The Effects of Haloperidol on Acute Carrageenan-Induced Inflammation

© 2017, Springer Science+Business Media New York.The objective of the study was to assess potential anti-inflammatory or pro-inflammatory effects of haloperidol, a classic typical neuroleptic, a butyrophenone derivative. It has been hypothesized that the anti-inflammatory mechanisms of some psychotropic drugs might become a rationale for their use for potential prevention of neurodegenirative diseases, including Alzheimer’s, which are known to include chronic inflammation as disease progression component. We looked at the effects of haloperidol on the acute carrageenan-induced inflammation of rat paws and showed that haloperidol with prolonged use (for 7 days prior to edema modeling) considerably increased the inflammatory response at 48 h. A single dose of haloperidol also stimulated the progression of inflammation but at earlier time points—at 3 and 4 h after carrageenan injection

The Effects of Haloperidol on the Progression of Chronic Autoimmune Inflammation Induced by Freund’s Adjuvant

© 2016, Springer Science+Business Media New York.Prophylactic administration to rats with the model of chronic autoimmune inflammation, induced by Freund’s adjuvant, of a typical neuroleptic haloperidol at a dose of 0.1 mg/kg increased the intensity of the primary inflammatory response (arthritis) and inhibited progression of the secondary arthritis

Analysis of factors associated with sterile inflammation in women with pe receiving different antihypertensive treatment strategies

Systemic inflammation alongside endothelial dysfunction is considered to play a crucial role in PE pathogenesis. Endothelial dysfunction can be assessed by endothelial glycocalyx (eGC) damage. eGC is a superficial layer of cells associated with endothelial membrane that provides all endothelial cells functions. Its damage can be evaluated by the levels of its circulating components in blood. Patients with PE generally receive methyldopa (Dopegyt) solely or in combination with nifedipine (Cordaflex), and there is no understanding of their effect on proinflammatory state of blood vessels. Our study aimed to assess levels of IL-6, IL-18, TNFα, galektin-3 and homocysteine as well as levels of syndecan-1, eCG structural component, representing system inflammatory response and endothelial dysfunction development in blood of women with early- and late-onset PE receiving different antihypertensive treatment strategies. Eighty-two patients were enrolled into this interventional longitudinal pilot study. The comparison group included 15 patients before 34 gestational weeks and 15 patients after 34 weeks. Study subgroup 1 included 12 patients with early- onset PE receiving Dopegyt solely and 16 patients with early-onset PE receiving Dopegyt together with Cordaflex. Study subgroup 2 included 12 patients with late-onset PE receiving Dopegyt solely and 12 patients with late-onset PE receiving combined therapy. As for early-onset PE, only IL-6 demonstrated statistically significant differences in patients receiving both treatment strategies compared to control. Proinflammatory state was more profound in late-onset PE. IL-6 levels were significantly increased in late-onset PE treated with Dopegyt. IL-6 and TNFa levels were significantly higher in late-onset PE patients treated with Dopegyt + Cordaflex compared to control. Syndecan-1 levels were statistically significantly higher in patients with early-onset PE treated with Dopegyt solely. There were no statistically significant differences between the groups despite elevated mean values of syndecan-1 in late-onset PE. Galectin-3 and homocysteine levels did not differ significantly between the groups, representing lack of pronounced inflammatory response and endothelial dysfunction

Thermally Induced Self-Assembly and Cyclization of l -Leucyl- l -Leucine in Solid State

© 2017 American Chemical Society. Thermal treatment of oligopeptides is one of the methods for synthesis of organic nanostructures. However, heating may lead not only to self-assembly of the initial molecules, but also to chemical reactions resulting in the formation of new unexpected nanostructures or change in the properties of the existing ones. In the present work, the reaction of cyclization of dipeptide l-leucyl-l-leucine in solid state under heating was studied. The change in morphology of dipeptide thin film and formation of nanostructures after heating was visualized using atomic force microscopy. This method also was used for demonstration of differences in self-assembly of linear and cyclic dipeptides. The chemical structure of reaction product was characterized by NMR spectrometry, FTIR spectroscopy and GC-MS analysis. Kinetic parameters of cyclization were estimated within the approaches of the nonisothermal kinetics ("model-free" kinetics and linear regression methods for detection of topochemical equation). The results of present work are useful for explanation the changes in the properties of nanostructures based on short-chain oligopeptides, notably leucyl-leucine, after thermal treatment, as well as for the synthesis of cyclic oligopeptides

