Medicinal Au(i) compounds targeting urease as prospective antimicrobial agents: unveiling the structural basis for enzyme inhibition

2021 ◽  
Author(s):  
Luca Mazzei ◽  
Lara Massai ◽  
Michele Cianci ◽  
Luigi Messori ◽  
Stefano Ciurli
Keyword(s):  
Antibiotic Resistance ◽  
Enzyme Inhibition ◽  
Antimicrobial Agents ◽  
Antimicrobial Properties ◽  
New Drugs ◽  
Structural Basis ◽  
Great Promise ◽  
Gold Compounds

A few gold compounds were recently found to show antimicrobial properties in vitro, holding great promise for the discovery of new drugs to overcome antibiotic resistance.

New Macrolide Antibiotics: Usefulness in Infections Caused by Mycobacteria other Than Mycobacterium Tuberculosis

1994 ◽  
Vol 28 (11) ◽  
pp. 1255-1263 ◽  
Author(s):  
Robert P. Rapp ◽  
Scott A. McCraney ◽  
Norman L. Goodman ◽  
David J. Shaddick
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Antimicrobial Agents ◽  
New Drugs ◽  
Vitro Activity ◽  
Great Promise ◽  
Macrolide Antibiotics ◽  
Mycobacterium Fortuitum ◽  
In Vitro Activity ◽  
Mycobacterium Chelonae

OBJECTIVE: To compare the pharmacology, in vitro activity, and clinical use of the new macrolide antibiotics, azithromycin and clarithromycin, in the treatment of infections caused by mycobacteria other than Mycobacterium tuberculosis. DATA IDENTIFICATION: An English-language literature search using MEDLINE (1987–1994), Index Medicus (1987–1994), Program and abstracts of the 31st (1991) and 32nd (1992) Interscience Conference on Antimicrobial Agents and Chemotherapy, and bibliographic reviews of related textbooks, review articles, and professional society publications. STUDY SELECTION: 105 articles were selected. In vitro and in vivo reports on the pharmacokinetics, microbiology, pharmacology, and effectiveness of clarithromycin and azithromycin were assessed to compare their effectiveness and safety. Emphasis was placed on the use of these new drugs in treating infections caused by Mycobacterium avium complex, Mycobacterium chelonae, and Mycobacterium fortuitum infections. RESULTS: A review of the in vitro activity of the new macrolides revealed moderate to very good activity against many strains of mycobacteria other than M. tuberculosis. Early clinical trials show promising results in pulmonary infections, lymphadenitis, cutaneous infections, and disseminated infections. CONCLUSIONS: The new macrolides, azithromycin and clarithromycin, show great promise for treating infections caused by these acid-fast bacteria. Clarithromycin is recommended as a component of combination therapy for the treatment of M. avium complex infections in patients with AIDS. The development of resistance in patients, particularly when these agents are used alone, has been reported.

scholarly journals The Beneficial Mechanical and Biological Outcomes of Thin Copper-Gallium Doped Silica-Rich Bio-Active Glass Implant-Type Coatings

Coatings ◽  
2020 ◽  
Vol 10 (11) ◽  
pp. 1119 ◽  
Author(s):  
George E. Stan ◽  
Teddy Tite ◽  
Adrian-Claudiu Popa ◽  
Iuliana Maria Chirica ◽  
Catalin C. Negrila ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
High Performance ◽  
Antimicrobial Agents ◽  
Antimicrobial Properties ◽  
Great Promise ◽  
Functional Coatings ◽  
Water Contact ◽  
Antibacterial Performance ◽  
Co Doped

