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BACKGROUND AND AIMS: Pancreas divisum (PD) is a congenital malformation of the pancreas and is implicated as a cause of pancreatitis. The role of endotherapy has been variable in symptomatic PD indicated by recurrent acute pancreatitis (RAP), chronic pancreatitis (CP), or chronic pancreatic-type abdominal pain (PP). The aim of this study was to analyze the pooled data to determine the success of endoscopic intervention for pancreas divisum. METHODS: We conducted a comprehensive search of several databases (inception to July 2023) to identify studies reporting on the use of endoscopic therapy in symptomatic pancreatic divisum. The random-effects model was used to calculate the pooled rates and I2% values were used to assess the heterogeneity. RESULTS: A total of 27 studies were retrieved that reported endoscopic intervention in pancreatic divisum. The calculated pooled rate of technical success was 92% (95% CI: 87-95; I2=63%). The calculated pooled rate of clinical success was 65% (95% CI: 60-70; I2=60%). The rate of clinical success by PD subtypes was highest in RAP at 71% (95% CI: 65-76; I2=24%). Available studies had significant heterogeneity in defining clinical success. The rate of adverse events was 71% (95% CI: 65-76; I2=24%). CONCLUSIONS: The role of endoscopic therapy in pancreatic divisum is variable with the highest success rate in recurrent acute pancreatitis. Endoscopic intervention is associated with a higher-than-usual rate of adverse events, including post-ERCP pancreatitis.
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Medicinal plants have long been studied for their therapeutic benifits. The present research aims to unveil complex phytochemical profile and therapeutic properties of ethyl acetate fraction of Phlomis stewartii, an important medicinal plant. In this context, the Gas Chromatography-Mass Spectrometry (GC-MS) analysis of the fraction identified 26 compounds. Additionally, the fraction exhibited concentration dependent antioxidant activity with an IC50 value lower than the standard antioxidant butylated hydroxytoluene. The antifungal activity of the fraction examined against F. oxysporum, A. alternate, and R. solani resulted in almost complete inhibition (>90%) of fungal growth. Furthermore, the fraction exhibited significant antibacterial potential against B. subtilus, S. aureus, E. coli, and S. dysenteriae, with inhibition zones of 18±0.22, 17±0.22, 12±0.11, and 10±0.12, respectively. Briefly, the plant extract was found to be highly potent, particularly in its antifungal action. Further studies, including natural products isolation coupled with bioassays, are recommended for promising drug candidates discovery.
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Terminalia arjuna possesses significant cardioprotective, antidiabetic and antioxidant properties as these properties are described in Ayurveda. In the present study, three flavonoids were isolated through the separation and chromatographic purification of the whole plant material of T. arjuna. Spectroscopic characterization identified one of them as a new flavonoid "Terminalone A (1)" and two known flavonoids i.e., 6-hydroxy-2-(4-hydroxyphenyl)-7-methoxy-4H-chromen-4-one (2) and 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one (3). The bioactivity studies showed considerable antibacterial and antioxidant (DPPH radical scavenging) potential for all the three compounds 1-3 where the compound 1 showed strong antibacterial and antioxidant activity.
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Antioxidantes , Terminalia , Antioxidantes/química , Terminalia/química , Extratos Vegetais/química , Flavonoides/farmacologia , Antibacterianos/farmacologia , BioensaioRESUMO
Efficient and excellent nanoparticles are required for the degradation of organic dyes in photocatalysis. In this study, silver-manganese oxide nanoparticles (Ag-Mn-NPs) were synthesized through a wet chemical precipitation method and characterized as an advanced catalyst that has enhanced photocatalytic activity under sunlight irradiation. The nanoparticles were characterized using scanning electron microscopy (SEM), XRD, UV-vis light spectra, and energy-dispersive X-ray (EDX) spectroscopy, revealing their spherical and agglomerated form. The EDX spectra confirmed the composition of the nanoparticles, indicating their presence in oxide form. These bimetallic oxide nanoparticles were employed as photocatalysts for the degradation of malachite green (MG) dye under sunlight irradiation in an aqueous medium. The study investigated the effects of various parameters, such as irradiation time, catalyst dosage, recovered catalyst dosage, dye concentration, and pH, on the dye's photodegradation. The results showed that Ag-Mn oxide nanoparticles exhibited high photocatalytic activity, degrading 92% of the dye in 100 min. A longer irradiation time led to increased dye degradation. Moreover, a higher catalyst dosage resulted in a higher dye degradation percentage, with 91% degradation achieved using 0.0017 g of the photocatalyst in 60 min. Increasing the pH of the medium also enhanced the dye degradation, with 99% degradation achieved at pH 10 in 60 min. However, the photodegradation rate decreased with increasing dye concentration. The Ag-Mn oxide nanoparticles demonstrate excellent potential as a reliable visible-light-responsive photocatalyst for the efficient degradation of organic pollutants in wastewater treatment.
