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BACKGROUND: Skin sensation changes are common after rhinoplasty and can be troublesome for patients postoperatively. The closed technique may be considered as causing less sensory loss compared to the open technique due to its conservative approach, minimal dissection and low tissue damage potential. A randomized study was planned to compare the sensory changes in the subunits of the nasal skin caused by the two main methods using objective and subjective parameters. METHODS: In the analysis of the patients, the nose was divided into seven subunits: nasion, rhinion, nasal tip, left alar wing, right alar wing, infratip lobule and columella base. Evaluations were done preoperatively and at the first, third, sixth and twelfth months postoperatively. Objective sensory evaluations were done using the Semmes-Weinstein monofilament test. The subjective sensory changes of each nasal unit were subjectively evaluated by the patients on a three-point Likert scale. RESULTS: Both objective and subjective evaluations showed a statistically significant decrease in sensation in the nasal tip and infratip lobule in the open group one month after surgery. In the closed group, no significant differences were observed between the preoperative and postoperative sensory values for nasal subunits across all periods. CONCLUSION: While a decrease in sensation was observed in the tip and infratip lobule in the open technique by the first month postoperatively, this loss of sensation returned to a normal level by the third month. In the closed technique, however, no significant loss of sensation was detected in the postoperative period. In light of our findings, surgeons can have a better insight into postoperative sensory changes in the subunits of nasal skin which makes them more confident and reassuring when there are concerns regarding altered sensation after rhinoplasty. Level of Evidence II This journal requires that authors assign a level of evidence to each article. For a full description of these Evidence-Based Medicine ratings, please refer to the Table of Contents or the online Instructions to Authors www.springer.com/00266 .
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Rinoplastia , Humanos , Rinoplastia/efectos adversos , Rinoplastia/métodos , Nariz/cirugía , Tabique Nasal/cirugía , Piel , Sensación , Estética , Resultado del TratamientoRESUMEN
BACKGROUND AND OBJECTIVES: We aimed to determine the effects of vanillic acid (VA) on fracture healing radiologically, histologically, immunohistochemically, and biomechanically using a rat femur open fracture injury model. METHODS: 32 male Wistar-Albino rats were used and divided into two groups: the study group (VA) and the control group. From the time they were operated on until they were sacrificed, the rats in the study group were given 100 mg/kg/day VA by oral gavage. After sacrification, the femurs were analyzed. RESULTS: It was observed that the Huo histological scoring was significantly higher in the VA group (p = 0.001), and the ratio of the amount of callus tissue compared to intact bone tissue was significantly higher. While no significant difference was observed in immunohistochemical H-scores in ColI antibody staining (p = 1.000), a borderline significant difference in favor of VA was observed in ColIII antibody staining (p = 0.078). In biomechanical analysis, failure load (N), total energy (J), maximum stress (MPa), and stiffness (N/mm) measurements were significantly higher in the VA group (p = 0.040, p = 0.021, p = 0.015, and p = 0.035, respectively). CONCLUSION: It has been observed that VA, with its antioxidative properties, increases fracture healing in rats, in which an open fracture model was created. We are hopeful that such an antioxidant, which is common in nature, will increase fracture healing. Since this study is the first to examine the effect of VA on fracture healing, further studies are needed.
