bluuebunny/crossref_metadata_2025 huggingface dataset:
Effects of Flotation Deinking on Environmentally Friendly Offset Paper Printing Ink
Authors: Yang Shujie , Shen Jianbin , He Tiefei , Chen Chao , Wang Junming , Tang Yanjun
Published: January 2022

Waste paper has become a promising raw material for the pulp and paper industry due to its low cost and because it is conducive to sustainable development. Unfortunately, waste paper contains a high volume of printed paper that is difficult to deink, which restricts its applications. Flotation deinking plays an essential role in the product quality and process cost of wastepaper recycling. This study was performed to evaluate the deinkability of environmentally friendly offset inks by flotation deinking. For this purpose, three series of four-color inks, namely, hybrid light emitting diode ultraviolet (LED‒UV), LED‒UV, and vegetable oil‒based inks, were printed on white lightweight coated papers under laboratory conditions. The deinking methodology involves repulping, deinking agent treatment, flotation, hand sheet making, and evaluation of the produced hand sheets. The obtained results indicated that the hybrid LED‒UV prints had the best deinkability. After flotation deinking, the deinking efficiency and the whiteness of the hybrid LED‒UV ink increased by 58.1% and 47.6%, respectively. LED‒UV ink had a 46.9% increase in the deinking efficiency and a 37.0% increase in the whiteness of the hand sheet. The deinking efficiency of the vegetable oil‒based ink was the lowest, at 42.1%, and the whiteness of the hand sheet increased only by 23.8%. The particle size distribution analysis demonstrated that the hybrid LED‒UV four-color ink exhibited a larger value of the average particle size than the two other. Scanning electron microscopy revealed that the hybrid LED‒UV ink particles on the surface of the fibers were the least abundant after deinking. The physical strength properties of the hand sheets, including tensile index, folding resistance, and cohesion of the hybrid LED‒UV, LED‒UV inks, and vegetable oil‒based inks, increased.
Greening Global Egalitarianism?
Authors: Mancilla Alejandra
Published: January 2022

In Justice and Natural Resources: An Egalitarian Theory (2017), Chris Armstrong proposes a version of global egalitarianism that – contra the default renderings of this approach – takes individual attachment to specific resources into account. By doing this, his theory has the potential for greening global egalitarianism both in terms of procedure and scope. In terms of procedure, its broad account of attachment and its focus on individuals rather than groups connects with participatory governance and management and, ultimately, participatory democracy – an essential ingredient in the toolkit of green politics and policy-making. In terms of scope, because it does not commit itself to any particular moral framework, Armstrong’s theory leaves the door open for non-human animals to become subjects of justice, thus extending the realm of the latter beyond its traditionally anthropocentric borders. I conclude that these greenings are promising, but not trouble-free.
Special Claims from Improvement: A Comment on Armstrong
Authors: Heyward Clare , Lenzi Dominic
Published: January 2022

Chris Armstrong argues that attempts at justifying special claims over natural resources generally take one of two forms: arguments from improvement and arguments from attachment. We argue that Armstrong fails to establish that the distinction between natural resources and improved resources has no normative significance. He succeeds only in showing that ‘improvers’ (whoever they may be) are not necessarily entitled to the full exchange value of the improvement. It can still be argued that the value of natural and improved resources should be distributed on different grounds, but that the value of improvements should be conceived differently.
Determining the Optimum Night Length for Flower Development in a Modern Poinsettia Cultivar
Authors: Alden Michael , Faust James E.
Published: January 2022

The effect of night length (NL) on the flower development of poinsettia (Euphorbia pulcherrima Willd. ex Klotzsch) ‘Prestige Red’ was evaluated. Flower initiation occurred by subjecting plants to a 14-hour NL for 10 or 17 days, termed short-day (SD) treatments, and then transferring the plants to each of four NL treatments (11, 12, 13, or 14 hours) to observe the effects of NL on flower development. The plants grown continuously with the 14-h NL treatment were the control group. The timing of first color, visible bud, and anthesis were recorded during flower development, and bract and leaf data were collected at anthesis. Leaf number was unaffected by the SD or NL treatments, suggesting that flower initiation occurred during the 10-day SD treatment before the start of NL treatments; thus, the NL treatments only affected flower development. The timing of first color and visible bud were significantly delayed with the 10-day SD × 11-hour NL treatment relative to the 14-hour NL control; however, first color and visible bud were not delayed with the 17-day SD × 11-hour NL treatment. The 11-hour NL treatment resulted in fewer plants reaching anthesis, and these plants had fewer stem bracts and less bract color development compared with the 12-hour, 13-hour, and 14-hour NL treatments. Therefore, an 11-hour NL is suboptimal for flower development; nonetheless, significant development did occur. The 12-hour NL resulted in less color development than the 13-hour and 14-hour NL treatments in the lowest stem bract positions, but the plants had a commercially acceptable appearance. These results demonstrate that minimal differences in flower development occur with NL ≥12 hours, but that optimal development required NL ≥13 hours.
History of Controlled Environment Horticulture: Indoor Farming and Its Key Technologies
Authors: Mitchell Cary A.
Published: January 2022

