scholarly journals Wide-Range Measurement of Thermal Preference—A Novel Method for Detecting Analgesics Reducing Thermally-Evoked Pain in Mice

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 612
Author(s):  
Kinga Sałat ◽  
Anna Furgała-Wojas ◽  
Michał Awtoniuk ◽  
Robert Sałat
Keyword(s):  
Analgesic Activity ◽  
Therapeutic Option ◽  
Thermal Preference ◽  
Drug Candidates ◽  
New Methods ◽  
Wide Range ◽  
Novel Method ◽  
Cold Hyperalgesia ◽  
Cold Hypersensitivity ◽  
Better Than

Background: Wide use of oxaliplatin as an antitumor drug is limited by severe neuropathy with pharmacoresistant cold hypersensitivity as the main symptom. Novel analgesics to attenuate cold hyperalgesia and new methods to detect drug candidates are needed. Methods: We developed a method to study thermal preference of oxaliplatin-treated mice and assessed analgesic activity of intraperitoneal duloxetine and pregabalin used at 30 mg/kg. A prototype analgesiameter and a broad range of temperatures (0–45 °C) were used. Advanced methods of image analysis (deep learning and machine learning) enabled us to determine the effectiveness of analgesics. The loss or reversal of thermal preference of oxaliplatin-treated mice was a measure of analgesia. Results: Duloxetine selectively attenuated cold-induced pain at temperatures between 0 and 10 °C. Pregabalin-treated mice showed preference towards a colder plate of the two used at temperatures between 0 and 45 °C. Conclusion: Unlike duloxetine, pregabalin was not selective for temperatures below thermal preferendum. It influenced pain sensation at a much wider range of temperatures applied. Therefore, for the attenuation of cold hypersensitivity duloxetine seems to be a better than pregabalin therapeutic option. We propose wide-range measurements of thermal preference as a novel method for the assessment of analgesic activity in mice.

scholarly journals Competition-Based Benchmarking of Influence Ranking Methods in Social Networks

Complexity ◽  
2018 ◽  
Vol 2018 ◽  
pp. 1-15 ◽  
Author(s):  
Alexandru Topîrceanu
Keyword(s):  
Diffusion Model ◽  
Ranking Method ◽  
Practical Significance ◽  
Ranking Methods ◽  
New Methods ◽  
Sir Epidemic ◽  
Node Ranking ◽  
Wide Range ◽  
Novel Method ◽  
Real World Datasets

The development of new methods to identify influential spreaders in complex networks has been a significant challenge in network science over the last decade. Practical significance spans from graph theory to interdisciplinary fields like biology, sociology, economics, and marketing. Despite rich literature in this direction, we find small notable effort to consistently compare and rank existing centralities considering both the topology and the opinion diffusion model, as well as considering the context of simultaneous spreading. To this end, our study introduces a new benchmarking framework targeting the scenario of competitive opinion diffusion; our method differs from classic SIR epidemic diffusion, by employing competition-based spreading supported by the realistic tolerance-based diffusion model. We review a wide range of state-of-the-art node ranking methods and apply our novel method on large synthetic and real-world datasets. Simulations show that our methodology offers much higher quantitative differentiation between ranking methods on the same dataset and notably high granularity for a ranking method over different datasets. We are able to pinpoint—with consistency—which influence the ranking method performs better against the other one, on a given complex network topology. We consider that our framework can offer a forward leap when analysing diffusion characterized by real-time competition between agents. These results can greatly benefit the tackling of social unrest, rumour spreading, political manipulation, and other vital and challenging applications in social network analysis.

Possession and Repetition

2012 ◽  
Vol 6 (1-3) ◽  
pp. 243-259 ◽  
Author(s):  
Yohan Yoo
Keyword(s):  
First Century ◽  
Daily Lives ◽  
Modern Times ◽  
Sacred Texts ◽  
New Methods ◽  
Wide Range ◽  
Lay Buddhists ◽  
Iconic Status ◽  
And Function ◽  
To Receive

