scholarly journals Lipidated Analogs of the LL-37-Derived Peptide Fragment KR12—Structural Analysis, Surface-Active Properties and Antimicrobial Activity

2020 ◽  
Vol 21 (3) ◽  
pp. 887 ◽  
Author(s):  
Elżbieta Kamysz ◽  
Emilia Sikorska ◽  
Maciej Jaśkiewicz ◽  
Marta Bauer ◽  
Damian Neubauer ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Self Assembly ◽  
Multidrug Resistant ◽  
Cd Spectroscopy ◽  
Modern Medicine ◽  
Aromatic Acids ◽  
Human Red Blood Cells ◽  
N Terminus ◽  
New Antibiotics ◽  
Assembly Behavior

An increasing number of multidrug-resistant pathogens is a serious problem of modern medicine and new antibiotics are highly demanded. In this study, different n-alkyl acids (C2-C14) and aromatic acids (benzoic and trans-cinnamic) were conjugated to the N-terminus of KR12 amide. The effect of this modification on antimicrobial activity (ESKAPE bacteria and biofilm of Staphylococcus aureus) and cytotoxicity (human red blood cells and HaCaT cell line) was examined. The effect of lipophilic modifications on helicity was studied by CD spectroscopy, whereas peptide self-assembly was studied by surface tension measurements and NMR spectroscopy. As shown, conjugation of the KR12-NH2 peptide with C4-C14 fatty acid chains enhanced the antimicrobial activity with an optimum demonstrated by C8-KR12-NH2 (MIC 1–4 μg/mL against ESKAPE strains; MBEC of S. aureus 4–16 μg/mL). Correlation between antimicrobial activity and self-assembly behavior of C14-KR12-NH2 and C8-KR12-NH2 has shown that the former self-assembled into larger aggregated structures, which reduced its antimicrobial activity. In conclusion, N-terminal modification can enhance antimicrobial activity of KR12-NH2; however, at the same time, the cytotoxicity increases. It seems that the selectivity against pathogens over human cells can be achieved through conjugation of peptide N-terminus with appropriate n-alkyl fatty and aromatic acids.

Antimicrobial activity and self-assembly behavior of antimicrobial peptide chensinin-1b with lipophilic alkyl tails

2018 ◽  
Vol 150 ◽  
pp. 546-558 ◽  
Author(s):  
Weibing Dong ◽  
Ziang Liu ◽  
Liying Sun ◽  
Cui Wang ◽  
Yue Guan ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Peptide ◽  
Self Assembly ◽  
Assembly Behavior

scholarly journals In vitro activity of hybrid lavender essential oils against multidrug resistant strains of Pseudomonas aeruginosa

2018 ◽  
Vol 12 (01) ◽  
pp. 009-014 ◽  
Author(s):  
Matthew Donadu ◽  
Donatella Usai ◽  
Antonio Pinna ◽  
Tiziana Porcu ◽  
Vittorio Mazzarello ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Essential Oils ◽  
Cell Model ◽  
Antimicrobial Properties ◽  
The United States ◽  
Multidrug Resistant ◽  
New Antibiotics ◽  
Mediterranean Regions ◽  
A Cell

Introduction: Lavender is an evergreen shrub native to Northern Africa and other mountainous Mediterranean regions. It grows throughout Southern Europe, the United States, and Australia. Lavender essential oil has been used since ancient times and is known for its anti-inflammatory, antidepressant, antiseptic, antifungal and antimicrobial properties. Methodology: in this study, the antimicrobial activity of two Lavender essential oils (Lavanda sumian and Lavanda grosso) against 16 multidrug-resistant P. aeruginosa strains from clinical ocular samples taken from migrant patients has been investigated. The in vitro cytotoxic activity on human Wong-Kilbourne derivative (WKD) conjunctiva cells from healthy patients and nitric oxide synthase (NOS) activity on murine macrophage (J774.1A) were also evaluated. Results: L. sumian showed lower antimicrobial activity when compared to L. grosso. Both lavender oils tested had no cytotoxic effect at very low concentrations, mostly L. grosso. The essential oils extracted from L. sumian and L. grosso significantly reduced NOS in a cell model. Conclusion: Increase in drug resistance and lack of new antibiotics may encourage the development of natural antimicrobial treatments.