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Fracturas del Fémur , Curación de Fractura , Ratas Wistar , Ácido Vanílico , Animales , Ácido Vanílico/farmacología , Ácido Vanílico/uso terapéutico , Curación de Fractura/efectos de los fármacos , Masculino , Fracturas del Fémur/tratamiento farmacológico , Fracturas del Fémur/patología , Ratas , Modelos Animales de Enfermedad , Fenómenos Biomecánicos/efectos de los fármacos , Fémur/efectos de los fármacos , Fémur/patología , Callo Óseo/efectos de los fármacos , Callo Óseo/patologíaRESUMEN
INTRODUCTION: Our study aimed to compare the short- and particularly long-term type 2 diabetes mellitus (T2DM) remission prediction abilities of ABCD, individualised metabolic surgery (IMS), DiaRem2, Ad-DiaRem and DiaBetter scoring systems in Turkish adult type 2 diabetic morbidly obese patients who underwent bariatric surgery. PATIENTS AND METHODS: Our study was planned as a retrospective cohort study. A total of 137 patients with T2DM, including 78 sleeve gastrectomy (SG) and 59 Roux-en-Y gastric bypass (RYGB) patients, were included in the 1st-year evaluation after bariatric surgery, and a total of 115 patients with T2DM, including 64 SG and 51 RYGB patients, were included in the evaluation at the end of the 5th year. RESULTS: In the 1st year after bariatric surgery, area under the ROC curve (AUC) values for diabetes remission scores were 0.863 for Ad-DiaRem, 0.896 for DiaBetter, 0.840 for DiaRem2, 0.727 for ABCD and 0.836 for IMS. At 5 years after bariatric surgery, the AUC values for diabetes remission were 0.834 for Ad-DiaRem, 0.888 for DiaBetter, 0.794 for DiaRem2, 0.730 for ABCD and 0.878 for IMS. CONCLUSIONS: According to our study, the DiaBetter score provided a better AUC value than the other scores both in the short and long term but showed similar predictive performance to Ad-DiaRem in the short term and IMS in the long term. We believe that DiaBetter and Ad-DiaRem scores might be more appropriate for short-term assessment and DiaBetter and IMS scores for long-term remission assessment.
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BACKGROUND: Pyogenic granuloma (PG) is a common benign vascular neoplasia. Optimal treatment should have an aesthetically pleasant scar and a low recurrence rate. No treatment method that is fully effective in solving these has been demonstrated. Silver nitrate cauterization is another method for the management of PG lesions. OBJECTIVE: The effects of silver nitrate on the treatment of PG have not been sufficiently investigated and should be investigated with objective data and a controlled study. METHODS: The prospective clinical trial was designed to compare silver nitrate cauterization with surgical excision treatment. Procedure times and procedure costs, comfort and satisfaction scales, recurrences, the Patient and Observer Scar Assessment Score, and the Vancouver Scar Scale were compared to evaluate treatments. RESULTS: Silver nitrate treatment had lower procedure times, costs, and better satisfaction and comfort scale scores. The scar assessment scores were better for the silver nitrate treatment. The patients in both groups were successfully treated and no recurrence was seen. CONCLUSION: Silver nitrate cauterization is low-cost, fast, safe, reliable, and effective with good aesthetic results for the treatment of PG lesions. This study shows that silver nitrate cauterization is a good alternative to surgical excision in the management of PG.
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Granuloma Piogénico , Nitrato de Plata , Humanos , Cauterización/métodos , Cicatriz/cirugía , Granuloma Piogénico/cirugía , Estudios Prospectivos , Nitrato de Plata/uso terapéuticoRESUMEN
OBJECTIVES: The inferior and middle turbinates have crucial roles in nasal function, but their enlargement can cause obstructive effects, which can lead to breathing difficulties, sleep and smell disorders, and headaches. Partial turbinectomy is a common surgical technique used to address this issue during septorhinoplasty, but it carries risks such as empty nose syndrome. A clinical trial was designed to evaluate the functional outcomes of middle and inferior partial turbinectomy with a holistic approach. METHODS: Patients with NOSE questionnaire scores of 30 or higher, and grade 4 inferior turbinates and/or advanced middle concha bullosa were included. Patients completed questionnaires related to breathing, empty nose syndrome, headache, and olfaction preoperatively and at one-month, three-month, six-month, and first-year periods postoperatively. The partial excisions of the inferior and middle turbinates were carried out with serrated scissors while trying to preserve adequate turbinate size to maintain function. RESULTS: This study found that NOSE scores, headache frequency, and severity improved postoperatively. The olfactory-related quality of life of the patients with impairments in this area significantly improved found to be improved at all postoperative evaluations. None of the patients experienced prolonged bleeding requiring surgical intervention. No cases of anosmia and empty nose syndrome were reported. CONCLUSION: Partial turbinectomy of middle and inferior turbinates during septorhinoplasty can alleviate symptoms of turbinate hypertrophy, such as breathing issues, olfactory disorders, and headaches. It is an easy, reliable, and efficient surgical maneuver. Proper technique can minimize the risk of empty nose syndrome and other complications of turbinectomy surgery. LEVEL OF EVIDENCE III: This journal requires that authors assign a level of evidence to each article. For a full description of these Evidence-Based Medicine ratings, please refer to the Table of Contents or the online Instructions to Authors www.springer.com/00266 .
