scholarly journals ANTITUMOR DRUGS BASED ON INDOLOCARBAZOL DERIVATIVES

2021 ◽  
Vol 9 (4) ◽  
pp. 252-265
Author(s):  
I. P. Kolpaksidi ◽  
M. V. Dmitrieva ◽  
I. V. Yarosh ◽  
I. I. Krasnyuk
Keyword(s):  
Clinical Trials ◽  
Antitumor Activity ◽  
Scientific Publications ◽  
Dna Topoisomerase ◽  
State Register ◽  
Kinase C ◽  
Medicinal Preparations ◽  
The Usa ◽  
The Russian Federation ◽  
High Antitumor Activity

The aim of the work is to generalize the literature data on indolocarbazole derivatives with an antitumor activity.Materials and methods. The objects of the study were the preparations based on indolocarbazole derivatives with the antitumor activity. To search for materials on the problem under study, the following search and information as well as library databases were used: ebibrary, PubMed, CyberLeninka, ResearchGate, the State Register of Medicines, clinical trials registries clinline.ru and clinicaltrials.gov. The search for the following words / phrases was performed: indolocarbazoles, indolocarbazole derivatives, staurosporine, rebeccamycin, staurosporine derivatives. The search was conducted from January 11 until March 1, 2021. The compounds with a biological activity which were undergoing or had undergone preclinical and clinical trials, were taken into account. All the materials from 1977 to January 1, 2021, were taken into account.Results. The materials obtained indicate that indolocarbazole derivatives are promising compounds for the creation of anticancer medicinal preparations due to their properties and peculiarities of the action mechanism. These drugs have a selective action due to the targeted interaction with specific molecular targets: kinases (especially protein kinase C and its isozymes), DNA and DNA topoisomerase. To date, many compounds from the class of indolocarbazoles have been synthesized and investigated. They have shown a high antitumor activity in the treatment of systemic and solid tumors. However, despite this, only one MP based on a staurosporine derivative, registered by the TN of Rydapt® (in the USA and EU countries) and Miticaid® (in the Russian Federation), is approved for use in the clinical practice.Conclusion. Thus, the basic data from scientific publications on promising anticancer medicinal preparations based on compounds from the class of indolocarbazoles, have been summarized. The information is provided, in particular, on their molecular structure, the origin, classification, the main representatives of the class, which are at various stages of the research and are approved for use in the clinic.

scholarly journals Peptides in COVID-19 Clinical Trials—A Snapshot

Biologics ◽  
2021 ◽  
Vol 1 (3) ◽  
pp. 300-311
Author(s):  
Kai Hilpert
Keyword(s):  
Clinical Trials ◽  
Antiviral Activity ◽  
Russian Federation ◽  
Current Situation ◽  
Routine Diagnostics ◽  
Current Review ◽  
The Usa ◽  
The Russian Federation ◽  
The Uk

Since the beginning of the COVID-19 pandemic, there has been a strong drive and desire to find effective treatments for and protection against the disease. On the webpage ClinicalTrials.gov, a total of 6505 clinical trials currently (September 2021) investigating various aspects of COVID-19 are registered. Of these, 124 studies involving peptides were identified. These 124 were further evaluated, and 88 trials that used peptides only for routine diagnostics were excluded. The remaining 36 trials were classified into 5 different classes according to their function: immunomodulatory (5 trials), regain homeostasis (10 trials), diagnostics/biomarkers (8 trials), vaccination (9 trials), and antiviral activity (4 trials, all overlap with immunomodulatory activities). In the current review, these 36 trials are briefly described and tabularly summarised. According to the estimated finish date, 14 trials have not yet finished. All of the finished trials are yet to report their results. Seven trials were based in the USA, and Egypt, France, the UK, Turkey, and the Russian Federation conducted three trials each. This review aims to present a snapshot of the current situation of peptides in COVID-19 clinical trials and provides a template to follow up on trials of interest; it does not claim to be a complete overview.