scholarly journals Application of iChip to Grow “Uncultivable” Microorganisms and its Impact on Antibiotic Discovery

2015 ◽  
Vol 18 (3) ◽  
pp. 303 ◽  
Author(s):  
Rinzhin T. Sherpa ◽  
Caretta J. Reese ◽  
Hamidreza Montazeri Aliabadi
Keyword(s):  
Antimicrobial Activity ◽  
Antibiotic Resistance ◽  
Pathogenic Bacteria ◽  
Modern Medicine ◽  
Natural Phenomenon ◽  
Significant Progress ◽  
Cultivation Method ◽  
New Antibiotics ◽  
Antibiotic Discovery

Antibiotics have revolutionized modern medicine, allowing significant progress in healthcare and improvement in life expectancy. Development of antibiotic resistance by pathogenic bacteria is a natural phenomenon; however, the rate of antibiotic resistance emergence is increasing at an alarming rate, due to indiscriminate use of antibiotics in healthcare, agriculture and even everyday products. Traditionally, antibiotic discovery has been conducted by screening extracts of microorganisms for antimicrobial activity. However, this conventional source has been over-used to such an extent that it poses the risk of “running out” of new antibiotics. Aiming to increase access to a greater diversity of microorganisms, a new cultivation method with an in situ approach called iChip has been designed. The iChip has already isolated many novel organisms, as well as Teixobactin, a novel antibiotic with significant potency against gram-positive bacteria.This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

scholarly journals In vitro activity of essential oils against Pseudomonas aeruginosa isolated from infected hip implants

2018 ◽  
Vol 12 (11) ◽  
pp. 996-1001 ◽  
Author(s):  
Veronica Amorese ◽  
Matthew Donadu ◽  
Donatella Usai ◽  
Angelino Sanna ◽  
Fabio Milia ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Essential Oils ◽  
Antimicrobial Properties ◽  
Multidrug Resistant ◽  
Thymus Vulgaris ◽  
Hip Implants ◽  
Melaleuca Alternifolia ◽  
New Antibiotics ◽  
Normal Human

Introduction: Essential oils have been used since ancient times and are known for their anti-inflammatory, anti-depressive, antiseptic, antifungal and antimicrobial properties. Methodology: in this study the antimicrobial activity of two essential oils from Melaleuca alternifolia and Thymus vulgaris–red thyme geraniol was tested against 16 multidrug-resistant P. aeruginosa strains from infected hip implants as well as the “in vitro” cytotoxic activity on normal human Wong-Kilbourne derivative (WKD) cells. Results: Thymus vulgaris–red thyme geraniol showed lower antimicrobial activity when compared to Melaleuca alternifolia. All tested oils were cytotoxic at concentrations lower than 0.12%. Conclusion: Increase in drug resistance and lack of new antibiotics may encourage the development of natural treatments together with higher concern on environmental issues and natural lifestyle.

scholarly journals In Vitro Evaluation of Antimicrobial Activity and Cytotoxicity of Different Nanobiotics Targeting Multidrug Resistant and Biofilm Forming Staphylococci

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Mennatallah A. Mohamed ◽  
Maha Nasr ◽  
Walid F. Elkhatib ◽  
Wafaa N. Eltayeb
Keyword(s):  
Antimicrobial Activity ◽  
Rat Hepatocytes ◽  
Antibacterial Activities ◽  
Multidrug Resistant ◽  
Antimicrobial Activities ◽  
Antibiotic Resistant ◽  
Diphenyltetrazolium Bromide ◽  
New Antibiotics ◽  
Conventional Antibiotics