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Background: The prognostic importance of nutritional indexes has been shown in some diseases. We aimed to examine the prognostic value of these indexes in patients implanted with the Carillon Mitral Contour System (CMCS). Methods: Fifty-four patients who underwent successful CMCS implantation were evaluated. Prognostic nutritional index (PNI), geriatric nutritional risk index (GNRI) and controlling nutritional status (CONUT) scores were calculated. The relationships between these indexes and 1-year clinical outcomes including all-cause mortality and re-hospitalization due to heart failure were investigated. Results: In Kaplan-Meier analysis, 1-year all-cause mortality rates were significantly higher in the patients with low PNI and GNRI and high CONUT scores (52.0% vs. 0%, p < 0.001; 54.2% vs. 0%, p < 0.001; 52.4%, 6.1%, p < 0.001; respectively). For the composite endpoint, a significant difference was observed between those below and above the cut-off values (70.0% vs. 16.7%, p < 0.001; 75.0% vs. 23.3%, p < 0.001; 66.7% vs. 20.8%, p < 0.001, respectively). In multivariate Cox regression analysis, GNRI was determined to be an independent predictor of 1-year all-cause mortality [hazard ratio: 0.707; 95% confidence interval: 0.510-0.979; p = 0.037]. Conclusions: Nutritional indexes have prognostic value in predicting 1-year all-cause mortality in severe functional mitral regurgitation patients undergoing CMCS implantation. In particular, GNRI can guide the selection of patients who will benefit from CMCS.
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Caseous calcification of the mitral annulus (CCMA) is a very rare form of mitral annular calcification (MAC). CCMA accounts for 0.63% of all cases and 0.06-0.07% of the total population and usually seen in elderly and female patients. It mostly affects the posterior leaflet of the mitral valve. The pathogenesis of CCMA remains unclear. Hypercholesterolemia and the dissolution of lipid-laden macrophages may be implicated in liquefaction necrosis. CCMA is composed of a mixture of calcium, fatty acid, and cholesterol. The name "caseous" comes from the cheese-like or toothpaste-like consistency of the mass. Cardiac magnetic resonance imaging may help in differentiating MAC from CCMA and should perform. The first treatment option should be conservative treatment because of surgical complications of the procedure. We presented a case report which is about CCMA with preoperative and intraoperative robotic images.
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Calcinosis/diagnóstico por imagen , Calcinosis/cirugía , Enfermedades de las Válvulas Cardíacas/diagnóstico por imagen , Enfermedades de las Válvulas Cardíacas/cirugía , Implantación de Prótesis de Válvulas Cardíacas/métodos , Válvula Mitral/diagnóstico por imagen , Válvula Mitral/cirugía , Imagen Multimodal , Procedimientos Quirúrgicos Robotizados/métodos , Anciano , Calcinosis/patología , Resultado Fatal , Femenino , Enfermedades de las Válvulas Cardíacas/patología , Humanos , Periodo Intraoperatorio , Válvula Mitral/patologíaRESUMEN
The one-pot reaction of chlorosulfonyl isocyanate (CSI) with epoxides having phenyl, benzyl and fused cyclic alkyl groups in different solvents under mild reaction conditions without additives and catalysts was studied. Oxazolidinones and five-membered cyclic carbonates were obtained in ratios close to 1:1 in the cyclization reactions. The best yields of these compounds were obtained in dichloromethane (DCM). Together with 16 known compounds, two novel oxazolidinone derivatives and two novel cyclic carbonates were synthesized with an efficient and straightforward method. Compared to the existing methods, the synthetic approach presented here provides the following distinct advantageous: being a one-pot reaction with metal-free reagent, having shorter reaction times, good yields and a very simple purification method. Moreover, using the density functional theory (DFT) method at the M06-2X/6-31+G(d,p) level of theory the mechanism of the cycloaddition reactions has been elucidated. The further investigation of the potential energy surfaces associated with two possible channels leading to oxazolidinones and five-membered cyclic carbonates disclosed that the cycloaddition reaction proceeds via an asynchronous concerted mechanism in gas phase and in DCM.
