Russian Journal of Bioorganic Chemistry最新文献

{"title":"Issues of the Structural Organization of Lignin and Prospects for Its Processing (A Review)","authors":"A. Yu. Kozhevnikov,&nbsp;S. L. Shestakov,&nbsp;Yu. A. Sypalova","doi":"10.1134/S1068162024070264","DOIUrl":"10.1134/S1068162024070264","url":null,"abstract":"<p>This article presents a review of the literature on studies of lignin, which is one of the most abundant biopolymers on Earth, basing on publications in the world’s most-cited sources. It is noted that, already nowadays, lignin is considered as a powerful renewable source of valuable organic raw materials, but the potential for lignin valorization is much broader than the presently exploited opportunities. Particular focus is placed on the structure and molecular organization of birch lignin; birch wood is actively used in chemical industry, while the literature on hardwood lignins is much scarcer compared to softwood lignins. The basic methods of structural investigation of such a complex and irregular polymer as lignin are discussed, and their advantages, disadvantages, and application prospects are analyzed. It is pointed out that, nowadays, the most effective methods for studying the lignin structural units are pyrolysis-gas chromatography and nuclear magnetic resonance spectroscopy. Various methods of lignin isolation from wood are described, and the influence of the isolation method on the structure of the isolated substance was evaluated. Also, the structural features of birch lignin and its distinctions from lignins of other species are shown.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 7","pages":"2675 - 2690"},"PeriodicalIF":1.1,"publicationDate":"2024-12-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142870437","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 Cytotoxicity Evaluation of 2-(4-((1,3-Dioxoisoindolin-2-yl)methyl)phenyl)-N-phenyl-thiazole-4-carboxamide Derivatives as Apoptosis Inducers with Potential Anticancer Effects","authors":"Leila Hosseinzadeh,&nbsp;Ghazal Mahmoudi,&nbsp;Masoumeh Mahsa Mohammadi,&nbsp;Amin Hosseini,&nbsp;Hossein Malekshahi,&nbsp;Alireza Aliabadi","doi":"10.1134/S1068162024060062","DOIUrl":"10.1134/S1068162024060062","url":null,"abstract":"<p><b>Objective:</b> Cancer chemotherapy for the discovery of new antineoplastic drugs is one of the updated areas of medical and pharmaceutical research. <b>Methods:</b> In the current project, a novel series of 1,3-thiazole derivatives were synthesized and their corresponding anticancer activity was evaluated by MTT assay using three cancer cell lines. A2780 (ovarian cancer), PC3 (prostatic carcinoma), and MCF-7 (breast cancer) were utilized for this purpose. Subsequently, Caspase-3 activation, mitochondrial membrane potential (MMP), and generation of reactive oxygen species (ROS) were also explored for some selected active compounds. <b>Results and Discussion:</b> Fortunately, tested compounds were so active against MCF-7 cells compared to other cell lines. Compounds (<b>VI</b>), (<b>VII</b>), (<b>VIII</b>), (<b>IX</b>), and (<b>XII</b>) enhanced Caspases-3 activity in the MCF-7 cell line that 3-Cl analog (<b>VII</b>) was illustrated as the most cytotoxic index against MCF-7 cells. This is while that among the above analogs (<b>VI–IX</b>), and (<b>XII</b>), just and just, 2-F derivative (<b>IV</b>) revealingly reduced the mitochondrial membrane potential (MMP). The current compounds demonstrated better anticancer activity compared to the other thiazole derivatives. Generally, derivatives bearing electron-withdrawing as well as electron-donating groups are active toward cancerous cell lines. <b>Conclusions:</b> The novel 1,3-thiazole derivatives presented in the current paper could be suggested as potential anticancer agents, especially against breast cancer.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2095 - 2106"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826349","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":"Novel Pyridazine-3(2H)-one Derivatives as SARS-CoV-2 Inhibitors: Design, Synthesis, Characterization, Molecular Docking, and Their In Silico ADMET Studies","authors":"Kilol M. Rabara,&nbsp;Jaydeep N. Lalpara,&nbsp;Gaurang G. Dubal","doi":"10.1134/S1068162024060086","DOIUrl":"10.1134/S1068162024060086","url":null,"abstract":"<p><b>Objective:</b> The objective of this study is to design and synthesize novel pyridazinone derivatives through Buchwald coupling reaction, followed by characterization using ¹H, ¹³C NMR, and LCMS. We aim to evaluate the potential antiviral activity of these compounds against SARS-CoV-2. <b>Methods:</b> The target protein 6LZG (SARS-CoV-2) was selected for docking studies. The synthesized compounds were docked using a molecular docking software, employing appropriate scoring functions, and parameters. Docking results were compared with those of the standard antiviral drug Remdesivir to evaluate relative potency. <b>Results and Discussion:</b> The molecular docking results indicated that the compound (VIIc) and (VIIe) displayed significant binding affinities for the SARS-CoV-2 protein 6LZG. Comparative analysis showed that compound (VIIc) and (VIIe) outperformed the standard drug Remdesivir in terms of binding energy, suggesting a potentially greater efficacy against the virus. <i>In silico</i> ADMET studies demonstrated favorable pharmacokinetic profiles for the synthesized compounds.