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BACKGROUND: Osteoporosis and atherosclerosis frequently afflict older adults, and recent insights suggest a deeper connection between these conditions that surpasses mere aging effects. The ratio of non-high-density to high-density lipoprotein cholesterol (NHHR) has emerged as a novel lipid marker for evaluating the risk of cardiovascular diseases. Nonetheless, investigations into the correlation of the NHHR with the risk of developing osteoporosis remain unexplored. METHODS: We collected NHHR and bone mineral density (BMD) data from 11,024 National Health and Nutrition Examination Survey (NHANES) participants between 2011 and 2018. Multivariate linear regression was employed to examine the correlation between BMD and NHHR. Smooth curves were employed to deal with the nonlinearity. To further account for the nonlinear link, we used a two-part linear regression model. The threshold effects were estimated using two components of a linear regression model. Subgroup and sensitivity analyses were carried out to ascertain the stability of the findings. RESULTS: We discovered a negative relationship between the NHHR and lumbar spine BMD in all three models. An L-shaped curvilinear association existed between the NHHR and lumbar spine BMD, with a key inflection point of 6.91. The fully adjusted model showed that the BMD of the lumbar spine fell by 0.03 g/cm2 in those who were in the fourth quartile as opposed to the lowest quartile. The sensitivity analysis using unweighted logistic analysis verified the stability of the results. In addition, BMD in the nondiabetic group was more significantly affected by the negative effect of the NHHR in the subgroup analysis. CONCLUSIONS: According to this research, there appears to be a negative correlation between BMD and NHHR in US Adults. To clarify the precise physiological mechanisms by which the NHHR contributes to the onset of osteoporosis, more research is necessary.
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Densidad Ósea , HDL-Colesterol , Encuestas Nutricionales , Osteoporosis , Humanos , Osteoporosis/sangre , Osteoporosis/epidemiología , Femenino , Masculino , Persona de Mediana Edad , HDL-Colesterol/sangre , Factores de Riesgo , Adulto , Anciano , Vértebras Lumbares , Modelos Lineales , Estados Unidos/epidemiologíaRESUMEN
Primary hyperparathyroidism (PHPT) is a rare disease in pregnancy and endangers the health of both pregnant women and fetuses. However, the treatments are very limited for PHPT and most of them are unsatisfactory because of the peculiar state in pregnancy. The only curable method is parathyroidectomy which can be safely performed in the second trimester of pregnancy. In this case, we reported a pregnant woman with primary parathyroid adenoma presenting hypercalcemia and severe vomit at the end of first trimester. Finally, she got cured by microwave ablation at the end of first trimester and gave birth to a healthy baby boy.
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OBJECTIVES: To determine the predictive effect of Hounsfield unit (HU) values in the cervical vertebral body measured by computed tomography (CT) and T-scores measured by dual-energy X-ray absorptiometry (DXA) on Zero-P subsidence after anterior cervical discectomy and fusion (ACDF)with Zero-P. In addition, we evaluated the most reliable measurement of cervical HU values. METHODS: We reviewed 76 patients who underwent single-level Zero-P fusion for cervical spondylosis. HU values were measured on CT images according to previous studies. Univariate analysis was used to screen the influencing factors of Zero-P subsidence, and then, logistic regression was used to determine the independent risk factors. The area under the receiver operating characteristic curve (AUC) was used to evaluate the ability to predict Zero-P subsidence. RESULTS: Twelve patients (15.8%) developed Zero-P subsidence. There were significant differences between subsidence group and non-subsidence group in terms of age, axial HU value, and HU value of midsagittal, midcoronal, and midaxial (MSCD), but there were no significant differences in lowest T-score and lowest BMD. The axial HU value (OR = 0.925) and HU value of MSCD (OR = 0.892) were independent risk factors for Zero-P subsidence, and the lowest T-score was not (OR = 1.186). The AUC of predicting Zero-P subsidence was 0.798 for axial HU value, 0.861 for HU value of MSCD, and 0.656 for T-score. CONCLUSIONS: Lower cervical HU value indicates a higher risk of subsidence in patients following Zero-P fusion for single-level cervical spondylosis. HU values were better predictors of Zero-P subsidence than DXA T-scores. In addition, the measurement of HU value in the midsagittal, midcoronal, and midaxial planes of the cervical vertebral body provides an effective method for predicting Zero-P subsidence.