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Enantioselective synthesis of functionalized cyclic allylic alcohols via kinetic resolution in transesterifcation with different lipase enzymes has been developed. The influence of the enzymes and temperature activity was studied. By determination of ideal reaction conditions, byproduct formation is minimized; this made it possible to prepare enantiomerically enriched allylic alcohols in high ee's and good yields. Enantiomerically enriched allylic alcohols were used for enantiomerically enriched oxazolidinone synthesis. Using benzoate as a leaving group means that 1â¯mol % of potassium osmate is necessary and can be obtained high yields 98%. Inhibitory activities of enantiomerically enriched oxazolidinones (8, 10 and 12) were tested against human carbonic anhydrase I and II isoenzymes (hCA I and hCA II), acetylcholinesterase (AChE), and α-glycosidase (α-Gly) enzymes. These enantiomerically enriched oxazolidinones derivatives had Ki values in the range of 11.6⯱â¯2.1-66.4⯱â¯22.7â¯nM for hCA I, 34.1⯱â¯6.7-45.2⯱â¯12.9â¯nM for hCA II, 16.5⯱â¯2.9 to 35.6⯱â¯13.9 for AChE, and 22.3⯱â¯6.0-70.9⯱â¯9.9â¯nM for α-glycosidase enzyme. Moreover, they had high binding affinity with -5.767, -6.568, -9.014, and -8.563â¯kcal/mol for hCA I, hCA II, AChE and α-glycosidase enzyme, respectively. These results strongly supported the promising nature of the enantiomerically enriched oxazolidinones as selective hCA, AChE, and α-glycosidase inhibitors. Overall, due to these derivatives' inhibitory potential on the tested enzymes, they are promising drug candidates for the treatment of diseases like glaucoma, leukemia, epilepsy; Alzheimer's disease; type-2 diabetes mellitus that are associated with high enzymatic activity of CA, AChE, and α-glycosidase.
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Inhibidores Enzimáticos/farmacología , Simulación del Acoplamiento Molecular , Oxindoles/farmacología , Propanoles/química , Acetilcolinesterasa/metabolismo , Anhidrasas Carbónicas/metabolismo , Relación Dosis-Respuesta a Droga , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/química , Glicósido Hidrolasas/antagonistas & inhibidores , Glicósido Hidrolasas/metabolismo , Humanos , Isoenzimas/antagonistas & inhibidores , Isoenzimas/metabolismo , Estructura Molecular , Oxindoles/síntesis química , Oxindoles/química , Estereoisomerismo , Relación Estructura-ActividadRESUMEN
Sulfamate and its derivatives have a range of biological activities. One-pot cyclocondensation of alkenes (1a-i) with chlorosulfonyl isocyanate generates ß-lactams. ß-Amino acid derivatives (2a-i) from ß-lactams were synthesized. Then, these highly reactive compounds were opened with MeOH to produce the corresponding sulfamate derivatives in good yields. The inhibitory effects of the novel sulfamate derivatives were tested on human carbonic anhydrase I and II isoenzymes (hCA I and hCA II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glycosidase (α-Gly). Novel sulfamate derivatives showed Ki values in the range of 23.81-42.97 nM against hCA I, 8.95-52.23 nM against hCA II, 8.10-45.51 nM against AChE, 23.16-81.84 nM against BChE, and 14.02-48.68 nM against α-Gly. As a result, the novel sulfamate derivatives had potent inhibitory effects against both isoenzymes. Overall, due to the inhibitory effects of the novel sulfamate derivatives on the tested metabolic enzymes, they are promising drug candidates for the treatment of diseases like glaucoma, epilepsy, leukemia, Alzheimer's disease, and type 2 diabetes mellitus, which are associated with high enzymatic activity of the indicated metabolic enzymes.
