Retinoic acid conjugates as potential antitumor agents: synthesis and biological activity of conjugates with Ara-A, Ara-C, 3(2H)-furanone, and aniline mustard moieties

In a dual targeting approach, to explore the ability of tretinoin (all-trans-retinoic acid) to behave as a covalent carrier for cytotoxic entities, conjugates of retinoic acid with a few representative molecules, being important examples of antitumor pharmacophores (i.e., nucleoside analogues and alkylating agents), have been synthesized and tested for their cytostatic and differentiating activity. All compounds were stable to in vitro hydrolysis in human plasma and more lipophilic than the parent compounds, thus consenting enhanced uptake into the cells. Among the nucleoside analogues the Ara-C derivatives 3 and 6 and the Ara-A derivative 7 proved the most cytostatic (IC50 < 0.32 microgram/mL) resulting from 25- to > 144-fold more active (Ara-A derivatives) or at least as equally active (Ara-C derivatives) as compared to the parent nucleosides. Compound 3, endowed with a highly lipophilic silyl moiety at the 3' and 5' positions, showed the highest differentiating activity (54% and 44% differentiated HL-60 cells at 0.2 and 0.05 microgram/mL respectively). With regard to the retinoic acid conjugates of alkylating agents, compound 10 was the most cytostatic agent (IC50 < 0.32 microgram/mL) and the most potent differentiating agent (33-34% at 0.32 and 0.08 microgram/mL). These structures may also be regarded as analogs of either retinoic acid or the cytotoxic compound.     

Primary lymphoma of the breast. Three cases of non-Hodgkin lymphoma

Primary and sole breast lymphoma is a very rare disease. With the review of our series of 616 cases operated on for breast cancer, only 3 cases (0.48%) of primary breast non-Hodgkin lymphoma (LNH) have been observed. The authors outline the problems concerning diagnosis and therapy of this rare disease: pathological and immunohistochemical aspects are discussed. They stress the importance of staging in order to plan a correct multidisciplinary approach.     

Thermoplastic elastomeric composition based on maleic anhydride–grafted ground rubber tire

Ground rubber tire (GRT) powder was maleated in an internal mixer using maleic anhydride and dicumyl peroxide at 160°C. Maleated GRT was characterized by using X‐ray photoelectron spectroscopy, Fourier transform infrared spectroscopy, wettability, and differential scanning calorimetry. The physical properties of the dynamically vulcanized 60 : 40, rubber : plastic composition based on acrylated high‐density polyethylene as the plastic phase and ethylene propylene diene rubber containing maleated GRT as the rubber phase were found to be greater than the corresponding composition containing nonmaleated GRT. The blend was found to be reprocessable, like themoplastic elastomers. © 2002 Wiley Periodicals, Inc. J Appl Polym Sci 84: 370–378, 2002; DOI 10.1002/app.10348     

Influence of heat transfer on anodic oxidation of aluminium

The influence of convective heat transfer on constant current density anodizing of aluminium in sulfuric acid has been examined in a wall-jet electrode reactor. The uniformity of the anodic film thickness is related to the local electrode temperature distribution, which is dependent on the convection. The higher the local temperature, the greater the local oxide thickness. An increased local temperature enhances local field assisted oxide dissolution at the pore bases, and consequently acts to increase the local current density. At relatively high current densities, local features develop on the electrode surface, accompanied by high initial, local temperature rises. The relevance of such local features, limiting useful oxide growth, is considered further.     

SCRATCH RESISTANT POLYIMIDE COATINGS FOR ALUMINOSILICATE GLASS SURFACES

Several polyimide resins were tested as possible scratch resistant coatings for aluminosilicate glass centrifuge tubes. Tubes with siloxane pretreatments provided the best adhesion between the polyimide and glass surface. Resins synthesized with an alkoxysilane group incorporated into the polyimide chain also showed improved adhesion, but the results were not as significant as when the pretreatment was used. Elastic recovery and effective Young's modulus of the polyimide coatings were calculated from nano-scratching. The results indicate that polyimides with a lower modulus, and higher elastic recovery, protected the glass surface best, exhibiting compression of the coating layer. An example was poly-4-4'-oxydiphenylene pyromellitimide (PMDA-ODA), whereas the coatings with a high effective Young's modulus and low elastic recovery ruptured. An example of a failed coating was poly-4,4'-carbonyldiphenylene 3,3',4,4'-biphenylenetetracarboximide (BPDA-DABP) which had low amount of elastic recovery, high effective Young's modulus and a large amount of flaking during macroscratch testing.     