Silica-based bioactive glasses (SBG) hold great promise as bio-functional coatings of metallic endo-osseous implants, due to their osteoproductive potential, and, in the case of designed formulations, suitable mechanical properties and antibacterial efficacy. In the framework of this study, the FastOs®BG alkali-free SBG system (mol%: SiO2—38.49, CaO—36.07, P2O5—5.61, MgO—19.24, CaF2—0.59), with CuO (2 mol%) and Ga2O3 (3 mol%) antimicrobial agents, partially substituting in the parent system CaO and MgO, respectively, was used as source material for the fabrication of intentionally silica-enriched implant-type thin coatings (~600 nm) onto titanium (Ti) substrates by radio-frequency magnetron sputtering. The physico-chemical and mechanical characteristics, as well as the in vitro preliminary cytocompatibility and antibacterial performance of an alkali-free silica-rich bio-active glass coating designs was further explored. The films were smooth (RRMS < 1 nm) and hydrophilic (water contact angle of ~65°). The SBG coatings deposited from alkali-free copper-gallium co-doped FastOs®BG-derived exhibited improved wear performance, with the coatings eliciting a bonding strength value of ~53 MPa, Lc3 critical load value of ~4.9 N, hardness of ~6.1 GPa and an elastic modulus of ~127 GPa. The Cu and Ga co-doped SBG layers had excellent cytocompatibility, while reducing after 24 h the Staphylococcus aureus bacterial development with 4 orders of magnitude with respect to the control situations (i.e., nutritive broth and Ti substrate). Thereby, such SBG constructs could pave the road towards high-performance bio-functional coatings with excellent mechanical properties and enhanced biological features (e.g., by coupling cytocompatibility with antimicrobial properties), which are in great demand nowadays.

scholarly journals An In Vitro Study on the Antimicrobial Properties of Essential Oil Modified Resin Composite against Oral Pathogens

Materials ◽  
2020 ◽  
Vol 13 (19) ◽  
pp. 4383
Author(s):  
Barbara Lapinska ◽  
Aleksandra Szram ◽  
Beata Zarzycka ◽  
Janina Grzegorczyk ◽  
Louis Hardan ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Resin Composite ◽  
Antimicrobial Properties ◽  
In Vitro Study ◽  
Diffusion Method ◽  
Oral Pathogens

Modifying the composition of dental restorative materials with antimicrobial agents might induce their antibacterial potential against cariogenic bacteria, e.g., S.mutans and L.acidophilus, as well as antifungal effect on C.albicans that are major oral pathogens. Essential oils (EOs) are widely known for antimicrobial activity and are successfully used in dental industry. The study aimed at evaluating antibacterial and antifungal activity of EOs and composite resin material (CR) modified with EO against oral pathogens. Ten EOs (i.e., anise, cinnamon, citronella, clove, geranium, lavender, limette, mint, rosemary thyme) were tested using agar diffusion method. Cinnamon and thyme EOs showed significantly highest antibacterial activity against S.mutans and L.acidophilus among all tested EOs. Anise and limette EOs showed no antibacterial activity against S.mutans. All tested EOs exhibited antifungal activity against C.albicans, whereas cinnamon EO showed significantly highest and limette EO significantly lowest activity. Next, 1, 2 or 5 µL of cinnamon EO was introduced into 2 g of CR and microbiologically tested. The modified CR showed higher antimicrobial activity in comparison to unmodified one. CR containing 2 µL of EO showed the best antimicrobial properties against S.mutans and C.albicans, while CR modified with 1 µL of EO showed the best antimicrobial properties against L.acidophilus.

scholarly journals Synthesis and Antimicrobial Properties of Highly Cross-Linked pH-Sensitive Hydrogels through Gamma Radiation

Polymers ◽  
2021 ◽  
Vol 13 (14) ◽  
pp. 2223
Author(s):  
Moises Bustamante-Torres ◽  
Victor H. Pino-Ramos ◽  
David Romero-Fierro ◽  
Sandra P. Hidalgo-Bonilla ◽  
Héctor Magaña ◽  
...  
Keyword(s):  
Bacterial Infections ◽  
Antimicrobial Agents ◽  
Film Formation ◽  
Antimicrobial Properties ◽  
Ph Sensitive ◽  
Scanning Calorimetry ◽  
Polymeric Systems ◽  
E Coli ◽  
High Prevalence

