Russian Journal of Bioorganic Chemistry最新文献

{"title":"Construct Design, Isolation, and Purification of the Human GPR17 Receptor Monomeric Form for Structural and Functional Studies","authors":"N. A. Safronova,&nbsp;A. P. Luginina,&nbsp;A. A. Sadova,&nbsp;M. B. Shevtsov,&nbsp;O. V. Moiseeva,&nbsp;V. I. Borshchevskiy,&nbsp;A. V. Mishin","doi":"10.1134/S106816202501025X","DOIUrl":"10.1134/S106816202501025X","url":null,"abstract":"<p><b>Objective:</b> G protein-coupled receptors (GPCRs) are a family of seven transmembrane domain proteins with more than 800 members in the human genome. They play a key role in the regulation of most of the processes in the human body and are the targets of one third of all modern drugs. Despite their importance in pharmacology, many GPCRs remain orphan receptors, i.e., their endogenous ligands are unknown. An orphan receptor GPR17, a class A GPCR representative, is predominantly expressed in the central nervous system and plays an important role in regulating the formation of the myelin sheath of neurons. It is a potential target for the development of new drugs against various disorders, such as multiple sclerosis, Alzheimer’s disease, and ischemia. The aim of this work was to prepare GPR17 for structural and functional studies starting from protein modification and ending with the receptor production. <b>Methods:</b> A screening of different genetically engineered constructs was performed, a series of point mutations were analyzed, and a significant number of potential ligands for this receptor were tested. The constructs were expressed in the Sf9 insect cell line using the Bac-to-Bac approach. The membrane fraction was extracted, the protein was solubilized into DDM/CHS detergent micelles, followed by purification by a metal affinity chromatography. Functional analysis of the purified protein included analytical gel filtration, polyacrylamide gel electrophoresis, and thermal stability analysis. <b>Results and Discussion:</b> Stabilizing point mutations were identified and the optimal position of the partner protein was found. The conditions for the expression, isolation, and purification of GPR17 were optimized to produce a sufficiently stable and monomeric protein sample suitable for further structural and functional studies. <b>Conclusions:</b> GPR17 is an orphan GPCR and the actively studied pharmacological target. The structural and functional investigation of this protein is a relevant problem for modern science and biomedicine. As a result of an in-depth study of GPR17, several stabilizing receptor modifications were developed, and optimal conditions for recombinant protein production were found. Our results can be used for further structural and functional studies of GPR17 and can serve as an example of a strategy that can be applied to perform investigation of other GPCRs.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 1","pages":"308 - 319"},"PeriodicalIF":1.1,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143396616","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":"Quantitative Analysis of Biomolecular Condensates on a Modified Support","authors":"A. S. Shtork,&nbsp;Iu. I. Pavlova,&nbsp;J. I. Svetlova,&nbsp;M. S. Iudin,&nbsp;E. N. Grafskaia,&nbsp;V. A. Manuvera,&nbsp;S. E. Alieva,&nbsp;A. M. Varizhuk,&nbsp;V. N. Lazarev,&nbsp;T. S. Vedekhina","doi":"10.1134/S1068162025010182","DOIUrl":"10.1134/S1068162025010182","url":null,"abstract":"&lt;p&gt;&lt;b&gt;Objective:&lt;/b&gt; Biomolecular condensates are associates of biopolymers formed in aqueous solutions &lt;i&gt;via&lt;/i&gt; “liquid-liquid” phase separation. Aberrant phase transitions of proteins or nucleic acids underlie several pathologies, and the need for their &lt;i&gt;in vitro&lt;/i&gt; models stimulates the development of methods for biocondensate investigation. This work addresses the key problem of visualizing labeled protein-RNA