scholarly journals Fulvic Acid: an Active Food Additive or Medication?

2020 ◽  
Vol 27 (3) ◽  
pp. 78-91
Author(s):  
N. S. Benderskii ◽  
O. M. Kudelina ◽  
E. V. Gantsgorn ◽  
A. V. Safronenko

This review article is devoted to the fundamental task of pharmacology, i.e. the research and discovery of novel medications that render the maximal therapeutic effect at the minimal side consequences to health. Over recent years, the world has witnessed a growing interest towards natural organic compounds on the basis of humic substances (HS), which are broadly applied in animal husbandry, agriculture and veterinary medicine due to a wide spectrum of biologically active properties. The results of chemical and biological trials demonstrate that HS have a great potential for various fields of medicine.Numerous studies have demonstrated the cardioprotective, antioxidant, antitumour, antibacterial, antiviral, antifungal, antiallergic, membranotropic, hepatoprotective and anti-inflammatory properties of HS. In addition, these substances exhibit a stimulating effect on metabolism, thus enhancing specific and non-specific organismal resistance. Published evidence suggests no toxicity of HS and no inherent teratogenic, embryotoxic, mutagenic or carcinogenic properties.Fulvic acid (FA) belongs to humic acids, a family of HS. In the present study, we review its chemical properties and biological activity from the standpoint of traditional medicine. Understanding biological properties of FA and its usage in novel drug design is a perspective avenue of research in contemporary medicine.Published sources referenced in this review are indexed in Scopus, Web of Science, MedLine, the Cochrane Library, eLIBRARY, PubMed and other relevant databases.

Química Nova ◽  
2021 ◽  
Author(s):  
Dartagnan Ferreira ◽  
Valter Murie ◽  
Thiago Santos ◽  
Paulo Vieira ◽  
Giuliano Clososki

RECENT ADVANCES IN SELECTIVE FUNCTIONALIZATION OF QUINOLINES. Heterocyclic compounds form an important and extensive group of organic substances. Among nitrogenous heterocyclic molecules, quinolines stand out for exhibiting attractive chemical and biological properties. These substances can be used as ligands, sensors, luminescent and agrochemical materials. In addition, quinoline-containing compounds can exhibit a wide spectrum of pharmacological properties, allowing their use in several approved drugs nowadays. Due to its importance, the synthesis of molecules containing this nucleus becomes a point of interest for synthetic chemists. In this way, several methodologies have been recently developed to prepare quinoline derivatives with high structural diversity. Such chemical transformations allow the chemical modification of these rings with high selectivity and tolerance to diverse functional groups and these properties have been conveniently used in the preparation of biologically active molecules containing this unit. Herein, we present a review of the main methodologies employed in the selective functionalization of quinolines in the last twenty years. In this context, a brief introduction addressing general synthetic and medicinal aspects related to the functionalization positions of the quinoline ring is presented. Several methodologies used in the functionalization of this moiety are discussed, as well relevant synthetic applications, both in the preparation and functionalization of substances of biological interest.


2021 ◽  
Vol 9 (A) ◽  
pp. 61-67
Author(s):  
Svetlana Ivasenko ◽  
Perizat Orazbayeva ◽  
Krystyna Skalicka–Wozniak ◽  
Agnieszka Ludwiczuk ◽  
Alexandr Marchenko ◽  
...  

BACKGROUND: The medicinal plant of Thymus serpyllum L. in nature, depending on the geographical region, climatic conditions, and growing environment, is represented with some chemotypes. Composition and quantitative content of the basic groups of the biologically active substances can be differed, and thus their biological properties are also various. AIM: The aim of the study was to determine possibility of the using the ultrasonic extracts of two chemotypes of T. serpyllum L. of Central Kazakhstan as an antimicrobial agent against test strains of microorganisms. MATERIALS AND METHODS: Two samples of T. serpyllum were extracted with 70% ethanol using ultrasound. The polyphenol content of the ultrasound extracts was determined using the LC-ultraviolet-ESI- tandem mass spectrometry technique. A study of an antimicrobial activity of the ultrasonic extracts was performed with eight strains of Gram-positive bacteria, six strains of Gram-negative bacteria, and four cultures of fungi. RESULTS: The ultrasonic extracts of two chemotypes of T. serpyllum L. are similar in composition of phenolic compounds but differ in a quantitative content of phenolic acids and flavonoids, except for a rosmarinic acid. The ultrasonic extracts have a wide spectrum of antimicrobial activity, exhibit the bactericidal or bacteriostatic activity against all tested bacteria and fungi at a concentration of 0.0625–20 mg/ml, but differ in their strength of action against test strains of microorganisms. CONCLUSION: The ultrasonic extracts of two chemotypes of T. serpyllum L. of Central Kazakhstan can be considered as a potential drug with a wide spectrum of antimicrobial activity. The results of chromatographic analysis will be used for standardization of a drug.


2021 ◽  
Vol 16 ◽  
Author(s):  
Nelson José Freitas da Silveira ◽  
Walter Filgueira de Azevedo Jr. ◽  
Rita Cardoso Guedes ◽  
Leandro Marcos Santos ◽  
Rodolfo Cabral Marcelino ◽  
...  

