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1.
Endocr J ; 71(8): 789-797, 2024 Aug 08.
Artículo en Inglés | MEDLINE | ID: mdl-38945931

RESUMEN

The aim of this study was to determine the tissue expressions of vascular endothelial growth factor (VEGF) and endocan in adrenal cortical tumors and the factors associated with them. The study included 6 subjects with adrenocortical adenoma (ACA), 7 subjects with adrenocortical carcinoma (ACC), and 13 control subjects with a normal adrenal cortex. The status of VEGF and endocan expression was determined by the proportions of cells staining on a scale ranging from negative (not staining at all) to strongly positive. VEGF expression was detected in 1 (16.7%) of 6 subjects in the ACA group and in 6 (85.7%) of 7 subjects in the ACC group. VEGF expression was not detected in any of the subjects in the control group. Endocan expression was detected in 6 (100%) of 6 subjects in the ACA group and in 7 (100%) of 7 subjects in the ACC group, while it was detected in only 4 (30.7%) of 13 subjects in the control group. VEGF was expressed with a high frequency in subjects with ACC and with a low frequency in subjects with ACA, but it was not expressed in subjects with normal adrenal cortex tissue. Although endocan was expressed with a higher frequency in subjects with ACC and ACA, it was also expressed in subjects with normal adrenal cortex tissue. The percentage of cells expressed endocan in subjects with ACC was also significantly higher than in subjects with both ACA and normal adrenal cortex.


Asunto(s)
Neoplasias de la Corteza Suprarrenal , Adenoma Corticosuprarrenal , Carcinoma Corticosuprarrenal , Proteínas de Neoplasias , Proteoglicanos , Factor A de Crecimiento Endotelial Vascular , Humanos , Neoplasias de la Corteza Suprarrenal/metabolismo , Neoplasias de la Corteza Suprarrenal/patología , Neoplasias de la Corteza Suprarrenal/genética , Masculino , Proteínas de Neoplasias/metabolismo , Proteínas de Neoplasias/biosíntesis , Femenino , Proteoglicanos/metabolismo , Proteoglicanos/genética , Persona de Mediana Edad , Factor A de Crecimiento Endotelial Vascular/metabolismo , Adulto , Pronóstico , Adenoma Corticosuprarrenal/metabolismo , Adenoma Corticosuprarrenal/patología , Adenoma Corticosuprarrenal/genética , Carcinoma Corticosuprarrenal/metabolismo , Carcinoma Corticosuprarrenal/patología , Anciano , Corteza Suprarrenal/metabolismo , Corteza Suprarrenal/patología , Adulto Joven
2.
Phys Chem Chem Phys ; 25(19): 13560-13576, 2023 May 17.
Artículo en Inglés | MEDLINE | ID: mdl-37139576

RESUMEN

Pyrogallol molecules were successfully immobilized onto aminopropyl molecule functionalized MCM41 nanoparticles to obtain a fast and high gold adsorption capacity. The Taguchi statistical method was used to determine the factors affecting the gold(III) adsorption efficiency. The effect of six factors, pH, rate, adsorbent mass, temperature, initial Au(III) concentration and time, each with 5 levels, on the adsorption capacity was investigated by forming an L25 orthogonal. The analysis of variance (ANOVA) of each factor showed that all factors had significant effects on adsorption. pH 5, 250 rpm stirring speed, 0.025 g adsorbent mass, 40 °C temperature, 600 mg L-1 Au(III) concentration and 15 min time were determined to be the optimum adsorption conditions. The maximum Langmuir monolayer adsorption capacity of APMCM1-Py for Au(III) was calculated to be 168.54 mg g-1 at 303 K. The adsorption mechanism fits the pseudo-second-order kinetic model assuming the formation of a single chemical adsorption layer on the adsorbent surface. The adsorption isotherms are best represented using the Langmuir isotherm model. It exhibits a spontaneous endothermic behavior. FTIR, SEM, EDX and XRD analyses showed that mostly phenolic -OH functional groups adsorb Au(III) ions on the APMCMC41-Py surface with their reducing character. These results enable the rapid recovery of gold ions from weakly acidic aqueous solutions by reduction of APMCM41-Py NPs.

3.
Endocr Pract ; 28(3): 298-303, 2022 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-34843972

RESUMEN

OBJECTIVE: Cardiovascular complications such as cardiomyopathy and endothelial dysfunction, which are frequently seen in patients with acromegaly, are among the most important causes of morbidity and mortality. In this study, we aimed to investigate arterial stiffness, carotid intima-media thickness, endocan level, and A disintegrin and metalloproteinase with thrombospondin type I motif 9 level and their relationship with disease activity in patients with acromegaly with and without cardiovascular risk factors. METHODS: A total of 60 patients with acromegaly-25 with active disease, 26 with well-controlled disease, and 9 with newly diagnosed disease-and 60 age-, sex-, and body mass index (BMI)-matched healthy control subjects were enrolled in this study. All the subjects' height, weight, BMI, systolic blood pressure (SBP), diastolic blood pressure (DBP), fasting plasma glucose (FPG) level, insulin, hemoglobin A1C (HbA1C), C-reactive protein , lipid, endocan, A disintegrin and metalloproteinase with thrombospondin type I motif 9 levels, pulse wave velocity (PWV), and carotid intima-media thickness were measured. RESULTS: The SBP, DBP, FPG level, HbA1C level, and PWV of the acromegaly group were higher than those of the control group. In patients with acromegaly with cardiovascular disease (CVD) risk factors, the PWV was higher than that in the control group, and in patients with acromegaly without CVD risk factors, the PWV was similar to that in the control group. In a correlation analysis, a positive correlation was found between PWV and age, BMI, SBP, DBP, FPG level, and HbA1C level in the acromegaly group. CONCLUSION: In our study, we found that arterial stiffness increased in patients with acromegaly with CVD risk factors and that increased arterial stiffness was associated with hemodynamic (SBP and DBP) and metabolic (BMI, FPG level, and HbA1C level) parameters.


