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1.
Int J Biol Macromol ; : 135896, 2024 Oct 05.
Article in English | MEDLINE | ID: mdl-39374716

ABSTRACT

Hydrogel wound dressings provide a moist environment, which promotes the formation of granulation tissue and epithelium in the wound area, accelerating the wound healing process. There have been numerous approaches to skin wound management and treatment, but the limitations of current methods highlight the need for more effective alternatives. A Chitosan polyherbal hydrogel integrated with AgNPs was synthesized to assess its wound-healing potential both in vitro and in vivo. The AgNPs were synthesized using Calotropis procera leaf extract and characterized via X-ray diffraction analysis (XRD), Scanning electron microscopy (SEM), and Fourier Transform Infrared Spectroscopy (FT-IR). In swelling kinetic analysis, the hydrogel's weight reached its maximum at 8 h of incubation and began to decrease from 12 h up to 72 h (49 % ±â€¯6.04). The hydrogel formulation demonstrated strong antimicrobial potential against E. coli and S. aureus with an inhibition zone of 18 mm and 25 mm, respectively. Furthermore, in mice studies, the formulation exhibited significant wound size reduction within 12 days, supported by histopathology analysis revealing higher angiogenic potential compared to commercial hydrogels. The concentrations of IL-6 and TNF-α in CS-polyherbal/AgNPs hydrogel were 500 pg/ml and 125 pg/ml, respectively. Additionally, a network pharmacology approach identified 11 chemical constituents in Aloe vera, Azadirachta indica, and Alternanthera brasiliana extracts, along with 326 potential targets, suggesting the superior wound healing properties of this formulation compared to commercially available hydrogels.

2.
Carbohydr Polym ; 345: 122577, 2024 Dec 01.
Article in English | MEDLINE | ID: mdl-39227109

ABSTRACT

This study was to investigate the antibacterial effects and metabolites derived from bifidobacterial fermentation of an exopolysaccharide EPS-LM produced by a medicinal fungus Cordyceps sinensis, Cs-HK1. EPS-LM was a partially purified polysaccharide fraction which was mainly composed of Man, Glc and Gal at 7.31:12.95:1.00 mol ratio with a maximum molecular weight of 360 kDa. After fermentation of EPS-LM in two bifidobacterial cultures, B. breve and B. longum, the culture digesta showed significant antibacterial activities, inhibiting the proliferation and biofilm formation of Escherichia coli. Based on untargeted metabolomic profiling of the digesta, the levels of short chain fatty acids, carboxylic acids, benzenoids and their derivatives were all increased significantly (p < 0.01), which probably contributed to the enhanced antibacterial activity by EPS-LM. Since EPS-LM was only slightly consumed for the bifidobacterial growth, it mainly stimulated the biosynthesis of bioactive metabolites in the bifidobacterial cells. The results also suggested that EPS-LM polysaccharide may have a regulatory function on the bifidobacterial metabolism leading to production of antibacterial metabolites, which may be of significance for further exploration.


Subject(s)
Anti-Bacterial Agents , Cordyceps , Escherichia coli , Fermentation , Polysaccharides, Bacterial , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Cordyceps/metabolism , Cordyceps/chemistry , Escherichia coli/drug effects , Escherichia coli/metabolism , Polysaccharides, Bacterial/pharmacology , Polysaccharides, Bacterial/chemistry , Polysaccharides, Bacterial/metabolism , Biofilms/drug effects , Fungal Polysaccharides/pharmacology , Fungal Polysaccharides/chemistry , Microbial Sensitivity Tests
3.
Chemosphere ; 364: 143232, 2024 Sep.
Article in English | MEDLINE | ID: mdl-39236914

ABSTRACT

We introduce a highly efficient method for the catalytic breakdown of organic compounds using nanorods embedded within hollow nanospheres structured magnetoelectric nanocatalyst (MENC). MENCs were fabricated through a single-step process utilizing the ultrasonic spray pyrolysis technique. The dynamic electric dipole generation capability due to synergistic interaction between nanorods at the core and the hollow nanosphere shell creates a nanoscale magnetoelectric device capable of electrocatalysis-assisted water purification through advanced oxidation processes under remotely applied magnetic field excitation. Our study examines the electrocatalytic degradation of organic pollutants by MENCs under magnetic field excitation, achieving an unprecedented 90% removal efficiency for synthetic dyes. This remarkable efficiency is a result of surface redox reactions facilitated by electron and hole transfer, resulting in the production of Reactive oxygen species (ROS) such as O2•- and •OH. Additionally, antioxidant experiments were performed to confirm the ROS generation capability of MENCs under magnetic field excitation. Furthermore, trapping experiments performed employing specific scavengers for individual reactive species reveal the mechanism responsible for the magnetic field-driven catalytic breakdown of organic contaminants by MENCs. Interestingly, the MENCs exhibit >95% reduction in Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus) bacteria, respectively, within 90 min of exposure to a (20 mT& 1.9 kHz) AC magnetic field.