Селекция и семеноводство картофеля в Камчатском крае

2018 ◽  
Author(s):  
N.I. Ryakhovskaya ◽  
T.P. Sherstyukova ◽  
M.L. Gamolina
Keyword(s):  
Russian Federation ◽  
Potato Yield ◽  
The State ◽  
Limiting Factors ◽  
State Register ◽  
Region Selection ◽  
New Varieties ◽  
The Russian Federation ◽  
Selection Of

Рассмотрены агроклиматические условия Камчатского края и лимитирующие факторы, сдерживающие рост урожайности картофеля. Приведены характеристики новых сортов картофеля селекции Камчатского НИИСХ созданных в соответствии с приоритетными для региона направлениями селекции, включенных в Государственный реестр селекционных достижений РФ и охраняемых патентами.Agroclimatic conditions of the Kamchatka Krai and limiting factors that restrain the growth of potato yield are considered. The characteristics of new varieties of potatoes of the selection of the Kamchatsky RIA are created in accordance with the priority for the region selection areas included in the State Register of Selection Achievements of the Russian Federation and protected by patents.

Condition of the Armenian Apostolic Church at the Time of Coming to Authority N. S. Khrushchev

2020 ◽  
pp. 245-265
Author(s):  
Арсен Артурович Григорян
Keyword(s):  
Soviet Union ◽  
Research Methods ◽  
Russian Federation ◽  
National Archive ◽  
The State ◽  
State Archive ◽  
The Soviet Union ◽  
The Usa ◽  
The Russian Federation ◽  
Apostolic Church

Цель данной статьи - описать условия, в которых Армянская Апостольская Церковь вступила в эпоху правления Н. С. Хрущёва, начавшуюся в 1953 г. По содержанию статью можно поделить на две части: в первой даются сведения о количестве приходов на территории Советского Союза и за его пределами, а также о составе армянского духовенства в СССР; во второй излагаются проблемы, существовавшие внутри Армянской Церкви, и рассматриваются их причины. Методы исследования - описание и анализ. Ценность исследования заключается в использовании ранее неопубликованных документов Государственного архива Российской Федерации и Национального архива Армении. По итогам изучения фактического материала выделяются основные проблемы Армянской Апостольской Церкви на 1953 г.: финансовый дефицит, конфликт армянских католикосатов и стремление враждующих СССР и США использовать церковь в своих политических целях. The purpose of this article is to describe the conditions in which the Armenian Apostolic Church entered the epoch of the reign of N. S. Khrushchev, which began in 1953. The article can be divided into two parts: first one gives information about the number of parishes in the territory of the Soviet Union and beyond, and about the structure of the Armenian clergy in the USSR; the second one sets out the problems that existed in the Armenian Church and discusses their causes. Research methods - description and analysis. The value of the study lies in the use of previously unpublished documents of the State Archive of the Russian Federation and the National Archive of Armenia. Based on the results of studying the materials, the main problems of the Armenian Apostolic Church in 1953 are: financial deficit, the conflict of Armenian Catholicosates and the eagerness of USSR and the USA, that feuded with each other, to use the Сhurch for their political purposes.

Digital tax: an instructive foreign experience

2020 ◽  
pp. 69-87
Author(s):  
K.S. Teteryatnikov ◽  
S.G. Каmolov ◽  
D.A. Blashkina
Keyword(s):  
Russian Federation ◽  
High Tech ◽  
Digital Products ◽  
Tax Reforms ◽  
Goods And Services ◽  
Russian Economy ◽  
Internet Users ◽  
The Usa ◽  
On Line ◽  
The Russian Federation

The article is meant to analyze current problems and prospects for the development of effective tax policy as part of digital transformation of Russian economy. Introduction of a digital tax and the consequences of the digital tax reforms in the EU, the USA and OECD countries are highlighted. The necessity of qualitative transformation of the tax system of the Russian Federation in response to modern challenges is substantiated, taking into account the changes of the Tax Code of the Russian Federation adopted at the end of July 2020. The authors suggested their own concept of a digital tax and the prospects for its adoption in Russia, and consider it inappropriate to impose taxes on Internet users who do not use the Internet for business. Today, the main focus should be made on creating and testing effective technologies that allow on-line monitoring the tax basis of digital economy entities, taking into account the cross-border movement or use of digital products (goods and services). In addition, it would be extremely important to provide for a potential tax exemption for part of the profits of international ICT companies that are received on the territory of the Russian Federation and reinvested in joint with Russian companies projects in the high-tech for civil purposes area.