The most recent platform for protected horticultural crop production, with the shortest history to date, is located entirely indoors, lacking even the benefit of free, natural sunlight. Although this may not sound offhand like a good idea for commercial specialty-crop production, the concept of indoor controlled-environment plant growth started originally for the benefit of researchers—to systematically investigate effects of specific environmental factors on plant growth and development in isolation from environmental factors varying in uncontrolled ways that would confound or change experimental findings. In addition to its value for basic and applied research, it soon was discovered that providing nonlimiting plant-growth environments greatly enhanced crop yield and enabled manipulation of plant development in ways that were never previously possible. As supporting technology for indoor crop production has improved in capability and efficiency, energy requirements have declined substantially for growing crops through entire production cycles in completely controlled environments, and this combination has spawned a new sector of the controlled-environment crop-production industry. This article chronicles the evolution of events, enabling technologies, and entrepreneurial efforts that have brought local, year-round indoor crop production to the forefront of public visibility and the threshold of profitability for a growing number of specialty crops in locations with seasonal climates.
High Tunnel Coverings Alter Crop Productivity and Microclimate of Tomato and Lettuce
Authors: Gude Kelly M. , Pliakoni Eleni D. , Cunningham Brianna , Ayub Kanwal , Kang Qing , Rajashekar Channa B. , Rivard Cary L.
Published: January 2022

The implementation of high tunnels has shown to increase marketability and/or yield of tomato (Solanum lycopersicum) and lettuce (Lactuca sativa) crops compared with open-field systems. These structures provide the opportunity to alter light intensity and spectral quality by using specific polyethylene (poly) films and/or shadecloth, which may affect microclimate and subsequent crop productivity. However, little is known about how specific high tunnel coverings affect these parameters. The overall goal of this study was to evaluate the impact of various high tunnel coverings on the microclimate and crop productivity of tomato and lettuce. The coverings included standard, ultraviolet (UV)-stabilized poly film (standard); diffuse poly (diffuse); full-spectrum clear poly (clear); UV-A/B blocking poly (block); standard + 55% shadecloth (shade); and removal of standard poly 2 weeks before initial harvest to simulate a movable tunnel (movable). Microclimate parameters that were observed included canopy and soil temperatures, canopy growing degree-days (GDD), and photosynthetic active radiation (PAR), and crop productivity included yield and net photosynthetic rate. Hybrid red ‘BHN 589’ tomatoes were grown during the summer, and red ‘New Red Fire’ and green ‘Two Star’ leaf lettuce were grown in both spring and fall in 2017 and 2018. Increased temperature, GDD, and PAR were observed during the spring and summer compared with the fall. The soil temperatures during the summer increased more under the clear covering compared with the others. For tomato, the shade produced lower total fruit yield and net photosynthetic rate (Pn) compared with the other treatments, which were similar (P < 0.001 and <0.001, respectively). The greatest yield was 7.39 kg/plant, which was produced under the clear covering. For red leaf lettuce grown in the spring, the plants under the clear, standard, and diffuse coverings had significantly greater yield than the movable and shade coverings (P < 0.001). The coverings had less effect on the yield during the fall lettuce trials, which may have been attributed to the decrease in PAR and environmental temperatures. The findings of this study suggest that high tunnel coverings affect both microclimate and yield of lettuce and tomato.
Study of a segmented ventilation system of the brake disc and determination of the aerodynamic and heat exchange characteristics of the airflow
Authors: Polyakov P. A.
Published: January 2022

This study aims determine a relationship between the aerodynamic and heat exchange characteristics of the air flow in a segmented ventilation system of the brake disc with improved heat dissipation in the boundary layer of the air flow. Classical equations of heat and mass transfer in the boundary layer of the air flow cooling the brake disc ventilation chamber were used. The cooling performance of the system was assessed using the method of similarity. The obtained theoretical findings were confirmed by CFD-modelling. Mathematical models were developed for vented discs with both continuous grooves and slotted grooves. A criterion for assessing the performance of brake disc ventilation systems was proposed, consisting in turbulization of the air flow inside the device under study. According to the obtained analytical dependencies, a 20-fold acceleration of the air flow decreases the turbulization parameter by 1.24 times. An increase in the temperature difference in the boundary layer by 8 times leads to an increase in the turbulization parame-ter by 86.2 times. Using the criterion proposed for assessing the work performance, the aerodynamic and heat exchange characteristics of the system under study were calculated. As a result, a relationship between the design parameters of the segmented ventilation system and improved heat dissipation in the boundary layer of the cooling air flow is proposed. The conducted CFD modelling confirmed the aerodynamic characteristics of the system under study obtained theoretical-ly. This mathematical model together with the turbulization parameter can be used when both developing modern vented brake discs and assessing the existing cooling systems of friction units in order to minimize the possibility of reduced heat exchange processes.
Power management of variable capacitors in electrical grid systems according to the criterion of mini-mum energy loss
Authors: Girshin S. S. , Andreeva E. G. , Khatsevskiy K. V. , Trotsenko V. M. , Melnikov N. A. , Petrova E. V. , Goryunov V. N.
Published: January 2022