Asunto(s)
Acromegalia , Enfermedades Cardiovasculares , Rigidez Vascular , Enfermedades Cardiovasculares/complicaciones , Enfermedades Cardiovasculares/etiología , Grosor Intima-Media Carotídeo , Desintegrinas , Factores de Riesgo de Enfermedad Cardiaca , Humanos , Metaloproteasas , Análisis de la Onda del Pulso , Factores de Riesgo , Trombospondinas
4.
Mikrochim Acta ; 189(10): 373, 2022 09 06.
Artículo en Inglés | MEDLINE | ID: mdl-36068359

RESUMEN

Peroxidase mimicking Fe3O4@Chitosan (Fe3O4@Chi) nanozyme was synthesized and used for high-sensitive enzyme-free colorimetric detection of H2O2. The nanozyme was characterized in comparison with  Fe3O4 nanoparticles (NPs) using X-ray diffraction, Fourier-transform infrared spectroscopy, dynamic light scattering, and thermogravimetric analysis. The catalytic performance of Fe3O4@Chi nanozyme was first evaluated by UV-Vis spectroscopy using 3,3',5,5'-tetramethylbenzidine. Unlike Fe3O4NPs, Fe3O4@Chi nanozyme exhibited an intrinsic peroxidase activity with a detection limit of 69 nM. Next, the nanozyme was applied to a microfluidic paper-based analytical device (µPAD) and colorimetric analysis was performed at varying concentrations of H2O2 using a machine learning-based smartphone app called "Hi-perox Sens++ ." The app with machine learning classifiers made the system user-friendly as well as more robust and adaptive against variation in illumination and camera optics. In order to train various machine learning classifiers, the images of the µPADs were taken at 30 s and 10 min by four smartphone brands under seven different illuminations. According to the results, linear discriminant analysis exhibited the highest classification accuracy (98.7%) with phone-independent repeatability at t = 30 s and the accuracy was preserved for 10 min. The proposed system also showed excellent selectivity in the presence of various interfering molecules and good detection performance in tap water.


Asunto(s)
Colorimetría , Peróxido de Hidrógeno , Inteligencia Artificial , Colorimetría/métodos , Peróxido de Hidrógeno/análisis , Peroxidasa/química , Peroxidasas
5.
Turk J Med Sci ; 52(4): 1033-1040, 2022 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-36326370

RESUMEN

BACKGROUND: Data on the presence and extent of cardiovascular disease (CVD) risk in primary hyperparathyroidism (PHPT) are conflicting. In our study, we aimed to investigate the increased CVD risk in patients with PHPT by carotid intima-media thickness (CIMT), epicardial adipose tissue (EAT) thickness, and serum levels of endocan and nesfatin-1. METHODS: Patients with PHPT (n = 44) and age- and sex-matched healthy control subjects (n = 40) were enrolled in this study. Demographic data of the participants were questioned. Serum endocan and nesfatin-1 concentrations were assessed using commercially available ELISA kits. Noninvasive measurements of CIMT and EAT thickness were made with high-resolution ultrasonography and B-mode echocardiography. RESULTS: There was no statistically significant difference in serum endocan and nesfatin-1 levels and EAT thickness in the PHPT group compared to controls. CIMT was statistically significantly higher in the PHPT group compared to controls (p = 0.001). A negative correlation was found between PTH and low-density lipoprotein cholesterol level (p = 0.001) but no significant relationship was found between other parameters. DISCUSSION: We found that CIMT is increased in patients with PHPT and consequently, CVD risk is high in these patients. More comprehensive studies are needed to identify other markers that predict increased CVD risk in patients with PHPT.


Asunto(s)
Enfermedades Cardiovasculares , Hiperparatiroidismo Primario , Humanos , Grosor Intima-Media Carotídeo , Enfermedades Cardiovasculares/epidemiología , Enfermedades Cardiovasculares/etiología , Pericardio/diagnóstico por imagen , Tejido Adiposo/diagnóstico por imagen , Factores de Riesgo
6.
Inorg Chem ; 60(7): 4410-4423, 2021 Apr 05.
Artículo en Inglés | MEDLINE | ID: mdl-33667070

