N-heterocyclic carbene-metal complexes as bio-organometallic antimicrobial and anticancer drugs, an update (2015–2020)

2020 ◽  
Vol 12 (24) ◽  
pp. 2239-2275
Author(s):  
Siddappa A Patil ◽  
Amy P Hoagland ◽  
Shivaputra A Patil ◽  
Alejandro Bugarin
Keyword(s):  
Metal Complexes ◽  
Biomedical Applications ◽  
Chemical Properties ◽  
Therapeutic Agents ◽  
Heterocyclic Carbenes ◽  
Design Synthesis ◽  
Drug Candidates ◽  
The Past ◽  
Simple Variation ◽  
Future Work

N-heterocyclic carbenes (NHCs) are organic compounds that typically mimic the chemical properties of phosphines. NHCs have made a significant impact on the field of coordination and organometallic chemistry because they are easy to prepare and handle and because of their versatility and stability. Importantly, the physicochemical properties of NHCs can be easily fine-tuned by simple variation of substituents on the nitrogen atoms. Over the past few years, various NHC–metal complexes have been extensively used as metal-based drug candidates and catalysts (homogeneous or heterogeneous) for various applications. To help assist future work with these compounds, this review provides a thorough review on the latest information involving some biomedical applications of NHC–metal complexes. Specifically, this article focuses on recent advances in the design, synthesis, characterization and biomedical applications (e.g., antimicrobial and anticancer activity) of various NHC–metal complexes (metal: silver, gold, palladium, rhodium, ruthenium, iridium and platinum) covering work published from 2015 to 2020. It is hoped that the promising discoveries to date will help accelerate studies on the encouraging potential of NHC–metal complexes as a class of effective therapeutic agents.

scholarly journals Hydrogel-Based Technologies for the Diagnosis of Skin Pathology

Technologies ◽  
2020 ◽  
Vol 8 (3) ◽  
pp. 47
Author(s):  
Christian Wiraja ◽  
Xiaoyu Ning ◽  
Mingyue Cui ◽  
Chenjie Xu
Keyword(s):  
Biomedical Applications ◽  
Polymer Networks ◽  
Therapeutic Agents ◽  
Cross Linking ◽  
Stimuli Responsive ◽  
On Demand ◽  
The Past ◽  
Skin Conditions ◽  
Chemical Cross Linking ◽  
Physical Entanglement

Hydrogels, swellable hydrophilic polymer networks fabricated through chemical cross-linking or physical entanglement are increasingly utilized in various biomedical applications over the past few decades. Hydrogel-based microparticles, dressings and microneedle patches have been explored to achieve safe, sustained and on-demand therapeutic purposes toward numerous skin pathologies, through incorporation of stimuli-responsive moieties and therapeutic agents. More recently, these platforms are expanded to fulfill the diagnostic and monitoring role. Herein, the development of hydrogel technology to achieve diagnosis and monitoring of pathological skin conditions are highlighted, with proteins, nucleic acids, metabolites, and reactive species employed as target biomarkers, among others. The scope of this review includes the characteristics of hydrogel materials, its fabrication procedures, examples of diagnostic studies, as well as discussion pertaining clinical translation of hydrogel systems.

How SIMS microscopy can be used in medicine

1992 ◽  
Vol 50 (2) ◽  
pp. 1602-1603
Author(s):  
Philippe Fragu
Keyword(s):  
Mass Spectrometry ◽  
Biomedical Applications ◽  
Secondary Ion Mass Spectrometry ◽  
Chemical Elements ◽  
Biological Applications ◽  
The Past ◽  
Potential Source ◽  
Secondary Ion ◽  
Chemical Integrity ◽  
Scientific Endeavour

The identification, localization and quantification of intracellular chemical elements is an area of scientific endeavour which has not ceased to develop over the past 30 years. Secondary Ion Mass Spectrometry (SIMS) microscopy is widely used for elemental localization problems in geochemistry, metallurgy and electronics. Although the first commercial instruments were available in 1968, biological applications have been gradual as investigators have systematically examined the potential source of artefacts inherent in the method and sought to develop strategies for the analysis of soft biological material with a lateral resolution equivalent to that of the light microscope. In 1992, the prospects offered by this technique are even more encouraging as prototypes of new ion probes appear capable of achieving the ultimate goal, namely the quantitative analysis of micron and submicron regions. The purpose of this review is to underline the requirements for biomedical applications of SIMS microscopy.Sample preparation methodology should preserve both the structural and the chemical integrity of the tissue.

