The Study of Main Physical-chemical Parameters of Chaenomeles and Products of Its Processing

In the article were considered the topical problems, connected with health worsening and human existence. The use of vegetable raw material as a source of biologically active components is prospective in production foodstuff. There were offered the rational methods of processing of chaenomeles for getting juice and puree. There were carried out an analysis of expedience of using chaenomeles and products of its processing for enrichment foodstuff. It was established, that maximal amount of phenol substances is contained in fruit peel and L-ascorbic acid - in flesh. It was determined, that apple acid prevails among organic ones, fructose - among sugars and phenol substances are mainly presented by procyanidins. Using chromotographic analysis in the products of chaenomeles processing were identified 48 names of aromatic compounds, alcohols, acids, ethers and unsaturated carbohydrates prevail among them. There were studied the physical-chemical parameters of fruit sauces and flour products with addition of chaenomeles processing products. The received results prove that the ready foodstuff that contain puree and juice of chaemomeles have the high organoleptic, physical-chemical parameters and also heightened biological value

Токсикологічна характеристика препарату ForticeptTM Hoof Oinment

Antibiotic resistance of the main infectious disease pathogens is one of the biggest problems of present time, which causes the need for searching for new antimicrobial medicinal substances and developing effective medicinal agents. One of the innovative medicinal preparations with the antimicrobial action, which is recommended for application for animals with hoof diseases, is ForticeptTM Hoof Oinment. Integration in the practice new medicinal preparations needs their strict toxicological control, which involves the exploring of acute and chronic toxicity and remote effects of possible side effect. The purpose of work was the determination of the acute toxicity parameters of the ForticeptTM Hoof Oinmentduring the oral administration to white laboratory mice and evaluation of the skin resorptive action of the preparation after it was administrated on rats’ skin. For determination of the acute toxicity there were used male laboratory mice with the average weight of the body 20 g – two groups with 10 animals in each. For the first group (the control one) with the help of the probe there was injected the distilled water (0.1 ml) into stomach. For the second group there was injected ForticeptTM Hoof Oinment (0.1 g), where the dose of the preparation is equal 500 mg/kg. For evaluation of the skin resorptive action of the preparation there were used 6 white rats with the average weight of the body 175 g. On the pre-prepared patch of skin there was administrated the preparation in the number that is equal 2857 mg/kg of body weight. For control there was leaved a free from preparation patch of bare skin. Exposition lasted for 4 hours. The indicators were explored in dynamics after 6, 24, 48 hours from the exposition started. After the research results there was established that ForticeptTM Hoof Oinment doesn’t cause death after its intragastric administration to the white laboratory mice in the number that is equal 5000 mg/kg of the body weight, that’s why depending on the degree of toxicity it belongs to the V toxicity class (Practically nontoxic). After one-time application of the preparation to the white rats in the number which is equal 2857 mg/kg of the body weight there wasn’t observes no death or pronounced changes in the behavior reactions, motor activity, state of the nervous system, amount of the consumed food and water. Therefore ForticeptTM Hoof Oinmentaccording to the results of the determination of the acute toxicity after its administration on the skin to the white rats depending on the degree of toxicity it belongs to the V toxicity class (Practically nontoxic). ForticeptTM Hoof Oinment doesn’t detect skin resorptive action, that points on the absence of toxic effects of the preparation due to its application on the skin.Антибіотикорезистентність основних збудників інфекційних захворювань є однією з найбільших проблем сучасності, що обумовлює необхідність пошуку нових лікарських речовин протимікробної дії та розробки ефективних лікарських засобів. Одним із інноваційних лікарських препаратів з протимікробною активністю, що рекомендується до застосування тваринам з хворобами копит, є ForticeptTM Hoof Oinment. Впровадження в практику нових лікарських препаратів потребує їхнього суворого токсикологічного контролю, який передбачає вивчення гострої та хронічної токсичності, а також віддалених ефектів можливої побічної дії. Метою роботи було визначення параметрів гострої токсичності препарату ForticeptTM Hoof Oinment за перорального введення білим лабораторним мишам, а також оцінка шкірно-резорбтивної дії препарату після його нанесення на шкіру щурам. Для визначення гострої токсичності використовували самців лабораторних мишей з середньою масою тіла 20 г – дві групи по 10 тварин у кожній. Тваринам першої групи (контрольна) уводили в шлунок за допомогою зонду дистильовану воду в кількості 0,1 мл. Тваринам другої – препарат ForticeptTM Hoof Oinment у кількості 0,1 г, за якої доза препарату відповідає 5000 мг/кг. Для оцінки шкірно-резорбтивної дії препарату було використано 6 білих щурів з середньою масою тіла 175 г. На заздалегідь підготовлену ділянку шкіри наносили препарат у кількості, що відповідала дозі 2857 мг/кг маси тіла. Для контролю залишали вільною від препарату частину оголеної ділянки шкіри. Експозиція складала 4 години. Показники вивчали у динаміці через 6, 24, 48 год від початку експозиції. У результаті досліджень встановлено, що ForticeptTM Hoof Oinment не спричиняє загибелі після його внутрішньошлункового введення білим лабораторним мишам у кількості, що відповідає дозі 5000 мг/кг маси тіла, тобто за ступенем токсичності належить до V класу токсичності (практично нетоксичні). Після одноразового нанесення на шкіру білим щурам препарату у кількості, що відповідає дозі 2857 мг/кг маси тіла, не спостерігали загибелі та виражених змін поведінкових реакцій, рухової активності, стану нервової системи, кількості спожитого корму та води. Отже, ForticeptTM Hoof Oinment за результатами визначення гострої токсичності після його нанесення на шкіру білим щурам за ступенем токсичності належить до V класу токсичності (практично нетоксичні). ForticeptTM Hoof Oinment не проявляє шкірно-резорбтивної дії, що вказує на відсутність токсичної дії препарату за його аплікації на шкіру

