scholarly journals Tyrosol as a neuroprotector: strong effects of a "weak" antioxidant

2020 ◽  
Vol 18 ◽  
Author(s):  
Mark B. Plotnikov ◽  
Tatiana M. Plotnikova

: The use of neuroprotective agents for stroke is pathogenetically justified, but the translation of results of preclinical studies of neuroprotectors into clinical practice has been a noticeable failure. One of the leading reasons for these failures is the one-target mechanism of their activity. p-Tyrosol (Tyr), a biophenol, is present in a variety of natural sources, mainly in foods, such as olive oil and wine. Tyr has a wide spectrum of biological activity: antioxidant, stress-protective, anti-inflammatory, anticancer, cardioprotective, neuroprotective and many others. This review analyzes data on the neuroprotective, antioxidant, anti-inflammatory, anti-apoptotic and other kinds of Tyr activity as well as data on the pharmacokinetics of the substance. The data presented in the review substantiate the acceptability of tyrosol as the basis for the development of a new neuroprotective drug with multitarget activity for the treatment of ischemic stroke. Tyr is a promising molecule for the development of an effective neuroprotective agent for use in ischemic stroke.

2012 ◽  
Vol 7 (2) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
George A. Kraus ◽  
Feng Liu

The uliginosins have potentially very useful biological activity, but their availability from natural sources is limited. Moreover, the one synthesis can not be reproduced. Here we report reproducible conditions for the synthesis of the uliginosins.


2019 ◽  
Vol 12 (3) ◽  
pp. 233-235 ◽  
Author(s):  
D Węgrzyn ◽  
◽  
◽  
A Kutwin-Chojnacka ◽  
J Bilski ◽  
...  

Finding neuroprotective agents to counteract the deleterious effects of hypoxia on neuronal cells successfully is one of the most critical targets of clinical research since preclinical studies have identified potential neuroprotective strategies. In clinical practice, amantadine and piracetam are used with reasonable success. We present the cases of three patients with acute brain hypoxia secondary to cardiac arrest, to whom Cerebrolysin was added to the standard neuroprotective treatment regimen, leading to a notable improvement in functional outcome.


2020 ◽  
pp. 235-241
Author(s):  
Elena Vital'yevna Averyanova ◽  
Marina Nikolayevna Shkolnikova ◽  
Evgeniy Dmitriyevich Rozhnov ◽  
Denis Viktorovich Minakov ◽  
Evgeniy Sergeyevich Batashov ◽  
...  

The need to expand the raw material base for obtaining flavonoids is due to the wide spectrum of their biological activity. The purpose of this work is to study the biological activity of a complex of bioflavonoids, quercetin and rutin on specific enzyme biotest systems in vitro. The objects of the study were: a complex of bioflavonoids from fat-free sea buckthorn meal Hippophae rhamnoides L. and individual flavonoids rutin and quercetin isolated from it. The study was carried out by methods of detecting the biological activity of substances using specific enzyme biotest systems in vitro. It was revealed that rutin and a complex of bioflavonoids have antioxidant properties – the rate of glutathione reductase reaction increased by 64 and 51% of control, respectively, and catalase – by 15%. Quercetin exhibits antimicrobial activity and also reduces the rate of the enzymatic iNOS reaction by 24% of the control, which indicates the anti-inflammatory properties of this sample. Rutin and a complex of bioflavonoids from sea buckthorn meal increased the iNOS reaction rate by 14 and 28%, respectively, which indicates the immunostimulating properties of these samples. In the course of a microbiological study, it was found that all samples have weak bacteriostatic activity against gram-positive and gram-negative bacteria Staphylococcus aureus ATCC 6538 (209-P) and Pseudomonas aeruginosa ATCC 9027. Fungistatic activity was confirmed against the yeast-like fungi Candida albicans ATCC 10231 of quercetin and the complex. The results obtained make it possible to consider a complex of bioflavonoids, quercetin and rutin as promising active substances in antioxidant, antimicrobial, fungistatic and anti-inflammatory drugs.


2021 ◽  
Vol 17 (5) ◽  
pp. 18-30
Author(s):  
S.P. Moskovko ◽  
O.V. Kyrychenko ◽  
H.S. Rudenko ◽  
Et Al.*

Ischemic stroke remains a pressing problem today. Its pathogenesis consists of a sequential cascade of reactions in the brain, which, in addition to ischemia, are responsible for further damage to brain tissue and slow down the development of compensatory and regenerative mechanisms. Attempts to break the pathological cascade have been going on for decades. The first promising molecule that demonstrated the potential of a scavenger (cleaner, absorber) of excessive aggressive peroxides in preclinical studies was MCI-186, which is used in clinical practice under the name edaravone. The aim of the study the results of which are presented in this paper was to establish the clinical effects of edaravone (Xavron) as a concomitant therapy of acute ischemic stroke (СТІКс) in real clinical practice.


