Magnetic Resonance Signal Amplification by Reversible Exchange of Selective PyFALGEA Oligopeptide Ligands Towards Epidermal Growth Factor Receptors

The biorelevant PyFALGEA oligopeptide ligand, which is selective towards the epidermal growth factor receptor (EGFR), has been successfully employed as a substrate in magnetic resonance signal amplification by reversible exchange (SABRE) experiments. It is demonstrated that PyFALGEA and the iridium catalyst IMes form a PyFALGEA:IMes molecular complex. The interaction between PyFALGEA:IMes and H₂ results in a ternary SABRE complex. Selective 1D EXSY experiments reveal that this complex is labile, which is an essential condition for successful hyperpolarization by SABRE. Polarization transfer from parahydrogen to PyFALGEA is observed leading to significant enhancement of the ¹H NMR signals of PyFALGEA. Different iridium catalysts and peptides are inspected to discuss the influence of their molecular structures on the efficiency of hyperpolarization. It is observed that PyFALGEA oligopeptide hyperpolarization is more efficient when an iridium catalyst with a sterically less demanding NHC ligand system such as IMesBn is employed. Experiments with shorter analogues of PyFALGEA, that is, PyLGEA and PyEA, show that the bulky phenylalanine from the PyFALGEA oligopeptide causes steric hindrance in the SABRE complex, which hampers hyperpolarization with IMes. Finally, a single-scan ¹H NMR SABRE experiment of PyFALGEA with IMesBn revealed a unique pattern of NMR lines in the hydride region, which can be treated as a fingerprint of this important oligopeptide.     

Cardiovascular effects of conventional sulfonylureas and glimepiride

Sulfonylureas have, in the past, been reported to have adverse cardiovascular effects. Glimepiride is a new sulfonylurea. In spite of stimulating less insulin secretion, it has, depending on the species, equal or higher blood glucose decreasing activity and according to preliminary studies less cardiovascular activity than glibenclamide. Further studies were performed to confirm the lower cardiovascular activity of glimepiride. The IC50 for inhibition of rilmakalim-activated KATP channel currents in isolated ventricular myocytes was 31.6 nM for glimepiride and 6.8 nM for glibenclamide. In endotoxin shock-rats at a dose of 1 x 2 mg/kg i.v., glibenclamide induced a significantly higher blood pressure increase than glimepiride. At two i.v. doses of 20 mg/kg 4 min apart, in normal rats, glibenclamide produced signs of ischemia in the ECG in nearly all animals, glimepiride almost none, in diabetic rats, glibenclamide produced in all animals a lethal cardiogenic shock preceeded by serious ECG changes, glimepiride only in one fifth of the animals. In open-chest dogs, on intracoronary infusion of equieffective blood glucose-lowering doses, glibenclamide, gliclazide and glimepiride all reduced coronary blood flow, increased coronary resistance, depressed the mechanical activity of the heart, enhanced myocardial O2-extraction, reduced the serum potassium level and induced a moderate endocardial ST-segment elevation, but glimepiride to a significantly less extent than glibenclamide and gliclazide. The presented data confirm that glimepiride at equivalent blood glucose decreasing doses has less cardiovascular activity than conventional sulfonylureas.     

The effect of structural features on mechanical properties of loose optical fiber poly(butylene terephthalate) tubes

Results of a study on the modifying mechanical properties of loose optical‐fiber poly(butylene terephthalate) (PBT) tubes, produced during the standard industrial extrusion process, show that heat treatment make the structure of their material to change. The study comprised measurements of mechanical strengths properties of the tubes (tensile strength, compression strength, kinking) and determination of tube material structure [by differential thermal analysis (DTA), wide angle X‐ray scattering analysis (WAXD), and scanning electron microscopy (SEM)]. Results of the study allowed observation that the annealing at 70°C for 34 h of the tubes caused the crystalline α phase to increase in the tube material from ～28.5% to ～31.5% and the structure of the existing crystallites to become more perfect. This made the values of certain mechanical properties of the tubes to increase even by as much as 30%. The tubes following such thermal treatment could be used in cables exposed to heavy‐duty operation in arduous environments, where a larger margin from the standpoint of mechanical properties is required. © 2002 Wiley Periodicals, Inc. J Appl Polym Sci 86: 2130–2134, 2002     

Modeling of systems with overflow multi-rate traffic

The article proposes an analytical method for determining occupancy distribution and blocking probability in systems which are offered overflow traffic composed of multi-service traffic streams. The described analytical model enables determination of parameters of traffic overflowed from primary groups in hierarchically constructed telecommunication networks. The proposed method is based on an appropriate modification of the Kaufman-Roberts recursion for the full-availability group with multi-rate traffic and uses the modified Fredericks & Hayward’s approximation. Additionally, an approximate method for dimensioning systems with multi-service overflow traffic is also presented. The analytical results of the blocking probability and the results obtained in the dimensioning processes calculated using the presented methodology are compared with the data obtained from the system simulation process.     

