Russian Journal of Bioorganic Chemistry最新文献

{"title":"Synthesis, Biological, and Computational Studies of Novel Isoxazolone-Coupled Azo Moieties and Their Photophysical Interactions","authors":"K. O. Karunasagar,&nbsp;Yadav D. Bodke,&nbsp;K. K. Vinay,&nbsp;Y. Surendranaik","doi":"10.1134/S1068162024605962","DOIUrl":"10.1134/S1068162024605962","url":null,"abstract":"<p><b>Objective:</b> In this study, we report the synthesis of new heterocyclic azo dyes (<b>IIIa–IIId</b>) <i>via</i> diazo-coupling reactions of sulfonamides with isoxazolone as the coupling component. The synthesized compounds (<b>IIIa–IIId</b>) were thoroughly characterized, and their biological activities were evaluated through antioxidant and α-amylase inhibition assays. <b>Methods:</b> The target compounds were synthesized by diazo-coupling reactions of different heterocyclic amines (<b>Ia–Id</b>) with 3-phenyl-5-isoxazolone (<b>II</b>). Density Functional Theory (DFT) calculations were performed using the B3LYP functional with the 6-31G(d,p) basis set. Furthermore, <i>in silico</i> molecular docking studies of the target ligands were conducted against the α-amylase receptor. <b>Results and Discussion:</b> The synthesized azo compounds were characterized by various spectroscopic techniques, including FT-IR, ¹H, ¹³C NMR, and HR-MS. DFT studies provided insight into quantum chemical parameters such as the HOMO–LUMO energy gap, electrophilicity index (ω), chemical potential (μ), global hardness (η), softness (S), and molecular electrostatic potential (MEP) surfaces. UV-Vis absorption spectra of the azo dyes were recorded in 5 different solvents, revealing distinct solvatochromic behavior. Antioxidant and α-amylase inhibition assays were employed to assess the pharmacological potential of the synthesized azo dyes. Antioxidant activity results indicated that compound (<b>IIIa</b>) exhibited strong activity with an IC₅₀ value of 21.581 µg/mL, comparable to the reference standard ascorbic acid. In α-amylase inhibition studies, compounds (<b>IIIc</b>) and (<b>IIId</b>) demonstrated significant activity relative to the standard drug acarbose. Molecular docking results further supported these findings, with compounds (<b>IIIc</b>) and (<b>IIId</b>) exhibiting the lowest binding energies of –6.4 and –6.3 kcal/mol, respectively, forming two and four hydrogen bonds with key amino acid residues in the active site of α-amylase. <b>Conclusions:</b> The synthesized isoxazolone-based azo dyes showed promising biological activities and photophysical properties. The combined experimental and computational data suggest their potential for further development as bioactive agents.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 3","pages":"1099 - 1114"},"PeriodicalIF":1.7,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145142272","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Role of Phospholipid Derivatives of Cyclodextrins in the Formation of Stable Lipid Nanoparticles for Drug Delivery","authors":"Е. D. Belitskaya,&nbsp;V. A. Oleinikov,&nbsp;A. V. Zalygin","doi":"10.1134/S1068162024606591","DOIUrl":"10.1134/S1068162024606591","url":null,"abstract":"<p>The review is devoted to the physical methods of investigation of the structural characteristics of inclusion complexes of supramers of phospholipid derivatives of cyclodextrins. Phospholipid derivatives of cyclodextrins are formed by attaching a phospholipid moiety to the cyclodextrin molecule. This modification imparts additional structural features to the cyclodextrin, increasing its solubility and stability in aqueous media. These new compounds can self-assemble in aqueous media into supramolecular nanocomplexes of different types. Biomedical applications are envisaged for nanoencapsulation of drug molecules in hydrophobic interchain volumes and nanocavities of amphiphilic cyclodextrins (serving as drug carriers or pharmaceutical excipients), antitumor phototherapy, gene delivery, and protection of unstable active ingredients by the complexation of inclusions in nanostructured media. Special attention is focused on the morphology of nanoparticles, because efficient delivery systems must meet certain requirements. Classical physical methods cannot provide detailed information on the properties of potential structures for biomedical applications. To this end, the search for new noninvasive approaches is necessary.