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Fusión Vertebral , Espondilosis , Humanos , Absorciometría de Fotón/métodos , Tomografía Computarizada por Rayos X/métodos , Discectomía , Curva ROC , Espondilosis/diagnóstico por imagen , Espondilosis/cirugía , Estudios Retrospectivos , Fusión Vertebral/métodos , Vértebras LumbaresRESUMEN
A method for the quantitative measurement of two-dimensional density field distributions based on deflectometry is proposed. With this method, from the point of view of the inverse Hartmann test, the light rays emitted from the camera reach the screen after being disturbed by the shock-wave flow field. After the coordinates of the point source are obtained by using the phase information, the deflection angle of the light ray can be calculated, and then the distribution of the density field can be determined. The principle of density field measurement deflectometry (DFMD) is described in detail. In the experiment, the density fields in wedge-shaped models with three different wedge angles are measured in supersonic wind tunnels, the experimental results from the proposed method are compared with the theoretical results, and the measurement error is found to be around 2.76 × 10-3kg/m3. This method has the advantages of fast measurement, a simple device, and low cost. It provides a new approach, to the best of our knowledge, to measuring the density field of a shock-wave flow field.
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Purpose: In this study, we aimed to develop and validate nomograms for predicting the survival outcomes in patients with T1-2N1 breast cancer to identify the patients who could not benefit from postmastectomy radiotherapy (PMRT). Methods: Data from 10191 patients with T1-2N1 breast cancer were extracted from the Surveillance, Epidemiology, and End Results (SEER) database. Of them, 6542 patients who had not received PMRT formed the training set. Concurrently, we retrospectively enrolled 419 patients from the Affiliated Hospital of North Sichuan Medical College (NSMC), and 286 patients who did not undergo PMRT formed the external validation set. The least absolute shrinkage and selection operator (LASSO) and multivariate Cox regression analyses were used for selecting prognostic factors in the training set. Using the selected factors, two prognostic nomograms were constructed. The nomograms' performance was assessed using the concordance index (C-index), calibration curves, decision curve analysis (DCA), and risk subgroup classification. The stabilized inverse probability of treatment weights (IPTWs) was used to balance the baseline characteristics of the different risk groups. Finally, the survival outcomes and effectiveness of PMRT after IPTW adjustment were evaluated using adjusted Kaplan-Meier curves and Cox regression models. Results: The 8-year overall survival (OS) and breast cancer-specific survival (BCSS) rates for the SEER cohort were 84.3% and 90.1%, with a median follow-up time of 76 months, while those for the NSMC cohort were 84.1% and 86.9%, with a median follow-up time of 73 months. Moreover, significant differences were observed in the survival curves for the different risk subgroups (P < 0.001) in both SEER and NSMC cohorts. The subgroup analysis after adjustment by IPTW revealed that PMRT was significantly associated with improved OS and BCSS in the intermediate- (hazard ratio [HR] = 0.72, 95% confidence interval [CI]: 0.59-0.88, P=0.001; HR = 0.77, 95% CI: 0.62-0.95, P = 0.015) and high- (HR=0.66, 95% CI: 0.52-0.83, P<0.001; HR=0.74, 95% CI: 0.56-0.99, P=0.039) risk groups. However, PMRT had no significant effects on patients in the low-risk groups. Conclusion: According to the prognostic nomogram, we performed risk subgroup classification and found that patients in the low-risk group did not benefit from PMRT.
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With the proliferation of synthetic drugs, research on the mechanism of action of addictive drugs and treatment methods is of great significance. Among them, methamphetamine (METH) is the most representative amphetamine synthetic drug, and the treatment of METH addiction has become an urgent medical and social problem. In recent years, the therapeutic effects of Chinese herbal medicines on METH addiction have gained widespread attention because of their non-addictiveness, multiple targets, low side effects, low cost, and other characteristics. Previous studies have identified a variety of Chinese herbal medicines with effects on METH addiction. Based on the research on METH in recent years, this article summarizes the mechanism of action of METH as the starting point and briefly reviews the Chinese herbal medicine-based treatment of METH.