condensates using fluorescence microscopy. &lt;b&gt;Methods:&lt;/b&gt; The SARS-CoV-2 N-protein with a C-terminal hexahistidine tag was expressed in &lt;i&gt;Escherichia coli&lt;/i&gt; BL21-Gold(DE3) and isolated by metal chelate chromatography. The N-protein was labeled with the RED dye, which emits fluorescence in the far-red range of the spectrum, using the RED-NHS dye. Commercially available RNA isolated from Torula yeast was used as random RNA to obtain condensates with the N-protein and SR-rich peptide. In experiments to test the colocalization of the condensate components, a labeled modified oligonucleotide forming an SL4 hairpin with an elongated stem was added to the random RNA. To obtain the APTES support, chemically polished glass was treated with 3-aminopropyltriethoxysilane in ethyl alcohol at pH 4.5–5.5. To obtain the DSC-APTES support, the APTES support was additionally functionalized by treating with &lt;i&gt;N&lt;/i&gt;,&lt;i&gt;N&lt;/i&gt;′-disuccinimidyl carbonate in the presence of diisopropylethylamine in anhydrous acetone. A quantitative assessment of condensate formation was performed using fluorescence microscopy data. The FastTrack program was used to assess droplet mobility. The Droplet_Calc program was used to assess the droplet area and curvature coefficient. &lt;b&gt;Results and Discussion:&lt;/b&gt; The mobility of the condensates in a sample layer on glass complicates data processing. In previous studies, condensate immobilization on 3-aminopropyltriethoxysilane-treated glass (APTES), was proposed to overcome this problem. The APTES support allows non-covalent RNA/DNA binding but is suboptimal for proteins. By treating APTES with &lt;i&gt;N&lt;/i&gt;,&lt;i&gt;N&lt;/i&gt;′-disuccinimidyl carbonate, we obtained an alternative support, DSC-APTES, which allows covalent binding of protein fragments via lysine residues. A comparative analysis of known condensates on the abovementioned supports revealed their decreased mobility on APTES/DSC-APTES, and the optimal type of support modification depended on the condensate composition. Condensate immobilization improved image quality and increased the colocalization of the oligonucleotide and protein components. It also facilitated the quantitative analysis of the phase separation based on the condensate fractions. New software, Droplet_Calc, was developed to automate condensate identification and fraction calculation. The results confirmed the advantages of APTES and DSC-APTES over glass when analyzing the concentration dependence of the condensate fraction and creating phase diagrams. &lt;b&gt;Conclusions:&lt;/b&gt; Thus, the optimization of the support a","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 1","pages":"273 - 284"},"PeriodicalIF":1.1,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143396450","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":"Chemical Synthesis of Novel DDR1 Inhibitors and Their Activity Against Gefitinib-Resistant Non-Small Cell Lung Cancer","authors":"Xuemei Xu,&nbsp;Siyu Chen,&nbsp;Doudou Sun,&nbsp;Xuebao Wang,&nbsp;Zhouyang Xu","doi":"10.1134/S1068162025010108","DOIUrl":"10.1134/S1068162025010108","url":null,"abstract":"<p><b>Objective:</b> The discoidin domain receptor-1 (DDR1) has been demonstrated as a potential target in gefitinib-resistant non-small cell lung cancer (NSCLC). However, drug development in this area remains limited. Therefore, this study aims to chemically synthesize novel DDR1 inhibitors and explore their activity against gefitinib-resistant NSCLC. <b>Methods:</b> The structures of the synthesized compounds were confirmed by electrospray ionization mass spectrometry (ESI-MS), ¹H, ¹³C NMR, and elemental analysis, followed by kinase screening experiments. The inhibitory impact of these compounds on the proliferation of PC-9 cells and gefitinib-resistant cell lines (PC-9GR and HCC827GR) was evaluated using the cell