<b> Conclusions:</b> The study highlights the promising antiviral activity of the synthesized pyridazinone derivatives against SARS-CoV-2.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2149 - 2161"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826300","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":"Non-Agglomerated Oligonucleotide-Containing Nanocomposites Based on Titanium Dioxide Nanoparticles","authors":"M. N. Repkova,&nbsp;O. Yu. Mazurkov,&nbsp;E. I. Filippova,&nbsp;N. A. Mazurkova,&nbsp;Yu. E. Poletaeva,&nbsp;E. I. Ryabchikova,&nbsp;B. F. Zarytova,&nbsp;A. S. Levina","doi":"10.1134/S1068162024060384","DOIUrl":"10.1134/S1068162024060384","url":null,"abstract":"<p><b>Objective:</b> Stability and monodispersity are important properties of nanoparticles and nanocomposites, that ensure the reliability of their application in biological systems and the reproducibility of results. The preparation of non-agglomerated oligonucleotide-containing nanocomposites based on anatase titanium dioxide nanoparticles (Ans~ODN) is the aim of this study. <b>Methods:</b> The immobilization of oligodeoxynucleotides on TiO₂ nanoparticles was studied by dynamic light scattering and transmission electron microscopy. The antiviral activity of the synthesized samples was evaluated against VERO cells infected with herpes simplex virus type 1. <b>Results and Discussion:</b> The effect of NaCl on the agglomeration of the nanoparticles and the nanocomposites in aqueous solutions was studied. The presence of NaCl leads to agglomeration of the nanoparticles and the nanocomposites. It was shown that the nanocomposites are formed in an aqueous solution in the absence of NaCl. A comparison of the biological activities of the nanocomposites prepared in water and in saline solution was carried out on the example of inhibition of replication of the herpes simplex virus type 1 in the cell culture. The studied nanocomposite, regardless of the preparation method (in water or in 0.9% NaCl), inhibited virus replication by 4.5 orders of magnitude when used 1 day after preparation. After 10 days of storage, the activity of the sample prepared in saline solution was two orders of magnitude lower than that of the active sample prepared in water. <b>Conclusions:</b> We have developed a method for the preparation of non-agglomerated oligonucleotide-containing nanocomposites based on anatase nanoparticles and demonstrated their potential use for the study of their biological activity. Unlike nanocomposites prepared in the presence of the salt, which lose their efficacy during storage, nanocomposites that are not prone to agglomeration can be obtained in water for future use.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2634 - 2643"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826091","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":"Acute Toxicity Evaluation of Pyridine Derivatives of 3,4-Dihydroquinoxalin-2-one and 3,4-Dihydro-2H-1,4-benzoxazin-2-one","authors":"S. A. Ternovskaya,&nbsp;V. S. Vlasenko,&nbsp;A. N. Novikov,&nbsp;N. A. Dengis,&nbsp;A. L. Stalinskaya,&nbsp;I. V. Kulakov","doi":"10.1134/S1068162024060268","DOIUrl":"10.1134/S1068162024060268","url":null,"abstract":"&lt;p&gt;&lt;b&gt;Objective:&lt;/b&gt; Compounds containing the quinoxaline and oxazine core have a diverse spectrum of biological activity, including antibacterial, antiviral, antitumor, antituberculosis, anti-inflammatory, and others. The introduction of a new pharmacophoric pyridine component into these derivatives can enhance the biochemical activity and metabolic stability of the resulting substance, increase cell permeability, and improve pharmacokinetic and pharmacodynamic properties. Previously, a number of pyridine derivatives of quinoxaline and oxazine were found to have pronounced and moderate antituberculosis, antibacterial, antifungal, and analgesic properties &lt;i&gt;in vitro&lt;/i&gt;. In this regard, the aim of this study is to evaluate the acute toxicity of bis(3,4-dihydroquinoxalin-2-one) and bis(3,4-dihydro-2&lt;i&gt;H&lt;/i&gt;-1,4-benzoxazin-2-one) derivatives upon intraperitoneal