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1.
Antonie Van Leeuwenhoek ; 117(1): 95, 2024 Jul 05.
Article in English | MEDLINE | ID: mdl-38967683

ABSTRACT

The decline of new antibiotics and the emergence of multidrug resistance in pathogens necessitates a revisit of strategies used for lead compound discovery. This study proposes to induce the production of bioactive compounds with sub-lethal concentrations of silver nanoparticles (Ag-NPs). A total of Forty-two Actinobacteria isolates from four Saudi soil samples were grown with and without sub-lethal concentration of Ag-NPs (50 µg ml-1). The spent broth grown with Ag-NPs, or without Ag-NPs were screened for antimicrobial activity against four bacteria. Interestingly, out of 42 strains, broths of three strains grown with sub-lethal concentration of Ag-NPs exhibit antimicrobial activity against Staphylococcus aureus and Micrococcus luteus. Among these, two strains S4-4 and S4-21 identified as Streptomyces labedae and Streptomyces tirandamycinicus based on 16S rRNA gene sequence were selected for detailed study. The change in the secondary metabolites profile in the presence of Ag-NPs was evaluated using GC-MS and LC-MS analyses. Butanol extracts of spent broth grown with Ag-NPs exhibit strong antimicrobial activity against M. luteus and S. aureus. While the extracts of the controls with the same concentration of Ag-NPs do not show any activity. GC-analysis revealed a clear change in the secondary metabolite profile when grown with Ag-NPs. Similarly, the LC-MS patterns also differ significantly. Results of this study, strongly suggest that sub-lethal concentrations of Ag-NPs influence the production of secondary metabolites by Streptomyces. Besides, LC-MS results identified possible secondary metabolites, associated with oxidative stress and antimicrobial activities. This strategy can be used to possibly induce cryptic biosynthetic gene clusters for the discovery of new lead compounds.


Subject(s)
Anti-Bacterial Agents , Metal Nanoparticles , Microbial Sensitivity Tests , RNA, Ribosomal, 16S , Silver , Staphylococcus aureus , Streptomyces , Streptomyces/metabolism , Streptomyces/genetics , Silver/pharmacology , Silver/chemistry , Silver/metabolism , Metal Nanoparticles/chemistry , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , RNA, Ribosomal, 16S/genetics , Staphylococcus aureus/drug effects , Staphylococcus aureus/growth & development , Soil Microbiology , Secondary Metabolism , Micrococcus luteus/drug effects , Micrococcus luteus/growth & development , Drug Discovery
2.
BMC Res Notes ; 17(1): 169, 2024 Jun 19.
Article in English | MEDLINE | ID: mdl-38898523

ABSTRACT

The purpose of this study was to evaluate antibacterial activity of pigment extracted from bacteria, isolated from soil samples. During the study, 20 soil samples were collected from different areas (forest, agriculture fields, river sides and dumping sites) of Kathmandu and Lalitpur districts which were processed for isolation of pigment producing bacteria by spread plate technique. The pigmented bacterial isolates were identified and enriched in nutrient broth. Then, pigment was extracted in 95% methanol as solvent, which was further characterized using UV-Vis Spectrophotometric and TLC analysis. The obtained crude pigment extract was processed to carry out the antimicrobial susceptibility assay using agar well diffusion method. Out of 13 total pigmented bacteria isolates, four different colored pigmented bacterial isolates (S4O, S11Y, S14P and S17G) which produced efficient pigment on nutrient agar were chosen and they were further processed. Among these isolates, S4O was identified as Staphylococcus aureus, S11Y was identified as Micrococcus luteus, S14P was identified as Micrococcus roseus and S17G was identified as Pseudomonas aeruginosa respectively. On characterization using UV-Vis Spectrophotometric and TLC analysis, the pigment extracted from isolates S4O, S11Y and S14P were found to be Carotenoids and from isolate S17G was found to be Pyocyanin in nature. The maximum antibacterial activity was shown against Staphylococcus aureus from all the four pigments extracts. The green color pigment extract from isolate S17G was found to be most effective against all the Gram-positive and Gram-negative test bacteria. This study suggests that these pigment extracts from pigmented bacteria may have beneficial antibacterial roles that can be exploited in controlling unwanted bacterial growth.