counting kit-8 (CCK-8) assay. Furthermore, the invasion capability of the cells was assessed using the Transwell assay. Additionally, Western blot analysis was employed to explore the targeting effects of these compounds on DDR1. <b>Results and Discussion:</b> Twenty-four 4,6-disubstituted pyrimidine derivatives were synthesized in series A, B, and C. Some compounds in series A and C exhibited promising inhibitory effects against DDR1 and DDR2, with compounds (<b>A04</b>), (<b>A05</b>), and (<b>C04</b>) demonstrating more pronounced activities. Moreover, compounds (<b>A02</b>), (<b>A03</b>), (<b>A07</b>), and (<b>C04</b>) significantly impeded the viability of PC-9 and PC-9GR cells, with (<b>A07</b>) exhibiting the strongest inhibition, with half-maximal inhibitory concentration (IC₅₀) values of 1.12 ± 0.07, 1.03 ± 0.18, and 1.56 ± 0.19 µM against PC-9, PC-9GR, and HCC827GR cells, respectively. Furthermore, 1 µM of (<b>A03</b>) and (<b>A07</b>) significantly inhibited the protein expression of <i>p</i>-DDR1 and DDR1, with compound (<b>A07</b>) being the most significant inhibitor (<i>p</i> &lt; 0.001). Additionally, the Transwell assay demonstrated that 1 µM of (<b>A07</b>) substantially inhibited the invasion of PC-9 (<i>p</i> = 0.0003) and PC-9GR cells (<i>p</i> = 0.0019). <b>Conclusions:</b> The newly synthesized DDR1 inhibitor (<b>A07</b>) effectively inhibits the proliferation and invasion of gefitinib-resistant NSCLC cells, offering a potential new therapeutic option for treating NSCLC.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 1","pages":"285 - 297"},"PeriodicalIF":1.1,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143396574","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":"Thiazolidine Based Quinazoline Hybrids: Synthesis, Docking, DFT, Molecular Dynamic Study, and In Vitro Antidiabetic Evaluation","authors":"S. Gharge,&nbsp;S. G. Alegaon,&nbsp;S. D. Ranade,&nbsp;R. S. Kavalapure","doi":"10.1134/S106816202501011X","DOIUrl":"10.1134/S106816202501011X","url":null,"abstract":"<p><b>Objective:</b> This study aimed to design, synthesize, and evaluate thiazolidinedione and rhodanine-based quinazoline derivatives (<b>Va–Vc</b>) as dual inhibitors of α-amylase and α-glucosidase, with an investigation into their pharmacokinetic properties and mechanism of action using a computational approach. <b>Methods:</b> The compounds were designed computationally and synthesized using appropriate synthons. <i>In silico</i> molecular docking and molecular dynamics simulations were employed to explore their interactions with α-amylase, GLUT-4, and homology-modeled α-glucosidase. Pharmacokinetic properties, including drug-likeness, ADME, and toxicity, were predicted. Network pharmacology and experimental validation were used to assess the modulation of PI3K-AKT, MAPK, and EGFR signaling pathways, as well as inhibitory activities against α-amylase, α-glucosidase, and glucose uptake by yeast cells. <b>Results and Discussion:</b> The derivatives exhibited promising inhibitory activities. Substituted benzylidine thiazolidine-2,4-dione showed IC₅₀ values of 22.59 ± 0.30 µM for α-amylase and 43.50 ± 1.23 µM for α-glucosidase, with 58.23 ± 0.14% glucose uptake. Substituted benzylidene-4-oxo-2-thioxothiazolidin-3-yl acetic acid displayed IC₅₀ values of 13.48 ± 1.38 µM for α-amylase and 65.94 ± 0.14 µM for α-glucosidase, with 57.23 ± 0.13% glucose uptake. These compounds modulated key signaling pathways, contributing to their inhibitory effects and favorable pharmacokinetic profiles. <b>Conclusions:</b> The study highlights the potential of thiazolidinedione and rhodanine-based quinazoline derivatives as novel α-amylase and α-glucosidase inhibitors, offering promising therapeutic potential for managing diabetes mellitus. </p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 1","pages":"177 - 201"},"PeriodicalIF":1.1,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143396576","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":"Arylidene-Imidazolones with Three Electron-Donating Substituents as Fluorogenic Dyes for Lipid Droplets of Living Cells","authors":"D. I. Rudik,&nbsp;A. R. Gil’vanov,&nbsp;A. Yu. Smirnov,&nbsp;Yu. A. Bogdanova,&nbsp;S. A. Krasnova,&nbsp;M. S. Baranov","doi":"10.1134/S1068162025010133","DOIUrl":"10.1134/S1068162025010133","url":null,"abstract":"<p><b>Objective:</b> A pair of fluorogenic dyes with three electron-donating groups, based on arylideneimidazolones, is presented.