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INTRODUCTION: Kisspeptin is involved in the hypothalamic pituitary gonadal-axis' seasonal regulation in rodents and sheep. Studies of kisspeptin signaling in regulating the transition between breeding and nonbreeding seasons have focused on kisspeptin expression, myelin basic protein (MBP) expression around kisspeptin-ir cells, and quantifying the synaptic connections between kisspeptin and gonadotropin-releasing hormone (GnRH) neurons in various animal models; however, the role of kisspeptin in regulating the seasonal breeding of primates has not been explored yet. OBJECTIVE: This study investigated changes in kisspeptin signaling during breeding and a non-breeding season in a non-human primate model, the rhesus monkey. METHODS: Three adult male monkeys (n = 3) from the breeding season and two monkeys (n = 2) from the non-breeding season were used in this study. After measuring the testicular volume and collecting a single blood sample, all animals were humanely euthanized under controlled conditions, and their hypothalami were collected and processed. Two 20 µm thick hypothalamic sections (mediobasal hypothalamus) from each animal were processed for kisspeptin-MBP and kisspeptin-GnRH immunohistochemistry (IHC). One section from each animal was used as a primary antibody omitted control to check the nonspecific binding in each IHC. RESULTS: Compared to the non-breeding season, plasma testosterone levels and testicular volumes were significantly higher in monkeys during the breeding season. Furthermore, compared to the non-breeding season, increased kisspeptin expression and a higher number of synaptic contacts between kisspeptin fibers and GnRH cell bodies were observed in the arcuate nucleus of the breeding season monkeys. In contrast, enlarged kisspeptin soma and higher MBP expression were observed in non-breeding monkeys. CONCLUSION: Our results indicated enhanced kisspeptin signaling in primate hypothalamus during the breeding season. These findings support the idea that kisspeptin acts as a mediator for the seasonal regulation of the reproductive axis in higher primates.
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Núcleo Arqueado do Hipotálamo , Kisspeptinas , Animais , Núcleo Arqueado do Hipotálamo/metabolismo , Hormônio Liberador de Gonadotropina/metabolismo , Kisspeptinas/metabolismo , Macaca mulatta/metabolismo , Masculino , Proteína Básica da Mielina/metabolismo , Neurônios/metabolismo , Estações do Ano , Ovinos , TestosteronaRESUMO
Currently, many deep learning models are being used to classify COVID-19 and normal cases from chest X-rays. However, the available data (X-rays) for COVID-19 is limited to train a robust deep-learning model. Researchers have used data augmentation techniques to tackle this issue by increasing the numbers of samples through flipping, translation, and rotation. However, by adopting this strategy, the model compromises for the learning of high-dimensional features for a given problem. Hence, there are high chances of overfitting. In this paper, we used deep-convolutional generative adversarial networks algorithm to address this issue, which generates synthetic images for all the classes (Normal, Pneumonia, and COVID-19). To validate whether the generated images are accurate, we used the k-mean clustering technique with three clusters (Normal, Pneumonia, and COVID-19). We only selected the X-ray images classified in the correct clusters for training. In this way, we formed a synthetic dataset with three classes. The generated dataset was then fed to The EfficientNetB4 for training. The experiments achieved promising results of 95% in terms of area under the curve (AUC). To validate that our network has learned discriminated features associated with lung in the X-rays, we used the Grad-CAM technique to visualize the underlying pattern, which leads the network to its final decision.
