Synthesis and antimicrobial and toxic properties of novel 1,3-bis(alkyl)-6-methyluracil derivatives containing 1,2,3- and 1,2,4-triazolium fragments

Voloshina, Alexandra D.; Семенов, В. Э.; Strobykina, A. S.; Кулик, Н. В.; Krylova, E. S.; Зобов, В. В.; Резник, В. С.

doi:10.1134/s1068162017020170

Cited by 59 publications

(16 citation statements)

References 8 publications

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“…SRA and p(6SRA‐5B) were tested for their hemolytic activities against human red blood cells (hRBC) . Fresh hRBC with heparin were rinsed 3 times with PBS (35 mM phosphate buffer/0.15 M NaCl, pH 7.3) by centrifugation for 10 min at 800 g and resuspended in PBS.…”

Section: Methodsmentioning

confidence: 99%

“…SRA and p(6SRA-5B) were tested for their hemolytic activities against human red blood cells (hRBC). [44] Fresh hRBC with heparin were rinsed 3 times with PBS (35 mM phosphate buffer/0.15 M NaCl, pH 7.3) by centrifugation for 10 min at 800 g and resuspended in PBS. SRA (or p(6SRA-5B) dissolved in PBS (concentrations 0.12-0.6 mg/mL of SRA; 0.13-0.62 mg/mL of p(6SRA-5B)) were then added to 0.5 mL of a solution of the stock hRBC in PBS to reach a final volume of 5 mL (final erythrocyte concentration, 10 % v/v).…”

Section: Hemolysis Of Human Red Blood Cellsmentioning

confidence: 99%

“…The cytotoxic effect was determined on the Cytell Cell Imaging multifunctional system (GE Healthcare Life Science, Sweden) using the Cell Viability BioApp based on the fluorescence intensity. [44] A cell culture WI-38 VA 13 subline 2RA (human embryo lung) from the Collection of the Institute of Cytology RAS (St. Petersburg) was used. For the cultivation of cells, standard culture medium "Igla" produced by the Moscow Institute of Poliomyelitis and Viral Encephalitis named after M.P.…”

Section: Cytotoxicitymentioning

confidence: 99%

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A Glucose‐Responsive Polymer Nanocarrier Based on Sulfonated Resorcinarene for Controlled Insulin Delivery

et al. 2019

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A nanocarrier (p(6SRA‐5B)) for glucose‐controlled insulin delivery consists of sulfonated resorcinarenes (SRA) that are assembled into a spherical shell and are attached to each other with phenylboronate linkers. p(6SRA‐5B) is stable in water and blood plasma at normal glucose concentrations. At high glucose levels (>5 mM), p(6SRA‐5B) dissociates into SRA and phenylboronates through competitive interaction with excess glucose. Insulin was successfully encapsulated into the cavity of p(6SRA‐5B) and its release was investigated in water and blood plasma by NMR, UV, CD, and fluorescence spectroscopy. The results show that the dissociation of the nanocarrier and the insulin release occurs with an increase in glucose concentration. At 5 mM glucose, the nanocarrier is stable, and the insulin release does not exceed 10 %. Increasing the glucose concentration to 7.5–10 mM results in a 40–100 % insulin release. p(6SRA‐5B) is thus a promising insulin nanocarrier for the treatment of type 1 diabetes.

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Section: Methodsmentioning

confidence: 99%

Section: Hemolysis Of Human Red Blood Cellsmentioning

confidence: 99%

Section: Cytotoxicitymentioning

confidence: 99%

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A Glucose‐Responsive Polymer Nanocarrier Based on Sulfonated Resorcinarene for Controlled Insulin Delivery

et al. 2019

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“…In vitro antibacterial and antifungal activities of cationic surfactants and their compositions were evaluated against pathogenic representatives of Gram-positive bacteria Staphylococcus aureus АТСС 209p (Sa) and fungi Candida albicans NCTC 885-653 (Ca). Minimal inhibitory concentrations (MICs) were estimated by conventional dilution methods for bacteria and fungi [60]. The antibacterial and antifungal assays were performed in Hottinger broth (HiMe-dia Laboratories Pvt.…”