<b> Methods:</b> The formation of imines of the corresponding aldehydes with the subsequent [3 + 2] cycloaddition was used for the synthesis of arylidene-imidazolones. The optical properties of the new compounds were studied. The fluorescence microscopy was used for imaging lipid droplets of the living cells, labeled by the dyes. <b>Results and Discussion:</b> We discovered that a pair of the proposed substances is characterized by a significant bathochromic shift of the absorption and emission maxima, as well as by a noticeable variation of the position of the emission maximum depending on the properties of the environment. We demonstrated that (<i>Z</i>)-5-(3,5-<i>bis</i>(dimethylamino)-4-(ethylamino)benzylidene)-2,3-dimethyl-3,5-dihydro-4<i>H</i>-imidazol-4-one can stain lipid droplets in HeLa Kyoto and Huh 7.5 cell lines. <b>Conclusions:</b> We designed a new selective fluorogenic dye based on arylidene-imidazolones and showed that it can be applicable for lipid droplets labeling in living cells.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 1","pages":"145 - 150"},"PeriodicalIF":1.1,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143396615","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 Mini-Review on Pyridine—A Versatile Compound in the Field of Therapeutic Agents","authors":"Shivani Kapletiya,&nbsp;Harsh Mehta,&nbsp;Sabirkhan Pathan","doi":"10.1134/S1068162025010121","DOIUrl":"10.1134/S1068162025010121","url":null,"abstract":"<p>The chemical reactivity profiles and structures of pyridine derivatives, as well as several techniques for their synthesis, are discussed. Several heterocycles, which are pharmacologically active natural molecules and agrochemicals, are synthesized using these substances as precursors. This review is based on a literature search that included several synthesis techniques and applications of pyridine derivatives. Important chemical compounds with a wide range of uses include pyridine and its derivatives. We have outlined the uses of several pyridine derivatives, both medicinal and non-medicinal, in this review. Numerous biological activities of pyridine derivatives have been documented, and several of the compounds are used in therapeutic settings. Additionally, pyridine derivatives are becoming increasingly significant for contemporary medical applications.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 1","pages":"251 - 265"},"PeriodicalIF":1.1,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143396645","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 the Hepatoprotective Activity of New Uracil Derivatives","authors":"Yu. Z. Khazimullina,&nbsp;A. R. Gimadieva,&nbsp;V. R. Khairullina,&nbsp;E. R. Kudoyarov,&nbsp;D. O. Karimov,&nbsp;A. G. Mustafin","doi":"10.1134/S1068162025010157","DOIUrl":"10.1134/S1068162025010157","url":null,"abstract":"<p><b>Objective:</b> Pyrimidine base derivatives having a wide spectrum of pharmacological activity along with low toxicity are used as active ingredients of many drugs. Specifically, a large number of uracil series compounds have antitumor, anti-inflammatory, antiviral, and immunomodulatory effects, which makes relevant the synthesis of new biologically active derivatives of the pyrimidine series. It is known that the mechanism of hepatotoxicity of chemical compounds is largely associated