scholarly journals Bactericidal Activity of Non-Cytotoxic Cationic Nanoparticles against Clinically and Environmentally Relevant Pseudomonas spp. Isolates

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1411
Author(s):  
Anna Maria Schito ◽  
Gabriella Piatti ◽  
Debora Caviglia ◽  
Guendalina Zuccari ◽  
Alessia Zorzoli ◽  
...  
Keyword(s):  
Bactericidal Activity ◽  
Bacterial Infections ◽  
Plant Pathogens ◽  
Human Keratinocytes ◽  
Water Soluble ◽  
Meat Spoilage ◽  
Viable Cells ◽  
Wide Range ◽  
Low Cytotoxicity ◽  
Time Kill

Difficult-to-treat bacterial infections caused by resistant human and plant pathogens severely afflict hospitals, and concern the agri-food sectors. Bacteria from the Pseudomonadaceae family, such as P. aeruginosa, P. putida, P. fluorescens, and P. straminea, can be responsible for severe nosocomial infections in humans. P. fragi is the major cause of dairy and meat spoilage, while P. syringae can infect a wide range of economically important plant species, including tobacco, kiwi, and tomato. Therefore, a cationic water-soluble lysine dendrimer (G5-PDK) was tested on several species of Pseudomonas genus. Interestingly, G5-PDK demonstrated variable minimum inhibitory concentrations (MICs), depending on their pigment production, on Pseudomonas aeruginosa (1.6-> 6.4 µM), MICs = 3.2–6.4 µM on P. putida clinical isolates producing pyoverdine, and very low MICs (0.2–1.6 µM) on strains that produced non-pigmented colonies. Time-kill experiments established the rapid bactericidal activity of G5-PDK. In the cytotoxicity experiments on human keratinocytes, after 4 h of treatment with G5-PDK at concentrations 16–500 × MIC, more than 80% of viable cells were observed, and after 24 h, the selectivity indices were maintained above the maximum value reported as acceptable. Due to its proven bactericidal potency and low cytotoxicity, G5-PDK should be seriously considered to counteract clinically and environmentally relevant Pseudomonas isolates.

scholarly journals Green Preparation of Fluorescent Carbon Quantum Dots from Cyanobacteria for Biological Imaging

Polymers ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 616 ◽  
Author(s):  
Xi Wang ◽  
Pei Yang ◽  
Qian Feng ◽  
Taotao Meng ◽  
Jing Wei ◽  
...  
Keyword(s):  
Quantum Dots ◽  
Carbon Source ◽  
Large Scale ◽  
Low Cost ◽  
Average Diameter ◽  
Carbon Quantum Dots ◽  
Water Soluble ◽  
High Concentration ◽  
Wide Range ◽  
Low Cytotoxicity

Biomass-based carbon quantum dots (CQDs) have become a significant carbon materials by their virtues of being cost-effective, easy to fabricate and low in environmental impact. However, there are few reports regarding using cyanobacteria as a carbon source for the synthesis of fluorescent CQDs. In this study, the low-cost biomass of cyanobacteria was used as the sole carbon source to synthesize water-soluble CQDs by a simple hydrothermal method. The synthesized CQDs were mono-dispersed with an average diameter of 2.48 nm and exhibited excitation-dependent emission performance with a quantum yield of 9.24%. Furthermore, the cyanobacteria-derived CQDs had almost no photobleaching under long-time UV irradiation, and exhibited high photostability in the solutions with a wide range of pH and salinity. Since no chemical reagent was involved in the synthesis of CQDs, the as-prepared CQDs were confirmed to have low cytotoxicity for PC12 cells even at a high concentration. Additionally, the CQDs could be efficiently taken up by cells to illuminate the whole cell and create a clear distinction between cytoplasm and nucleus. The combined advantages of green synthesis, cost-effectiveness and low cytotoxicity make synthesized CQDs a significant carbon source and broaden the application of cyanobacteria and provide an economical route to fabricate CQDs on a large scale.

scholarly journals Combinatorial Pharmacodynamics of Ceftolozane-Tazobactam against Genotypically Defined β-Lactamase-Producing Escherichia coli: Insights into the Pharmacokinetics/Pharmacodynamics of β-Lactam–β-Lactamase Inhibitor Combinations

