Russian Journal of Bioorganic Chemistry最新文献

{"title":"Design, Synthesis, and Biological Evaluation of 7-Chloroquinoline Derivatives Against Mycobacterium tuberculosis H37Rv","authors":"S. G. Alegaon,&nbsp;J. Chand,&nbsp;S. Gharge,&nbsp;R. S. Kavalapure,&nbsp;S. D. Ranade,&nbsp;D. Sriram,&nbsp;M. Singh,&nbsp;N. R. Sutar,&nbsp;G. A. Govind","doi":"10.1134/S1068162025601806","DOIUrl":"10.1134/S1068162025601806","url":null,"abstract":"<p><b>Objective:</b> To identify and evaluate novel 7-chloroquinoline-based derivatives as potential inhibitors of <i>Mycobacterium tuberculosis</i> H37Rv. <b>Methods:</b> A series of 7-chloroquinoline derivatives (<b>IVa–IVn</b>) was designed using a structure-based drug design approach. The compounds were synthesized and purified following standard organic synthesis procedures. <i>In vitro</i> biological activity was assessed through whole-cell screening using the microplate Alamar Blue assay (MABA) to determine minimum inhibitory concentrations (MIC) and half-maximal inhibitory concentrations (IC₅₀). Computational studies, including molecular docking, molecular dynamics (MD) simulations, and MM-GBSA free energy calculations, were performed to elucidate binding interactions and complex stability. Quantum chemical calculations were also conducted to investigate the electronic properties and conformational preferences of the most active compounds. <b>Results and Discussion:</b> Among the synthesized derivatives, compounds <b>IVm</b>, <b>IVl</b>, and <b>IVn</b> demonstrated potent antitubercular activity with IC₅₀ values ranging from 0.7 to 25 µg/mL. Notably, compounds <b>IVm</b> and <b>IVl</b>, bearing 4-methylthiophene and 4-bromothiophene substituents, respectively, exhibited the highest activity, with MIC values of 0.7 and 3.1 µg/mL. Molecular docking studies revealed that <b>IVm</b> forms stable interactions with key residues ARG324 and TYR60 in the active site, yielding a docking score of –8.44, glide energy of –71.24 kcal/mol, and an MM-GBSA Δ<i>G</i>_bind of –72.41 kcal/mol. MD simulations confirmed the stability of the <b>IVm</b>–protein complex, while quantum chemical analysis provided insights into the conformational features contributing to the observed activity. <b>Conclusions:</b> The integrated <i>in vitro</i> and <i>in silico</i> approach successfully identified 7-chloroquinoline derivatives, particularly <b>IVl</b> and <b>IVm</b>, as promising lead compounds for further optimization in antitubercular drug discovery. These findings contribute valuable insights into quinoline-based drug design and support the continued exploration of thiophene-substituted analogs for tuberculosis therapy.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 5","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148459180","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":"Acylthioureas Based on Ursane-Type Amines: Synthesis and Study of Anti-Inflammatory and Cytotoxic Properties","authors":"S. A. Popov,&nbsp;T. D. Borisova,&nbsp;E. E. Shults,&nbsp;D.A. Kiseleva,&nbsp;M. K. Marenina,&nbsp;Yu. V. Meshkova,&nbsp;T. G. Tolstikova","doi":"10.1134/S106816202560477X","DOIUrl":"10.1134/S106816202560477X","url":null,"abstract":"<p><b>Objective:</b> The design of three small groups of ursane acylthioureas containing terpenyl-carbamothioyl fragments and study of their anti-inflammatory and cytotoxic activity is presented. <b>Methods:</b> A series of 15 terpene acylthioureas were synthesized by condensation of three ursane primary amino derivatives holding amino groups at different distances from the triterpene skeleton with aromatic acyl isothiocyanates. The anti-inflammatory activity of the new compounds was studied in a histamine-induced inflammation model in male CD-1 mice. The cytotoxicity of hybrids was tested on tumor cells MCF7, HepG2, HeLa and hTERT-BJ1 (non-cancer control, fibroblasts). <b>Results and Discussion:</b> An anti-inflammatory effect significantly superior to that of ursolic acid was observed for a group of 28-norursane hybrids. The presence of a –CH₂– linker between the triterpene backbone and the carbamothioyl moiety significantly reduced the anti-inflammatory effect. Compounds with a – COOCH₂CH₂– linker demonstrated enhanced histamine phlogogen activity. An MTT assay on MCF7, HepG2, and HeLa tumor cells, as well as on hTERT-BJ1 cells, revealed insignificant or no cytotoxicity for all derivatives. <b>Conclusions:</b> Novel acylthioureas with terpenyl-carbamothioyl fragments are promising as synthons for heterocyclic hybrid compounds, the preparation of metal complexes, and further study of the properties and mechanisms of anti-inflammatory activity.