In Silico Study,Physicochemical, and In Vitro Lipase Inhibitory Activity of α,β-Amyrenone Inclusion Complexes with Cyclodextrins

α,β-amyrenone (ABAME) is a triterpene derivative with many biological activities; however, its potential pharmacological use is hindered by its low solubility in water. In this context, the present work aimed to develop inclusion complexes (ICs) of ABAME with γ- and β-cyclodextrins (CD), which were systematically characterized through molecular modeling studies as well as FTIR, XRD, DSC, TGA, and SEM analyses. In vitro analyses of lipase activity were performed to evaluate possible anti-obesity properties. Molecular modeling studies indicated that the CD:ABAME ICs prepared at a 2:1 molar ratio would be more stable to the complexation process than those prepared at a 1:1 molar ratio. The physicochemical characterization showed strong evidence that corroborates with the in silico results, and the formation of ICs with CD was capable of inducing changes in ABAME physicochemical properties. ICs was shown to be a stronger inhibitor of lipase activity than Orlistat and to potentiate the inhibitory effects of ABAME on porcine pancreatic enzymes. In conclusion, a new pharmaceutical preparation with potentially improved physicochemical characteristics and inhibitory activity toward lipases was developed in this study, which could prove to be a promising ingredient for future formulations.     

Naloxone and baclofen attenuate ethanol's locomotor-activating effects in preweanling Sprague-Dawley rats.

Heterogeneous rat strains appear to be particularly sensitive to the sedative effects of ethanol as adults and insensitive to ethanol's stimulant effects. Recently, the authors found that ethanol induces stimulant effects in preweanling Sprague-Dawley rats. In adult mice, these effects seem to be governed by the mesocorticolimbic dopaminergic pathway, which can be modulated by means of GABA B agonist (baclofen) or opioid antagonist (naloxone) treatments. This study tested whether these pharmacological treatments might reduce the activating effect of ethanol in preweanling Sprague-Dawley rats. Twelve-day-old pups given naloxone (Experiment 1A) or baclofen (Experiment 1B) before ethanol administration were tested in terms of locomotor activity in a novel environment. Naloxone and baclofen significantly reduced the stimulating effect of ethanol but had no effect on locomotor activity patterns in water-treated controls. Blood ethanol levels were not affected by naloxone or baclofen (Experiment 2). During the preweanling period, opioid and GABA B receptors seem to be involved in the stimulating effect of ethanol. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Hot carrier-induced degradation of gate overlapped lightly dopeddrain (GOLDD) polysilicon TFTs

Hot-carrier injection is known to produce interface states and oxide trapped charge, which, depending upon their spatial distribution, can strongly influence the local electric fields as well as the current flow. In this work, we analyze the hot carrier-induced degradation of gate overlapped lightly doped drain (GOLDD) polysilicon thin film transistors (TFTs) and a new model, which correlates the interface state generation with the hot carrier injection current, is proposed. The defect generation rate has been assumed to depend upon the product of hot electron and hole currents J_eh, and the resulting interface state distribution has been evaluated self-consistently with the current density and carrier concentration distributions. By successive iterations, a complete spatial and time evolution of the interface state distribution has been determined, and the electrical characteristics, calculated with these interface state distributions are in good agreement with the experimental data     

Bio-hydrogen production during acidogenic fermentation in a multistage stirred tank reactor

The objective of this study was to evaluate the production of hydrogen in a two-stage CSTR system – both reactors having the same volume – and compare its performance with a conventional one-stage process. The lab-scale two-stage and one-stage systems were operated at five pHs and five hydraulic retention time (HRTs). The maximum volumetric hydrogen productivity and yield obtained with the two-stage system were 5.8 mmol L⁻¹ h⁻¹ and 2.7 mol H₂ mol glucose⁻¹, respectively, at an HRT of 12 h and pH 5.5. Overall, the two-stage system showed, at steady state, a better performance that the one-stage system for all the evaluated pHs. However, a comparison between the one-stage system, operating at 6 h of HRT, and the first reactor of the two-stage system at the same HRT did not show any significant difference, highlighting the positive impact of having a two-stage process. The determination of the ratio between the experimental measured H₂ in the gas phase and the theoretical H₂ generated in the liquid phase (discrepancy factor) indicated that an important part of the hydrogen produced in the first reactor was transferred into the second reactor instead of being desorbed in the headspace. Therefore, the improving of hydrogen production in the two-stage system is rather attributed to the increased transfer of hydrogen from liquid to gas than an actual total hydrogen production increase.     