Antibiotic-resistant and biofilm-forming bacteria have surprisingly increased over recent years. On the contrary, the rate of development of new antibiotics to treat these emerging superbugs is very slow. Therefore, the aim of this study was to prepare novel nanobiotic formulations to improve the antimicrobial activity of three antibiotics (linezolid, doxycycline, and clindamycin) against Staphylococci. Antibiotics were formulated as nanoemulsions and evaluated for their antimicrobial activities and cytotoxicities. Cytotoxicity of the conventional antibiotics and nanobiotics was analyzed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on rat hepatocytes. Half-maximal inhibitory concentration (IC50) was estimated from an experimentally derived dose-response curve for each concentration using GraphPad Prism software. Upon quantitative assessment of Staphylococcus biofilm formation, eighty-four isolates (66.14 %) were biofilm forming. Linezolid and doxycycline nanobiotics exhibited promising antibacterial activities. On the contrary, clindamycin nanobiotic exhibited poor antibacterial activity. Minimum biofilm inhibitory concentrations showed that 73.68 %, 45.6%, and 5.2% of isolates were sensitive to linezolid, doxycycline, and clindamycin nanobiotics, respectively. Results of this study revealed that antibiotics loaded in nanosystems had a higher antimicrobial activity and lower cytotoxicities as compared to those of conventional free antibiotics, indicating their potential therapeutic values.

scholarly journals Nanostructure, Self-Assembly, Mechanical Properties, and Antioxidant Activity of a Lupin-Derived Peptide Hydrogel

Biomedicines ◽  
2021 ◽  
Vol 9 (3) ◽  
pp. 294
Author(s):  
Raffaele Pugliese ◽  
Anna Arnoldi ◽  
Carmen Lammi
Keyword(s):  
Mechanical Properties ◽  
Antioxidant Activity ◽  
Self Assembly ◽  
Antioxidant Activities ◽  
Functional Materials ◽  
Cd Spectroscopy ◽  
Beneficial Effects ◽  
Naturally Occurring ◽  
New Research ◽  
Peptide Hydrogel

Naturally occurring food peptides are frequently used in the life sciences due to their beneficial effects through their impact on specific biochemical pathways. Furthermore, they are often leveraged for applications in areas as diverse as bioengineering, medicine, agriculture, and even fashion. However, progress toward understanding their self-assembling properties as functional materials are often hindered by their long aromatic and charged residue-enriched sequences encrypted in the parent protein sequence. In this study, we elucidate the nanostructure and the hierarchical self-assembly propensity of a lupin-derived peptide which belongs to the α-conglutin (11S globulin, legumin-like protein), with a straightforward N-terminal biotinylated oligoglycine tag-based methodology for controlling the nanostructures, biomechanics, and biological features. Extensive characterization was performed via Circular Dichroism (CD) spectroscopy, Fourier Transform Infrared spectroscopy (FT-IR), rheological measurements, and Atomic Force Microscopy (AFM) analyses. By using the biotin tag, we obtained a thixotropic lupin-derived peptide hydrogel (named BT13) with tunable mechanical properties (from 2 to 11 kPa), without impairing its spontaneous formation of β-sheet secondary structures. Lastly, we demonstrated that this hydrogel has antioxidant activity. Altogether, our findings address multiple challenges associated with the development of naturally occurring food peptide-based hydrogels, offering a new tool to both fine tune the mechanical properties and tailor the antioxidant activities, providing new research directions across food chemistry, biochemistry, and bioengineering.

scholarly journals Rhamnolipids Nano-Micelles as a Potential Hand Sanitizer

Antibiotics ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 751
Author(s):  
Marwa Reda Bakkar ◽  
Ahmed Hassan Ibrahim Faraag ◽  
Elham R. S. Soliman ◽  
Manar S. Fouda ◽  
Amir Mahfouz Mokhtar Sarguos ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Active Sites ◽  
Specific Interaction ◽  
Virus Transmission ◽  
Multidrug Resistant ◽  
Future Perspective ◽  
Resistant Bacteria ◽  
In Silico Studies