RESUMEN

Amber color emitting novel Ir(III) complexes were synthesized: [Ir(Meppy)2(Fpbpy)][PF6] (1bPF6), [Ir(Meppy)2(Fpbpy)][TFSI] (1bTFSI), [Ir(Meppy)2(MeObpy)][PF6] (2bPF6) and [Ir(Meppy)2(MeObpy)][TFSI] (2bTFSI), where Meppy = 2-(p-methylphenyl)-pyridine (b), Fpbpy = 4,4'-bis(4-fluorophenyl)-2,2'-bipyridine (1), and MeObpy = 4,4'-bis(4-methoxy)-2,2'-bipyridine (2). The photophysical and X-ray results showed that the complexes have aggregation-induced phosphorescent emission (AIPE) and a salt-induced polymorphism effect. The highest photoluminescence intensity was observed in complex 2bTFSI compared to other complexes in the solid state. Their theoretical absorption and phosphorescence emission transitions in acetonitrile were also investigated by using double- and triple-ζ basis sets with B3LYP and PBE0 hybrid functional. The best light-emitting electrochemical cell (LEC) performance was exhibited by complex 2bTFSI, and the data obtained were as follows: Luminance, current density, luminous efficiency, turn-on time, power efficiency, and external quantum efficiency were measured as 16 156 cd/m2, 554 mA/cm2, 8.49 cd/A, 17 s, 3.95 lm/W and 6.37%, respectively. The investigation of crystallographic characteristics have shown that the LEC performance of these complexes depends on cationic-anionic interaction which has a significant influence on molecular stacking of the molecules. Because, complex 2bTFSI, with weak cationic-anionic interactions, shows strong π···π stacking interactions between the adjacent molecules, it is the best lighting application candidate among the complexes.

7.
Int J Mol Sci ; 22(20)2021 Oct 11.
Artículo en Inglés | MEDLINE | ID: mdl-34681605

RESUMEN

Glioma, particularly its most malignant form, glioblastoma multiforme (GBM), is the most common and aggressive malignant central nervous system tumor. The drawbacks of the current chemotherapy for GBM have aroused curiosity in the search for targeted therapies. Aberrantly overexpressed epidermal growth factor receptor (EGFR) in GBM results in poor prognosis, low survival rates, poor responses to therapy and recurrence, and therefore EGFR-targeted therapy stands out as a promising approach for the treatment of gliomas. In this context, a series of pentacyclic triterpene analogues were subjected to in vitro and in silico assays, which were conducted to assess their potency as EGFR-targeted anti-glioma agents. In particular, compound 10 was the most potent anti-glioma agent with an IC50 value of 5.82 µM towards U251 human glioblastoma cells. Taking into account its low cytotoxicity to peripheral blood mononuclear cells (PBMCs), compound 10 exerts selective antitumor action towards Jurkat human leukemic T-cells. This compound also induced apoptosis and inhibited EGFR with an IC50 value of 9.43 µM compared to erlotinib (IC50 = 0.06 µM). Based on in vitro and in silico data, compound 10 stands out as a potential orally bioavailable EGFR-targeted anti-glioma agent endowed with the ability to cross the blood-brain barrier (BBB).


Asunto(s)
Triterpenos Pentacíclicos/química , Apoptosis/efectos de los fármacos , Sitios de Unión , Neoplasias Encefálicas/metabolismo , Neoplasias Encefálicas/patología , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Receptores ErbB/antagonistas & inhibidores , Receptores ErbB/metabolismo , Glioma/metabolismo , Glioma/patología , Semivida , Humanos , Leucocitos Mononucleares/citología , Leucocitos Mononucleares/efectos de los fármacos , Leucocitos Mononucleares/metabolismo , Simulación del Acoplamiento Molecular , Triterpenos Pentacíclicos/metabolismo , Triterpenos Pentacíclicos/farmacología
8.
Turk J Med Sci ; 51(4): 2023-2028, 2021 08 30.
Artículo en Inglés | MEDLINE | ID: mdl-33957725

RESUMEN

Background/aim: Primary hyperparathyroidism (PHPT) is a disease that is diagnosed more frequently and generally in the asymptomatic period, with widely available biochemical tests. Evidence suggesting an association between PHPT and malignancy risk is increasing. Clarification of this association will be useful in PHPT for malignancy screening and management of patients with PHPT. In this study, we aimed to investigate the frequency of cancer in PHPT patients. Materials and methods: A total of 775 PHPT patients were included in the retrospective study. Demographic, clinical and laboratory data of the patients were evaluated retrospectively. Results: Malignancy was detected in 128 (16.50%) of 775 PHPT patients (female/male: 625/150). The mean age at diagnosis of PHPT was 57.99 ± 10.86 years, and the mean age at diagnosis of malignancy was 57.46 ± 11.17 years. Of the 128 patients with malignancy, 53 (41.40%) were diagnosed in the same year as PHPT. In terms of malignancy types, 51 (6.50%) of 775 PHPT patients had thyroid cancer. Thyroid cancer was followed by breast cancer (2.30%) and stomach cancer (1%) in order of frequency. Conclusion: We think that PHPT patients should be examined more carefully in terms of cancer risk, especially thyroid cancer. More comprehensive studies are needed to clarify the relationship between PHPT and cancer.