Age-dependent, subunit specific action of hydrogen sulfide on GluN1/2A and GluN1/2B NMDA receptors

© 2017 Yakovlev, Kurmasheva, Ishchenko, Giniatullin and Sitdikova. Hydrogen sulfide (H 2 S) is an endogenously produced neuroactive gas implicated in many key processes in the peripheral and central nervous system. Whereas the neuroprotective role of H 2 S has been shown in adult brain, the action of this messenger in newborns remains unclear. One of the known targets of H 2 S in the nervous system is the N-methyl-D-aspartate (NMDA) glutamate receptor which can be composed of different subunits with distinct functional properties. In the present study, using patch clamp technique, we compared the effects of the H 2 S donor sodium hydrosulfide (NaHS, 100 µM) on hippocampal NMDA receptor mediated currents in rats of the first and third postnatal weeks. This was supplemented by testing effects of NaHS on recombinant GluN1/2A and GluN1/2B NMDA receptors expressed in HEK293T cells. The main finding is that NaHS action on NMDA currents is age-dependent. Currents were reduced in newborns but increased in older juvenile rats. Consistent with an age-dependent switch in NMDA receptor composition, in HEK239T cells expressing GluN1/2A receptors, NaHS increased NMDA activated currents associated with acceleration of desensitization and decrease of the deactivation rate. In contrast, in GluN1/2B NMDA receptors, which are prevalent in newborns, NaHS decreased currents and reduced receptor deactivation without effect on the desensitization rate. Adenylate cyclase inhibitor MDL-12330A (10 µM) did not prevent the age-dependent effects of NaHS on NMDA evoked currents in pyramidal neurons of hippocampus. The reducing agent dithiothreitol (DTT, 2 mM) applied on HEK293T cells prevented facilitation induced by NaHS on GluN1/2A NMDA receptors, however in GluN1/2B NMDA receptors the inhibitory effect of NaHS was still observed. Our data indicate age-dependent effect of H 2 S on NMDA receptor mediated currents determined by glutamate receptor subunit composition. While the inhibitory action of H 2 Son GluN1/2B receptors could limit the excessive activation in early age, the enhanced functionality of GluN1/2A receptor in the presence of this gasotransmitter can enlarge synaptic efficacy and promote synaptic plasticity in adults

Radioluminescence properties of nanocomposite scintillators with BaF 2 fillers

In this paper, studies of the luminescence properties of nanocrystalline BaF 2 samples synthesized by laser ablation and pulse electron beam evaporation method are presented. The measurements of X-ray excited luminescence (XEL) showed the dependence between luminescence intensity and the shape of the spectrum on the morphology and particle size. Also, studies of X-ray excited luminescence, decay curves and optical transmittance for nanocomposite materials containing BaF 2 nanopowder are presented. Barium fluoride nanopowder, obtained by pulsed electron beam evaporation method is characterized by a lower intensity than the initial microcrystalline powder, but at the same time, XEL spectrum of the nanocomposite material with this nanocrystalline filler is more intense, then that for nanocomposite material with initial powder. © Published under licence by IOP Publishing Ltd