Subject(s)
Environmental Restoration and Remediation , Escherichia coli , Nanospheres , Nanotubes , Staphylococcus aureus , Catalysis , Nanotubes/chemistry , Environmental Restoration and Remediation/methods , Nanospheres/chemistry , Reactive Oxygen Species/chemistry , Water Pollutants, Chemical/chemistry , Oxidation-Reduction , Water Purification/methods , Electrochemical Techniques/methods , Coloring Agents/chemistry
4.
Sci Rep ; 14(1): 22063, 2024 09 27.
Article in English | MEDLINE | ID: mdl-39333179

ABSTRACT

The present study aimed to identify nutrients (UPLC-PDA-ESI-MS/MS, HPLC-RI method) and biological activities (antioxidant activity to reduce Fe3+ and ABTS·+, pancreatic lipase inhibitory effect, α-amylase, and α-glucosidase, anti-bacterial) of 14 highbush blueberries (Vaccinium corymbosum L.) cultivars (Northern type) as well as a principal component analysis (PCA) to assess the variation of these properties in the context of biodiversity. Most of the cultivars in this research have been first presented in this paper. Phytochemical profiling of the tested highbush blueberry fruit revealed 75 bioactive compounds, including 5 macroelements, 7 microelements, 7 monophosphate nucleotides, 15 anthocyanins, 1 phenolic acid, 14 flavonols, 11 essential amino acids, 8 non-essential amino acids, 2 sugars, 7 organic acids. The PCA showed that the profile and contents of the analyzed compounds as well as their anti-bacterial, antioxidant, anti-diabetic, and anti-obesity potentials depended significantly on the tested cultivars. Thus, the study provides comprehensive data on cultivar-specific biodiversity and correlations that can be used to design novel extracts rich in polyphenolic, amino acids, and/or minerals extracts from the selected cultivars of highbush blueberry as natural and alternative sources to fulfill the growing industry demand for supplements, pharmaceuticals, and nutraceutical products.


Subject(s)
Antioxidants , Biodiversity , Blueberry Plants , Blueberry Plants/chemistry , Antioxidants/pharmacology , Antioxidants/analysis , Antioxidants/chemistry , Phytochemicals/analysis , Phytochemicals/pharmacology , Phytochemicals/chemistry , Plant Extracts/pharmacology , Plant Extracts/chemistry , Fruit/chemistry , Nutrients/analysis , Tandem Mass Spectrometry/methods , Principal Component Analysis , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/analysis , alpha-Amylases/antagonists & inhibitors , alpha-Amylases/metabolism , Chromatography, High Pressure Liquid
5.
Fitoterapia ; 179: 106228, 2024 Sep 25.
Article in English | MEDLINE | ID: mdl-39332505

ABSTRACT

BACKGROUND: Apigenin, a naturally occurring compound with a flavone core structure, is known for its diverse bioactivities, including anti-inflammation, anti-toxicant, anti-cancer and so on. There has been significant interest in the medicinal chemistry community. To address these challenges, researchers have developed various derivatives of apigenin to address challenges such as poor water-solubility and low intestinal absorption, aiming to enhance the pharmacological activities and pharmacokinetic properties of this compound. OBJECTIVE: In recent years, there has been a proliferation of apigenin derivatives with enhanced bioactivity. However, there is a lack of comprehensive reviews on the function-based modification of these derivatives. In this paper, we provide an overview of the apigenin derivatives with varying bioactivities and explored their structure activity relationships. And the functions of different groups of apigenin derivatives were also analyzed. CONCLUSION: This review summarized the current achievements that could provide some clues for further study of apigenin-based drugs.

6.
Environ Sci Technol ; 58(32): 14271-14281, 2024 Aug 13.
Article in English | MEDLINE | ID: mdl-39078411

ABSTRACT

Sudden jump of transmembrane pressure (TMP) in membrane bioreactors (MBRs), associated with abrupt aggravation of membrane fouling, limits practical applications of MBRs and calls for effective mitigation strategies. While the TMP jump is generally related to the bacterial activity of biocakes, the mechanisms underlying the TMP jump remain unclear. Herein, we conducted various backwash protocols with different nutrient (e.g., nitrate and sodium acetate) loadings on fouled membranes in MBRs to reveal the critical role of bacterial activity of biocakes for the TMP jump. The filtration tests showed a lower TMP jump rate for the membrane backwashed with a nutrient solution (a mixture of 180 mg/L NaNO3 and 200 mg/L NaAc, averaged at 1.40 kPa/d) than that backwashed with tap water (averaged at 3.56 kPa/d), implying that TMP jump could be efficiently mitigated by providing sufficient nutrients to biocake bacteria. The characterization of biocakes showed that high-nutrient solution backwash considerably increased bacterial viability and activity, while considerably reducing biomolecule accumulation on membranes. The keystone taxa (e.g., g_Aeromonas and o_Chitinophagaceae) in the network of nutrient-enriched biocake communities were involved in nitrate reduction and biomolecule degradation. Ecological null model analyses revealed that the deterministic manner mainly shaped biocake communities with high-nutrient availability. Overall, this study highlights the significance of the bacterial activity of biocakes for TMP development and provides potential alternatives for controlling membrane fouling.


