Carbonic anhydrase inhibitors: design of membrane-impermeant copper(II) complexes of DTPA-, DOTA-, and TETA-tailed sulfonamides targeting the tumor-associated transmembrane isoform IX

The synthesis and carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of two series of aromatic sulfonamides and their Cu(II) derivatives, incorporating metal-complexing moieties of the DTPA, DOTA, and TETA type are reported. The new compounds were designed in such a way as to possess high affinity for Cu(II) ions, exploiting four pendant carboxylate moieties in the DTPA derivatives, as well as the cyclen/cyclam macrocyles, and three pendant acetate moieties in the DOTA and TETA derivatives. The new derivatives showed modest inhibition of the cytosolic isoform CA I (K(I) values in the range of 66-2130 nM), were better CA II inhibitors (K(I) values in the range of 21-360 nM), and excellent inhibitors of the tumor-associated isoform CA IX (K(I) values in the range of 4.1-110 nM), with selectivity ratios for the inhibition of the tumor (CA IX) over the cytosolic (CA II) isozyme in the range of 10.74-20.88 for the best derivatives. Copper complexes were more inhibitory than the corresponding ligand sulfonamides, and showed membrane impermeability, thus, having the possibility to specifically target the transmembrane CA IX that has an extracellular active site. Incorporation of radioactive copper isotopes in this type of CA inhibitor may lead to interesting diagnostic/therapeutic applications for such compounds.     

Nanomaterials for Antiangiogenic Therapies for Cancer: A Promising Tool for Personalized Medicine

Angiogenesis is one of the hallmarks of cancer. Several studies have shown that vascular endothelium growth factor (VEGF) plays a leading role in angiogenesis progression. Antiangiogenic medication has gained substantial recognition and is commonly administered in many forms of human cancer, leading to a rising interest in cancer therapy. However, this treatment method can lead to a deteriorating outcome of resistance, invasion, distant metastasis, and overall survival relative to its cytotoxicity. Furthermore, there are significant obstacles in tracking the efficacy of antiangiogenic treatments by incorporating positive biomarkers into clinical settings. These shortcomings underline the essential need to identify additional angiogenic inhibitors that target numerous angiogenic factors or to develop a new method for drug delivery of current inhibitors. The great benefits of nanoparticles are their potential, based on their specific properties, to be effective mechanisms that concentrate on the biological system and control various important functions. Among various therapeutic approaches, nanotechnology has emerged as a new strategy for treating different cancer types. This article attempts to demonstrate the huge potential for targeted nanoparticles and their molecular imaging applications. Notably, several nanoparticles have been developed and engineered to demonstrate antiangiogenic features. This nanomedicine could effectively treat a number of cancers using antiangiogenic therapies as an alternative approach. We also discuss the latest antiangiogenic and nanotherapeutic strategies and highlight tumor vessels and their microenvironments.     

UV-shielding by a polyurethane/f-Oil fly ash-CeO2 protective coating

A waste material called oil fly ash (OFA) was acid-functionalized, yielding f-OFA-COOH, which was then reacted with cerium oxide (CeO₂) to make CeO₂-functionalized OFA, or f-OFA-CeO₂. Pristine OFA and f-OFA-CeO₂ were used to make waterborne polyurethane (WBPU) dispersions, referred to as WBPU/OFA and WBPU/f-OFA-CeO₂, respectively, with defined OFA and f-OFA-CeO₂ content. All the dispersions were applied to mild steel as organic coatings to evaluate their protective properties, such as their hydrophobicity, adhesive strength and UV-shielding resistance. These protective properties varied based on the OFA and f-OFA-CeO₂ content. The highest water contact angle, minimum water swelling and maximum adhesive strength were found using WBPU/f-OFA-CeO₂-20 coating (using 2.00 wt% f-OFA-CeO₂), which also showed the maximum ultraviolet (UV) absorption via UV–vis spectroscopy analysis. This UV shielding result also matched field test results, as that coating was found to exhibit the lowest UV degradation near a marine atmosphere, as shown by X-ray photoelectron spectroscopy (XPS) analysis. The least affected hydrophobicity was also recorded for the sample with the WBPU/f-OFA-CeO₂-20 coating.     

Deep penetration analysis with dynamic cylindrical cavitation fields

Dynamic cylindrical cavitation fields are studied for a family of plastic orthotropic solids with arbitrary strain hardening response. Analysis is within the framework of plane-strain, steady state flow theory of associated plasticity. New formulae for cavitation pressure are validated against accurate numerical analysis and contact is made with existing studies. A uniform procedure is presented for estimating penetration depth of rigid axisymmetric projectiles at normal impact. Comparison with available experimental data reveals a very good agreement for both spherical and cylindrical dynamic cavitation models. Quasi-static cavitation pressure formulae can predict penetration depth with an appropriate scaling of the yield stress. The scaling factors appear to be independent of material properties but reflect the shape of head profile.     

