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Along with bright fluorescence in the near-IR range, heptamethine carbocyanine dyes possess affinity to cancer cells. Thus, these dyes could be utilized as fluorescent labels and vectors for drug delivery as covalent conjugates with cytotoxic compounds. To test the properties, structure-activity relationship, and scope of such conjugates, we synthesized drug-dye dyads of tricarbocyanine dyes with anthracycline drug daunorubicin. We used hydrophilic zwitterionic and hydrophobic positively charged benzoindoline-benzothiazole-based heptamethine dyes as terminal alkyne derivatives and N-acylated or oxime-linked daunorubicin as azido-derivatives. These two alkynes and two azides were coupled to each other by Cu-catalyzed Huisgen-Meldal-Sharpless cycloaddition (click reaction) to afford four conjugates. Molecules based on hydrophobic dyes possess submicromolar cytotoxicity to HCT116 cells. Cytotoxicity, cell penetration, intracellular distribution, apoptosis induction and the effect of antioxidants on toxicity were evaluated. The results show that the structure of the cyanine-anthracycline conjugate (hydrophilicity/hydrophobicity, charge, linker, attachment site) is important for its biological activity, thus, expansion of the chemical space of such conjugates could provide new molecular research tools for diagnostics and therapy.

Owing to the changes in the general ecological situation in Russia, livestock losses from ovine anaplasmosis have rapidly increased in recent years. The development of a vaccine against this disease is therefore all the more relevant. A continuous culture of tick cells could be used as an appropriate substrate for producing biomass of the pathogen of ovine anaplasmosis, Anaplasma ovis, for the purpose of manufacturing a cell-cultural inactivated vaccine. Such a continuous cell line of the tick Dermacentor marginatus, the definitive reservoir host of A. ovis, has been obtained by cultivation of homogenized tick eggs on a modified Leibovitz medium L15. The established cell line DM-77 has an undifferentiated phenotype: the cells are rounded, with large nuclei and well-visible nucleoli. By the end of the study, the cell line was passaged eight times and did not express signs of growth rate decrease. The duplication time was 2.8 ± 0.3 days for cultivation in a medium with 10% fetal serum at 32°C.

Davydov, A.S., Teoriya moleculyarnykh eksitonov (Theory of Molecular Excitons), Moscow: Nauka, 1968. Borisevich, Yu.E., Dokl. Akad. Nauk. SSSR, 1978, vol. 241, p. 743. Borisevich, Yu.E., Kuzmin, V.A., Mikhailenko, F.A., and Dyadyusha, G.G., Dokl. Akad. Nauk. SSSR, 1976, vol. 228, p. 375. Borisevich, Yu.E., Kuzmin, V.A., Dyadyusha, G.G., and Mikhailenko, F.A., Dokl. Akad. Nauk. SSSR, 1976, vol. 229, p. 131. Schaberle, F.A., Kuzmin, V.A., and Borissevitch, I.E., Biochim. Biophys. Acta, 2003, vol. 1621, part 2, p. 183. Murakami, L.S., Ferreira, L.P., Santos, J.S., Silva, R.S., Nomizo, A., Kuzmin V.A., and Borissevitch, I.E., Biochim. Biophys. Acta, 2015, vol. 1850, p. 1150. Jiao, L., Song, F., Cui, J., and Peng, X., Chem. Comm., 2018, vol. 54, p. 9198. Kuzmin, V.A., Tatikolov, A.S., and Borisevich, Y.E., Chem. Phys. Lett., 1978, vol. 53, p. 52. Kostyukov, A.A., Nekipelova, T.D., Borissevitch, I.E., and Kuzmin, V.A., High. Energy Chem., 2019, vol. 53, p. 87. Kostyukov, A.A., Nekipelova, T.D., Radchenko, A.S., Golovina, G.V., Klimovich, O.N., Shtil, A.A., Codograto, D.C.K., Goncalves, P.J., Pavanelli, A.L.S., Ferreira, L.P., Amado, A.M., Borissevitch, I.E., and Kuzmin, V.A., High. Energy Chem., 2017, vol. 51, p. 148. Radchenko, A.S., Kostyukov, A.A., Mestergazi, M.G., Borissevitch, I.E., and Kuzmin. V.A., 17th International Congress on Photobiology, Barcelona, Spain, August 25−30,2019, Book of Abstracts, p. 759. Download references Spectral measurements were carried out on the spectrophotometric complex of the Shared Facilities of Institute of Biochemical Physics, Russian Academy of Sciences. The study was supported by the Russian Scientific Foundation, agreement no. 18-13-00463. Correspondence to A. E. Egorov. Translated by T. Nekipelova Reprints and Permissions Egorov, A.E., Kostyukov, A.A., Nekipelova, T.D. et al. Photoreduction of the Triplet State of Biscarbocyanine Dye. High Energy Chem 54, 142–144 (2020). https://doi.org/10.1134/S001814392002006X Download citation Received: 26 September 2019 Revised: 26 September 2019 Accepted: 23 October 2019 Published: 25 March 2020 Issue Date: March 2020 DOI: https://doi.org/10.1134/S001814392002006X

