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7,036
result(s) for
"Anti-Infective Agents - chemistry"
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Antimicrobial Efficacy of Two Surface Barrier Discharges with Air Plasma against In Vitro Biofilms
by
Bender, Claudia
,
Schlüter, Rabea
,
Lademann, Jürgen
in
Air plasma
,
Anti-Infective Agents - chemistry
,
Anti-Infective Agents - pharmacology
2013
The treatment of infected wounds is one possible therapeutic aspect of plasma medicine. Chronic wounds are often associated with microbial biofilms which limit the efficacy of antiseptics. The present study investigates two different surface barrier discharges with air plasma to compare their efficacy against microbial biofilms with chlorhexidine digluconate solution (CHX) as representative of an important antibiofilm antiseptic. Pseudomonas aeruginosa SG81 and Staphylococcus epidermidis RP62A were cultivated on polycarbonate discs. The biofilms were treated for 30, 60, 150, 300 or 600 s with plasma or for 600 s with 0.1% CHX, respectively. After treatment, biofilms were dispensed by ultrasound and the antimicrobial effects were determined as difference in the number of the colony forming units by microbial culture. A high antimicrobial efficacy on biofilms of both plasma sources in comparison to CHX treatment was shown. The efficacy differs between the used strains and plasma sources. For illustration, the biofilms were examined under a scanning electron microscope before and after treatment. Additionally, cytotoxicity was determined by the MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay with L929 mouse fibroblast cell line. The cell toxicity of the used plasma limits its applicability on human tissue to maximally 150 s. The emitted UV irradiance was measured to estimate whether UV could limit the application on human tissue at the given parameters. It was found that the UV emission is negligibly low. In conclusion, the results support the assumption that air plasma could be an option for therapy of chronic wounds.
Journal Article
Role of Phenolic Compounds in Human Disease: Current Knowledge and Future Prospects
by
Islam, Md. Rezaul
,
Rahman, Md. Mominur
,
Mithi, Faria Mannan
in
Acids
,
Alzheimer's disease
,
Animals
2021
Inflammation is a natural protective mechanism that occurs when the body’s tissue homeostatic mechanisms are disrupted by biotic, physical, or chemical agents. The immune response generates pro-inflammatory mediators, but excessive output, such as chronic inflammation, contributes to many persistent diseases. Some phenolic compounds work in tandem with nonsteroidal anti-inflammatory drugs (NSAIDs) to inhibit pro-inflammatory mediators’ activity or gene expression, including cyclooxygenase (COX). Various phenolic compounds can also act on transcription factors, such as nuclear factor-κB (NF-κB) or nuclear factor-erythroid factor 2-related factor 2 (Nrf-2), to up-or downregulate elements within the antioxidant response pathways. Phenolic compounds can inhibit enzymes associated with the development of human diseases and have been used to treat various common human ailments, including hypertension, metabolic problems, incendiary infections, and neurodegenerative diseases. The inhibition of the angiotensin-converting enzyme (ACE) by phenolic compounds has been used to treat hypertension. The inhibition of carbohydrate hydrolyzing enzyme represents a type 2 diabetes mellitus therapy, and cholinesterase inhibition has been applied to treat Alzheimer’s disease (AD). Phenolic compounds have also demonstrated anti-inflammatory properties to treat skin diseases, rheumatoid arthritis, and inflammatory bowel disease. Plant extracts and phenolic compounds exert protective effects against oxidative stress and inflammation caused by airborne particulate matter, in addition to a range of anti-inflammatory, anticancer, anti-aging, antibacterial, and antiviral activities. Dietary polyphenols have been used to prevent and treat allergy-related diseases. The chemical and biological contributions of phenolic compounds to cardiovascular disease have also been described. This review summarizes the recent progress delineating the multifunctional roles of phenolic compounds, including their anti-inflammatory properties and the molecular pathways through which they exert anti-inflammatory effects on metabolic disorders. This study also discusses current issues and potential prospects for the therapeutic application of phenolic compounds to various human diseases.
