antimicrobial agent
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Biomimetic antimicrobial polymers have been an area of great interest as the need for novel antimicrobial compounds grows due to the development of resistance. These polymers were designed and developed to mimic naturally occurring antimicrobial peptides in both physicochemical composition and mechanism of action. These antimicrobial peptide mimetic polymers have been extensively investigated using chemical, biophysical, microbiological, and computational approaches to gain a deeper understanding of the molecular interactions that drive function. These studies have helped inform SARs, mechanism of action, and general physicochemical factors that influence the activity and properties of antimicrobial polymers. However, there are still lingering questions in this field regarding 3D structural patterning, bioavailability, and applicability to alternative targets. In this review, we present a perspective on the development and characterization of several antimicrobial polymers and discuss novel applications of these molecules emerging in the field. This article is categorized under: Therapeutic Approaches and Drug Discovery > Emerging Technologies Therapeutic Approaches and Drug Discovery > Nanomedicine for Infectious Disease.
- Klíčová slova
- antimicrobial polymers, cancer, cyanobacteria, liposome, simulations,
- MeSH
- antibakteriální látky farmakologie terapeutické užití MeSH
- antiinfekční látky * farmakologie chemie terapeutické užití MeSH
- biomimetika MeSH
- kationické antimikrobiální peptidy * chemie farmakologie MeSH
- polymery chemie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- přehledy MeSH
- Názvy látek
- antibakteriální látky MeSH
- antiinfekční látky * MeSH
- kationické antimikrobiální peptidy * MeSH
- polymery MeSH
Acute diarrhoea is a common presentation in dogs, and a common reason for antimicrobial prescription and nutraceutical use. This evidence-based guideline provides recommendations for antimicrobial and probiotic treatment of canine acute diarrhoea (CAD). A multidisciplinary panel developed the recommendations by adhering to the Grading of Recommendations Assessment, Development and Evaluation (GRADE) framework. The opinions of stakeholders (general veterinary practitioners and dog owners) were collected and incorporated to ensure the applicability of this guideline. Four strong recommendations informed by high certainty evidence, and three conditional recommendations informed by very low or low certainty evidence, were drafted by the panel, along with an ungraded section on diagnostic work-up of dogs with acute diarrhoea. The ENOVAT guidelines initiative encourages national or regional guideline makers to use the evidence presented in this document, and the supporting systematic review, to draft national or local guidance documents.
- Klíčová slova
- Antibiotics, Antimicrobial stewardship, Enteritis, Evidence based, GRADE,
- MeSH
- akutní nemoc MeSH
- antibakteriální látky terapeutické užití MeSH
- antiinfekční látky terapeutické užití MeSH
- nemoci psů * farmakoterapie MeSH
- probiotika terapeutické užití MeSH
- průjem * veterinární farmakoterapie MeSH
- psi MeSH
- zvířata MeSH
- Check Tag
- psi MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- směrnice pro lékařskou praxi MeSH
- Geografické názvy
- Evropa MeSH
- Názvy látek
- antibakteriální látky MeSH
- antiinfekční látky MeSH
Amides of betulinic acid with cystamine were synthesized to investigate their antimicrobial and antitumor activity, and their influence on the cell cycle and cell apoptosis. The former target amide (6) displayed cytotoxicity in CEM cell line after 72 h of treatment (IC50 = 3.0 ± 0.7 μM; TI = 20), and induced apoptosis by caspase-3/7 activation in CEM cells. The latter target amide (9) displayed antimicrobial activity against Streptococcus mutans (MIC 3.125 μM; MBC 3.125 μM) and Bacillus cereus (MIC 25 μM; MBC 25 μM). The achieved results demonstrate enhancing of their biological activity over that of the parent compounds. However, two intermediate compounds (2 and 7) displayed either considerable cytotoxicity (2; 7.5 ± 0.8 μM; TI = 10, against G361) or antimicrobial activity (7; both against Actinomyces odontolycus and Clostridium perfrigens with MIC 12.5 µM and MBC 12.5 µM). The experimental data were compared with the in silico calculated physico-chemical and ADME parameters of the target compounds, including successful intermediates.