Influence of Alkaline Additives and Buffers on Mineral Trapping of CO2 under Mild Conditions

Carbon dioxide (CO₂) gas is the main contributor to climate change. CO₂ storage in underground brines and oil‐field brines by mineral trapping has been considered as a promising alternative in order to reduce CO₂ emissions. However, permanent storage of CO₂ in stable carbonate minerals is greatly dependent on brine pH, being favored over an alkaline pH. The effect of alkaline additives (NaOH, KOH, CaO) and buffer solutions (NaHCO₃/NaOH, Na₂HPO₄/NaOH, NH₄Cl/NH₄OH) on the mineral trapping of CO₂ under mild conditions using a synthetic brine is investigated. The results indicate that both NaOH+NH₄Cl/NH₄OH and KOH+NH₄Cl/NH₄OH mixtures promote precipitation mainly of calcium carbonate (CaCO₃).     

The Challenge of Diagnosing Constitutional Mismatch Repair Deficiency Syndrome in Brain Malignancies from Young Individuals

Biallelic germline mismatch repair (MMR) gene (MLH1, MSH2, MSH6, and PMS2) mutations are an extremely rare event that causes constitutional mismatch repair deficiency (CMMRD) syndrome. CMMRD is underdiagnosed and often debuts with pediatric malignant brain tumors. A high degree of clinical awareness of the CMMRD phenotype is needed to identify new cases. Immunohistochemical (IHC) assessment of MMR protein expression and analysis of microsatellite instability (MSI) are the first tools with which to initiate the study of this syndrome in solid malignancies. MMR IHC shows a hallmark pattern with absence of staining in both neoplastic and non-neoplastic cells for the biallelic mutated gene. However, MSI often fails in brain malignancies. The aim of this report is to draw attention to the peculiar IHC profile that characterizes CMMRD syndrome and to review the difficulties in reaching an accurate diagnosis by describing the case of two siblings with biallelic MSH6 germline mutations and brain tumors. Given the difficulties involved in early diagnosis of CMMRD we propose the use of the IHC of MMR proteins in all malignant brain tumors diagnosed in individuals younger than 25 years-old to facilitate the diagnosis of CMMRD and to select those neoplasms that will benefit from immunotherapy treatment.     

A new procedure for evaluating crack arrest in reactor vessels

This paper presents a fracture mechanics evaluation of a reactor vessel nearing the end of its life. The analysis procedure used is based on a new method for calculating K_I at crack arrest, and was developed from crack arrest experiments performed by Combustion Engineering for EPRI. The method, already used to analyze data from large specimen crack arrest tests', demonstrates that cracks initiated during severe pressurized thermal shock (PTS) conditions will propagate very much shorter distances than previous methods indicated.     

Negative gate bias instability in polycrystalline silicon TFT's

Degradation of the device characteristics of poly-Si TFT's are seen following negative gate bias stress at elevated temperatures. The degradation has two components, One component is the trapping of holes in the gate oxide; this is a similar phenomenon to the so called `negative bias instability' seen in mono-Si MOSFETs. The other component is state formation and removal in the poly-Si bulk, or at the poly-Si-SiO₂ interface, and this is similar to that seen in αSi:H TFT's. The states formed are not the same as those produced by hot carrier stressing     

Advances in fetal echocardiography

Fetal echocardiography is the primary modality for defining and evaluating fetal cardiac status and requires detailed analysis of the cardiac anatomy from numerous views and Doppler interrogation of the intracardiac structures, great vessels, and umbilical artery. Referrals for fetal echocardiography are determined by fetal, maternal, or familial risk factors; however, approximately 50% of neonates diagnosed with a congenital cardiac defect have no risk factor, and most have undergone an obstetrical ultrasound during the pregnancy that did not detect a cardiac defect. Advances in transducer technology have resulted in the development of small high-frequency transvaginal probes that allow fetal cardiac interrogation earlier during gestation. On the horizon is 3-dimensional fetal echocardiography, which provides rapid image acquisition and tremendous computer image reconstruction ability. At present, the computer image data analysis process is lengthy, and several technical limitations must be overcome before 3-dimensional fetal echocardiography becomes the primary modality of fetal cardiac imaging. New Doppler Tissue Imaging using color Doppler energy mapping allows more precise anatomic definition of the fetal endocardium, facilitating diagnosis of small ventricular septal defects. These new advances, along with improved image resolution, provide obstetricians and pediatric cardiologists with more tools and techniques for earlier and more precise detection of fetuses with cardiac defects.