Asunto(s)
Hiperparatiroidismo Primario , Neoplasias de la Tiroides , Calcio , Femenino , Humanos , Hiperparatiroidismo Primario/complicaciones , Hiperparatiroidismo Primario/epidemiología , Incidencia , Masculino , Estudios Retrospectivos , Neoplasias de la Tiroides/epidemiología
9.
Turk J Med Sci ; 51(3): 1146-1152, 2021 06 28.
Artículo en Inglés | MEDLINE | ID: mdl-33389987

RESUMEN

Background/aim: The presence of comorbidities in patients with acromegaly causes an increase in morbidity and/or mortality and a decrease in quality of life. In this study, we aimed to investigate the demographic, clinical and laboratory features, prevalence of acro- megaly-related comorbidities, and factors associated with these comorbidities in patients with acromegaly. Materials and methods: In the study, 96 patients who were followed up with the diagnosis of acromegaly were included. Clinical, labo- ratory and imaging features, and accompanying comorbidities of the patients were recorded from the patient files. Results: Of the patients included in the study, 63 (65.6%) were female and 33 (34.4%) were male. The mean age of diagnosis was 42.61± 12.08, and the mean follow-up period was 9.97 ± 7.26 years. Median insulin-like growth factor 1 level was 238.16 ng/mL (30.5­820), median growth hormone level was 2.05 ug/L (0.1­29.4). A total of 60 (62.5%) of the patients were in the well-controlled group, and 36 (37.5%) had active disease at the time of inclusion. Diabetes mellitus (DM) was detected in 30 (31.3%) patients, prediabetes in 19 (28.8%) patients, hypertriglyceridemia in 38 (42.2%) patients, hypertension (HT) in 41 (42.7%) patients, cardiovascular disease in 5 (5.2%) patients, malignancy in 9 (9.4%) patients, obstructive sleep apnea syndrome in 8 (8.3%) patients, carpal tunnel syndrome in 11 (11.5%) patients, arthropathy in 5 (5.2%) patients, hearing loss in 7 (7.3%) patients, thyroid nodule in 56 (67.5%) patients, thyroid cancer in 4 (4.2%) patients, colonic polyp in 19 (38.8%) patients. Conclusion: In this study, we revealed that the most common comorbidities in acromegaly patients in the Turkish population are thyroid nodules, low high-density lipoprotein (HDL cholesterol (HDL-C) level, hypertriglyceridemia, HT, colonic polyps, DM, and prediabetes, and female sex and age at diagnosis are the most important factors associated with comorbidities.


Asunto(s)
Acromegalia , Pólipos del Colon , Diabetes Mellitus , Hipertensión , Hipertrigliceridemia , Estado Prediabético , Acromegalia/epidemiología , Adolescente , Niño , Preescolar , Diabetes Mellitus/epidemiología , Femenino , Humanos , Hipertensión/epidemiología , Lipoproteínas LDL , Masculino , Prevalencia , Calidad de Vida
10.
Invest New Drugs ; 38(5): 1326-1333, 2020 10.
Artículo en Inglés | MEDLINE | ID: mdl-32062733

RESUMEN

Marine natural products have drawn a great deal of attention as a vital source of new drugs for the last five decades. However, marine organisms in the seas surrounding Turkey (the Black Sea, the Aegean Sea and the Mediterranean Sea) haven't been yet extensively explored. In the present study, three marine organisms (Dysidea avara, Microcosmus sabatieri and Echinaster sepositus) were sampled from the Dardanelles (Turkish Straits System, Western Turkey) by scientific divers, transferred to the laboratory and then were extracted with 70% ethanol. The extracts were tested for their cytotoxic effect against K562, KMS-12PE, A549, and A375 cancer cell lines. The sponge extract elicited the most promising cytotoxic activity, thus it was further evaluated against H929, MCF-7, HeLa, and HCT116 cancer cells. Most of the designated cells showed a considerable sensitivity for the sponge extract particularly H929, K562, KMS-12PE and HeLa cells with IC50 less than 10 µg/mL. On the contrary, the other two extracts exhibited no cytotoxic activity on all cells at 100 µg/mL concentration. The sponge extract was tested for its capacity to induce apoptosis in cancer cells and to inhibit a panel of tyrosine kinases showing remarkable results. The outcome of this study represents a platform for discovery of new chemotherapeutic agents of marine natural origin.


Asunto(s)
Antineoplásicos/farmacología , Productos Biológicos/farmacología , Neoplasias/tratamiento farmacológico , Poríferos , Inhibidores de Proteínas Quinasas/farmacología , Receptor beta de Factor de Crecimiento Derivado de Plaquetas/antagonistas & inhibidores , Receptor 2 de Factores de Crecimiento Endotelial Vascular/antagonistas & inhibidores , Animales , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Humanos , Neoplasias/metabolismo , Turquía
11.
Molecules ; 24(19)2019 Sep 30.
Artículo en Inglés | MEDLINE | ID: mdl-31574910