This article demonstrates the need for the iconic status and function of Buddhist scripture to receive more attention by illuminating how lay Korean Buddhists try to appropriate the power of sutras. The oral and aural aspects of scripture, explained by Wilfred Cantwell Smith, provide only a limited understanding of the characteristics of scripture. It should be noted that, before modern times, most lay people, not only in Buddhist cultures but also in Christian and other traditions, neither had the chance to recite scriptures nor to listen to their recitations regularly. Several clear examples demonstrate contemporary Korean Buddhists’ acceptance of the iconic status of sutras and their attempt to appropriate the power and status of those sacred texts. In contemporary Korea, lay Buddhists try to claim the power of scriptures in their daily lives by repeating and possessing them. Twenty-first century lay believers who cannot read or recite in a traditional style have found new methods of repetition, such as internet programs for copying sacred texts and for playing recordings of their recitations. In addition, many Korean Buddhists consider the act of having sutras in one’s possession to be an effective way of accessing the sacred status and power of these texts. Hence, various ways of possessing them have been developed in a wide range of products, from fancy gilded sutras to sneakers embroidered with mantras.

Variable Precision Depth Encoding for 3D Range Geometry Compression

2020 ◽  
Vol 2020 (17) ◽  
pp. 34-1-34-7
Author(s):  
Matthew G. Finley ◽  
Tyler Bell
Keyword(s):  
Normal Distribution ◽  
Arbitrary Distribution ◽  
File Size ◽  
Geometry Compression ◽  
Variable Precision ◽  
Wide Range ◽  
Novel Method ◽  
Encoding Method ◽  
Rgb Image ◽  
Color Channels

This paper presents a novel method for accurately encoding 3D range geometry within the color channels of a 2D RGB image that allows the encoding frequency—and therefore the encoding precision—to be uniquely determined for each coordinate. The proposed method can thus be used to balance between encoding precision and file size by encoding geometry along a normal distribution; encoding more precisely where the density of data is high and less precisely where the density is low. Alternative distributions may be followed to produce encodings optimized for specific applications. In general, the nature of the proposed encoding method is such that the precision of each point can be freely controlled or derived from an arbitrary distribution, ideally enabling this method for use within a wide range of applications.

Research of the activity and viability of spermatozoa at different concentrations and proportions of diluents after incubation

2020 ◽  
pp. 88-95
Author(s):  
Svitlana Lobchenko ◽  
Tetiana Husar ◽  
Viktor Lobchenko
Keyword(s):  
Plasma Concentration ◽  
Incubation Time ◽  
Coefficient Of Variation ◽  
Incubation Medium ◽  
Wide Range ◽  
Series Of Experiments ◽  
The Subject ◽  
Boar Spermatozoa ◽  
Native Plasma ◽  
Better Than

The results of studies of the viability of spermatozoa with different incubation time at different concentrations and using different diluents are highlighted in the article. (Un) concentrated spermatozoa were diluented: 1) with their native plasma; 2) medium 199; 3) a mixture of equal volumes of plasma and medium 199. The experiment was designed to generate experimental samples with spermatozoa concentrations prepared according to the method, namely: 0.2; 0.1; 0.05; 0.025 billion / ml. The sperm was evaluated after 2, 4, 6 and 8 hours. The perspective of such a study is significant and makes it possible to research various aspects of the subject in a wide range. In this regard, a series of experiments were conducted in this area. The data obtained are statistically processed and allow us to highlight the results that relate to each stage of the study. In particular, in this article it was found out some regularities between the viability of sperm, the type of diluent and the rate of rarefaction, as evidenced by the data presented in the tables. As a result of sperm incubation, the viability of spermatozoa remains at least the highest trend when sperm are diluted to a concentration of 0.1 billion / ml, regardless of the type of diluent used. To maintain the viability of sperm using this concentration of medium 199 is not better than its native plasma, and its mixture with an equal volume of plasma through any length of time incubation of such sperm. Most often it is at this concentration of sperm that their viability is characterized by the lowest coefficient of variation, regardless of the type of diluent used, which may indicate the greatest stability of the result under these conditions. The viability of spermatozoa with a concentration of 0.1 billion / ml is statistically significantly reduced only after 6 or even 8 hours of incubation. If the sperm are incubated for only 2 hours, regardless of the type of diluent used, the sperm concentrations tested do not affect the viability of the sperm. Key words: boar, spermatozoa, sperm plasma, concentration, incubation, medium 199, activity, viability, rarefaction.