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 3","pages":"1022 - 1033"},"PeriodicalIF":1.7,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145142274","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Mass Spectrometric Analysis of Post-Translational Modifications of Xenopus laevis Cytoskeletal Protein Zyxin","authors":"E. D. Ivanova,&nbsp;R. H. Ziganshin,&nbsp;E. A. Parshina,&nbsp;A. G. Zaraisky,&nbsp;N. Y. Martynova","doi":"10.1134/S1068162024606530","DOIUrl":"10.1134/S1068162024606530","url":null,"abstract":"<p><b>Objective:</b> Zyxin, a LIM-domain protein within the cytoskeletal system, is actively researched due to its involvement in fundamental cellular processes, from mechanosensory functions and regulation of actin polymerization at cell junctions to gene expression modulation. Disruption of zyxin expression and processing has been linked to carcinogenesis and cardiovascular diseases, and it plays a crucial role in tumor invasion and metastasis. Additionally, the post-translational modifications of zyxin in mammals regulate its activity and subcellular localization. <b>Methods:</b> Given highly conserved evolutionary nature of zyxin, we conducted a search for post-translational modifications of the zyxin homolog in <i>Xenopus laevis</i> using chromatographic mass spectrometry. To identify modified peptides, we utilized an enrichment method involving the co-immunoprecipitation of endogenous zyxin from gastrula-stage embryonic cell lysates. Furthermore, to identify zyxin isoforms with varying electrophoretic mobilities, separation was achieved through polyacrylamide gel electrophoresis. <b>Results and Discussion:</b> Our findings revealed previously unknown modifications of zyxin, specifically, <i>N</i>-terminal acetylation at methionine position 1 and phosphorylation at Ser197 and Ser386. Zyxin was observed in bands corresponding to electrophoretic mobilities of 70 and 105 kDa. This study thus presents novel data regarding the post-translational modifications of zyxin in <i>X. laevis</i>. <b>Conclusions:</b> Since defects in mechanical signal transduction are associated with developmental disorders, oncogenesis, and metastasis, the study of mechanosensitive protein zyxin modifications and processing on the model organism <i>X. laevis</i> opens up opportunities for diagnostic studies at the molecular level, which can be used in the future to determine the prospects for drugs use in pharmacology.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 3","pages":"1083 - 1091"},"PeriodicalIF":1.7,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145141944","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Naturally Occurring Alkaloids: Their Structural Elucidation and Biological Activity (2020–2024)","authors":"Fatima Choudry,&nbsp;Moonsa Haq,&nbsp;Shaneeza Tariq,&nbsp;Rimsha Kiran,&nbsp;Faiza Batool,&nbsp;Momna Haq,&nbsp;Ghulam Shabir,&nbsp;Aamer Saeed","doi":"10.1134/S1068162025070222","DOIUrl":"10.1134/S1068162025070222","url":null,"abstract":"<p>Alkaloids are naturally occurring secondary metabolites produced by plants, bacteria, and fungi. They are renowned for their complex chemical structures and diverse biological activities. These compounds have long captivated researchers due to their significant pharmacological potential, rendering them invaluable in natural product chemistry and drug discovery. The structural diversity of alkaloids—originating from a variety of biosynthetic pathways and heterocyclic ring systems—enables them to interact with a wide range of biological targets, leading to numerous therapeutic effects. This review aims to explore the structural elucidation and biological activities of alkaloids derived from plants, bacteria, and fungi, emphasizing their roles as key bioactive molecules in the development of modern medicine. By examining these compounds, we can gain deeper insights into their mechanisms of action and their potential in treating life-threatening diseases, including cancer, as well as their broader implications for human health.