The design of new polymeric systems for antimicrobial drug release focused on medical/surgical procedures is of great interest in the biomedical area due to the high prevalence of bacterial infections in patients with wounds or burns. For this reason, in this work, we present a new design of pH-sensitive hydrogels copolymerized by a graft polymerization method (gamma rays), intended for localized prophylactic release of ciprofloxacin and silver nanoparticles (AgNPs) for potential topical bacterial infections. The synthesized hydrogels were copolymerized from acrylic acid (AAc) and agar. Cross-linked hydrogel film formation depended on monomer concentrations and the degree of radiation used (Cobalt-60). The obtained hydrogel films were characterized by attenuated total reflectance Fourier-transform infrared spectroscopy (ATR-FTIR), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), and mechanical testing. The swelling of the hydrogels was evidenced by the influence of their pH-sensitiveness. The hydrogel was loaded with antimicrobial agents (AgNPs or ciprofloxacin), and their related activity was evaluated. Finally, the antimicrobial activity of biocidal-loaded hydrogel was tested against Escherichia coli (E. coli) and methicillin-resistant Staphylococcus aureus (MRSA) on in vitro conditions.

scholarly journals Nanostructures and their application in antimicrobial drug delivery system

2017 ◽  
Vol 4 (1-4) ◽  
pp. 81-90
Keyword(s):  
Carbon Nanotubes ◽  
Noble Metals ◽  
Antimicrobial Properties ◽  
High Reactivity ◽  
Great Promise ◽  
Antimicrobial Drugs ◽  
Microbial Inhibition ◽  
Carbon Based Nanomaterials ◽  
Walled Carbon Nanotubes

As multiresistant and pan-resistant infections continue to emerge, and because the development of novel antimicrobial drugs is a slow process, nanotechnology offers valuable alternatives for fighting resistant bugs, mainly by improving the therapeutic effect of current antimicrobials. Antibiotic resistance is one of the greatest global health threats of the 21st century, but nanotechnology is offering new solutions to the problem. Nanostructured biomaterials, nanoparticles in particular, have unique physicochemical properties such as ultra small and controllable size, large surface area to mass ratio, high reactivity, and functionalizable structure. These properties can be applied to facilitate the administration of antimicrobial drugs, thereby overcoming some of the limitations in traditional antimicrobial therapeutics. Carbon-based nanomaterials such as fullerenes, carbon nanotubes (CNTs) (especially single-walled carbon nanotubes (SWCNTs)) and graphene oxide (GO) nanoparticles) show potent antimicrobial properties. Nanocoating and shuttle systems have shown great promise in vitro and animal models. Noble metals nanostructures, particularly silver, have attracted much attention in the fields of medicine due to their unique properties which are strongly dependent on the size and shape of metal nanomaterials. Recent development of nanocarriers, improved the drug therapy of different diseases, together with the mechanisms of microbial inhibition.

scholarly journals ABC-F Proteins Mediate Antibiotic Resistance through Ribosomal Protection

mBio ◽  
2016 ◽  
Vol 7 (2) ◽  
Author(s):  
Liam K. R. Sharkey ◽  
Thomas A. Edwards ◽  
Alex J. O’Neill
Keyword(s):  
Antibiotic Resistance ◽  
Direct Evidence ◽  
New Drugs ◽  
Bacterial Ribosome ◽  
Broad Array ◽  
Clinically Significant ◽  
Antibiotic Efflux ◽  
Dose Dependent ◽  
Ribosomal Protection