Subject(s)
Anti-Bacterial Agents , Microbial Sensitivity Tests , Pigments, Biological , Soil Microbiology , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/isolation & purification , Pigments, Biological/pharmacology , Pigments, Biological/isolation & purification , Staphylococcus aureus/drug effects , Pseudomonas aeruginosa/drug effects , Bacteria/drug effects , Bacteria/isolation & purification , Micrococcus luteus/drug effects
3.
PeerJ ; 12: e17328, 2024.
Article in English | MEDLINE | ID: mdl-38770094

ABSTRACT

Nanotechnology and nanoparticles have gained massive attention in the scientific community in recent years due to their valuable properties. Among various AgNPs synthesis methods, microbial approaches offer distinct advantages in terms of cost-effectiveness, biocompatibility, and eco-friendliness. In the present research work, investigators have synthesized three different types of silver nanoparticles (AgNPs), namely AgNPs-K, AgNPs-M, and AgNPs-E, by using Klebsiella pneumoniae (MBC34), Micrococcus luteus (MBC23), and Enterobacter aerogenes (MBX6), respectively. The morphological, chemical, and elemental features of the synthesized AgNPs were analyzed by using UV-Vis spectroscopy (UV-Vis), Fourier transform-infrared spectroscopy (FTIR), X-ray diffraction (XRD), field emission scanning electron microscope (FESEM) and energy-dispersive spectroscopy (EDX). UV-Vis absorbance peaks were obtained at 475, 428, and 503 nm for AgNPs-K, AgNPs-M, and AgNPs-E, respectively. The XRD analysis confirmed the crystalline nature of the synthesized AgNPs, having peaks at 26.2°, 32.1°, and 47.2°. At the same time, the FTIR showed bands at 599, 963, 1,693, 2,299, 2,891, and 3,780 cm-1 for all the types of AgNPs indicating the presence of bacterial biomolecules with the developed AgNPs. The size and morphology of the AgNPs varied from 10 nm to several microns and exhibited spherical to porous sheets-like structures. The percentage of Ag varied from 37.8% (wt.%) to 61.6%, i.e., highest in AgNPs-K and lowest in AgNPs-M. Furthermore, the synthesized AgNPs exhibited potential for environmental remediation, with AgNPs-M exhibiting the highest removal efficiency (19.24% at 120 min) for methyl orange dye in simulated wastewater. Further, all three types of AgNPs were evaluated for the removal of methyl orange dye from the simulated wastewater, where the highest dye removal percentage was 19.24% at 120 min by AgNPs-M. Antibacterial potential of the synthesized AgNPs assessment against both Gram-positive (GPB) Bacillus subtilis (MBC23), B. cereus (MBC24), and Gram-negative bacteria Enterococcus faecalis (MBP13) revealed promising results, with AgNPs-M, exhibiting the largest zone of inhibition (12 mm) against GPB B. megaterium. Such investigation exhibits the potential of the bacteria for the synthesis of AgNPs with diverse morphology and potential applications in environmental remediation and antibacterial therapy-based synthesis of AgNPs.


Subject(s)
Azo Compounds , Metal Nanoparticles , Micrococcus luteus , Silver , Silver/chemistry , Silver/pharmacology , Silver/metabolism , Metal Nanoparticles/chemistry , Azo Compounds/chemistry , Azo Compounds/pharmacology , Azo Compounds/metabolism , Micrococcus luteus/drug effects , Spectroscopy, Fourier Transform Infrared , Anti-Infective Agents/pharmacology , Anti-Infective Agents/chemistry , Klebsiella pneumoniae/drug effects , Klebsiella pneumoniae/metabolism , Microbial Sensitivity Tests , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Enterobacter aerogenes/drug effects , Enterobacter aerogenes/metabolism , X-Ray Diffraction , Water Pollutants, Chemical/metabolism , Coloring Agents/chemistry , Coloring Agents/pharmacology
4.
J Antibiot (Tokyo) ; 77(7): 471-474, 2024 Jul.
Article in English | MEDLINE | ID: mdl-38664572

ABSTRACT

Benastatin K (1), a new chlorinated benastatin derivative, was isolated from the culture broth of the actinomycete Streptomyces sp. HGTA384. The structure of 1 was determined on the basis of spectroscopic analysis, including 1D and 2D NMR, as well as HRESI-MS, UV and IR, and comparison with data reported in the literature. Compound 1 and benastatins A and B exhibited inhibitory activity against Micrococcus luteus (MIC 7.8, 31.3, and 3.9 µM, respectively), and IgE-mediated ß-hexosaminidase release in RBL-2H3 cells with IC50 values of 42, 79, and 19 µM, respectively.


Subject(s)
Anti-Bacterial Agents , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Micrococcus luteus , Streptomyces , Streptomyces/chemistry , Streptomyces/metabolism , Micrococcus luteus/drug effects , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/chemistry , Animals , Rats , beta-N-Acetylhexosaminidases/antagonists & inhibitors , beta-N-Acetylhexosaminidases/metabolism , Inhibitory Concentration 50 , Cell Line, Tumor , Molecular Structure
5.
Braz J Microbiol ; 55(2): 1139-1150, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38378880