administration to guinea pigs. &lt;b&gt;Methods:&lt;/b&gt; The acute toxicity of the bis-derivatives synthesized on the basis of 3,5-diacetyl-2,6-dimethylpyridine was studied after a single intraperitoneal administration to guinea pigs (6 groups of 6 individuals) at doses of 100, 200, and 400 mg/kg. The control group was group 7, which received 1.0 mL of physiological solution. Observation was carried out for 14 days. In the next stage, on the 15th day of the experiment, blood was collected for hematological and biochemical studies from the guinea pigs that were intraperitoneally administered with the test compounds, as well as from the guinea pigs of the control group. &lt;b&gt;Results and Discussion:&lt;/b&gt; It was established that, according to K.K. Sidorov’s classification, pyridine derivative (3&lt;i&gt;Z&lt;/i&gt;,3′&lt;i&gt;Z&lt;/i&gt;)-3,3′-[(2,6-dimethylpyridin-3,5-diyl)bis(2-oxoethane-2-yl-1-ylidene)]bis(3,4-dihydroquinoxalin-2(1&lt;i&gt;H&lt;/i&gt;)-one) had low toxicity, as evidenced by the absence of lethal outcomes from its administration to animals in the range of 100–400 μg/kg, which, however, was accompanied by signs of nervous disorder regardless of the dose of the compound, which disappeared within 24 h. When the guinea pigs were inoculated with another pyridine derivative, (3&lt;i&gt;Z&lt;/i&gt;,3′&lt;i&gt;Z&lt;/i&gt;)-3,3′-[(2,6-dimethylpyridin-3,5-diyl)bis(2-oxoethane-2-yl-1-ylidene)]bis(3,4-dihydro-2&lt;i&gt;H&lt;/i&gt;-1,4-benzoxazin-2-one), more pronounced and prolonged signs of intoxication were observed as manifested by convulsive twitching of the hind limbs, decreased mobility, and a slow reaction to environmental stimuli, followed by the death of 33% of animals, when the compound was administered at a dose of 100 mg/kg, 66% at a dose of 200 mg/kg, and 100% at a dose of 400 mg/kg. The hematological and biochemical studies conducted on the 15th day after the administration of the test compounds showed the absence of significant deviations from normal physiological values, despite the presence of a reliable difference in individual indicators compared to the control group.&lt;b&gt; Conclusions:&lt;/b&gt; Thus, the acute toxicity parameters of the test compounds were o","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2627 - 2633"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826090","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":"Exploring the Mechanisms of Indole-Oxadiazole Benzamide Hybrids as Tyrosinase Inhibitors: Insights from Lineweaver-Burk Plot Analysis and Computational Studies","authors":"M. Nazir,&nbsp;U. Khan,&nbsp;M. Jahangir,&nbsp;K. Hayat,&nbsp;S. A. R. Bokhari,&nbsp;A. Shakoor,&nbsp;E. Ahmad,&nbsp;H. M. F. Haider","doi":"10.1134/S106816202406013X","DOIUrl":"10.1134/S106816202406013X","url":null,"abstract":"<p><b>Objective:</b> This study aimed to synthesize hybrid compounds incorporating indole, oxadiazole, and benzamide moieties, leveraging their known biological activities, to evaluate their potential as tyrosinase inhibitors.<b> Methods:</b> A convergent synthetic approach was employed to develop the hybrid compounds. Structural confirmation was achieved through infrared spectroscopy (IR), proton nuclear magnetic resonance (¹H NMR), carbon nuclear magnetic resonance (¹³C NMR), and elemental analysis (CHN). The inhibitory effects on tyrosinase were assessed using enzyme kinetics, with Lineweaver-Burk plots utilized to determine the mechanism of inhibition.<b> Results and Discussion:</b> The synthesized bi-heterocyclic benzamides demonstrated excellent inhibitory activities against tyrosinase compared to the standard control. Compound (<b>VIIIf</b>) exhibited non-competitive inhibition, forming an enzyme-inhibitor complex, with an inhibition constant (<i>K</i>_i) of 0.0033 µM. Computational analysis indicated favorable binding energy values for these compounds. The study highlights the promising potential of these hybrid molecules as effective tyrosinase inhibitors. The structure-activity relationship analysis suggests that the incorporation of indole, oxadiazole, and benzamide moieties enhances the inhibitory efficacy against tyrosinase, which is crucial for developing treatments for skin disorders.<b> Conclusions:</b> The synthesized indole-oxadiazole-benzamide hybrids are identified as potent tyrosinase inhibitors with significant potential as medicinal scaffolds for treating skin conditions. Further investigations into their therapeutic applications are warranted.