with the activation of lipid peroxidation, therefore, the objects of the study were uracil derivatives containing a proton-donating group in position C5, which significantly increases the antioxidant properties of the compound. <b>Methods:</b> For the synthesis of uracil derivatives, modification of 5-hydroxy- and 5-amino-6-methyluracils, containing pre-protected C5 functional groups, with various alkyl substituents introduced at <i>N</i>^<i>1</i>,<i>N</i>^<i>3</i> positions was carried out. The method of preliminary etching of cells with the hepatotoxicant carbon tetrachloride and their treatment with the tested compounds was selected for the study of the hepatoprotective activity. <b>Results and Discussion:</b> The introduction of various alkyl substituents at the <i>N</i>^<i>1</i>,<i>N</i>^<i>3</i> positions of 5-hydroxy- and 5-amino-6-methyluracils was shown to increase the solubility of these compounds; the hepatoprotective activity of the synthesized compounds was revealed. <b>Conclusions:</b> New di- and monoalkyl derivatives of 5-hydroxy- and 5-amino-6-methyluracils were obtained, and their hepatoprotective activity was tested <i>in vitro</i>. According to the test results, five of the 20 new compounds synthesized promote cell survival when pretreated with carbon tetrachloride.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 1","pages":"117 - 127"},"PeriodicalIF":1.1,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143396675","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 Quantum-Mechanical Method Reveals the Potential Basis of Antioxidant Activities of Phytomolecules from Jasminum Species: Isolation, Spectral Characterization, DFT, and In Vitro Studies","authors":"Arun Mittal,&nbsp;Suraj N. Mali,&nbsp;Anima Pandey,&nbsp;A. Kuznetsov,&nbsp;Satish Sardana","doi":"10.1134/S1068162025010029","DOIUrl":"10.1134/S1068162025010029","url":null,"abstract":"<p><b>Objective:</b> This study aims to identify and characterize secondary metabolites from the leaves of <i>Jasminum sambac</i> and <i>Jasminum grandiflorum</i>, focusing on their bioactive compounds and antioxidant potential. <b>Methods:</b> Ethanolic extracts of <i>Jasminum sambac</i> and <i>Jasminum grandiflorum</i> were used to isolate secondary metabolites ((<b>JG-3–JG-5</b>), (<b>JS-3–JS-5</b>)). These compounds were characterized using IR, NMR, and mass spectrometry. Density functional theory (DFT) was applied to analyze their antioxidant potential through electronic properties (HOMO–LUMO gaps and molecular electrostatic potential). <b>Results and Discussion:</b> Six compounds ((<b>JG-3–JG-5</b>), (<b>JS-3–JS-5</b>)) were successfully isolated and characterized. The DFT analysis revealed potential antioxidant properties based on HOMO–LUMO gaps and MEP maps. The study enhances the knowledge of the secondary metabolites of <i>Jasminum sambac</i> and <i>Jasminum grandiflorum</i>. Computational analysis supports the antioxidant activity of the isolated compounds, suggesting their therapeutic potential and use as quality control markers. <b>Conclusions:</b> Six bioactive compounds were identified and characterized, providing insights into their antioxidant potential and offering opportunities for further pharmacological investigation.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 1","pages":"53 - 64"},"PeriodicalIF":1.1,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143396572","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 Antimicrobial Evaluation of (E)-2-(4-((4-((1-(2,4-Dichlorophenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene)methyl)-2-methoxyphenoxy)methyl)-1H-1,2,3-triazol-1-yl)-N-phenylacetamide Derivatives","authors":"Cheryl T. Mascarenhas,&nbsp;Jaidip B. Wable,&nbsp;Hemantkumar N. Akolkar,&nbsp;Nirmala R. Darekar,&nbsp;Pradnya J. Prabhu","doi":"10.1134/S1068162025010091","DOIUrl":"10.1134/S1068162025010091","url":null,"abstract":"<p><b>Objective:</b> There