Diagnostic value of tissue polypeptide-specific antigen (TPS) in neuroblastoma and Wilms' tumour

Although tissue polypeptide-specific antigen (TPS) has been described as a potentially useful serum marker of tumour activity in adult epithelial tumours, few data are available for childhood malignancies. Neuroblastomas and Wilms' tumours are the commonest types of solid malignancies found in the retroperitoneum of children. At this time, a widely used marker for Wilms' tumour is not available. Using an enzyme-linked immunosorbent assay (ELISA) kit, serum TPS levels in 23 children with neuroblastomas, nine with Wilms' tumours and 22 with benign tumours were evaluated to test the usefulness of the marker in identifying malignancies. Compared with healthy children (n = 110), the preoperative least-square means (LSM) of serum TPS were considerably elevated in both neuroblastoma (LSM = 209 U l(-1)) and Wilms' tumour (LSM = 235 U l(-1)), whereas values in benign tumours were only slightly elevated. Although the Wilms' tumours were associated with higher preoperative serum TPS levels, there was no statistically significant difference compared with neuroblastomas. Receiver operating characteristic analysis (ROC curves) showed a high sensitivity and specificity for both malignancies. Successful treatment resulted in decrease in TPS serum values. Serum TPS measurements in children presenting with abdominal masses can help in diagnosing the two commonest extracranial solid malignancies of childhood. Furthermore, TPS could acquire a pivotal role in monitoring therapy.     

Co-Channel Interference of Spread Spectrum Systems in a Multiple User Environment

This paper considers the mutual interference problem of several users employing the same spread spectrum technique in selected multiple user environments. The spread spectrum techniques consist of pseudo noise (PN), time division multiple access/PN, synchronous and asynchronous frequency hopping (FH). The environment consists of a desired transmitter-receiver pair located in an area where there areMinterfering users distributed in accordance with a specified probability density function. Both coherent phase-shift-keyed-and noncoherent frequency-shift-keyed modulations are considered. The general relationship between the probability of bit error of PN and FH systems is derived which is independent of the signal modulation and distribution of users. The degradation of the communication system performance (average probability of bit error) of the desired link as a function of the total number of interfering users within the considered area is investigated. The analysis shows that the mutual interference problem is less severe with users employing synchronous FH than with the other spread spectrum techniques. The comparison between asynchronous FH and PN is highly dependent on the relative location of interferers to the desired link and the time duty factor of the hopping.     

Investigation of microstructure and wear behaviors of al matrix composites reinforced by carbon nanotube

In this study, the effect of CNT amount in Al-CNT composites produced by adding carbon nanotube (CNT) to 7075 Al alloy in various amounts on microstructure and wear behaviors of aluminum matrix composites was investigated. CNT was added to 7075 Al alloy powder at five different amounts. The powders were mechanically milled for 2 hours. Mechanical milled powders were cold pressed and then pre-shaped by hot pressing. Pre-shaped samples were sintered for 1 hour under 10^?6 millibar in 580°C. Microstructure examinations, hardness measurements, and wear tests were carried out. The results show that CNT's in the microstructure were agglomerated as nanotube amount increases and there was no uniform distribution. The highest hardness value was obtained in AMC reinforced with 1% CNT while it is seen that hardness of the composite decreases and weight loss increases as CNT amount increases.     

An Optimal Algorithm for Resource Allocation in D2D Communication

The number of mobile devices accessing wireless networks is skyrocketing due to the rapid advancement of sensors and wireless communication technology. In the upcoming years, it is anticipated that mobile data traffic would rise even more. The development of a new cellular network paradigm is being driven by the Internet of Things, smart homes, and more sophisticated applications with greater data rates and latency requirements. Resources are being used up quickly due to the steady growth of smartphone devices and multimedia apps. Computation offloading to either several distant clouds or close mobile devices has consistently improved the performance of mobile devices. The computation latency can also be decreased by offloading computing duties to edge servers with a specific level of computing power. Device-to-device (D2D) collaboration can assist in processing small-scale activities that are time-sensitive in order to further reduce task delays. The task offloading performance is drastically reduced due to the variation of different performance capabilities of edge nodes. Therefore, this paper addressed this problem and proposed a new method for D2D communication. In this method, the time delay is reduced by enabling the edge nodes to exchange data samples. Simulation results show that the proposed algorithm has better performance than traditional algorithm.