticosteroids and immunosuppressive agents, whereas anticoagulant treatment remains controversial.


Asunto(s)
Síndrome de Behçet , Síndrome de Budd-Chiari , Síndrome de Behçet/complicaciones , Síndrome de Behçet/tratamiento farmacológico , Síndrome de Behçet/epidemiología , Síndrome de Budd-Chiari/complicaciones , Síndrome de Budd-Chiari/epidemiología , Estudios de Cohortes , Humanos , Inmunosupresores/uso terapéutico , Estudios Retrospectivos , Vena Cava Inferior
8.
Mod Rheumatol ; 32(6): 1102-1107, 2022 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-34865095

RESUMEN

BACKGROUND: This study aimed to investigate the efficacy of local oxygen-ozone therapy in systemic sclerosis (SSc) patients with digital ulcers (DUs) who were resistant to medical therapy and had impairment in activities of daily living. METHODS: Participants' demographic data, and clinical parameters were recorded. Twenty-five SSc patients with DUs were randomized to the ozone group (I) (n = 13) to receive medical treatment plus local oxygen-ozone therapy and the control group (II) (n = 12) to receive medical treatment only. Hand functions were assessed using the Health Assessment Questionnaire (HAQ) and the Modified Hand Mobility in Scleroderma (HAMISm) test. Clinical parameters, HAQ, and mHAMIS scores were re-evaluated in participants 4 weeks after the initiation of treatment. RESULTS: Demographic and clinical characteristics of the two groups showed no significant differences. At 4 weeks after the initial treatment, the efficacy rate was significantly higher in the ozone group than that in the control group (92% versus 42% P = 0.010). Clinical parameters, HAQ, and HAMISm scores were significantly improved in the treatment group compared to those in the control group (P < 0.05). CONCLUSION: Local oxygen-ozone therapy was effective in the treatment of SSc patients with resistant DUs and improved clinical parameters and functional disability.


Asunto(s)
Ozono , Esclerodermia Localizada , Esclerodermia Sistémica , Úlcera Cutánea , Humanos , Actividades Cotidianas , Dedos , Oxígeno/uso terapéutico , Ozono/uso terapéutico , Esclerodermia Sistémica/complicaciones , Esclerodermia Sistémica/terapia , Úlcera Cutánea/tratamiento farmacológico , Úlcera Cutánea/etiología , Úlcera
9.
Rom J Intern Med ; 59(3): 278-285, 2021 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-33544548

RESUMEN

Background. A large number of comparative studies have been conducted for ankylosing spondylitis (AS) and non-radiographic axial spondyloarthritis (nr-axSpA), including disease burden, treatment modalities and patient characteristics. The aim of this study was to compare physician related diagnostic delay time between patients with AS and nr-axSpA. Methods. In our retrospective study we included 266 patients with axSpA. Patients were classified into two subgroups, AS and nr-axSpA. The time from back pain onset until diagnosis of axSpA was defined as the diagnostic delay. The first specialist referred to and the first diagnosis for each patient was noted in detail. Patient characteristics, clinical manifestations and laboratory and imaging results at diagnosis were also compared between subgroups. Results. The diagnostic delay time was significantly longer for AS patients [6 ± 8.14 years vs 1.62 ± 2.54 years]. 40.9% of all patients were initially consulted by specialists in physical therapy and rehabilitation, followed by 29.7% consulted by a neurosurgeon and 19.9% by a rheumatologist. The most common initial diagnosis was fibromyalgia, 52.6% (140), followed by ankylosing spondylitis, 28.9% (77), and lumbar disc hernia, 12.7% (34). Conclusion. The vast majority of patients were initially evaluated by healthcare providers other than rheumatologists and mostly diagnosed with fibromyalgia. Efforts to increase awareness and to educate first healthcare providers may shorten the diagnostic delay time.