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This work reports experimental and computational magnetic phase transition from superconducting-diamagnet to ferromagnet in lanthanum (La)-doped functionalized Nb2C MXene. Co-precipitation method is used to synthesize La-doped Nb2C MXene. Structure and morphology of the compound are studied through x-ray diffraction, scanning electron microscopy, high-resolution transmission electron microscopy and energy dispersion spectroscopy, confirming the successful doping of La while retaining the two-dimensional (2D) structure of MXene. The magnetic properties of doped sample are studied using field-cooled and zero-field-cooled curves as well as from magnetization (M) versus applied magnetic field (H) graphs. Contrary to the superconductivity-like diamagnetic behavior in pristine Nb2C MXene, the La-doped MXene converts the diamagnetism into the ferromagnetic (FM) phases at all temperatures. The ferromagnetism arises due to the pinning of magnetic spins pinned by Lanthanum itself. The computational analysis of pristine Nb2C MXene confirms its diamagnetic behavior and further clarifies the role of La and functional groups (O and F) in the reduction of diamagnetic behavior in La-doped Nb2C MXene while inducing FM nature. This work provides an interesting superconducting-diamagnetic to FM transition with a possibility of its implementation in 2D spintronics.
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Two-dimensional piezoelectric materials have attracted great attention as they could play a vital role in nano-electromagnetic systems. Herein, we investigate the compelling piezoelectric properties of Janus ZrSeO in monolayer and bulk structures using density functional theory calculations with a van der Waals correction. One of the two independent out-of-plane piezoelectric coefficients (e31) of the bulk ZrSeO is as high as 287.60 pC m-1, which is over five times larger than that of monolayer ZrSeO due to charge changes in the internal structure within each Zr, Se, and O layer. Interestingly, another large negative out-of-plane piezoelectric stress coefficient (e33) of bulk ZrSeO (-467.40 pC m-1) results from the displacement difference between the electronic and ionic center positions, which is at least three times larger than those previously reported for Janus Mo/W/Hf-based transition metal dichalcogenides. The charge transformation between atoms under strain induces negative piezoelectric stress, a process that is clarified using maximally localized Wannier functions (MLWF) and Bader charge analysis. This research also reveals the dependence of piezoelectricity in Janus MXY on the metal (M = Zr, Hf, W, Mo) and chalcogenide (X,Y = S, Se, O) components, which are directly proportional to the electronegativity and the atomic size difference.
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INTRODUCTION: Colorectal cancer is the third most common type of cancer in the world and in Pakistan it ranks at fifth position. The present study was conducted to evaluate the knowledge, attitude, preventive practices and perceived barriers to screening about colorectal cancer among university students. METHOD: A cross-sectional study was conducted after developing a self-administered questionnaire among the university students of newly merged districts of Kpk, Pakistan. RESULT: A total of 302 students (232 male and 70 female) participated in the study. The knowledge score of the participants regarding the risk factors and warning signs of colorectal cancer was 59.9% and 40%. More than 90% of the participants were of the view that colorectal cancer diagnosis at initial stages can improve treatment and around 80% were in favor of undergoing regular physical examination to avoid colorectal cancer. Only 37.7% of the participants had intentionally collected information about colorectal cancer. The percentage of participants who intentionally participated in educational activities related to colorectal cancer was 33.1%. Furthermore, only 24.4% of the participant had ever taken part in colorectal cancer screening. The barriers toward colorectal cancer screening were fear of finding colorectal cancer and the anxiety of screening procedures. However, around 32% of the participants had no knowledge about colorectal cancer screening. CONCLUSION: In view of the findings of this study, it can be suggested that community awareness programs that are focused towards screening of colorectal cancer may be initiated in the newly merged districts of Kpk, Pakistan. The implementation of such colorectal cancer screening program can help in its early detection and can potentially lower the associated mortality and morbidity risk with this disease.