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 4","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148380621","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":"Red Shift of the Absorption Maximum of Mutant Exiguobacterium sibiricum Proteorhodopsin: Influence of Amino Acid Substitutions in Helices E and F","authors":"L. E. Petrovskaya,&nbsp;E. P. Lukashev,&nbsp;E. A. Kryukova,&nbsp;D. A. Dolgikh,&nbsp;M. P. Kirpichnikov","doi":"10.1134/S1068162026601242","DOIUrl":"10.1134/S1068162026601242","url":null,"abstract":"<p><b>Objective:</b> To engineer a mutant variant of the <i>Exiguobacterium sibiricum</i> proteorhodopsin (ESR) by introducing amino acid substitutions in helices E and F, based on the carotenoid-binding site of xanthorhodopsin (XR) from <i>Salinibacter ruber</i>, and to investigate the effects of these mutations on the absorption spectrum, photocycle kinetics, and carotenoid-binding ability. <b>Methods:</b> Three mutant variants were constructed: Car3 (substitutions Y147G, C151T, W154F in helix E), Car4 (substitution of fragment A199-L202 in helix F with the corresponding XR fragment M208-M211), and Car5 (combining both modifications). Genes were obtained by SOE-PCR and expressed in <i>E. coli</i>. Proteins were purified by metal-affinity chromatography. Absorption spectra were recorded at pH 5–9, and photocycle kinetics were measured at 410, 510, 550, and 590 nm using laser flash photolysis. Carotenoid binding was tested by co-expression of the rhodopsin genes with carotenoid biosynthesis genes. <b>Results and Discussion:</b> Car5 exhibited a red shift of 9–16 nm compared to wild-type ESR across pH 5–9 (e.g., 542 nm at pH 7), while Car3 and Car4 showed no substantial shift. The pH dependence of Car5's absorption maximum revealed two transitions: a red shift from 538 to 550 nm (pKa 3.9) and a blue shift to 535 nm (p<i>K</i>_a 6.8). This contrasts with wild-type ESR, which exhibits only blue shifts (p<i>K</i>_a 6.0 and 9.1) and no red shift in this pH range. In the photocycle, Car5 formed the M intermediate already at pH 8 (unlike wild type), with faster M formation and decay at pH 9. Car5 also lacked the slow component of M formation observed in Car3, Car4, and wild type. No carotenoid binding was detected for Car3 or Car5, suggesting that additional mutations are required. These changes likely arise from altered electrostatic interactions and protonation states of the Schiff base counterion (D85 and H57), as well as conformational adjustments near the retinal β-ionone ring. <b>Conclusions:</b> Combined mutations in helices E and F of ESR produce a significant red shift in the absorption maximum and alter photocycle kinetics, shifting M intermediate formation to lower pH. These findings contribute to the rational design of microbial rhodopsins with tailored spectral properties for optogenetic applications. However, creation of a functional carotenoid-binding site in ESR requires further mutagenesis.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 4","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148380622","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":"8-Oxo-2′-deoxyguanosine: From Oxidative Stress Marker to Epigenetic Regulator","authors":"V. G. Snyga,&nbsp;V. Yu. Savitskaya,&nbsp;E. S. Gromova,&nbsp;M. I. Zvereva,&nbsp;T. S. Oretskaya,&nbsp;E. A. Kubareva","doi":"10.1134/S1068162025604720","DOIUrl":"10.1134/S1068162025604720","url":null,"abstract":"<p>8-Oxo-2′-deoxyguanosine (8-oxoG) is one of the most common and biologically significant oxidative lesions of heterocyclic bases in DNA, caused by reactive oxygen and nitrogen species. Its accumulation leads to genomic instability and the development of a wide range of pathologies, including cancer, neurodegenerative, and cardiovascular diseases, making 8-oxoG a universal marker of oxidative stress. The presence of this modification in the DNA template strand promotes base pairing errors during replication, enhancing mutagenesis. Conversely, 8-oxoG is removed by the enzyme 8-oxoguanine DNA glycosylase during base excision repair, the effectiveness of which is determined by the local structural and epigenetic context of DNA. Modern detection methods have shown that 8-oxoG accumulates in GC-rich promoters and regulatory regions, where its presence can influence G-quadruplex formation, cytosine methylation, and gene transcriptional activity. Thus, 8-oxoG is considered not only as a marker of oxidative stress but also as a potential element of epigenetic regulation. This review focuses on current understanding of the mutagenic and regulatory potential of 8-oxoG, as well as the influence of modified units and structural features – from canonical duplexes to non-canonical structures and chromatin – on replication and repair processes, gene expression, and DNA methylation.