N. Hula, A. Chumak, A. Berdyshev, G. V. Kosiakova, T. M. Goridko, O. F. Meged', V. S. Asmolkova, Yu. I. Porva, S. Rybalko, S. T. Dyadun, D. Starosyla, O. Deryabin
{"title":"N-stearoylethanolamine - a new inhibitor of the hepatitis C virus reproduction","authors":"N. Hula, A. Chumak, A. Berdyshev, G. V. Kosiakova, T. M. Goridko, O. F. Meged', V. S. Asmolkova, Yu. I. Porva, S. Rybalko, S. T. Dyadun, D. Starosyla, O. Deryabin","doi":"10.7124/bc.000a54","DOIUrl":"https://doi.org/10.7124/bc.000a54","url":null,"abstract":"Aim. The study of the effect of endogenous cannabimimetic compound - N-stearoylethanolamine (NSE) on the hepatitis C virus (HCV) reproduction. Methods. The model of the surrogate HCV is a bovine diarrhea virus; cell culture model is cells transfected with cDNA of the human HCV and molecular docking has been used. Results. In vitro studies showed that NSE effectively inhibited the reproduction of a surrogate HCV in both MDBK cells and transfected Jurkat cells. Molecular docking suggested that NSE can bind to the active centers of both NS3 serine protease and HCV NS5B-polymerase and has an inhibitory effect on their activity. Conclusions. The obtained data confirm that using NSE is promising for the develop-ment","PeriodicalId":39444,"journal":{"name":"Biopolymers and Cell","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49079331","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Changes in the human placental transcriptome during the physiological course of pregnancy","authors":"O. Lykhenko, A. Frolova, M. Obolenskaya","doi":"10.7124/BC.000A4D","DOIUrl":"https://doi.org/10.7124/BC.000A4D","url":null,"abstract":"Аim . To determine the chan ges of gene expression in human placenta during the physiological course of pregnancy. Methods the integrative analysis of publicly available data. Results. We have revealed that between the first and second trimesters of gestation the main changes relate to immune processes, morphogenesis and intercellular communication through the surface receptors of the cellular membrane. In the interval between the second and third trimesters, the main changes concern the regulation of the response to external stimuli, metabolic processes, morphogenesis of individual tissues, regulation of signaling pathways via transmembrane serine / threonine protein kinase receptors. Conclusion. The changes in gene expression in human placenta in the course of physiological gestation will serve as a reliable control with the changes during the pathological course of gestation.","PeriodicalId":39444,"journal":{"name":"Biopolymers and Cell","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-02-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49657679","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
M. Protopopov, V. Vdovin, S. S. Lukashov, O. V. Ostrynska, I. Borysenko, O. Borovykov, S. Starosyla, Y. Bilokin, O. P. Kukharenko, V. Bdzhola, S. Yarmoluk
{"title":"Evaluation of in vitro activity and SAR study of the novel hetarylamino-3-aryl-1H-indazole derivatives as inhibitors of protein kinase CK2","authors":"M. Protopopov, V. Vdovin, S. S. Lukashov, O. V. Ostrynska, I. Borysenko, O. Borovykov, S. Starosyla, Y. Bilokin, O. P. Kukharenko, V. Bdzhola, S. Yarmoluk","doi":"10.7124/BC.000A4C","DOIUrl":"https://doi.org/10.7124/BC.000A4C","url":null,"abstract":"Aim. To identify novel protein kinase CK2 inhibitors among the 5-hetarylamino-1H-indazoles. Methods. Biochemical testing was carried out with the aid of γ- 32 P ATP in vitro kinase assay. Molecular docking via the Autodock 4.2.6 program package was executed, rescoring of docking results was performed using DrugScore scoring function. Results. Among the 17 studied 5-amino-3-arylindazole derivatives 11 inhibitors of protein kinase CK2 with IC 50 in nanomolar range were identified. The most active compound has IC 50 = 2 nM. SAR study and addi-tional molecular modeling of these compounds allowed us to select prospective substituents for construction of novel compounds with improved activity and physicochemical properties. Conclusions. As a result of this work 11 nanomolar protein kinase CK2 inhibitors were de-veloped and the binding modes of these compounds with the ATP-acceptor site were proposed using molecular docking methods. The physicochemical properties and SAR of substituents of studied compounds were analyzed and 6 novel compounds were designed for further development as protein kinase CK2 inhibitors. Summarizing, 5-heterylamino-1H-indazoles are a good basis for further CK2 inhibitors development.","PeriodicalId":39444,"journal":{"name":"Biopolymers and Cell","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-02-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46812230","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