Subject(s)
Bioreactors , Membranes, Artificial , Pressure , Filtration , Bacteria/metabolism
7.
Sci Rep ; 14(1): 14355, 2024 06 21.
Article in English | MEDLINE | ID: mdl-38906908

ABSTRACT

Intensification of staple crops through conventional agricultural practices with chemical synthetic inputs has yielded positive outcomes in food security but with negative environmental impacts. Ecological intensification using cropping systems such as maize edible-legume intercropping (MLI) systems has the potential to enhance soil health, agrobiodiversity and significantly influence crop productivity. However, mechanisms underlying enhancement of biological soil health have not been well studied. This study investigated the shifts in rhizospheric soil and maize-root microbiomes and associated soil physico-chemical parameters in MLI systems of smallholder farms in comparison to maize-monoculture cropping systems (MMC). Maize-root and rhizospheric soil samples were collected from twenty-five farms each conditioned by MLI and MMC systems in eastern Kenya. Soil characteristics were assessed using Black oxidation and Walkley methods. High-throughput amplicon sequencing was employed to analyze fungal and bacterial communities, predicting their functional roles and diversity. The different MLI systems significantly impacted soil and maize-root microbial communities, resulting in distinct microbe sets. Specific fungal and bacterial genera and species were mainly influenced and enriched in the MLI systems (e.g., Bionectria solani, Sarocladium zeae, Fusarium algeriense, and Acremonium persicinum for fungi, and Bradyrhizobium elkanii, Enterobacter roggenkampii, Pantoea dispersa and Mitsuaria chitosanitabida for bacteria), which contribute to nutrient solubilization, decomposition, carbon utilization, plant protection, bio-insecticides/fertilizer production, and nitrogen fixation. Conversely, the MMC systems enriched phytopathogenic microbial species like Sphingomonas leidyi and Alternaria argroxiphii. Each MLI system exhibited a unique composition of fungal and bacterial communities that shape belowground biodiversity, notably affecting soil attributes, plant well-being, disease control, and agroecological services. Indeed, soil physico-chemical properties, including pH, nitrogen, organic carbon, phosphorus, and potassium were enriched in MLI compared to MMC cropping systems. Thus, diversification of agroecosystems with MLI systems enhances soil properties and shifts rhizosphere and maize-root microbiome in favor of ecologically important microbial communities.


Subject(s)
Soil Microbiology , Soil , Zea mays , Zea mays/growth & development , Zea mays/microbiology , Soil/chemistry , Agriculture/methods , Rhizosphere , Microbiota , Crops, Agricultural/growth & development , Crops, Agricultural/microbiology , Ecosystem , Plant Roots/microbiology , Plant Roots/growth & development , Biodiversity , Bacteria/classification , Bacteria/genetics , Bacteria/growth & development , Fungi/genetics , Fungi/classification , Kenya , Crop Production/methods
8.
Tissue Eng Regen Med ; 21(7): 1007-1019, 2024 Oct.
Article in English | MEDLINE | ID: mdl-38877361

ABSTRACT

BACKGROUND: Treatment of skin wounds with diverse pathological characteristics presents significant challenges due to the limited specific and efficacy of current wound healing approaches. Microneedle (MN) patches incorporating bioactive and stimulus materials have emerged as a promising strategy to overcome these limitations and integrating bioactive materials with anti-bacterial and anti-inflammatory properties for advanced wound dressing. METHODS: We isolated diphlorethohydroxycarmalol (DPHC) from Ishige okamurae and assessed its anti-inflammatory and anti-bacterial effects on macrophages and its antibacterial activity against Cutibacterium acnes. Subsequently, we fabricated polylactic acid (PLA) MN patches containing DPHC at various concentrations (0-0.3%) (PDPHC MN patches) and evaluated their mechanical properties and biological effects using in vitro and in vivo models. RESUTLS: Our findings demonstrated that DPHC effectively inhibited nitric oxide production in macrophages and exhibited rapid bactericidal activity against C. acnes. The PDPHC MN patches displayed potent antibacterial effects without cytotoxicity. Moreover, in 2,4-Dinitrochlorobenzene-stimulated mouse model, the PDPHC MN patches significantly suppressed inflammatory response and cutaneous lichenification. CONCLUSION: The results suggest that the PDPHC MN patches holds promise as a multifunctional wound dressing for skin tissue engineering, offering antibacterial properties and anti-inflammatory properties to promote wound healing process.