ABSTRACT

In recent years, some microorganisms have shown resistance to conventional treatments. Considering this increase in resistant pathogens, treatment alternatives are needed to promote greater treatment efficiency. In this sense, antimicrobial photodynamic therapy (aPDT) has been an alternative treatment. This technique uses a photosensitizer that is activated by light with a specific wavelength producing reactive species, leading to the death of pathogenic microorganisms. In this study, bacteriochlorophyll derivatives such as bacteriochlorin metoxi (Bchl-M) and bacteriochlorin trizma (Bchl-T) obtained from purple bacterium (Rhodopseudomonas faecalis), were evaluated as photosensitizers in the aPDT. Photodynamic inactivation (PDI) of the microorganisms Staphylococcus aureus, Micrococcus luteus, Candida albicans and Pseudomonas aeruginosa was investigated with both bacteriochlorins (Bchl-M and Bchl-T) at different concentrations (1, 15 and 30 µM for S. aureus; 1, 15, 30, 45, 60 and 75 µM for M. luteus; 30, 60, 90, 105, 120 and 150 µM for C. albicans; and 200 µM for P. aeruginosa) and different doses of light (20 and 30 J/cm2 for S. aureus and M. luteus; 30 and 45 J/cm2 for C. albicans; and 45 J/cm2 for P. aeruginosa) to inactivate them. Both photosensitizers showed good activation against S. aureus and for M. luteus, we observed the inactivation of these microorganisms at approximately 3 log, showing to be a good photosensitizers for these microorganisms.


Subject(s)
Candida albicans , Light , Photochemotherapy , Photosensitizing Agents , Pseudomonas aeruginosa , Staphylococcus aureus , Photosensitizing Agents/pharmacology , Photosensitizing Agents/chemistry , Candida albicans/drug effects , Candida albicans/radiation effects , Pseudomonas aeruginosa/drug effects , Pseudomonas aeruginosa/radiation effects , Staphylococcus aureus/drug effects , Staphylococcus aureus/radiation effects , Photochemotherapy/methods , Porphyrins/pharmacology , Porphyrins/chemistry , Microbial Viability/drug effects , Microbial Viability/radiation effects , Micrococcus luteus/drug effects , Micrococcus luteus/radiation effects , Bacteria/drug effects , Bacteria/radiation effects
6.
Sci Rep ; 12(1): 2638, 2022 02 16.
Article in English | MEDLINE | ID: mdl-35173259

ABSTRACT

The capture and safe storage of radioactive iodine (129I or 131I) are of a compelling significance in the generation of nuclear energy and waste storage. Because of their physiochemical properties, Porous Organic Polymers (POPs) are considered to be one of the most sought classes of materials for iodine capture and storage. Herein, we report on the preparation and characterization of two triazine-based, nitrogen-rich, porous organic polymers, NRPOP-1 (SABET = 519 m2 g-1) and NRPOP-2 (SABET = 456 m2 g-1), by reacting 1,3,5-triazine-2,4,6-triamine or 1,4-bis-(2,4-diamino-1,3,5-triazine)-benzene with thieno[2,3-b]thiophene-2,5-dicarboxaldehyde, respectively, and their use in the capture of volatile iodine. NRPOP-1 and NRPOP-2 showed a high adsorption capacity of iodine vapor with an uptake of up to 317 wt % at 80 °C and 1 bar and adequate recyclability. The NRPOPs were also capable of removing up to 87% of iodine from 300 mg L-1 iodine-cyclohexane solution. Furthermore, the iodine-loaded polymers, I2@NRPOP-1 and I2@NRPOP-2, displayed good antibacterial activity against Micrococcus luteus (ML), Escherichia coli (EC), and Pseudomonas aeruginosa (PSA). The synergic functionality of these novel polymers makes them promising materials to the environment and public health.


Subject(s)
Anti-Bacterial Agents , Drug Storage/methods , Iodine Radioisotopes , Organic Chemicals , Polymers , Porosity , Triazines , Adsorption , Drug Resistance, Bacterial , Escherichia coli/drug effects , Micrococcus luteus/drug effects , Nitrogen , Organic Chemicals/pharmacology , Polymers/pharmacology , Triazines/pharmacology , Volatilization
7.
Pak J Pharm Sci ; 34(3(Supplementary)): 1149-1156, 2021 May.
Article in English | MEDLINE | ID: mdl-34602445