ВНЕШНЕПОЛИТИЧЕСКАЯ СИТУАЦИЯ В ЦЕНТРАЛЬНОЙ АЗИИ: В КОНТЕКСТЕ МЕЖДУНАРОДНЫХ ОТНОШЕНИЙ И НОВЫХ ТЕНДЕНЦИЙ В МИРОВОЙ ПОЛИТИКЕ

2020 ◽  
Author(s):  
Токтобек Рыскулов
Keyword(s):  
Central Asia ◽  
Transnational Corporation ◽  
World Politics ◽  
Energy Resources ◽  
Gas Oil ◽  
Political Events ◽  
Central Asian ◽  
The Usa ◽  
The Russian Federation ◽  
Near Future

Аннотация. В статье очерчено геополитическое и геостратегическое положение ЦА. Охарактеризована внешнеполитическая ситуация в ЦА в контексте новых тенденций в мировой политике. Показаны основные интересы и политические тренды РФ, США, КНР по отношения к государствам ЦА. Отмечено, что современная Центральная Азия, притягивает к себе все большее внимание внешних игроков. Объяснение кроется в том, что Центральная Азия обладает не только удобным геополитическим и выгодным геостратегическим положением, но и большим количеством природных ресурсов. Анализируя современные российско-китайские отношения приходим к мысли, что не все так безоблачно во взаимоотношениях двух государств, ведь еще никто не опроверг постулат о постоянных интересах государств и о непостоянстве друзей. В недалеком будущем конкуренция за энергоресурсы (газ, нефть) ЦА приведет к обострению отношений, к конфликту интересов России и Китая, практически это политическая аксиома. Готовы ли государства ЦА и России к такому сценарию политических событий? Ключевые слова: Центральна Азия, геополитика и геостратегия. Большая Игра, РФ, США, КНР. ЕАЭС, Большая Центральная Азия, ТНК, терроризм, экстремизм. Аннотация. Макалада геосаясий жана геостратегиялык абалдары чийилген. Борбордук Азиядагы тышкы саясий кырдаал дүйнөлүк саясаттагы жаңы тенденциялардын контекстинде мүнөздөлдү. БА мамлекеттеринин мамилелери боюнча РФ, АКШ, КЭР негизги кызыкчылыктары жана саясий тренддери көрсөтүлдү. Учурдагы Борбордук Азия тышкы оюнчулардын көбүрөөк көңүлүн өзүнө тартып жаткандыгы байкалган. Түшүндүрмө берүү, Борбордук Азия ыңгайлуу геосаясий жана пайдалуу геостратегиялык абалга гана ээ болбостон, көптөгөн жаратылыш ресурстарына ээ. Анализируя заманбап российско-кытай мамилелери приходим карата ойлорун, бул эмес баары эле безоблачно өз ара мамилелеринде эки мамлекеттин, анткени дагы эч ким опроверг постулат жөнүндө туруктуу кызыкчылыгында мамлекеттердин жөнүндө жана непостоянстве досторунун. Жакынкы келечекте ба энергия ресурстары үчүн атаандаштык (газ, мунай) Россия жана Кытайдын таламдарынын кагылышына, мамилелердин күчөшүнө алып келет, бул иш жүзүндө саясий аксиома. Борбордук Азия жана Орусия мамлекеттери мындай жагдайды саясий окуяларга даярбы? Түйүндүү сөздөр: Борбор Азия, геополитика жана геостратегия. Чоң оюн, РФ, АКШ, КЭР. ЕАЭС, Чоң Борбордук Азия, ТНК, терроризм, экстремизм. Annotation. The article outlines the geopolitical and geostrategic position of Central Asia. The article describes the foreign policy situation in Central Asia in the context of new trends in world politics. The main interests and political trends of the Russian Federation, the USA, China in relation to the Central Asian States are shown. It is noted that modern Central Asia attracts more and more attention of external players. The explanation lies in the fact that Central Asia has not only a convenient geopolitical and advantageous geostrategic position, but also a large number of natural resources. Analyzing the current Russian-Chinese relations, we come to the conclusion that not everything is so cloudless in the relations between the two States, because no one has yet refuted the postulate about the permanent interests of States and the impermanence of friends. In the near future, competition for energy resources (gas, oil) in Central Asia will lead to an aggravation of relations, to a conflict of interests between Russia and China, this is practically a political axiom. Are the Central Asian and Russian States ready for such a scenario of political events? Key words: Central Asia, geopolitics & geostrategy. Big Game, the RF, the USA, the CPR. EAEC, Big Central Asia, Transnational Corporation, terrorism, extremism