Subject(s)
Anti-Bacterial Agents , Bandages , Wound Healing , Animals , Mice , Wound Healing/drug effects , Anti-Bacterial Agents/pharmacology , RAW 264.7 Cells , Needles , Macrophages/drug effects , Macrophages/metabolism , Propionibacterium acnes/drug effects , Male , Anti-Inflammatory Agents/pharmacology , Skin/drug effects , Propionibacteriaceae
9.
J Oleo Sci ; 73(5): 787-799, 2024.
Article in English | MEDLINE | ID: mdl-38692900

ABSTRACT

Launaea sarmentosa, also known as Sa Sam Nam, is a widely used remedy in Vietnamese traditional medicine and cuisine. However, the chemical composition and bioactivity of its essential oil have not been elucidated yet. In this study, we identified 40 compounds (98.6% of total peak area) in the essential oil via GC-MS analysis at the first time. Among them, five main compounds including Thymohydroquinone dimethyl ether (52.4%), (E)-α-Atlantone (9.0%), Neryl isovalerate (6.6%), Davanol D2 (isomer 2) (3.9%), and trans-Sesquisabinene hydrate (3.9%) have accounted for 75.8% of total peak area. The anti-bacterial activity of the essential oil against 4 microorganisms including Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa has also investigated via agar well diffusion assay. The results showed that the essential oil exhibited a strong antibacterial activity against Bacillus subtilis with the inhibition zones ranging from 8.2 to 18.7 mm. To elucidate the anti-bacterial effect mechanism of the essential oil, docking study of five main compounds of the essential oil (Thymohydroquinone dimethyl ether, (E)-α-Atlantone, Neryl isovalerate, Davanol D2 (isomer 2), and trans-Sesquisabinene hydrate) against some key proteins for bacterial growth such as DNA gyrase B, penicillin binding protein 2A, tyrosyl-tRNA synthetase, and dihydrofolate reductase were performed. The results showed that the main constituents of essential oil were highly bound with penicillin binding protein 2A with the free energies ranging -27.7 to -44.8 kcal/mol, which suggests the relationship between the antibacterial effect of essential oil and the affinity of main compounds with penicillin binding protein. In addition, the free energies of main compounds of the essential oil with human cyclooxygenase 1, cyclooxygenase 2, and phospholipase A2, the crucial proteins related with inflammatory response were less than diclofenac, a non-steroidal antiinflammatory drug. These findings propose the essential oil as a novel and promising anti-bacterial and anti-inflammatory medicine or cosmetic products.


Subject(s)
Anti-Bacterial Agents , Bacillus subtilis , Hemiterpenes , Molecular Docking Simulation , Oils, Volatile , Pentanoic Acids , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/chemistry , Oils, Volatile/pharmacology , Oils, Volatile/chemistry , Oils, Volatile/isolation & purification , Bacillus subtilis/drug effects , Staphylococcus aureus/drug effects , Pseudomonas aeruginosa/drug effects , Escherichia coli/drug effects , Tetrahydrofolate Dehydrogenase/metabolism , DNA Gyrase/metabolism , Sesquiterpenes/isolation & purification , Sesquiterpenes/pharmacology , Microbial Sensitivity Tests , Gas Chromatography-Mass Spectrometry
10.
Water Res ; 256: 121551, 2024 Jun 01.
Article in English | MEDLINE | ID: mdl-38581981

ABSTRACT

Many antibiotic disinfection byproducts have been detected but their toxicity has not been evaluated adequately. In this report, the chlorination reaction kinetics of five common sulfamides (SAs), reaction intermediates and their toxicity were investigated. Chlorination of sulfapyridine (SPD), sulfamethazine (SMT), sulfathiazole (STZ), and sulfisoxazole (SIZ) followed the second-order kinetics, and were degraded completely within 10 min. A large number of reaction intermediates were deteced by LC-MS, among which a total of 16 intermediates were detected for the first time. Toxicity of the five SAs chlorination solutions was evaluated separately by examining their effects on the growth rate of S. salivarius K12, a commensal bacterium in the human digestive system. After 30 min chlorination, solutions of SMT, STZ and sulfadiazine (SDZ) each exhibited severe toxicity by inhibiting the bacteria growth completely, whereas the inhibition was only 50 % and 20  % by SIZ and SPD respectively. Based on the comparison between toxicity test results and mass spectra, three SA chlorination intermediates, m/z 187.2 (C10H10N4), m/z 287.2 (C9H7N3O4S2) and m/z 215 (C7H10N4O2S/C12H14N4) were proposed to be the primary toxicants in the chlorination products. Our study demonstrated the power of combined approach of chemical analysis and toxicity testing in identifying toxic disinfection byproducts, and highlighted the ne ed for more research on the toxicity evaluation and risk assessment of antibiotic disinfection byproducts.


Subject(s)
Disinfection , Sulfonamides , Humans , Sulfonamides/toxicity , Halogenation , Bacteria/drug effects , Disinfectants/toxicity , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/toxicity , Anti-Bacterial Agents/chemistry , Water Pollutants, Chemical/toxicity , Water Pollutants, Chemical/chemistry
11.
Pak J Biol Sci ; 27(3): 119-124, 2024 Mar.
Article in English | MEDLINE | ID: mdl-38686733