2016 ◽  
Vol 60 (4) ◽  
pp. 1967-1973 ◽  
Author(s):  
Rachel L. Soon ◽  
Justin R. Lenhard ◽  
Zackery P. Bulman ◽  
Patricia N. Holden ◽  
Pamela Kelchlin ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Bactericidal Activity ◽  
Fold Increase ◽  
Multidrug Resistant ◽  
Content Type ◽  
Log Reduction ◽  
Wide Range ◽  
Tract Infections ◽  
Time Kill ◽  
The Hill

ABSTRACTDespite a dearth of new agents currently being developed to combat multidrug-resistant Gram-negative pathogens, the combination of ceftolozane and tazobactam was recently approved by the Food and Drug Administration to treat complicated intra-abdominal and urinary tract infections. To characterize the activity of the combination product, time-kill studies were conducted against 4 strains ofEscherichia colithat differed in the type of β-lactamase they expressed. The four investigational strains included 2805 (no β-lactamase), 2890 (AmpC β-lactamase), 2842 (CMY-10 β-lactamase), and 2807 (CTX-M-15 β-lactamase), with MICs to ceftolozane of 0.25, 4, 8, and >128 mg/liter with no tazobactam, and MICs of 0.25, 1, 4, and 8 mg/liter with 4 mg/liter tazobactam, respectively. All four strains were exposed to a 6 by 5 array of ceftolozane (0, 1, 4, 16, 64, and 256 mg/liter) and tazobactam (0, 1, 4, 16, and 64 mg/liter) over 48 h using starting inocula of 106and 108CFU/ml. While ceftolozane-tazobactam achieved bactericidal activity against all 4 strains, the concentrations of ceftolozane and tazobactam required for a ≥3-log reduction varied between the two starting inocula and the 4 strains. At both inocula, the Hill plots (R2> 0.882) of ceftolozane revealed significantly higher 50% effective concentrations (EC50s) at tazobactam concentrations of ≤4 mg/liter than those at concentrations of ≥16 mg/liter (P< 0.01). Moreover, the EC50s at 108CFU/ml were 2.81 to 66.5 times greater than the EC50s at 106CFU/ml (median, 10.7-fold increase;P= 0.002). These promising results indicate that ceftolozane-tazobactam achieves bactericidal activity against a wide range of β-lactamase-producingE. colistrains.

scholarly journals Efficacy of Ursolic Acid-Enriched Water-Soluble and Not Cytotoxic Nanoparticles against Enterococci

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1976
Author(s):  
Anna Maria Schito ◽  
Debora Caviglia ◽  
Gabriella Piatti ◽  
Alessia Zorzoli ◽  
Danilo Marimpietri ◽  
...  
Keyword(s):  
Ursolic Acid ◽  
Therapeutic Option ◽  
Human Keratinocytes ◽  
Biological Properties ◽  
Water Soluble ◽  
Pentacyclic Triterpenoid ◽  
Different Strains ◽  
Time Kill

Ursolic acid (UA), a pentacyclic triterpenoid acid found in many medicinal plants and aromas, is known for its antibacterial effects against multi-drug-resistant (MDR) Gram-positive bacteria, which seriously threaten human health. Unfortunately, UA water-insolubility, low bioavailability, and systemic toxicity limit the possibilities of its application in vivo. Consequently, the beneficial activities of UA observed in vitro lose their potential clinical relevance unless water-soluble, not cytotoxic UA formulations are developed. With a nano-technologic approach, we have recently prepared water-soluble UA-loaded dendrimer nanoparticles (UA-G4K NPs) non-cytotoxic on HeLa cells, with promising physicochemical properties for their clinical applications. In this work, with the aim of developing a new antibacterial agent based on UA, UA-G4K has been tested on different strains of the Enterococcus genus, including marine isolates, toward which UA-G4K has shown minimum inhibitory concentrations (MICs) very low (0.5–4.3 µM), regardless of their resistance to antibiotics. Time-kill experiments, in addition to confirming the previously reported bactericidal activity of UA against E. faecium, also established it for UA-G4K. Furthermore, cytotoxicity experiments on human keratinocytes revealed that nanomanipulation of UA significantly reduced the cytotoxicity of UA, providing UA-G4K NPs with very high LD50 (96.4 µM) and selectivity indices, which were in the range 22.4–192.8, depending on the enterococcal strain tested. Due to its physicochemical and biological properties, UA-G4K could be seriously evaluated as a novel oral-administrable therapeutic option for tackling difficult-to-treat enterococcal infections.