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 3","pages":"947 - 990"},"PeriodicalIF":1.7,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145141993","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design, Synthesis, Molecular Docking, and Biological Evaluation of Novel 1,2,4-Oxadiazole-Based Derivatives as Inhibitors of Trypsin, ALDH2, and iNOS","authors":"Mohammed Salah Ayoup,&nbsp;Rabia E. Alashhab,&nbsp;Hamida Abdel-Hamid,&nbsp;Doaa A. Ghareeb,&nbsp;Aliaa Masoud,&nbsp;Amr Sonousi,&nbsp;Asmaa E. Kassab,&nbsp;Mohamed N. Abd Al Moaty","doi":"10.1134/S1068162024606128","DOIUrl":"10.1134/S1068162024606128","url":null,"abstract":"<p><b>Objective:</b> A series of novel derivatives based on a 1,2,4-oxadiazole scaffold were designed, synthesized, and evaluated <i>in vitro</i> for their inhibitory activity against trypsin, aldehyde dehydrogenase 2 (ALDH2), and inducible nitric oxide synthase (iNOS), aiming to identify potential anticancer agents. <b>Methods:</b> The synthesized 1,2,4-oxadiazole derivatives were characterized by NMR, IR spectroscopy, and elemental analysis. Their biological activity was evaluated through <i>in vitro</i> enzyme inhibition assays and supported by molecular docking studies using MOE software. <b>Results and Discussion:</b> The results demonstrated that compounds (<b>Va</b>), (<b>Vb</b>), and (<b>VIIb</b>) exhibited potent trypsin inhibition, exceeding that of the reference compound benzamidine hydrochloride. Additionally, derivatives (<b>IIIa</b>) and (<b>IIIb</b>) also showed notable trypsin inhibitory activity. Compounds (<b>Va</b>) and (<b>VIa</b>) displayed significant ALDH2 inhibition, comparable to that of tetraethylthiuram disulfide. Furthermore, derivatives (<b>VIa</b>), (<b>VIb</b>), and (<b>VIIIb</b>) effectively inhibited iNOS. The pronounced inhibitory activities of the most potent compounds (<b>Va</b>, <b>VIa</b>, and <b>VIIb</b>) may be attributed to strong interactions within the active sites of trypsin and ALDH2, as supported by molecular docking studies. Compound (<b>Va</b>) also exhibited favorable physicochemical properties, suggesting its potential as a promising lead compound for further drug development. <b>Conclusions:</b> 1,2,4-Oxadiazole derivative (<b>Va</b>) appears to be a promising anticancer lead compound for further investigation and development.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 3","pages":"1171 - 1188"},"PeriodicalIF":1.7,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145161248","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis and Study of Cytotoxicity of 3β-Acetoxyurs-12-en-28-oyl-thiourea Derivatives","authors":"S. A. Popov,&nbsp;T. D. Borisova,&nbsp;E. E. Shults,&nbsp;M. K. Marenina,&nbsp;Yu. V. Meshkova,&nbsp;T. G. Tolstikova","doi":"10.1134/S1068162024606748","DOIUrl":"10.1134/S1068162024606748","url":null,"abstract":"<p><b>Objective:</b> The design and study of cytotoxicity of acylthiourea derivatives of the ursane series were presented. <b>Methods:</b> A series of substituted 3β-acetoxy-urs-12-en-28-oyl-thioureas were synthesized by condensation of triterpenoid acyl isothiocyanate with amino derivatives. The CuAAC reactions of intermediate acylthioureas containing propargyl and azide substituents led to the formation of hybrid acylthioureas holding a 1,2,3-triazole linker. The cytotoxicity of the new derivatives on tumor cells MCF7, HepG2, and HeLa and on human dermal fibroblasts DF-2 was studied. <b>Results and Discussion:</b> Polar hybrids containing carboxyl or alcohol groups and the compound with (1<i>H</i>-1,2,3-triazol-4-yl)methanol substituent exhibited high inhibitory activity, significantly superior to the parent compound ursolic acid, and were more selective than doxorubicin. <b>Conclusions:</b> We designed new ursane-derived acylthioureas and showed that compounds of this series may exhibit significant cytotoxicity towards human cancer cells. Ursane hybrids with acylthiourea derivatives are of interest for further investigation as promising antitumor agents.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 3","pages":"1147 - 1160"},"PeriodicalIF":1.7,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145161247","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis, Computational, and UV-Vis Absorption Studies of Novel Benzothiazole Azo Derivatives and Their Biological Potentials","authors":"K. K. Vinay,&nbsp;Yadav D. Bodke,&nbsp;Shivakumar Naik,&nbsp;Udayakumar Dalimba","doi":"10.1134/S1068162024606165","DOIUrl":"10.1134/S1068162024606165","url":null,"abstract":"<p><b>Objective:</b> In the present work, a series of novel mono-azo benzothiazole derivatives were synthesized <i>via</i> the diazo-coupling reaction of cyclopentane-1,3-dione