ACE-2-Receptors of the Epidermis, Dermal Vascular Walls and Sebaceous Gland Cells: The Way of COVID-19 Entry into the Body?

2020 ◽  
Author(s):  
Stefan Bittmann
Keyword(s):  
Clinical Trials ◽  
Viral Infection ◽  
Sebaceous Gland ◽  
The Body ◽  
Viral Agent ◽  
Therapy Options ◽  
Vascular Walls ◽  
Fish Market ◽  
The World ◽  
The Usa

Since the outbreak near a fish market in Wuhan, China, in December 2019, researchers have been searching for an effective therapy to control the spreading of the new coronavirus SARS-CoV-2 and inhibit COVID-19 infection. Many countries like Italy, Spain, and the USA were ambushed by this viral agent. To date, more than 2.5 million people were infected with SARS-CoV-2. There is no clear answer, why SARS-CoV-2 infects so many people so fast. To date of April 2020, no effective drug has been found to treat this new severe viral infection. There are many therapy options under review and clinical trials were initiated to get clearer information, what kind of drug can help in this devastating and serious situation. The world has no time.

ANTIBODY-DRUG CONJUGATES FOR TARGETED CANCER THERAPY

2019 ◽  
Vol 65 (6) ◽  
pp. 777-784
Author(s):  
David Korman
Keyword(s):  
Clinical Trials ◽  
Clinical Practice ◽  
Gemtuzumab Ozogamicin ◽  
Brentuximab Vedotin ◽  
Cytostatic Agent ◽  
Cytostatic Agents ◽  
Drug Conjugates ◽  
Natural Substances ◽  
Intracellular Release ◽  
High Antitumor Activity

Monoclonal antibody (MAB) conjugates with cytostatic agents (ADC) are intended for selective delivery of a cytostatic agent to a tumor cell. Three ADC have been approved for clinical use (gemtuzumab ozogamicin, brentuximab vedotin, trastuzumab-DM1); a few dozens of other ADC are undergoing clinical trials. Several derivatives of natural substances (antibiotics and inhibitors of microtubules) having a high antitumor activity are used as cytostatic agents included in ADC. They are inapplicable in clinical practice as self-sustained drugs due to their considerable toxicity. Of great importance for the implementation of the ADC effect is the character of a linker connecting MAB with a cytostatic agent and ensuring selective intracellular release after ADC internalization. The structure, mechanisms of action, and the results of clinical trials of a number of ADC are considered here as an illustration (by way of example). The development of ADC can help introduce new effective cytostatic agents into clinical practice.

scholarly journals Global research activity on antimicrobial resistance in food-producing animals

2021 ◽  
Vol 79 (1) ◽  
Author(s):  
Waleed M. Sweileh
Keyword(s):  
Antimicrobial Resistance ◽  
Hot Spots ◽  
One Health ◽  
Research Collaboration ◽  
Search Query ◽  
Scientific Publications ◽  
Research Theme ◽  
The Usa ◽  
Number Of Publications ◽  
Number Of Citations

