Active Anti-Inflammatory and Hypolipidemic Derivatives of Lorazepam.

Novel derivatives of some non steroidal anti-inflammatory drugs, as well as of the antioxidants α-lipoic acid, trolox and ()-3-(3,5-di-tert-butyl-4-hydroxyphenyl)acrylic acid with lorazepam were synthesised by a straightforward method at satisfactory to high yields (40%-93%). All the tested derivatives strongly decreased lipidemic indices in rat plasma after Triton induced hyperlipidaemia. They also reduced acute inflammation and a number of them demonstrated lipoxygenase inhibitory activity.

The ossification of the vertebral column, thorax and sternum in the quail ().

The ossification centers onset of the quail vertebrae, ribs, and sternum in embryos and hatchling birds was studied. Specimens were cleared, stained with Alcian Blue and Alizarin Red S and examined using stereomicroscope. The chondral rudiments of the vertebrae were observed at the 6 day of incubation (E6).

Xenobiotic Metabolising Enzymes: Impact on Pathologic Conditions, Drug Interactions and Drug Design.

Background: The biotransformation of xenobiotics is a homeostatic defensive response of the body against bioactive invaders. Xenobiotic metabolizing enzymes, important for the metabolism, elimination and detoxification of exogenous agents, are found in most tissues and organs and are distinguished into phase I and phase II enzymes, as well as phase III transporters. The cytochrome P450 superfamily of enzymes plays a major role in the biotransformation of most xenobiotics as well as in the metabolism of important endogenous substrates such as steroids and fatty acids.

Clinical Outcomes and Neuroimaging Profiles in Nondisabled Patients With Anticoagulant-Related Intracerebral Hemorrhage.

Background and Purpose- The aim of this study was to prospectively validate our prior findings of smaller hematoma volume and lesser neurological deficit in nonvitamin K oral anticoagulant (NOAC) compared with Vitamin K antagonist (VKA)-related intracerebral hemorrhage (ICH). Methods- Prospective 12-month observational study in 15 tertiary stroke centers in the United States, Europe, and Asia. Consecutive patients with premorbid modified Rankin Scale score of <2 with acute nontraumatic anticoagulant-related ICH divided into 2 groups according to the type of anticoagulant: NOAC versus VKA.

[Restraints in Greek mental health services: Ethics, practice and costs].

The use of physical and mechanical restraints in mental health services in Greece arise many ethical and practical issues. The justification of the use of such procedures is rather controversial and subjective to scientific debate. The practice of restraint puts both patients and staff at risk for injury and death.

The O-β-linked N-acetylglucosaminylation of the Lamin B receptor and its impact on DNA binding and phosphorylation.

Unlabelled: Lamin B Receptor (LBR) is an integral protein of the interphase inner nuclear membrane that is implicated in chromatin anchorage to the nuclear envelope. Phosphorylation of a stretch of arginine-serine (RS) dipeptides in the amino-terminal nucleoplasmic domain of LBR regulates the interactions of the receptor with other nuclear proteins, DNA and RNA and thus modulates tethering of heterochromatin to the nuclear envelope. While phosphorylation has been extensively studied, very little is known about other post-translational modifications of the protein.

Survey on current practice within the European Low-Grade Glioma Network: where do we stand and what is the next step?

Diffuse low-grade glioma form a rare entity affecting young people. Despite advances in surgery, chemotherapy, and radiation therapy, diffuse low-grade glioma are still incurable. According to current guidelines, maximum safe resection, when feasible, is the first line of treatment.

Left ventricular geometry as a major determinant of left ventricular ejection fraction: physiological considerations and clinical implications.

The limited myocardial fibre thickening and shortening alone cannot explain the marked left ventricular (LV) volume reduction during LV ejection. This can only be achieved with LV helical (spiral) orientation of myocardial fibres, which is determined by the non-contractile LV myocardial components (intrasarcomeric and extrasarcomeric cytoskeleton, extracellular matrix). Preservation of LV ejection fraction (LVEF) in heart failure (HF) is due to the presence of normal ellipsoid LV configuration and spiral myocardial fibre orientation.

Dual antioxidant structures with potent anti-inflammatory, hypolipidemic and cytoprotective properties.

Novel amide derivatives of trolox, 3,5-di-tert-butyl-4-hydroxybenzoic acid, (E)-3-(3,5-di-tert-butyl-4-hydroxyphenyl)acrylic acid and cinnamic acid with cysteamine and l-cysteine ethyl ester were synthesised. In four cases, the disulfide derivatives were also isolated and tested. All compounds were examined for antioxidant activity, expressed as their ability to inhibit lipid peroxidation and to scavenge free radicals.

Direct oral anticoagulant- vs vitamin K antagonist-related nontraumatic intracerebral hemorrhage.

Objective: To compare the neuroimaging profile and clinical outcomes among patients with intracerebral hemorrhage (ICH) related to use of vitamin K antagonists (VKAs) or direct oral anticoagulants (DOACs) for nonvalvular atrial fibrillation (NVAF).