Effects of e-enforcement in the Netherlands

E-enforcement, or electronic enforcement, is the use of electronic tools in law enforcement. We shall distinguish between the first and second generations of e-enforcement. The first generation of e-enforcement tools provided means of "automated enforcement". This article is based on our research into the effects of two forms of second generation e-enforcement: the digital tachograph and 'Weigh in Motion' (WIM). The digital tachograph replaces the analog tachograph in all heavy goods vehicles within the European Union. The equipment registers drivers' driving and rest times. Weigh in Motion with Video (WIM-Vid) is a system involving sensors in the road and cameras, which detect and register overloading of heavy goods vehicles. The WIM-Vid system was developed and implemented in the Netherlands and is currently attracting international attention. We compare the situation prior to the introduction of these e-enforcement measures to the situation after the introduction of e-enforcement.     

A variational principle for magneto-elastic buckling

A variational principle that can serve as the basis for a magneto-elastic stability (or buckling) problem is constructed. For the two cases of soft ferromagnetic media and superconductors, respectively, it is shown how the variational principle directly yields an explicit expression for the buckling value. The formulation starts from a specific choice for a magneto-elastic Lagrangian L (associated with the so-called Maxwell-Minkowski model for magneto-elastic interactions). For the evaluation of the principle the first and second variations of L are calculated both inside and outside the solid magneto-elastic body. Thus, a general buckling criterion, consisting of an expression for the critical field value, together with a set of constraints for the field variables occurring in the right-hand side of this expression, is constructed. Finally, more detailed formulations are given for, successively, soft ferromagnetic bodies and superconductors. Applications to specific structures, yielding explicit numerical values for the magneto-elastic buckling fields, will be given in a forthcoming paper.     

Adaptive Radar Detection of Distributed Targets in Homogeneous and Partially Homogeneous Noise Plus Subspace Interference

This paper addresses adaptive radar detection of distributed targets in noise plus interference assumed to belong to a known or unknown subspace of the observables. At the design stage we resort to either the GLRT or the so-called two-step GLRT-based design procedure and assume that a set of noise-only data is available (the so-called secondary data). Detection algorithms have been derived modeling noise vectors, corresponding to different range cells, as independent, zero-mean, complex normal ones, sharing either the same covariance matrix (homogeneous environment) or the same covariance matrix up to possibly different (mean) power levels between primary data, i.e., range cells under test, and secondary ones (partially homogeneous environment). The performance assessment has been conducted by Monte Carlo simulation, also in comparison to previously proposed detection algorithms, and confirms the effectiveness of the newly proposed ones     

β-hydroxyacyl-coa-dehydrogenase (HADH) activity of unfrozen and frozen—thawed frog (Rana esculenta) legs

The β-hydroxyacyl-CoA-dehydrogenase (HADH) activity of unfrozen and thawed frog legs was investigated. The enzyme was extracted by either immersing frog legs in phosphate buffer 0.1 M, pH 6.0 at 25°C for 15 min or pressing them between trichinoscopy glasses. The enzyme activity was assayed using acetoacetyl-CoA as substrate and measured spectrophotometrically at 340 nm. It was possible by both extraction methods to distinguish between thawed and unfrozen samples although when the juice was obtained by pressing the HADH activity of the dilution was ～ 1.5 times higher than that obtained by immersion. The HADH activity was significantly higher (P≤0·001) in frozen-thawed frogs than in unfrozen legs because during freezing there is a release of HADH. No significative differences were found in the HADH activity in samples frozen in the temperature range -10 to -196°C. HADH activity was not affected by the storage time in crushed ice up to 6 days.     

Recurrent hyperparathyroidism due to parathyroid autografts: incidence, presentation, and management

Recurrent hyperparathyroidism (HPT) occurs in a small percentage of patients undergoing parathyroidectomy for primary HPT and is usually due to inadequate excision of hyperfunctioning parathyroid tissue in the neck, a missed ectopic and hyperplastic parathyroid, or, less commonly, parathyroid carcinoma and parathyroid autografts. In order to determine the incidence, clinical characteristics, and outcome of patients with recurrent HPT due to parathyroid autografts, we reviewed our experience with 604 consecutive patients operated on for primary HPT between 1965 and 1989. One hundred of these patients received parathyroid autografts consisting of portions of one or more parathyroid glands. Three patients with autografts, placed in the sternocleidomastoid muscle, developed recurrent HPT due to their autografts for an incidence of 3 per cent. Recurrent disease was diagnosed between 62 and 113 months with an average of 89 months. The autotransplants in all three of these patients were from hyperplastic or adenomatous parathyroid tissue. Two patients had a history of neck irradiation. Preoperative thallium scans accurately localized the hyperfunctioning parathyroid tissue in all three patients. At operation, the hyperfunctioning autografts had grown into a discrete mass with a single vascular pedicle and were resected. Histologic examination disclosed either hyperplastic or adenomatous tissue, and corresponded to the histology and location of the original tissue transplanted in each case. Follow-up ranges from 12 to 67 months, with an average of 48 months. All patients remain cured and none require oral calcium supplementation. We conclude that graft-dependent recurrent HPT is due to the autotransplantation of hyperplastic or adenomatous parathyroid tissue and that thallium scanning is instrumental for diagnosis and localization.(ABSTRACT TRUNCATED AT 250 WORDS)