Study on stress-strain state and deformations occurring in existing roller tables

The design of a new diverting roller table is presented, containing continuous series of sections with diverting rollers. Using the program product of finite element analysis of Autodesk Inventor, the stress-strain state rollers of the new outrigger roller table is calculated. It is proved that the maximum concentrations of stresses and deformations are observed in barrels and necks of rollers a new outrigger roller table. At the same time, the value of these indices is much smaller in comparison with the values of stresses and deformations occurring in existing roller tables

Study on stress-strain state and deformations occurring in existing roller tables

The design of a new diverting roller table is presented, containing continuous series of sections with diverting rollers. Using the program product of finite element analysis of Autodesk Inventor, the stress-strain state rollers of the new outrigger roller table is calculated. It is proved that the maximum concentrations of stresses and deformations are observed in barrels and necks of rollers a new outrigger roller table. At the same time, the value of these indices is much smaller in comparison with the values of stresses and deformations occurring in existing roller tables

Probing Reactivity and Substrate Specificity of Both Subunits of the Dimeric \u3ci\u3eMycobacterium tuberculosis\u3c/i\u3e FabH Using alkyl-CoA Disulfide Inhibitors and acyl-CoA Substrates

The dimeric Mycobacterium tuberculosis FabH (mtFabH) catalyses a Claisen-type condensation between an acyl-CoA and malonyl-acyl carrier protein (ACP) to initiate the Type II fatty acid synthase cycle. To analyze the initial covalent acylation of mtFabH with acyl-CoA, we challenged it with mixture of C6-C20 acyl-CoAs and the ESI-MS analysis showed reaction at both subunits and a strict specificity for C12 acyl CoA. Crystallographic and ESI-MS studies of mtFabH with a decyl-CoA disulfide inhibitor revealed a decyl chain bound in acyl-binding channels of both subunits through disulfide linkage to the active site cysteine. These data provide the first unequivocal evidence that both subunits of mtFabH can react with substrates or inhibitor. The discrepancy between the observed C12 acyl-CoA substrate specificity in the initial acylation step and the higher catalytic efficiency of mtFabH for C18-C20 acyl-CoA substrates in the overall mtFabH catalyzed reaction suggests a role for M. tuberculosis ACP as a specificity determinant in this reaction

Sanitary status of the Eurasian wild grapevine in the South Caucasian region

A prospecting on the sanitary status of the aerial organs and roots of the Eurasian wild grapevine, Vitis vinifera L. ssp. sylvestris (Gmelin) Hegi, was carried out on 14 natural populations situated along river bank forests, floodplains and colluvial positions in Georgia (Marneuli, Mtskheta and Gori districts, Gardabani Protected area and Lagodekhi Reserve), Armenia (Akhtala and Tavoush regions) and Azerbaijan (Quba region). These zones are included within the Holarctic kingdom, Eurosiberian region, and to the Caucasian, Euxine and Hyrcanian biogeographical provinces. The results of study indicate that roots are free of symptoms caused by phylloxera, rot fungi and root-knot nematodes. Symptoms caused by the erineum strain of Colomerus vitis (Pagenstecher) and Calepitrimerus vitis (Nalepa) (Acari, Eriophyidae) are frequent. On the other hand, damages caused by powdery and downy mildews, Erysiphe necator (Schweinitz) Burrill and Plasmopara viticola (Berkeley and Curtis) Berlease and de Toni), respectively, show an irregular intensity on leaves belonging to different vines from each location

Separate Entrance and Exit Portals for Ligand Traffic in Mycobacterium tuberculosis FabH

SummaryMycobacterium tuberculosis FabH initiates type II fatty acid synthase-catalyzed formation of the long chain (C16–C22) acyl-coenzyme A (CoA) precursors of mycolic acids, which are major constituents of the bacterial cell envelope. Crystal structures of M. tuberculosis FabH (mtFabH) show the substrate binding site to be a buried, extended L-shaped channel with only a single solvent access portal. Entrance of an acyl-CoA substrate through the solvent portal would require energetically unfavorable reptational threading of the substrate to its reactive position. Using a class of FabH inhibitors, we have tested an alternative hypothesis that FabH exists in an “open” form during substrate binding and product release, and a “closed” form in which catalysis and intermediate steps occur. This hypothesis is supported by mass spectrometric analysis of the product profile and crystal structures of complexes of mtFabH with these inhibitors

