Synthesis of Benzophenones and in vitro Evaluation of Their Anticancer Potential in Breast and Prostate Cancer Cells

Breast and prostate cancers are frequently treated with chemotherapy. Several novel chemicals are being reported for this purpose, particularly synthetic and natural benzophenones. This work reports the synthesis of substituted 2-hydroxybenzophenones through 1,4-conjugate addition/intramolecular cycloaddition/dehydration of nitromethane on key intermediate chromones. Structures were extensively studied by means of 2D NMR spectroscopy and single-crystal XRD. Their cytotoxicity was evaluated in vitro in two breast cancer cell lines (MDA-MB-231 and T47-D) and one prostate cancer cell line (PC3). The most potent compound exhibited good cytotoxic effects against the three cancer cell lines (IC₅₀ values ranging from 12.09 to 26.49 μm ) and induced cell-cycle retardation only on prostate cancer cells, which suggested that it might exert cell-type-specific effects.     

Development of an empirical model for determining G*/sin δ in crumb rubber modified binders

This paper describes the development of an empirical model which may be used for predicting the G*/sin δ for neat and crumb rubber modified (CRM) binders. The model was developed using 36 unique CRM binder combinations, crumb rubber concentrations were varied at 5% intervals between 5% and 20%. The effects of crumb rubber particle size on model accuracy were also studied, ultimately a model was produced with the capability of predicting G*/sin δ values over a range of temperatures and crumb rubber concentrations. By definition, the upper limit of the performance grade is dependent on the G*/sin δ value; therefore, the relationship was also considered in terms of high end failure temperature.The rubber coefficient for G*/sin δ (R_cg) was identified as an important parameter in the estimation of G*/sin δ in addition to the CRM. This term is a quantitative representation of the increase typically witnessed in G*/sin δ values with the addition of CRM. Ambient ground CRM exhibited higher R_cg values than cryogenically ground particles. Additionally, 95% confidence intervals were generated for the predictive model, thus providing a range of accuracy for the model. The resulting confidence intervals were approximately ±1300 Pa, these confidence intervals were seen to capture 92.6% of the 462 data points used. Findings from this research suggest that the differences between cryogenic and ambient CRM binder are accurately described using the R_cg, furthermore binder properties may be predicted using an empirical equation.     

钢筋混凝土膜单元的简化设计和剪切强度计算

提出了在面内剪应力与正应力联合作用下膜单元破坏模式识别、设计和强度计算的简化方法。该SMCS(合成应力简化模型)的非迭代方法以修正受压理论(MCFT)的简化结果为基础。除了钢筋的作用大于"平衡"钢筋用量而被忽略,以及最大剪应力不超过断裂强度以外,这种简化使得方程与塑性理论方程相类似,断裂强度从普通和高强混凝土(100兆帕)膜试验数据中得到。以平面内剪应力和正应力为条件,对84个钢筋混凝土膜试验结果进行对比,试验剪切力强度与计算结果的比值平均为1·03,变异系数为11.3%。对于原始的修正受压理论,对应的值分别为0.99和11.1%。所提出方法的结果与ACI规范、简化的修正受压理论以及塑性理论也进行了比较,得到了满意的结果。49个试件中有45个破坏模式可以用所提出的合成应力简化模型准确计算,通过设计和承载力计算案例,对简化模型进行了验证。     

Selected 1,3-Benzodioxine-Containing Chalcones as Multipotent Oxidase and Acetylcholinesterase Inhibitors

Chalcones are considered effective templates for the development of monoamine oxidase (MAO) and cholinesterase (ChE) inhibitors. The present work describes the syntheses of selected 1,3-benzodioxine-containing chalcones ( CD3, CD8 and CD10 ), and their inhibitory activities against MAO-A, MAO-B, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). Compound CD8 most potently inhibited MAO-B with an IC₅₀ value of 0.026 μM, followed by CD10 and CD3 (1.54 and 1.68 μM, respectively). CD8 potently and non-selectively inhibited MAO-A (IC₅₀ value of 0.023 μM). On the other hand, CD10 and CD8 inhibited AChE with IC₅₀ values of 5.40 and 9.57 μM, respectively. Kinetics and reversibility experiments showed that all synthesized molecules were competitive and reversible inhibitors, and the K_i values of CD8 for MAO-A and MAO-B were 0.018 and 0.0019 μM, respectively. By in vitro and in silico analyses, all compounds were found to have high passive human gastrointestinal absorptions, blood-brain barrier permeabilities, and non-toxicities. Molecular docking simulations revealed that docking affinity of each compound for MAO-B was higher than that for MAO-A. The results indicate that CD8 is a potent non-selective MAO inhibitor, and CD10 is an effective selective MAO-B inhibitor, and both possess AChE inhibitory activity. Therefore, we suggest that CD8 and CD10 be considered potential dual-targeting inhibitors of MAO and AChE for the treatment of various neurodegenerative disorders.     