scholarly journals Mode of action of Elasnin as biofilm-formation eradicator of Methicillin-Resistant Staphylococcus aureus

2021 ◽  
Author(s):  
Lexin Long ◽  
Jordy Evan Sulaiman ◽  
Yao Xiao ◽  
Aifang Cheng ◽  
Ruojun WANG ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Biofilm Formation ◽  
Bacterial Infections ◽  
Penicillin G ◽  
Dependent Manner ◽  
Resistance Development ◽  
Methicillin Resistant ◽  
Wide Range ◽  
Increased Sensitivity ◽  
Low Cytotoxicity

Abstract Biofilm is made by microbes and often offers protection by making them more tolerant, resistant, and resilient to wide-range antimicrobials. Biofilm-related infections account for more than 80% of human bacterial infections and are especially prevalent in chronic tissue and device-related infections. Owing to the great challenge in treating biofilms, novel and effective antibiofilm compounds urgently need to be identified. We herein identified elasnin as a potent biofilm-targeting compound against methicillin-resistant Staphylococcus aureus (MRSA) through bioassay-guided isolation of bioactive compounds from Actinobacteria. Elasnin effectively inhibited biofilm formation and eradicated pre-formed biofilms of MRSA, and it displays low cytotoxicity with a low risk of resistance development. Transcriptomic and proteomic analyses combined with confocal microscopy observation revealed that elasnin destroyed the biofilm matrix in a time-dependent manner and interfered with cell cycle during the exponential phase, primarily by repressing the expression of virulence factors. Moreover, the biofilm cells released from elasnin treatment showed increased sensitivity to penicillin G. Overall, this study identified elasnin as a promising biofilm-eradicating compound against MRSA and shed light on its action mechanism.

scholarly journals Mycofumigation through production of the volatile DNA-methylating agent N-methyl-N-nitrosoisobutyramide by fungi in the genus Muscodor

2017 ◽  
Vol 292 (18) ◽  
pp. 7358-7371 ◽  
Author(s):  
Michelle L. Hutchings ◽  
Cambria J. Alpha-Cobb ◽  
David A. Hiller ◽  
Julien Berro ◽  
Scott A. Strobel
Keyword(s):  
Dna Methylation ◽  
Building Materials ◽  
Plant Pathogens ◽  
Water Soluble ◽  
Dominant Factor ◽  
Heterogeneous Environments ◽  
Antagonistic Microorganisms ◽  
Wide Range ◽  
Chemical Strategies

Antagonistic microorganisms produce antimicrobials to inhibit the growth of competitors. Although water-soluble antimicrobials are limited to proximal interactions via aqueous diffusion, volatile antimicrobials are able to act at a distance and diffuse through heterogeneous environments. Here, we identify the mechanism of action of Muscodor albus, an endophytic fungus known for its volatile antimicrobial activity toward a wide range of human and plant pathogens and its potential use in mycofumigation. Proposed uses of the Muscodor species include protecting crops, produce, and building materials from undesired fungal or bacterial growth. By analyzing a collection of Muscodor isolates with varying toxicity, we demonstrate that the volatile mycotoxin, N-methyl-N-nitrosoisobutyramide, is the dominant factor in Muscodor toxicity and acts primarily through DNA methylation. Additionally, Muscodor isolates exhibit higher resistance to DNA methylation compared with other fungi. This work contributes to the evaluation of Muscodor isolates as potential mycofumigants, provides insight into chemical strategies that organisms use to manipulate their environment, and provokes questions regarding the mechanisms of resistance used to tolerate constitutive, long-term exposure to DNA methylation.

scholarly journals In Vitro and In Vivo Activities of Novel 2-(Thiazol-2-ylthio)-1β-Methylcarbapenems with Potent Activities against Multiresistant Gram-Positive Bacteria