Privileged Structures in the Design of Potential Drug Candidates for Neglected Diseases

2019 ◽  
Vol 26 (23) ◽  
pp. 4323-4354 ◽  
Author(s):  
Ana Cristina Lima Leite ◽  
José Wanderlan Pontes Espíndola ◽  
Marcos Veríssimo de Oliveira Cardoso ◽  
Gevanio Bezerra de Oliveira Filho
Keyword(s):  
Biologically Active ◽  
Neglected Diseases ◽  
Financial Return ◽  
Drug Candidates ◽  
Lead Compounds ◽  
Wide Range ◽  
Methods Of Synthesis ◽  
Current Therapies ◽  
Resistant Strains ◽  
Privileged Structures

Background: Privileged motifs are recurring in a wide range of biologically active compounds that reach different pharmaceutical targets and pathways and could represent a suitable start point to access potential candidates in the neglected diseases field. The current therapies to treat these diseases are based in drugs that lack of the desired effectiveness, affordable methods of synthesis and allow a way to emergence of resistant strains. Due the lack of financial return, only few pharmaceutical companies have been investing in research for new therapeutics for neglected diseases (ND). Methods: Based on the literature search from 2002 to 2016, we discuss how six privileged motifs, focusing phthalimide, isatin, indole, thiosemicarbazone, thiazole, and thiazolidinone are particularly recurrent in compounds active against some of neglected diseases. Results: It was observed that attention was paid particularly for Chagas disease, malaria, tuberculosis, schistosomiasis, leishmaniasis, dengue, African sleeping sickness (Human African Trypanosomiasis - HAT) and toxoplasmosis. It was possible to verify that, among the ND, antitrypanosomal and antiplasmodial activities were between the most searched. Besides, thiosemicarbazone moiety seems to be the most versatile and frequently explored scaffold. As well, phthalimide, isatin, thiazole, and thiazolidone nucleus have been also explored in the ND field. Conclusion: Some described compounds, appear to be promising drug candidates, while others could represent a valuable inspiration in the research for new lead compounds.

A Novel Amino Acid Sequence-based Computational Approach to Predicting Cell-penetrating Peptides

2019 ◽  
Vol 15 (3) ◽  
pp. 206-211 ◽  
Author(s):  
Jihui Tang ◽  
Jie Ning ◽  
Xiaoyan Liu ◽  
Baoming Wu ◽  
Rongfeng Hu
Keyword(s):  
Machine Learning ◽  
Amino Acid ◽  
Amino Acid Position ◽  
Cell Penetrating Peptides ◽  
Support Vector ◽  
Cell Penetration ◽  
Drug Candidates ◽  
Machine Learning Model ◽  
Cell Penetrating ◽  
Novel Method

<P>Introduction: Machine Learning is a useful tool for the prediction of cell-penetration compounds as drug candidates. </P><P> Materials and Methods: In this study, we developed a novel method for predicting Cell-Penetrating Peptides (CPPs) membrane penetrating capability. For this, we used orthogonal encoding to encode amino acid and each amino acid position as one variable. Then a software of IBM spss modeler and a dataset including 533 CPPs, were used for model screening. </P><P> Results: The results indicated that the machine learning model of Support Vector Machine (SVM) was suitable for predicting membrane penetrating capability. For improvement, the three CPPs with the most longer lengths were used to predict CPPs. The penetration capability can be predicted with an accuracy of close to 95%. </P><P> Conclusion: All the results indicated that by using amino acid position as a variable can be a perspective method for predicting CPPs membrane penetrating capability.</P>

Cucurbitacins as Anticancer Agents: A Patent Review

2019 ◽  
Vol 14 (2) ◽  
pp. 133-143 ◽  
Author(s):  
Hidayat Hussain ◽  
Ivan R. Green ◽  
Muhammad Saleem ◽  
Khanzadi F. Khattak ◽  
Muhammad Irshad ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Wide Spectrum ◽  
Biological Effects ◽  
Therapeutic Effects ◽  
Cytotoxic Effects ◽  
Natural Sources ◽  
Oh Groups ◽  
Drug Candidates ◽  
The Past ◽  
Wide Range

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.