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Alquenos/química , Aminoácidos/síntesis química , Inhibidores Enzimáticos/síntesis química , Isocianatos/química , Ácidos Sulfónicos/química , Acetilcolinesterasa/metabolismo , Aminoácidos/química , Aminoácidos/farmacología , Butirilcolinesterasa/metabolismo , Anhidrasas Carbónicas/metabolismo , Reacción de Cicloadición , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Glicósido Hidrolasas/antagonistas & inhibidores , Estructura MolecularRESUMEN
In this study, we aimed to determine the inhibition effects of novel synthesized sulfamates (2a-g), sulfonamides (3b-f), carbonyl sulfonamides (3h and i), and carbonyl sulfamates (4h and 4i), which were tested against two human cytosolic carbonic anhydrase I and II isozymes (hCA I and II) and acetylcholinesterase (AChE) enzyme. For inhibition properties of allylic sulfamates, the half maximal inhibitory concentration (IC50 ) and inhibition constant (Ki ) were calculated for each novel compounds. The allylic sulfamates showed that Ki values are in the range of 187.33-510.31 pM for hCA I, 104.22-290.09 pM against hCA II, and 12.73-103.63 pM against AChE. The results demonstrated that all newly synthesized compounds had shown effective inhibition against hCA I and II isoenzymes and AChE enzyme.
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Acetilcolinesterasa/efectos de los fármacos , Alcohol Bencilo/química , Anhidrasa Carbónica II/efectos de los fármacos , Anhidrasa Carbónica I/efectos de los fármacos , Inhibidores de Anhidrasa Carbónica/farmacología , Inhibidores de la Colinesterasa/farmacología , Propanoles/química , Aminación , Citosol/enzimología , Humanos , Concentración 50 InhibidoraRESUMEN
Sulfamates have a large spectrum of biological activities including enzyme inhibition. Eight sulfamates derived from menthol (2a-h) were synthesized. Also, in the other section of this study, novel sulfamate derivatives of menthol were tested against some metabolic enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and carbonic anhydrase I and II enzymes (hCAs I and II). The newly synthesized novel menthol sulfamate and menthol carbonyl sulfamate derivatives showed Ki values in the range of 34.37 ± 8.17 to 53.40 ± 10.61 nM against hCA I, 12.91 ± 4.57 to 38.67 ± 6.22 nM against hCA II, 111.17 ± 52.36 to 522.86 ± 120.08 nM against AChE, and 50.01 ± 11.73 to 109.63 ± 50.08 nM against BChE. As a result, the novel menthol sulfamate and menthol carbonyl sulfamate derivatives can be promising Alzheimer's disease drug candidates and novel hCA I and hCA II enzymes inhibitors.
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Inhibidores de Anhidrasa Carbónica/farmacología , Inhibidores de la Colinesterasa/farmacología , Mentol/química , Ácidos Sulfónicos/farmacología , Acetilcolinesterasa/metabolismo , Butirilcolinesterasa/metabolismo , Inhibidores de Anhidrasa Carbónica/síntesis química , Inhibidores de Anhidrasa Carbónica/química , Anhidrasas Carbónicas/metabolismo , Inhibidores de la Colinesterasa/síntesis química , Inhibidores de la Colinesterasa/química , Relación Dosis-Respuesta a Droga , Humanos , Estructura Molecular , Relación Estructura-Actividad , Ácidos Sulfónicos/síntesis química , Ácidos Sulfónicos/químicaRESUMEN
Aortic regurgitation (AR) is characterized by the backflow of blood from the aorta to the left ventricle. Acute AR typically causes severe pulmonary edema and hypotension, and is a surgical emergency. In chronic AR, however, compensatory mechanisms can clinically compensate for years, with normal left ventricular function and no symptoms. While the hemodynamic mechanisms of chronic AR on the left ventricle are well described, the hemodynamic mechanisms of acute AR are not clear. Most of the literature on acute AR includes either small series or case reports. During the past decade the number of transcatheter aortic valve replacements (TAVRs) performed has increased dramatically, and TAVR is now an accepted treatment option for patients with severe aortic stenosis who are not surgical candidates or are at high risk for surgery. However, potential acute mild to severe AR occurring after TAVR seems a new and common cause of AR. Since more than mild AR increases the risk of mortality, the quantification of AR severity is a major challenge after TAVR. More accurate, reproducible and quantitative criteria need to be developed to assess and highlight the unknowns of acute AR. Information relating to the pathophysiology and hemodynamics of acute AR and TAVR-related acute AR, respectively, are collated in this review.