Determinants of metabolic acidosis among hemodialysis patients

Metabolic acidosis is frequently present, poorly controlled, and associated with adverse effects among hemodialysis patients. Potential determinants of metabolic acidosis include endogenous acid production, administration of alkali, neutralization of acid by buffers, dilution of serum bicarbonate by interdialytic fluid gain, and loss of bicarbonate in stool. Understanding the relative importance of these determinants may help guide efforts to manage metabolic acidosis. We used chart abstraction, patient interviews, and laboratory testing to assess variables related to acid production (protein breakdown), alkali administration (dialysis dose, missed treatments, dialysate bicarbonate concentration, oral bicarbonate supplements), acid buffering (phosphorus binders), dilution of bicarbonate (interdialytic weight gain), and loss of bicarbonate in stool (diarrhea) for 190 randomly selected patients from 44 hemodialysis facilities. We used multivariate analyses to determine which potential determinants were independently associated with predialysis serum bicarbonate levels. Of all patients, 30% had metabolic acidosis (serum bicarbonate level <22 mEq/L). On multivariate analysis, metabolic acidosis was more likely with increased protein nitrogen appearance (odds ratio [OR] 1.60 per 0.2 g/kg/day, p=0.001) and less likely with increased Kt/V (OR 0.61 per 0.20 increase in Kt/V, p<0.001) and with increased calcium carbonate use (OR 0.38 per 2 g/day, p=0.003). Key determinants of metabolic acidosis among hemodialysis patients are protein breakdown, dialysis dose, and specific phosphorus binders. Further work is needed to develop interventions to address these determinants.     

Effect of crumb rubber characteristics on crumb rubber modified (CRM) binder viscosity

Asphalt binder viscosity is of great importance during the production process of hot mix asphalt mixture as typically asphalt plants will store binders between 149 °C and 177 °C. SHRP guidelines state that asphalt binder viscosity must not exceed 3 Pa s. Therefore, given the documented increases in asphalt viscosity when modified with crumb rubber modifier (CRM) it is necessary to produce asphalt binder that fulfills the SHRP criteria while not exceeding plant mixing and storing requirements. This paper reports the results of an investigation of the importance of CRM properties on viscosity of CRM binder. Two binder sources were modified at four concentration levels using four different crumb rubber sources; the viscosities of the produced binders were evaluated by AASHTO T 316. Crumb rubber properties were evaluated by elemental analysis using a scanning electron microscope (SEM) and by determination of glass transition temperature (T_g) using a differential scanning calorimeter (DSC). In general, results indicate that processing procedure and tire type plays an important role in the determination of CRM binder viscosity.     

A shared secret-based algorithm for securing the OLSR routing protocol

The strongest feature of ad hoc networks is its capability to be rapidly deployed anywhere and anytime without relying on a pre-existing infrastructure. From there, ad hoc networks offer the advantages to be auto-organized, ubiquitous, dynamic and completely autonomous. As a counter part, securing them becomes a more difficult task, especially because of the absence of centralized entities in the network. Inevitably, the security problem presents currently a hot topic raising more and more challenges within industrials and researchers, and many interesting securing solutions were meanwhile proposed, omitting however to suit to ad hoc networks characteristics and therefore disadvantaging them. In this paper, we propose a securing scheme for the OLSR routing protocol based on the secret sharing idea. We initially expose the general characteristics and the security problems related to ad hoc routing protocols. We then address the security requirements of ad hoc routing protocols and the security requirements we focus on. Finally, we define our completely and distributed securing algorithm based on threshold cryptography. A primary main conception objective being to suit as much as possible to ad hoc networks characteristics by avoiding as much as possible assumptions contradictory with the auto-organized and dynamic nature of ad hoc networks. Simulation results depict the additional delay due to security enhancements. Results show that this delay stills suitable to OLSR routing specifications.     

Network coding for MPR-based flooding in ad hoc wireless networks under mobility conditions

We propose a novel distributed coding scheme for broadcast over mobile ad hoc networks. In this scheme, we combine MPR technique with network coding. Only multipoint relay (MPR) nodes perform coding using a rateless code. Rather than waiting for a large number of encoded packets to be received before MPR nodes could decode and resend coded packets, we design a new degree distribution that enables the nodes to start decoding even when small number of encoded packets are received. Thus, we decrease the delay introduced at the intermediate nodes. The main advantage of using a rateless code for encoding instead of using a random linear combination of the previously received packets is to reduce significantly the encoding and decoding complexities. We provide a performance evaluation using a simulation to demonstrate the efficiency of our code even under mobility condition.     

Integration of Mobile-IP and OLSR for a Universal Mobility

Trends in fourth generation (4G) wireless networks are clearly identified by the full-IP concept where all traffic (data, control, voice and video services, etc.) will be transported in IP packets. Many proposals are being made to enhance IP with the functionalities necessary to manage the mobility of nodes, so that networks can provide global seamless roaming between heterogeneous wireless and wired networks. In this paper, we focus on the management of universal mobility, including both large scale macro-mobility and local scale micro-mobility. We propose a hierachical architecture (i) extending micro-mobility management of a wireless access network to an ad-hoc access network, (ii) connecting this ad-hoc network to the Internet and (iii) integrating Mobile IP and OLSR, a routing protocol for ad-hoc networks, to manage universal mobility. This architecture is validated by an implementation based on DynamicsMobile-IP and OLSR version 7. We show how the brodcast of Mobile-IP Agent Advertisement can be optimized using OLSR MPR-flooding.