ABSTRACT

As part of our continuous research to understand the interaction mechanism of drug and metallo-elements, heavy metal complexes of azithromycin (AZI) were synthesized with arsenic oxide, lead carbonate and silver chloride salts in molar ratio of 2: 1 (L: M). Synthesized heavy metal complexes have shown good percent yield and characterized through spectroscopic parameters including UV-Visible, TLC, FT-IR, NMR and elemental analysis (CHN). Spectroscopic characterization reveals the binding of ligand AZI with heavy metals in bi-dentate manner involving the hydroxide and 9a-NCH3 group of the aglycone ring of AZI. These newly synthesized heavy metal complexes were evaluated for their antimicrobial response against selected gram positive and gram negative organisms and antifungal species. It was noted that all newly synthesized complexes exhibits increased activity against B.subtilus whereas, AZI itself didn't show any activity, while synthesized complexes have low to moderate response against all the studied organisms. Complex A-M12 possess greater enzymatic response against both urease and alpha chymotrypsin among all the studied complexes. Results obtained were then statistically analyzed through one way ANOVA and Dunnett's test by using SPSS version 20.0 suggesting the significant response of complexes against selected organisms.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Arsenic Trioxide/pharmacology , Azithromycin/pharmacology , Carbonates/pharmacology , Coordination Complexes/pharmacology , Lead/pharmacology , Silver Compounds/pharmacology , Arsenic Trioxide/chemistry , Azithromycin/analogs & derivatives , Azithromycin/chemistry , Bacillus subtilis/drug effects , Candida albicans/drug effects , Carbonates/chemistry , Chymotrypsin/metabolism , Citrobacter/drug effects , Coordination Complexes/chemistry , Disk Diffusion Antimicrobial Tests , Enzyme Assays , Escherichia coli/drug effects , Klebsiella pneumoniae/drug effects , Lead/chemistry , Micrococcus luteus/drug effects , Proteus mirabilis/drug effects , Pseudomonas aeruginosa/drug effects , Salmonella typhi/drug effects , Shigella flexneri/drug effects , Silver Compounds/chemistry , Staphylococcus aureus/drug effects , Streptococcus/drug effects , Urease/metabolism
8.
Fitoterapia ; 152: 104937, 2021 Jul.
Article in English | MEDLINE | ID: mdl-34000328

ABSTRACT

Five new phenylspirodrimanes, stachybomycins A - E (1-5), together with four known compounds (6-9), were isolated from the marine-derived fungus Stachybotrys sp. SCSIO 40434. Their structures were elucidated by comprehensive spectroscopic analyses of NMR and HRESIMS. The absolute configuration of 1 was confirmed by single crystal X-ray diffraction analysis. Compounds 5 and 7 showed moderate antibacterial activities against Micrococcus luteus, Staphylococcus aureus and methicillin resistant Staphylococcus aureus with minimal inhibition concentration (MIC) values of 8, 16 and 16 µg mL-1, respectively.


Subject(s)
Anti-Bacterial Agents/pharmacology , Biological Products/pharmacology , Stachybotrys/chemistry , Anti-Bacterial Agents/isolation & purification , Aquatic Organisms/chemistry , Biological Products/isolation & purification , China , Methicillin-Resistant Staphylococcus aureus/drug effects , Micrococcus luteus/drug effects , Molecular Structure , Pacific Ocean , Staphylococcus aureus/drug effects
9.
Microb Cell Fact ; 20(1): 30, 2021 Feb 02.
Article in English | MEDLINE | ID: mdl-33531005

ABSTRACT

BACKGROUND: Protein aggregation is a biological event observed in expression systems in which the recombinant protein is produced under stressful conditions surpassing the homeostasis of the protein quality control system. In addition, protein aggregation is also related to conformational diseases in animals as transmissible prion diseases or non-transmissible neurodegenerative diseases including Alzheimer, Parkinson's disease, amyloidosis and multiple system atrophy among others. At the molecular level, the presence of aggregation-prone domains in protein molecules act as seeding igniters to induce the accumulation of protein molecules in protease-resistant clusters by intermolecular interactions. RESULTS: In this work we have studied the aggregating-prone performance of a small peptide (L6K2) with additional antimicrobial activity and we have elucidated the relevance of the accompanying scaffold protein to enhance the aggregating profile of the fusion protein. Furthermore, we demonstrated that the fusion of L6K2 to highly soluble recombinant proteins directs the protein to inclusion bodies (IBs) in E. coli through stereospecific interactions in the presence of an insoluble protein displaying the same aggregating-prone peptide (APP). CONCLUSIONS: These data suggest that the molecular bases of protein aggregation are related to the net balance of protein aggregation potential and not only to the presence of APPs. This is then presented as a generic platform to generate hybrid protein aggregates in microbial cell factories for biopharmaceutical and biotechnological applications.


Subject(s)
Inclusion Bodies/metabolism , Peptides/metabolism , Protein Aggregates , Anti-Infective Agents/pharmacology , Escherichia coli/drug effects , Escherichia coli/metabolism , Fluorescence , Green Fluorescent Proteins/metabolism , Microbial Sensitivity Tests , Microbial Viability/drug effects , Micrococcus luteus/drug effects , Recombinant Proteins/metabolism , Solubility , Staphylococcus aureus/drug effects
10.
Vet Res ; 52(1): 32, 2021 Feb 25.
Article in English | MEDLINE | ID: mdl-33632337

