Vol 62, No 5-6 (2017)
View or download the full issue
PDF
ORIGINAL PAPERS
3-11 442
Abstract
Novel compounds among 3,4-disubstituted maleimlde derivatives that reveal a pronounced antimicrobial activity in vitro against Gram-positive bacteria, yeast Candida albicans, and fungi Aspergillus niger were obtained through total chemical synthesis. All these derivatives were simultaneously inactive against Gram-negative bacteria Escherichia coli, indicating the specific nature of their antimicrobial action. A number of derivatives appeared to be active in Halobacterium salinarum test system, which is used for selecting biologically active compounds among sterol biosynthesis inhibitors and antitumor antibiotics. This data suggests that such derivatives seem to have potential antitumor properties. The most active compounds were 3-bromo-4-thioaryl and 3,4-bisthioaryl maleimides, which are related to a new type of chemical compounds, that are promising for further elaboration and development of new antimicrobial and antitumordrugs on their basis.
12-20 1700
Abstract
A study of the protective activity of the Sage-leaved Rockrose extract (Cistus salviifolius) and the biologically active additive Forcys in the MDCK cell culture and on the model of lethal influenza pneumonia in white mice was carried out.The studied extract inhibited the reproduction of all used influenza viruses. The most sensitive to it were the viruses A/California/07/09 (H1N1)pdm09, A/mallard/Pennsylvania/10218/84 (H5N2), and A/Vladivostok/02/09 (H1N1). The IC50 values of the listed viruses were 0.5, 0.5, and 0.4 μg/ml, and the selectivity indexes were 382, 382, and 478, respectively, which is characteristic for preparations with high antiviral activity. Type B influenza viruses were less sensitive to the extract.The inhibitory activity of the extract did not depend on the susceptibility or resistance of the viruses to the anti-influenza drugs used, oseltamivir and rimantadine. The reduction in specific mortality with influenza pneumonia in animals was 40% compared with the placebo group.The use of the biologically active supplement Forcys did not affect the infectious activity of the influenza virus in the tissues of the animals lungs and led to a moderate limitation of the degree of damage to lung tissue. The maximum effectiveness of the biologically active supplement Forcys was achieved with the therapeutic and prophylactic regimens of its use.
21-25 746
Abstract
The study examined the qualitative and the quantitative composition of the cavitary and parietal microflora of the small intestine under the influence of ceftriaxone in the monthly experiment on animals. The study was carried out on Wistar rats, divided into two groups. Control group (n=50) - animals were injected intramuscularly with a 1.0 ml physiological solution daily for 10 days. Experimental group (n=50) - animals were injected intramuscularly with ceftriaxone 15 mg/kg/day, daily for 10 days. Intestinal contents from the distal third of the small intestine were sent for a bacteriological study. The investigated material was inoculated on nutrient media to isolate nonfermenting gram-negative bacteria (NGNB, including pseudomonads), enterobacteria, bifidobacteria, lactobacilli, clostridia, escherichia, enterococci, staphylococci, yeast-like fungi. Antibacterial therapy with ceftriaxone causes more pronounced changes in the parietal microflora of the small intestine. After a course of antibacterial therapy, the cavitary microflora is restored faster than the parietal microflora (in particular, the amount of bifido- and lactobacilli). An increase in the incidence of E.coli with typical enzymatic properties in the small intestine (up to 103-105 cfu/g) has been revealed, especially in the parietal microflora. Ceftriaxone leads to a quantitative increase in opportunistic enterobacteria and non-fermenting gramnegative bacteria after the course of antibiotic therapy.
GUIDELINES FOR PRACTITIONERS
26-34 318
Abstract
The aim of this study was to determine the prevalent path of extended spectrum beta-lactamase (ESBL) producing Enterobacteriaceae transmission in hematological patients. Methods. Prospective study was performed from 2013 to 2015 and included cases of bacteremia caused by Enterobacteriaceae. Rectal swabs were taken within the first three days after positive blood culture. ESBL-production was confirmed by phenotypic tests. The genes of blaTEM, blaSHV and blaCTX-M were determined by PCR. Genotyping was performed by ERIC-PCR. Results. A total of 91 enterobacteria isolates (56% - E.coli, 26% - K.pneumoniae, 18% - other) derived from blood were obtained in 89 cases of bacteremia in 82 patients (median age - 50 years). Production of ESBL was found in 19 (21%) isolates (E.coli - n=11, K.pneumoniae n=8). Beta-lactamase CTX-M type was identified in 95% of isolates. Colonization of gut with the same species was detected in all 19 episodes of bacteremia caused by ESBL positive isolates and only in 8 (11%) of 72 episodes of bacteremia caused ESBL-negative isolates (P<0.0001). Genotyping of 19 ESBL producers from blood culture revealed a genetic identity of only two isolates of E.coli, taken from the same patient within two months. Genetically related isolates from blood and gut in the same patients were identified in 26% of the pairs. Conclusion. The endogenous path of infection caused by ESBL producing Enterobacteriaceae prevailed in patients with hematological malignancies.
