An alternative approach for daily perineal care of patients with indwelling urinary catheterization: Photodynamic inactivation with cationic porphyrin derivatives

Background: Catheter-associated urinary tract infections (CAUTI) constitute a significant portion of healthcare-associated infections. Using antiseptic for routine daily perineal care of patients with IUC may reduce CAUTIs. Aim: This study aimed to examine antimicrobial photodynamic inactivation (aPDI) against clinical isolates for use in the daily perineal care of patients with IUC. In addition, it was also aimed to compare the antimicrobial activities of aPDI and 0.1% chlorhexidine gluconate. Methods:  In this in-vitro study, cationic porphyrin derivatives (CPDs) were used as photosensitizers in the experiments. CPDs, named PM, PE, PN, and PL were synthesized by the researchers. A diode laser device emitting light with a wavelength of 450 nm (blue light) was used as the light source. Methicillin-resistant Staphylococcus aureus (MRSA), Escherichia coli and Klebsiella pneumoniae with multidrug-resistant (MDR) properties and Candida albicans were used.  Photosensitizer (PS), aPDI, light (L), and control (C) groups in aPDI experiments; control (C) and chlorhexidine gluconate 0.1% groups were used in the chlorhexidine gluconate experiments. Survival was calculated based on CFU/mL in the control group. Results: In experiments, combinations of 25 J/cm² with 6.25 and 3.125 µM PM, PE reduced E. coli, K. pneumoniae, MRSA, and C. albicans survival in the range of 8.70 to 11.53 log₁₀. In aPDI experiments performed with 6.25 and 3.125 µM PN and PL concentrations at the same energy density, reductions in the range of 4.41 to 0.17 log₁₀ were observed in all four clinical isolates. In experiments where 1.5625 µM concentration was used, survival decreased in the range of 8.29 to 10.87 log₁₀ in PM and PE, while antimicrobial activity was limited in PN and PL. In the 0.1% chlorhexidine gluconate experiments, the survival reduction in all four clinical isolates ranged from 8.87 to 10.24 log₁₀. Conclusion: For PM and PE, a very strong aPDI was obtained in C. albicans, E.coli, K. pneumoniae, and MRSA at low concentrations and energy density. The same antimicrobial activity was found in experiments using 0.1% chlorhexidine gluconate. In this context, we would like to inform you that aPDI to be performed with a combination of 25 J/cm² at 6.25 and 3.125 µM concentrations of PM and PE has the potential to be an antiseptic in the daily perineal care of patients with IUC

Synthesis and Antimicrobial Activity of Some Pyridinium Salts

Some substituted benzylidenehydrazinylpyridinium derivatives bearing benzyl, ethylphenyl and propylphenyl groups on the pyridinium nitrogen were synthesized and screened for possible antibacterial and antifungal activities against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Candida albicans using the microdilution method. Antimicrobial test results indicated that compounds containing a 3-phenylpropyl chain displayed the highest antimicrobial activity against Staphylococcus aureus and the compound 3d was the most active in the series against all tested bacteria and fungi strains

The Trail, 1939-12-15

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A Novel Molecule: 1-(2,6 Dichlorobenzyl)-4-(2-(2-4-hydroxybenzylidene)hydrazinyl)pyridinium Chloride and its Interaction with DNA

Herein, a novel pyridine derivative, 1-(2,6 dichlorobenzyl)-4-(2-(2-4-hydroxybenzylidene)hydrazinyl)pyridinium chloride (DHPC), was synthesized as a candidate drug molecule. Interaction of DHPC with DNA was used to explore its effect on DNA via Differential Pulse Voltammetry, Cyclic Voltammetry, and Electrochemical Impedance Spectroscopy. We demonstrated that oxidation signal of guanine bases of DNA decreased significantly while that of DHPC increased after its interaction with one another. Our candidate drug molecule exhibits LOD and LOQ, e.g., 1.5 mu g/mL and 4.9 mu g/mL, respectively. Toxicity effect value for DHPC (S%) was calculated as %31, demonstrating the candidate drug molecule's toxic effect on DNA.Tekirdag Namik Kemal University [NKUBAP.00]; Izmir Katip Celebi UniversityIzmir Katip Celebi University [:2018-GAP-ECZF-0002]; TUBITAK-BIDEBTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [1929B011800172]We acknowledge partly financial support from Tekirdag Namik Kemal University (Project No:NKUBAP.00.GA.19.217) and Izmir Katip Celebi University (Project No:2018-GAP-ECZF-0002). Ayca Karasakal acknowledges TUBITAK-BIDEB (1929B011800172) for the support during her stay in Izmir Katip Celebi University

A Novel Molecule: 1‐(2,6 Dichlorobenzyl)‐4‐(2‐(2‐4‐hydroxybenzylidene)hydrazinyl)pyridinium Chloride and its Interaction with DNA

Herein, a novel pyridine derivative, 1-(2,6 dichlorobenzyl)-4-(2-(2-4-hydroxybenzylidene)hydrazinyl)pyridinium chloride (DHPC), was synthesized as a candidate drug molecule. Interaction of DHPC with DNA was used to explore its effect on DNA via Differential Pulse Voltammetry, Cyclic Voltammetry, and Electrochemical Impedance Spectroscopy. We demonstrated that oxidation signal of guanine bases of DNA decreased significantly while that of DHPC increased after its interaction with one another. Our candidate drug molecule exhibits LOD and LOQ, e.g., 1.5 mu g/mL and 4.9 mu g/mL, respectively. Toxicity effect value for DHPC (S%) was calculated as %31, demonstrating the candidate drug molecule's toxic effect on DNA.Tekirdag Namik Kemal University [NKUBAP.00]; Izmir Katip Celebi UniversityIzmir Katip Celebi University [:2018-GAP-ECZF-0002]; TUBITAK-BIDEBTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [1929B011800172]We acknowledge partly financial support from Tekirdag Namik Kemal University (Project No:NKUBAP.00.GA.19.217) and Izmir Katip Celebi University (Project No:2018-GAP-ECZF-0002). Ayca Karasakal acknowledges TUBITAK-BIDEB (1929B011800172) for the support during her stay in Izmir Katip Celebi University

Targeting acetylcholinesterase to treat neurodegeneration

WOS: 000243579000006PubMed ID: 17227232Neurodegenerative disorders, such as Alzheimer's disease, are often characterised by the degeneration of the cholinergic system. Thus, the aim of many treatment regimens is to support this system either by means of muscarinic agonists or by inhibitors of acetylcholinesterase (AChE), the latter being able to increase the concentration of acetylcholine. However, both pharmacological groups of drugs can only help in the beginning of the progressive disease. The finding that the occupation of the peripheral anionic site of AChE is able to stop the formation of the amyloid plaque led to the development of bivalent ligands that occupy both the active and the peripheral site. This dual action might be more beneficial for treatment of Alzheimer's disease than simple inhibition of the acetylcholine hydrolysis. Thus, the new bivalent ligands are the focus of this review