ABSTRACT

<b>Background and Objective:</b> A new strain of cannabis, <i>Cannabis sativa</i> L. Tanao Si Kan Dang RD1, has been approved and registered by the Rajamangala University of Technology Isan, Thailand. The <i>C. sativa</i> is acknowledged for its medicinal properties which demonstrated various therapeutic properties, such as anti-cancer and antibacterial activities. This study aimed to investigate the antibacterial activity of ethanolic extracts from the stems and leaves of the Tanao Si Kan Dang RD1 strain against seven antibiotic-resistant bacteria. <b>Materials and Methods:</b> The primary antibacterial activity of ethanolic Tanao Si Kan Dang RD1 extracts were determined using the disc diffusion method, while the minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) were determined using the broth microdilution method. <b>Results:</b> The largest inhibition zone, measuring 12 mm, was observed in leaf extracts against <i>Pseudomonas aeruginosa</i> 101. The lowest MIC, at 0.78 mg/mL, was obtained from stem extracts against <i>Stenotrophomonas maltophilia</i>. The lowest MBCs, at 12.5 mg/mL, were observed in leaf extracts against <i>Enterococcus faecalis</i>, <i>Acinetobacter baumannii</i>, multidrug-resistant <i>Klebsiella</i> <i>pneumoniae</i>, <i>Stenotrophomonas maltophilia</i> and <i>Pseudomonas aeruginosa</i> 101 and stem extracts against <i>Acinetobacter baumannii</i>, multidrug-resistant <i>Klebsiella pneumoniae</i>, <i>Stenotrophomonas maltophilia</i> and <i>Pseudomonas aeruginosa</i> 101. <b>Conclusion:</b> This study presents a novel finding regarding the antibacterial activity of ethanolic extracts from the leaves and stems of Tanao Si Kan Dang RD1 against antibiotic-resistant bacteria. The potential application of these cannabis plant extracts in the development of antibiotics capable of combating antibiotic-resistant pathogenic bacteria represents a promising strategy to address a significant global health concern.


Subject(s)
Anti-Bacterial Agents , Cannabis , Microbial Sensitivity Tests , Plant Extracts , Plant Extracts/pharmacology , Plant Extracts/chemistry , Anti-Bacterial Agents/pharmacology , Cannabis/chemistry , Humans , Bacteria/drug effects , Bacteria/growth & development , Plant Leaves/chemistry , Ethanol/chemistry , Drug Resistance, Bacterial/drug effects , Plant Stems/chemistry
12.
BMC Chem ; 18(1): 75, 2024 Apr 16.
Article in English | MEDLINE | ID: mdl-38627757

ABSTRACT

Two new Cobalt(II) complexes 12 and 13 have been synthesized from 2-[(E)-(3-acetyl-4-hydroxyphenyl)diazenyl]-4-(2-hydroxyphenyl)thiophene-3-carboxylic acid (11) as a novel ligand. These three new compounds were characterized on the basis of their powder X-Ray Diffraction, UV-Vis, IR, NMR, elemental analysis and MS spectral data. DFT/B3LYP mode of calculations were carried out to determine some theorical parameters of the molecular structure of the ligand. The purity of the azoic ligand and the metal complexes were ascertained by TLC and melting points. The analysis of the IR spectra of the polyfunctionalized azo compound 11 and its metal complexes 12 and 13, reveals that the coordination patterns of the ligand are hexadentate and tetradentate respectively. Based on the UV-Vis electronic spectral data and relevant literature reports, the ligand and derived complexes were assigned the E (trans) isomer form. Likewise, octahedral and square-planar geometries were respectively assigned to the cobalt(II) complexes. The broth microdilution method was used for antibacterial assays through the determination of minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). The ligand 11 displayed moderate antibacterial activity (MIC = 32-128 µg/mL) against Staphylococcus aureus ATCC25923, Escherichia coli ATCC25922, Pseudomonas aeruginosa and Klebsiella pneumoniae 22. The octahedral cobalt(II) complex 12 showed moderate activity against Pseudomonas aeruginosa (MIC = 128 µg/mL) and Klebsiella pneumoniae 22 (MIC = 64 µg/mL) and none against Staphylococcus aureus ATCC25923 and Escherichia coli ATCC25922, whereas the square-planar complex 13 displayed moderate activity only on Klebsiella pneumoniae 22 (MIC = 64 µg/mL).

13.
AAPS PharmSciTech ; 25(5): 90, 2024 Apr 22.
Article in English | MEDLINE | ID: mdl-38649513

ABSTRACT

To formulate and optimize Ozenoxacin nano-emulsion using Quality by Design (QbD) concept by means of Box-Behnken Design (BBD) and converting it to a gel to form Ozenoxacin nano-emulgel followed by physico-chemical, in-vitro, ex-vivo and in-vivo evaluation. This study demonstrates the application of QbD methodology for the development and optimization of an effective topical nanoemulgel formulation for the treatment of Impetigo focusing on the selection of appropriate excipients, optimization of formulation and process variables, and characterization of critical quality attributes. BBD was used to study the effect of "% of oil, % of Smix and homogenization speed" on critical quality attributes "globule size and % entrapment efficiency" for the optimisation of Ozenoxacin Nano-emulsion. Ozenoxacin loaded nano-emulgel was characterized for "description, identification, pH, specific gravity, amplitude sweep, viscosity, assay, organic impurities, antimicrobial effectiveness testing, in-vitro release testing, ex-vivo permeation testing, skin retention and in-vivo anti-bacterial activity". In-vitro release and ex-vivo permeation, skin retention and in-vivo anti-bacterial activity were found to be significantly (p < 0.01) higher for the nano-emulgel formulation compared to the innovator formulation (OZANEX™). Antimicrobial effectiveness testing was performed and found that even at 70% label claim of benzoic acid is effective to inhibit microbial growth in the drug product. The systematic application of QbD principles facilitated the successful development and optimization of a Ozenoxacin Nano-Emulsion. Optimised Ozenoxacin Nano-Emulgel can be considered as an effective alternative and found to be stable at least for 6 months at 40 °C / 75% RH and 30 °C / 75% RH.