An area of great interest in recent years has been chalcones. Chalcones are the important component of many natural sources and have variety of biological activities. Chalcones which are also known as α,βunsaturated ketones is an significant class of organic compounds and reported to possess a wide spectrum of biological activities such as antibacterial, antifungal, anticancer, anti-inflammatory etc. Abundant research papers have been published and chalcones continue to show promise for new drug investigations. The derivative of chalcones were prepared using Claisen–Schmidt condensation scheme. The structure of the synthesized was confirmed by UV and IR. The compound was also tested for their antimicrobial activity


1973 ◽  
Vol 72 (3) ◽  
pp. 495-505 ◽  
Author(s):  
Oddmund Søvik ◽  
Svein Oseid

ABSTRACT The biological activity of plasma insulin from 4 cases of congenital generalized lipodystrophy has been studied, using rat diaphragm and epididymal adipose tissue in vivo. The results are compared with previous data on plasma immunoreactive insulin obtained in these patients. 2 of the 4 cases exhibited unusually high biological insulin activities during the fasting state as well as after an intravenous (iv) glucose load. In the fat pad assay activities as high as 10 000 μU insulin per ml were observed. During childhood the biological insulin activities were generally high, although there were large individual variations. However, in the one case studied after the age of puberty, the insulin response to a glucose load was negligible. Taken together, the biological and immunological activities observed strongly suggest the presence of pancreatic insulin in these patients. It appears that the circulating insulin has a fully biological activity. The decreasing insulin activities after cessation of growth are in agreement with the appearance of frank diabetes at this time.


Author(s):  
Yuri Morales López ◽  
Marianela Alpízar Vargas ◽  
Ana Lucía Alfaro Arce ◽  
Vicenç Font-Moll

The purpose of this presentation is to show elements associated to the study and analysis of pedagogical practices used by mathematics teachers, taking into consideration different approaches and conceptions derived from theories related to the role of the math teacher. The project highlights the need to use different strategies to analyze the processes occurring in the activities and tasks organized and implemented by the teacher. One of the main tasks in teacher training is to promote the capacity to noticing on the pedagogical activity, where noticing is understood as an inherent process to improve the quality of classroom management. In addition, different analysis models should be compared using examples and experiential practices and the different theories and research projects developed in this field related to this type of analysis. Knowing what happens in the classroom is a task inherent to the math teacher. For sure, if the teacher does not understand or is even able to perceive what is happening in the class, improvement actions are very difficult to implement. Consequently, math teachers must develop the capability of analyzing their pedagogical activity and the related elements. It is not about isolating variables and looking for causal relationships, but rather about understanding the teacher’s activity as the center of the multiple situations occurring in the classroom, which may be known more in depth, if the attention is focused on the organization, ordering, and execution of the tasks planned by the teacher. It must also be understood that the competence of analyzing mentioned here is not an isolated activity without an effect. Such analysis must be approached from an active perspective where scenarios are generated to mitigate complex situations or to value an approach different than the one happening in the classroom. Being aware that there are many aspects to analyze (most likely almost everything that happens is analyzable), we must take a stand on which situations are highly related to what happens in our classroom and which could eventually happen. With such a wide spectrum, some questions that need to be addressed are: What is important in the math education activity and who defines what is important? What elements are of interest to math teachers? How does the analysis conducted relate to the different models of the teacher's knowledge? How does our previous experience influence the assessments we make? How do we distinguish elements of interest to analysis? What is the relationship between reflecting and analyzing? At what stages of the teacher’s activity is an analysis required? What is the ultimate purpose of analyzing teaching activities? What competencies or skills are related to the analysis? What types of analysis are appropriate (content, cognitive, media, among others)? How can we balance the actions derived from the analyses we conduct? From all these questions the most important one that can guide the study of this reflection would be: What should be assessed in pedagogical activities and what is the objective of analyzing such pedagogical activities in math education?


2019 ◽  
Author(s):  
Chem Int

A series of heterocyclic compounds incorporating pyridazine moiety were for diverse biological activities. Pyridazines and pyridazinones derivatives showed wide spectrum of biological activities such as vasodialator, cardiotonic, anticonvulsant, antihypertensive, antimicrobial, anti-inflammatory, analgesic, anti-feedant, herbicidal, and various other biological, agrochemical and industrial chemical activities. The results illustrated that the synthesized pyridazine/pyridazine compounds have diverse and significant biological activities. Mechanistic insights into the biological properties of pyridazinone derivatives and various synthetic techniques used for their synthesis are also described.


2019 ◽  
Vol 14 (2) ◽  
pp. 133-143 ◽  
Author(s):  
Hidayat Hussain ◽  
Ivan R. Green ◽  
Muhammad Saleem ◽  
Khanzadi F. Khattak ◽  
Muhammad Irshad ◽  
...  

Background: Cucurbitacins belong to a group of tetracyclic triterpenoids that display a wide range of biological effects. In the past, numerous cucurbitacins have been isolated from natural sources and many active compounds have been synthesized using the privileged scaffold in order to enhance its cytotoxic effects. Objective: his review covers patents on the therapeutic effects of natural cucurbitacins and their synthetic analogs published during the past decade. By far, the majority of patents published are related to cancer and Structure-Activity Relationships (SAR) of these compounds are included to lend gravitas to this important class of natural products. Methods: The date about the published patents was downloaded via online open access patent databases. Results: Cucurbitacins display significant cytotoxic properties, in particular cucurbitacins B and D which possess very potent effects towards a number of cancer cells. Numerous cucurbitacins isolated from natural sources have been derivatized through chemical modification at the C(2)-OH and C(25)- OH groups. Most importantly, an acyl ester of the C(25)-OH and, iso-propyl, n-propyl and ethyl ether groups of the C(2)-OH demonstrated the most increased cytotoxic activity. Conclusion: The significant cytotoxic effects of natural and semi-synthetic cucurbitacins make them attractive as new drug candidates. Moreover, cucurbitacins have the capability to form conjugates with other anticancer drugs which will synergistically enhance their anticancer effects. The authors believe that in order to get lead compounds, there should be a greater focus on the synthesis of homodimers, heterodimers, and halo derivatives of cucurbitacins. In the opinion of the authors the analysis of the published patents on the cucurbitacins indicates that these compounds can be developed into a regimen to treat a wide spectrum of cancers.


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