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Insuficiencia de la Válvula Aórtica , Estenosis de la Válvula Aórtica , Implantación de Prótesis de Válvulas Cardíacas , Prótesis Valvulares Cardíacas , Reemplazo de la Válvula Aórtica Transcatéter , Válvula Aórtica , Hemodinámica , Humanos , Diseño de Prótesis , Factores de Riesgo , Resultado del TratamientoRESUMEN
OBJECTIVE: The present study was undertaken to investigate the prognostic value of the frontal planar QRS-T angle in patients without angiographically apparent coronary atherosclerosis. SUBJECTS AND METHODS: Three hundred and seven patients with normal coronary arteries on coronary angiography were included. The absolute difference between the frontal QRS- and T-wave axes was defined as the frontal planar QRS-T angle, and patients were divided into 3 subgroups based on the frontal planar QRS-T angle (<45, 45-90, and >90°). Demographic, clinical, laboratory, and angiographic data were compared between groups. Based on the regression analysis results, patients were recategorized into 4 groups according to their luminal calibers of left main coronary artery (LMCA) and history of hypertension (HT) (nonhypertensive LMCA ≤4.13 mm, nonhypertensive LMCA >4.13 mm, hypertensive LMCA ≤4.13 mm, and hypertensive LMCA >4.13 mm). RESULTS: The median value of the frontal planar QRS-T angle of all participants was 38°. Subjects with the widest frontal planar QRS-T angle were older (p = 0.027), were hypertensive (p = 0.001), and had higher corrected QT values (p = 0.001). Patients with the widest frontal planar QRS-T angle had larger LMCA and left anterior descending coronary artery diameters compared to subjects with a normal and borderline frontal QRS-T angle (p = 0.004 and p = 0.028, respectively). Corrected QT, HT, and LMCA diameter were found as independent predictors of the frontal planar QRS-T angle. Subjects with HT and a larger luminal caliber of LMCA had the widest frontal planar QRS-T angle. CONCLUSION: Patients with a history of HT and a larger luminal caliber of LMCA had the widest frontal planar QRS-T angle. Since HT-induced electrophysiological changes are still not well established and we observed that changes in the luminal caliber of coronary arteries are associated with an abnormal frontal QRS-T angle, the frontal QRS-T angle could serve as a marker of ventricular repolarization heterogeneity in hypertensive patients in addition to keeping track of arrhythmic events, even before overt disease.
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Aterosclerosis/diagnóstico , Aterosclerosis/epidemiología , Vasos Coronarios/diagnóstico por imagen , Electrocardiografía , Hipertensión/epidemiología , Adulto , Factores de Edad , Anciano , Aterosclerosis/diagnóstico por imagen , Aterosclerosis/fisiopatología , Angiografía Coronaria , Femenino , Humanos , Hipertensión/fisiopatología , Masculino , Persona de Mediana Edad , Factores de Riesgo , Factores SocioeconómicosRESUMEN
OBJECTIVE: To investigate any possible effects of mean platelet volume (MPV) on short-term stroke prognosis and functional outcome in patients with first-ever acute ischemic stroke (FEAIS). METHODS: This retrospective cross-sectional study included 798 FEAIS patients admitted to the emergency department of a tertiary care hospital in Adiyaman, Turkey between January 2013 and June 2015. The data were evaluated according to whether alive or dead, MPV levels, modified Rankin scale (MRS) scores, National Institutes of Health Stroke Scale (NIHSS) scores. The patients were divided into 3 groups based on MPV level as 4.4-7.4 fL, 7.5-10.4 fL, higher than 10.4 fL. RESULTS: A total of 250 patients with FEAIS were included in the study. In both those who survived and those who died, the area under the curve related to hospitalization days, time interval of venipuncture (TIV), and MPV measurements was not statistically significant (p>0.05). The 3 MPV groups showed no significant differences in terms of MRS score, median NIHSS score, hospitalization, and TIV. In subgroups based on MRS scores, there were no statistically significant differences according to median latency (p=0.087), median hospitalization (p=0.394), TIV (p=0.201), and MPV levels (p=0.847). Furthermore, there were no differences in MPV levels between the MRS based groups (p=0.527). CONCLUSION: The results showed that MPV was not a significantly associated and reliable marker for the prediction of prognosis or functional outcome of FEAIS attack.