RESUMEN

Imatinib, an Abelson (ABL) tyrosine kinase inhibitor, is a lead molecular-targeted drug against chronic myelogenous leukemia (CML). To overcome its resistance and adverse effects, new inhibitors of ABL kinase are needed. Our previous study showed that the benzyl ester of gypsogenin (1c), a pentacyclic triterpene, has anti-ABL kinase and a subsequent anti-CML activity. To optimize its activities, benzyl esters of carefully selected triterpenes (PT1-PT6), from different classes comprising oleanane, ursane and lupane, and new substituted benzyl esters of gypsogenin (GP1-GP5) were synthesized. All of the synthesized compounds were purified and charachterized by different spectroscopic methods. Cytotoxicity of the parent triterpenes and the synthesized compounds against CML cell line K562 was examined; revealing three promising compounds PT5, GP2 and GP5 (IC50 5.46, 4.78 and 3.19 µM, respectively). These compounds were shown to inhibit extracellular signal-regulated kinase (ERK) downstream signaling, and induce apoptosis in K562 cells. Among them, PT5 was identified to have in vitro activity (IC50 = 1.44 µM) against ABL1 kinase, about sixfold of 1c, which was justified by molecular docking. The in vitro activities of GP2 and GP5 are less than PT5, hence they were supposed to possess other more mechanisms of cytotoxicity. In general, our design and derivatizations resulted in enhancing the activity against ABL1 kinase and CML cells.


Asunto(s)
Diseño de Fármacos , Triterpenos Pentacíclicos/síntesis química , Triterpenos Pentacíclicos/farmacología , Inhibidores de Proteínas Quinasas/síntesis química , Inhibidores de Proteínas Quinasas/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Antineoplásicos/farmacología , Supervivencia Celular/efectos de los fármacos , Técnicas de Química Sintética , Relación Dosis-Respuesta a Droga , Humanos , Células K562 , Modelos Moleculares , Conformación Molecular , Estructura Molecular , Triterpenos Pentacíclicos/química , Inhibidores de Proteínas Quinasas/química , Proteínas Proto-Oncogénicas c-abl/antagonistas & inhibidores , Proteínas Proto-Oncogénicas c-abl/química , Relación Estructura-Actividad
12.
Turk J Med Sci ; 49(5): 1529-1533, 2019 Oct 24.
Artículo en Inglés | MEDLINE | ID: mdl-31651125

RESUMEN

Background/aim: Thyroid cancer is the most common endocrine malignancy. Recently the incidence has been increasing faster compared to other malignancies. Different studies have shown that the incidence of breast cancer in patients followed due to thyroid cancer has increased, and vice versa. The aim of this study was to evaluate the frequency of second primary cancers in the follow-up of patients with thyroid cancer. Materials and methods: In this study, 1196 patients with thyroid cancer were evaluated in the Necmettin Erbakan University Meram Medical School's Department of Endocrinology between 2004 and 2018. Demographic characteristics and radiological and pathological results of the patients were recorded. The presence of accompanying second malignancies in patients with thyroid cancer was investigated. Results: In our study, 985 (82.4%) women (mean age: 46.1 ± 13.3 years) and 211 (17.6%) men (mean age: 49.9 ± 14.2 years) were evaluated. The median follow-up was 63 months (2­164 months). Of the 1196 patients, 1126 (94.1%) had no additional cancer and 70 (5.9%) patients had a second malignancy. The accompanying second malignancies were breast cancer in 24 (2%) patients, skin cancer in 8 (0.7%) patients, renal cell cancer in 5 (0.4%) patients, lung cancer in 5 (0.4%) patients, colon cancer in 5 (0.4%) patients, lymphoma in 5 (0.4%) patients, endometrial cancer in 4 (0.3%) patients, and 14 cases of other rare types of cancer. Conclusion: In our study, it was found that the most common second primary malignancy in patients with thyroid cancer was breast cancer. However, other cancers (skin cancer, renal cell cancer, lymphoma, and colon, lung, or endometrial cancer) may occur in patients with thyroid cancer.


Asunto(s)
Neoplasias Primarias Secundarias/epidemiología , Neoplasias de la Tiroides/epidemiología , Adulto , Femenino , Humanos , Incidencia , Masculino , Persona de Mediana Edad , Estudios Retrospectivos , Turquía
13.
Biol Pharm Bull ; 41(4): 570-574, 2018 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-29386476