The aim is to manage the transmitted reactive power in electrical grids using variable capacitor batteries according to the criterion of minimum energy loss under different annual reactive load schedules and different numbers of variable capacitor sections. The main theoretical relations were obtained by the methods of mathematical modelling and integral calculus using the theory of optimal control. The influence of the power and number of sections in a capacitor battery on energy losses in the grid was estimated using computational experiments. Dependencies for energy losses in a capacitor battery, as well as for reducing energy losses in the grid, were obtained. These expressions are valid for linearized load schedules. It is shown that the dependences of energy losses in a capacitor battery and the reduction of losses in the grid on the section power have inflection points and pass through a maximum. The presence of inflection points is associated with a change in the number of capacitor sections operating throughout the year. The presence of a maximum is explained by the fact that, with an increase in the power of the capacitor battery, its operating time decreases under the complete number of variable sections. It is established that the batteries of static capacitors with two variable sections can reduce energy losses when transmitting reactive power by over 90%. For three- and four-section static capacitors, the loss reduction is close to 100%. The reduction in energy losses increases when approaching maximal levels of annual reactive load. Energy losses in electrical grid systems can be reduced by capacitor batteries with no more than three or four variable sections. In most cases, this can be achieved by two-section capacitor batteries.
Tuberculosis Situation in Volga Federal District in 2016-2020
Authors: Yunusbaeva M. M. , Borodina L. Ya. , Sharipov R. A. , Bilalov E. S. , Аzamatova M. M. , Yunusbaev B. B.
Published: January 2022

The objective of the study: to assess changes in the incidence and prevalence of multiple drug resistant tuberculosis (MDR TB) and TB/HIV coinfection (TB/HIV) in Volga Federal District (VFD) and its regions during 2016-2020.

Subjects and Methods. Data from FGSN Forms No. 8, 33, and 61, and analytical reviews of main statistical TB rates in the Russian Federation have been studied. The number of those died is presented as per the Rosstat data.

Results. An increase in the incidence and prevalence of MDR TB and TB/HIV coinfection has been detected in certain region of Volga Federal District. Perm Region, the Republic of Bashkortostan, the Republic of Udmurtia, and Orenburg and Samara Regions have the highest prevalence of MDR TB and TB/HIV coinfection. In 2020, the Republic of Bashkortostan was the only region where the incidence and prevalence of MDR TB were growing (164.7% and 47.3%, respectively). The highest incidence and prevalence of TB/HIV coinfection was reported in the Republic of Bashkortostan, Perm Kray, Orenburg Region, the Chuvash and Udmurt Republics. Over the last 5 years, the maximum increase in TB/HIV incidence and prevalence was observed in the Republic of Bashkortostan (38.8% and 41.3%, respectively).
Evaluation of the role of rs2227983 polymorphism of EGFR gene in the development of allergic asthma
Authors: Аveryanov A. B. , Cherkashina I. I. , Nikulina S. Yu. , Kuznetsova E. Yu. , Maksimov V. N.
Published: January 2022

The objective of the study: to study rs2227983 polymorphism of EGFR gene in patients with allergic asthma and healthy individuals.

Subjects and Methods. 179 patients suffering from allergic asthma were included in the study. The diagnosis and degree of severity were established in accordance with the GINA recommendations. The Control Group included apparently healthy individuals (n = 217). Patients with allergic asthma underwent standard laboratory and instrumental examinations and DNA typing.

Results. A statistically significant predominance of AG genotype frequency in the group of patients with allergic asthma, including women, versus the group of healthy individuals, was established. AG rs2227983 genotype of EGFR gene was found to be significantly more common in patients with mild and moderate allergic asthma including women, than in healthy individuals, including women.

Conclusion. The association of rs2227983 polymorphism of EGFR gene with allergic asthma has been established. A homozygous GG genotype may play a protective role against the disease.
A clinical case of concurrent mycoplasma pneumonia and dengue hemorrhagic fever in a tourist from Thailand
Authors: Rozanova N. A. , Sayfullin M. A. , Zvereva N. N. , Larichev V. E. , Grigorieva Ya. E. , Butenko A. M.
Published: January 2022

The article describes a clinical case of concurrent infectious diseases - dengue hemorrhagic fever and mycoplasma pneumonia in a patient who came back from the area endemic for dengue fever. Further, the patient was diagnosed with clostridial colitis which was the complication. Clinical, laboratory, and radiological parameters used in the diagnosis of diseases were evaluated.
How clay delamination supports aseismic slip
Authors: Zhou Huijun , Chen Meng , Zhu Runliang , Zhu Jianxi , He Hongping
Published: January 2022

Aseismic slip is a stable fault slip, which allows strain to be relieved smoothly. Aseismic slip prevents the earthquake propagation, but it could nucleate an earthquake elsewhere. Understanding the mechanism of aseismic slip is promising in revealing the seismic cycle. Experimental evidence showed clay-rich fault gouge bears a low-friction strength, and the friction is strengthened with slip velocity (velocity-strengthening), which was thought to support aseismic slip. Clay minerals are comprised of platy crystalline layers with water intercalated between them, which may act as a lubricant. Sliding between clay layers was suspected to support aseismic slip but lacked a clarified mechanistic insight. We use non-equilibrium molecular dynamics simulations to show that shear-induced interlayer sliding is frictionally weak and velocity-strengthening, which evidences the role of clay minerals in aseismic slip. We find that interlayer water is a viscous fluid at most times, which explains the shear response of interlayer sliding. Depending on temperature and pressure conditions, intercalated water can be monolayer or bilayer, fluidic or ice like. Shear induces ice-like water to transform into fluidic water, which happens as a stick-slip phenomenon reflecting a first-order transition. Increased pore fluid pressure leads to the transformation from monolayer to bilayer intercalated water, resulting in a lower friction strength and enhanced velocity-strengthening behavior. Our work suggests that disclosing the hydration state of a clay mineral is preliminary when studying fault mechanics.
Effects of hydrostaticity and Mn-substitution on dolomite stability at high pressure
Authors: Wang Faxiang , Zhao Chaoshuai , Xu Liangxu , Liu Jin
Published: January 2022