Asunto(s)
Espondiloartritis Axial/diagnóstico , Dolor de Espalda/etiología , Diagnóstico Tardío , Espondilitis Anquilosante/diagnóstico por imagen , Adolescente , Adulto , Anciano , Femenino , Fibromialgia/diagnóstico , Humanos , Masculino , Persona de Mediana Edad , Médicos , Estudios Retrospectivos , Espondiloartritis/diagnóstico por imagen , Factores de Tiempo , Adulto Joven
10.
Mod Rheumatol ; 31(2): 442-450, 2021 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-32202181

RESUMEN

OBJECTIVE: To investigate the effect of the addition of aerobic training to spinal mobility exercises on disease-specific outcomes and functional exercise capacity, aerobic capacity and respiratory muscle strength of ankylosing spondylitis (AS) patients. METHODS: The study included 31 volunteers (mean age: 44.90 ± 11.52 years) diagnosed with AS. The demographic characteristics and disease-related data of all subjects were recorded, then, the Bath AS Disease Activity Index (BASDAI), Bath AS Metrology Index (BASMI) and Bath AS Disease Function Index (BASFI), the 6-minute walk test, the Bruce Treadmill Test and spirometry were used, respectively. The intervention group attended a 12-week program of aerobic exercise sessions, plus supervised spinal mobility exercises, 3 days a week. The control group performed the supervised spinal mobility exercises only, 3 times a week, for 12 weeks. RESULTS: There was a significant improvement in BASDAI (p = .002), BASMI (p = .021), 6 DYT (p = .036), VO2 max (p = .000), MIP (p = .005) and MEP (p = .022) results in the intervention group after 12 weeks of training. In the comparisons of the pre-treatment and post-treatment differences, BASDAI (p = .032) decreased and VO2 (p = .001) max increased, showing significant improvements in the intervention group and these values were maintained. CONCLUSION: It is striking that improvements in all parameters except BASFI were achieved in the aerobic training group. These results demonstrate that an aerobic exercise program should be included in an individual exercise prescription for the management of AS.


Asunto(s)
Terapia por Ejercicio/métodos , Espondilitis Anquilosante/terapia , Adulto , Femenino , Humanos , Masculino , Persona de Mediana Edad , Índice de Severidad de la Enfermedad , Resultado del Tratamiento
11.
Environ Sci Pollut Res Int ; 28(8): 9753-9759, 2021 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-33155116

RESUMEN

The aim of the present study was to evaluate physical carrying capacity of a potential cage aquaculture site near a Cittaslow area in the northern part of the Mediterranean (Sigacik Bay, Turkey). Developing tools for timely management of marine aquaculture facilities are important to minimize harmful influences of fish farming. The physical carrying capacity was estimated by mathematical formulations previously developed for the same area, using data of topographical characteristics of the site, production capacities, and leased area information of fish farms in total. Based on the findings of the present study, estimated physical carrying capacity of the potential aquaculture site with a total area of 38.9 ha near the Cittaslow residential area of "Sigacik Bay" was found as 27,694 tons of fish production which is more than 2-fold of the present production level that is around 11,800 tons in the area. Therefore, it might be concluded from a physical point of view that the production level of the present cage farms in Sigacik Bay is below risk levels.


Asunto(s)
Bahías , Conservación de los Recursos Naturales , Animales , Acuicultura , Peces , Turquía
12.
Fish Shellfish Immunol ; 107(Pt A): 211-217, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-33007366

RESUMEN

The present study investigated the effects of black mulberry (Morus nigra) syrup supplementation on growth performance, hematological, serum biochemical, innate immune parameters, immune and antioxidant related gene expression responses, and disease resistance of Nile tilapia, Oreochromis niloticus. Five isonitrogenous and isoenergetic diets were formulated to contain black mulberry syrup at levels of 0%, 0.75%, 1.5%, 2.0%, and 3.0%. Fish were fed experimental diets for 60 days. Dietary black mulberry syrup increased activities of serum lysozyme, myeloperoxidase, superoxide dismutase and catalase, and increased the expression levels of immune-related genes (interleukin 1, beta, tumor necrosis factor, immunoglobulin M, interferon gamma and heat shock protein 70) in the spleen and antioxidant-related genes (superoxide dismutase, catalase and glutathione peroxidase) in the liver of fish fed especially with 1.5%, 2.0%, and 3.0% black mulberry syrup supplemented diets. Furthermore, at 2.0% incorporation level, growth performance increased. The findings of the present study indicate that Nile tilapia fed with diet containing 2.0% black mulberry might be adequate to improve the growth performance, innate immune parameters, antioxidant related gene expression responses, and disease resistance against Aeromonas veronii.