Journal Article
Antibiofilm activity of host defence peptides: complexity provides opportunities
by
Alford, Morgan A
,
Haney, Evan F
,
Hancock Robert E W
in
Antibacterial activity
,
Antibiotics
,
Antifungal agents
2021
Host defence peptides (HDPs) are integral components of innate immunity across all living organisms. These peptides can exert direct antibacterial effects, targeting planktonic cells (referred to as antimicrobial peptides), and exhibit antibiofilm (referred to as antibiofilm peptides), antiviral, antifungal and host-directed immunomodulatory activities. In this Review, we discuss how the complex functional attributes of HDPs provide many opportunities for the development of antimicrobial therapeutics, focusing particularly on their emerging antibiofilm properties. The mechanisms of action of antibiofilm peptides are compared and contrasted with those of antimicrobial peptides. Furthermore, obstacles for the practical translation of candidate peptides into therapeutics and the potential solutions are discussed. Critically, HDPs have the value-added assets of complex functional attributes, particularly antibiofilm and anti-inflammatory activities and their synergy with conventional antibiotics.In this Review, Hancock, Alford and Haney discuss how the complex functional attributes of host defence peptides provide many opportunities for the development of antimicrobial therapeutics, focusing on their emerging antibiofilm properties.
Journal Article
Structural Basis of Multiple Drug-Binding Capacity of the AcrB Multidrug Efflux Pump
by
McDermott, Gerry
,
Nikaido, Hiroshi
,
Zgurskaya, Helen I.
in
Amino acids
,
Analysis
,
Anti-Infective Agents - chemistry
2003
Multidrug efflux pumps cause serious problems in cancer chemotherapy and treatment of bacterial infections. Yet high-resolution structures of ligand-transporter complexes have previously been unavailable. We obtained x-ray crystallographic structures of the trimeric AcrB pump from Escherichia coli with four structurally diverse ligands. The structures show that three molecules of ligands bind simultaneously to the extremely large central cavity of 5000 cubic angstroms, primarily by hydrophobic, aromatic stacking and van der Waals interactions. Each ligand uses a slightly different subset of AcrB residues for binding. The bound ligand molecules often interact with each other, stabilizing the binding.
Journal Article
The re-emergence of natural products for drug discovery in the genomics era
2015
Key Points
Natural products continue to be an important source of leads for new medicines, despite reduced interest from large pharmaceutical companies.
Screening collections of natural products can be assembled economically to provide excellent coverage of drug-like chemical space and in formats that are compatible with high-throughput bioassays.
Metabolomics enables the rapid identification of novel compounds in complex mixtures of natural products and also provides a means to monitor the production of target molecules during fermentation or other production processes.
Metagenomics and other genetic engineering techniques are enabling the production of target compounds in convenient systems, breaking away from the bottleneck otherwise created by microorganisms that are difficult to culture.
Examples of recent and current applications of natural products are described for the discovery of antimicrobials and for inhibitors of protein–protein interactions, particularly as anticancer agents.
The screening of natural products for lead molecules is an attractive strategy, as most natural products fall within biologically relevant chemical space. In this Review, Harvey, Edrada-Ebel and Quinn discuss how advanced screening, metabolomics and metagenomics approaches can be used in the identification, validation and production of naturally sourced compounds, and highlight examples of naturally derived antimicrobials and inhibitors of protein–protein interactions.
Natural products have been a rich source of compounds for drug discovery. However, their use has diminished in the past two decades, in part because of technical barriers to screening natural products in high-throughput assays against molecular targets. Here, we review strategies for natural product screening that harness the recent technical advances that have reduced these barriers. We also assess the use of genomic and metabolomic approaches to augment traditional methods of studying natural products, and highlight recent examples of natural products in antimicrobial drug discovery and as inhibitors of protein–protein interactions. The growing appreciation of functional assays and phenotypic screens may further contribute to a revival of interest in natural products for drug discovery.