Studying the structural evolution of the dolomite group at high pressure is crucial for constraining the deep carbon cycle and mantle dynamics. Here we collected high-pressure laser Raman spectra of natural Mg-dolomite CaMg(CO3)2 and Mn-dolomite kutnohorite Ca1.11Mn0.89(CO3)2 samples up to 56 GPa at room temperature in a diamond-anvil cell (DAC) using helium and neon as a pressure-transmitting medium (PTM), respectively. Using helium or neon can ensure samples stay under relatively hydrostatic conditions over the investigated pressure range, resembling the hydrostatic conditions of the deep mantle. Phase transitions in CaMg(CO3)2 were observed at 36.1(25) GPa in helium and 35.2(10) GPa in neon PTM from dolomite-II to -III, respectively. Moreover, the onset pressure of Mn-dolomite Ca1.11Mn0.89(CO3)2-III occurs at 23−25 GPa, about 10 GPa lower than that of Mg-dolomite-III, suggesting that cation substitution could significantly change the onset pressure of the phase transitions in the dolomite group. These results provide new insights into deep carbon carriers within the Earth’s mantle.
PNEUMOCYSTIS IN PATIENTS LIVING WITH HIV: EXPERIENCE OF THE INFECTIOUS DISEASES DEPARTMENT OF CHU MOHAMED VI-MARRAKECH
Authors:   Infectious Diseases Service CHU Mohamed VI Marrakech- Cadi Ayaad University., Etoughe N. F. , Ihbibane F. ,   Infectious Diseases Service CHU Mohamed VI Marrakech- Cadi Ayaad University., Annaoui M.El ,   Infectious Diseases Service CHU Mohamed VI Marrakech- Cadi Ayaad University., Mezouari M.El ,   Parasitology Mycology Department Avicenne Military Hospital Marrakech., Moutaj R. ,   Parasitology Mycology Department Avicenne Military Hospital Marrakech., Tassi N. ,   Infectious Diseases Service CHU Mohamed VI Marrakech- Cadi Ayaad University.
Published: January 2022

Pneumocystis is the most serious and common respiratory opportunistic infection after tuberculosis during HIV infection. To describe the epidemiological, clinical, therapeutic and evolutionary aspects of HIV-infected patients who presented with pneumocystis. Retrospective study of the records of 45 HIV-infected patients followed at the Department of Infectious Diseases of the CHU Mohamed VI and hospitalized for Pneumocystis jirovecii infection between January 2007 and March 2021. Out of 1286 HIV-infected patients followed at the department during the study period, 45 patients (3.5%) had pneumocystis. Pneumocystis was inaugural to HIV infection in 36 cases (80%). The predominance was male in 63% of cases (28 males to 17 females), with an average age of 35.5 years [16-64 years]. The mean TCD4 cell count was 74 cells/mm3 [0- 656 cells/mm3]. The mean LDH level was 874.89 IU/L. The clinical picture was marked by cough in 84% of cases and dyspnea in 64% of cases. The most frequent radiological signs were a diffuse interstitial syndrome in 84.4% of cases on chest X-ray and ground glass appearance in 63% of cases on chest CT. The diagnosis of pneumocystis was confirmed in 16 patients by the detection of Pneumocystis jIrovecii in sputum and BAL. All our patients were treated with Trimethoprim-Sulfamethoxazole combination. Antiretroviral treatment was started in 32 patients, i.e. 71% of the patients, with a favorable evolution in 24 patients, i.e. 53%. Pneumocystis is a serious infection in immunocompromised patients especially PLHIV. In Morocco, it is still frequent during HIV infection and is one of the main causes of death.
ASSESSMENT OF THE USE OF DIGITAL SERVICES FOR SOCIAL AND POLITICAL ACTIVITY BY THE RESIDENTS OF THE TYUMEN REGION
Authors: BATYREVA Maria V. , KARAGULYAN Egine A.
Published: January 2022

In recent decades, the forms of social and political participation and interaction between authorities and citizens have expanded due to the development of modern information and communication technologies. According to most scientists, modern technologies will allow citizens to be heard by the authorities, as well as to actively participate in social and political processes. At the same time, the level of demand and the real use of smart technologies by citizens for socio-political activity, in our opinion, largely depend on the level of their information competence and civic-mindedness.
The purpose of this study is to assess the demand, analyze the nature and purpose of the use of modern digital services for social and political activity of the residents of the Tyumen region. The article is based on the sociological study conducted in the summer of 2021 through a questionnaire survey of the residents of cities and rural municipal districts in the south of the Tyumen region.
The article presents the results of a study on the level of digital competence of the region’s residents, their awareness of the existing “smart” technologies in the country and the region to manifest socio-political activity, as well as the demand for these technologies. The article also presents an analysis of the purpose of the use of electronic services and the specific nature of these forms of interaction between the authority and the population (political, non-political).
It was found out that electronic resources are used by 40% of the population to express their civic-mindedness, and they are more often used by respondents with a higher level of information competence. Most residents of the region are at lower levels of political participation, their interaction with the authorities is mainly limited to information sharing. The share of the population with a higher level of participation is small and is represented by members of political parties and public organizations.
URGENT ISSUES OF LEGAL REGULATION IN THE FIELD OF PROTECTION OF POPULATION AND TERRITORIES IN EMERGENCY SITUATIONS
Authors: DEMCHENKO Maxim S.
Published: January 2022