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Neoplasias Colorretais/prevenção & controle , Detecção Precoce de Câncer/estatística & dados numéricos , Conhecimentos, Atitudes e Prática em Saúde , Estudantes/estatística & dados numéricos , Universidades , Adolescente , Adulto , Ansiedade/etiologia , Neoplasias Colorretais/diagnóstico , Estudos Transversais , Detecção Precoce de Câncer/psicologia , Medo , Feminino , Humanos , Comportamento de Busca de Informação , Masculino , Paquistão , Fatores de Risco , Estudantes/psicologia , Inquéritos e Questionários , Adulto JovemRESUMO
This study aims to determine the nitrate exposure and their health assessment in spring water used for drinking in Harnai. Total 24 water samples were collected from four springs used for drinking. Three samples from starting point and three from the end point of each spring were collected. DR/890 multi-parameter portable calorimeter was used for the measurement of nitrate. The concentration of nitrate was ranged from 0.1 to 1.1 mg/l with an average of 0.389 mg/l. The results show that the concentration of nitrate in spring water is 93%, and 99% less than permissible limits recommended by Pakistan Standards & Quality Control Authority (PSQCA) and World Health Organization (WHO), respectively. The values of physiochemical parameters like potential of Hydrogen (pH), Electrical Conductivity (EC) and Total Dissolved Solid (TDS) were ranged from 7.8 to 8.3, 564 to 749 µS/cm, and 36 to 479 mg/l with average values 8.025, 630.5 µS/cm, and 403.5 mg/l, respectively. The calculated mean chronic daily intake (CDI) in three age groups was found 0.01, 0.02, and 0.03 in adults, children, and infants, respectively. Hence, it is concluded that spring water used for drinking in Harnai was considered safe and do not pose any health hazards associated with nitrate.
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Água Potável/química , Nitratos/análise , Poluentes Químicos da Água/análise , Adulto , Criança , Humanos , Lactente , Nascentes Naturais , Nitratos/toxicidade , Paquistão , Medição de Risco , Poluentes Químicos da Água/toxicidadeRESUMO
The present study was designed to assess the responsiveness of hypothalamic-pituitary-gonadal axis to kisspeptin administration with increasing age in men. Human kisspeptin-10 was administered in single iv bolus dose (1 µg/kg BW) to healthy adult, middle and advanced age men. Serial blood samples were collected for 30 min pre- and 120 min post-kisspeptin injection periods at 30-min interval. Analysis of plasma LH by ELISA showed a significant (p < 0.05) increase after kisspeptin-10 administration in all groups, whereas plasma testosterone concentration was significantly elevated (p < 0.05) after kisspeptin-10 injection only in the adult men group. Present results suggest that in men, central hypothalamic-pituitary axis remains active and shows responsiveness to kisspeptin stimulation across life. However, Leydig cell responsiveness to kisspeptin-induced LH decreases with age in men.
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Sistema Hipotálamo-Hipofisário/efeitos dos fármacos , Kisspeptinas/administração & dosagem , Hormônio Luteinizante/sangue , Testosterona/sangue , Adulto , Fatores Etários , Idoso , Voluntários Saudáveis , Humanos , Injeções Intravenosas , Masculino , Pessoa de Meia-IdadeRESUMO
Present review discuss the reported work on structures, origins and the potent biologically active natural products isolated from Genus Buddleja, which is known for having many important pharmacologically active substances. The Genus Buddleja have more than 100 species, many of them are distributed in Mediterranean and Asian regions. A very small number of common species of the Genus in majority of fruiting plants have been investigated for their biological potential. So for, isolation of about 153 or more new/novel chemical substances have been reported. Purposes of the review is to discuss the structurally established and pharmacologically significant natural substances from wide variety of different species of this genus. Traditionally, species of the genus are reported to be used for healing, treatment of liver diseases, bronchial complaints, preventing several other diseases by exhibiting diuretic properties, sedative functions, analgesic potential, antirheumatic actions, antimicrobial activities, anti hyperglycemic functions and antioxidant properties. In this review we will describe recently established medicinal chemistry aspects and complete list of phytoconstituents as well as their sources and reference.
