Turning Fear of Boron Toxicity into Boron-containing Drug Design

2019 ◽  
Vol 26 (26) ◽  
pp. 5005-5018 ◽  
Author(s):  
Marvin A. Soriano-Ursúa ◽  
Eunice D. Farfán-García ◽  
Simonetta Geninatti-Crich

Background: Despite the historical employment of boron-containing compounds (BCCs) with medicinal purposes, the reported cases of BCC toxicity in humans during the twentieth-century drived us towards a “boron-withdrawal” period. Fortunately, the use of boric acid for specific purposes remains, and the discovery of natural BCCs with biological action attractive for therapeutic purposes as well as the introduction of some new BCCs for clinical use has reactivated the interest in studying the properties of these BCCs. Methods: We carried out a structured search of bibliographic databases for scientific peerreviewed research literature regarding boron toxicity and linked that information to that of BCCs in drug design and development. A deductive qualitative content analysis methodology was applied to analyse the interventions and findings of the included studies using a theoretical outline. Results: This review recapitulates the following on a timeline: the boron uses in medicine, the data known about the toxicological profiles of some BCCs, the pharmacological properties of some BCCs that are employed in cancer and infectious disease therapies, and the known properties of BCCs recently introduced into clinical assays as well as the identification of their structure-activity relationships for toxicity and therapeutic use. Then, we discuss the use of new approaches taking advantage of some toxicological data to identify potent and efficient BCCs for prevention and therapy while limiting their toxic effects. Conclusion: Data for boron toxicity can be strategically used for boron-containing drug design.

2020 ◽  
Vol 11 (1) ◽  
pp. 8502-8537 ◽  

The world population is aging, and cancer is always considered to be one of the major causes of death all over the globe. The advent of recent drug-targeted therapies undoubtedly is going to reduce the incidence of cancer over the coming years. However, the frequency of occurrence of such chronic diseases like cancer would continue to increase. Therefore, the search for a safer and cost-effective treatment is urgently needed. Phytochemicals found in plants, foods, vegetables, tea, etc. have emerged as proven therapeutic compounds modulating signaling pathways involved in cancer. We carried out a structured search of bibliographic databases for peer-reviewed research literature using the keywords: cancer chemoprevention, flavonoids, dietary polyphenols, terpenoids, bioactive, microbiota. Quality of the retrieved papers and characteristic outcomes of the articles included in the study was assessed by employing standard tools and deductive qualitative content analysis methodology. The development of personalized supplements comprising particular phytochemicals has been the key, especially dealing with chronic inflammatory disorders like cancer. Better understanding at the molecular level explains the influence of phytochemicals on human health, which has been extensively covered through this review. Moreover, the wide collection of dietary polyphenols that has significant properties in reference to human health has been highlighted. Furthermore, the etiology of end products of such phytochemicals, especially on the modulation of gut microbiota and the host-microbial interactions thereof, need to be properly understood. The present study summarizes the chemoprevention and treatment of cancer using the bioactive components, including flavonoids, dietary polyphenols, and terpenoids. Likewise, the effect of dietary polyphenols on the human gut microbiota has been realized more recently. However, more research is needed in this field, especially focused on the communications, interlinks between the gut microbiota and polyphenols with the precise mechanism of action.


2020 ◽  
Vol 27 ◽  
Author(s):  
Anil K. Sharma ◽  
Varruchi Sharma ◽  
Arun Sharma ◽  
Suresh Pallikkuth

Background: Recent pandemic of coronavirus disease caused by a novel coronavirus SARS-CoV-2 in humans is the third outbreak by this family of viruses leading to an acute respiratory infection which has been a major cause of morbidity and mortality worldwide.The virus belongs to the genus, Betacoronavirus which has been recently reported to have significant similarity (>89%) to a severe acute respiratory syndrome (SARS)-related member of the Sarbecoviruses. Current researches are not sufficient to understand the etiological and immunopathobiological parameters related to COVID-19 so as to have a therapeutic solution to the problem. Methods: A structured search of bibliographic databases for peer-reviewed research literature has been carried out using focused review questions and inclusion/exclusion criteria. Further Standard tools were implied in order to appraise the quality of retrieved papers. The characteristic outcomes of screened research and review articles along with analysis of the interventions and findings of included studies using a conceptual framework have been described employing a deductive qualitative content analysis methodology. Results: This review systematically summarizes the immune-pathobiological characteristics, diagnosis, potential therapeutic options for the treatment and prevention of COVID-19 based on the current published literature and evidence. The current review has covered 125 peer-reviewed articles, majority of which are from high-income technically developed countries providing the most recent updates about the current understanding of the COVID-19 bringing all the significant findings and related researches together at a single platform. In addition, possible therapeutic interventions, treatment strategies and vaccine development initiatives to manage COVID-19 have been proposed. Conclusions: It is anticipated that this review would certainly assist the public in general and scientific community in particular to recognize and effectively deal with COVID-19, providing a reference guide for futuristic studies.


