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.     

Use of climate scenarios to aid in decision analysis for interannual water supply planning

This work addresses the issue of climate change in the context of water resource planning on the time scale of a few years. Planning on this time scale generally ignores the role of climate change. However, where the climate of a region has already shifted, the use of historical data for planning purposes may be misleading. In order to test this, a case study is conducted for a region, the Australian Capital Territory, where long term drought is raising concerns of a possible climate shift. The issue is cast in terms of a particular planning decision; the option to augment water supply in the next few years to hedge against the drought persisting. A set of climate scenarios are constructed for the region corresponding to the historical climate regime and to regimes where progressively greater levels of change are assumed to have already taken place (5%, 10%, 20% reductions in mean rainfall). Probabilities of the drought persisting are calculated for each of the scenarios. The results show substantial increases in the probability of the drought persisting for even moderate reductions in mean rainfall. The sensitivity of the decision to augment supply to the scenario results depends ultimately on the planners tolerable thresholds for the probability of the drought persisting. The use of different scenarios enables planners to explore the sensitivity of the decision in terms of their risk tolerance to ongoing drought and to their degree of belief in each of the scenarios tested.     

Bacteroides fragilis enterotoxin cleaves the zonula adherens protein, E-cadherin

Strains of Bacteroides fragilis associated with diarrheal disease (enterotoxigenic B. fragilis) produce a 20-kDa zinc-dependent metalloprotease toxin (B. fragilis enterotoxin; BFT) that reversibly stimulates chloride secretion and alters tight junctional function in polarized intestinal epithelial cells. BFT alters cellular morphology and physiology most potently and rapidly when placed on the basolateral membrane of epithelial cells, suggesting that the cellular substrate for BFT may be present on this membrane. Herein, we demonstrate that BFT specifically cleaves within 1 min the extracellular domain of the zonula adherens protein, E-cadherin. Cleavage of E-cadherin by BFT is ATP-independent and essential to the morphologic and physiologic activity of BFT. However, the morphologic changes occurring in response to BFT are dependent on target-cell ATP. E-cadherin is shown here to be a cellular substrate for a bacterial toxin and represents the identification of a mechanism of action, cell-surface proteolytic activity, for a bacterial toxin.     

Carbon segregation and inclusions effects on surface fracture morphology of a 12% chromium stainless steel

Martensitic 12% chromium stainless steel is generally used for the manufacture of water vapour turbine blades. This material, under these environmental conditions, develops fatigue corrosion with failure as a result of the segregation of certain constituent elements such as phosphorus (P) and sulphur (S),^[1–3] or the presence of some types of inclusions.^[2–4] To be able to understand and explain these phenomena, in situ characterization of the fractured surfaces were performed for two types of samples: steel 1 as manufactured turbine material whose fracture mode is intergranular and steel 2 issued from last stage turbine blades after 100 000 h service at 40 °C whose fracture mode is transgranular. The techniques used for characterization were scanning electron microscopy (SEM) coupled with the x-ray analysis by energy dispersive spectroscopy (EDS), and auger electron spectroscopy (AES). The Auger results enabled the understanding of the brittle to ductile transition for the material by showing the simultaneous diffusion of carbon from grain boundaries (GB) to grains (G) and chromium from G to GB. Furthermore, the heavy segregation of phosphorus at the GBs could explain the intergranular crack rupture traces observed in steel 2. SEM observations coupled with EDS analysis showed the presence of different types of non-metallic inclusions such as silicon-based complex inclusions and manganese sulfides (MnS). The presence of silicon-based complex inclusions at GB could explain the intergranular fracture mode previously reported. The characterization of the fracture appearance suggests also that MnS inclusions can act as nucleation sites for secondary microcracks at the GB level that were observed after service.     