Abstract Background Antimicrobial resistance (AMR) is a global challenge that requires a “One Health” approach to achieve better public health outcomes for people, animals, and the environment. Numerous bibliometric studies were published on AMR in humans. However, none was published in food-producing animals. The current study aimed at assessing and analyzing scientific publications on AMR in food-producing animals. Method A validated search query was developed and entered in Scopus advanced search function to retrieve and quantitatively analyze relevant documents. Bibliometric indicators and mapping were presented. The study period was from 2000 to 2019. Results The search query retrieved 2852 documents. During the period from 2015 to 2019, approximately 48% of the retrieved documents were published. The article about the discovery of plasmid-mediated colistin resistance in pigs received the highest number of citations (n = 1970). The Journal of Food Protection (n = 123; 4.3%) ranked first in the number of publications while the Applied and Environmental Microbiology journal ranked first in the number of citations per document. The USA led with 576 (20.2%) documents followed by China (n = 375; 13.1%). When the number of publications was standardized by income and population size, India (n = 51.5) ranked first followed by China (n = 38.3) and Brazil (n = 13.4). The growth of publications from China exceeded that of the USA in the last 3 years of the study period. Research collaboration in this field was inadequate. Mapping author keywords showed that E. coli, Salmonella, poultry, Campylobacter, chicken, cattle, and resistant genes were most frequent. The retrieved documents existed in five research themes. The largest research theme was about AMR in Salmonella in food-producing animals. The most recent research theme was about the dissemination and molecular transfer of AMR genes into the environment and among different bacterial strains. Conclusion Hot spots of research on AMR in food-producing animals match the world regions of reported hot spots of AMR in animals. Research collaboration in this field is of great importance, especially with low- and middle-income countries. Data on AMR need to be collected nationally and internationally to implement the “One Health” approach in the fight against AMR.

scholarly journals Anti-Malignant Ascites Effect of Total Diterpenoids from Euphorbiae ebracteolatae Radix Is Attributable to Alterations of Aquaporins via Inhibiting PKC Activity in the Kidney

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 942
Author(s):  
Yuanbin Zhang ◽  
Dongfang Liu ◽  
Fan Xue ◽  
Hongli Yu ◽  
Hao Wu ◽  
...  
Keyword(s):  
Protein Kinase C ◽  
Antitumor Activity ◽  
Membrane Fraction ◽  
Collecting Duct ◽  
Human Kidney ◽  
Underlying Mechanism ◽  
Malignant Ascites ◽  
Kinase C ◽  
Collecting Duct Cells ◽  
Medullary Collecting Duct

This study evaluated the anti-ascites effect of total diterpenoids extracted from Euphorbiae ebracteolatae Radix (TDEE) on malignant ascitic mice and elucidated its underlying mechanism. TDEE was extracted by dichloromethane and subjected to column chromatography. The purity of six diterpenoids isolated from TDEE was determined to be 77.18% by HPLC. TDEE (3 and 0.6 g raw herbs/kg, p.o.) reduced ascites and increased urine output. Meanwhile, analysis of tumor cell viability, cycle and apoptosis indicated that TDEE had no antitumor activity. In addition, the expression levels of aquaporins (AQPs) and the membrane translocation levels of protein kinase C (PKC) α and PKCβ in kidney and cells were measured. TDEE reduced the levels of AQP1–4, and inhibited PKCβ expression in membrane fraction. Four main diterpenoids, except compound 2, reduced AQP1 level in human kidney-2 cells. Compounds 4 and 5 inhibited AQP2–4 expression in murine inner medullary collecting duct cells. The diterpenoid-induced inhibition of AQP1–4 expression was blocked by phorbol-12-myristate-13-acetate (PMA; agonist of PKC). The diterpenoids from TDEE are the main anti-ascites components. The anti-ascites effect of diterpenoids may be associated with alterations in AQPs in the kidneys to promote diuresis. The inhibition of AQP1–4 expression by TDEE is related to the inhibition of PKCβ activation.

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