Click Reactions in Chemistry of Triterpenes - Advances Towards Development of Potential Therapeutics

2018 ◽  
Vol 25 (5) ◽  
pp. 636-658 ◽  
Author(s):  
Jan Pokorny ◽  
Lucie Borkova ◽  
Milan Urban
Keyword(s):  
Biological Activities ◽  
Synthetic Approach ◽  
Clinical Use ◽  
New Approach ◽  
Click Reactions ◽  
Drug Candidates ◽  
The Past ◽  
Low Toxicity ◽  
New Compounds ◽  
Potential Therapeutics

Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use. This review summarizes a new approach to improve both, the activity and ADME-Tox properties by connecting active terpenes to another modifying molecules using click reactions. Within the past few years, this synthetic approach was well explored yielding a lot of great improvements of the parent compounds along with some less successful attempts. A large quantity of the new compounds presented here are superior in both activity and ADME-Tox properties to their parents. This review should serve the researchers who need to promote their hit triterpenic structures towards their clinical use and it is intended as a guide for the chemical synthesis of better drug candidates.

The Potential of Fucose-Containing Sulfated Polysaccharides As Scaffolds for Biomedical Applications

2019 ◽  
Vol 26 (35) ◽  
pp. 6399-6411 ◽  
Author(s):  
Cláudia Nunes ◽  
Manuel A. Coimbra
Keyword(s):  
Tissue Regeneration ◽  
Cell Walls ◽  
Biomedical Applications ◽  
Structural Features ◽  
Therapeutic Agents ◽  
Sulfated Polysaccharides ◽  
Clinical Use ◽  
Health Related ◽  
Pathogen Inhibition ◽  
Health Applications

Marine environments have a high quantity and diversity of sulfated polysaccharides. In coastal regions brown algae are the most abundant biomass producers and their cell walls have fucosecontaining sulfated polysaccharides (FCSP), known as fucans and/or fucoidans. These sulfated compounds have been widely researched for their biomedical properties, namely the immunomodulatory, haemostasis, pathogen inhibition, anti-inflammatory capacity, and antitumoral. These activities are probably due to their ability to mimic the carbohydrate moieties of mammalian glycosaminoglycans. Therefore, the FCSP are interesting compounds for application in health-related subjects, mainly for developing scaffolds for delivery systems or tissue regeneration. FCSP showed potential for these applications also due to their ability to form stable 3D structures with other polymers able to entrap therapeutic agents or cell and growth factors, besides their biocompatibility and biodegradability. However, for the clinical use of these biopolymers well-defined reproducible molecules are required in order to accurately establish relationships between structural features and human health applications.

Current Status in the Design and Development of Agonists and Antagonists of Adenosine A3 Receptor as Potential Therapeutic Agents

2019 ◽  
Vol 25 (25) ◽  
pp. 2772-2787 ◽  
Author(s):  
Raghu P. Mailavaram ◽  
Omar H.A. Al-Attraqchi ◽  
Supratik Kar ◽  
Shinjita Ghosh
Keyword(s):  
Drug Target ◽  
Therapeutic Agents ◽  
G Protein Coupled Receptors ◽  
Current Status ◽  
Renal Diseases ◽  
Adenosine A3 Receptor ◽  
Drug Candidates ◽  
Novel Drugs ◽  
The Family ◽  
G Protein Coupled

Adenosine receptors (ARs) belongs to the family of G-protein coupled receptors (GPCR) that are responsible for the modulation of a wide variety of physiological functions. The ARs are also implicated in many diseases such as cancer, arthritis, cardiovascular and renal diseases. The adenosine A3 receptor (A3AR) has emerged as a potential drug target for the progress of new and effective therapeutic agents for the treatment of various pathological conditions. This receptor’s involvement in many diseases and its validity as a target has been established by many studies. Both agonists and antagonists of A3AR have been extensively investigated in the last decade with the goal of developing novel drugs for treating diseases related to immune disorders, inflammation, cancer, and others. In this review, we shall focus on the medicinal chemistry of A3AR ligands, exploring the diverse chemical classes that have been projected as future leading drug candidates. Also, the recent advances in the therapeuetic applications of A3AR ligands are highlighted.

Design, Synthesis and Pharmacological Evaluation of Novel Antiinflammatory and Analgesic O-Benzyloxime Compounds Derived From Natural Eugenol

2019 ◽  
Vol 16 (10) ◽  
pp. 1157-1166
Author(s):  
Rodrigo César da Silva ◽  
Fabiano Veiga ◽  
Fabiana Cardoso Vilela ◽  
André Victor Pereira ◽  
Thayssa Tavares da Silva Cunha ◽  
...  
Keyword(s):  
Formalin Test ◽  
Docking Studies ◽  
Paw Edema ◽  
Inhibitory Effects ◽  
Structural Pattern ◽  
Design Synthesis ◽  
Drug Candidates ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Cox 1