RESUMEN

The discovery of the chimeric tyrosine kinase breakpoint cluster region kinase-Abelson kinase (BCR-ABL)-targeted drug imatinib conceptually changed the treatment of chronic myelogenous leukemia (CML). However, some CML patients show drug resistance to imatinib. To address this issue, some artificial heterocyclic compounds have been identified as BCR-ABL inhibitors. Here we examined whether plant-derived pentacyclic triterpenoid gypsogenin and/or their derivatives show inhibitory activity against BCR-ABL. Among the three derivatives, benzyl 3-hydroxy-23-oxoolean-12-en-28-oate (1c) was found to be the most effective anticancer agent on the CML cell line K562, with an IC50 value of 9.3 µM. In contrast, the IC50 against normal peripheral blood mononuclear cells was 276.0 µM, showing better selectivity than imatinib. Compound 1c had in vitro inhibitory activity against Abelson kinase 1 (ABL1) (IC50=8.7 µM), the kinase component of BCR-ABL. In addition, compound 1c showed a different inhibitory profile against eight kinases compared with imatinib. The interaction between ATP binding site of ABL and 1c was examined by molecular docking study, and the binding mode was different from imatinib and newer generation inhibitors. Furthermore, 1c suppressed signaling downstream of BCR-ABL. This study suggests the possibility that plant extracts may be a source for CML treatment and offer a strategy to overcome drug resistance to known BCR-ABL inhibitors.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Proteínas de Fusión bcr-abl/antagonistas & inhibidores , Leucemia Mielógena Crónica BCR-ABL Positiva/tratamiento farmacológico , Inhibidores de Proteínas Quinasas/farmacología , Saponinas/farmacología , Transducción de Señal/efectos de los fármacos , Triterpenos/farmacología , Antineoplásicos Fitogénicos/efectos adversos , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/metabolismo , Sitios de Unión , Caryophyllaceae/química , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Resistencia a Múltiples Medicamentos , Resistencia a Antineoplásicos , Proteínas de Fusión bcr-abl/química , Proteínas de Fusión bcr-abl/metabolismo , Humanos , Mesilato de Imatinib/química , Mesilato de Imatinib/metabolismo , Mesilato de Imatinib/farmacología , Células K562 , Cinética , Leucocitos Mononucleares/citología , Leucocitos Mononucleares/efectos de los fármacos , Leucocitos Mononucleares/inmunología , Simulación del Acoplamiento Molecular , Estructura Molecular , Inhibidores de Proteínas Quinasas/efectos adversos , Inhibidores de Proteínas Quinasas/química , Inhibidores de Proteínas Quinasas/metabolismo , Saponinas/efectos adversos , Saponinas/química , Saponinas/metabolismo , Triterpenos/efectos adversos , Triterpenos/química , Triterpenos/metabolismo
14.
Water Sci Technol ; 71(12): 1901-11, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-26067512

RESUMEN

Linear and non-linear regression procedures have been applied to the Langmuir, Freundlich, Tempkin, Dubinin-Radushkevich, and Redlich-Peterson isotherms for adsorption of acid yellow 132 (AY132) dye onto red pine (Pinus resinosa) sawdust. The effects of parameters such as particle size, stirring rate, contact time, dye concentration, adsorption dose, pH, and temperature were investigated, and interaction was characterized by Fourier transform infrared spectroscopy and field emission scanning electron microscope. The non-linear method of the Langmuir isotherm equation was found to be the best fitting model to the equilibrium data. The maximum monolayer adsorption capacity was found as 79.5 mg/g. The calculated thermodynamic results suggested that AY132 adsorption onto red pine sawdust was an exothermic, physisorption, and spontaneous process. Kinetics was analyzed by four different kinetic equations using non-linear regression analysis. The pseudo-second-order equation provides the best fit with experimental data.


Asunto(s)
Colorantes/química , Pinus , Madera/química , Adsorción , Concentración de Iones de Hidrógeno , Cinética , Tamaño de la Partícula , Espectroscopía Infrarroja por Transformada de Fourier , Temperatura , Termodinámica , Contaminantes Químicos del Agua/química
15.
Phys Med Biol ; 69(12)2024 Jun 13.
Artículo en Inglés | MEDLINE | ID: mdl-38830364

RESUMEN

ObjectiveFull-form Magnetic Resonance Electrical Properties Tomography (MREPT) requires bothB1+magnitude and phase information. SinceB1+phase can be obtained faster and with higher SNR compared toB1+magnitude, several phase-based methods have been developed for conductivity imaging. However, phase-based methods suffer from a concave bias due to the assumption that∇|B1+|is negligible in the ROI.ApproachIn this paper, we re-derive the central equation of phase-based cr-MREPT without assuming that∇|B1+|is negligible and thus propose a correction method directly integrated into the equation system.Main resultsProposed method successfully corrects the concave bias on both simulated and experimental data and significantly increases image quality.SignificanceThe proposed correction method depends on a very low-resolution|B1+|map, and therefore the imaging time does not increase significantly for obtainingB1+magnitude. Moreover, correction can be achieved using simulatedB1+magnitude, hence completely removing the additional imaging requirement.


Asunto(s)
Procesamiento de Imagen Asistido por Computador , Procesamiento de Imagen Asistido por Computador/métodos , Imagen por Resonancia Magnética , Tomografía/métodos , Conductividad Eléctrica , Fantasmas de Imagen
16.
ACS Omega ; 9(7): 7413-7423, 2024 Feb 20.
Artículo en Inglés | MEDLINE | ID: mdl-38405451

RESUMEN

A series of self-assembled monolayer (SAM)-based benzoic acid derivatives such as 4-[5'-phenyl-2,2'-bitien-5-yl] benzoic acid (ZE-Ph), 4-[5'-(4-fluorophenyl)-2,2'-bitien-5-yl]benzoic acid (ZE-1F), and 4-[5'-(3,5-difluorophenyl)-2,2'-bitien-5-yl]benzoic acid (ZE-2F) were synthesized to use an interlayer between an ITO electrode and a MoO3 thin film layer in an organic solar cell (OSC) having poly-3 hexylthiophene (P3HT): [6,6]-phenyl C61 butyric acid methyl ester (PC61BM) blend. The work function and surface wetting properties of the ITO were tuned by SAM molecules. The power conversion efficiency of fabricated OSC devices was improved compared to that of the control device from 1.93 to 2.20% and 2.22% with ZE-Ph and ZE-1F-modified ITO electrodes, respectively. The short-circuit current density (Jsc) was increased from 6.16 to 7.10 mA/cm2 and 6.94 mA/cm2 with control, ZE-Ph, and ZE-1F-modified solar cells, respectively. The increase in short-circuit current density (Jsc) shows that the hole-transporting properties between ITO and MoO3 were improved by the use of ZE-Ph and ZE-1F compared with that of the ITO/MoO3 electrode configuration. The open-circuit voltage (Voc) of the SAM-modified ITO-based devices was also improved compared with the Voc of unmodified ITO-based devices. These results show that using a monolayer as an interlayer in OSCs is an important strategy to improve the performance of OSCs. All the device parameters were characterized by Kelvin probe force microscopy, cyclic voltammetry, contact angle, and I-V measurements.