ABSTRACTMembers of the ABC-F subfamily of ATP-binding cassette proteins mediate resistance to a broad array of clinically important antibiotic classes that target the ribosome of Gram-positive pathogens. The mechanism by which these proteins act has been a subject of long-standing controversy, with two competing hypotheses each having gained considerable support: antibiotic efflux versus ribosomal protection. Here, we report on studies employing a combination of bacteriological and biochemical techniques to unravel the mechanism of resistance of these proteins, and provide several lines of evidence that together offer clear support to the ribosomal protection hypothesis. Of particular note, we show that addition of purified ABC-F proteins to anin vitrotranslation assay prompts dose-dependent rescue of translation, and demonstrate that such proteins are capable of displacing antibiotic from the ribosomein vitro. To our knowledge, these experiments constitute the first direct evidence that ABC-F proteins mediate antibiotic resistance through ribosomal protection.IMPORTANCEAntimicrobial resistance ranks among the greatest threats currently facing human health. Elucidation of the mechanisms by which microorganisms resist the effect of antibiotics is central to understanding the biology of this phenomenon and has the potential to inform the development of new drugs capable of blocking or circumventing resistance. Members of the ABC-F family, which includelsa(A),msr(A),optr(A), andvga(A), collectively yield resistance to a broader range of clinically significant antibiotic classes than any other family of resistance determinants, although their mechanism of action has been controversial since their discovery 25 years ago. Here we present the first direct evidence that proteins of the ABC-F family act to protect the bacterial ribosome from antibiotic-mediated inhibition.

Synthesis, in silico pharmacokinetics and biological evaluation of some new thiazolidinedione as PPAR-γ agonists and antibacterial agents

2021 ◽  
Vol 18 ◽  
Author(s):  
Zohor Mohammad Mahdi Alzhrani ◽  
Mohammad Mahboob Alam ◽  
Syed Nazreen
Keyword(s):  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Antibacterial Activities ◽  
Biological Evaluation ◽  
New Drugs ◽  
Diabetic Patients ◽  
Spectroscopic Techniques ◽  
Standard Drug ◽  
Ppar Γ

Background: The frequent uses of antimicrobial agents to treat infections in diabetic patients make them more drug resistance than non diabetic patients which accounts for higher mortality rate of diabetic patients. Therefore, it is a necessity today to synthesize new drugs with dual mode of action as antidiabetic and antibacterial agents. In the present work, new derivatives containing thiazolidinedione and 1,3,4-oxadiaozle have been synthesized and screened for PPAR-γ and antibacterial activities. Methods: Compound 5-12 have been synthesized from 2-methoxy benzaldehyde and thiazolidinedione and characterized using different spectroscopic techniques such as IR, NMR and mass spectrometry. These compounds were tested for in vitro PPAR-γ transactivation, PPAR-γ gene expression and antibacterial activities. Finally molecular docking was carried out to see the binding interactions of molecules with the target protein. Results: All the compounds follow Lipinski rule suggesting the synthesized derivatives have good drug likeness properties. Compound 11 and 12 exhibited promising PPAR-γ transactivation with 73.69% and 76.50%, respectively as well as showed significant antibacterial activity with comparable MIC of 3.12 μg/disc to standard drug amoxicillin. The docking result was found to be in consistent with the in vitro PPAR-γ transactivation results. Conclusion: Compounds 11 and 12 can be further investigated as lead molecules for the development of new and effective antidiabetic and antibacterial agents.

scholarly journals Facile Synthesis of Antimicrobial Aloe Vera-“Smart” Triiodide-PVP Biomaterials

Biomimetics ◽  
2020 ◽  
Vol 5 (3) ◽  
pp. 45 ◽  
Author(s):  
Zehra Edis ◽  
Samir Haj Bloukh
Keyword(s):  
Antimicrobial Agents ◽  
Microstructural Analysis ◽  
Aloe Vera ◽  
Antimicrobial Properties ◽  
Surgical Site Infections ◽  
Halogen Bonding ◽  
Polyglycolic Acid ◽  
Antimicrobial Activities ◽  
One Pot