O. Mankovska, A. Korsakova, K. Cherniavskyi, O. Kononenko, E. O. Stakhovskyy, Y. Bondarenko, V. Kashuba, G. Gerashchenko
{"title":"Methylation pattern of tumor-suppressor gene promoters as putative noninvasive diagnostic markers for prostate cancer","authors":"O. Mankovska, A. Korsakova, K. Cherniavskyi, O. Kononenko, E. O. Stakhovskyy, Y. Bondarenko, V. Kashuba, G. Gerashchenko","doi":"10.7124/BC.000A49","DOIUrl":"https://doi.org/10.7124/BC.000A49","url":null,"abstract":"Aim. To assess the rate of promoter methylation of putative TSGs for PCa in tumor tissue and in urine of PCa patients for better understanding of regulation of gene expression upon the PCa development and to evaluate the possibility to use the data on TSGs’ methylation for the development of noninvasive PCa markers. Methods. A quantitative methyl-specific PCR (qMSP) was used for the analysis of a methylation rate in prostate tissues and cell lines, and an ordinary MSP was performed for the study of urine samples. Results. We found that the RASSF1A promoter demonstrated a higher methylation rate in the TMPRSS2:ERG fusion positive PCa. The methylation of NKX3.1, PTEN and RASSF1A in DNA from urine was more common for cancer patients than for healthy donors. The promoters of CDH1 and GDF15 were methylated more frequently in PCa patients, than in patients with inflammatory disease. Conclusions. The abovementioned five genes can form a panel for early non-invasive detection of PCa. This set can be combined with the detection of the TMPRSS2:ERG fusion transcript. More work should be done to understand the molecular mechanisms explaining the functional role of promoter methylation of the selected genes.","PeriodicalId":39444,"journal":{"name":"Biopolymers and Cell","volume":"48 22","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-02-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41307215","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
I. Hnatiuk, O. Varchenko, M. Kuchuk, M. Parii, Y. Symonenko
{"title":"Creation of winter rapeseed Brassica napus L. commercial line of biotechnological plants, resistant to the glyphosate action","authors":"I. Hnatiuk, O. Varchenko, M. Kuchuk, M. Parii, Y. Symonenko","doi":"10.7124/BC.000A40","DOIUrl":"https://doi.org/10.7124/BC.000A40","url":null,"abstract":"Aim. To create biotechnological plants of a commercial line winter rapeseed, which carry the glyphosate and phosphinostricin resistance genes. Methods. In vitro tissue culture method, Agrobacterium -mediated genetic transformation, polymerase chain reaction and χ 2 methods were used. Results. The PCR analysis results are presented for the biotechnological winter rapeseed plants obtained after genetic transformation to confirm the presence of CP4 epsps gene insert in 11 of 12 plants, as well as the presence of bar gene integration in 6 of 7 plants. All obtained regenerant plants were adapted to in vivo conditions, treated with glyphosate and vernalized. The obtained seeds were sterile germinated and the segregation was determined based on the resistance to the selective agent. Conclusion. 11 biotechnological plants with the glyphosate ( epsps ) and kanamycin ( nptII ) resistance genes were obtained, as well as 6 biotechnological plants, which carry phosphinothricin ( bar ) resistance genes in addition to the epsps gene. The presence of the CP4 EPSPS protein in transgenic rapeseed plants has been proven by the molecular analysis of protein expression using an immunoassay system. The expression of selective agents resistance genes was confirmed in T 1 generation.","PeriodicalId":39444,"journal":{"name":"Biopolymers and Cell","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42410058","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Transfection of mesenchymal stem cells at physiological oxygen concentrations","authors":"N. Shuvalova, E. K. Toporova, V. Kordium","doi":"10.7124/BC.000A41","DOIUrl":"https://doi.org/10.7124/BC.000A41","url":null,"abstract":"Aim. Numerous works showed the beneficial effect of oxygen in physiological concentrations on mesenchymal stem cells (MSC) cultures. The aim of the present work was to study the impact of physiological oxygen tensions on non-viral transfection of MSC from human Wharton jelly (WJ-MSC). Methods. WJ-MSC at passage 2 were cultivated for 48 hours in different gas mixtures: nitrogen-based (oxygen – 3 %, CO 2 – 5 %, nitrogen – 92 %) and argon-based (oxygen – 3 %, CO 2 – 5 %, argon – 92 %), while the control