Experimental Study of Antispasmodic Activity of 2-Oksoindolin-3-Glyoxylic Acid Derivatives

Clinical psychiatry and neurology requires a creation of new means with difficult many component range of psychotropic action, so psychoemotional disturbances ＂boundary type＂ and difficult mental disorders have high level of heterogeneity, various clinical manifestations, which are caused by different pathogenetic factors. One of the most often used preparation for the treatment of these diseases is anxiolytic medications. It is known that anxiolytic action combines with anticonvulsive. Perspective medications are simple amides and ethers of 2-oksoindolin-3-glyoxylic acid, which have not recognized and practically observed. The aim of this research is to determine anticonvulsant action in 2-oksoindolin-3-glyoxylic acid derivatives on the model of acute myoclonic pentylentetrazol, piktrotoxic, and bikukullin convulsions. In experiments on mature mice of both sex Wistar line were studied an influence of ethyl ester 4-[2-hydroxy-2-（2-oxo-1,2-dihydro-indol-3-ylidene）-acetylamino]-butyric acid and 2-hydroxy-N-naphthalen-l-yl-2-（2-oxo-l,2-dihydro-indol-3-ylidene）-acetamide on chemoinduced epileptogenesis. An intake of proconvulsants is accompanied by a development of syndrome convulsion, which was estimated by convulsion＇s intensity （grades）, latent period of convulsions （sec.）, number of convulsions acts, and duration of convulsions （sec.） and number of survived animals in a group. It was showed that a combination of 2-hydroxy-N-naphthalen-1-yl-2-（2-oxo-1,2-dihydro-indol-3-ylidene）-acetamide （12 acetamide mg/kg） is similar to reference preparation diazepam in （2 mg/kg） which decreased a manifestation of syndrome convulsion. It demonstrated an increase of intensity of convulsions, decrease of latent period of the convulsion＇s start which is caused by all blockers GAMKA-receptors, decrease of number convulsive acts on the background of korazol and pikrotoxin, a decrease of convulsive syndrome duration during an intake ofkorazol and bikukullin, and a decrease of animal＇s mortalit     

Combined In Silico,Ex Vivo,and In Vivo Assessment of L-17, a Thiadiazine Derivative with Putative Neuro- and Cardioprotective and Antidepressant Effects

Depression associated with poor general medical condition, such as post-stroke (PSD) or post-myocardial infarction (PMID) depression, is characterized by resistance to classical antidepressants. Special treatment strategies should thus be developed for these conditions. Our study aims to investigate the mechanism of action of 2-morpholino-5-phenyl-6H-1,3,4-thiadiazine, hydrobromide (L-17), a recently designed thiadiazine derivative with putative neuro- and cardioprotective and antidepressant-like effects, using combined in silico (for prediction of the molecular binding mechanisms), ex vivo (for assessment of the neural excitability using c-Fos immunocytochemistry), and in vivo (for direct examination of the neuronal excitability) methodological approaches. We found that the predicted binding affinities of L-17 to serotonin (5-HT) transporter (SERT) and 5-HT₃ and 5-HT_1A receptors are compatible with selective 5-HT serotonin reuptake inhibitors (SSRIs) and antagonists of 5-HT₃ and 5-HT_1A receptors, respectively. L-17 robustly increased c-Fos immunoreactivity in the amygdala and decreased it in the hippocampus. L-17 dose-dependently inhibited 5-HT neurons of the dorsal raphe nucleus; this inhibition was partially reversed by the 5-HT_1A antagonist WAY100135. We suggest that L-17 is a potent 5-HT reuptake inhibitor and partial antagonist of 5-HT₃ and 5-HT_1A receptors; the effects of L-17 on amygdaloid and hippocampal excitability might be mediated via 5-HT, and putatively mediate the antidepressant-like effects of this drug. Since L-17 also possesses neuro- and cardioprotective properties, it can be beneficial in PSD and PMID. Combined in silico predictions with ex vivo neurochemical and in vivo electrophysiological assessments might be a useful strategy for early assessment of the efficacy and neural mechanism of action of novel CNS drugs.     

The Effect of Duration of Amidation of Fatty Acids with Diethanolamine on the Surfactant Properties

The effects of the duration of direct amidation of fatty acids (FA) with diethanolamine on the composition of the products obtained, their surface-active properties, and ability to stabilize water-in-oil emulsions are studied using the example of tall oil distillate. A certain range of synthesis time that corresponds to the maximum content of diethanolamides in the reaction products, and, as a consequence, the highest surface-active and emulsifying properties of the products is shown to exist. An increase in the synthesis duration time leads to a deterioration of these properties due to accumulation of the products of secondary reactions. A new mechanism of the amidation process that includes secondary transformations of diethanolamine and its condensation products with FA into 1,4-bis(2-hydroxyethyl)piperazine derivatives is proposed. The structures of by-products are confirmed using high-performance liquid chromatography-mass spectrometry (HPLC–MS), infrared (IR), and nuclear magnetic resonance (NMR) spectroscopy methods. It is concluded that the acid value of the product as well as the amount of water released during the synthesis cannot serve as a reliable criterion for completion of the process.     

Effect of operating conditions on catechin extraction from betel nuts using supercritical CO2-methanol extraction

In this work, the effect of extraction parameters on catechin extraction from betel nuts was studied. The supercritical carbon dioxide extraction parameters were pressure, temperature, and solvent flow rate while using average particle size of 177.5 μm and 5% (v/v) methanol as modifiers. Detection and quantification of catechin were achieved using HPLC analysis. The highest amount of extract and catechin concentration were 34.00 mg extract/g sample and 565.38 ppm of catechin obtained at 30 MPa, 70°C, and 4 mL/min. The results given by optimization tools suggest the same operating conditions with less than 3% difference.     

Using Blockchain Technology in Mobile Network to create decentralized Home Location Registry (HLR)

Blockchain can mean many things to many people. It is a set of protocols and encryption technologies for securely storing data on a distributed network for the developers. It is a distributed ledger for business and finance and the technology underlying the explosion of new digital currencies. For technologists, it is the driving force behind the next generation of the internet. On the other hand, it is a transformational technology facilitating large-scale human progress in previously unimagined ways for the rest of the people, a tool for radically reshaping society and economy. Some view it as a disruptive technology that can be the source of a great deal of fraud, illegal activity, where others see opportunities to bring into existing systems by providing decentralization, transparency, and efficiency. This complex technological, economic, and social phenomenon has been the subject of fervent debate. It calls into question what might have been seen to be established parameters of the modern world like currency, economics, trust, value, and exchange. It is a revolutionary new computing paradigm and one of the most significant, fundamental digital platforms’ advances since the internet. It is an emergent technology experiencing very rapid evolution, and so is our understanding of what it is and what it can be. This paper is subject to the use of Blockchain concepts in mobile networks to strengthen the Home Location Registry (HLR) database and make it decentralized for secure transactions and in banking and financial centers. Blockchain also holds potential implications for global commerce. It could make trade more efficient by removing the manual and paper-based processes and introducing streamlined and automated processes.