Buoyancy effects on gaseous slip flow in a vertical rectangular microchannel

Consideration is given to the buoyancy effects on the fully developed gaseous slip flow in a vertical rectangular microduct. Two different cases of the thermal boundary conditions are considered, namely uniform temperature at two facing duct walls with different temperatures and adiabatic other walls (case A) and uniform heat flux at two walls and uniform temperature at other walls (case B). The rarefaction effects are treated using the first-order slip boundary conditions. By means of finite Fourier transform method, analytical solutions are obtained for the velocity and temperature distributions as well as the Poiseuille number. Furthermore, the threshold value of the mixed convection parameter to start the flow reversal is evaluated. The results show that the Poiseuille number of case A is an increasing function of the mixed convection parameter and a decreasing function of the channel aspect ratio, whereas its functionality on the Knudsen number is not monotonic. For case B, the Poiseuille number is decreased by increasing each of the mixed convection parameter, the Knudsen number, and the channel aspect ratio.     

Supervised collaboration for syntactic annotation of Quranic Arabic

The Quranic Arabic Corpus (http://corpus.quran.com) is a collaboratively constructed linguistic resource initiated at the University of Leeds, with multiple layers of annotation including part-of-speech tagging, morphological segmentation (Dukes and Habash 2010) and syntactic analysis using dependency grammar (Dukes and Buckwalter 2010). The motivation behind this work is to produce a resource that enables further analysis of the Quran, the 1,400 year-old central religious text of Islam. This project contrasts with other Arabic treebanks by providing a deep linguistic model based on the historical traditional grammar known as i′rāb (?????). By adapting this well-known canon of Quranic grammar into a familiar tagset, it is possible to encourage online annotation by Arabic linguists and Quranic experts. This article presents a new approach to linguistic annotation of an Arabic corpus: online supervised collaboration using a multi-stage approach. The different stages include automatic rule-based tagging, initial manual verification, and online supervised collaborative proofreading. A popular website attracting thousands of visitors per day, the Quranic Arabic Corpus has approximately 100 unpaid volunteer annotators each suggesting corrections to existing linguistic tagging. To ensure a high-quality resource, a small number of expert annotators are promoted to a supervisory role, allowing them to review or veto suggestions made by other collaborators. The Quran also benefits from a large body of existing historical grammatical analysis, which may be leveraged during this review. In this paper we evaluate and report on the effectiveness of the chosen annotation methodology. We also discuss the unique challenges of annotating Quranic Arabic online and describe the custom linguistic software used to aid collaborative annotation.     

Bending-stretching analysis of thick functionally graded micro-plates using higher-order shear and normal deformable plate theory

In the present article, higher-order shear and normal deformable plate theory together with modified couple stress theory are developed to study the bending analysis of thick functionally graded rectangular micro-plates. One material length scale parameter is used for capturing the size effects. Utilizing the variational approach and also a principle of virtual displacement, a new form of equilibrium equations and the corresponding boundary conditions are derived. It is assumed that material properties vary through the thickness according to the power law function. Finally, an analytical solution for the bending problem of a simply supported FG rectangular micro-plate is presented.     

Minimizing the total completion time in a two-machine flowshop problem with time delays

This article proposes to solve the problem of minimizing the total completion time in a two-machine permutation flowshop environment in which time delays between the machines are considered. For this purpose, an enumeration algorithm based on the branch-and-bound framework is developed, which includes new lower and upper bounds as well as dominance rules. The computational study shows that problems with up to 40 jobs can be solved in a reasonable amount of time.     

Symbolic abstraction and deadlock-freeness verification of inter-enterprise processes

The design of complex inter-enterprise business processes (IEBP) is generally performed in a modular way. Each process is designed separately and then the whole IEBP is obtained by composition. Even if such a modular approach is intuitive and facilitates the design problem, it poses the problem that correct behavior of each business process of the IEBP taken alone does not guarantee a correct behavior of the composed IEBP (i.e. properties are not preserved by composition). Proving correctness of the (unknown) composed process is strongly related to the model checking problem of a system model. Among others, the symbolic observation graph based approach has proven to be very helpful for efficient model checking in general. Since it is heavily based on abstraction techniques and thus hides detailed information about system components that are not relevant for the correctness decision, it is promising to transfer this concept to the problem raised in this paper: How can the symbolic observation graph technique be adapted and employed for process composition? Answering this question is the aim of this paper.