Subject(s)
Anti-Bacterial Agents , Emulsions , Impetigo , Quinolones , Animals , Impetigo/drug therapy , Mice , Quinolones/administration & dosage , Quinolones/chemistry , Quinolones/pharmacology , Quinolones/pharmacokinetics , Anti-Bacterial Agents/administration & dosage , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Emulsions/chemistry , Nanoparticles/chemistry , Gels/chemistry , Chemistry, Pharmaceutical/methods , Disease Models, Animal , Aminopyridines/administration & dosage , Aminopyridines/pharmacology , Aminopyridines/chemistry , Aminopyridines/pharmacokinetics , Excipients/chemistry , Skin/drug effects , Skin/metabolism , Microbial Sensitivity Tests/methods , Skin Absorption/drug effects , Administration, Topical , Viscosity , Drug Compounding/methods
14.
Microbiol Spectr ; 12(3): e0294323, 2024 Mar 05.
Article in English | MEDLINE | ID: mdl-38329329

ABSTRACT

Teleost gill mucus has a highly diverse microbiota, which plays an essential role in the host's fitness and is greatly influenced by the environment. Arctic char (Salvelinus alpinus), a salmonid well adapted to northern conditions, faces multiple stressors in the Arctic, including water chemistry modifications, that could negatively impact the gill microbiota dynamics related to the host's health. In the context of increasing environmental disturbances, we aimed to characterize the taxonomic distribution of transcriptionally active taxa within the bacterial gill microbiota of Arctic char in the Canadian Arctic in order to identify active bacterial composition that correlates with environmental factors. For this purpose, a total of 140 adult anadromous individuals were collected from rivers, lakes, and bays belonging to five Inuit communities located in four distinct hydrologic basins in the Canadian Arctic (Nunavut and Nunavik) during spring (May) and autumn (August). Various environmental factors were collected, including latitudes, water and air temperatures, oxygen concentration, pH, dissolved organic carbon (DOC), salinity, and chlorophyll-a concentration. The taxonomic distribution of transcriptionally active taxa within the gill microbiota was quantified by 16S rRNA gene transcripts sequencing. The results showed differential bacterial activity between the different geographical locations, explained by latitude, salinity, and, to a lesser extent, air temperature. Network analysis allowed the detection of a potential dysbiosis signature (i.e., bacterial imbalance) in fish gill microbiota from Duquet Lake in the Hudson Strait and the system Five Mile Inlet connected to the Hudson Bay, both showing the lowest alpha diversity and connectivity between taxa.IMPORTANCEThis paper aims to decipher the complex relationship between Arctic char (Salvelinus alpinus) and its symbiotic microbial consortium in gills. This salmonid is widespread in the Canadian Arctic and is the main protein and polyunsaturated fatty acids source for Inuit people. The influence of environmental parameters on gill microbiota in wild populations remains poorly understood. However, assessing the Arctic char's active gill bacterial community is essential to look for potential pathogens or dysbiosis that could threaten wild populations. Here, we concluded that Arctic char gill microbiota was mainly influenced by latitude and air temperature, the latter being correlated with water temperature. In addition, a dysbiosis signature detected in gill microbiota was potentially associated with poor fish health status recorded in these disturbed environments. With those results, we hypothesized that rapid climate change and increasing anthropic activities in the Arctic might profoundly disturb Arctic char gill microbiota, affecting their survival.


Subject(s)
Lakes , Microbiota , Animals , Bays , Canada , Dysbiosis , Gills , RNA, Ribosomal, 16S/genetics , Trout/genetics , Trout/metabolism , Water/metabolism
15.
Chem Biodivers ; 21(4): e202400026, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38372467

ABSTRACT

Ruta chalepensis L. is a versatile herb used in culinary arts and traditional medicine. The study aimed to determine the chemical composition of an ethanolic extract from R. chalepensis and the total phenolic and flavonoid content. Additionally, the extracts' antimicrobial and antioxidant activities were tested. The disc diffusion method and minimum inhibitory concentration (MIC) were used to test the antibacterial properties on four types of bacteria: Escherichia coli, Proteus penneri, Bacillus cereus, and Staphylococcus aureus. A colorimetric assay was used to evaluate the total phenolic and flavonoid content, and the DPPH method was used to assess the antioxidant activity. The phytochemical constituents were determined using LC-MS/MS. The results indicated that R. chalepensis ethanolic extract had 34 compounds, and the predominant compounds were quercetin (9.2 %), myricetin (8.8 %), and camphene (8.0 %). Moreover, the extract had a good level of polyphenols and flavonoids, as demonstrated by inhibiting free radicals (DPPH) (IC50 was 41.2±0.1). Also, the extract exhibited robust antimicrobial activity against P. penneri and S. aureus with an MIC of 12.5 and 25.0 µg/mL, respectively. In conclusion, the results suggest that the R. chalepensis ethanolic extract has good antioxidant and antibacterial properties that could be utilized to develop new antibacterial agents.