On January 30, 2020, the spread of a new coronavirus infection was declared an international emergency by the World Health Organization. The state authorities of the Russian Federation have developed measures aimed at minimizing and eliminating the consequences caused by coronavirus infection, which in turn caused the need for rapid changes and additions to the regulatory framework in the field of protecting the population and territories from emergency situations.
The question on the features of the emergency and high-alert mode, as well as the legality of restrictions on individual rights and freedoms introduced in the high-alert mode, has caused a scientific discussion in the field of protecting the population and territories from emergency situations. In this article, the author examines changes in legislation in this field, offers his interpretation of the basis and features of the legal regulation of the high-alert mode and restrictions on the rights and freedoms of an individual associated with the spread of the COVID-19 coronavirus infection.
According to the author, taking into account the current epidemiological situation, Federal Law No. 68-FZ of December 21, 1994, “On the protection of the population and territories from natural and man-made emergencies” needs prompt and consistent changes in order to fully and comprehensively ensure the rights and freedoms of an individual. For example, it is necessary to introduce the concept of a biological and social emergency as one of the types of emergency situations that fall under legislative regulation. Analyzing the current legislation for legality of the introduced high-alert mode and restrictions on individual rights and freedoms, it is concluded that the existing mechanism for restricting individual rights and freedoms does not fully comply with the Constitution of the Russian Federation. Regarding the current epidemiological situation, it should be considered as an emergency situation with the need for introducing an appropriate mode.
The research methodology is based on both general scientific and specific scientific methods of cognition: formal-logical, systematic, formal-legal, comparative, dialectical, predictive, modeling method, etc.
FREELANCING IN DIGITAL PROFILES: A CONTENT ANALYSIS EXPERIENCE
Authors: ANDRIANOVA Elena V. , ELYSHEV Egor I.
Published: January 2022

Nowadays, the issue of self-employment is extremely urgent and it requires attention as its significance and prevalence will only grow. The Russian self-employed are mostly concentrated in traditional kinds of business and occupied with low-skilled activities, and cannot demonstrate an outstanding level of innovative potential. Nevertheless, thanks to the active development of information society, its digitalization and the wide spread of the Internet, the number of highly qualified self-employed professionals, engaged mainly in intellectual work, who stand out from the general pool of the self-employed, is growing rapidly in our country. In their job, they actively use technology and work mainly through Internet-based remote work websites. Considering marked differentiation within the pool of self-employed, in order to concretize the portrait of an online freelancer, we conducted a content analysis of personal pages of freelancers in the “Best Performers” category of FL.ru website, which is the largest Russian-language remote work website. The method consisted of a mass observation of the presented profiles. The results made it possible to describe the socio-demographic characteristics of freelancers, make conclusions about the professional composition of the “Best Performers”, identify the most popular specializations and determine average rating of online freelancers. The article reviews performance rating of the freelancers, reveals the average number of years of work in the field of freelancing, characterizes the content of personal profiles, analyzes information about the cost of services, reveals the availability of information about the legal status of the “Best Performers”. The data obtained are useful and relevant in the light of the growth of the segment of online freelancers in Russia and the processes of institutionalization of self-employment nationwide.
Recent Developments in the Synthesis of Bicyclic Condensed Pyrimidinones
Authors: Naikoo Rayees Ahmad , Kumar Rupesh , Kumar Vipan , Bhargava Gaurav
Published: January 2022

Functionalized bicyclic pyrimidinones and their derivatives are significant heterocyclic
scaffolds being their all-around prevalence in biologically potent compounds. In several
attempts to explore the different synthetic methodologies for the construction of bicyclic
condensed pyrimidinones, different researchers from all across the globe have reported numerous
substantial methods. In the present review, considerable work has been critically
compiled on the synthesis of substituted and functionalized bicyclic pyrimidinones from 2000
onwards.
Directing Hypoxic Tumor Microenvironment and HIF to Illuminate Cancer
Immunotherapy's Existing Prospects and Challenges in Drug Targets
Authors: Ray Suman Kumar , Mukherjee Sukhes
Published: January 2022

Cancer is now also reflected as a disease of the tumor microenvironment, which is primarily
supposed to be a decontrolled genetic and cellular expression disease. Over the past two decades,
significant and rapid progress has been made in recognizing the dynamics of the tumor's microenvironment
and its contribution to influencing the response to various anti-cancer therapies
and drugs. Modulations in the tumor microenvironment and immune checkpoint blockade are interesting
in cancer immunotherapy and drug targets.
Simultaneously, the immunotherapeutic strategy can be implemented by modulating the immune
regulatory pathway; however, the tumor microenvironment plays an essential role in suppressing
the antitumor's immunity by its substantial heterogeneity. Hypoxia inducible factor (HIF) is a significant
contributor to solid tumor heterogeneity and a key stressor in the tumor microenvironment to
drive adaptations to prevent immune surveillance. Checkpoint inhibitors here halt the ability of cancer
cells to stop the immune system from activating, and in turn, amplify the body's immune system
to help destroy cancer cells. Common checkpoints that these inhibitors affect are the PD-1/PDL1
and CTLA-4 pathways, and important drugs involved are Ipilimumab and Nivolumab mainly,
along with other drugs in this group.
Targeting the hypoxic tumor microenvironment may provide a novel immunotherapy strategy,
break down traditional cancer therapy resistance, and build the framework for personalized precision
medicine and cancer drug targets. We hope that this knowledge can provide insight into the
therapeutic potential of targeting hypoxia and help develop novel combination approaches of cancer
drugs to increase the effectiveness of existing cancer therapies, including immunotherapy.
Pyrimidine-fused Dinitrogenous Penta-heterocycles as a Privileged Scaffold
for Anti-Cancer Drug Discovery
Authors: Li Wen , Zhang Jinyang , Wang Min , Dong Ru , Zhou Xin , Zheng Xin , Sun Liping
Published: January 2022