Alkyl-CoA Disulfides as Inhibitors and Mechanistic Probes for FabH Enzymes

SummaryThe first step of the reaction catalyzed by the homodimeric FabH from a dissociated fatty acid synthase is acyl transfer from acyl-CoA to an active site cysteine. We report that C1 to C10 alkyl-CoA disulfides irreversibly inhibit Escherichia coli FabH (ecFabH) and Mycobacterium tuberculosis FabH with relative efficiencies that reflect these enzymes' differential acyl-group specificity. Crystallographic and kinetic studies with MeSSCoA show rapid inhibition of one monomer of ecFabH through formation of a methyl disulfide conjugate with this cysteine. Reaction of the second subunit with either MeSSCoA or acetyl-CoA is much slower. In the presence of malonyl-ACP, the acylation rate of the second subunit is restored to that of the native ecFabH. These observations suggest a catalytic model in which a structurally disordered apo-ecFabH dimer orders on binding either the first substrate, acetyl-CoA, or the inhibitor MeSSCoA, and is restored to a disordered state on binding of malonyl-ACP

АНТИГЕЛЬМИНТНАЯ ЭФФЕКТИВНОСТЬ И ТИТРАЦИЯ ТЕРАПЕВТИЧЕСКИХ ДОЗ ОТЕЧЕСТВЕННОГО АНТИГЕЛЬМИН-ТИКА МИТРАНОКСА ПРИ МОНИЕЗИОЗЕ И НЕМАТОДОЗАХ ОВЕЦ

Efficacy of mitranox, a domestic anthhelmintic drug of the group of acetylated salicylanilides, is tested. Experiments were conducted on sheep spontaneously infected with Mоniezia expansa, М. benedini, gastrointestinal nematodes and Muel- lerius capillaris. Mitranox was administered at the dose of 50, 75 and 100 mg/kg orally, individually, as a single dose in form of water suspension. Efficacy of mi- tranox at moniesiosis at the dose of 50, 75 и 100 mg/kg made respectively 73,3 %, 94,2 и 100 %. The highest efficacy of mitranox applied at the dose of 100 mg/kg against nematodes, gastrointestinal strongylatosis, trichocephalosis and mulleriosis made respectively 97,4 %, 97,2; 86,9 and 93,2 %. The dose of 100 mg/kg is rec- ommended for treatment of moniesiosis and nematodosis in sheep.Проведено испытание эффективности митранокса - отечественного антигельминтного препарата из группы ацетиллированных салициланилидов. Опыты проводили на овцах, спонтанно инвазированных Mоniezia expansa, М. benedini, нематодами пищеварительного тракта и мюллериями. Митранокс задавали в дозах 50, 75 и 100 мг/кг перорально, индивидуально, однократно в форме водной взвеси. Эффективность митранокса при мониезиозе в дозах 50, 75 и 100 мг/кг составила соответственно 73,3 %, 94,2 и 100 %. Наибольшая эффективность против нематодир, стронгилят пищеварительного тракта, трихоцефал и мюллерий, 97,4 %, 97,2; 86,9 и 93,2 % соответственно, получена при применении препарата также в дозе 100 мг/кг. Доза митранокса 100 мг/кг рекомендована при мониезиозе и нематодозах овец

Peptidomimetic and Non- Peptidomimetic Derivatives as Possible SARS-CoV-2 Main Protease (Mpro) Inhibitors

To design novel inhibitors of the SARS-CoV-2 main protease (Mpro), we investigated the binding mode of the recently reported α-ketoamide inhibitors of this enzyme. Following, we utilized in-silico screening to identify 168 peptidomimetic and non-peptidomimetic compounds that are high probability Mpro binding candidates. The compounds were synthesized in 5 to 10 mg for initial screening for their potential inhibition of Mpro using Fluorescence Resonance Energy Transfer (FRET) assay. The study was conducted using the main protease, MBP-tagged (SARS-CoV-2) Assay Kit (BPS Bioscience, #79955-2), and the fluorescence due to enzymatic cleavage of substrate measured using BMG LABTECH CLARIOstar™, a fluorescent microplate reader, with an excited/emission wavelength of 360 nm/460 nm, respectively. The FRET assay showed 29 compounds to exhibit lower fluorescence compared to the positive control, indicating inhibitory activity, with three of the compounds exhibiting over 50% enzymatic inhibition. The assay average scores were plotted as dose inhibition curves using variable parameter nonlinear regression to calculate the IC50 values. To design more potent inhibitors, an in-silico molecular docking simulation using the SARS-CoV-2 Mpro crystal structure was conducted to investigate on a molecular level the key binding residues at the active site, as well as the possible binding modes and affinity of the lead inhibitors. Additionally, an in-silico study of the compounds\u27 molecular properties and physicochemical profiles was performed to predict their pharmacokinetic properties and assess their suitability as potential orally active drug candidates.https://scholarscompass.vcu.edu/gradposters/1139/thumbnail.jp