with various substituted benzothiazole amines. The synthesized compounds were thoroughly characterized, and their biological potential was evaluated by testing their antitubercular and antimicrobial activities. <b>Methods:</b> The target compounds were synthesized through a diazo-coupling reaction of different benzothiazole amines with cyclopentane-1,3-dione. Computational studies were performed using the DFT/B3LYP method with the 6-31G++(d,p) basis set. Additionally, <i>in silico</i> molecular docking studies of the target compounds were conducted with the enoyl-ACP reductase receptor. <b>Results and Discussion:</b> The structures of the target azo compounds were confirmed by various spectroscopic techniques, including FT-IR, NMR (¹H and ¹³C), and HRMS. Quantum chemical parameters, frontier molecular orbitals, and molecular electrostatic potential surfaces were evaluated using DFT to elucidate the electronic properties of the benzothiazole azo dyes. The UV-Vis absorption studies of the synthesized compounds were conducted in 6 organic solvents. The target azo dyes were screened for their antitubercular activity against the <i>M. tuberculosis</i> H37Rv strain. The antibacterial activity of the target compounds was tested against four bacterial pathogens (<i>S. aureus</i>, <i>S. mutans</i>, <i>E. coli</i>, and <i>S. typhi</i>), and their antifungal activity was evaluated against the fungal strain <i>A. niger</i>. <b>Conclusions:</b> Antitubercular activity results revealed that the compound 3-hydroxy-2-{[4-methylbenzo(<i>d</i>)thiazol-2-yl]diazinyl}cyclopent-2-en-1-one displayed promising activity with a minimal inhibitory concentration of 3.25 µg/mL compared to the other synthesized compounds. In antimicrobial activity, the compounds 2-[benzo(<i>d</i>)thiazol-2-yl]diazenyl-3-hydroxycyclopent-2-en-1-one, 3-hydroxy-2-{[4-methylbenzo(<i>d</i>)thiazol-2-yl]diazinyl}cyclopent-2-en-1-one, and 3-hydroxy-2-{[6-methylbenzo(<i>d</i>)thiazol-2-yl]diazinyl}cyclopent-2-en-1-one exhibited significant activity against the tested pathogens. Furthermore, docking results suggested that the target compounds displayed favorable docking scores and showed significant binding interactions with amino acid residues.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 3","pages":"1233 - 1248"},"PeriodicalIF":1.7,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145161583","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Method for Increasing the Efficiency of Selection of Aptamers to Cellular Receptors","authors":"V. E. Kuznetsova,&nbsp;T. D. Lebedev,&nbsp;V. E. Shershov,&nbsp;G. F. Shtylev,&nbsp;I. Yu. Shishkin,&nbsp;R. A. Miftakhov,&nbsp;V. I. Butvilovskaya,&nbsp;I. V. Grechishnikova,&nbsp;O. A. Zasedateleva,&nbsp;A. V. Chudinov","doi":"10.1134/S1068162024606979","DOIUrl":"10.1134/S1068162024606979","url":null,"abstract":"<p><b>Objective:</b> A method to increase the efficiency of cell-SELEX-based selection of aptamers to cellular receptors, in particular, to the receptor tyrosine kinase c-KIT, was presented. <b>Methods:</b> Direct monitoring of each aptamer selection cycle by analyzing the shift of the melting curve towards higher temperatures allows monitoring the enrichment of a combinatorial oligonucleotide library due to the correlation of increasing GC content and melting temperature with an increase of aptamer affinity for the corresponding target. <b>Results and Discussion:</b> The use of non-ionic surfactants (Tween 20) in the composition of buffer solutions, as well as trypsinolysis of surface proteins at the stage of elution of the oligonucleotide library bound to the cell surface, significantly reduce non-specific sorption. Non-ionic surfactants in low concentrations can be incorporated into the lipid bilayer, forming polar defects that change the physical properties of cell membranes and lead to their reversible solubilization, which causes a decrease in non-specific sorption. Trypsin, an enzyme of the hydrolase class, possessing proteolytic activity, cleaves peptide bonds of proteins on the cell surface without compromising the integrity of the membrane and DNA aptamer. <b>Conclusions:</b> We presented a method that allows increasing the specificity of aptamers and decreasing non-specific sorption, according to the results of fluorescence microscopy, thermofluorimetric analysis, and high-precision sequencing.