Subject(s)
Anti-Infective Agents , Ruta , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Infective Agents/chemistry , Anti-Infective Agents/isolation & purification , Anti-Infective Agents/pharmacology , Antioxidants/pharmacology , Antioxidants/chemistry , Chromatography, Liquid , Ethanol , Flavonoids/chemistry , Flavonoids/pharmacology , Phenols/pharmacology , Phenols/analysis , Plant Extracts/pharmacology , Plant Extracts/chemistry , Ruta/chemistry , Staphylococcus aureus , Tandem Mass Spectrometry , Polyphenols/chemistry , Polyphenols/pharmacology , Quercetin/chemistry , Quercetin/isolation & purification , Quercetin/pharmacology
16.
Microbiology (Reading) ; 170(2)2024 02.
Article in English | MEDLINE | ID: mdl-38376387

ABSTRACT

The mammalian colon is one of the most densely populated habitats currently recognised, with 1011-1013 commensal bacteria per gram of colonic contents. Enteric pathogens must compete with the resident intestinal microbiota to cause infection. Among these enteric pathogens are Shigella species which cause approximately 125 million infections annually, of which over 90 % are caused by Shigella flexneri and Shigella sonnei. Shigella sonnei was previously reported to use a Type VI Secretion System (T6SS) to outcompete E. coli and S. flexneri in in vitro and in vivo experiments. S. sonnei strains have also been reported to harbour colicinogenic plasmids, which are an alternative anti-bacterial mechanism that could provide a competitive advantage against the intestinal microbiota. We sought to determine the contribution of both T6SS and colicins to the anti-bacterial killing activity of S. sonnei. We reveal that whilst the T6SS operon is present in S. sonnei, there is evidence of functional degradation of the system through SNPs, indels and IS within key components of the system. We created strains with synthetically inducible T6SS operons but were still unable to demonstrate anti-bacterial activity of the T6SS. We demonstrate that the anti-bacterial activity observed in our in vitro assays was due to colicin activity. We show that S. sonnei no longer displayed anti-bacterial activity against bacteria that were resistant to colicins, and removal of the colicin plasmid from S. sonnei abrogated anti-bacterial activity of S. sonnei. We propose that the anti-bacterial activity demonstrated by colicins may be sufficient for niche competition by S. sonnei within the gastrointestinal environment.


Subject(s)
Colicins , Shigella sonnei , Animals , Shigella sonnei/genetics , Escherichia coli/genetics , Bacteria , Gastrointestinal Contents , Mammals
17.
Environ Pollut ; 345: 123476, 2024 Mar 15.
Article in English | MEDLINE | ID: mdl-38311160

ABSTRACT

A biochar-intensified phytoremediation experiment was designed to investigate the dynamic effects of different biochars on polycyclic aromatic hydrocarbon (PAH) removal in ryegrass rhizosphere contaminated soil. Maize and wheat straw biochar pyrolyzed at 300 °C and 500 °C were amended into PAH-contaminated soil, and then ryegrass (Lolium multiflorum L.) was planted for 90 days. Spearman's correlations among PAH removal, enzyme activity, abundance of PAH-ring hydroxylating dioxygenase (PAH-RHDα), and fungal and bacterial community structure were analyzed to elucidate the microbial degradation mechanisms during the combined remediation process. The results showed that 500 °C wheat straw biochar had higher surface area and more nutrients, and significantly accelerated the phytoremediation of PAHs (62.5 %), especially for high molecular weight PAH in contaminated soil. The activities of urease and dehydrogenase and the abundance of total and PAH-degrading bacteria, which improved with time by biochar and ryegrass, had a positive correlation with the removal rate of PAHs. Biochar enhanced the abundance of gram-negative (GN) PAH-RHDα genes. The GN PAH-degraders, Sphingomonas, bacteriap25, Haliangium, and Dongia may play vital roles in PAH degradation in biochar-amended rhizosphere soils. Principal coordinate analysis indicated that biochar led to significant differences in fungal community structures before 30 days, while the diversity of the bacterial community composition depended on planting ryegrass after 60 days. These findings imply that the structural reshaping of microbial communities results from incubation time and the selection of biochar and ryegrass in PAH-contaminated soils. Applying 500 °C wheat straw biochar could enhance the rhizoremediation of PAH-contaminated soil and benefit the soil microbial ecology.