ABSTRACT

Tissue factor pathway inhibitors (TFPI), including TFPI-1 and TFPI-2, are Kunitz-type serine protease inhibitors that mainly inhibit the blood coagulation induced by tissue factors. Previous reports on teleost proved TFPI play important roles in innate immunity. In this study, two TFPI (PoTFPI-1 and PoTFPI-2) molecules from Japanese flounder (Paralichthys olivaceus) were analyzed and characterized for their expression patterns, antibacterial and anticancer activities of the C-terminal derived peptides. Quantitative real time RT-PCR analysis shows that constitutive PoTFPI-1 expression occurred, in increasing order, in the brain, muscle, spleen, gills, head kidney, blood, intestine, heart, and liver; PoTFPI-2 was expressed, in increasing order, in the brain, gills, head kidney, muscle, intestine, spleen, liver, heart, and blood. Under the stimulation of fish pathogens, both PoTFPI-1 and PoTFPI-2 expressions increased significantly in a manner that depended on the pathogens, tissue type, and infection stage. Furthermore, C-terminal peptides TP25 and TP26, derived from PoTFPI-1 and PoTFPI-2, respectively, were synthesized and proved to be active against Micrococcus luteus (for TP25 and TP26) and Staphylococcus aureus (for TP25) via retardation effects on bacterial nucleic acids. In addition, TP25 and TP26 also displayed significant inhibitory effects on human colon cancer cell line HT-29. These results reveal that both PoTFPI-1 and PoTFPI-2 play important roles in host innate immunity. The antibacterial activity and anticancer cells function of TP25 and TP26 will add new insights into the roles of teleost TFPI.


Subject(s)
Fish Diseases/immunology , Fish Proteins/genetics , Fish Proteins/immunology , Flatfishes/genetics , Flatfishes/immunology , Gene Expression Regulation/immunology , Immunity, Innate/genetics , Amino Acid Sequence , Animals , Anti-Bacterial Agents/pharmacology , Antineoplastic Agents/pharmacology , Gene Expression Profiling/veterinary , Glycoproteins/chemistry , Glycoproteins/genetics , Glycoproteins/immunology , Lipoproteins/chemistry , Lipoproteins/genetics , Lipoproteins/immunology , Micrococcus luteus/drug effects , Phylogeny , Staphylococcus aureus/drug effects
11.
Biochem J ; 478(1): 63-78, 2021 01 15.
Article in English | MEDLINE | ID: mdl-33313751

ABSTRACT

Multidrug resistant (MDR) bacteria have adapted to most clinical antibiotics and are a growing threat to human health. One promising type of candidates for the everlasting demand of new antibiotic compounds constitute antimicrobial peptides (AMPs). These peptides act against different types of microbes by permeabilizing pathogen cell membranes, whereas being harmless to mammalian cells. Contrarily, another class of membrane-active peptides, namely cell-penetrating peptides (CPPs), is known to translocate in eukaryotic cells without substantially affecting the cell membrane. Since CPPs and AMPs share several physicochemical characteristics, we hypothesized if we can rationally direct the activity of a CPP towards antimicrobial activity. Herein, we describe the screening of a synthetic library, based on the CPP sC18, including structure-based design to identify the active residues within a CPP sequence and to discover novel AMPs with high activity. Peptides with increased hydrophobicity were tested against various bacterial strains, and hits were further optimized leading to four generations of peptides, with the last also comprising fluorinated amino acid building blocks. Interestingly, beside strong antibacterial activities, we also detected activity in cancer cells, while non-cancerous cells remained unharmed. The results highlight our new candidates, particularly those from generation 4, as a valuable and promising source for the development of future therapeutics with antibacterial activity and beyond.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antimicrobial Cationic Peptides/chemistry , Antineoplastic Agents/pharmacology , Bacteria/drug effects , Cell Membrane/drug effects , Cell-Penetrating Peptides/chemistry , Antimicrobial Cationic Peptides/chemical synthesis , Antimicrobial Cationic Peptides/pharmacology , Bacillus subtilis/drug effects , Bacillus subtilis/ultrastructure , Cell Line, Tumor , Cell Survival/drug effects , Cell-Penetrating Peptides/chemical synthesis , Cell-Penetrating Peptides/pharmacology , Circular Dichroism , Corynebacterium glutamicum/drug effects , Corynebacterium glutamicum/ultrastructure , Halogenation , Hemolysis/drug effects , Humans , Hydrophobic and Hydrophilic Interactions , Inhibitory Concentration 50 , Microbial Sensitivity Tests , Micrococcus luteus/drug effects , Microscopy, Electron, Scanning , Pseudomonas fluorescens/drug effects , Pseudomonas fluorescens/ultrastructure
12.
Curr Pharm Biotechnol ; 22(1): 115-122, 2021.
Article in English | MEDLINE | ID: mdl-32525768