Novel self-assembling system based on resorcinarene and cationic surfactant

Mixed association of calix[4]resorcinarene with ethyl sulfonate groups on the lower rim and dimethylaminomethyl groups on the upper rim (CR) and cationic surfactant 4-aza-1-hexadecyl-azoniabicyclo[2.2.2]octane bromide (DABCO-16) is studied by methods of tensiometry, conductometry, potentiometry and NMR spectroscopy at fixed CR concentration and varied surfactant concentration. Beyond ca. 0.4 mM of DABCO-16, mixed aggregates enriched by CR are proved to be formed due to electrostatic forces, while beyond ca. 5 mM, aggregates enriched by surfactant occur due to the hydrophobic effect. Spectrophotometry monitoring of the solubilization of a hydrophobic dye, Orange OT, demonstrated that only the second type of mixed aggregate enriched by DABCO-16 is capable of binding the organic probe, while the mixed system where the surfactant is a minor component shows no binding capacity towards Orange OT. This finding can be used for the design of nanocontainers with controllable binding/release properties.Dieser Beitrag ist mit Zustimmung des Rechteinhabers aufgrund einer (DFG-geförderten) Allianz- bzw. Nationallizenz frei zugänglich

Radionuclide Diagnosis of Esophageal Dysmotility and Gastroesophageal Reflux in Patients with Systemic Sclerosis

Objective: to evaluate the possibilities of dynamic scintigraphy for the diagnosis of esophageal dysmotility (ED) and gastroesophageal reflux (GER) in patients with systemic sclerosis (SS).Material and methods. The study group included 77 patients with established SS of different disease duration (from several months to 30 years) who underwent Technephyt 99mTc dynamic esophageal scintigraphy using two-stage protocol. During the first stage, the esophageal transport function was evaluated; during the second stage, the presence and severity of GER were assessed. Scans were analyzed using visual assessment, quantitative estimation of time/activity curves, and a proposed three-point scale for evaluating ED and GER severity. The control group consisted of 19 practically healthy individuals who underwent a routine examination to exclude digestive system and gastrointestinal tract diseases, the algorithm of which included dynamic scintigraphy.Results. ED was found in 74 of 77 patients (96%). According to three-point scale, severe ED (3 points) was registrated in 41 (55%) patients, moderate ED (2 points) in 15 (21%), and mild ED in 18 (24%). GER was diagnosed in 35 of 77 cases (45%): mild GER in 13 (37%), moderate GER (2 points) in 22 (63%), and none of the patients was found to have severe GER (3 points). A significant relationship between the presence of GER and the severity of ED was not obtained, but a direct correlation was established between ED and GER severity.Conclusion. Most SS patients demonstrated ED of varying severity associated with mild and moderate GER in nearly 45% of the cases. The study results confirm the practical significance of dynamic scintigraphy for assessing the esophageal transport function and GER in SS patients

An Organic Spin Crossover Material in Water from a Covalently Linked Radical Dyad

A covalently linked viologen radical cation dyad acts as a reversible thermomagnetic switch in water. Cycling between diamagnetic and paramagnetic forms by heating and cooling is accompanied by changes in optical and magnetic properties with high radical fidelity. Thermomagnetic switches in water may eventually find use as novel biological thermometers and in temperature-responsive organic materials where the changes in properties originate from a change in electronic spin configuration rather than a change in structure

Mechanical Bonds and Topological Effects in Radical Dimer Stabilization

While mechanical bonding stabilizes tetrathiafulvalene (TTF) radical dimers, the question arises: what role does topology play in catenanes containing TTF units? Here, we report how topology, together with mechanical bonding, in isomeric [3]- and doubly interlocked [2]catenanes controls the formation of TTF radical dimers within their structural frameworks, including a ring-in-ring complex (formed between an organoplatinum square and a {2+2} macrocyclic polyether containing two 1,5-dioxynaphthalene (DNP) and two TTF units) that is topologically isomeric with the doubly interlocked [2]catenane. The separate TTF units in the two {1+1} macrocycles (each containing also one DNP unit) of the isomeric [3]catenane exhibit slightly different redox properties compared with those in the {2+2} macrocycle present in the [2]catenane, while comparison with its topological isomer reveals substantially different redox behavior. Although the stabilities of the mixed-valence (TTF2)^(•+) dimers are similar in the two catenanes, the radical cationic (TTF^(•+))_2 dimer in the [2]catenane occurs only fleetingly compared with its prominent existence in the [3]catenane, while both dimers are absent altogether in the ring-in-ring complex. The electrochemical behavior of these three radically configurable isomers demonstrates that a fundamental relationship exists between topology and redox properties