Background: In the rational drug development field, a bioisosterism is a tool that improves lead compounds performance, reffering to molecular fragment substitution that has similar physical-chemical properties. Thus, it is possible to modulate drug properties such as absorption, toxicity, and half-life increase. This modulation is of pivotal importance in the discovery, development, identification, and interpretation of the mode of action of biologically active compounds. Objective: Our purpose here is to review the development and application of bioisosterism in drug discovery. In this study history, applications, and use of bioisosteric molecules to create new drugs with high binding affinity in the protein-ligand complexes are described. Method: It is an approach for molecular modification of a prototype based on the replacement of molecular fragments with similar physicochemical properties, being related to the pharmacokinetic and pharmacodynamic phase, aiming at the optimization of the molecules. Results: Discovery, development, identification, and interpretation of the mode of action of biologically active compounds are the most important factors for drug design. The strategy adopted for the improvement of leading compounds is bioisosterism. Conclusion: Bioisosterism methodology is a great advance for obtaining new analogs to existing drugs, enabling the development of new drugs with reduced toxicity, in a comparative analysis with existing drugs. Bioisosterism has a wide spectrum to assist in several research areas.


Author(s):  
Abdualrahman Mohammed Abdualkader ◽  
Muhammad Taher ◽  
Nik Idris Nik Yusoff

Various literature sources have documented sydnones as important molecules with exclusive chemical properties and a wide spectrum of bioactivities. Sydnone can be defined as a five-membered pseudo-aromatic heterocyclic molecule. Classically, 1,2,3-oxadiazole forms the main skeleton of sydnone. The molecule has delocalized balanced positive and negative charges. The five annular atoms share the positive charge and the enolate-like exocyclic oxygen atom bears the negative charge. The hydrogen atom at the position C4 was proved to have acidic and nucleophilic functionalities making the sydnone ring reactive towards electrophilic reagents. These unique chemical features enable sydnones to interact with biomolecules resulting in important therapeutic effects like anticancer, antidiabetic, antimicrobial, antioxidant and anti-inflammatory. Consequently, we aim from the current article to review the available chemical and pharmacological information on sydnone and its derivatives.


Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7264
Author(s):  
Piotr Rosiak ◽  
Ilona Latanska ◽  
Paulina Paul ◽  
Witold Sujka ◽  
Beata Kolesinska

Modified alginates have a wide range of applications, including in the manufacture of dressings and scaffolds used for regenerative medicine, in systems for selective drug delivery, and as hydrogel materials. This literature review discusses the methods used to modify alginates and obtain materials with new or improved functional properties. It discusses the diverse biological and functional activity of alginates. It presents methods of modification that utilize both natural and synthetic peptides, and describes their influence on the biological properties of the alginates. The success of functionalization depends on the reaction conditions being sufficient to guarantee the desired transformations and provide modified alginates with new desirable properties, but mild enough to prevent degradation of the alginates. This review is a literature description of efficient methods of alginate functionalization using biologically active ligands. Particular attention was paid to methods of alginate functionalization with peptides, because the combination of the properties of alginates and peptides leads to the obtaining of conjugates with properties resulting from both components as well as a completely new, different functionality.


2020 ◽  
Vol 63 (5) ◽  
pp. 1618-1635
Author(s):  
Céline Richard ◽  
Mary Lauren Neel ◽  
Arnaud Jeanvoine ◽  
Sharon Mc Connell ◽  
Alison Gehred ◽  
...  

Purpose We sought to critically analyze and evaluate published evidence regarding feasibility and clinical potential for predicting neurodevelopmental outcomes of the frequency-following responses (FFRs) to speech recordings in neonates (birth to 28 days). Method A systematic search of MeSH terms in the Cumulative Index to Nursing and Allied HealthLiterature, Embase, Google Scholar, Ovid Medline (R) and E-Pub Ahead of Print, In-Process & Other Non-Indexed Citations and Daily, Web of Science, SCOPUS, COCHRANE Library, and ClinicalTrials.gov was performed. Manual review of all items identified in the search was performed by two independent reviewers. Articles were evaluated based on the level of methodological quality and evidence according to the RTI item bank. Results Seven articles met inclusion criteria. None of the included studies reported neurodevelopmental outcomes past 3 months of age. Quality of the evidence ranged from moderate to high. Protocol variations were frequent. Conclusions Based on this systematic review, the FFR to speech can capture both temporal and spectral acoustic features in neonates. It can accurately be recorded in a fast and easy manner at the infant's bedside. However, at this time, further studies are needed to identify and validate which FFR features could be incorporated as an addition to standard evaluation of infant sound processing evaluation in subcortico-cortical networks. This review identifies the need for further research focused on identifying specific features of the neonatal FFRs, those with predictive value for early childhood outcomes to help guide targeted early speech and hearing interventions.