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 3","pages":"1287 - 1296"},"PeriodicalIF":1.7,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145161585","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"2-Fluorocordycepin: Chemoenzymatic Synthesis and Study of Anticancer Activities In Vitro","authors":"A. O. Arnautova,&nbsp;K. V. Antonov,&nbsp;E. A. Zorina,&nbsp;M. A. Simonova,&nbsp;A. S. Paramonov,&nbsp;O. S. Zhukova,&nbsp;M. V. Kiselevskiy,&nbsp;A. L. Kayushin,&nbsp;I. V. Fateev,&nbsp;E. V. Dorofeeva,&nbsp;B. Z. Eletskaya,&nbsp;M. Ya. Berzina,&nbsp;O. S. Smirnova,&nbsp;T. V. Egorova,&nbsp;R. S. Esipov,&nbsp;A. I. Miroshnikov,&nbsp;I. D. Konstantinova","doi":"10.1134/S1068162025601144","DOIUrl":"10.1134/S1068162025601144","url":null,"abstract":"<p><b>Objective:</b> The aim of this study was to develop an efficient method for the preparation of 2-fluorocordycepin and to evaluate its anticancer activity <i>in vitro</i>. <b>Methods:</b> An approach to chemical synthesis of 2-fluorocordycepin was developed. The conditions of chemoenzymatic synthesis of this compound were optimized. <b>Results and Discussion:</b> 2-Fluorocordycepin was prepared chemically using α-acetoxyisobutyryl bromide in three steps with 34% yield and by enzymatic method using <i>E. coli</i> purine nucleoside phosphorylase and 1-alpha phosphate of 3-deoxyribose with 66% yield. The latter compound was synthesized in eight steps: the protected isopropylidene derivative of 3-deoxyribose was obtained in four steps, followed by an attempt at direct “one pot” phosphorylation. <b>Conclusions:</b> Two methods of 2-fluorocordycepin preparation were proposed and implemented: chemical synthesis from 2-fluoradenosine and chemoenzymatic synthesis, including preparation of 3-deoxyerythropentofuranoso-1-phosphate, followed by transglycosylation using <i>E. coli</i> purine nucleoside phosphorylase. The cytotoxic activity of 2-fluorocordycepin <i>in vitro</i> was evaluated. It was shown that 2-fluorocordycepin exhibits antimetabolic effect against a number of cancer cell lines (Jurkat, Raji, MCF-7, THP-1, U937, A549, LS174T), which allows us to consider this compound as a promising candidate for the development of anticancer drugs.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 3","pages":"1189 - 1205"},"PeriodicalIF":1.7,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145161724","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fluorescence Labeling of GC-Rich DNA Matrix with Different Nucleotide Derivatives for Hybridization Analysis on a Biological Microarray","authors":"I. O. Barinova,&nbsp;V. E. Shershov,&nbsp;V. O. Varachev,&nbsp;S. A. Surzhikov,&nbsp;I. V. Grechishnikova,&nbsp;O. A. Zasedateleva,&nbsp;T. V. Nasedkina,&nbsp;A. V. Chudinov","doi":"10.1134/S1068162024606918","DOIUrl":"10.1134/S1068162024606918","url":null,"abstract":"<p><b>Objective:</b> We investigated the efficiency of labeling the GC-rich promoter region of the <i>TERT</i> gene in the human genome with derivatives of 5′-triphosphates of 2′-deoxyuridine (dU) and 2'-deoxycytidine (dC) containing cyanine dyes Cy5 and Cy7 as a fluorescent label. <b>Methods:</b> The effect of modified nucleotides on the efficiency of the polymerase chain reaction was evaluated by real-time PCR, and the extent of nucleotide incorporation into the PCR product was also determined. The efficiency of DNA matrix labeling was determined by the intensity of fluorescent signal during allele-specific hybridization on a biological microarray (biochip). <b>Results and Discussion:</b> The highest level of biochip gel drops fluorescence was observed for dU-Cy7 derivatives compared to dU- and dC-Cy5 derivatives. At the same time, in the case of GC-rich DNA matrix, the use of dC-Cy5 derivatives provided a fundamentally better result compared to dU-Cy5 derivative. Thus, modified Cy7 analogs capable of incorporation into DNA during PCR are less dependent on the GC composition of the DNA matrix and are more universal fluorescent labels for diagnostic purposes. <b>Conclusions:</b> Further application of modified Cy7 analogs in the development of laboratory-on-a-chip test systems seems to be the most promising.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 3","pages":"1249 - 1254"},"PeriodicalIF":1.7,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145161244","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}