2019 ◽  
Vol 26 (30) ◽  
pp. 5711-5726 ◽  
Author(s):  
Naveed Ahmed Khan ◽  
Ayaz Anwar ◽  
Ruqaiyyah Siddiqui

Background:First discovered in the early 1970s, Acanthamoeba keratitis has remained a major eye infection and presents a significant threat to the public health, especially in developing countries. The aim is to present a timely review of our current understanding of the advances made in this field in a comprehensible manner and includes novel concepts and provides clear directions for immediate research priorities.Methods:We undertook a search of bibliographic databases for peer-reviewed research literature and also summarized our published results in this field.Results:The present review focuses on novel diagnostic and therapeutic strategies in details which can provide access to management and treatment of Acanthamoeba keratitis. This coupled with the recently available genome sequence information together with high throughput genomics technology and innovative approaches should stimulate interest in the rational design of preventative and therapeutic measures. Current treatment of Acanthamoeba keratitis is problematic and often leads to infection recurrence. Better understanding of diagnosis, pathogenesis, pathophysiology and therapeutic regimens, would lead to novel strategies in treatment and prophylaxis.


2021 ◽  
Author(s):  
◽  
Gemma Amy Helleur Hiscock

<p>This qualitative content analysis research study examines how Margaret Mahy used emotion in the School Journal to form insights into reader appeal, reader response and the social construction of childhood. This research study examines Mahy’s contribution to the School Journal. The study explores this body of work in terms of how its author uses emotion to captivate readers by evoking the feelings associated with childhood. The underlying objective of the study was to provide insights into why Mahy’s work is so treasured and memorable; to explain how she uses emotion to captivate readers, and how this contributes to the social construction of childhood. The prose and poetry Mahy contributed to the School Journal prove to be a significant, rich and uncharted resource for the purposes of this research investigation. Analysis of this body of work has allowed for greater insights and understanding into Mahy’s contribution to children’s literature. It has also allowed for a greater appreciation of how Mahy’s use of emotion contributes to the social construction of childhood. This type of content analysis research study proves to be invaluable in the development of reader’s advisory services to young people. The employment of a content analysis methodology, underpinned by a discourse analysis approach, enabled the emotional narratives of Mahy’s text to be explained and understood. The study’s findings, that lightness and aliveness are the most prevalent and persuasive emotions operating within Mahy’s text, was substantiated through analysis of actual reader responses. This investigation is most applicable to school librarians, children’s librarians and educators. The study has broader implications for the improvement of client interaction and collection development in youth library services</p>


Author(s):  
Ranita Pal ◽  
Pratim Kumar Chattaraj

In the current pandemic-stricken world, quantitative structure-activity relationship (QSAR) analysis has become a necessity in the domain of molecular biology and drug design, realizing that it helps estimate properties and activities of a compound, without actually having to spend time and resources to synthesize it in the laboratory. Correlating the molecular structure of a compound with its activity depends on the choice of the descriptors, which becomes a difficult and confusing task when we have so many to choose from. In this mini-review, the authors delineate the importance of very simple and easy to compute descriptors in estimating various molecular properties/toxicity.


Author(s):  
Mohamed Jawed Ahsan

Background: Cancer is the first or second leading cause of premature death in 134 of 183 countries in the world. 1,3,4-Oxadiazoles are five memebered heterocyclic rings containing two nitrogen (two atoms) and oxygen (one atom). They show better thermal stability, metabolic stability, aqueous solubility and lower lipophilicity than the other isomeric oxadiazoles. They are important class of heterocycles present in many drug structures like Raltegravir, Furamizole Tidazosin, Nesapidil, Setileuton (MK-0633) and Zibotentan. Presence of this nucleus in the therapeutics has made them an indispensable anchor for drug design and development. Several 1,3,4-oxadiazoles are prepared and reported as anticancer agents by numerous scientists worldwide. Objectives: The present review discusses the anticancer potentials together with the molecular targets of 1,3,4-oxadiazoles reported since 2010. The structure activity relationship (SAR) and molecular docking simulation on different targets have also been discussed herein. Some of the important cancer targets have also been explored. Methods: The most potent 1,3,4-oxadiazoles reported in literature was highlighted in the manuscript. The anticancer activity was reported in terms of growth percent (GP), percent growth inhibition (%GI), GI50, IC50, and LC50 and TGI. Results: 1,3,4-Oxadiazoles are an important heterocyclic scaffolds with broad spectrum biological activities. They may be either mono substituted or disubstituted and act as an indispensable anchor for drug design and discovery due to their thermal stability together with low lipophilicity. They exhibited anticancer potentials and showed the inhibitions of various cancer targets. Conclusion: The discussion outlined herein will proved to be a helpful and vital tool for medicinal chemists investigating and working with 1,3,4-oxadiazoles and anticancer research programs.


Author(s):  
Lynna J. Ausburn ◽  
Floyd B. Ausburn ◽  
Paul J. Kroutter

This study used a cross-case analysis methodology to compare four line-of-inquiry studies of Desktop Virtual Environments (DVEs) to examine the relationships of gender and computer gaming experience to learning performance and perceptions. Comparison was made of learning patterns in a general non-technical DVE with patterns in technically complex, occupationally-specific DVEs. Two oppositely-gendered occupations were sampled in the technical studies: surgical technology and policing. The cross-case analysis confirmed in the occupationally-specific DVEs the gender effect in favor of males on spatial learning that has been documented in previous research literature. It also supported a gaming experience effect in favor of more experienced gamers, but did not clearly demonstrate a relationship between gender and gaming experience. Several implications and recommendations are presented for practitioners and researchers in adult vocational, career, and technical education.


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