The total of 54 patients with chronic periodontitis of different severity was tested using real-time PCR (Dentoflor kit). The group included 38 patients with chronic gastritis. For the first time, a higher prevalence of Treponema denticola in periodontium of males in comparison with females was demonstrated. The patients with chronic gastritis had more human genome DNA at their periodontium than healthy individuals. Non-parametric statistical analysis demonstrated high association of periodontium colonization with. T. forsythensis and T. denticola (but not Aggregatibacter actinomycetemcomitans, Porphyromonas gingivalis, and Prevotella intermedia) with the severity of the chronic periodontitis.

The work explores the molecular genetic features of anaplastic astrocytomas and oligodendrogliomas in a series of 43 cases. The mutational status was studied using domestic chemicals and reagent kits. We revealed clear genetic differences between astrocytic and oligodendroglial tumors and proposed an algorithm to study diagnostic and prognostic markers.Работа посвящена изучению молекулярно-генетических особенностей анапластических астроцитом и анапластических олигодендроглиом в серии из 43 наблюдений. Для изучения мутационного статуса использованы в том числе наборы реагентов и реактивов отечественного производства. Выявлены четкие генетические различия между астроцитарными и олигодендроглиальными опухолями и предложен алгоритм исследования диагностических и прогностических маркеров.

The paper describes a clinical case of atypical teratoid/rhabdoid tumor with preserved INI1 expression and SMARCA4 gene mutations in an 8-month-old girl. Genome-wide DNA methylation, hierarchical clustering, and next-generation sequencing were used to make a tumor diagnosis. However, BRG1 immunohistochemical examination may be recommended in the routine practice of diagnosis and study of childhood CNS malignant tumors.Представлено клиническое наблюдение атипической тератоидно-рабдоидной опухоли с сохранной экспрессией INI1 и мутациями гена SMARCA4 у 8-месячной девочки. Для диагностики опухоли использовали методы выявления структуры метилирования ДНК на уровне генома, иерархическое кластерирование и секвенирование нового поколения. Однако в рутинной практике диагностики и исследования детских злокачественных опухолей ЦНС может быть рекомендовано иммуногистохимическое исследование с BRG1.

The total of 54 patients with chronic periodontitis of different severity was tested using real-time PCR (Dentoflor kit). The group included 38 patients with chronic gastritis. For the first time, a higher prevalence of Treponema denticola in periodontium of males in comparison with females was demonstrated. The patients with chronic gastritis had more human genome DNA at their periodontium than healthy individuals. Non-parametric statistical analysis demonstrated high association of periodontium colonization with. T. forsythensis and T. denticola (but not Aggregatibacter actinomycetemcomitans, Porphyromonas gingivalis, and Prevotella intermedia) with the severity of the chronic periodontitis.

Biological material of 92 patients (18-85 years old) with different severity chronic periodontitis were analyzed for bacterial pathogen colonization by using Dentofol kit (DNA-technology, Moscow). The cohort included 70 individuals with chronic gastritis, 2 patients with gastric and duodenal ulceration and 20 individuals with no gastric/duodenal pathology. The tight- est association with severity of the chronic periodontitis in the analyzed sub-cohort with the chronic gastritis was found with the prevalence of a complex T. for sythensis/T. denticola. Key contribution of this complex to progression of periodon- titis in males of the eldest group (above 55) was hypothesized. This data essentially differ from published results of other research groups where T. forsythensis and T. denticola were never reported as the principal causative agents of the chronic periodonitis in the gender/age/combined pathology normalized cohorts.