Journal Article
Traditional Uses, Bioactive Chemical Constituents, and Pharmacological and Toxicological Activities of Glycyrrhiza glabra L. (Fabaceae)
by
El-Saber Batiha, Gaber
,
Magdy Beshbishy, Amany
,
M. Abdel-Daim, Mohamed
in
Animals
,
Anti-Infective Agents - adverse effects
,
Anti-Infective Agents - chemistry
2020
Traditional herbal remedies have been attracting attention as prospective alternative resources of therapy for diverse diseases across many nations. In recent decades, medicinal plants have been gaining wider acceptance due to the perception that these plants, as natural products, have fewer side effects and improved efficacy compared to their synthetic counterparts. Glycyrrhiza glabra L. (Licorice) is a small perennial herb that has been traditionally used to treat many diseases, such as respiratory disorders, hyperdipsia, epilepsy, fever, sexual debility, paralysis, stomach ulcers, rheumatism, skin diseases, hemorrhagic diseases, and jaundice. Moreover, chemical analysis of the G. glabra extracts revealed the presence of several organic acids, liquirtin, rhamnoliquirilin, liquiritigenin, prenyllicoflavone A, glucoliquiritin apioside, 1-metho-xyphaseolin, shinpterocarpin, shinflavanone, licopyranocoumarin, glisoflavone, licoarylcoumarin, glycyrrhizin, isoangustone A, semilicoisoflavone B, licoriphenone, and 1-methoxyficifolinol, kanzonol R and several volatile components. Pharmacological activities of G. glabra have been evaluated against various microorganisms and parasites, including pathogenic bacteria, viruses, and Plasmodium falciparum, and completely eradicated P. yoelii parasites. Additionally, it shows antioxidant, antifungal, anticarcinogenic, anti-inflammatory, and cytotoxic activities. The current review examined the phytochemical composition, pharmacological activities, pharmacokinetics, and toxic activities of G. glabra extracts as well as its phytoconstituents.
Journal Article
Chia Seeds (Salvia Hispanica L.): An Overview—Phytochemical Profile, Isolation Methods, and Application
by
Cör, Darija
,
Knez Hrnčič, Maša
,
Knez, Željko
in
Anti-Infective Agents - analysis
,
Anti-Infective Agents - chemistry
,
Anti-Infective Agents - isolation & purification
2019
Chia (Salvia hispanica L.) is a small seed that comes from an annual herbaceous plant, Salvia hispanica L. In recent years, usage of Chia seeds has tremendously grown due to their high nutritional and medicinal values. Chia was cultivated by Mesopotamian cultures, but then disappeared for centuries until the middle of the 20th century, when it was rediscovered. Chia seeds contain healthy ω-3 fatty acids, polyunsaturated fatty acids, dietary fiber, proteins, vitamins, and some minerals. Besides this, the seeds are an excellent source of polyphenols and antioxidants, such as caffeic acid, rosmarinic acid, myricetin, quercetin, and others. Today, chia has been analyzed in different areas of research. Researches around the world have been investigating the benefits of chia seeds in the medicinal, pharmaceutical, and food industry. Chia oil is today one of the most valuable oils on the market. Different extraction methods have been used to produce the oil. In the present study, an extensive overview of the chemical composition, nutritional properties, and antioxidant and antimicrobial activities, along with extraction methods used to produce chia oil, will be discussed.
Journal Article
Broccoli or Sulforaphane: Is It the Source or Dose That Matters?
by
Kensler, Thomas W.
,
Yagishita, Yoko
,
Fahey, Jed W.
in
allometric scaling
,
Animals
,
Anti-Infective Agents - chemistry
2019
There is robust epidemiological evidence for the beneficial effects of broccoli consumption on health, many of them clearly mediated by the isothiocyanate sulforaphane. Present in the plant as its precursor, glucoraphanin, sulforaphane is formed through the actions of myrosinase, a β-thioglucosidase present in either the plant tissue or the mammalian microbiome. Since first isolated from broccoli and demonstrated to have cancer chemoprotective properties in rats in the early 1990s, over 3000 publications have described its efficacy in rodent disease models, underlying mechanisms of action or, to date, over 50 clinical trials examining pharmacokinetics, pharmacodynamics and disease mitigation. This review evaluates the current state of knowledge regarding the relationships between formulation (e.g., plants, sprouts, beverages, supplements), bioavailability and efficacy, and the doses of glucoraphanin and/or sulforaphane that have been used in pre-clinical and clinical studies. We pay special attention to the challenges for better integration of animal model and clinical studies, particularly with regard to selection of dose and route of administration. More effort is required to elucidate underlying mechanisms of action and to develop and validate biomarkers of pharmacodynamic action in humans. A sobering lesson is that changes in approach will be required to implement a public health paradigm for dispensing benefit across all spectrums of the global population.