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Trastornos Relacionados con Anfetaminas , Conducta Adictiva , Medicamentos Herbarios Chinos , Metanfetamina , Humanos , Metanfetamina/efectos adversos , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/uso terapéutico , Anfetamina/uso terapéutico , Conducta Adictiva/tratamiento farmacológico , Trastornos Relacionados con Anfetaminas/tratamiento farmacológicoRESUMEN
Objective: The same clinicopathological features and prognosis have been reported between single progesterone receptor-positive (sPR-positive) and triple-negative phenotype in early-stage breast cancer, but such similarity has not been studied in metastatic breast cancer (MBC). Therefore, the purpose of this study was to estimate the difference between sPR-positive phenotype and other phenotypes in MBC. Methods: Patients with HER-2-negative MBC were selected from the Surveillance, Epidemiology and End Results database. Pearson's χ2 test was used to compare the difference of clinicopathologic factors between sPR-positive phenotype and other phenotypes. Univariate and multivariate analyses were performed to evaluate the effects of hormone receptor (HoR) phenotypes and other clinicopathologic factors on the cancer-specific survival (CSS) and overall survival (OS). Results: Overall, 10877 patients including 7060 patients (64.9%) with double HoR-positive (dHoR-positive), 1533 patients (14.1%) with single estrogen receptor-positive (sER-positive), 126 patients (1.2%) with sPR-positive and 2158 patients (19.8%) with double HoR-negative (dHoR-negative) were analyzed. The patients with sPR-positive or dHoR-negative were more likely to be younger, higher grade and tumor stage, visceral and brain metastasis than ER-positive phenotypes (P<0.001). MBC with sPR-positive had the similar CSS (HR: 1.135, 95%CI: 0.909-1.417, P=2.623) and OS (HR: 1.141, 95%CI: 0.921-1.413, P=0.229) as dHoR-negative, but worse outcome than ER-positive phenotypes. Chemotherapy significantly improved the survival for MBC, especially for sPR-positive MBC (CSS, HR: 0.39, 95%CI: 0.213-0.714, P=0.002; OS, HR: 0.366, 95%CI: 0.203-0.662, P=0.001). Conclusions: Patients with sPR-positive and triple-negative have similar biological behavior and prognosis in MBC. Chemotherapy may be a preferred recommendation for MBC with sPR-positive.
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BACKGROUND: Posterior lumbar interbody fusion (PLIF) has become a classic treatment modality for lumbar degenerative diseases, with cage subsidence as a potentially fatal complication due to low bone mineral density (BMD), which can be measured by forearm T-score. Hounsfield units (HU) derived from computed tomography have been a reliable method for assessing BMD. OBJECTIVE: To determine the accuracy of forearm T-score in predicting cage subsidence after PLIF compared with lumbar spine HU values. METHODS: We retrospectively analyzed the clinical data of 71 patients who underwent PLIF and divided them into cage subsidence group and nonsubsidence group. The differences in preoperative HU value and forearm T-score were compared between groups, and the correlation between cage subsidence and clinical efficacy was analyzed. RESULTS: The subsidence rate for all 71 patients (31 men and 40 women) was 23.9%. There was no significant difference in age, sex ratio, body mass index, smoking status, follow-up time, spine BMD, and spine T-score between groups, except in the forearm T-score and lumbar spine HU values (P < 0.05). The forearm T-score (AUC, 0.840; 95% CI, 0.672-1.000) predicted cage subsidence more accurately than the mean global HU value (AUC, 0.744; 95% CI, 0.544-0.943). In logistic regression analysis, both forearm T-score and mean global HU value were found to be independent risk factors for cage subsidence (P < 0.05). CONCLUSIONS: Lower forearm T-scores and lower lumbar spine HU values were significantly associated with the occurrence of cage subsidence. Lower forearm T-scores indicated a higher risk of cage subsidence than lumbar spine HU values. Forearm T-score is more effective in predicting cage subsidence than spine T-score. Therefore, forearm dual-energy X-ray absorptiometry may be a fast, simple, and reliable method for predicting cage subsidence following PLIF. However, our results suggest that the degree of cage subsidence is not associated with clinical efficacy.