Background: : A new series of O-benzyloximes derived from eugenol was synthesized and was evaluated for its antinociceptive and anti-inflammatory properties. Methods: : The target compounds were obtained in good global 25-28% yields over 6 steps, which led us to identify compounds (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-(4- (methylthio)benzyloxime (8b), (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-4- bromobenzyloxime (8d) and (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-4- (methylsulfonyl)benzyloxime (8f) as promising bioactive prototypes. Results:: These compounds have significant analgesic and anti-inflammatory effects, as evidenced by formalin-induced mice paw edema and carrageenan-induced mice paw edema tests. In the formalin test, compounds 8b and 8f evidenced both anti-inflammatory and direct analgesic activities and in the carrageenan-induced paw edema, with compounds 8c, 8d, and 8f showing the best inhibitory effects, exceeding the standard drugs indomethacin and celecoxib. Conclusion: : Molecular docking studies have provided additional evidence that the pharmacological profile of these compounds may be related to inhibition of COX enzymes, with slight preference for COX-1. These results led us to identify the new O-benzyloxime ethers 8b, 8d and 8f as orally bioactive prototypes, with a novel structural pattern capable of being explored in further studies aiming at their optimization and development as drug candidates.

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.

Chemistry of Variable Charge Soils

1997 ◽  
Keyword(s):  
Soil Pollution ◽  
Management Practices ◽  
Chemical Properties ◽  
Soil Management ◽  
Soil Productivity ◽  
Basic Difference ◽  
The Past ◽  
Variable Charge ◽  
Constant Charge ◽  
Variable Charge Soils

This book, based on research carried out at the Academia Sinica over the past 30 years, explains the basic difference between the variable charge soils of tropical and subtropical regions, and the constant charge soils of temperate regions. It will focus on the chemical properties of the variable charge soils--properties which have important bearing on soil management practices, including maximizing soil productivity and combating soil pollution.

Evoking Issues of Race and Ethnicity in Research on Physiology and Interpersonal Communication

2020 ◽  
pp. 260-287
Author(s):  
Shardé M. Davis
Keyword(s):  
Interpersonal Communication ◽  
Race And Ethnicity ◽  
Communication Research ◽  
Interpersonal Interactions ◽  
The Past ◽  
Race Ethnicity ◽  
Diverse Groups ◽  
Future Work ◽  
Area Of Study

Investigating the role of physiology in communication research is a burgeoning area of study that has gained considerable attention by relational scholars in the past decade. Unfortunately, very few published studies on this topic have evoked important questions about the role of race and ethnicity. Exploring issues of ethnicity and race provides a more holistic and inclusive view of interpersonal communication across diverse groups and communities. This chapter addresses the gap in literature by considering the ways in which race and ethnicity matter in work on physiology and interpersonal interactions. More specifically, this chapter will first discuss the conceptual underpinnings of race, ethnicity, and other relevant concepts and then review extant research within and beyond the field of communication on race, ethnicity, interpersonal interactions, and physiology. These discussions set the foundation for this chapter to propose new lines of research that pointedly connect these four concepts and advance key principles that scholars should consider in future work.

scholarly journals How to Improve Physico-Chemical Properties of Silk Fibroin Materials for Biomedical Applications?—Blending and Cross-Linking of Silk Fibroin—A Review

Materials ◽  
2021 ◽  
Vol 14 (6) ◽  
pp. 1510
Author(s):  
Sylwia Grabska-Zielińska ◽  
Alina Sionkowska
Keyword(s):  
Silk Fibroin ◽  
Biomedical Applications ◽  
Magnetic Particles ◽  
Chemical Properties ◽  
Ternary Mixtures ◽  
Cross Linking ◽  
Advantages And Disadvantages ◽  
Physico Chemical ◽  
Binary And Ternary Mixtures ◽  
To Receive

This review supplies a report on fresh advances in the field of silk fibroin (SF) biopolymer and its blends with biopolymers as new biomaterials. The review also includes a subsection about silk fibroin mixtures with synthetic polymers. Silk fibroin is commonly used to receive biomaterials. However, the materials based on pure polymer present low mechanical parameters, and high enzymatic degradation rate. These properties can be problematic for tissue engineering applications. An increased interest in two- and three-component mixtures and chemically cross-linked materials has been observed due to their improved physico-chemical properties. These materials can be attractive and desirable for both academic, and, industrial attention because they expose improvements in properties required in the biomedical field. The structure, forms, methods of preparation, and some physico-chemical properties of silk fibroin are discussed in this review. Detailed examples are also given from scientific reports and practical experiments. The most common biopolymers: collagen (Coll), chitosan (CTS), alginate (AL), and hyaluronic acid (HA) are discussed as components of silk fibroin-based mixtures. Examples of binary and ternary mixtures, composites with the addition of magnetic particles, hydroxyapatite or titanium dioxide are also included and given. Additionally, the advantages and disadvantages of chemical, physical, and enzymatic cross-linking were demonstrated.

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