ABSTRACT

BACKGROUND: Bacteriocins (Bac1, Bac2, and Bac3) from Weissella confusa MBF8-1, weissellicin- MBF, have been reported as potential alternative substances as well as complements to the existing antibiotics against many antimicrobial-resistant pathogens. Previously, the genes encoded in the large plasmid, pWcMBF8-1, and the spermicidal activity of their synthetic peptides, originally discovered Indonesia, have been studied. Three synthetic bacteriocins peptides of this weissellicin-MBF have been reported for their potential activities, i.e. antibacterial and spermicidal. OBJECTIVE: The aim of this study was to construct the recombinant Bacteriocin (r-Bac) genes, as well as to investigate the gene expressions and their functional analysis. METHODS: Here, the recombinant Bacteriocin (r-Bac) genes were constructed and the recombinant peptides (r-Bac1, r-Bac2, and r-Bac3) in B. subtilis DB403 cells were produced on a large scale. After purification, using the His-tag affinity column, their potential bioactivities were measured as well as their antibacterial minimum inhibitory concentrations against Leuconostoc mesenteroides and Micrococcus luteus, were determined. RESULTS: Pure His-tag-recombinant Bac1, Bac2, and Bac3 were obtained and they could inhibit the growth of L. mesenteroides and M. luteus. CONCLUSION: The recombinant bacteriocin could be obtained although with weak activity in inhibiting gram-positive bacterial growth.


Subject(s)
Anti-Bacterial Agents/pharmacology , Bacteriocins/pharmacology , Recombinant Proteins/pharmacology , Weissella/metabolism , Bacteriocins/genetics , Cloning, Molecular , Genes, Bacterial , Leuconostoc mesenteroides/drug effects , Microbial Sensitivity Tests , Micrococcus luteus/drug effects , Plasmids , Recombinant Proteins/genetics
13.
Mol Divers ; 25(2): 981-993, 2021 May.
Article in English | MEDLINE | ID: mdl-32301033

ABSTRACT

One palladium-catalyzed sequential coupling reactions were successfully used as a new protocol for the synthesis of unsymmetrical 2,3-diethynyl quinoxalines and 4-ethynyl-substituted pyrrolo[1,2-a]quinoxalines. The one-pot two coupling reactions of 2,3-dichloroquinoxaline, with two different terminal alkynes, under controlled conditions produced selectively unsymmetrical 2,3-diethynyl quinoxalines with high yields. When one of the two terminal alkynes was 3-propyne-1-ol, in the presence of secondary amines, cyclization occurred and 4-ethynyl-substituted pyrrolo[1,2-a]quinoxalines were successfully formed. All synthesized compounds were tested against the two bacterial strains including Micrococcus luteus and Pseudomonas aeruginosa.


Subject(s)
Anti-Bacterial Agents , Pyrroles , Quinoxalines , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Catalysis , Micrococcus luteus/drug effects , Micrococcus luteus/growth & development , Palladium/chemistry , Pseudomonas aeruginosa/drug effects , Pseudomonas aeruginosa/growth & development , Pyrroles/chemical synthesis , Pyrroles/chemistry , Pyrroles/pharmacology , Quinoxalines/chemical synthesis , Quinoxalines/chemistry , Quinoxalines/pharmacology
14.
Chem Biodivers ; 17(11): e2000566, 2020 Nov.
Article in English | MEDLINE | ID: mdl-32954632

ABSTRACT

The AcOEt extract of Artemisia argyi-derived fungus Trichoderma koningiopsis QA-3 showed potent inhibitory activity against pathogenic bacteria. Fractionation of the extract resulted in the isolation of three new polyketides (1-3) and two new terpenoids (4 and 5), together with three known metabolites (6-8). Their chemical structures were analyzed by NMR spectra, ECD, HR-ESI-MS or HR-EI-MS, optical rotation, and X-ray crystallographic data, as well as by comparison with literature reports. In the antibacterial assays, 3-hydroxyharziandione (4) showed potent activity against human pathogen Escherichia coli with an MIC value of 0.5 µg/mL, while 6-(3-hydroxypent-1-en-1-yl)-2H-pyran-2-one exhibited strong activity against marine-derived aquatic pathogen Micrococcus luteus with an MIC value of 1.0 µg/mL.


Subject(s)
Anti-Bacterial Agents/chemistry , Artemisia/microbiology , Hypocreales/chemistry , Polyketides/chemistry , Terpenes/chemistry , Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/pharmacology , Crystallography, X-Ray , Escherichia coli/drug effects , Hypocreales/metabolism , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Micrococcus luteus/drug effects , Molecular Conformation , Polyketides/isolation & purification , Polyketides/pharmacology , Spectrometry, Mass, Electrospray Ionization , Terpenes/isolation & purification , Terpenes/pharmacology
15.
Nat Commun ; 11(1): 3894, 2020 08 04.
Article in English | MEDLINE | ID: mdl-32753597

