Dihydroartemisinin–Bile Acid Hybridization as an Effective Approach to Enhance Dihydroartemisinin Anticancer Activity

A series of hybrid compounds based on natural products—bile acids and dihydroartemisinin—were prepared by different synthetic methodologies and investigated for their in vitro biological activity against HL-60 leukemia and HepG2 hepatocellular carcinoma cell lines. Most of these hybrids presented significantly improved antiproliferative activities with respect to dihydroartemisinin and the parent bile acid. The two most potent hybrids of the series exhibited a 10.5- and 15.4-fold increase in cytotoxic activity respect to dihydroartemisinin alone in HL-60 and HepG2 cells, respectively. Strong evidence that an ursodeoxycholic acid hybrid induced apoptosis was obtained by flow cytometric analysis and western blot analysis.     

On the evaluation and improvement of Arabic WordNet coverage and usability

Built on the basis of the methods developed for Princeton WordNet and EuroWordNet, Arabic WordNet (AWN) has been an interesting project which combines WordNet structure compliance with Arabic particularities. In this paper, some AWN shortcomings related to coverage and usability are addressed. The use of AWN in question/answering (Q/A) helped us to deeply evaluate the resource from an experience-based perspective. Accordingly, an enrichment of AWN was built by semi-automatically extending its content. Indeed, existing approaches and/or resources developed for other languages were adapted and used for AWN. The experiments conducted in Arabic Q/A have shown an improvement of both AWN coverage as well as usability. Concerning coverage, a great amount of named entities extracted from YAGO were connected with corresponding AWN synsets. Also, a significant number of new verbs and nouns (including Broken Plural forms) were added. In terms of usability, thanks to the use of AWN, the performance for the AWN-based Q/A application registered an overall improvement with respect to the following three measures: accuracy (+9.27 % improvement), mean reciprocal rank (+3.6 improvement) and number of answered questions (+12.79 % improvement).     

SCIDDICA-SS3: a new version of cellular automata model for simulating fast moving landslides

Cellular Automata (CA) are discrete and parallel computational models useful for simulating dynamic systems that evolve on the basis on local interactions. Some natural events, such as some types of landslides, fall into this type of phenomena and lend themselves well to be simulated with this approach. This paper describes the latest version of the SCIDDICA CA family models, specifically developed to simulate debris-flows type landslides. The latest model of the family, named SCIDDICA-SS₃, inherits all the features of its predecessor, SCIDDICA-SS₂, with the addition of a particular strategy to manage momentum. The introduction of the latter permits a better approximation of inertial effects that characterize some rapid debris flows. First simulations attempts of real landslides with SCIDDICA-SS₃ have produced quite satisfactory results, comparable with the previous model.     

Synthesis and characterization of conjugated polymers for the obtainment of conductive patterns through laser tracing

This article describes the preparation of thin films of conjugated polymers which can enhance their specific electrical conductivity by several orders of magnitude by changing their state from insulating to conducting materials. The examined polymers, i.e., a polyacetylenic and a polythiophenic derivative, are functionalized with thioalkylic side chains and are soluble in common organic solvents from which they lead to thick homogeneous films. The films can be deposited on different substrates, either rigid or flexible, and can be easily exposed to laser radiation to make them conductive. The process is irreversible, and the final conductivity is stable over time, even in the presence of high temperatures (up to 180 °C), moisture, and air. The high stability of treated samples, easy polymer synthesis and quick and inexpensive suitably tailored laser tracing procedure make these materials very promising for applications in organic electronics and in the development of new electronic circuitry.     

J-Integral for Deep and Shallow Notches Under Torsion

J-integral has been calculated along the free-of-stress border of deep and shallow rounded notches under torsion, under the hypothesis of a linear elastic behaviour of the material. Two exact closed-form solutions have been obtained which make it explicit the influence of the notch opening angle and the notch root radius. When the notch root radius tends to zero the proposed solution matches the expression for the corresponding pointed V-notch case.     

Susceptor-assisted fast microwave sintering of TiN reinforced SiAlON composites in a single mode cavity

In the present study, 17 wt % TiN reinforced α-β SiAlON composites were sintered at low temperature by susceptor-assisted microwave heating. The effect of TiN addition on dielectrical properties of starting powders, as well as the influence of sintering temperature on phase evolution, microstructure development and mechanical properties of α/β-SiAlON-TiN composites were investigated. The obtained results showed that TiN addition increased the microwave absorbing properties which is reflected in the peak sintering temperature. Thus, the α:β ratio decreased and mechanical properties were improved, especially the fracture toughness of the composites. Furthermore, an estimate of energy consumption during microwave assisted sintering at the laboratory scale is presented. As a result, the highest values for relative density (97.1%), Vickers hardness (13.35 ± 0.47 GPa), and fracture toughness (7.52 ± 0.54 MPa m^1/2) were obtained by microwave sintering for 30 min at 1300 °C.     

Strategies to Modulate Specialized Metabolism in Mediterranean Crops: From Molecular Aspects to Field

Plant specialized metabolites (SMs) play an important role in the interaction with the environment and are part of the plant defense response. These natural products are volatile, semi-volatile and non-volatile compounds produced from common building blocks deriving from primary metabolic pathways and rapidly evolved to allow a better adaptation of plants to environmental cues. Specialized metabolites include terpenes, flavonoids, alkaloids, glucosinolates, tannins, resins, etc. that can be used as phytochemicals, food additives, flavoring agents and pharmaceutical compounds. This review will be focused on Mediterranean crop plants as a source of SMs, with a special attention on the strategies that can be used to modulate their production, including abiotic stresses, interaction with beneficial soil microorganisms and novel genetic approaches.     

A Variant in the Osteoprotegerin Gene Is Associated with Coronary Atherosclerosis in Patients with Rheumatoid Arthritis: Results from a Candidate Gene Study

Objective: Patients with rheumatoid arthritis (RA) have accelerated atherosclerosis, but there is limited information about the genetic contribution to atherosclerosis in this population. Therefore, we examined the association between selected genetic polymorphisms and coronary atherosclerosis in patients with RA. Methods: Genotypes for single-nucleotide polymorphisms (SNPs) in 152 candidate genes linked with autoimmune or cardiovascular risk were measured in 140 patients with RA. The association between the presence of coronary artery calcium (CAC) and SNP allele frequency was assessed by logistic regression with adjustment for age, sex, and race. To adjust for multiple comparisons, a false discovery rate (FDR) threshold was set at 20%. Results: Patients with RA were 54 ± 11 years old and predominantly Caucasian (89%) and female (69%). CAC was present in 70 patients (50%). A variant in rs2073618 that encodes an Asn3Lys missense substitution in the osteoprotegerin gene (OPG, TNFRSF11B) was significantly associated with the presence of CAC (OR = 4.09, p < 0.00026) and withstands FDR correction. Conclusion: Our results suggest that a polymorphism of the TNFRSF11B gene, which encodes osteoprotegerin, is associated with the presence of coronary atherosclerosis in patients with RA. Replication of this finding in independent validation cohorts will be of interest.