Pyrimidine-fused derivatives that are the inextricable part of DNA and RNA play a key role in the normal life cycle of cells. Pyrimidine-fused dinitrogenous penta-heterocycles, including pyrazolopyrimidines and imidazopyrimidines are a special class of pyrimidine-fused compounds contributing to an important portion in anti-cancer drug discovery, which has been discovered as the core structure for promising anti-cancer agents used in the clinic or clinical evaluations. Pyrimidine-fused dinitrogenous penta-heterocycles have become one privileged scaffold for anti-cancer drug discovery. This review consists of the recent progress of pyrimidine-fused dinitrogenous penta-heterocycles as anti-cancer agents and their synthetic strategies. In addition, this review also summa-rizes some key structure-activity relationships (SARs) of pyrimidine-fused dinitrogenous penta-heterocycle derivatives as anti-cancer agents.
First Total Synthesis of Isopsoralenoside
Authors: Wu Min , Xu Lijia , Song Mingwei , Li Ying , Wang Yingying , Dong Hongbo
Published: January 2022

The first total synthesis of the natural product iopsoralenoside, isolated from the n-butyl
alcohol extract of Fructus Psoraleae (FP), was achieved in 17% yield over 7 steps. The key steps of
the process were glycosylation and irradiation promoted by ultraviolet light. This synthesis provided
a sufficient amount of synthesized trans- and cis-isopsoralenoside for further bioassays.
Microwave Irradiated Synthesis of Pyrimidine Containing, Thiazolidin-4-
ones: Antimicrobial, Anti-Tuberculosis, Antimalarial and Anti-Protozoa
Evaluation
Authors: Soni Hetal I. , Patel Navin B. , Parmar Rahul B. , Chan-Bacab Manuel J. , Rivera Gildardo
Published: January 2022

Aim:

This study aims to synthesize thiazolidine-4-one compounds with a pyrimidine
nucleus and evaluate against different species of bacteria, fungi, protozoa, and the malaria parasite.

Background:

Microwave irradiation was the best method for synthesizing the thiazolidin-4-one
ring system. It took only 15 minutes for synthesizing thiazolidin-4-one while the conventional
method required 12 hours. The rapid reaction was the main concern of this research.

Objective:

Pyrimidine and Thiazolidin-4-one nucleus have broad-spectrum biological activity and
when it is introduced with other hetero atoms containing moiety, many types of biological activities
have been found; antimicrobial, anti-tuberculosis, anti-protozoa, antimalarial are the main activities.
The activity of these compounds inspired us to do extra research on Thiazolidin-4-one fused pyrimidines
with different functional groups. The aim of this study is to synthesize a combination of these
two ring systems in less time by using a microwave irradiation method and to evaluate new
compounds for different bioactivity.

Method:

2-(4-Chlorophenyl)-3-(4-(substituted phenyl)-6-(substituted aryl) pyrimidin-2-yl) thiazolidin-
4-ones (6A-J) were synthesized by microwave irradiation to save energy and time. The structure
of all newly synthesized motifs was characterized by spectral analysis (1H NMR, 13C NMR, IR,
spectroscopy) and screened for antibacterial activity against Escherichia coli, Pseudomonas aeruginosa,
Staphylococcus aureus, and Streptococcus pyogenes, antifungal activity against Candida
albicans, Aspergillus niger, Aspergillus clavatus, anti-tuberculosis activity against M. tuberculosis
H37RV, antimalarial activity against Plasmodium falciparum and anti-protozoa activity against L.
mexicana and T. cruzi.

Result:

Because of microwave irradiation synthesis, time period is very less for preparing the new
compound. Biological response given by compounds 6B, 6C, 6D, 6E, 6G, 6H, and 6J was found excellent.