Influence of the amount of ferromagnetic addition on the rheological properties of spinning solutions,the structure,the strength,and thermal properties of polyacrylonitrile fibres

The rheological properties of spinning solutions of polyacrylonitrile in dimethyl formamide (DMF) containing various amounts of a ferromagnetic nanoaddition were investigated. The porous structure, the strength and thermal properties of fibers obtained from these solutions were assessed, as well as the uniformity of the nanoaddition distribution on the fiber surface was estimated. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci, 2008     

Linkages between spouses' psychological distress and marital conflict in the home.

To elucidate the processes that underlie the established association between psychopathology and marital functioning, researchers have given attention to how symptomatic individuals manage their interpersonal contexts, particularly during the handling of disagreements. In the current study, the authors evaluate the role of marital conflict strategies in relation to wives' and husbands' psychological distress levels. A sample of 100 community-based couples completed assessments of psychological distress and diaries describing marital conflict that occurred at home during a 15-day reporting period. Findings from multilevel modeling of dyadic data revealed associations between both spouses' psychological distress and multiple behavioral and emotional conflict expressions in the home. Psychological symptoms uniquely predicted the occurrence of certain conflict expressions, even when accounting for global negative marital sentiments. The findings encourage subsequent consideration of marital conflict expressions and resolution strategies when studying processes involved in the marriage-psychological adjustment link. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

(R,R)-2,2'-[1,2-ethanediylbis[imino(1-methyl-2,1-ethanediyl)]]- bis[5-nitro-1H-benz[de]isoquinoline-1,3-(2H)-dione] dimethanesulfonate (DMP 840), a novel bis-naphthalimide with potent nonselective tumoricidal activity in vitro

(R,R)-2,2'-[1,2-ethanediylbis[imino(1-methyl-2,1-ethanediyl)]]- bis[5-nitro-1H-benz[de]isoquinoline-1,3-(2H)-dione] dimethanesulfonate (DMP 840), is a bis-naphthalimide anticancer tumoricidal agent currently in phase I clinical trials. DMP 840 exhibits curative activity in human tumor xenografts, where it shows selectivity for human solid tumors over murine leukemias. In contrast to the selectivity found for DMP 840 in vivo, DMP 840 exhibits potent antiproliferative activity in vitro against a variety of human and murine leukemia and solid tumor cell lines in culture, with inhibitory doses that reduce the number of treated cells to one half (IC50) values ranging from 2.3 to 53 nM. DMP 840 was growth inhibitory to three doxorubicin-resistant cell lines with IC50 values also in the nanomolar range. Clonogenic survival experiments showed that DMP 840 was equally cytotoxic to both exponentially growing and quiescent human clone A colon carcinoma cells. A 1-h incubation of DMP 840 (1.22-12 microM) caused 5-log cell kill in KB-3-1 human epidermoid carcinoma, clone A human colon carcinoma, and L1210 murine leukemia cell lines. The rapid cell killing by DMP 840 in clonogenic survival experiments and initial mechanism of action studies was consistent with a DNA-interactive mechanism for DMP 840 cytotoxicity. Mechanism of action studies in L1210 leukemia cells demonstrated that DMP 840 inhibited the incorporation of thymidine and uridine into DNA and RNA with IC50 values of 0.55 and 0.08 microM, respectively. DMP 840 produced DNA single-strand breaks in a dose-dependent manner. Double-strand breaks were not observed with DMP 840 treatment, even at higher concentrations of compound. Chinese hamster ovary (CHO) and P388 cells resistant to camptothecin and containing a mutant form of topoisomerase I were also used to evaluate whether DMP 840 was cross-resistant with agents active against topoisomerase I. While the CHOR line was 163-fold resistant to camptothecin, the CHOR line was only 1.7-fold resistant to DMP 840. In summary, DMP 840 is a DNA-interactive agent that demonstrates excellent antiproliferative activity in vitro against cultured tumor cells from both human and murine sources. Its mechanism of tumoricidal activity may be novel.     

Terahertz time domain spectroscopy of graphene and MXene polymer composites

The rising demand for faster and more efficient electronic devices forces electronics industry to shift toward terahertz frequencies. Therefore there is a growing need for efficient, lightweight, and easy to produce absorbing materials in the terahertz range for electromagnetic interference (EMI) shielding and related applications. This study presents a study on basic optical properties of two types polymer-based composites loaded with two-dimensional structures—graphene and MXene phases (Ti₂C). In said range, total EMI shielding efficiency (SE) and its components, the absorption coefficient (α ), refractive index, and complex dielectric function are investigated. The ratio of SE absorption component to reflection component (SE_ABS :SE_R ) of fabricated composites is equal or higher than 30:1 in over 80% of studied range. The fabricated composites exhibit low (<0.1) loss tangent in studied range. The addition of 1 wt% of graphene increases the composite α over 10-fold in respect to pure polymer–up to 60 cm⁻¹ for frequency higher than 2 THz.