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Plaquetas/patología , Accidente Cerebrovascular/sangre , Accidente Cerebrovascular/diagnóstico , Adulto , Anciano , Anciano de 80 o más Años , Isquemia Encefálica/complicaciones , Estudios Transversales , Femenino , Humanos , Masculino , Persona de Mediana Edad , Valor Predictivo de las Pruebas , Curva ROC , Estudios Retrospectivos , Índice de Severidad de la EnfermedadRESUMEN
The carbonic anhydrases (CAs, EC 4.2.1.1) represent a superfamily of widespread enzymes, which catalyze a crucial biochemical reaction, the reversible hydration of carbon dioxide to bicarbonate and protons. Human CA isoenzymes I and II (hCA I and hCA II) are ubiquitous cytosolic isoforms. In this study, a series of hydroperoxides, alcohols, and acetates were tested for the inhibition of the cytosolic hCA I and II isoenzymes. These compounds inhibited both hCA isozymes in the low nanomolar ranges. These compounds were good hCA I inhibitors (Kis in the range of 24.93-97.99 nM) and hCA II inhibitors (Kis in the range of 26.04-68.56 nM) compared to acetazolamide as CA inhibitor (Ki: 34.50 nM for hCA I and Ki: 28.93 nM for hCA II).
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Acetatos/farmacología , Alcoholes/farmacología , Anhidrasa Carbónica II/antagonistas & inhibidores , Anhidrasa Carbónica I/antagonistas & inhibidores , Inhibidores de Anhidrasa Carbónica/farmacología , Peróxido de Hidrógeno/farmacología , HumanosRESUMEN
N-substituted maleimides were synthesized from maleic anhydride and primary amines. 1,4-Dibromo-dibenzo[e,h]bicyclo-[2,2,2]octane-2,3-dicarboximide derivatives (4a-f) were prepared by the [4+2] cycloaddition reaction of dibromoanthracenes with the N-substituted maleimide derivatives. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory effects of the new derivatives were assayed against the human (h) isozymes hCA I, II, IX, and XII. All tested bicyclo dicarboximide derivatives exhibited excellent inhibitory effects in the nanomolar range, with Ki values in the range of 117.73-232.87 nM against hCA I and of 69.74-111.51 nM against hCA II, whereas they were low micromolar inhibitors against hCA IX and XII.
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Antracenos/síntesis química , Antracenos/farmacología , Inhibidores de Anhidrasa Carbónica/síntesis química , Inhibidores de Anhidrasa Carbónica/farmacología , Anhidrasas Carbónicas/metabolismo , Antracenos/química , Relación Dosis-Respuesta a Droga , Humanos , Isoenzimas/antagonistas & inhibidores , Relación Estructura-ActividadRESUMEN
Sulfonamides represent a significant class of biologically active compounds that inhibit carbonic anhydrase (CA, EC.: 4.2.1.1) isoenzymes involved in different pathological and physiological events. Sulfonamide CA inhibitors are used therapeutically as diuretic, antiglaucoma, antiobesity and anticancer agents. A series of new sulfonamides were synthesized using imides and tosyl chloride as starting materials. These N-acylsulfonamides efficiently inhibited the cytosolic human carbonic anhydrase isoenzymes I, and II (hCA I, and II), with nanomolar range inhibition constants ranging between 36.4 ± 6.0-254.6 ± 18.0 and 58.3 ± 0.6-273.3 ± 2.5 nM, respectively.