Antibiotic resistance is an eminent threat for the survival of mankind. Nosocomial infections caused by multidrug resistant microorganisms are a reason for morbidity and mortality worldwide. Plant-based antimicrobial agents are based on synergistic mechanisms which prevent resistance and have been used for centuries against ailments. We suggest the use of cost-effective, eco-friendly Aloe Vera Barbadensis Miller (AV)-iodine biomaterials as a new generation of antimicrobial agents. In a facile, one-pot synthesis, we encapsulated fresh AV gel with polyvinylpyrrolidone (PVP) as a stabilizing agent and incorporated iodine moieties in the form of iodine (I2) and sodium iodide (NaI) into the polymer matrix. Ultraviolet-visible spectroscopy (UV-Vis), Fourier transform infrared spectroscopy (FT-IR), x-ray diffraction (XRD), microstructural analysis by scanning electron microscopy (SEM) and energy dispersive spectroscopy (EDS) verified the composition of AV-PVP-I2, AV-PVP-I2-NaI. AV, AV-PVP, AV-PVP-I2, AV-PVP-I2-NaI, and AV-PVP-NaI were tested in-vitro by disc diffusion assay and dip-coated on polyglycolic acid (PGA) sutures against ten microbial reference strains. All the tested pathogens were more susceptible towards AV-PVP-I2 due to the inclusion of “smart” triiodides with halogen bonding in vitro and on dip-coated sutures. The biocomplexes AV-PVP-I2, AV-PVP-I2-NaI showed remarkable antimicrobial properties. “Smart” biohybrids with triiodide inclusions have excellent antifungal and promising antimicrobial activities, with potential use against surgical site infections (SSI) and as disinfecting agents.

scholarly journals Plant Products as Antimicrobial Agents

1999 ◽  
Vol 12 (4) ◽  
pp. 564-582 ◽  
Author(s):  
Marjorie Murphy Cowan
Keyword(s):  
Secondary Metabolites ◽  
Antimicrobial Agents ◽  
Antimicrobial Properties ◽  
Traditional Healers ◽  
In Vivo Studies ◽  
Current Status ◽  
The Public ◽  
The Earth

SUMMARY The use of and search for drugs and dietary supplements derived from plants have accelerated in recent years. Ethnopharmacologists, botanists, microbiologists, and natural-products chemists are combing the Earth for phytochemicals and “leads” which could be developed for treatment of infectious diseases. While 25 to 50% of current pharmaceuticals are derived from plants, none are used as antimicrobials. Traditional healers have long used plants to prevent or cure infectious conditions; Western medicine is trying to duplicate their successes. Plants are rich in a wide variety of secondary metabolites, such as tannins, terpenoids, alkaloids, and flavonoids, which have been found in vitro to have antimicrobial properties. This review attempts to summarize the current status of botanical screening efforts, as well as in vivo studies of their effectiveness and toxicity. The structure and antimicrobial properties of phytochemicals are also addressed. Since many of these compounds are currently available as unregulated botanical preparations and their use by the public is increasing rapidly, clinicians need to consider the consequences of patients self-medicating with these preparations.

The Activity of Alkanna Species in vitro Culture and Intact Plant Extracts Against Antibiotic Resistant Bacteria

2019 ◽  
Vol 25 (16) ◽  
pp. 1861-1865 ◽  
Author(s):  
Naira Sahakyan ◽  
Margarit Petrosyan ◽  
Armen Trchounian
Keyword(s):  
Antibiotic Resistance ◽  
Antibacterial Agents ◽  
Bacterial Resistance ◽  
Antimicrobial Agents ◽  
Resistant Bacteria ◽  
Plant Origin ◽  
Bacterial Strains ◽  
Biotechnological Production ◽  
Antibiotic Resistant

Overcoming the antibiotic resistance is nowadays a challenge. There is still no clear strategy to combat this problem. Therefore, the urgent need to find new sources of antibacterial agents exists. According to some literature, substances of plant origin are able to overcome bacterial resistance against antibiotics. Alkanna species plants are among the valuable producers of these metabolites. But there is a problem of obtaining the standardized product. So, this review is focused on the discussion of the possibilities of biotechnological production of antimicrobial agents from Alkanna genus species against some microorganisms including antibiotic resistant bacterial strains.

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