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Medicinal leads that are also compatible with imaging technologies are attractive, as they facilitate the development of therapeutics through direct mechanistic observations at the molecular level. In this context, the uptake and antimicrobial activities of several luminescent dinuclear Ru complexes against E. coli were assessed and compared to results obtained for another ESKAPE pathogen, the Gram-positive major opportunistic pathogen Enterococcus faecalis, V583. The most promising lead displays potent activity, particularly against the Gram-negative bacteria, and potency is retained in the uropathogenic multidrug resistant EC958 ST131 strain. Exploiting the inherent luminescent properties of this complex, super-resolution STED nanoscopy was used to image its initial localization at/in cellular membranes and its subsequent transfer to the cell poles. Membrane damage assays confirm that the complex disrupts the bacterial membrane structure before internalization. Mammalian cell culture and animal model studies indicate that the complex is not toxic to eukaryotes, even at concentrations that are several orders of magnitude higher than its minimum inhibitory concentration (MIC). Taken together, these results have identified a lead molecular architecture for hard-to-treat, multiresistant, Gram-negative bacteria, which displays activities that are already comparable to optimized natural product-based leads.
This article was published in the following journal.
Name: ACS nano
The potential of live-cell stimulated emission depletion (STED) nanoscopy has not yet been fully exploited. Currently, the main limitation is the small number of fluorophores and probes that can susta...
ε-Poly-l-lysine (PL) has high antimicrobial activity and a wide antimicrobial spectrum and is applied broadly in the food industry. However, PL may lose part of its activity in phosphate systems, whi...
Antimicrobial resistance is a global health problem with strong social and economic impacts. The development of new antimicrobial agents is considered an urgent challenge. In this regard, antimicrobia...
Legumain, a lysosomal cysteine protease, is critical for pathological progression and has been found to play an important role in the occurrence and development of several cancers. However, its biolog...
In this study, antimicrobial activities of two different samples of L. from Turkey (TR) (Taşköprü, Kastamonu, Turkey) and China (CN) were determined. A broad spectrum of Gram-negative and Gram-pos...
Patient perception of pain on periodontal probing using a controlled-force, electronic probe was not significantly affected by the use of a modified (ball-end) probe tip design except for ...
The purpose of this study is to assess the surface cutaneous antimicrobial activity of IV Clear™ Dressing, Tegaderm CHG™ Dressing and a Silicone Vehicle Control Dressing.
Antimicrobial resistance is one of the greatest threats to human health, and is driven by inappropriate antimicrobial use. Antimicrobial stewardship programs (ASPs) improve the use of anti...
This is a four-year study, funded by the Center for Disease Control and Prevention, related to antimicrobial resistance in rural communities. The project consists of four components: A) ...
Antimicrobial resistance is one of today's most urgent public health problems. One of the most important strategies to slow the spread of antimicrobial resistance is the promotion of judic...
Any of a variety of procedures which use biomolecular probes to measure the presence or concentration of biological molecules, biological structures, microorganisms, etc., by translating a biochemical interaction at the probe surface into a quantifiable physical signal.
Complex pharmaceutical substances, preparations, or agents of organic origin, usually obtained by biological methods or assay. They are used especially in diagnosis and treatment of disease (as vaccines or pollen extracts). Biological products are differentiated from BIOLOGICAL FACTORS in that the latter are compounds with biological or physiological activity made by living organisms. (From Webster's 3d ed)
A type of scanning probe microscopy in which a probe systematically rides across the surface of a sample being scanned in a raster pattern. The vertical position is recorded as a spring attached to the probe rises and falls in response to peaks and valleys on the surface. These deflections produce a topographic map of the sample.
The natural bactericidal property of BLOOD due to normally occurring antibacterial substances such as beta lysin, leukin, etc. This activity needs to be distinguished from the bactericidal activity contained in a patient's serum as a result of antimicrobial therapy, which is measured by a SERUM BACTERICIDAL TEST.
A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.
Biological therapy involves the use of living organisms, substances derived from living organisms, or laboratory-produced versions of such substances to treat disease. Some biological therapies for cancer use vaccines or bacteria to stimulate the body&rs...