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Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Buddleja/química , Parassimpatolíticos/farmacologia , Plantas Medicinais/química , Analgésicos/farmacologia , Animais , Anti-Infecciosos/química , Antioxidantes/química , Buddleja/metabolismo , Diuréticos/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Flavonoides/química , Flavonoides/isolamento & purificação , Humanos , Hipnóticos e Sedativos/farmacologia , Parassimpatolíticos/química , Plantas Medicinais/metabolismo , Esteroides/química , Esteroides/isolamento & purificação , Terpenos/química , Terpenos/isolamento & purificaçãoRESUMO
A Schiff base 3 has been synthesized by equimolar reaction (condensation) of sulfonamide i.e. sulfamethoxypyridazine 1 and substituted aromatic aldehyde i.e. 2-Hydroxy-1-Napthalene aldehyde 2. The synthesized Schiff base 3 and its Metal (II) complexes were characterized by its physical, analytical (CHN analysis) and spectral (UV & IR) analysis. The Staphylococcus aureus and Escherichia coli bacterial strains were used for antibacterial activity of Sulfamethoxypyridazine 1, its Schiff base 3 and its transition metal (II) complexes 4-8. All of them showed varied levels of activity.
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Antibacterianos , Complexos de Coordenação , Bases de Schiff/química , Sulfonamidas/química , Antibacterianos/síntese química , Antibacterianos/farmacologia , Complexos de Coordenação/síntese química , Complexos de Coordenação/farmacologia , Escherichia coli/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Staphylococcus aureus/efeitos dos fármacosRESUMO
Hymenolepiasis is a helminthic and occasionally fatal disease of human imposing heavy economic losses to human society. Present study was aimed to diagnose the school children for the prevalence and control of Hymenolepiasis. A school based cross-sectional analysis of stool samples collected from 188 children aged 06-15 years was carried out (February to June 2016). Two stool samples were collected from each student before diagnosing and after treatment. The samples were fixed in 10% formalin and observed under the light microscope using the methods of direct smear in Lugol's solution, normal saline and flotation techniques. On the basis of drugs accessibility all the H. nana infected children were divided in to 2- groups. Children in group A were treated with albendazole (bendazol) 400mg once orally, group B was treated with albendazole (zentel) 200mg orally. Eggs per gram of faeces were counted in each group before and after treatment. Of the 188 children, current study reveals only 6.08% (n=18/296) infection with H.nana and 10.5% (n=16/151) were diagnosed with co infections. The % efficacy of albendazole (Zentel) and albendazole (bendazol) against Hymenolepis nana infection was reported as 83% and 75% respectively. Present study was concluded that albendazole (zentel) is the drug of choice for the treatment of hymenolepiasis in children.
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Albendazol/uso terapêutico , Anticestoides/uso terapêutico , Himenolepíase/tratamento farmacológico , Administração Oral , Adolescente , Albendazol/administração & dosagem , Animais , Anticestoides/administração & dosagem , Criança , Estudos Transversais , Fezes/parasitologia , Feminino , Humanos , Himenolepíase/epidemiologia , Hymenolepis nana/efeitos dos fármacos , Óvulo/efeitos dos fármacos , Paquistão/epidemiologia , Cooperação do Paciente , Resultado do TratamentoRESUMO
BACKGROUND AND AIMS: Prophylactic endotracheal intubation (PEI) is often advocated to mitigate the risk of cardiopulmonary adverse events in patients presenting with brisk upper GI bleeding (UGIB). However, the benefit of such a measure remains controversial. Our study aimed to compare the incidence of cardiopulmonary unplanned events between critically ill patients with brisk UGIB who underwent endotracheal intubation versus those who did not. METHODS: Patients aged 18 years or older who presented at Cleveland Clinic between 2011 and 2014 with hematemesis and/or patients with melena with consequential hypovolemic shock were included. The primary outcome was a composite of several cardiopulmonary unplanned events (pneumonia, pulmonary edema, acute respiratory distress syndrome, persistent shock/hypotension after the procedure, arrhythmia, myocardial infarction, and cardiac arrest) occurring within 48 hours of the endoscopic procedure. Propensity score matching was used to match each patient 1:1 in variables that could influence the decision to intubate. These included Glasgow Blatchford Score, Charleston Comorbidity Index, and Acute Physiology and Chronic Health Evaluation scores. RESULTS: Two hundred patients were included in the final analysis. The baseline characteristics, comorbidity scores, and prognostic scores were similar between the 2 groups. The overall cardiopulmonary unplanned event rates were significantly higher in the intubated group compared with the nonintubated group (20% vs 6%, P = .008), which remained significant (P = .012) after adjusting for the presence of esophageal varices. CONCLUSIONS: PEI before an EGD for brisk UGIB in critically ill patients is associated with an increased risk of unplanned cardiopulmonary events. The benefits and risks of intubation should be carefully weighed when considering airway protection before an EGD in this group of patients.