ABSTRACT

Here, we demonstrate the self-assembly of the antimicrobial human LL-37 active core (residues 17-29) into a protein fibril of densely packed helices. The surface of the fibril encompasses alternating hydrophobic and positively charged zigzagged belts, which likely underlie interactions with and subsequent disruption of negatively charged lipid bilayers, such as bacterial membranes. LL-3717-29 correspondingly forms wide, ribbon-like, thermostable fibrils in solution, which co-localize with bacterial cells. Structure-guided mutagenesis analyses supports the role of self-assembly in antibacterial activity. LL-3717-29 resembles, in sequence and in the ability to form amphipathic helical fibrils, the bacterial cytotoxic PSMα3 peptide that assembles into cross-α amyloid fibrils. This argues helical, self-assembling, basic building blocks across kingdoms of life and points to potential structural mimicry mechanisms. The findings expose a protein fibril which performs a biological activity, and offer a scaffold for functional and durable biomaterials for a wide range of medical and technological applications.


Subject(s)
Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Antimicrobial Cationic Peptides/chemistry , Antimicrobial Cationic Peptides/pharmacology , Bacteria/drug effects , Amyloid/metabolism , Animals , Antimicrobial Cationic Peptides/genetics , Bacteria/metabolism , Benzothiazoles , Cathelicidins/pharmacology , Crystallography, X-Ray , Gorilla gorilla , Humans , Microbial Sensitivity Tests , Micrococcus luteus/drug effects , Microscopy, Confocal , Microscopy, Electron, Transmission , Models, Molecular , Protein Conformation , Staphylococcus hominis/drug effects , X-Ray Diffraction
16.
J Pept Sci ; 26(10): e3276, 2020 Oct.
Article in English | MEDLINE | ID: mdl-32715598

ABSTRACT

A novel antimicrobial peptide derived from ovalbumin has been discovered. First, the peptide fragment RKIKVYLPRMK (TK9.1) was identified based on computerized predictions of the secondary structure of peptides in a protein data bank. Using HeliQuest, the sequence was developed into RKIKRYLRRMI (TK9.1.3), which was synthesized using Fmoc-solid phase peptide synthesis, and found to have strongly antimicrobial activity against Gram-positive and Gram-negative bacteria, and fungi but not cytotoxic to HeLa cells and hemolysis in mouse red blood cells. Although ovalbumin itself does not have an antibacterial activity, our results suggest that it may supply the organisms that consume it with antimicrobial peptides, in support of their immunodefence.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Ovalbumin/chemistry , Peptide Fragments/pharmacology , Amino Acid Sequence , Animals , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry , Aspergillus oryzae/drug effects , Candida/drug effects , Escherichia coli/drug effects , HeLa Cells , Humans , Mice , Microbial Sensitivity Tests , Micrococcus luteus/drug effects , Peptide Fragments/chemical synthesis , Peptide Fragments/chemistry , Protein Structure, Secondary , Pseudomonas/drug effects , Staphylococcus epidermidis/drug effects
17.
Molecules ; 25(13)2020 Jul 02.
Article in English | MEDLINE | ID: mdl-32630666

ABSTRACT

Microbial conversion of oleic acid (1) to form value-added industrial products has gained increasing scientific and economic interest. So far, the production of natural lactones with flavor and fragrance properties from fatty acids by non-genetically modified organisms (non-GMO) involves whole cells of bacteria catalyzing the hydration of unsaturated fatty acids as well as yeast strains responsible for further ß-oxidation processes. Development of a non-GMO process, involving a sole strain possessing both enzymatic activities, significantly lowers the costs of the process and constitutes a better method from the customers' point of view regarding biosafety issues. Twenty bacteria from the genus of Bacillus, Comamonas, Dietzia, Gordonia, Micrococcus, Pseudomonas, Rhodococcus and Streptomyces were screened for oxidative functionalization of oleic acid (1). Micrococcus luteus PCM525 was selected as the sole strain catalyzing the one-pot transformation of oleic acid (1) into natural valuable peach and strawberry-flavored γ-dodecalactone (6) used in the food, beverage, cosmetics and pharmaceutical industries. Based on the identified products formed during the process of biotransformation, we clearly established a pathway showing that oleic acid (1) is hydrated to 10-hydroxystearic acid (2), then oxidized to 10-ketostearic acid (3), giving 4-ketolauric acid (4) after three cycles of ß-oxidation, which is subsequently reduced and cyclized to γ-dodecalactone (6) (Scheme 1). Moreover, three other strains (Rhodococcus erythropolis DSM44534, Rhodococcus ruber PCM2166, Dietzia sp. DSM44016), with high concomitant activities of oleate hydratase and alcohol dehydrogenase, were identified as efficient producers of 10-ketostearic acid (3), which can be used in lubricant and detergent formulations. Considering the prevalence of γ-dodecalactone (6) and 10-ketostearic acid (3) applications and the economic benefits of sustainable management, microbial bioconversion of oleic acid (1) is an undeniably attractive approach.