Asunto(s)
Cíclidos/inmunología , Resistencia a la Enfermedad , Enfermedades de los Peces/inmunología , Proteínas de Peces/genética , Expresión Génica/inmunología , Morus/química , Extractos Vegetales/metabolismo , Aeromonas veronii/fisiología , Alimentación Animal/análisis , Animales , Cíclidos/genética , Cíclidos/crecimiento & desarrollo , Cíclidos/fisiología , Dieta/veterinaria , Suplementos Dietéticos/análisis , Resistencia a la Enfermedad/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Proteínas de Peces/metabolismo , Expresión Génica/efectos de los fármacos , Infecciones por Bacterias Gramnegativas/inmunología , Infecciones por Bacterias Gramnegativas/veterinaria , Extractos Vegetales/administración & dosificación , Distribución Aleatoria
13.
Acta Crystallogr C Struct Chem ; 75(Pt 7): 941-950, 2019 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-31271383

RESUMEN

The molecular structure of the benzimidazol-2-ylidene-PdCl2-pyridine-type PEPPSI (pyridine-enhanced precatalyst, preparation, stabilization and initiation) complex {1,3-bis[2-(diisopropylamino)ethyl]benzimidazol-2-ylidene-κC2}dichlorido(pyridine-κN)palladium(II), [PdCl2(C5H5N)(C23H40N4)], has been characterized by elemental analysis, IR and NMR spectroscopy, and natural bond orbital (NBO) and charge decomposition analysis (CDA). Cambridge Structural Database (CSD) searches were used to understand the structural characteristics of the PEPPSI complexes in comparison with the usual N-heterocyclic carbene (NHC) complexes. The presence of weak C-H...Cl-type hydrogen-bond and π-π stacking interactions between benzene rings were verified using NCI plots and Hirshfeld surface analysis. The preferred method in the CDA of PEPPSI complexes is to separate their geometries into only two fragments, i.e. the bulky NHC ligand and the remaining fragment. In this study, the geometry of the PEPPSI complex is separated into five fragments, namely benzimidazol-2-ylidene (Bimy), two chlorides, pyridine (Py) and the PdII ion. Thus, the individual roles of the Pd atom and the Py ligand in the donation and back-donation mechanisms have been clearly revealed. The NHC ligand in the PEPPSI complex in this study acts as a strong σ-donor with a considerable amount of π-back-donation from Pd to Ccarbene. The electron-poor character of PdII is supported by π-back-donation from the Pd centre and the weakness of the Pd-N(Py) bond. According to CSD searches, Bimy ligands in PEPPSI complexes have a stronger σ-donating ability than imidazol-2-ylidene ligands in PEPPSI complexes.

14.
J Trace Elem Med Biol ; 50: 356-361, 2018 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-30262304

RESUMEN

Axillary seabream (Pagellus acarne) farmed in a copper alloy mesh pen and wild individuals of P. acarne aggregated near the copper-alloy cages presented higher concentrations of trace metals in the liver, skin and gills than in fish muscle tissues in two batches of small and large fish sizes. Elevated mean levels of metals (mg kg-1) in muscle tissues in both small and large fish size groups were observed in the rank order of Zn(3.43) > Fe(3.01) > Cu(0.59) > Mn(0.13) and Fe(3.82) > Zn(3.32) > Cu(0.62) > Mn(0.17) for copper cage-farmed fish, relative to ranked mean levels for Zn(2.64) > Fe(1.95) > Cu(0.25) > Mn(0.09) and Fe(5.79) > Zn(3.58) > Cu(0.58) > Mn(0.28) for the copper cage-aggregated wild fish. Nevertheless, trace metal concentrations in fish harvested from the copper cage or those of the cage-aggregated wild individuals in both size groups were far below maximum levels of seafood safety recommended by USEPA and FAO/WHO. Target hazard quotients, calculated to estimate the non-carcinogenic health risks of metals by consuming these fish, were below "1″ (THQ < 1), indicating that there were no potential health risks for humans when consuming copper-caged fish or wild-caught individuals aggregated around the copper mesh pen, with respect to the limits suggested by US Food and Drug Administration and EU Regulations for Seafood Consumption.