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Anhidrasa Carbónica II/antagonistas & inhibidores , Anhidrasa Carbónica I/antagonistas & inhibidores , Inhibidores de Anhidrasa Carbónica/química , Sulfonamidas/química , Inhibidores de Anhidrasa Carbónica/síntesis química , Humanos , Imidas/química , Cinética , Estructura Molecular , Relación Estructura-Actividad , Sulfonamidas/síntesis química , Compuestos de Tosilo/químicaRESUMEN
OBJECTIVE: There is an increasing interest for the value of right ventricle (RV) in predicting exercise tolerance and prognosis in cardiovascular disease. However, there is relatively few data evaluating the effect of age on RV diastolic filling velocities during rest or exercise in healthy subjects. METHODS: A total of 54 healthy subjects were enrolled in this study. Patients were divided into 2 groups according to their age: Group 1 (≤45-years-old) and Group 2 (>45-years-old). A treadmill exercise test was performed using modified Bruce protocol. Conventional pulsed-wave Doppler and tissue Doppler velocities were obtained both at rest and immediately after the end of exercise, respectively. RESULTS: In the overall analysis, tricuspid flow Doppler analysis showed a significant increase in A-wave velocity, less marked rise in E-wave velocity, decreased E/A ratio and decreased E-wave deceleration time (EDT) with exercise. Tissue Doppler analysis revealed increased Aa velocity, decreased in Ea/Aa ratio and IVRT. No significant change was observed in Ea velocity and E/Ea ratio with exercise. Although diastolic velocities changed significantly with exercise, systolic velocities did not. Cardiac response to exercise differed slightly in the older subjects compared to younger ones. The older subjects were more likely to have a reduced mean rate of RV filling for the second half of diastole from baseline to peak exercise. CONCLUSION: To distinguish normal physiological changes due to aging from those of pathologic conditions may provide benefits while evaluating patients with known or suspected cardiovascular disease.
Asunto(s)
Envejecimiento/fisiología , Ecocardiografía de Estrés/métodos , Prueba de Esfuerzo/métodos , Tolerancia al Ejercicio/fisiología , Ventrículos Cardíacos/diagnóstico por imagen , Función Ventricular Izquierda/fisiología , Adulto , Anciano , Femenino , Humanos , Interpretación de Imagen Asistida por Computador/métodos , Masculino , Persona de Mediana Edad , Reproducibilidad de los Resultados , Sensibilidad y Especificidad , Volumen SistólicoRESUMEN
PURPOSE: Paraquat (PQ; 1,1'dimethyl-bipyridilium 4,4'-dichloride), which is used extensively throughout the world, is highly toxic to humans. We aimed to investigate the protective effects of different doses of caffeic acid phenethyl ester (CAPE) on PQ-intoxicated rats. MATERIALS AND METHODS: A total of 80 rats were divided into the following eight groups, comprising 10 rats in each group: group 1: control; group 2: administered with CAPE (10 µmol/kg); group 3: administered with 15 mg/kg PQ (PQ15 group); group 4: administered with 30 mg/kg PQ (PQ30 group); group 5: administered with 45 mg/kg PQ (PQ45 group); group 6: administered with 15 mg/kg PQ + CAPE; group 7: administered with 30 mg/kg PQ + CAPE and group 8: administered with 45 mg/kg PQ + CAPE. Both PQ and CAPE were injected intraperitoneally. Pancreatic tissue was examined with both haematoxylin and eosin and immunochemical staining. RESULTS: The ratio of the immunohistochemical staining area to the total pancreatic area of the ß cells revealed that statistically significant differences were observed only between the PQ and PQ + CAPE groups (p < 0.05). DISCUSSION: The evaluation of the data suggests that CAPE can be used to prevent acute effects of PQ intoxication.