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Fusión Vertebral , Masculino , Humanos , Femenino , Fusión Vertebral/efectos adversos , Fusión Vertebral/métodos , Estudios Retrospectivos , Antebrazo , Vértebras Lumbares/diagnóstico por imagen , Vértebras Lumbares/cirugía , Región LumbosacraRESUMEN
To investigate the subcellular localization of ANXA2 in breast cancer of different cell densities in humans and its relationship with the clinicopathological features of patients. To investigate the differences in ANXA2 subcellular localization in MDA-MB-231 cells of different cell densities. To compare the proliferation, invasion, and migration ability of MDA-MB-231 cells under different ANXA2 subcellular localization.MethodsImmunohistochemistry was applied to detect the subcellular localization of ANXA2 in tissue sections of 60 breast cancer patients, and the association with ANXA2 subcellular localization was verified in conjunction with cell density. To investigate the relationship between cell density and clinicopathological data of breast cancer patients. To establish high- and low-density models of MDA-MB-231 breast cancer cell lines and verify the subcellular localization of ANXA2 using immunofluorescence and observation under confocal microscopy. The proliferation, migration, and invasion ability of MDA-MB-231 cells under different subcellular localization of ANXA2 were detected and compared using CCK-8 assay and Transwell assay. After changing the subcellular localization of ANXA2 in high-density MDA-MB-231 cells with PY-60, changes in biological behaviors of the compared MDA-MB-231 cells were observed. Two different 4T1 cell lines with high and low densities were implanted subcutaneously in nude mice to observe the effects of different cell densities on tumor growth in nude mice.ResultsThe clinical data showed that breast cancer with high cell density had higher T stage and higher TNM stage, and the cell density was positively correlated with breast cancer mass size. ANXA2 was mainly localized to the cell membrane when the cell density of breast cancer cells was high and to the cytoplasm when the cell density was low. (AU)
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Humanos , Animales , Anexina A2 , Neoplasias de la Mama/patología , Línea Celular Tumoral , Proliferación Celular , Sincalida/metabolismo , Movimiento Celular , RatonesRESUMEN
OBJECTIVE: To investigate the subcellular localization of ANXA2 in breast cancer of different cell densities in humans and its relationship with the clinicopathological features of patients. To investigate the differences in ANXA2 subcellular localization in MDA-MB-231 cells of different cell densities. To compare the proliferation, invasion, and migration ability of MDA-MB-231 cells under different ANXA2 subcellular localization. METHODS: Immunohistochemistry was applied to detect the subcellular localization of ANXA2 in tissue sections of 60 breast cancer patients, and the association with ANXA2 subcellular localization was verified in conjunction with cell density. To investigate the relationship between cell density and clinicopathological data of breast cancer patients. To establish high- and low-density models of MDA-MB-231 breast cancer cell lines and verify the subcellular localization of ANXA2 using immunofluorescence and observation under confocal microscopy. The proliferation, migration, and invasion ability of MDA-MB-231 cells under different subcellular localization of ANXA2 were detected and compared using CCK-8 assay and Transwell assay. After changing the subcellular localization of ANXA2 in high-density MDA-MB-231 cells with PY-60, changes in biological behaviors of the compared MDA-MB-231 cells were observed. Two different 4T1 cell lines with high and low densities were implanted subcutaneously in nude mice to observe the effects of different cell densities on tumor growth in nude mice. RESULTS: The clinical data showed that breast cancer with high cell density had higher T stage and higher TNM stage, and the cell density was positively correlated with breast cancer mass size. ANXA2 was mainly localized to the cell membrane when the cell density of breast cancer cells was high and to the cytoplasm when the cell density was low. The CCK-8 assay showed that the proliferation rate of MDA-MB-231 cells increased (P < 0.05) after shifting the subcellular localization of ANXA2 from the cell membrane to the cytoplasm. Transwell invasion assay and Transwell migration assay showed that the invasion and migration ability of MDA-MB-231 cells increased significantly after the subcellular localization of ANXA2 was transferred from the cell membrane to the cytoplasm (P < 0.05). The animal experiments showed that high-density breast cancer cells could promote the growth of subcutaneous tumors in nude mice relative to low-density breast cancer cells. CONCLUSION: Cell density can regulate the subcellular localization of ANXA2, and changes in the subcellular localization of ANXA2 are accompanied by the changes in the biological behavior of breast cancer.