COVID-19 is a pandemic disease caused by the SARS-CoV-2, which continues to cause global health and economic problems since emerging in China in late 2019. Until now, there are no standard antiviral treatments. Thus, several strategies were adopted to minimize virus transmission, such as social distancing, face covering protection and hand hygiene. Rhamnolipids are glycolipids produced formally by Pseudomonas aeruginosa and as biosurfactants, they were shown to have broad antimicrobial activity. In this study, we investigated the antimicrobial activity of rhamnolipids against selected multidrug resistant bacteria and SARS-CoV-2. Rhamnolipids were produced by growing Pseudomonas aeruginosa strain LeS3 in a new medium formulated from chicken carcass soup. The isolated rhamnolipids were characterized for their molecular composition, formulated into nano-micelles, and the antibacterial activity of the nano-micelles was demonstrated in vitro against both Gram-negative and Gram-positive drug resistant bacteria. In silico studies docking rhamnolipids to structural and non-structural proteins of SARS-CoV-2 was also performed. We demonstrated the efficient and specific interaction of rhamnolipids with the active sites of these proteins. Additionally, the computational studies suggested that rhamnolipids have membrane permeability activity. Thus, the obtained results indicate that SARS-CoV-2 could be another target of rhamnolipids and could find utility in the fight against COVID-19, a future perspective to be considered.

scholarly journals Sulfaguanidine Hybrid with Some New Pyridine-2-One Derivatives: Design, Synthesis, and Antimicrobial Activity against Multidrug-Resistant Bacteria as Dual DNA Gyrase and DHFR Inhibitors

Antibiotics ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 162
Author(s):  
Ahmed Ragab ◽  
Sawsan A. Fouad ◽  
Ola A. Abu Ali ◽  
Entsar M. Ahmed ◽  
Abeer M. Ali ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Fungal Growth ◽  
Dna Gyrase ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Design Synthesis ◽  
Potent Inhibition ◽  
Ic50 Values ◽  
Dhfr Inhibitors ◽  
Positive Controls

Herein, a series of novel hybrid sulfaguanidine moieties, bearing 2-cyanoacrylamide 2a–d, pyridine-2-one 3–10, and 2-imino-2H-chromene-3-carboxamide 11, 12 derivatives, were synthesized, and their structure confirmed by spectral data and elemental analysis. All the synthesized compounds showed moderate to good antimicrobial activity against eight pathogens. The most promising six derivatives, 2a, 2b, 2d, 3a, 8, and 11, revealed to be best in inhibiting bacterial and fungal growth, thus showing bactericidal and fungicidal activity. These derivatives exhibited moderate to potent inhibition against DNA gyrase and DHFR enzymes, with three derivatives 2d, 3a, and 2a demonstrating inhibition of DNA gyrase, with IC50 values of 18.17–23.87 µM, and of DHFR, with IC50 values of 4.33–5.54 µM; their potency is near to that of the positive controls. Further, the six derivatives exhibited immunomodulatory potential and three derivatives, 2d, 8, and 11, were selected for further study and displayed an increase in spleen and thymus weight and enhanced the activation of CD4+ and CD8+ T lymphocytes. Finally, molecular docking and some AMED studies were performed.

Self-Assembly of Single Chain Janus Nanoparticles from Azobenzene-Containing Block Copolymers and Reversible Photoinduced Morphology Transition

2021 ◽  
Author(s):  
Wei Wen ◽  
Aihua Chen
Keyword(s):  
Block Copolymers ◽  
Experimental Research ◽  
Self Assembly ◽  
The Self ◽  
Single Chain ◽  
Morphology Transition ◽  
Janus Nanoparticles ◽  
Assembly Behavior

Self-assembly of amphiphilic single chain Janus nanoparticles (SCJNPs) is a novel and promising approach to fabricate assemblies with diversified morphologies. However, the experimental research of the self-assembly behavior of SCJNPs...

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