Reconstructed Serine 288 in the Left Flipper Region of the Rat P2X7 Receptor Stabilizes Nonsensitized States

© 2017 American Chemical Society. Serine 275, a conserved residue of the left flipper region of ATP-gated P2X3 receptors, plays a key role in both agonist binding and receptor desensitization. It is conserved in most of the P2X receptors except P2X7 and P2X6. By combining experimental patch-clamp and modeling approaches, we explored the role of the corresponding residue in the rat P2X7 receptor (rP2X7) by replacing the phenylalanine at position 288 with serine and characterizing the membrane currents generated by either the wild-type (WT) or the mutated rP2X7 receptor. F288S, an rP2X7 mutation, slowed the deactivation subsequent to 2 and 20 s applications of 1 mM ATP. F288S also prevented sensitization (a progressive current growth) observed with the WT in response to a 20 s application of 1 mM ATP. Increasing the ATP concentration to 5 mM promoted sensitization also in the mutated rP2X7 receptor, accelerating the deactivation rate to typical WT values. YO-PRO1 uptake in cells expressing either the WT or the F288S P2X7 receptor was consistent with recorded membrane current data. Interestingly, in the human P2X7 (hP2X7) receptor, substitution Y288S did not change the deactivation rate, while the Y288F mutant generated a "rat-like" phenotype with a fast deactivation rate. Our combined experimental, kinetic, and molecular modeling data suggest that the rat F288S novel phenotype is due to a slower rate of ATP binding and/or unbinding and stabilization of nonsensitized receptor states

THE STUDY OF MAIN PHYSICAL-CHEMICAL PARAMETERS OF CHAENOMELES AND PRODUCTS OF ITS PROCESSING

In the article were considered the topical problems, connected with health worsening and human existence. The use of vegetable raw material as a source of biologically active components is prospective in production foodstuff. There were offered the rational methods of processing of chaenomeles for getting juice and puree. There were carried out an analysis of expedience of using chaenomeles and products of its processing for enrichment foodstuff. It was established, that maximal amount of phenol substances is contained in fruit peel and L-ascorbic acid - in flesh. It was determined, that apple acid prevails among organic ones, fructose - among sugars and phenol substances are mainly presented by procyanidins. Using chromotographic analysis in the products of chaenomeles processing were identified 48 names of aromatic compounds, alcohols, acids, ethers and unsaturated carbohydrates prevail among them. There were studied the physical-chemical parameters of fruit sauces and flour products with addition of chaenomeles processing products. The received results prove that the ready foodstuff that contain puree and juice of chaemomeles have the high organoleptic, physical-chemical parameters and also heightened biological value

ТЕОРЕТИЧНІ ПЕРЕДУМОВИ ТЕХНОЛОГІЇ КУЛІНАРНОГО НАПІВФАБРИКАТУ ДЛЯ ПЮРЕПОДІБНИХ ПЕРШИХ СТРАВ

The results of theoretical justification of the culinary semi product for the first dishes, that allow to speed up the process of soups puree cooking, expand its assortment in the institutions of restaurant household, are presented. It is determined, that among hydro colloids it is advisable to choose modified starches, that are able to cope with the temperature of pasteurization. For emulsion stabilization it is proposed to use surface active substances in the technology of the culinary semi product.   В статье проанализированы современные технологии полуфабрикатов для первых блюд и установлено, что большинство разработок касается сухих концентратов, которые имеют полностью сформирован вкусовой фон и требуют определенных условий восстановления. Представлены результаты теоретического обоснования технологии кулинарного полуфабриката для первых блюд, который позволяет ускорить процесс приготовления супов-пюре, расширить их ассортимент в заведениях ресторанного хозяйства. Определено, что среди гидроколоидив целесообразно использовать модифицированные крахмалы, которые способны выдерживать температуру пастеризации. Для стабилизации эмульсии предложено использование поверхностно-активных веществ (ПАВ) в технологии кулинарного полуфабриката.У статті проаналізовано сучасні технології напівфабрикатів для перших страв та встановлено, що більшість розробок стосується сухих концентратів, які мають повністю сформований смаковий фон та потребують певних умов відновлення. Представлено результати теоретичного обґрунтування технології кулінарного напівфабрикату для перших страв, що дозволяє прискорити процес приготування супів-пюре, розширити їх асортимент у закладах ресторанного господарства. Визначено, що серед гідроколоїдів доцільно обирати модифіковані крохмалі, які здатні витримувати температуру пастеризації.  Для стабілізації емульсії запропоновано використання поверхнево-активних речовин (ПАР) в технології кулінарного напівфабрикату. &nbsp