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Anexina A2 , Neoplasias de la Mama , Animales , Neoplasias de la Mama/patología , Recuento de Células , Línea Celular Tumoral , Movimiento Celular , Proliferación Celular , Femenino , Humanos , Ratones , Ratones Desnudos , Invasividad NeoplásicaRESUMEN
OBJECTIVE: Based on physical examination, to explore the relationship between breast mass (BM) and thyroid nodule (TN) prevalence, and to further explore other related factors that affect the occurrence of BM and TN. METHODS: From January 1, 2018, to January 1, 2021, 12,538 female subjects received breast and thyroid ultrasound examinations at the same time in the health examination center of the Affiliated Hospital of North Sichuan Medical College. Univariate analysis and multivariate logistic analysis were used to screen the relevant factors affecting TN and BM, and propensity score matching was used to further verify the results of the relationship between breast and thyroid. RESULTS: A total of 4975 (39.7%) of the included subjects have BM and a total of 6315 (50.4%) have TN,2557 (20.4%) had both BM and TN. The logistic regression results show that patients with TN are more likely to suffer from BM [OR = 1.185, 95% CI (1.099-1.278), p<0.0001]. In addition, age, free T4, HDL, height, BMI, systolic blood pressure, diastolic blood pressure, and albumin are independent factors affecting the occurrence of BM; patients with BM are more likely to have TN [OR = 1.180, 95% CI (1.094-1.272), p<0.0001], and age, free T3, free T4, AST, ALT, albumin, height, and BMI are independent influencing factors on the occurrence of TN. The result of propensity score matching confirmed the relationship between BM and TN. CONCLUSION: There is a bidirectional pathogenic relationship between BM and TN, women with BM are at increased risk of TN, and women with TN are more likely to have BM. Thyroid hormone is not only related to the occurrence of TN but also affects the occurrence of BM.
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The presence of dyes in a water system has potential adverse effects on the ecological environment. The conventional cyclodextrin (CD) polymer only has CD cavities as adsorption sites and exhibits slow adsorption for dye removal. In this study, we designed a novel carboxymethyl ß-CD polymer (ß-CDP-COOH). The structural properties of ß-CDP-COOH were characterized as an irregular cross-linked polymer with negative surface charge, and the introduction of carboxymethyl groups greatly enhanced the adsorption ability of the ß-CD polymer to basic fuchsin (BF). The maximum removal efficiency of ß-CDP-COOH (96%) could be achieved within 1 min, whereas that of conventional ß-CD polymer (70%) was achieved after 50 min. The adsorption mechanism revealed that the adsorption behavior of ß-CDP-COOH could be effectively fitted with the pseudo-second-order kinetic model and Langmuir isotherm. Both CD cavities and carboxymethyl groups were effective adsorption sites, so ß-CDP-COOH had an advantage in adsorption capacity over the conventional ß-CD polymer. This study indicated that ß-CDP-COOH is a potential highly efficient adsorbent for the removal of cationic dye contaminants.
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The study mainly aimed to improve the aqueous solubility of Balofloxacin (BLFX) by preparing the inclusion complexes (ICs) of BLFX with cyclodextrins (CDs). In this study, ICs in solid state were obtained by using beta-CD (ß-CD), 2-hydroxypropyl-ß-CD (HP-ß-CD), 2, 6-dimethyl-ß-CD (DM-ß-CD) through a freeze-drying technique. The formation of ICs was confirmed through Fourier-transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffraction, nuclear magnetic resonance, and scanning electron microscopy. Results demonstrated that the water solubility and dissolution rates of three ICs were distinctly improved than that of parent BLFX. Bacteriostatic experiment manifested that the antibacterial effect of BLFX was not inhibited after encapsulation in CDs. The damage of BLFX to kidney and liver cells was reduced. Consequently, successful preparation of the ICs of BLFX with CDs provided possibility for devising new dosage form of BLFX, which held great promise for further applications in clinical fields.
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Fluoroquinolonas/química , beta-Ciclodextrinas/química , Rastreo Diferencial de Calorimetría , Composición de Medicamentos , Liofilización/métodos , Espectroscopía de Resonancia Magnética , Microscopía Electrónica de Rastreo , Polvos , Espectroscopía Infrarroja por Transformada de Fourier/métodos , Difracción de Rayos XRESUMEN
The binding properties between γ-lactone essences and HSA were investigated to explore interactional mechanism and influence of ligand side chains on binding via computer simulations, microscopy, and multiple-spectroscopies. Docking and molecular dynamics presented protein recognition mode with low fluctuations. NMR analysis revealed that the lactone ring of ligands was the main group bound to HSA. UV-vis and lifetime results revealed that the combination was static quenching mechanism with binding constants of 102-103â¯L/mol. FTIR and CD spectra showed conformational changes in the protein secondary structure induced by ligands. Side chains affect the binding process through steric hindrance and hydrophobicity. AFM images showed the four compounds caused different effects on molecular size of HSA. In conclusion, the binding ability and the protein secondary structure changes had a positive correlation with the length of side chain. These studies are beneficial for understanding the safety and biological action of γ-lactone essences.