2003 ◽  
Vol 47 (8) ◽  
pp. 2471-2480 ◽  
Author(s):  
Yutaka Ueda ◽  
Makoto Sunagawa
Keyword(s):  
Bactericidal Activity ◽  
Bacterial Infections ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Log Reduction ◽  
Highly Active ◽  
Time Kill

ABSTRACT SM-197436, SM-232721, and SM-232724 are new 1β-methylcarbapenems with a unique 4-substituted thiazol-2-ylthio moiety at the C-2 side chain. In agar dilution susceptibility testing these novel carbapenems were active against methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE) with a MIC90 of ≤4 μg/ml. Furthermore, SM-232724 showed strong bactericidal activity against MRSA, in contrast to linezolid, which was bacteriostatic up to four times the MIC. SM-232724 showed good therapeutic efficacy comparable to those of vancomycin and linezolid against systemic infections of MRSA in cyclophosphamide-treated mice. The MICs of SM-197436, SM-232721, and SM-232724 for streptococci, including penicillin-intermediate and penicillin-resistant Streptococcus pneumoniae strains, ranged from ≤0.063 to 0.5 μg/ml. These drugs were the most active β-lactams tested against Enterococcus faecium, and the MIC90 s for ampicillin-resistant E. faecium ranged between 8 and 16 μg/ml, which were slightly higher than the value for linezolid. However, time-kill assays revealed the superior bactericidal activity of SM-232724 compared to those of quinupristin-dalfopristin and linezolid against an E. faecium strain with a 4-log reduction in CFU at four times the MIC after 24 h of exposure to antibiotics. In addition, SM-232724 significantly reduced the numbers of bacteria in a murine abscess model with the E. faecium strain: its efficacy was superior to that of linezolid, although the MICs (2 μg/ml) of these two agents are the same. Among gram-negative bacteria, these three carbapenems were highly active against Haemophilus influenzae (including ampicillin-resistant strains), Moraxella catarrhalis, and Bacteroides fragilis, and showed antibacterial activity equivalent to that of imipenem for Escherichia coli, Klebsiella pneumoniae, and Proteus spp. Thus, these new carbapenems are promising candidates for agents to treat nosocomial bacterial infections by gram-positive and gram-negative bacteria, especially multiresistant gram-positive cocci, including MRSA and vancomycin-resistant enterococci.

Microsponges: An Overview

2017 ◽  
Vol 4 (4) ◽  
Author(s):  
Hamid Hussain ◽  
Divya Juyal ◽  
Archana Dhyani
Keyword(s):  
Controlled Release ◽  
Delivery System ◽  
Oral Delivery ◽  
Active Agent ◽  
Topical Delivery ◽  
Water Soluble ◽  
Wide Range ◽  
Porous Beads

Microsponge and Nanosponge delivery System was originally developed for topical delivery of drugs can also be used for controlled oral delivery of drugs using water soluble and bioerodible polymers. Microsponge delivery system (MDS) can entrap wide range of drugs and then release them onto the skin over a time by difussion mechanism to the skin. It is a unique technology for the controlled release of topical agents and consists of nano or micro porous beads loaded with active agent and also use for oral delivery of drugs using bioerodible polymers.

The content of decenoic acids in drone brood preparations and combined preparations based on it

Biomics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 389-393
Author(s):  
D.V. Mitrofanov ◽  
N.V. Budnikova
Keyword(s):  
Royal Jelly ◽  
Storage Conditions ◽  
Water Soluble ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Strict Adherence ◽  
Drone Brood ◽  
Wide Range ◽  
Active Substances ◽  
Melanin Complex

The drone brood contains a large number of substances with antioxidant activity. These substances require stabilization and strict adherence to storage conditions. Among these substances are unique decenoic acids, the content of which is an indicator of the quality of drone brood and products based on it. The ability of drone brood to reduce the manifestations of oxidative stress is shown. There are dietary supplements for food and drugs based on drone brood, which are used for a wide range of diseases. Together with drone brood, chitosan-containing products, propolis, royal jelly can be used. They enrich the composition with their own biologically active substances and affect the preservation of the biologically active substances of the drone brood. Promising are the products containing, in addition to the drone brood, a chitin-chitosan-melanin complex from bees, propolis, royal jelly. The chitin-chitosan-melanin complex in the amount of 5% in the composition of the adsorbent practically does not affect the preservation of decenic acids, while in the amount of 2% and 10% it somewhat worsens. The acid-soluble and water-soluble chitosan of marine crustaceans significantly worsens the preservation of decenoic acids in the product. Drone brood with royal jelly demonstrates a rather high content of decenoic acids. When propolis is introduced into the composition of the product, the content of decenoic acids increases according to the content of propolis.