group was cultivated under standard conditions of CO 2 -incubator (ambient oxygen concentration, CO 2 – 5 %). After 48 hours of cultivation the cells were transfected with polyplexes pEGFP-C1/PEI/ and pEGFP-C1/TurboFect, containing 3 μg of plasmid DNA. The cultures were in contact with com plexes for 1 hour, at standard conditions of CO 2 -incubator. Next, the media were changed, and WJ-MSC were cultivated for 48 hours in described gas mixtures, and CO 2 – incubator. Transfection effectiveness was estimated by flow cytometry as the number of eGFP+ fluores cent cells, (BD FACSAria). Results. In the groups cultivated in gas mixtures containing 3 % of oxygen, the number of cells, synthesizing eGFP+ before and after the transfection procedure, was on average 2.58 times higher in the nitrogen-based mixture and 1.37 times higher in the argon-based mixture than in control groups from the CO 2 –incubator. Conclusions. The cul tivation of human WJ-MSC under physiological oxygen tensions allowed an increase in the percentage of transfected cells, and is promising to be used as a method for optimization of transfection.","PeriodicalId":39444,"journal":{"name":"Biopolymers and Cell","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49393018","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
M. Protopopov, V. Vdovin, S. S. Lukashov, O. V. Ostrynska, I. Borysenko, O. Borovykov, S. Starosyla, Y. Bilokin, O. P. Kukharenko, V. Bdzhola, S. Yarmoluk
{"title":"The synthesis of 5-hetarylamino-3-aryl-1H-indazoles as inhibitors of protein kinase CK2","authors":"M. Protopopov, V. Vdovin, S. S. Lukashov, O. V. Ostrynska, I. Borysenko, O. Borovykov, S. Starosyla, Y. Bilokin, O. P. Kukharenko, V. Bdzhola, S. Yarmoluk","doi":"10.7124/BC.000A44","DOIUrl":"https://doi.org/10.7124/BC.000A44","url":null,"abstract":"Aim. Basing on our earlier finding of inhibitory activity of 5-(4-quinazolylamino)-3-arylinda-zoles against human protein kinase CK2, the synthesis of new nitrogen containing heterocyclic derivatives was performed in order to find novel inhibitors of this kinase. Methods. Organic synthesis, NMR spectroscopy. Results. A series of 4-chloroquinazolines, 4-chloroquinolines, 4-chloropyrazolo[3,4-d]pyrimidines and 4-chlorothieno[2,3-d]pyrimidine was synthesized. Reaction of these intermediates with 5-amino-3-(3,4-dichlorophenyl)-indazole gave us a series of 14 novel heterоcyclic derivatives of 5-amino-3-arylindazole. Conclusions. Besides new quinazoline derivatives – the quinoline and thieno[2,3-d]pyrimidine derivatives of similar structure but different polarity were obtained. Also a series of 1-methylpyrazolo[3,4-d]py-rimidine derivatives with decreased lipophilicity was synthesized.","PeriodicalId":39444,"journal":{"name":"Biopolymers and Cell","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71341987","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Comparative analysis of the effect of 6-azacytidine, ribavirin and cyclocytidine on the synthesis of adenoviral polypeptides","authors":"L. Nosach, L. Usenko, I. Alexeeva","doi":"10.7124/BC.000A42","DOIUrl":"https://doi.org/10.7124/BC.000A42","url":null,"abstract":"Aim. Comparative study of the effect of antiviral nucleoside analogues 6-azacytidine (6-azaC), ribavirin (Rbv) and cyclocytidine (CycloC) on the synthesis of adenoviral (ADV) polypeptides in cell cultures. Methods. Luminescent microscopy, immunofluorescent assay of hexon antigen, SDS-polyacrylamide gel electrophoresis of 14 C-labeled proteins. Results. 6-AzaC and Rbv are able to block completely the expression of adenoviral genome, switching off the synthesis of both early and late structural viral polypeptides. Rbv can also inhibit the formation of immunologically active hexon trimers and intranuclear inclusion bodies of the late type. The effect of CycloC on the functional activity of adenoviral genome is different: it is able to completely block the late, but not early function of the viral genome associated with the synthesis of 72K DNA-binding protein. The synthesis of this protein stopped only after the synthesis of the whole spectrum of polypeptides of structural proteins. Conclusion. The peculiarities of the effect of nucleoside analogues on the synthesis of adenoviral polypeptides were established. All studied nucleosides are able to suppress the synthesis; however, the specific profiles of their biological activity are determined by the structure and concentration of the compounds.","PeriodicalId":39444,"journal":{"name":"Biopolymers and Cell","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43331667","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}