- Klíčová slova
- Antimicrobial activity, Apoptosis, Betulinic acid, Cystamine, Cytotoxicity,
- MeSH
- Actinomyces účinky léků MeSH
- amidy chemie farmakologie MeSH
- antibakteriální látky chemická syntéza chemie farmakologie MeSH
- apoptóza účinky léků MeSH
- Bacillus cereus účinky léků MeSH
- Clostridium účinky léků MeSH
- cystamin chemie farmakologie MeSH
- kultivované buňky MeSH
- kyselina betulinová MeSH
- lidé MeSH
- mikrobiální testy citlivosti MeSH
- molekulární konformace MeSH
- pentacyklické triterpeny MeSH
- proliferace buněk účinky léků MeSH
- protinádorové látky chemická syntéza chemie farmakologie MeSH
- screeningové testy protinádorových léčiv MeSH
- Streptococcus mutans účinky léků MeSH
- triterpeny chemie farmakologie MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- amidy MeSH
- antibakteriální látky MeSH
- cystamin MeSH
- kyselina betulinová MeSH
- pentacyklické triterpeny MeSH
- protinádorové látky MeSH
- triterpeny MeSH
Antimicrobial Peptides (AMPs) are one of the most common components of the innate immune system that protect multicellular organisms against microbial invasion. The vast majority of AMPs are isolated from the frog skin. Anuran (frogs and toads) skin contains abundant AMPs that can be developed therapeutically. Such peptides are a unique but diverse group of molecules. In general, more than 50% of the amino acid residues form the hydrophobic part of the molecule. Normally, there are no conserved structural motifs responsible for activity, although the vast majority of the AMPs are cationic due to the presence of multiple lysine residues; this cationicity has a close relationship with antibacterial activity. Notably, recent evidence suggests that synthesis of AMPs in frog skin may confer an advantage on a particular species, although they are not essential for survival. Frog skin AMPs exert potent activity against antibiotic-resistant bacteria, protozoa, yeasts, and fungi by permeating and destroying the plasma membrane and inactivating intracellular targets. Importantly, since they do not bind to a specific receptor, AMPs are less likely to induce resistance mechanisms. Currently, the best known amphibian AMPs are esculentins, brevinins, ranacyclins, ranatuerins, nigrocin-2, magainins, dermaseptins, bombinins, temporins, and japonicins-1 and -2, and palustrin-2. This review focuses on these frog skin AMPs and the mechanisms underlying their antimicrobial activity. We hope that this review will provide further information that will facilitate further study of AMPs and cast new light on novel and safer microbicides.
- Klíčová slova
- Antimicrobial peptides (AMPs), amphibian defense peptides, antibacterial, brevinins, esculentins, ranacyclins, ranatuerins.,
- MeSH
- antiinfekční látky chemie farmakologie MeSH
- Bacteria účinky léků MeSH
- Eukaryota účinky léků MeSH
- houby účinky léků MeSH
- kationické antimikrobiální peptidy chemie farmakologie MeSH
- kůže chemie MeSH
- lidé MeSH
- žáby MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
- Názvy látek
- antiinfekční látky MeSH
- kationické antimikrobiální peptidy MeSH
Plant antimicrobial peptides (AMPs) are a component of barrier defense system of plants. They have been isolated from roots, seeds, flowers, stems, and leaves of a wide variety of species and have activities towards phytopathogens, as well as against bacteria pathogenic to humans. Thus, plant AMPs are considered as promising antibiotic compounds with important biotechnological applications. Plant AMPs are grouped into several families and share general features such as positive charge, the presence of disulfide bonds (which stabilize the structure), and the mechanism of action targeting outer membrane structures.