Heterocycle Compounds with Antimicrobial Activity

2020 ◽  
Vol 26 (8) ◽  
pp. 867-904 ◽  
Author(s):  
Maria Fesatidou ◽  
Anthi Petrou ◽  
Geronikaki Athina
Keyword(s):  
Heterocyclic Compounds ◽  
Bacterial Infections ◽  
Scientific Community ◽  
Antimicrobial Agents ◽  
Fungal Infections ◽  
Biological Activities ◽  
Literature Survey ◽  
New Findings ◽  
Wide Range ◽  
Number Of Microorganisms

Background: Bacterial infections are a growing problem worldwide causing morbidity and mortality mainly in developing countries. Moreover, the increased number of microorganisms, developing multiple resistances to known drugs, due to abuse of antibiotics, is another serious problem. This problem becomes more serious for immunocompromised patients and those who are often disposed to opportunistic fungal infections. Objective: The objective of this manuscript is to give an overview of new findings in the field of antimicrobial agents among five-membered heterocyclic compounds. These heterocyclic compounds especially five-membered attracted the interest of the scientific community not only for their occurrence in nature but also due to their wide range of biological activities. Method: To reach our goal, a literature survey that covers the last decade was performed. Results: As a result, recent data on the biological activity of thiazole, thiazolidinone, benzothiazole and thiadiazole derivatives are mentioned. Conclusion: It should be mentioned that despite the progress in the development of new antimicrobial agents, there is still room for new findings. Thus, research still continues.

Studies on the EC50 of Natural Monoterpenes as Fungal Inhibitors with Quantitative Structure-Activity Relationships (QSARs)

2020 ◽  
Vol 10 (1) ◽  
pp. 44-60
Author(s):  
Mohamed E.I. Badawy ◽  
Entsar I. Rabea ◽  
Samir A.M. Abdelgaleil
Keyword(s):  
Biological Activity ◽  
Plant Pathogens ◽  
Molecular Descriptors ◽  
Microbial Pathogens ◽  
Quantitative Structure ◽  
Qsar Study ◽  
Qsar Analysis ◽  
Pharmacophore Modelling ◽  
Structure Activity ◽  
Wide Range

Background:Monoterpenes are the main constituents of the essential oils obtained from plants. These natural products offered wide spectra of biological activity and extensively tested against microbial pathogens and other agricultural pests.Methods:Antifungal activity of 10 monoterpenes, including two hydrocarbons (camphene and (S)- limonene) and eight oxygenated hydrocarbons ((R)-camphor, (R)-carvone, (S)-fenchone, geraniol, (R)-linalool, (+)-menthol, menthone, and thymol), was determined against fungi of Alternaria alternata, Botrytis cinerea, Botryodiplodia theobromae, Fusarium graminearum, Phoma exigua, Phytophthora infestans, and Sclerotinia sclerotiorum by the mycelia radial growth technique. Subsequently, Quantitative Structure-Activity Relationship (QSAR) analysis using different molecular descriptors with multiple regression analysis based on systematic search and LOOCV technique was performed. Moreover, pharmacophore modelling was carried out using LigandScout software to evaluate the common features essential for the activity and the hypothetical geometries adopted by these ligands in their most active forms.Results:The results showed that the antifungal activities were high, but depended on the chemical structure and the type of microorganism. Thymol showed the highest effect against all fungi tested with respective EC50 in the range of 10-86 mg/L. The QSAR study proved that the molecular descriptors HBA, MR, Pz, tPSA, and Vp were correlated positively with the biological activity in all of the best models with a correlation coefficient (r) ≥ 0.98 and cross-validated values (Q2) ≥ 0.77.Conclusion:The results of this work offer the opportunity to choose monoterpenes with preferential antimicrobial activity against a wide range of plant pathogens.

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