Subject(s)
4-Butyrolactone/analogs & derivatives , Micrococcus luteus/metabolism , Oleic Acid/metabolism , Stearic Acids/metabolism , 4-Butyrolactone/biosynthesis , Carbon/metabolism , Culture Media/chemistry , Culture Media/pharmacology , Gas Chromatography-Mass Spectrometry , Industrial Microbiology/methods , Linoleic Acid/metabolism , Micrococcus luteus/drug effects , Micrococcus luteus/growth & development , Oleic Acid/pharmacokinetics , Oxidation-Reduction , Surface-Active Agents/chemistry , Surface-Active Agents/metabolism , alpha-Linolenic Acid/metabolism
18.
Biosci Biotechnol Biochem ; 84(8): 1570-1575, 2020 Aug.
Article in English | MEDLINE | ID: mdl-32338185

ABSTRACT

Chemical screening of culture medium from the soil fungus Stachybotrys sp. resulted in the isolation of the three new phenylspirodrimanes MBJ-0030 (1), MBJ-0031 (2) and MBJ-0032 (3). Their structures were determined by detailed analysis of spectroscopic data. The absolute configurations of 1-3 were determined by modified Mosher's and Marfey's methods. In addition, cytotoxic and antimicrobial evaluations of the compounds were conducted.


Subject(s)
Polycyclic Sesquiterpenes/chemistry , Spiro Compounds/chemistry , Stachybotrys/chemistry , Cell Line, Tumor , Cell Survival/drug effects , Humans , Micrococcus luteus/drug effects , Micrococcus luteus/growth & development , Polycyclic Sesquiterpenes/isolation & purification , Soil Microbiology , Spiro Compounds/isolation & purification , Stachybotrys/isolation & purification
19.
J Antibiot (Tokyo) ; 73(7): 429-434, 2020 07.
Article in English | MEDLINE | ID: mdl-32203125

ABSTRACT

Microbial-derived natural products provide unique bioactivities and serve as a unique source of drug leads. In the present study, we isolated one new chresdihydrochalcone (1), one new chresphenylacetone (2), and one known streptimidone (3) from Streptomyces chrestomyceticus BCC 24770 using antibacterial activity-guided isolation and purification procedures. We determined their molecular weights using MS and HRMS and elucidated their chemical structures from their 1D and 2D NMR and electronic circular dichroism (ECD) spectra. Compound 1 showed moderate inhibitory activities against the Gram-positive bacteria Methicillin-resistant Staphylococcus aureus, Bacillus subtilis, and Micrococcus luteus. Cytotoxicity and hemolytic activity were not observed at a concentration of up to 100 µg ml-1. The specific antimicrobial activity and low toxicity of compound 1 indicate this compound to be a potential antibiotic candidate, especially as antibiotic resistance has become a significant public health threat.


Subject(s)
Anti-Bacterial Agents/pharmacology , Anti-Infective Agents/pharmacology , Gram-Positive Bacteria/drug effects , Streptomyces/metabolism , Bacillus subtilis/drug effects , Methicillin-Resistant Staphylococcus aureus/drug effects , Microbial Sensitivity Tests/methods , Micrococcus luteus/drug effects
20.
Carbohydr Res ; 491: 107979, 2020 May.
Article in English | MEDLINE | ID: mdl-32171995

ABSTRACT

Bacterial cellulose (BC) is an excellent natural biopolymer with wide range of applications. The present study reports a potential BC producing thermophile, identified as Bacillus licheniformis strain ZBT2. The thermophile produced pellicle form of BC (3.0 g/l) under static conditions. Statistical optimization of BC was carried out by Plackett-Burman and central composite design. Results suggest that BC yield (9.2 g/l) was enhanced with 6.6-fold after optimization. BC-gelatin hydrogels composites were developed to assess various properties. The water retention capability and moisture content properties of BC and composites were promising and also exhibited negligible protein adsorption. The composites also demonstrated to be consistent during controlled drug delivery profiling. Furthermore, the composites also demonstrated antibacterial efficiency against Escherichia coli and Micrococcus luteus. The structural, morphological and thermal properties were assessed by analytical techniques such as, fourier transform infrared spectroscopy, scanning electron microscopy with energy dispersive X-ray analysis, thermogravimetric analysis and differential scanning calorimetry analysis. The study reflects the exploitation of a thermophile for development of BC which can be a preferred choice as a scaffold for tissue engineering and drug-delivery systems.


Subject(s)
Anti-Bacterial Agents/biosynthesis , Bacillus licheniformis/chemistry , Cellulose/biosynthesis , Temperature , Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/pharmacology , Bacillus licheniformis/metabolism , Cellulose/isolation & purification , Cellulose/pharmacology , Escherichia coli/drug effects , Microbial Sensitivity Tests , Micrococcus luteus/drug effects , Particle Size , Surface Properties
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