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Endoscopia do Sistema Digestório/métodos , Hemorragia Gastrointestinal/cirurgia , Cardiopatias/epidemiologia , Intubação Intratraqueal/métodos , Pneumopatias/epidemiologia , Complicações Pós-Operatórias/epidemiologia , Cuidados Pré-Operatórios/métodos , Idoso , Arritmias Cardíacas/epidemiologia , Estudos de Casos e Controles , Estudos de Coortes , Estado Terminal , Varizes Esofágicas e Gástricas/complicações , Varizes Esofágicas e Gástricas/cirurgia , Feminino , Hemorragia Gastrointestinal/etiologia , Parada Cardíaca/epidemiologia , Hematemese , Humanos , Masculino , Melena , Pessoa de Meia-Idade , Infarto do Miocárdio/epidemiologia , Úlcera Péptica Hemorrágica/cirurgia , Pneumonia/epidemiologia , Pontuação de Propensão , Edema Pulmonar/epidemiologia , Síndrome do Desconforto Respiratório/epidemiologia , Estudos Retrospectivos , Choque Hemorrágico/epidemiologiaRESUMO
The present studies cover antibacterial activity of the crude methanolic extracts of 11 medicinal plants viz. Adhatoda vasica, Bauhenia variegate, Bombax ceiba, Carrisa opaca, Caryopteris grata, Debregeasia salicifolia, Lantana camara, Melia azedarach, Phyllanthus emblica, Pinus roxburghii and Olea ferruginea collected from lower Himalayas against two Gram positive (Staphylococcus aureus, Micrococcus luteus) and two Gram negative (Escherichia coli, Pseudomonas aureginosa) bacterial strains. The extracts were applied at four different concentrations (120 mg/mL, 90mg/mL, 60mg/mL and 30mg/mL) in dimethyl sulfoxide (DMSO) by using agar well diffusion method. Antibacterial activities against Staphylococcus aureus and Micrococcus luteus were observed formethanolic extracts of all the above mentioned plants. Greater antibacterial activity against Pseudomonas aeruginosa was only exhibited by Phyllanthus emblica, Pinus roxburghii, Debregeasia salicifolia and Lantana camara. Escherichia coli was highly resistant to all the plant extracts at all concentrations. It is inferred that methanolic crude extracts of the above mentioned plantsexhibitantibacterial activities against pathogenic bacteria, which proved the ethnobotanical importance of the selected plants that indigenous people use for cure against various diseases.
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Antibacterianos/farmacologia , Extratos Vegetais/farmacologia , Plantas Medicinais , Testes de Sensibilidade MicrobianaRESUMO
The precise manipulation of electromagnetic and thermoelectric characteristics in the miniaturization of electronic devices offers a promising foundation for practical applications in quantum computing. Double perovskites characterized by stability, non-toxicity, and spin polarization, have emerged as appealing candidates for spintronic applications. This study explores the theoretical elucidation of the influence of iridium's 5d electrons on the magnetic characteristics of Sr2AIrO6 (A = Y, Lu, Sc) with WIEN2k code. The determined formation energies confirm the thermodynamic stability while an analysis of band structure and the density of states (DOS) reveals a half-metallic ferromagnetic character. This characteristic is comprehensible through the analysis of exchange constants and exchange energies. The current analysis suggests that crystal field effects, a fundamental hybridization process and exchange energies contribute to the emergence of ferromagnetism due to electron-spin interactions. Finally, assessments of electrical and thermal conductivities, Seebeck coefficient, power factor, figure of merit and magnetic susceptibility are conducted to assess the potential of the investigated materials for the applications in thermoelectric devices.