Section: Antibacterial and Antifungal Activitymentioning

confidence: 99%

Nontoxic antimicrobial micellar systems based on mono- and dicationic Dabco-surfactants and furazolidone: Structure-solubilization properties relationships

Pashirova

Burilova

Лукашенко

et al. 2019

Journal of Molecular Liquids

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Self-assembly and solubilization properties of amphiphilic mono-and bisquaternized derivatives of 1,4diazabicyclo[2.2.2]octane (mono-CS-n and di-CS-n, where CScationic surfactant, n = 12, 14, 16, 18) was investigated by nuclear magnetic resonance with magnetic field pulse gradient. The influence of Dabco-surfactant structure (head group and length of alkyl chains) on critical micelle concentration and aggregation number of micelles was studied. The CMC of mono-CS-n are lower than CMC of di-CS-n. The aggregation numbers of mono-CS-n micelles are higher than for di-CS-n micelles. The solubilization capacity of mono-CS-n is higher than di-CS-n. The solubilization capacity of mono-CS-16 is 2.5 times higher than CTAB in the case of Orange OT as a solute, and it is close to CTAB in the case of Sudan I. The solubility of a poorly water-soluble antibacterial drug furazolidone was improved by micellar solubilization based on mono-and di-Dabco-surfactants. Mono-CSn is the best solubilizing agents toward furazolidone. The use of mixed composition mono-Dabco-16-furazolidone provides a significant increase in antimicrobial activity (by 2 times against bacteria and 8 times against fungi) and reduces by 2 times the dose of each of the components in combination formulation and causes b2% haemolysis of human red blood cells at the active dose.

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“…The cytotoxicity determination is based on the analysis of fluorescence intensity. 18 The cell culture WI-38 VA 13 subline 2RA (human embryo lung) form the collection of the Institute of Cytology of Russian Academy of Sciences has been used for cytotoxicity evaluation. The standard nutrient medium 'Igla' with an addition of 10% of calf embryo serum and 1% of essential amino acids was applied for cell cultivation.…”

Section: 2i Cytotoxicity Evaluationmentioning

confidence: 99%

Silica-coated iron-oxide nanoparticles doped with Gd(III) complexes as potential double contrast agents for magnetic resonance imaging at different field strengths

et al. 2018

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In the present work, we have prepared the ∼10 nm superparamagnetic iron-oxide nanoparticles by means of high-temperature decomposition of iron oleate precursor. Then they were coated with silica shell to impart water-solubility and an ability to accommodate paramagnetic Gd(III)-based complexes inside silica coating. All of the prepared nanoparticles form stable in time aqueous dispersions and show good negative or/and positive contrasting effect at different magnetic field strengths (0.47, 1.41, 14.1 T). It has been also exemplified that the incorporation of [Gd(TCAS)] complexes into silica shell triggers a significant increase of the transverse relaxivity of the core-shell nanoparticles. The correlation between relaxometric properties and morphology of the obtained nanoparticles was revealed. The non-toxicity of the obtained nanoparticles along with their ability to shorten both transverse and longitudinal relaxation rates of water protons make them good candidates for their use as dual-mode contrast agents in MRI.

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Synthesis and antimicrobial and toxic properties of novel 1,3-bis(alkyl)-6-methyluracil derivatives containing 1,2,3- and 1,2,4-triazolium fragments

Cited by 59 publications

References 8 publications

A Glucose‐Responsive Polymer Nanocarrier Based on Sulfonated Resorcinarene for Controlled Insulin Delivery

A Glucose‐Responsive Polymer Nanocarrier Based on Sulfonated Resorcinarene for Controlled Insulin Delivery

Nontoxic antimicrobial micellar systems based on mono- and dicationic Dabco-surfactants and furazolidone: Structure-solubilization properties relationships

Silica-coated iron-oxide nanoparticles doped with Gd(III) complexes as potential double contrast agents for magnetic resonance imaging at different field strengths

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