35-42 384
Abstract
Introduction. Colonization of S.pneumoniae is considered as a factor in the spreading of pneumococcus in the population, and is a predictor of the development of pneumococcal infection. Vaccination against pneumococcal infection can significantly reduce the spread of S.pneumoniae and the number of carriers of invasive strains. The vaccination against pneumococcal infection in the Republic of Kazakhstan was carried out with a phased coverage throughout the country in the framework of the national program «Salamatty Kazakhstan» in 2011. Purpose. To characterize the nasopharyngeal carriage of S.pneumoniae in children under 2 years in two different regions of the country with different histories of immunization against pneumococcal infection. Methods. A prospective multicenter cross-sectional study was conducted in two cities - Almaty and Karaganda - for a two-year period. Nasopharyngeal samples were identified by microbiological and molecular/genetic methods, taking into account the vaccinal status of children. Results: During the study, 500 children from Almaty and 1000 children from Karaganda at the age of 2 years were examined. The prevalence of pneumococcal carriage in the first stage of the study was 15.6% in Almaty and 4.7% in Karaganda. In the second year of the study, the prevalence of pneumococcal carriage was 14.1% in Almaty and 17.6% in Karaganda. The most common serotypes in Almaty before the vaccination were: 13 - 12%, 6ABC - 8%, 15B/C - 8% and 17F - 8%, in Karaganda, where the vaccination was carried out for 2 years: 15V - 19%, 31 - 14, 3%, 38 - 14.3% and non-typed strains - 23.8%. At the second stage of the study, common serotypes in Almaty were: 15A - 11.1%, 39F - 11.1%, 22F - 8.3%, 31 - 8.3% and non-typed strains - 27.8%. The most frequently detected serotypes in Karaganda in 2016 were: 8 - 14.3%, 10F/10C/33C - 10.4%, 15B/C - 9.1% and non-typed strains - 23.4%. Discussion. The received data confirms the necessity of the monitoring measures within the framework of the current anti-pneumococcal vaccination.
43-53 665
Abstract
Objective: an array of special publications data extracted from reviewed scientific journals and concerning the efficacy of the Cycloferon drug in viral hepatitis B and C treatment. The aim of the work is a generalized evaluation of Cycloferon efficacy by comparison of the results (outcomes) of its use against the background of the basic therapy for acute and chronic hepatitis B and C. Heterogeneous groups’ design and the variability of clinical response parameters were considered. The database included information about 1856 patients. Generalized control group (n=898) received standard drug therapy (active placebo). Experimental group (n=958) additionally received cycloferon. All groups included children and adults with viral B and C hepatitis. The comparative analysis of formalized parameters of clinical efficacy of cycloferon (increase of the absolute and the relative benefits, odds ratio, NNT, etc.) in the treatment of acute and chronic viral hepatitis B and C in adults and children. The variability of the parameters made it difficult to unambiguously interpret the results, however, the combination of homogeneous comparison groups in the meta-analysis process increased the statistical power of the study and allowed to perform a general assessment of the clinical efficacy of the drug. It has been shown that the use of Cycloferon for the treatment and prophylaxis of viral hepatitis B and C in adults and children more than doubles the probability of complete remission and relapse of the disease (OR = 2.6 [2.4; 2.9], NNT = 6.7 [3.2; 9.8]).
54-62 381
Abstract
The article covers basic scales and tests used in clinical trials and medical practice for the assessment of the effectiveness of treatment of spasticity syndrome with preparations of botulinum toxin type A in children with cerebral palsy. The article gives the information about the recommended methods of assessment, suggests the scales that can be used in evaluation of the effectiveness, as well as carries out an analysis of their informativity and sensitivity.
DRUG STANDARDIZATION AND CONTROL
63-67 677
Abstract
The present article reviews the modern approaches for the standardization of synthetic pharmaceutical substances that are realized in the form of national pharmacopoeial standards - monographs published in State Pharmacopoeia of Russian Federation. The test parameters of pharmaceutical substances, the methods for their determination, and the applicable regulatory requirements involved in the pharmacopoeial monographs should be reproducible for every substance declared under the appropriate name.
REVIEWS
68-76 372
Abstract
Marine-derived fungi are a rich source of structurally diverse bioactive secondary metabolites which might be useful for drug design. Up to date, a lot of structurally and pharmacologically novel and interesting bioactive secondary metabolites have been isolated from marine-derived fungi. Some of them have high toxicity toward cancer cells, however they are also cytotoxic to normal cells. These compounds require structural modifications to decrease the toxicity and increase the antitumor activity. A large number of substances have antibacterial, antifungal, anti-imflammatory and immunomodulatory activities.
ISSN 0235-2990 (Print)