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In this study, we applied density functional theory to compute the electronic, optical, and thermal properties of MP (M = Li, Na, K). We find that the materials under consideration are stable, owing to the lack of negative frequencies in the phonon spectra. LiP exhibits an indirect band gap of 1.43 eV. NaP and KP have direct band gaps of 1.67 and 1.76 eV, respectively. The family of these composites shows strong absorption, observed by their very sharp absorption edges and confirmed by their direct transition from the valence to conduction band. They exhibit strong absorption below 4.0 eV in the optical spectra, which could serve in a solar cell device. The thermal calculations show high zT values of 0.74, 0.78, and 0.64 at 300 K for LiP, NaP, and KP, respectively. Thus, our results could be promising for electronic and thermal devices.
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BACKGROUND: Buspirone is used for the management of depression and anxiety disorders. Due to its short half-life and low bioavailability, it requires multiple daily doses and is associated with some side effects. AIM: This study aimed to develop chitosan-based hydrogels as drug-controlled release carriers. OBJECTIVE: The objective of this study is to prepare chitosan-based hydrogels as controlled release carriers in order to overcome the side effects of buspirone HCl and improve patients' compliance and their life quality. METHODS: Polymer chitosan was polymerized with two monomers, acrylic acid and itaconic acid, to synthesize pH-sensitive hydrogel. The Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC) analysis were performed to confirm the structure formation and thermal stability. Water penetration capability and loading of the drug were performed by porosity and drug loading studies. The swelling and dissolution tests were performed to analyze the pH-sensitive nature of the developed hydrogels. RESULTS: FTIR, TGA, and DSC demonstrated that the chitosan-based hydrogels were successfully prepared. An increase in water penetration and drug loading into the hydrogel network was seen with the high incorporation of chitosan, acrylic acid, and itaconic acid. The swelling and dissolution studies revealed that prepared hydrogel offered the greatest swelling and drug release at a high pH of 7.4. The swelling and drug release from the hydrogel were affected by the concentrations of the incorporated contents. A controlled release of the drug was achieved by using chitosan-based hydrogel as a delivery carrier compared to commercial tablets of buspirone. CONCLUSION: The results showed that the developed chitosan-based hydrogel can be considered one of the most suitable drug carrier systems for the controlled delivery of buspirone.
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Buspirona , Quitosana , Preparações de Ação Retardada , Liberação Controlada de Fármacos , Hidrogéis , Quitosana/química , Hidrogéis/química , Buspirona/química , Buspirona/administração & dosagem , Buspirona/farmacocinética , Preparações de Ação Retardada/química , Preparações de Ação Retardada/administração & dosagem , Preparações de Ação Retardada/farmacocinética , Portadores de Fármacos/química , Concentração de Íons de Hidrogênio , Espectroscopia de Infravermelho com Transformada de Fourier , Ansiolíticos/administração & dosagem , Ansiolíticos/química , Ansiolíticos/farmacocinéticaRESUMO
Humans suffer from various diseases that require more specific drugs to target them. Among the different potent agents, ß-lactamases serve as good antibacterial agents; however, ß-lactamases are resistant to such antibiotics. The present study was designed to prepare efficient ß-lactamase inhibitor amides (12-15) from inexpensive, easily accessible, and bioactive precursors; Morita Baylis Hillman (MBH) adducts (5-8). The adducts (5-8) were primarily prepared by treating their respective aldehydes with the corresponding acrylate in the presence of an organic Lewis base at ambient temperature. The compounds were characterized using mass spectrometry, FTIR and NMR spectroscopy. Furthermore, in silico studies (using AutoDock Tools and AutoDock Vina programs) on the adduct and corresponding amide product revealed that all MBH adducts (5-8) and their product amides (12-15) are significant inhibitors of ß-lactamase. Additionally, among the MBH adducts, adduct 7 showed the highest binding affinity with ß-lactamase, whereas amide 15 was identified as a highly potent antibacterial based on its docking score (-8.6). In addition, the absorption, distribution, metabolism, and excretion (ADME) test of the synthesized compounds demonstrated that all compounds showed drug-likeness properties.