ИНСТРУМЕНТАЛЬНО-БИОФИЗИЧЕСКИЙ МЕТОД ОЦЕНКИ КАЧЕСТВА СЕМЯН ЗЕЛЕННЫХ ОВОЩНЫХ КУЛЬТУР

Questions of quality of the sowed seeds in agriculture have paramount value. Use of highquality uniform seeds is the key to successful production of crop production. Vegetable seeds, in particular, leaf vegetables, are most vulnerable in this plan in view of their shallow amount, the long period of fructing time and some other factors. The modern tool methods of evaluation test allow to glance in internal structure of seeds and to scoop more information. The most suitable for these purposes is us the developed method of microfocal X-ray of vegetable seeds. In this work seeds of different types of green and spicy and flavoring vegetable crops are analysed: melissa, marjoram, asparagus, spinach and garden cress. The analysis was carried out both by a method of r of seeds, and by a standard technique. The most typical defects and shortcomings of internal structure of seeds influencing their economic and biological indicators are identified. Comparison of methods is carried out. It is shown that X-ray analysis of quality of seeds, in particular, viability, by visualization of images efficient and rather precise. The small error of a method is compensated with its bigger informational content: that is, the analysis is carried out not by the principle of viable and not viable seeds, there is their division as on viability (full, low quality), and on defects and shortcomings (outstanding, ugly, the defective, injured, etc.). At the same time seeds as a result of the analysis aren't utilized and remain for further work. The method differs in speed and ease of execution. The prospects of development of a method are specified. It is the integrated automatic analysis of quality of seeds. The algorithm of automatic computer X-ray analysis of quality of vegetable seeds is so far developed, the first version of the program is approved.Вопросы качества высеваемых семян в земледелии имеют первостепенное значение. Использование высококачественных однородных семян является залогом успешного производства продукции растениеводства. Семена овощных культур, в частности, зеленных и пряно-вкусовых, наиболее уязвимы в этом плане ввиду мелких их размеров, длительного периода плодоношения и ряда других факторов. Современные инструментальные методы оценки качества позволяют заглянуть во внутреннюю структуру семян и черпать больше информации. Наиболее подходящим для этих целей является нами разработанный метод микрофокусной рентгенографии семян овощных культур. В данной работе проанализированы семена различных видов зеленных и пряно-вкусовых овощных культур: мелиссы, майорана, спаржи, шпината и кресс-салата. Анализ проводился как по методу рентгенографии семян, так и по стандартной методике. Идентифицированы наиболее типичные дефекты и недостатки внутренней структуры семян, влияющие на их хозяйственно-биологические показатели. Проведено сравнение методов. Показано, что рентгенографический анализ качества семян, в частности, жизнеспособности, путем визуализации изображений эффективный и достаточно точный. Небольшая погрешность метода компенсируется с его большей информативностью: то есть, анализ проводится не по принципу всхожих и невсхожих семян, идет их разделение как по жизнеспособности (полноценные, некондиционные), так и по дефектам и недостаткам (невыполненные, уродливые, поврежденные, травмированные и др.). В то же время семена в результате анализа не утилизируются и сохраняются для дальнейшей работы. Метод отличается быстротой и легкостью исполнения. Указаны перспективы развития метода. Это полный автоматический анализ качества семян. К настоящему времени разработан алгоритм автоматического компьютерного рентгенографического анализа качества семян овощных культур, апробирована первая версия программы

СРОКИ ВЫВЕДЕНИЯ ФЕНБЕНДАЗОЛА ИЗ ОРГАНИЗМА ЛОШАДЕЙ ПОСЛЕ ЛЕЧЕНИЯ ПРАЗИФЕНOМ

The terms of elimination of fenbendazole from horses body after prazifen treatment were established by the method of highly effective liquid chromatography. In 10 days after treatment fenbendazole and its metabolite oxfendazole were not found in horses' organism.Методом высокоэффективной жидкостной хроматографии установлены сроки выведения фенбендазола из организма лошадей после их дегельминтизации празифеном. Через 10 сут после лечения фенбендазол и его метаболит оксфендазол в организме лошадей не обнаруживают