17.
Acta Orthop Traumatol Turc ; 58(2): 116-123, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-39128106

RESUMEN

OBJECTIVE:  It is important to protect the mobile segment in the lumbar region in scoliosis surgery. The aim of this study was to compare the clinical and radiological results of patients who underwent surgery for a diagnosis of adolescent idiopathic scoliosis (AIS) with the lowest instrumented vertebra (LIV) at L3 or L4 level. METHODS:  The study included 36 patients who underwent surgical treatment in our institution for a diagnosis of Lenke type 5 and 6 AIS with a follow-up period of at least 24 months. The patients were separated into 2 groups according to the LIV level of L3 (n=21) and L4 (n=15). These 2 groups were compared preoperatively (PO), early postoperative (EPO), and at the final follow-up examination (last control (LC)) with respect to radiological parameters in the coronal and sagittal planes, and the Scoliosis Research Society - 22 (SRS-22) questionnaire values. RESULTS:  In both groups the mean age (L3: 16 ± 7.3; L4: 17 ± 6.1 years) and follow-up periods (L3: 44 ± 20; L4: 47 ± 18 months) were similar. Radiologically, the L4 group had a greater Cobb angle in the scoliosis main curves measured PO (P=.001). The Cobb angles measured at EPO (P=.767) and at LC (P=.674) were similar in both groups. No significant difference was observed between the 2 groups in respect of the LIV tilt values at PO (P=.469), EPO (P=.297), and LC (P=.065). When the groups were evaluated separately, the LIV tilt values at EPO and LC were similar in the L4 group (EPO: 6.93 ± 3.058; LC: 7.26 ± 2.313; P=.618). In the L3 patients, although there seemed to be a significant increase in LIV tilt values when EPO values were compared with LC values (EPO: 8.47 ± 3.970; LC: 9.57 ± 3.76; P=.030), this was within the error range of Cobb angle measurement. The results of the SRS-22 questionnaire showed significantly better results in the L3 group in the domains of pain, function/activity, mental health, and satisfaction with treatment (P=.011, P=.002, P=.019, P=.046, respectively). CONCLUSION:  There was no radiological superiority between L3 and L4 LIV groups in the thoracolumbar/lumbar curve patients. However, according to the SRS-22 questionnaire, the results of patients with L3 level LIV were better in the areas of pain, function/activity, mental health, and satisfaction with treatment. Cite this article as: Baymurat AC, Tokgoz MA, Abdulaliyev F, Tosun MF, Can MM, Senkoylu A. Which lumbar vertebra should be the lowest level of fusion in adolescent idiopathic scoliosis of Lenke types 5 and 6? Acta Orthop Traumatol Turc., 2024;58(2):116-123.


Asunto(s)
Vértebras Lumbares , Radiografía , Escoliosis , Fusión Vertebral , Humanos , Escoliosis/cirugía , Fusión Vertebral/métodos , Adolescente , Vértebras Lumbares/cirugía , Vértebras Lumbares/diagnóstico por imagen , Femenino , Masculino , Radiografía/métodos , Resultado del Tratamiento , Niño , Estudios Retrospectivos , Estudios de Seguimiento , Adulto Joven , Encuestas y Cuestionarios
18.
Biomacromolecules ; 14(10): 3532-41, 2013 Oct 14.
Artículo en Inglés | MEDLINE | ID: mdl-23987303

RESUMEN

Single-walled carbon nanotubes (SWNTs) are unique nanostructures used as cargo systems for variety of diagnostic and therapeutic agents. For taking advantage of these structures in biological processes, they should be visible. Therefore, fluorescence labeling of SWCNTs with various probes is a significant issue. Herein, we demonstrate a simple approach for cell specific imaging and diagnosis by combining SWCNTs with a copolymer poly(para-phenylene) (PPP) containing polystyrene (PSt) and poly(ε-caprolactone) (PCL) side chains (PPP-g-PSt-PCL). In this approach PPP-g-PSt-PCL is noncovalently attached on carboxyl functional SWCNTs. The obtained fluorescent probe is bound to folic acid (FA) for targeted imaging of folate receptor (FR) positive HeLa cells. In vitro studies demonstrate that this conjugate can specifically bind to HeLa cells and indicate great potential for targeting and imaging studies.