Author(s):  
Mariane Beatriz Sordi ◽  
Ariadne Cristiane Cabral da Cruz ◽  
Águedo Aragones ◽  
Mabel Mariela Rodríguez Cordeiro ◽  
Ricardo de Souza Magini

The aim of this study was to synthesize, characterize, and evaluate degradation and biocompatibility of poly(lactic-co-glycolic acid) + hydroxyapatite / β-tricalcium phosphate (PLGA+HA/βTCP) scaffolds incorporating simvastatin (SIM) to verify if this biomaterial might be promising for bone tissue engineering. Samples were obtained by the solvent evaporation technique. Biphasic ceramic particles (70% HA, 30% βTCP) were added to PLGA in a ratio of 1:1. Samples with SIM received 1% (m:m) of this medication. Scaffolds were synthesized in a cylindric-shape and sterilized by ethylene oxide. For degradation analysis, samples were immersed in PBS at 37 °C under constant stirring for 7, 14, 21, and 28 days. Non-degraded samples were taken as reference. Mass variation, scanning electron microscopy, porosity analysis, Fourier transform infrared spectroscopy, differential scanning calorimetry, and thermogravimetry were performed to evaluate physico-chemical properties. Wettability and cytotoxicity tests were conducted to evaluate the biocompatibility. Microscopic images revealed the presence of macro, meso, and micropores in the polymer structure with HA/βTCP particles homogeneously dispersed. Chemical and thermal analyses presented very similar results for both PLGA+HA/βTCP and PLGA+HA/βTCP+SIM. The incorporation of simvastatin improved the hydrophilicity of scaffolds. Additionally, PLGA+HA/βTCP and PLGA+HA/βTCP+SIM scaffolds were biocompatible for osteoblasts and mesenchymal stem cells. In summary, PLGA+HA/βTCP scaffolds incorporating simvastatin presented adequate structural, chemical, thermal, and biological properties for bone tissue engineering.


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.


Author(s):  
G. Bezrukova ◽  
M. Shalashova ◽  
T. Novikova ◽  
V. Spirin

On the basis of updated data, the influence of working conditions on the nosological structure of professional morbidity of workers in the basic branches of animal husbandry of the Russian Federation is analyzed. In total, from 2011 to 2017, occupational diseases were detected in 823 livestock workers, who received 881 diagnoses, of which the share of cattle breeders, poultry breeders and pig breeders accounted for 95,0, 3,4 and 1,6 % of cases, respectively. Harmful labor factors that cause the formation of professional pathology in livestock breeders were: physical overload (64,6 %), industrial contact with cattle infected with Brucella abortus bovis (32,6 %) and the presence of dust in the work area containing toxic chemicals and aggressive biological mixes (2,3 %). A high etiopathogenetic relationship between the nosological form of the disease and working conditions in the profession was revealed. In livestock workers, occupational diseases were formed under the influence of physical overloads (64,6 %) and infection with the brucellosis pathogen (34,6 %); in pig farming, as a result of the severity of labor (84.5 %) and air pollution of the working area with dust, chemical toxicants and biologically active substances (7,7 %); in poultry farming, occupational health risk was associated with allergization of working with poultry products (50 %) and physical overloads (42,9 %). In the nosological spectrum of accumulated occupational diseases of livestock workers, the first rank places were occupied by residual brucellosis (32,6 %), radiculopathy of the cervical and lumbo-sacral levels (25,8 %), mono- and polyneuropathy (25,2 %), arthrosis and polyarthrosis (8,2 %), shoulder and shoulder periarthrosis (5,4 %). In poultry workers ¾ respiratory diseases: allergic bronchial asthma (39,3 %), allergic rhinopharyngitis (10,7 %) and cervical and lumbo-sacral radiculopathy (21,4 %). Pig workers were mainly diagnosed with cervical and lumbo-sacral radiculopathy (46,2 %), mono- and polyneuropathy (23,1 %), shoulder periarthrosis (15.4 %).


2020 ◽  
Vol 27 (28) ◽  
pp. 4584-4592 ◽  
Author(s):  
Avik Khan ◽  
Baobin Wang ◽  
Yonghao Ni

Regenerative medicine represents an emerging multidisciplinary field that brings together engineering methods and complexity of life sciences into a unified fundamental understanding of structure-property relationship in micro/nano environment to develop the next generation of scaffolds and hydrogels to restore or improve tissue functions. Chitosan has several unique physico-chemical properties that make it a highly desirable polysaccharide for various applications such as, biomedical, food, nutraceutical, agriculture, packaging, coating, etc. However, the utilization of chitosan in regenerative medicine is often limited due to its inadequate mechanical, barrier and thermal properties. Cellulosic nanomaterials (CNs), owing to their exceptional mechanical strength, ease of chemical modification, biocompatibility and favorable interaction with chitosan, represent an attractive candidate for the fabrication of chitosan/ CNs scaffolds and hydrogels. The unique mechanical and biological properties of the chitosan/CNs bio-nanocomposite make them a material of choice for the development of next generation bio-scaffolds and hydrogels for regenerative medicine applications. In this review, we have summarized the preparation method, mechanical properties, morphology, cytotoxicity/ biocompatibility of chitosan/CNs nanocomposites for regenerative medicine applications, which comprises tissue engineering and wound dressing applications.


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