The purposeful development of synthetic antibacterial compounds requires an understanding of the relationship between effects of compounds and their chemical structure. This knowledge can be obtained by studying changes in bacteria ultrastructure under the action of antibacterial compounds of a certain chemical structure. Our study was aimed at examination of ultrastructural changes in cells caused by polycationic amphiphile based on 1,4‒diazabicyclo[2.2.2]octane (DL12), ciprofloxacin and their hybrid (DLCip6); the samples were incubated for 15 and 45 min. DL12 first directly interacted with bacterial cell wall, damaging it, then penetrated into the cell and disrupted cytoplasm. Ciprofloxacin penetrated into cell without visually damaging the cell wall, but altered the cell membrane and cytoplasm, and inhibited the division of bacteria. The ultrastructural characteristics of cells damaged by the hybrid clearly differed from those under ciprofloxacin or DL12 action. Signs associated with ciprofloxacin predominated in cell damage patterns from the hybrid. We studied the effect of ciprofloxacin, DL12 and their hybrid on biofilm morphology using paraffin sections. Clear differences in compound effects on biofilm (45 min incubation) were observed. The results obtained allow us to recommend this simple and cheap approach for the initial assessment of antibiofilm properties of synthesized compounds.
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http://dx.doi.org/10.3390/microorganisms11092192 | DOI Listing |
Bioorg Med Chem Lett
April 2024
Department of Chemistry, Carleton University, 1125 Colonel By Drive, Ottawa, Ontario K1S 5B6, Canada; Institute of Biochemistry, Carleton University, 1125 Colonel By Drive, Ottawa, Ontario K1S 5B6, Canada. Electronic address:
Amphiphilic peptide sequences are conducive to secondary structures that self-assemble into higher-ordered peptide nanostructures. A select set of amphiphilic polycationic peptides displayed stable helical-coiled structures that self-assembled into peptide nanofibers. The progression of peptide fibril formation revealed short protofibrils that extended into thin filaments and into an entangled network of nanofibers over an extended (5 days) incubation period.
View Article and Find Full Text PDFPharmaceutics
August 2023
Institute of Chemical Biology and Fundamental Medicine SB RAS, Lavrentieva Ave. 8, 630090 Novosibirsk, Russia.
In this study, the impact of different delivery systems on the cytokine-inducing, antiproliferative, and antitumor activities of short immunostimulatory double-stranded RNA (isRNA) was investigated. The delivery systems, consisting of the polycationic amphiphile 1,26-bis(cholest-5-en-3-yloxycarbonylamino)-7,11,16,20 tetraazahexacosan tetrahydrochloride (2X3), and the lipid-helper dioleoylphosphatidylethanolamine (DOPE), were equipped with polyethylene glycol lipoconjugates differing in molecular weight and structure. The main findings of this work are as follows: (i) significant activation of MCP-1 and INF-α, β, and γ production in CBA mice occurs under the action of isRNA complexes with liposomes containing lipoconjugates with long PEG chains, while activation of MCP-1 and INF-γ, but not INF-α or β, was observed under the action of isRNA lipoplexes containing lipoconjugates with short PEG chains; (ii) a pronounced antiproliferative effect on B16 melanoma cells in vitro, as well as an antitumor and hepatoprotective effect in vivo, was induced by isRNA pre-complexes with non-pegylated liposomes, while complexes containing lipoconjugates with long-chain liposomes were inactive; (iii) the antitumor activity of isRNA correlated with the efficiency of its accumulation in the cells and did not explicitly depend on the activation of cytokine and interferon production.
View Article and Find Full Text PDFMicroorganisms
August 2023
Institute of Chemical Biology and Fundamental Medicine, Siberian Branch of Russian Academy of Science, Lavrent'ev av., 8, 630090 Novosibirsk, Russia.
The purposeful development of synthetic antibacterial compounds requires an understanding of the relationship between effects of compounds and their chemical structure. This knowledge can be obtained by studying changes in bacteria ultrastructure under the action of antibacterial compounds of a certain chemical structure. Our study was aimed at examination of ultrastructural changes in cells caused by polycationic amphiphile based on 1,4‒diazabicyclo[2.
View Article and Find Full Text PDFRuss J Bioorg Chem
May 2023
Lomonosov Institute of Fine Chemical Technologies, MIREA-Russian Technological University, 119571 Moscow, Russia.
Some new polycationic amphiphiles containing a disulfide group were synthesized. Cationic liposomes formed from the compounds synthesized and a helper lipid 1,2-dioleoyl--glycero-3-phosphatidylethanolamine were not toxic for HEK293 and HeLa cells and were highly effective when delivering a fluorescently labeled oligodeoxyribonucleotide. The efficacy of plasmid DNA delivery depended on the cell line and the amphiphile structure, liposomes based on tetracationic amphiphiles being the most effective transfectants.
View Article and Find Full Text PDFiScience
March 2023
BTSB-UR 7417, Université de Toulouse, Institut National Universitaire Jean-François Champollion, Place de Verdun, 81000 Albi, France.
Hymenopterans represent one of the most abundant groups of venomous organisms but remain little explored due to the difficult access to their venom. The development of proteo-transcriptomic allowed us to explore diversity of their toxins offering interesting perspectives to identify new biological active peptides. This study focuses on U function, a linear, amphiphilic and polycationic peptide isolated from ant venom.
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