has never been a compilation of (<i>E</i>)-2-(4-((4-((1-(2,4-dichlorophenyl)-3-methyl-5-oxo-1<i>H</i>-pyrazol-4(5<i>H</i>)-ylidene)methyl)-2-methoxyphenoxy)methyl)-1<i>H</i>-1,2,3-triazol-1-yl)-<i>N</i>-phenylacetamide derivatives produced before. For the synthesis of (<b>VIIa–VIIh</b>), (<i>E</i>)-1-(2,4-dichlorophenyl)-4-(3-methoxy-4-(prop-2-yn-1-yloxy)benzylidene)-3-methyl-1<i>H</i>-pyrazol-5(4<i>H</i>)-one (<b>V</b>) was utilized. <b>Methods:</b> The compounds were synthesized using the Click chemistry process. We used the tube-dilution approach to test for antimicrobial and antifungal activity. <b>Results and Discussion:</b> Mass spectrometry, ¹H, ¹³C NMR, and IR spectroscopy were used to validate the eight newly produced compounds. The antibacterial and antifungal properties of the new compounds were tested. While seven compounds ((<b>VIIa–VIIc</b>), (<b>VIIe–VIIh</b>)) demonstrated antimicrobial activity against a range of bacterial strains, including <i>Escherichia coli</i>, <i>Pseudomonas aeruginosa</i>, <i>Staphylococcus aureus</i>, and <i>Streptococcus pyogenes</i>, the activity was comparable to that of the drug ampicillin, whereas (<b>VIIh</b>) exhibited good antifungal activity compared to its standard drug Griseofulvin against <i>Candida albicans</i>. <b>Conclusions:</b> We conclude that the newly synthesized 1,2,3-triazoles showed good antibacterial activity and can be used as precursors for drug molecules in the future.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 1","pages":"151 - 159"},"PeriodicalIF":1.1,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143396448","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":"Analysis of the Content of Membrane Lipids of Mytilid Bivalve Mollusks and Strongylocentrotid Sea Urchins with Different Lifespans","authors":"A. L. Drozdov,&nbsp;T. V. Sikorskaya,&nbsp;V. P. Grigorchuk","doi":"10.1134/S1068162025010169","DOIUrl":"10.1134/S1068162025010169","url":null,"abstract":"<p><b>Objective:</b> In order to understand whether the lipid composition of the plasma membrane is related to the lifespan, we conducted a comparative study of the profiles of molecular species of four main classes of plasma membrane phospholipids (phosphatidylcholines (PC), phosphatidylethanolamines (PE), phosphatidylserines (PS), and phosphatidylinositols (PI)) for the long-lived mussel <i>Crenomytilus grayanus</i> and the long-lived sea urchin <i>Mesocentrotus nudus</i> and the short-lived mussel <i>Mytilus trossulus</i> and sea urchin <i>Strongylocentrotus intermedius</i>. <b>Methods:</b> The molecular profiles of these membrane lipids were determined using high-performance liquid chromatography in combination with high-resolution mass spectrometry. <b>Results and Discussion:</b> It was shown that the profile of PI molecular species is not related to the lifespan of the mussels and the sea urchins, in contrast to the profiles of PC, PE, and PS molecular species. Sea urchins <i>M. nudus</i> and mussel <i>C. grayanus</i> with longer lifespans were characterized by an increased content of PC, PE, and PS with odd-numbered alkyl/acyl chains, as well as of molecular species with arachidonic acid (20:4<i>n</i>-6), whose higher content can contribute to a better adaptation of the mussel <i>C. grayanus</i> and of the sea urchin <i>M. nudus</i> and, thereby, to a longer lifespan. <b>Conclusions:</b> The lipidomic approach to studying the gerontological problem using sea urchins and bivalves as an example has revealed a clear relationship between the profile of molecular species of the membrane lipids and the lifespan. The exact mechanisms of this relationship need to be further clarified.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"51 1","pages":"160 - 170"},"PeriodicalIF":1.1,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143396618","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}