Selective Calcium-Dependent Inhibition of ATP-Gated P2X3 Receptors by Bisphosphonate-Induced Endogenous ATP Analog ApppI

Copyright © 2017 by The American Society for Pharmacology and Experimental Therapeutics. Pain is the most unbearable symptom accompanying primary bone cancers and bone metastases. Bone resorptive disorders are often associated with hypercalcemia, contributing to the pathologic process. Nitrogen-containing bisphosphonates (NBPs) are efficiently used to treat bone cancers and metastases. Apart from their toxic effect on cancer cells, NBPs also provide analgesia via poorly understood mechanisms. We previously showed that NBPs, by inhibiting the mevalonate pathway, induced formation of novel ATP analogs such as ApppI [1-adenosin-5'-yl ester 3-(3-methylbut-3-enyl) triphosphoric acid diester], which can potentially be involved in NBP analgesia. In this study, we used the patch-clamp technique to explore the action of ApppI on native ATP-gated P2X receptors in rat sensory neurons and rat and human P2X3, P2X2, and P2X7 receptors expressed in human embryonic kidney cells. We found that although ApppI has weak agonist activity, it is a potent inhibitor of P2X3 receptors operating in the nanomolar range. The inhibitory action of ApppI was completely blocked in hypercalcemia-like conditions and was stronger in human than in rat P2X3 receptors. In contrast, P2X2 and P2X7 receptors were insensitive to ApppI, suggesting a high selectivity of ApppI for the P2X3 receptor subtype. NBP, metabolite isopentenyl pyrophosphate, and endogenous AMP did not exert any inhibitory action, indicating that only intact ApppI has inhibitory activity. Ca2+-dependent inhibition was stronger in trigeminal neurons preferentially expressing desensitizing P2X3 subunits than in nodose ganglia neurons, which also express nondesensitizing P2X2 subunits. Altogether, we characterized previously unknown purinergic mechanisms of NBP-induced metabolites and suggest ApppI as the endogenous pain inhibitor contributing to cancer treatment with NBPs

Stable, synthetic analogs of diadenosine tetraphosphate inhibit rat and human P2X3 receptors and inflammatory pain

© 2016, © The Author(s) 2016.Background: A growing body of evidence suggests that ATP-gated P2X3 receptors (P2X3Rs) are implicated in chronic pain. We address the possibility that stable, synthetic analogs of diadenosine tetraphosphate (Ap4A) might induce antinociceptive effects by inhibiting P2X3Rs in peripheral sensory neurons. Results: The effects of two stable, synthetic Ap4A analogs (AppNHppA and AppCH2ppA) are studied firstly in vitro on HEK293 cells expressing recombinant rat P2XRs (P2X2Rs, P2X3Rs, P2X4Rs, and P2X7Rs) and then using native rat brain cells (cultured trigeminal, nodose, or dorsal root ganglion neurons). Thereafter, the action of these stable, synthetic Ap4A analogs on inflammatory pain and thermal hyperalgesia is studied through the measurement of antinociceptive effects in formalin and Hargreaves plantar tests in rats in vivo. In vitro inhibition of rat P2X3Rs (not P2X2Rs, P2X4Rs nor P2X7Rs) is shown to take place mediated by high-affinity desensitization (at low concentrations; IC50 values 100–250 nM) giving way to only weak partial agonism at much higher concentrations (EC50 values ≥ 10 µM). Similar inhibitory activity is observed with human recombinant P2X3Rs. The inhibitory effects of AppNHppA on nodose, dorsal root, and trigeminal neuron whole cell currents suggest that stable, synthetic Ap4A analogs inhibit homomeric P2X3Rs in preference to heteromeric P2X2/3Rs. Both Ap4A analogs mediate clear inhibition of pain responses in both in vivo inflammation models. Conclusions: Stable, synthetic Ap4A analogs (AppNHppA and AppCH2ppA) being weak partial agonist provoke potent high-affinity desensitization-mediated inhibition of homomeric P2X3Rs at low concentrations. Therefore, both analogs demonstrate clear potential as potent analgesic agents for use in the management of chronic pain associated with heightened P2X3R activation

Assessing the impact off chemicals on the job in the production off synthetic rubber

The aim was to evaluate the impact of complex chemical compounds, including carcinogens released during the manufacture of synthetic rubber on the health of workers.Целью исследований явилась оценка воздействия комплекса химических со-единений, в том числе канцерогенных, выделяющихся при производстве синтетического каучука, на здоровье работающих