Subject(s)
Charcoal , Microbiota , Polycyclic Aromatic Hydrocarbons , Soil Pollutants , Polycyclic Aromatic Hydrocarbons/analysis , Soil/chemistry , Biodegradation, Environmental , Soil Pollutants/analysis , Soil Microbiology , Bacteria/genetics , Bacteria/metabolism
18.
J Agric Food Chem ; 72(9): 4622-4629, 2024 Mar 06.
Article in English | MEDLINE | ID: mdl-38386000

ABSTRACT

A new class of chiral pyranone fused indole derivatives were prepared by means of N-heterocyclic carbene (NHC) organocatalysis and demonstrated notable antibacterial activity against Xanthomonas oryzae pv oryzae (Xoo). Bioassays showed that compounds (3S,4R)-5b, (3S,4R)-5d, and (3S,4R)-5l exhibited promising in vitro efficacy against Xoo, with EC50 values of 9.05, 9.71, and 5.84 mg/L, respectively, which were superior to that of the positive controls with commercial antibacterial agents, bismerthiazol (BT, EC50 = 27.8 mg/L) and thiodiazole copper (TC, EC50 = 70.1 mg/L). Furthermore, single enantiomer (3S,4R)-5l was identified as an optimal structure displaying 55.3% and 52.0% curative and protective activities against Xoo in vivo tests at a concentration of 200 mg/L, which slightly surpassed the positive control with TC (curative and protective activities of 47.2% and 48.8%, respectively). Mechanistic studies through molecular docking analysis revealed preliminary insights into the distinct anti-Xoo activity of the two single enantiomers (3S,4R)-5l and (3R,4S)-5l, wherein the (3S,4R)-configured stereoisomer could form a more stable interaction with XooDHPS (dihydropteroate synthase). These findings underscore the significant anti-Xoo potential of these chiral pyranone fused indole derivatives, and shall inspire further exploration as promising lead structures for a novel class of bactericides to combat bacterial infections and other plant diseases.


Subject(s)
Oryza , Xanthomonas , Oryza/microbiology , Stereoisomerism , Molecular Docking Simulation , Microbial Sensitivity Tests , Oxadiazoles/chemistry , Anti-Bacterial Agents/chemistry , Plant Diseases/prevention & control , Plant Diseases/microbiology , Indoles/pharmacology
19.
Sci Total Environ ; 921: 171176, 2024 Apr 15.
Article in English | MEDLINE | ID: mdl-38395175

ABSTRACT

The exogenous hydroxylamine dosing has been proven to enhance nitrite supply for anammox bacteria. In this study, exogenous hydroxylamine was fed into a sequencing batch reactor to investigate its long-term effect on anammox granular sludge. The results showed that hydroxylamine enhanced the reactor's performance with an increase in total nitrogen removal rate from 0.23 to 0.52 kg N/m3/d and an increase in bacterial activity from 11.65 to 78.24 mg N/g VSS/h. Meanwhile, hydroxylamine promoted granulation by eluting flocs. And higher anammox activity and granulation were supported by extracellular polymeric substances (EPS) characteristics. Moreover, Candidatus Brocadia's abundance increased from 1.10 % to 3.03 %, and its symbiosis with heterotrophic bacteria was intensified. Additionally, molecular docking detailed the mechanism of the hydroxylamine effect. Overall, this study would provide new insights into the hydroxylamine dosing strategy application.


Subject(s)
Bioreactors , Sewage , Sewage/microbiology , Bioreactors/microbiology , Hydroxylamine , Anaerobic Ammonia Oxidation , Molecular Docking Simulation , Bacteria , Hydroxylamines , Nitrogen , Oxidation-Reduction , Denitrification , Anaerobiosis
20.
Biomed Mater ; 19(2)2024 Feb 09.
Article in English | MEDLINE | ID: mdl-38290149

ABSTRACT

Natural plant-derived small molecules have shown great potential for their antimicrobial and anti-inflammatory properties. In this study, we successfully developed a nanocomplex consisting of magnolol (Mag), a surfactant with an 18 carbon hydrocarbon chain and multi-amine head groups (C18N3), and a peptide (cyclic 9-amino acid peptide (CARG)) with targeting capabilities forStaphylococcus aureus(S. aureus). The obtained Mag/C18N3/CARG nanocomplexes exhibited strong antibacterial activity againstS. aureus. Furthermore, they demonstrated anti-inflammatory effects by reducing the secretion of pro-inflammatory cytokines such as TNF-α, IL-6, and IL-1ßfrom macrophage inflammatory cells. This was achieved through downregulating the activation of NF-κB, KEAP1, and NRF2 signaling pathways. In a murine skin infection model, the Mag/C18N3/CARG nanocomplexes effectively suppressed the growth ofS. aureusin the infected area and promoted wound healing. Additionally, in a mouse model of acute kidney injury (AKI), the nanocomplexes significantly reduced the levels of blood urea nitrogen and creatinine, leading to a decrease in mortality rate. These findings demonstrate the potential of combining natural plant-derived small molecules with C18N3/CARG assemblies as a novel approach for the development of effective and safe antibacterial agents.


Subject(s)
Biphenyl Compounds , Lignans , NF-E2-Related Factor 2 , Staphylococcus aureus , Animals , Mice , Kelch-Like ECH-Associated Protein 1 , Anti-Inflammatory Agents , Anti-Bacterial Agents
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