Methods: We evaluated consecutive patients with NVAF with nontraumatic, anticoagulant-related ICH admitted at 13 tertiary stroke care centers over a 12-month period. We also performed a systematic review and meta-analysis of eligible observational studies reporting baseline characteristics and outcomes among patients with VKA- or DOAC-related ICH.

Characterization of boscalid-resistance conferring mutations in the SdhB subunit of respiratory complex II and impact on fitness and mycotoxin production in Penicillium expansum laboratory strains.

Laboratory mutants of Penicillium expansum highly resistant (Rfs: 90 to >500, based on EC) to Succinate Dehydrogenase Inhibitors (SDHIs) were isolated after UV-mutagenesis and selection on media containing boscalid. A positive correlation was found between sensitivity of isolates to boscalid and other SDHIs such as isopyrazam and carboxin but not to fungicides affecting other cellular pathways or processes, such as the triazole flusilazole, the phenylpyrrole fludioxonil, the anilinopyrimidine cyprodinil and the benzimidazole benomyl. Most of the boscalid-resistant strains were more sensitive to the SDHI fluopyram and the QoI pyraclostrobin.

Biologic Stress, Oxidative Stress, and Resistance to Drugs: What Is Hidden Behind.

Stress can be defined as the homeostatic, nonspecific defensive response of the organism to challenges. It is expressed by morphological, biochemical, and functional changes. In this review, we present biological and oxidative stress, as well as their interrelation.

Iliac Crest Regeneration: A Retrospective Study of 14 Years of Follow-up.

Study Design: This is a retrospective study analysis.

Objective: The purpose of our study was to evaluate the healing process of the ilium after being used as a bone graft donor site in the treatment of adolescent idiopathic scoliosis.

Summary Of Background Data: Iliac crest bone grafts have been proven to be the most reliable means for solid fusion in spine surgery.

Medicinal Chemistry Approaches of Controlling Gastrointestinal Side Effects of Non-Steroidal Anti-Inflammatory Drugs. Endogenous Protective Mechanisms and Drug Design.

Background: Non-steroidal anti-inflammatory drugs are the oldest and most widely used medicines. However, their untoward effects, especially gastrointestinal toxicity, remain the main obstacle to their application. Because of their mechanism of action, cycloxygenase (COX) inhibition, in combination with the weekly acidic character of most of them, major protective mechanisms of the gastrointestinal system are suppressed and deregulated.

Detection of B Gene Mutations in SDHI-Resistant Isolates of Using High Resolution Melting (HRM) Analysis.

, is a high risk pathogen for fungicide resistance development. Pathogen' resistance to SDHIs is associated with several mutations in gene. The diversity of mutations and their differential effect on cross-resistance patterns among SDHIs and the fitness of resistant strains necessitate the availability of a tool for their rapid identification.

Anti-inflammatory and Hypolipidemic Effect of Novel Conjugates with Trolox and Other Antioxidant Acids.

Objectives: A series of esters and amides, incorporating an antioxidant residue, such as trolox or caffeic acid, and various moieties with different biological activities, were synthesised. The obtained compounds demonstrated considerable anti-inflammatory, radical scavenging and antioxidant action. Thus, they could reduce carrageenan-induced rat paw oedema by 31-60% at 150 μmol/kg and inhibit rat microsomal membrane lipid peroxidation with IC50 values as low as 1.

Global left atrial failure in heart failure.

The left atrium plays an important role in the maintenance of cardiovascular and neurohumoral homeostasis in heart failure. However, with progressive left ventricular dysfunction, left atrial (LA) dilation and mechanical failure develop, which frequently culminate in atrial fibrillation. Moreover, LA mechanical failure is accompanied by LA endocrine failure [deficient atrial natriuretic peptide (ANP) processing-synthesis/development of ANP resistance) and LA regulatory failure (dominance of sympathetic nervous system excitatory mechanisms, excessive vasopressin release) contributing to neurohumoral overactivity, vasoconstriction, and volume overload (global LA failure).

Mortality and survival patterns of childhood lymphomas: geographic and age-specific patterns in Southern-Eastern European and SEER/US registration data.

Childhood (0-14 years) lymphomas, nowadays, present a highly curable malignancy compared with other types of cancer. We used readily available cancer registration data to assess mortality and survival disparities among children residing in Southern-Eastern European (SEE) countries and those in the United States. Average age-standardized mortality rates and time trends of Hodgkin (HL) and non-Hodgkin (NHL; including Burkitt [BL]) lymphomas in 14 SEE cancer registries (1990-2014) and the Surveillance, Epidemiology, and End Results Program (SEER, United States; 1990-2012) were calculated.

Tumour Budding Correlates with Aggressiveness of Cutaneous Squamous-cell Carcinoma.

Background/aim: Tumour budding (TB) is a specific pathological feature that has been found to be associated with an aggressive outcome in several cancer types; however, to our knowledge, TB has not yet been assessed in squamous-cell carcinomas of the skin (SCC). The aim of the study was to study whether TB correlates with aggressiveness in cutaneous SCC.

Materials And Methods: We examined 31 aggressive SCC (that later developed local recurrences or metastases) in comparison with 21 non-aggressive SCC (not complicated by recurrence or metastasis).