Asunto(s)
Aleaciones/química , Cobre/análisis , Dorada , Alimentos Marinos/análisis , Oligoelementos/análisis , Contaminantes Químicos del Agua/análisis , Animales , Monitoreo del Ambiente , Contaminación de Alimentos/análisis , Humanos
15.
Arch Pharm (Weinheim) ; 351(9): e1800146, 2018 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-30033646

RESUMEN

Three series of symmetrical Schiff bases were synthesized from 1,2-diaminoethane, 1,3-diaminopropane and 1,4-diaminobutane and substituted benzaldehydes, and reduced by sodium borohydride to the corresponding benzylic diamines 4-6. All of the compounds obtained were characterized using elemental analysis, FT-IR, 1 H NMR, and 13 C NMR spectroscopy. The enzyme inhibitory properties of these compounds were tested and the influence of the alkane chain length and the substituents on the phenyl group on the enzyme inhibition activity were examined. The novel Schiff bases and their amine derivatives (1a-d, 2a-d, 3b-d, 4a-c, 5a-c, 6a, 6c, 6d) were effective inhibitors of the cytosolic carbonic anhydrase I and II isoforms (hCA I and II), and acetylcholinesterase (AChE) with Ki values in the range of 159.43 ± 30.03 to 563.73 ± 115.30 nM for hCA I, 104.88 ± 18.44 to 524.32 ± 95.03 nM for hCA II, and 3.95 ± 0.74 to 30.83 ± 6.81 nM for AChE.


Asunto(s)
Aminas/farmacología , Inhibidores de Anhidrasa Carbónica/farmacología , Inhibidores de la Colinesterasa/farmacología , Descubrimiento de Drogas , Acetilcolinesterasa/metabolismo , Aminas/síntesis química , Aminas/química , Animales , Butirilcolinesterasa/metabolismo , Anhidrasa Carbónica I/antagonistas & inhibidores , Anhidrasa Carbónica I/aislamiento & purificación , Anhidrasa Carbónica I/metabolismo , Anhidrasa Carbónica II/antagonistas & inhibidores , Anhidrasa Carbónica II/aislamiento & purificación , Anhidrasa Carbónica II/metabolismo , Inhibidores de Anhidrasa Carbónica/síntesis química , Inhibidores de Anhidrasa Carbónica/química , Inhibidores de la Colinesterasa/síntesis química , Inhibidores de la Colinesterasa/química , Relación Dosis-Respuesta a Droga , Órgano Eléctrico , Eritrocitos/enzimología , Caballos , Humanos , Estructura Molecular , Bases de Schiff/síntesis química , Bases de Schiff/química , Bases de Schiff/farmacología , Relación Estructura-Actividad
16.
Mol Clin Oncol ; 6(5): 708-712, 2017 May.
Artículo en Inglés | MEDLINE | ID: mdl-28515924

RESUMEN

Due to poor prognosis in advanced non-small cell lung cancer (NSCLC), new effective markers are required in the monitoring of the disease. The present study aimed to investigate the association between the serum IL-1 receptor antagonist (IL-1Ra) level, overall survival (OS), and treatment response in NSCLC, and to evaluate the usefulness of the serum IL-1Ra level as a prognostic marker for NSCLC. Eighty patients (72 men and 8 women) and 40 healthy volunteers (13 men and 27 women) were included in the present study. The median progression-free survival was 16 weeks for patients with high serum IL-1Ra levels, and 35 weeks for patients with low serum IL-1Ra levels (P=0.027). The median OS was 38 weeks in patients with a high serum IL-1Ra level, and 62 weeks in patients with a low serum IL-1Ra level (P=0.065). The results of the present study have demonstrated that there was a significant correlation between IL-1Ra levels and NSCLC progression and survival, although the correlation between IL-1Ra levels and the response to treatment was not statistically significant. Therefore, the pre-treatment IL-1Ra level has been identified as a putative prognostic factor for NSCLC.

17.
Molecules ; 14(6): 2032-42, 2009 Jun 05.
Artículo en Inglés | MEDLINE | ID: mdl-19513003

RESUMEN

Novel 1,3-dialkylperhydrobenzimidazolinium chloride salts were prepared as precursors of N-heterocyclic carbenes 3a-e by reacting N,N'-dialkylcyclohexandiamine, triethyl orthoformate and ammonium chloride. The salts were characterized spectroscopically and the complexes formed in situ from Pd(OAc)2 and 3 have been tested as catalysts in homogenous Heck and Suzuki reactions.


Asunto(s)
Imidazoles/química , Cloruro de Amonio/química , Ácidos Borónicos/química , Catálisis , Imidazoles/síntesis química , Espectroscopía de Resonancia Magnética , Estructura Molecular , Organofosfatos/química , Paladio/química
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