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Tony Velkov et al.
Cell chemical biology, 25(4), 380-391 (2018-02-06)
Resistance to the last-resort antibiotic colistin is now widespread and new therapeutics are urgently required. We report the first in toto chemical synthesis and pre-clinical evaluation of octapeptins, a class of lipopeptides structurally related to colistin. The octapeptin biosynthetic cluster consisted
Angelo Frei et al.
Chemical science, 11(10), 2627-2639 (2020-03-25)
There is a dire need for new antimicrobial compounds to combat the growing threat of widespread antibiotic resistance. With a currently very scarce drug pipeline, consisting mostly of derivatives of known antibiotics, new classes of antibiotics are urgently required. Metal
Sergii Demchenko et al.
Molecules (Basel, Switzerland), 26(14) (2021-07-25)
A series of novel 3-aryl-5H-pyrrolo[1,2-a]imidazole and 5H-imidazo[1,2-a]azepine quaternary salts were synthesized in 58-85% yields via the reaction of 3-aryl-6, 7-dihydro-5H-pyrrolo[1,2-a]imidazoles or 3-aryl-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepines and various alkylating reagents. All compounds were characterized by 1H NMR, 13C NMR, and LC-MS. The conducted screening
David J Tennent et al.
Journal of orthopaedic trauma, 30(10), 531-537 (2016-04-29)
To evaluate the effectiveness of locally applied vancomycin powder at different times postinfection in a contaminated traumatic animal model. This study used an established segmental defect rat femur model contaminated with Staphylococcus aureus UAMS-1 followed by treatment at 6 or
Marie Boegh et al.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 95(Pt A), 136-143 (2015-01-28)
The mucus lining of the gastrointestinal tract epithelium is recognized as a barrier to efficient oral drug delivery. Recently, a new in vitro model for assessment of drug permeation across intestinal mucosa was established by applying a biosimilar mucus matrix
Mia M Kiamco et al.
Biotechnology and bioengineering, 115(6), 1594-1603 (2018-02-21)
Biofilms alter their metabolism in response to environmental stress. This study explores the effect of a hyperosmotic agent-antibiotic treatment on the metabolism of Staphylococcus aureus biofilms through the use of nuclear magnetic resonance (NMR) techniques. To determine the metabolic activity
Roya Sheybani et al.
Biosensors & bioelectronics, 92, 425-433 (2016-11-15)
Wound infections are a critical healthcare concern worldwide. Rapid and effective antibiotic treatments that can mitigate infection severity and prevent the spread of antibiotic resistance are contingent upon timely infection detection. In this work, dual electrochemical pH and cell-attachment sensor
Chien-Lin Pan et al.
Acta biomaterialia, 47, 159-169 (2016-10-08)
Many non-antibiotic strategies, such as photocatalysis and photodynamic therapy, have been proposed to inhibit and/or kill bacteria. However, these approaches still have drawbacks such as insufficient bacterial specificity and the limited penetration depth of ultraviolet and near-infrared light. To overcome
Mu Cheng et al.
Antimicrobial agents and chemotherapy, 58(11), 6819-6827 (2014-09-04)
Ramoplanin is an actinomycetes-derived antibiotic with broad-spectrum activity against Gram-positive bacteria that has been evaluated in clinical trials for the treatment of gastrointestinal vancomycin-resistant enterococci (VRE) and Clostridium difficile infections. Recent studies have proposed that ramoplanin binds to bacterial membranes
D Cacciari et al.
Redox report : communications in free radical research, 22(4), 166-175 (2016-04-16)
Sensitized photooxidation processes in the presence of natural pigments may provide an alternative to antibiotics degradation since these compounds are transparent to natural light irradiation, therefore, they can be degraded by the action of photosensitizers which absorb light and produce
Inês C Santos et al.
Journal of the American Society for Mass Spectrometry, 26(7), 1204-1212 (2015-04-03)
Described is a new method based on the concept of controlled band dispersion, achieved by hyphenating flow injection analysis with ESI-MS for noncovalent binding determinations. A continuous stirred tank reactor (CSTR) was used as a FIA device for exponential dilution
Olga Zalevskaya et al.
Antibiotics (Basel, Switzerland), 9(5) (2020-05-30)
In an era of multidrug-resistant bacterial infections overshadowed by a lack of innovation in the antimicrobial drug development pipeline, there has been a resurgence in multidisciplinary approaches aimed at tackling this global health problem. One such approach is to use
Jan Gessmann et al.
Tissue engineering. Part A, 24(9-10), 809-818 (2017-11-04)
Platelet-free blood plasma clots were loaded either with antibiotics (vancomycin, gentamicin, or linezolid) at concentrations of 5-300 μg/mL or with silver ions (silver acetate) at concentrations of 3.3-129 μg/mL. The release of antibiotics or silver from the clot matrix was analyzed after
Shuaidong Huo et al.