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Lactonas/química , Albúmina Sérica Humana/química , Albúmina Sérica Humana/metabolismo , Sitios de Unión , Dicroismo Circular , Humanos , Interacciones Hidrofóbicas e Hidrofílicas , Lactonas/metabolismo , Ligandos , Espectroscopía de Resonancia Magnética , Microscopía de Fuerza Atómica , Simulación del Acoplamiento Molecular , Simulación de Dinámica Molecular , Unión Proteica , Conformación Proteica , Estructura Secundaria de Proteína , Espectrofotometría Ultravioleta , Espectroscopía Infrarroja por Transformada de FourierRESUMEN
This study aimed to develop a novel sustained release system for mesalazine (MSZ) by preparing hydroxypropyl-ß-cyclodextrin (HP-ß-CD) inclusion complex loaded chitosan (CS) nanoparticles (NPs). The HP-ß-CD/MSZ complex was prepared at 1:1 stoichiometry and characterized by using various analysis techniques. The HP-ß-CD/MSZ/CS NPs prepared under the optimum condition had a spherical shape (90±17 nm diameter), a narrow size distribution, and a high loading efficiency. Compared with free MSZ, the HP-ß-CD/MSZ/CS NPs exhibited an obvious sustained release of MSZ. The activity of the NPs against a cytokine-triggered inflammatory response was evaluated in cytokine-stimulated HT-29 cell lines by monitoring key inflammatory mediators. The results revealed that compared with free MSZ, the NPs more strongly inhibited the production of NO, PGE2, and IL-8, indicating the NPs possibly had better anti-inflammatory effects. Therefore, the established HP-ß-CD/MSZ/CS NPs may be a promising delivery system of MSZ.
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2-Hidroxipropil-beta-Ciclodextrina/administración & dosificación , Antiinflamatorios no Esteroideos/administración & dosificación , Quitosano/administración & dosificación , Portadores de Fármacos/administración & dosificación , Mesalamina/administración & dosificación , Nanopartículas/administración & dosificación , 2-Hidroxipropil-beta-Ciclodextrina/química , Antiinflamatorios no Esteroideos/química , Supervivencia Celular/efectos de los fármacos , Quitosano/química , Preparaciones de Acción Retardada/administración & dosificación , Preparaciones de Acción Retardada/química , Dinoprostona/metabolismo , Portadores de Fármacos/química , Liberación de Fármacos , Células HT29 , Humanos , Interleucina-8/metabolismo , Mesalamina/química , Nanopartículas/química , Óxido Nítrico/metabolismo , SolubilidadRESUMEN
This study aims to design a novel nano-sized anticancer drug delivery system that can enhance the therapeutic effects of the loaded drug. With this idea in mind, this work reported the design and characterization of epigallocatechin-3-gallate (EGCG) functionalized chitin (CH) derivative, and its application in nano-drug delivery system. The EGCG-functionalized CH (CE) polymer was firstly prepared and characterized. The nanoparticles (NPs) of CE-loaded honokiol (HK), which was prepared by ionic crosslinking, exhibited a size of 80â¯nm, zeta potential of +33.8â¯mV, and spherical morphology. The antitumor activity of the CE-HK NPs in vitro and in vivo was investigated and compared to free HK. As a result, the CE-HK NPs can effectively inhibited cell proliferation of HepG2 cell by inhibiting more cells in the G2/M phase and decreasing mitochondrial membrane potential. The CE-HK NPs (40â¯mg/kg) inhibited tumor growth by 83.55% (pâ¯<â¯0.05), which was far higher than the 30.15% inhibition of free HK (40â¯mg/kg). The proposed delivery system exhibits better tumor selectivity and growth reduction both in vitro and in vivo, and does not induce any side effects. Therefore, the CE-HK NPs may act as an effective delivery system of liver cancer agent HK.