Conclusion:

Good yield with purity of the newly synthesized thiazolidine-4-one compounds obtained
in less time by using microwave irradiation. The biological response of some of the compounds
of this series was found excellent.
Green Synthesis of 2-thioxothiazolidin-4-one Derivatives in Deep Eutectic
Solvents via Knoevenagel Condensation
Authors: Lončarić Melita , Molnar Maja
Published: January 2022

Recently, more and more researchers are resorting to green methods and techniques to avoid
environmental pollution. Accordingly, many researchers have been working on the development of
new green synthetic procedures trying to avoid the use of toxic organic solvents. A sustainable concept
of green and environmentally friendly solvents in chemical synthesis nowadays encompasses a
relatively new generation of solvents called deep eutectic solvents (DESs). DESs often have a dual role
in the synthesis, acting as both solvents and catalysts. In this study, DESs are used in the Knoevenagel
synthesis of rhodanine derivatives, with no addition of conventional catalysts. A model reaction of
rhodanine and salicylaldehyde was performed in 20 different DESs at 80°C, in order to find the best
solvent, which was further used for the synthesis of the series of desired compounds. A series of
rhodanines was synthesized in choline chloride: acetamide (ChCl:acetamide) DES with good to
excellent yields (51.4-99.7%).
Estrogen Receptor Beta (ERβ) Expression in Different Subtypes of Malignant
Pleural Mesothelioma
Authors: Shamaei Masoud , Pourabdollah Mihan , Pourdowlat Guitti , Parvizi Maryam , Boyadjian Shogher
Published: January 2022

Background:

Estrogen receptor beta (ERβ) is a potential target for cancer therapy as a
tumor suppressor. Malignant pleural mesothelioma (MPM) is a rare but fatal cancer. This study
tries to estimate the incidence of ERβ expression in the various subtypes of MPM tumors.

Methods and Materials:

In a retrospective study performed at a pulmonary tertiary referral hospital,
formalin-fixed paraffin-embedded human tissues of 46 definitive MPM were evaluated for expression
of ERβ by immunohistochemistry.

Results:

ERβ was detected in 14 cases (30.4%) out of the total 46 patients with a mean age of
58.08±11.59 SD, including 33 (71.7%) males. There was no statistically significant difference in
patients with positive ERβ staining versus negative cases in age and sex (P >0.05). MPM subtypes
included 36 (78.2%) cases of epithelioid mesothelioma, 3 (6.5%) cases of sarcomatoid, 5 (10.8%)
cases of biphasic, and 2 (4.3%) cases of desmoplastic subtype. ERβ expression was observed only
in epithelioid (11 of total 36 cases) and biphasic (3 of total 5 cases) tumors. There was no significant
difference in the incidence of ERβ expression in different subtypes of malignant pleural mesothelioma.
Statistical analysis shows a significant difference in the expression of ERβ in the
epithelioid subtype (with a more favorable prognosis) versus non-epithelioid subtypes (with poor
prognosis, including sarcomatoid, desmoplastic, and biphasic) (P = 0.024).

Discussion and Conclusion:

Considering the higher proportion of the epithelioid type of MPM
with ERβ expression, this highlights the role of ERβ in target therapy of MPM tumor, especially in
the epithelioid subtype with a more favorable prognosis. A better understanding of the pathology
of mesothelioma will eventually contribute to the development of therapies beyond the existing
therapeutic platform
Correlation Analysis of Surgical Efficacy and Risk Factors of Cervical
Spondylotic Myelopathy with High Signal Intensity on MRI-T2WI
Authors: Xu Hongguang , Xu Ziang , Xiao Liang , Liu Chen , Zhao Quanlai , Zhang Yu
Published: January 2022

Objectives:

The purpose of this study was to investigate the surgical efficacy and risk
factors of cervical spondylotic myelopathy (CSM) patients with increased signal intensity (ISI) on
T2-weighted magnetic resonance imaging (MRI-T2WI).

Methods:

We compared the surgical outcomes of CSM patients with and without ISI. In addition,
we compared the efficacy of anterior and posterior cervical decompression in CSM patients with
ISI. We also analyzed the risk factors of MRI-T2WI ISI in CSM patients.

Results:

The incidence of ISI among 153 CSM patients was 71.89 %. The JOA score and JOA remission
rate were better in the ISI-free than in the ISI group. The postoperative JOA score and
JOA remission rate were better in the posterior than the anterior approach surgery group. The disease
duration and vertebral canal volume were found to be risk factors for ISI in CSM patients.

Conclusion:

Among patients with CSM, the prognosis is worse for those with ISI than those without
ISI. Posterior cervical decompression surgery produces a better curative effect than anterior cervical
decompression surgery in CSM patients with ISI. CSM patients with longer disease duration
and small vertebral canal volume should undergo surgical treatment as early as possible.
Chalcone-thiosemicarbazone Hybrids as Inhibitors of Human Hepatocellular
Carcinoma HepG2 Cells Viability and Oxygen Consumption
Authors: Rodrigues Vivian Cordeiro , Felippe William Queiroz , Goulart Carla Marins , Echevarria Aurea , da Silva Ana Paula Pereira
Published: January 2022

Background:

Chalcones are open-chain flavonoids especially attractive to medicinal
chemistry due to their easy synthesis and the possibility of structural modifications.

Objective:

This study aims to evaluate the in vitro anticancer activity of a series of hybrids chalcones-
thiosemicarbazones against the human hepatocellular carcinoma cell line HepG2.

Methods:

Seven hybrid chalcones-thiosemicarbazones (CTs), 3-(4’-X-phenyl)-1-phenylprop-
2-en-1-one thiosemicarbazone, where X=H (CT-H), CH3 (CT-CH3), NO2 (CT-NO2), Cl (CTCl),
CN (CT-CN), F (CT-F), and Br (CT-Br), were synthesized and their effects on cells’ viability
and mitochondrial oxygen consumption were assessed.