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 4","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148380146","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":"Synthetic Transformations of Higher Terpenoids. 46. Synthesis and Cytotoxic Properties of 16-(1,2,4-Oxadiazolyl)lambertianic Acid Derivatives","authors":"Yu. V. Kharitonov,&nbsp;M. K. Marenina,&nbsp;Yu. V. Meshkova,&nbsp;T. G. Tolstikova,&nbsp;E. E. Shults","doi":"10.1134/S1068162025604689","DOIUrl":"10.1134/S1068162025604689","url":null,"abstract":"<p><b>Objective:</b> Design, synthesis and cytoxic properties of a series of new derivatives of lambertianic acid with 1,2,4-oxadiazole substituent in the Furan ring and amido function at C4 position of the labdane core are presented. <b>Methods:</b> The three step formation of original lambertianic acid nitrile and its reaction with hydroxylamine hydrochloride followed by reaction of diterpenoid 16-amidooxime with activated carboxylic acids or a wide variety of their derivatives and cyclodehydration was used for the preparation of 16-(5-substituted-1,2,4-oxadiazolyl)lambertianic acid derivatives. The reaction of <i>in situ</i> generated oxadiazolyl modified lambertianic acid chloroanhydrides with hydroxylamine hydrochloride, hydrochloride of glycyne methyl ester or morpholine was used for selective modification of the diterpenoids in the C4 position. The screening <i>—itro</i> was used for studying the cytotoxicity of new compounds (MTT test). <b>Results and Discussion:</b> The obtained diterpenoid-type 1,2,4-oxadiazoles include compounds with phenyl, 4-fluoro-, 4-methyl-, 4-methoxy-, 3,4,5-trimethoxy-, 2-amino-, 3-amino- and 4-aminophenyl substituents, methyl, trifluoromethyl, <i>tert</i>-butyl and vinyl groups and also with a fragment of shikimic acid. <b>Conclusions:</b> We demonstrated that the introduction of a 1,2,4-oxadiazole substituent into the furan cycle of lambertianic acid, as well as the subsequent modification of the carboxyl group with the introduction of an oxime function, can significantly increase the cytotoxic effect against human MCF7 tumor cells. The results confirm the potential of targeted modification of the plant diterpenoid lambertianic acid for the creation of selective antitumor agents.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 4","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148380623","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":"Co-Administration of mRNAs Encoding HA, M1, and NP Antigens of the Influenza Virus Leads to the Formation of Virus-Like Particles and an Enhanced Immune Response","authors":"O. V. Markov,&nbsp;M. V. Sergeeva,&nbsp;D. N. Shcherbakov,&nbsp;D. N. Antropov,&nbsp;E. P. Goncharova,&nbsp;E. S. Zhuravlev,&nbsp;A. S. Dome,&nbsp;A. S. Fomin,&nbsp;S. I. Gayvoronsky,&nbsp;K. S. Kudrya,&nbsp;A. A. Isaeva,&nbsp;E. A. Volosnikova,&nbsp;A. V. Chechushkov,&nbsp;E. V. Shmendel,&nbsp;P. A. Puchkov,&nbsp;Y. E. Poletaeva,&nbsp;E. S. Ryabova,&nbsp;M. A. Maslov,&nbsp;V. V. Koval,&nbsp;G. A. Stepanov","doi":"10.1134/S1068162025604203","DOIUrl":"10.1134/S1068162025604203","url":null,"abstract":"<p><b>Objective:</b> Influenza remains a serious global health threat due to viral variability and limitations of current vaccines. This study developed an mRNA vaccine encoding three influenza A virus antigens: hemagglutinin (HA), nucleoprotein (NP), and matrix protein (M1). <b>Methods:</b> The mRNA was encapsulated in liposomes for efficient delivery. Mice received two immunizations: one group received HA alone (30 μg), while the other received a combination of HA + NP + M1 (10 μg each). Electron microscopy was used to confirm the formation of virus-like particles (VLPs). <b>Results and Discussion:</b> The trivalent vaccine induced higher antibody titers (geometric mean titer 4677 vs 3243) compared to the monovalent HA vaccine. Electron microscopy confirmed the formation of VLPs upon co-expression of HA, NP and M1, which enhanced immune responses. Against heterologous A/WSN/1933 (H1N1) challenge, the trivalent vaccine provided 83% survival, compared to only 50% with the monovalent vaccine. <b>Conclusions:</b> These results demonstrate the promise of VLP-based mRNA vaccines for protection against diverse influenza strains.