Nature chemistry, 13(2), 131-139 (2021-01-31)
Pharmaceutical drug therapy is often hindered by issues caused by poor drug selectivity, including unwanted side effects and drug resistance. Spatial and temporal control over drug activation in response to stimuli is a promising strategy to attenuate and circumvent these
Freija Van den Driessche et al.
International journal of antimicrobial agents, 49(3), 315-320 (2017-02-06)
Staphylococcus aureus biofilms are involved in a wide range of infections that are extremely difficult to treat with conventional antibiotic therapy. We aimed to identify potentiators of antibiotics against mature biofilms of S. aureus Mu50, a methicillin-resistant and vancomycin-intermediate-resistant strain.
Sergii Demchenko et al.
European journal of medicinal chemistry, 201, 112477-112477 (2020-07-04)
Novel 1-aryl-3-biphenyl-4-yl-3-hydroxy-2,5,6,7,8,9-hexahydro-3H-imidazo[1,2-a]azepin-1-ium bromides and their 2,5-dehydrogenated analogues were designed and synthesized using a reaction of aryl-(4,5,6,7-tetrahydro-3H-azepin-2-yl)-amines with 1-biphenyl-4-yl-2-bromoethanone. Among the 16 novel compounds 5 derivatives displayed in vitro antimicrobial activity; while three of them showed promising activity against Staphylococcus aureus, Cryptococcus
Ling Shen et al.
Frontiers in microbiology, 11, 856-856 (2020-06-18)
Six previously undescribed ophiobolin-type sesterterpenes, namely, bipolatoxins A-F (1-6); and one previously undescribed pimarane-type diterpene, namely, 1β-hydroxy momilactone A (7); together with three known compounds, namely, 25-hydroxyophiobolin I (8), ophiobolin I (9), and ophiobolin A lactone (10); were isolated and
Anna K Hiltunen et al.
Microorganisms, 7(12) (2019-11-24)
Medical device-associated staphylococcal infections are a common and challenging problem. However, detailed knowledge of staphylococcal biofilm dynamics on clinically relevant surfaces is still limited. In the present study, biofilm formation of the Staphylococcusaureus ATCC 25923 strain was studied on clinically
Aleksandra S Chikina et al.
Cell, 183(2), 411-428 (2020-09-25)
The colon is primarily responsible for absorbing fluids. It contains a large number of microorganisms including fungi, which are enriched in its distal segment. The colonic mucosa must therefore tightly regulate fluid influx to control absorption of fungal metabolites, which
Natalya Doroshenko et al.
Biomaterials science, 6(8), 2101-2109 (2018-06-09)
Microbial keratitis can arise from penetrating injuries to the cornea. Corneal trauma promotes bacterial attachment and biofilm growth, which decrease the effectiveness of antimicrobials against microbial keratitis. Improved therapeutic efficacy can be achieved by reducing microbial burden prior to antimicrobial
Rohitesh Kumar et al.
Magnetic resonance in chemistry : MRC, 54(11), 880-886 (2016-10-19)
Previous investigations of the aerial parts of the Australian plant Eremophila microtheca and Syzygium tierneyanum resulted in the isolation of the antimicrobial flavonoid jaceosidin (4) and 2',6'-dihydroxy-4'-methoxy-3',5'-dimethyl chalcone (7), respectively. In this current study, compounds 4 and 7 were derivatized
Jiankang Song et al.
Macromolecular bioscience, 15(7), 901-911 (2015-03-17)
In this study, we investigated the fundamental relationship between the physicochemical characteristics of antibiotics and the kinetics of their release from gelatin nanospheres. We observed that antibiotics of high molecular weight (colistin and vancomycin) were released in a sustained manner
Chetna Dhand et al.
Biomaterials, 138, 153-168 (2017-06-05)
There is a growing demand for durable advanced wound dressings for the management of persistent infections after deep burn injuries. Herein, we demonstrated the preparation of durable antimicrobial nanofiber mats, by taking advantage of strong interfacial interactions between polyhydroxy antibiotics
Karren D Beattie et al.
Phytochemistry, 124, 79-85 (2016-01-09)
Eighteen natural products sourced from Australian micro- or macro-fungi were screened for antibacterial and antifungal activity. This focused library was comprised of caprolactams, polyamines, quinones, and polyketides, with additional large-scale isolation studies undertaken in order to resupply previously identified compounds.
Chetna Dhand et al.
ACS applied materials & interfaces, 8(47), 32266-32281 (2016-11-02)
Electrospinning of naturally occurring biopolymers for biological applications requires postspinning cross-linking for endurance in protease-rich microenvironments and prevention of rapid dissolution. The most commonly used cross-linkers often generate cytotoxic byproducts, which necessitate high concentrations or time-consuming procedures. Herein, we report
Shihao Wen et al.
Materials science & engineering. C, Materials for biological applications, 100, 514-522 (2019-04-06)
Acute wounds are worldwide problems affecting millions of people and causing heavy economic burden to national healthcare systems. Herein, we describe novel wound dressing materials relying on core/shell electrospun mats incorporated with flurbiprofen and vancomycin for achieving programmable release of
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