Effect of acute high-intensity interval exercise on a mouse model of doxorubicin-induced cardiotoxicity: a pilot study.

Background: It is unknown whether high-intensity interval exercise (HIIE) may potentiate or attenuate the cardiotoxic effect of chemotherapy agents such as doxorubicin (DOX) when performed shortly after treatment. The study aimed to investigate the effect of acute HIIE on cardiac function and structure performed either 1, 2 or 3 days after DOX injection in an animal model.

Methods: Female C57bl/6 mice (n = 28), 70 days old, received a bolus 20 mg/kg intravenous tail vein DOX injection.

Novel O-[C]-methylated derivatives of the neprilysin inhibitor sacubitril: Radiosynthesis, autoradiography and plasma stability evaluation.

Introduction: The O-[C]methylated derivatives of the clinically used neprilysin inhibitor (NEPi) sacubitril ([C]SacOMe, (2R,4S)-ethyl 5-([biphenyl]-4-yl)-4-(4-[C]methoxy-4-oxobutanamido)-2-methylpentanoate) and LBQ657 ([C]MeOLBQ, (2R,4S)-5-(biphenyl-4-yl)-4-[(3-carboxypropionyl)amino]-2-methylpentanoic acid [C]methyl ester and [C]LBQOMe, (2R,4S)-5-(biphenyl-4-yl)-4-[(4-[C]methoxy-4-oxobutanamido)]-2-methylpentanoic acid) were evaluated to determine their potential as PET imaging tracers and investigate the effect of such labeling esterification on neprilysin (NEP) binding.

Methods: [C]MeOLBQ, [C]SacOMe and [C]LBQOMe were synthesized by O-[C]methylation using [C]methyl triflate. Binding of these radiolabeled derivatives (5 nM) were assessed by autoradiography on rat neprilysin rich kidney slices with or without 10 μM NEPi (thiorphan or sacubitril) for 20 min at 37 °C.

Evaluation of the high affinity [F]fluoropyridine-candesartan in rats for PET imaging of renal AT receptors.

Introduction: Alterations in the expression of the Angiotensin II type 1 receptors (ATR) have been demonstrated in the development of several heart and renal diseases. The aim of this study was to evaluate the novel compound [F]fluoropyridine-candesartan as a PET imaging tracer of ATR in rat kidneys.

Methods: Competition binding assays were carried out with membranes from CHO-K1 cells expressing human ATR.

Synthesis of a C-Isotopologue of the B-Raf-Selective Inhibitor Encorafenib Using In-Loop [C]CO Fixation.

The serine/threonine kinase B-Raf is an essential regulator of cellular growth, differentiation, and survival. B-Raf protein expression is elevated throughout melanoma progression, making it an attractive target for noninvasive imaging using positron-emission tomography. Encorafenib is a potent and highly selective inhibitor of B-Raf used in the clinical management of melanoma.

Synthesis of the Novel AT Receptor Tracer [F]Fluoropyridine-Candesartan via Click Chemistry.

A novel 7-((4-(3-((2-[F]fluoropyridin-3-yl)oxy)propyl)-1-1,2,3-triazol-1-yl)methyl)-1-benzo[]imidazole derivative of the angiotensin II type-1 receptor (ATR) blocker candesartan, [F]fluoropyridine-candesartan, was synthesized via the copper-catalyzed azide-alkyne cycloaddition click reaction between 2-[F]fluoro-3-(pent-4-yn-1-yloxy)pyridine ([F]FPyKYNE) and the tetrazole-protected azido-candesartan derivative, followed by acid deprotection. This three-step, two-pot, and two-step purification synthesis was done within 2 h. The use of tris[(1-hydroxypropyl-1-1,2,3-triazol-4-yl)methyl]amine (THPTA) as a Cu(I) stabilizing agent increased the overall radiochemical yield by 4-fold (10 ± 2%, = 13) compared to the reaction without THPTA (2.

Is Implant Coating With Tyrosol- and Antibiotic-loaded Hydrogel Effective in Reducing Cutibacterium (Propionibacterium) acnes Biofilm Formation? A Preliminary In Vitro Study.

Background: Studies have suggested that Cutibacterium acnes (formerly known as Propionibacterium) is the most frequently isolated pathogen after shoulder arthroplasty. To address the burden of periprosthetic joint infections associated with this pathogen, new prevention methods are needed. Tyrosol has a promising record of effectiveness in the field of biofilm-associated infections; however, to our knowledge, it has not been tested against C.

The Potential Roles of MELF-Pattern, Microvessel Density, and VEGF Expression in Survival of Patients with Endometrioid Endometrial Carcinoma: A Morphometrical and Immunohistochemical Analysis of 100 Cases.

Background: In this study, we hypothesized that microcystic, elongated, fragmented (MELF)-pattern, vascular endothelial growth factor (VEGF) expression by cancer cells and microvessel density of cancer stroma may be associated with progression of endometrioid adenocarcinoma.

Methods: The study used data from the Belarus Cancer Registry and archival histological material of 100 patients with retrospectively known good (survival) and poor (disease progression and death) outcomes. All cases were immunohistochemically stained for CD34 and VEGF.