Results:

Incubation with CTs caused a decrease in HepG2 cells viability in a time-concentration-dependent
manner. The most effective compounds in inhibiting cell viability, after 24 hours of treatment,
were CT-Cl and CT-CH3 (IC50 20.9 and 23.63 μM, respectively). In addition, using 10 μM
and only 1 hour of pre-incubation, CT-CH3 caused a reduction in basal respiration (-37 %), oxygen
consumption coupled with ATP synthesis (-60 %), and maximum oxygen consumption (-54 %). These
alterations in respiratory parameters may be involved with the inhibitory effects of CT-CH3
since significant changes in oxygen consumption rates were observed in a condition that anticipates
more significant losses of cell viability. The ADME parameters and the no violation of Lipinski
Rule of Five showed that all compounds are safe.

Conclusion:

These results may contribute to the knowledge about the effects of CTs on these cells
and the development of new treatments against HCCs.
Bioactive Extracts: Strategies to Generate Diversified Natural Product-
Like Libraries
Authors: Aggarwal Meenu , Singh Raman , Ahlawat Priyanka , Singh Kuldeep
Published: January 2022

Natural products have stimulated the interest of chemists owing to their abundant structural
diversity and complexity. Indeed, natural products have performed an essential role, particularly
in the cure of cancerous and infectious diseases, thereby providing medicinal researchers with
several unexplored chemotypes for the innovation of new drugs. Fusion of chemical derivatization
and combinatorial synthesis forms the basis of the concept of chemo diversification of plants. Diverse
libraries of natural product analogs are constructed through existing biological and chemical
approaches using unique schemes to expand natural product frameworks. This review aims to present
several approaches employed to offer innovative opportunities to synthesize NP-inspired compound
libraries. Reactive molecular fragments present in most natural products are chemically
converted to chemically engineered extracts (CEEs) or semisynthetic compounds constituting distinct
libraries. Bio-guided isolation for natural products required vital tools like reverse phase
chromatography and bioautographic assays. Different established strategies from DTS, BIOS, CtD,
FOS, FBDD to late-stage diversification facilitate the expansion of molecules with physicochemical
properties. In particular, fragment-like natural products with novel skeletons may be used as
preliminary points for chemical biology and medicinal chemistry programs with great capacity. In
this review, we sum up how NPs have proven fruitful for the novel methodologies responsible for
the diversification of complex natural products; therefore, it is worth going over the upcoming
integration of natural products with combinatorial chemistry.
Investigation of Antiblastic and Antibacterial Properties of Binuclear Platinum
(II)-Interferon Conjugate
Authors: Plotnikov Evgenii , Plotnikov Vladimir
Published: January 2022

Introduction:

This work aimed to create a new platinum-interferon conjugate and investigate
its properties.

Background:

Multiple drug resistance of tumor cells is a serious challenge in modern medicine.
Neoplastic diseases are often complicated by persistent bacterial infections, which impairs efficacy
and the outcome of anticancer therapy. The development of new bifunctional drugs for the treatment
of tumor growth and bacterial complications is an urgent task.

Objective:

The objective of this study was to evaluate the complex antiblastic and antibacterial
properties of interferon-platinum conjugate in vitro.

Material and Methods:

The coordination complex of dichloro-N,N,N,N-tetrakis-(2-aminoethyl)-
1,6-hexamethylenediaminobisplatin dichloride was used for production of conjugate with
human α-interferon. The binding of a metal complex with protein was established by means of radiochemical
neutron activation analysis. As test objects, we used lympholeukemic Jurkat cells line,
human lymphocytes in reaction of lymphocyte blastic transformation and different strains of microorganisms,
including Staphylococcus aureus and Pseudomonas aeruginosa.

Results:

Binuclear platinum human α-interferon conjugate has a significant dose-dependent
antibacterial and antiproliferative suppressive effect on target cells and bacteria.

Conclusion:

The tested preparation can be of a certain interest in drug designing for rational antiblastic
therapy, especially in the case of infectious complications. This conjugate can be a convenient
platform for creating drugs for the complex therapy of oncological diseases with bacterial
complications.
Neuroprotective Potential of Bacopa monnieri: Modulation of Inflammatory
Signals
Authors: Reale Marcella , Costantini Erica , Jarlapoodi Srinivas , Serra Federica , Aielli Lisa , Khan Haroon , Belwal Tarun , Falasca Katia
Published: January 2022

Background:

To date, much evidence has shown the increased interest in natural
molecules and traditional herbal medicine as alternative bioactive compounds to fight many inflammatory
conditions, both in relation to immunomodulation and in terms of their wound healing potential.
Bacopa monnieri is a herb that is used in the Ayurvedic medicine tradition for its anti-inflammatory
activity.

Objective:

In this study, we evaluate the anti-inflammatory and regenerative properties of the Bacopa
monnieri extract (BME) in vitro model of neuroinflammation.

Methods:

Neuronal SH-SY5Y cells were stimulated with TNFα and IFNγ and used to evaluate the
effect of BME on cell viability, cytotoxicity, cytokine gene expression, and healing rate.

Results:

Our results showed that BME protects against the Okadaic acid-induced cytotoxicity in
SH-SY5Y cells. Moreover, in TNFα and IFNγ primed cells, BME reduces IL-1β, IL-6, COX-2,
and iNOS, mitigates the mechanical trauma injury-induced damage, and accelerates the healing of
wounds.

Conclusion:

This study indicates that BME might become a promising candidate for the treatment
of neuroinflammation.