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 4","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148380624","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":"Alterations of Tryptophan Metabolism Pathways in Immunoglobulin A Nephropathy: an Exploratory Study","authors":"E. I. Savelieva,&nbsp;M. D. Shachneva,&nbsp;T. I. Alyushina,&nbsp;Z. K. Kochoyan,&nbsp;O. V. Galkina,&nbsp;V. A. Dobronravov","doi":"10.1134/S106816202560463X","DOIUrl":"10.1134/S106816202560463X","url":null,"abstract":"<p><b>Objective:</b> Dysregulation of tryptophan metabolism can play a significant role in the pathogenesis of various diseases, including chronic kidney diseases, among which immunoglobulin A nephropathy (IgAN) is the most common form of primary glomerulopathy in young and middle-aged people. Analysis of tryptophan metabolism disorders may be useful for precision diagnosis of IgAN and identification of additional molecular targets for disease therapy. <b>Methods:</b> High-performance liquid chromatography with mass spectrometric detection was used to measure the concentrations of tryptophan and its metabolites: 5-hydroxytryptophan, kynurenine, kynurenic, indoleacetic, and indolelactic acids in blood serum samples from patients diagnosed with IgAN with disease activity (IgAN-A, <i>n</i> = 85) and in remission (IgAN-R, <i>n</i> = 28), as well as in blood serum samples from healthy volunteers (K1, <i>n</i> = 33) and patients with other kidney diseases (K2, <i>n</i> = 31). Untargeted and targeted metabolomic analysis were performed. <b>Results and Discussion:</b> Untargeted and targeted metabolomic analysis showed that significant changes in tryptophan metabolism in IgAN are associated with activation of the kynurenine and serotonin pathways. <b>Conclusions:</b> The conducted exploratory study indicates the need for additional research to study the relationship between the pathogenesis of IgAN and tryptophan metabolism.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 4","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148380147","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":"Mutant Forms of Nucleoside Phosphorylases and Other Nucleic Acid Metabolism Enzymes for the Optimization of Cascade Synthesis of Modified Nucleosides","authors":"E. A. Zayats,&nbsp;Y. A. Abramchik,&nbsp;M. A. Kostromina,&nbsp;I. D. Konstantinova,&nbsp;R. S. Esipov","doi":"10.1134/S1068162025604471","DOIUrl":"10.1134/S1068162025604471","url":null,"abstract":"<p>Modified nucleoside drugs are used in clinical practice to treat oncohematological diseases (nelarabine, fludarabine, cladribine, clofarabine) and viral infections (vidarabine, ribavirin, etc.) in the human body. The development of efficient technologies for the production of pharmaceutical substances is an important task for medical biotechnology. There are two main approaches to the synthesis of modified nucleosides: chemical and enzymatic. Traditional chemical synthesis technologies are often complex, labor-intensive, and environmentally unfriendly. As an alternative, enzymatic synthesis using nucleoside phosphorylases and other nucleic acid metabolism enzymes allows the synthesis of nucleosides in one pot with exceptional stereo- and regioselectivity. The desired compounds can be obtained either through enzymatic transglycosylation or multienzymatic cascades, which allow synthesis to begin from pentofuranoses or other readily available substrates. In some cases, the narrow substrate specificity of natural biocatalysts and low stability under industrial conditions can become an obstacle for the enzymatic synthesis of modified nucleosides. This paper offers an overview of the reported examples of the application of rational design and directed evolution approaches for the optimization of nucleoside production. The review focuses on both monoenzymatic variants (nucleoside phosphorylases) and multienzyme cascades for the synthesis of modified nucleosides.