Spectral, luminescent, and photochemical properties of 7,7,9-trimethyl-6,7-dihydrofuro[3,2-f]quinoline (FDHQ) have been studied in hexane, alcohols, and water. Unlike 1,2-dihydroquinolines without the furo substituent, the fluorescence quantum yields for FDHQ in water and methanol are high (0.4 and 0.2, respectively), thereby indicating a difference in routes of excitation energy degradation in these compounds. The regularities in the FDHQ phototransformations have been studied by steady-state photolysis. The composition and the yield of final products depend on the presence or absence of oxygen in the system to a higher extent than on the solvent nature. This indicates the participation of the triplet excited state in the photo-chemical reactions in oxygen-free systems.

Hydroxyapatite/calcium carbonate (CC) composite powders containing up to 50 wt % CO32−, have been prepared via precipitation from aqueous solutions. According to chemical analysis data, the CO32− content of the powders coincides with the intended one over the entire composition range studied. With increasing CO32− content, the specific surface area of the powders decreases because of the formation and growth of large needlelike CC crystals up to 1.5 μm in size. The addition of low-melting-point alkali carbonates to the starting powder mixture reduces the sintering temperature of the powders to below 720°C, thereby preventing the thermal decomposition of CC. The highest bending strength, up to 76 MPa, is offered by the materials with the lowest CC content, about 20 wt %, and an average crystal size of 100 nm. The solubility of the composites gradually increases with CC content. In vitro experiments with a human fibroblast model (MTT test) demonstrate that the composites have zero cytotoxicity.

New medical engineering processes for repair of human bone tissue damaged upon diseases or injury are based on implanting porous scaffolds made of bio� compatible materials with cultivated osteoforming cells into the defect site [1–5]. With time, this struc� ture is replaced by bone tissue formed de novo. Apart from biocompatibility with the body, the requirements to the scaffold material include also time coherence between the resorption and the formation of a new bone tissue. Materials based on calcium phosphates, especially hydroxyapatite (HA), which is analogous in the chemical and phase composition to the mineral component of bone tissue, is best suited for this pur� pose. However, HA is the calcium phosphate most resistant to resorption. The resorption kinetics can be controlled by introducing a second, more soluble phase to the HA. To this end, composite materials in the HA–tricalcium phosphate system were developed [4, 5]; however, these materials still suffer from a num�

Real-time quantitative PCR (Dentofl or kit) was used to detect DNA of periodontal pathogens in specimens from 92 patients with chronic periodontitis and from a control sample of 12 normal subjects. A bimodal distribution of patients by periodontium colonization with A. actinomycetemcomitans, P. gingivalis, P. intermedia, T. forsythensis, and T. denticola was demonstrated. A new approach to interpretation of the results of quantitative evaluation of periodontal pathogens, including the notion of pathological colonization level, led to classification of all cases with chronic generalized periodontitis into 3 groups: associated with A. actinomycetemcomitans, with T. forsythensis/T. denticola complex, and cases of uncertain genesis.

It is shown that reduction of the 6-methyl-1-(p-tolyl)-2,4-diphenylpyrimidinium cation proceeds in two one-electron stages. In the first stage, an unstable radical is formed, and in the second stage, an unstable anion. As a result of dehydrogenation of the radical, the anhydro base 6-methylene-1-p-tolyl-2,4-diphenyl-6H-pyrimidine is formed. Oxidation of this compound in a single one-electron stage forms an unstable cation radical, the hydrogenation of which leads to the original pyrimidinium cation. Data obtained by cyclic voltametry and electrosynthesis with subsequent identification of the products have shown that, the same as in the reaction with the hydroxide anion, the methyl-substituted pyrimidinium cation acts as a CH-acid.

It has been shown that recyclization of 4-acylmethyl-3-azapyrylium salts under the influence of primary amines affords 4-(β-hydrozystyryl)pyrimidinium salts, which, upon further heating with the amine, are recyclized to form 4-acylaminopyridinium salts. It has been established that nucleophilic attack of 6-acylmethyl-substituted 3-azapyrylium salts in aqueous NaOH solution leads to functionally substituted pyridines. By means of MNDO quantum-chemical calculations with an accounting for solvation effects, in a continuum model, it has been shown that two directions of nucleophilic attack of the azapyrylium ring — at positions 2 and 6 — are equally probable.