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Antineoplásicos Fitogénicos/administración & dosificación , Compuestos de Bifenilo/administración & dosificación , Carcinoma Hepatocelular/tratamiento farmacológico , Catequina/análogos & derivados , Quitina/química , Portadores de Fármacos , Lignanos/administración & dosificación , Neoplasias Hepáticas/tratamiento farmacológico , Nanopartículas , Animales , Antineoplásicos Fitogénicos/química , Apoptosis/efectos de los fármacos , Compuestos de Bifenilo/química , Carcinoma Hepatocelular/patología , Catequina/administración & dosificación , Catequina/química , Proliferación Celular/efectos de los fármacos , Reactivos de Enlaces Cruzados/química , Relación Dosis-Respuesta a Droga , Composición de Medicamentos , Liberación de Fármacos , Puntos de Control de la Fase G2 del Ciclo Celular/efectos de los fármacos , Células Hep G2 , Humanos , Cinética , Lignanos/química , Neoplasias Hepáticas/patología , Masculino , Potencial de la Membrana Mitocondrial/efectos de los fármacos , Ratones Endogámicos BALB C , Nanotecnología , Tamaño de la Partícula , Solubilidad , Propiedades de Superficie , Tecnología Farmacéutica/métodos , Carga Tumoral/efectos de los fármacos , Ensayos Antitumor por Modelo de XenoinjertoRESUMEN
This work aims to explore the inclusion mechanism and structure of cinnamaldehyde (CNMA) and cyclodextrins (CDs), and to provide some theoretical information for the application of CNMA and its inclusion. In this study, we prepared three kinds of inclusion and investigated the mechanism and structure by theory and experiment. Molecular docking and dynamical simulations presented a stable 1:1 inclusion complex and the visual structure model. The structural features indicated that the benzene ring of CNMA was enclosed in the hydrophobic cavity of CDs, which were consistent with the results of 1H NMR, 2D-ROESY, Fourier transform infrared spectroscopy. The inclusion mechanism studies showed that the inclusion process was driven mainly by enthalpy with the binding constant following the order of DM (dimethyl)â¯>â¯HP (hydroxypropyl)â¯>â¯ß-CD. Moreover, the inclusion complex showed an advantageous water solubility and dissolution rate compared with CNMA.
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Tertiary butylhydroquinone (TBHQ) is a water-insoluble antioxidant. In this study, three cyclodextrin inclusion complexes were prepared to improve the water solubility of TBHQ and expand its range of application. Analysis of phase solubility indicated that TBHQ can form 1:1 inclusion complex with hydroxypropyl-beta-cyclodextrin (HP-ß-CD) and dimethyl-beta-cyclodextrin (DM-ß-CD) and 1:2 inclusion complex with beta-cyclodextrin (ß-CD). The possible inclusion configuration between TBHQ and CDs was determined through FT-IR, PXRD, DSC, NMR, and SEM analyses. Results were validated by theoretical study of AutoDock molecular docking. The scavenging effects of the inclusion complexes were not effective on DPPH radical but higher on hydroxyl, superoxide and ABTS+ radicals than that of TBHQ monomer. Moreover, the water solubility of TBHQ increased after complexation with HP-ß-CD and DM-ß-CD. The stability of TBHQ is related to the type of storage materials used, and the stability can be improved by complexation with CDs.
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Antioxidantes/química , Antioxidantes/farmacología , Hidroquinonas/química , beta-Ciclodextrinas/química , 2-Hidroxipropil-beta-Ciclodextrina/química , Compuestos de Bifenilo/química , Línea Celular , Humanos , Espectroscopía de Resonancia Magnética , Microscopía Electrónica de Rastreo , Simulación del Acoplamiento Molecular , Picratos/química , Solubilidad , Soluciones , Espectroscopía Infrarroja por Transformada de Fourier , Agua/química , Difracción de Rayos XRESUMEN
This study prepared and investigated the inclusion complexes of propyl gallate (PG) with beta-cyclodextrin (ß-CD) and its water-soluble derivatives dimethyl-beta-cyclodextrin (DM-ß-CD), hydroxypropyl-beta-cyclodextrin (HP-ß-CD), and sulfobutylether-beta-cyclodextrin (SBE-ß-CD). Phase solubility studies indicated that the formed complexes were in 1:1 stoichiometry. FT-IR, PXRD, DSC, 1H-NMR, ROESY-NMR, and SEM analysis results confirmed the formation of the complexes. The NMR results indicated that the aromatic ring of PG was embedded into the CD cavity. The aqueous solubility of PG was markedly improved, and that of the PG/DM-ß-CD complex increased by 365.3 times. In addition, the results of the antioxidant activity assay showed that the hydroxyl radical and superoxide radical scavenging capacities of the complexes increased by 3-11 times and 1-6.5 times, respectively, compared with those of PG under the same concentration. Therefore, CD/PG inclusion complexes with improved solubility and radical scavenging capacity can be used as water-soluble antioxidants in the food industry.