- MeSH
- antibakteriální látky chemie farmakologie MeSH
- antifungální látky chemie farmakologie MeSH
- antiinfekční látky chemie klasifikace farmakologie MeSH
- biotechnologie MeSH
- fyziologie rostlin * MeSH
- kationické antimikrobiální peptidy chemie klasifikace farmakologie MeSH
- penetrační peptidy chemie farmakologie MeSH
- rostliny chemie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- přehledy MeSH
- Názvy látek
- antibakteriální látky MeSH
- antifungální látky MeSH
- antiinfekční látky MeSH
- kationické antimikrobiální peptidy MeSH
- penetrační peptidy MeSH
Recently, the interest is increasing to find alternatives to replace the usage of antibiotics since their massive and improper usage enhance the antibiotic resistance in human pathogens. In this study, for the first time we showed that the soil proteins have very high antibacterial activity (98% of growth inhibition) against methicillin resistant Staphylococcus aureus (MRSA), one of the most threatening human pathogens. We found that the protein extract (C3) from the forest with past intensive management showed higher antibacterial activity than that of unmanaged forest. The MIC and IC50 were found to be 30 and 15.0 μg protein g-1 dry soil respectively. C3 was found to kill the bacteria by cell wall disruption and genotoxicity which was confirmed by optical and fluorescent microscopy and comet assay. According to qPCR study, the mecA (the antibiotic resistant gene) expression in MRSA was found to be down-regulated after C3 treatment. In contrast, C3 showed no hemolytic toxicity on human red blood cells which was confirmed by hemolytic assay. According to ultra-high performance liquid chromatography-mass spectrometry (UHPLC-MS), 144 proteins were identified in C3 among which the majority belonged to Gram negative bacteria (45.8%). Altogether, our results will help to develop novel, cost-effective, non-toxic and highly efficient antibacterial medicines from natural sources against antibiotic resistant infections.
- Klíčová slova
- Antibacterial, Forest soil, MRSA, Natural products, Soil protein,
- MeSH
- antibakteriální látky farmakologie MeSH
- lidé MeSH
- methicilin rezistentní Staphylococcus aureus * MeSH
- methicilin MeSH
- mikrobiální testy citlivosti MeSH
- půda MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- antibakteriální látky MeSH
- methicilin MeSH
- půda MeSH
Biomechanical preparation alone does not completely eradicate microorganisms from the root canal, hence the next logical step is to perform root canal procedures in conjunction with antimicrobials. The use of an antimicrobial agent improves the efficacy and prognosis of endodontic treatment. This review enumerates the most widely used antimicrobial agents, their mechanism of action and their potential use in reducing the microbial load.
- MeSH
- antibiotická rezistence MeSH
- antiinfekční látky lokální terapeutické užití MeSH
- lidé MeSH
- terapie kořenového kanálku * MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- přehledy MeSH
- Názvy látek
- antiinfekční látky lokální MeSH
Over the last decades, multidrug-resistant bacteria have emerged and spread, increasing the number of bacteria, against which commonly used antibiotics are no longer effective. It has become a serious public health problem whose solution requires medical research in order to explore novel effective antimicrobial molecules. On the one hand, antimicrobial peptides (AMPs) are regarded as good alternatives because of their generally broad-spectrum activities, but sometimes they can be easily degraded by the organism or be toxic to animal cells. On the other hand, cationic carbosilane dendrons, whose focal point can be functionalized in many different ways, have also shown good antimicrobial activity. In this work, we synthetized first- and second-generation cationic carbosilane dendrons with a maleimide molecule on their focal point, enabling their functionalization with three different AMPs. After different microbiology studies, we found an additive effect between first-generation dendron and AMP3 whose study reveals three interesting effects: (i) bacteria aggregation due to AMP3, which could facilitate bacteria detection or even contribute to antibacterial activity by preventing host cell attack, (ii) bacteria disaggregation capability of second-generation cationic dendrons, and (iii) a higher AMP3 aggregation ability when dendrons were added previously to peptide treatment. These compounds and their different effects observed over bacteria constitute an interesting system for further mechanism studies.