Expressing the Self

2018 ◽  
Keyword(s):  
Philosophy Of Mind ◽  
The Self ◽  
Epistemic Status ◽  
First Person ◽  
Semantic Categories ◽  
Wide Range ◽  
Person Reference ◽  
De Se ◽  
Novel Method ◽  
Cultural Pragmatics

This book addresses different linguistic and philosophical aspects of referring to the self in a wide range of languages from different language families, including Amharic, English, French, Japanese, Korean, Mandarin, Newari (Sino-Tibetan), Polish, Tariana (Arawak), and Thai. In the domain of speaking about oneself, languages use a myriad of expressions that cut across grammatical and semantic categories, as well as a wide variety of constructions. Languages of Southeast and East Asia famously employ a great number of terms for first-person reference to signal honorification. The number and mixed properties of these terms make them debatable candidates for pronounhood, with many grammar-driven classifications opting to classify them with nouns. Some languages make use of egophors or logophors, and many exhibit an interaction between expressing the self and expressing evidentiality qua the epistemic status of information held from the ego perspective. The volume’s focus on expressing the self, however, is not directly motivated by an interest in the grammar or lexicon, but instead stems from philosophical discussions of the special status of thoughts about oneself, known as de se thoughts. It is this interdisciplinary understanding of expressing the self that underlies this volume, comprising philosophy of mind at one end of the spectrum and cross-cultural pragmatics of self-expression at the other. This unprecedented juxtaposition results in a novel method of approaching de se and de se expressions, in which research methods from linguistics and philosophy inform each other. The importance of this interdisciplinary perspective on expressing the self cannot be overemphasized. Crucially, the volume also demonstrates that linguistic research on first-person reference makes a valuable contribution to research on the self tout court, by exploring the ways in which the self is expressed, and thereby adding to the insights gained through philosophy, psychology, and cognitive science.

Effect of Contact Ratio on Spur Gear Dynamic Load With No Tooth Profile Modifications

1996 ◽  
Vol 118 (3) ◽  
pp. 439-443 ◽  
Author(s):  
Chuen-Huei Liou ◽  
Hsiang Hsi Lin ◽  
F. B. Oswald ◽  
D. P. Townsend
Keyword(s):  
Dynamic Load ◽  
Spur Gear ◽  
Tooth Size ◽  
Contact Ratio ◽  
Gear Dynamics ◽  
Wide Range ◽  
Gear Contact ◽  
Center Distance ◽  
Selection Of ◽  
Better Than

This paper presents a computer simulation showing how the gear contact ratio affects the dynamic load on a spur gear transmission. The contact ratio can be affected by the tooth addendum, the pressure angle, the tooth size (diametral pitch), and the center distance. The analysis presented in this paper was performed by using the NASA gear dynamics code DANST. In the analysis, the contact ratio was varied over the range 1.20 to 2.40 by changing the length of the tooth addendum. In order to simplify the analysis, other parameters related to contact ratio were held constant. The contact ratio was found to have a significant influence on gear dynamics. Over a wide range of operating speeds, a contact ratio close to 2.0 minimized dynamic load. For low-contact-ratio gears (contact ratio less than two), increasing the contact ratio reduced gear dynamic load. For high-contact-ratio gears (contact ratio equal to or greater than 2.0), the selection of contact ratio should take into consideration the intended operating speeds. In general, high-contact-ratio gears minimized dynamic load better than low-contact-ratio gears.

scholarly journals Modern Synthetic Methods for the Stereoselective Construction of 1,3-Dienes

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 249
Author(s):  
Raquel G. Soengas ◽  
Humberto Rodríguez-Solla
Keyword(s):  
Organic Chemistry ◽  
Natural Products ◽  
Functional Group ◽  
Biological Activities ◽  
Synthetic Methods ◽  
Bond Forming ◽  
Drug Candidates ◽  
The Past ◽  
Wide Range

The 1,3-butadiene motif is widely found in many natural products and drug candidates with relevant biological activities. Moreover, dienes are important targets for synthetic chemists, due to their ability to give access to a wide range of functional group transformations, including a broad range of C-C bond-forming processes. Therefore, the stereoselective preparation of dienes have attracted much attention over the past decades, and the search for new synthetic protocols continues unabated. The aim of this review is to give an overview of the diverse methodologies that have emerged in the last decade, with a focus on the synthetic processes that meet the requirements of efficiency and sustainability of modern organic chemistry.

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