Journal Article
Anticancer and antimicrobial activity of biosynthesized Red Sea marine algal silver nanoparticles
2022
Biosynthesis of silver nanoparticles (AgNPs) is emerging as a simple and eco-friendly alternative to conventional chemical synthesis methods. The role of AgNPs is expanding as antimicrobial and anticancer agents, sensors, nanoelectronic devices, and imaging contrast agents. In this study, biogenic AgNPs were synthesized using extracts of different marine algae species, including
Ulva rigida
(green alga),
Cystoseira myrica
(brown alga), and
Gracilaria foliifera
(red alga), as reducing and capping agents. The Physiochemical properties, cytotoxicity, anticancer and antimicrobial activities of the biosynthesized AgNPs were assessed. Surface plasmonic bands of the biosynthesized AgNPs capped with
U. rigida
,
C. myrica
, and
G. foliifera
extracts were visually observed to determine a colour change, and their peaks were observed at 424 nm, 409 nm, and 415 nm, respectively, by UV–Vis spectroscopy; transmission electron microscopy (TEM) indicated an almost spherical shape of AgNPs with nanoscale sizes of 12 nm, 17 nm, and 24 nm, respectively. Fourier transform-infrared (FTIR) spectroscopy analysis suggested that different molecules attached to AgNPs through OH, C=O, and amide groups. The major constituents of the aqueous algal extracts included, terpenoids, polyphenols, sulfonates, polysaccharides, fatty acids, chlorophylls, amide proteins, flavonoids, carotenoids, aliphatic fluoro compounds, volatile compounds, alkalines, pyruvic acid and agar groups. The cytotoxicity and anticancer activities of the biosynthesized AgNPs were assessed using
Artemia salina
nauplii, normal skin cell lines (HFb-4), and breast cancer cell lines (MCF-7 cell line). The lethality was found to be directly proportional to the AgNP concentration. The IC
50
values of
C. myrica
and G
. foliifera
AgNPs against
A. saline
nauplii were 5 and 10 μg ml
−1
after 4 h and 16 h, respectively, whereas
U. rigida
AgNPs did not exhibit cytotoxic effects. Anticancer activity of the biosynthesized AgNPs was dose dependent. The IC
50
values of the biosynthesized AgNPs were 13, 13, and 43 µg ml
−1
for
U. rigida, C. myrica,
and
G. foliifera
, respectively.
U. rigida
AgNPs particularly exhibited potent anticancer activity (92.62%) against a human breast adenocarcinoma cell line (MCF-7) with high selectivity compared the normal cells (IC
50
= 13 µg/ml, SI = 3.2), followed by
C. myrica
AgNPs (IC
50
= 13 µg/ml, SI = 3.07). Furthermore, the biosynthesized AgNPs exhibited strong antifungal activity against dermatophyte pathogenic moulds and mild antibacterial activity against the food borne pathogen bacteria. The highest antimicrobial activity was recorded for the
U. rigida
AgNPs, followed by those capped with
C. myrica
and
G. foliifera
extracts, respectively. AgNPs capped with the
U. rigida
extract exhibited the highest antimicrobial activity against
Trichophyton mantigrophytes
(40 mm), followed by
Trichosporon cataneum
(30 mm) and
E. coli
(19 mm), with minimal lethal concentration of 32 and 64 μg ml
−1
respectively. The study finally revealed that extracts of marine algal species, particularly
U. rigida
extracts, could be effectively used as reducing agents for the green synthesis of AgNPs. These AgNPs are considered efficient alternative antidermatophytes for skin infections and anticancer agents against the MCF-7 cell line.
Journal Article
Pharmacological Update Properties of Aloe Vera and its Major Active Constituents
by
Sánchez, Marta
,
Iglesias, Irene
,
González-Burgos, Elena
in
Aloe - chemistry
,
aloe vera
,
Anti-Infective Agents - chemistry
2020
Aloe vera has been traditionally used to treat skin injuries (burns, cuts, insect bites, and eczemas) and digestive problems because its anti-inflammatory, antimicrobial, and wound healing properties. Research on this medicinal plant has been aimed at validating traditional uses and deepening the mechanism of action, identifying the compounds responsible for these activities. The most investigated active compounds are aloe-emodin, aloin, aloesin, emodin, and acemannan. Likewise, new actions have been investigated for Aloe vera and its active compounds. This review provides an overview of current pharmacological studies (in vitro, in vivo, and clinical trials), written in English during the last six years (2014–2019). In particular, new pharmacological data research has shown that most studies refer to anti-cancer action, skin and digestive protective activity, and antimicrobial properties. Most recent works are in vitro and in vivo. Clinical trials have been conducted just with Aloe vera, but not with isolated compounds; therefore, it would be interesting to study the clinical effect of relevant metabolites in different human conditions and pathologies. The promising results of these studies in basic research encourage a greater number of clinical trials to test the clinical application of Aloe vera and its main compounds, particularly on bone protection, cancer, and diabetes.
Journal Article