We compared efficacy of combined treatment of males with anogenital warts given intramuscular cycloferon or cycloferon electrophoresis. Patients with manifest HPV infection (n=107) were divided into two groups. Group 1 (n=72) received intramuscular cycloferon (2 ml 12.5% solution each other day for 10 days), group 2 (n=35) received cycloferon electrophoresis on genital region (2 ml 12.5% solution daily in 1-2 days, 5 injections). Measurements were made of local cytokines in urethral secretion, IFN-alpha, IFN-gamma, lactoferrin, sexual hormones (estradiol and testosterone) in blood serum before and after treatment. Focal immunophysiotherapy with cycloferon in combined treatment of males with anogenital warts vs intramuscular cycloferon treatment reduces recurrence rate 2 times, has no negative effect on serum level of sexual hormones, a course dose and duration of immunotherapy decreased 2-fold, is well tolerated, is not painful. Cycloferon electrophoresis has a more potent effect on improvement of local immunity. Thus, local immunophysiotherapy with cycloferon can be a method of choice in the treatment of manifest HPV infection in males.

It is shown that reduction of the 6-methyl-1-(p-tolyl)-2,4-diphenylpyrimidinium cation proceeds in two one-electron stages. In the first stage, an unstable radical is formed, and in the second stage, an unstable anion. As a result of dehydrogenation of the radical, the anhydro base 6-methylene-1-p-tolyl-2,4-diphenyl-6H-pyrimidine is formed. Oxidation of this compound in a single one-electron stage forms an unstable cation radical, the hydrogenation of which leads to the original pyrimidinium cation. Data obtained by cyclic voltametry and electrosynthesis with subsequent identification of the products have shown that, the same as in the reaction with the hydroxide anion, the methyl-substituted pyrimidinium cation acts as a CH-acid.

It has been found that aceto- and benzonitriles and 3,4-dimethoxyphenylacetone in the presence of acetylperchlorate or upon heating in polyphosphoric acid or polyphosphoric ester form the corresponding isoquinoline. The data indicate that the reaction proceeds like a typical Ritter reaction and is defined by electrophilic activation of the carbonyl group of the ketone and the nucleophilicity of the nitrile. This methodology gave the alkaloid dioxyline (dimoxyline), obtained in high yield by the use of benzoylhexachloroantimonate.

Under the influence of DMF/Ac2O 2,4-diphenyl-6-methyl-3-azapyrylium perchlorates undergo condensation to give pyrido[1,2-c]pyrimidinium perchlorates. The structure of one of the perchlorates was proved by x-ray diffraction analysis.

4-Alkyl-3-azapyrylium salts undergo acylation at the alkyl group under acid-catalyzed conditions to give 4-acylmethyl-3-azapyrylium derivatives, which upon heating in proton-donating solvents recyclize to give 4-acylaminopyrylium salts.

Cerebral hemodynamics has been studied rheoencephalographically in 39 infants early in the course of complicated pneumonia and in 19 healthy controls. The former exhibited phasic changes in cerebral circulation. On the disease day 3 and 10, a significant reduction in the blood flow took place. In children under 6 months of age cerebral circulation is less active than in those over 6 months throughout the whole acute period of complicated pneumonia.

Blood rheology was assessed in 23 infants with acute pneumonia complicated with respiratory infectious toxicosis during hospitalization to intensive care wards, a control group consisted of 19 healthy infants. Plasma viscosity, red cell deformability, surface architectonics, and aggregation were studied. Patients developed increased plasma viscosity, marked reduction of red cell deformability, and increased aggregation index parallelled by reduced rate of aggregate formation. Changed red cell surface architectonics was associated with a reduced count of discocytes and parallel increase of echinocytes and cupola-like red cell forms. These data evidence marked disorders of blood rheology which should be not disregarded when choosing therapeutic policy.

Study of red cell surface structure is a highly informative method for the assessment of the body status in health and disease. The authors have examined the surface red cell structure of infants in health and disease by phase-contrast and scanning electron microscopy and came to the conclusion on the high reliability of the data obtained by phase-contrast microscopy. They recommend this unsophisticated and informative method for clinical practice.