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 4","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-07-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148380145","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":"Exosome-Derived miR-25-3p Inhibits Mitochondrial Damage by Targeting SOX4 and Attenuates Sepsis-Induced Myocardial Injury","authors":"Rong Huang,&nbsp;Jing Cao,&nbsp;Hongyan Zhao,&nbsp;Weirong Tao,&nbsp;Chao Xu","doi":"10.1134/S1068162025603027","DOIUrl":"10.1134/S1068162025603027","url":null,"abstract":"<p><b>Objective:</b> To investigate the regulatory role and underlying molecular mechanisms of exosomal miR-25-3p in the pathogenesis of sepsis-induced myocardial injury. <b>Methods:</b> Serum exosomes from patients with sepsis-associated myocardial injury (Sepsis-exo) and healthy controls (NC-exo) were isolated and characterized. Using LPS-stimulated AC16 cardiomyocytes as an <i>in vitro</i> model, we evaluated cell viability, apoptosis, mitochondrial function, and organelle dynamics. Bioinformatics tools were employed to predict miR-25-3p target genes, which were subsequently validated using luciferase reporter and RNA immunoprecipitation (RIP) assays. The cardioprotective effects of miR-25-3p were further evaluated <i>in vivo</i> using a cecal ligation and puncture (CLP) mouse model, characterized by echocardiography and histological (HE) staining. <b>Results and Discussion:</b> Sepsis-exo significantly exacerbated LPS-induced cardiomyocyte damage, characterized by decreased cell viability, increased apoptosis, and profound mitochondrial dysfunction. Notably, miR-25-3p was markedly downregulated in Sepsis-exo. Restoration of miR-25-3p levels effectively attenuated these pathological alterations, enhancing cell survival and preserving mitochondrial integrity. Mechanistically, miR-25-3p directly targets and negatively regulates SOX4 expression. Overexpression of SOX4 diminished the protective effects conferred by miR-25-3p. <i>In vivo</i>, administration of a miR-25-3p mimic improved cardiac function and significantly reduced myocardial injury markers. <b>Conclusions:</b> Our findings demonstrate that exosomal miR-25-3p protects against sepsis-induced myocardial injury by targeting SOX4 and maintaining mitochondrial homeostasis. Thus, miR-25-3p represents a promising therapeutic target for the management of sepsis-associated myocardial damage.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 4","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-06-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148281863","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":"Albumin Nanoparticles as a Carrier System for the Delivery of the Antiarrhythmic Drug Amiodarone","authors":"A. V. Doroshchenko,&nbsp;A. D. Lapanik,&nbsp;P. D. Orlova,&nbsp;A. V. Lopukhov,&nbsp;I. M. Le-Deygen,&nbsp;Yu. I. Oshchepkova,&nbsp;Sh. I. Salikhov,&nbsp;N. L. Klyachko","doi":"10.1134/S1068162025604926","DOIUrl":"10.1134/S1068162025604926","url":null,"abstract":"<p><b>Objective:</b> The study aimed to develop and characterize albumin-based nanoparticles loaded with the antiarrhythmic drug amiodarone to afford enhancement of therapeutic efficacy and reduction of systemic toxicity of the drug. <b>Methods:</b> Bovine serum albumin nanoparticles were synthesized by sequentially using the methods of desolvation, surface modification with cationic block copolymer PEG_5k-b-PLL₅₀, and crosslinking with 3,3′-dithiobis(sulfosuccinimidyl propionate) (DTSSP). The obtained nanoparticles were characterized by dynamic light scattering (DLS) and nanoparticle tracking analysis (NTA). The encapsulation efficiency (EE) and loading capacity (LC) were determined spectrophotometrically. Drug release kinetics were studied in <i>vitro</i> under physiological conditions. <b>Results and Discussion:</b> It was shown that the particles had a hydrodynamic size ranging from ~180 to ~250 nm. The ζ-potential values demonstrated high colloidal stability of the obtained systems. The loading capacity and encapsulation efficiency for amiodarone were 23.4 and 36.8%, respectively. <i>In vitro</i> release studies revealed a sustained release profile, with 55.8% of the drug released within 120 h. The release kinetics followed a first-order model, suggesting concentration-dependent drug desorption from the albumin matrix. <b>Conclusions:</b> The developed amiodarone-loaded albumin nanoparticles exhibit favorable physicochemical properties and prolonged release behavior, indicating their potential as a nanocarrier system for targeted delivery of amiodarone in antiarrhythmic therapy.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"52 4","pages":""},"PeriodicalIF":1.7,"publicationDate":"2026-06-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148281865","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}