- Klíčová slova
- antibacterial peptides, carbosilane dendrons, molecular modeling and molecular dynamics,
- MeSH
- antiinfekční látky chemie MeSH
- dendrimery chemie MeSH
- maleimidy chemie MeSH
- nanokonjugáty chemie MeSH
- silany chemie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- antiinfekční látky MeSH
- carbosilane MeSH Prohlížeč
- dendrimery MeSH
- maleimide MeSH Prohlížeč
- maleimidy MeSH
- nanokonjugáty MeSH
- silany MeSH
Antimicrobial decapeptide anoplin was tested for its antifungal activity against plant pathogen Leptosphaeria maculans and protection of Brassica napus plants from disease. To reveal the mode of action of the peptide, a natural form of anoplin amidated on C-terminus (ANP-NH2), and its carboxylated analog (ANP-OH) were used in the study. We demonstrated strong antifungal activity of anoplin in vitro regardless C-terminus modification. In addition we show that both ANP-NH2 and ANP-OH induce expression of defence genes in B. napus and protects plants from L. maculans infection. The results indicate that the amidation of anoplin is not essential for its antifungal and plant defence stimulating activities.
- Klíčová slova
- Anoplin, Antifungal, Antimicrobial peptide, Brassica napus, Leptosphaeria maculans,
- MeSH
- amidy chemie farmakologie MeSH
- antifungální látky chemie farmakologie MeSH
- Ascomycota účinky léků MeSH
- Brassica napus genetika mikrobiologie MeSH
- kationické antimikrobiální peptidy chemie farmakologie MeSH
- nemoci rostlin mikrobiologie prevence a kontrola MeSH
- regulace genové exprese u rostlin účinky léků MeSH
- vosí jedy chemie farmakologie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- amidy MeSH
- anoplin MeSH Prohlížeč
- antifungální látky MeSH
- kationické antimikrobiální peptidy MeSH
- vosí jedy MeSH
This article presents the results of the study of the antimicrobial and antifungal properties among 1,2,4-triazole derivatives synthesized at the Department of Physical and Colloidal Chemistry of the Zaporizhzhia State Medical University. Previous studies have established the antimicrobial and antifungal activity of 1,2,4-triazole derivatives. Therefore, it was reasonable to investigate highly effective substances with antimicrobial and antifungal properties among synthesized compounds. In the first stage of our research, acute toxicity prediction was performed. The antimicrobial and antifungal properties were carried out by the method of “serial dilutions” on a liquid nutrient. Forty-seven compounds of the different classes were studied for these types of activities. According to our research, derivatives of 3-amino-1,2,4-triazole showed better performance than 3-thio-1,2.4-triazoles for Staphylococcus aureus and Candida albicans. 5-(1Н-tetrazole-1-іl)methyl-4Н- -1,2,4-triazole-3-yl-1-(5-nitrofuran-2-yl)methanimin (11.6) was showed the greatest antimicrobial and antifungal activity. Deeper research for compound 11.6 was done by diffusion in agar (method of “wells”). Studies have shown that molecule 11.6 showed antimicrobial and antifungal action to the studied test strains at a concentration of 2 μg/ml. Hence, this compound can be developed as a helpful therapeutic agent after establishing its safety pharmacology and toxicity.
- Klíčová slova
- 1,2,4-triazole, antifungal activity, antimicrobial activity,
- MeSH
- agar MeSH
- amitrol MeSH
- antibakteriální látky farmakologie MeSH
- antifungální látky farmakologie MeSH
- antiinfekční látky * farmakologie MeSH
- lidé MeSH
- mikrobiální testy citlivosti MeSH
- nitrofurany * MeSH
- tetrazoly MeSH
- triazoly chemie farmakologie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- agar MeSH
- amitrol MeSH
- antibakteriální látky MeSH
- antifungální látky MeSH
- antiinfekční látky * MeSH
- nitrofurany * MeSH
- tetrazoly MeSH
- triazoly MeSH