Asunto(s)
Fluorescencia , Colorantes Fluorescentes , Imagen Molecular , Nanotubos de Carbono/química , Línea Celular Tumoral , Colorantes Fluorescentes/síntesis química , Colorantes Fluorescentes/química , Ácido Fólico/química , Transportadores de Ácido Fólico/química , Células HeLa , Humanos , Estructura Molecular
19.
J Mol Graph Model ; 121: 108462, 2023 06.
Artículo en Inglés | MEDLINE | ID: mdl-37001439

RESUMEN

In this paper, we design new forms of organic conjugated compounds-based quinoxaline derivatives. Specifically, we exploit density functional theory and time-dependent-density functional theory in order to study the structure, the optic, the electronic, the reorganization energy and the photovoltaic features of such new molecules. Particularly, all engineered compounds have a narrow band gap in the range of 0.696-0.721 eV, high oscillator frequency and good optical properties. Moreover, the PCBM is employed as an electron acceptor. Employing global reactivity descriptors, we demonstrate that the molecules can efficiently emit electrons into the PCBM and the electrons are attracted to PCBM from molecules. In addition, the results show an appropriate open circuit voltage in the range of 0.338-0.362 V. The proposed compounds exhibit excellent electron transport and charge conduction from the donor to the acceptor. These new molecules show potential properties to develop bulk heterojunction organic photovoltaic cells.


Asunto(s)
Electrones , Quinoxalinas , Electrónica , Teoría Funcional de la Densidad , Transporte de Electrón
20.
Rev Bras Ginecol Obstet ; 45(2): 82-88, 2023 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-36977405

RESUMEN

OBJECTIVE: It was aimed to compare visceral adiposity index (VAI) levels in patients with normal bone mineral density (BMD), osteopenia, and osteoporosis. METHODS: One hundred twenty postmenopausal women (40 with normal BMD, 40 with osteopenia, and 40 with osteoporosis) between the ages of 50 to 70 years were included in the study. For females, the VAI was calculated using the formula (waist circumference [WC]/[36.58 + (1.89 x body mass index (BMI))]) x (1.52/High-density lipoprotein [HDL]-cholesterol [mmol/L]) x (triglyceride [TG]/0.81 [mmol/L]). RESULTS: The time of menopause from the beginning was similar in all groups. Waist circumference was found to be higher in those with normal BMD than in the osteopenic and osteoporotic groups (p = 0.018 and p < 0.001, respectively), and it was also higher in the osteopenic group than in the osteoporotic group (p = 0.003). Height and body weight, BMI, blood pressure, insulin, glucose, HDL-cholesterol, and homeostasis model assessment-insulin resistance (HOMA-IR) levels were similar in all groups. Triglyceride levels were found to be higher in the normal BMD group, compared with the osteoporotic group (p = 0.005). The level of VAI was detected as higher in those with normal BMD, compared with the women with osteoporosis (p = 0.002). Additionally, the correlation analysis showed a positive correlation between dual-energy X-ray absorptiometry (DXA) spine T-scores, WC, VAI, and a negative correlation between DXA spine T-scores and age. CONCLUSION: In our study, we found higher VAI levels in those with normal BMD, compared with women with osteoporosis. We consider that further studies with a larger sample size will be beneficial in elucidating the entity.


OBJETIVO: O objetivo foi comparar os níveis de índice de adiposidade visceral (IVA) em pacientes com densidade mineral óssea (DMO) normal osteopenia e osteoporose. MéTODOS: Cento e vinte mulheres na pós-menopausa (40 com DMO normal 40 com osteopenia e 40 com osteoporose) com idades entre 50 e 70 anos foram incluídas no estudo. Para o sexo feminino o VAI foi calculado pela fórmula (circunferência da cintura [CC]/[36 58 + (1 89 x índice de massa corporal (IMC))]) x (1 52/lipoproteína de alta densidade [HDL]-colesterol [mmol/L] ) x (triglicerídeo [TG]/0 81 [mmol/L]). RESULTADOS: O tempo de menopausa desde o início foi semelhante em todos os grupos. A circunferência da cintura foi maior naqueles com DMO normal do que nos grupos osteopênicos e osteoporóticos (p = 0 018 e p < 0 001 respectivamente) e também foi maior no grupo osteopênico do que no grupo osteoporótico (p = 0 003) . Altura e peso corporal IMC pressão arterial insulina glicose HDL-colesterol e os níveis de avaliação do modelo de homeostase-resistência à insulina (HOMA-IR) foram semelhantes em todos os grupos. Os níveis de triglicerídeos foram maiores no grupo DMO normal em comparação com o grupo osteoporótico (p = 0 005). O nível de VAI foi detectado como maior naquelas com DMO normal em comparação com as mulheres com osteoporose (p = 0 002). Além disso a análise de correlação mostrou uma correlação positiva entre a absorciometria de raios-X de dupla energia (DXA) nas pontuações T da coluna CC VAI e uma correlação negativa entre as pontuações T da coluna DXA e a idade. CONCLUSãO: Em nosso estudo encontramos níveis mais elevados de VAI naquelas com DMO normal em comparação com mulheres com osteoporose. Consideramos que novos estudos com maior tamanho amostral serão benéficos na elucidação da entidade.


Asunto(s)
Enfermedades Óseas Metabólicas , Osteoporosis Posmenopáusica , Osteoporosis , Humanos , Femenino , Persona de Mediana Edad , Anciano , Posmenopausia , Osteoporosis Posmenopáusica/diagnóstico por imagen , Adiposidad , Densidad Ósea , Absorciometría de Fotón , Índice de Masa Corporal , Triglicéridos , Colesterol
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