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2325 - 2343"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826255","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":"Molecular Biological Approaches to Human Oocyte Developmental Competence Prognosis","authors":"A. R. Smolyaninova,&nbsp;E. O. Bashendjieva,&nbsp;N. V. Ponomartsev,&nbsp;D. I. Ostromyshenskii,&nbsp;J. A. Tatishcheva,&nbsp;A. S. Kalugina,&nbsp;N. I. Enukashvily","doi":"10.1134/S1068162024090012","DOIUrl":"10.1134/S1068162024090012","url":null,"abstract":"<p><b>Objective:</b> Cumulus cells respond to the effects of hormones and signalling molecules synthesised by the oocyte by changing their expression profile. In turn, cumulus cells control the growth and maturation of the oocyte. Therefore, analysis of the transcriptional profile of cumulus cells is likely to be one of the approaches for non-invasive prediction of oocyte quality in assisted reproductive technology programs. To evaluate the expression of selected genes in cumulus cells in women with primary and secondary types of infertility with positive and negative results of assisted reproductive technologies. <b>Methods:</b> 9 healthy donors and 19 patients undergoing infertility treatment with ART methods participated in the study. RNA was isolated from cumulus cells obtained during oocyte preparation for fertilisation, and cDNA was synthesised and used as a matrix for real-time PCR with primers for AREG, SCD4, PTGS, SCD5, HAS2, VCAN, STAR and two lncRNA genes (ANXA2P2, MALAT1). <b>Results and Discussion:</b> The genes of interest expression did not depend on the type of infertility but rather on the IVF attempt outcome. The panel of mRNA biomarkers (<i>SDC4</i>^up<i>AREG</i>^up<i>MALAT1</i>^{not changed}<i>ANXA2P2</i>^{not changed} ) was associated with poorer oocyte competence prognosis and <i>SDC4</i>^{not changed}<i>AREG</i>^down<i>MALAT1</i>^down<i>ANXA2P2</i>^down set of biomarkers was associated with better quality of oocytes. <b>Conclusions:</b> This non-invasive method can be used to access oocyte quality in patients with primary and secondary infertility.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2499 - 2508"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826088","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":"Structural Analysis of the LZTFL1 Protein by Principal Component Analysis (PCA-seq)","authors":"I. I. Khegai,&nbsp;X. Yu,&nbsp;V. M. Efimov","doi":"10.1134/S1068162024060244","DOIUrl":"10.1134/S1068162024060244","url":null,"abstract":"<p><b>Objective:</b> The single-nucleotide mutation rs17713054G&gt;A in the promoter region of <i>LZTFL1</i> (leucine zipper transcription factor like 1) gene is a factor in the severe course of coronavirus infection COVID-19. Structure of coded protein is not studied well still. <b>Methods:</b> We used the principal component analysis (PCA-seq) for computer statistical analysis of protein LZTFL1 aminoacid sequence. <b>Results and Discussion:</b> It is revealed that the presence of a high correlation between the first principal component of the translated amino acid sequence and eleven amino acid indices of the AA-index database, characterizing the physicochemical and biochemical properties of the protein. The indices BEGF750102, CHOP780209, PALJ810110, GEIM800107, QIAN880121, LEVM780102, PRAM900103 are associated with β-folding parameters. The LZTFL1 protein is part of the Bardet-Biedl Syndrome (BBS) protein complexes that regulate intracellular transport in the ciliated epithelium of the lungs. <b>Conclusions:</b> It is assumed that the presence of β-sheet elements in the structure of the LZTFL1 protein plays an important role in ACE2 receptor-mediated endocytosis, stimulating the rate of angiotensin-converting enzyme 2 recycling and accelerating the delivery of adherented coronavirus SARS-CoV-2 virions into the cell followed by the initiation of severe acute respiratory syndrome COVID-19.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2611 - 2617"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826105","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":"Investigation of Novel Thiazolin-2,4-diones: Synthesis, Biological Evaluation, and Docking Studies for Enhanced Insights","authors":"M. Yadav,&nbsp;R. Dinkar,&nbsp;S. N. Mali,&nbsp;S. Sharma,&nbsp;A. Jain","doi":"10.1134/S1068162024060220","DOIUrl":"10.1134/S1068162024060220","url":null,"abstract":"<p><b>Objective:</b> A newer series of compounds, including 3-benzoyl-5-(substituted-benzylidin)-thiazolidin-2,4-dione (<b>IVa–IVh</b>) and 3-<i>p</i>-tolyl-5-(substituted-benzylidine)-thiazolidin-2,4-dione (<b>Va–Vh</b>), were synthesized through a nucleophilic reaction involving benzoyl chloride and <i>p</i>-chlorotoluene. These compounds were obtained in conjunction with various 5-(substituted-benzylidine)-thiazolidin-2,4-dione derivatives, which were prepared by condensing thiazolidin-2,4-dione with different substituted benzaldehydes. Comprehensive structural characterization was achieved through UV, FT-IR, ¹H NMR, and mass spectroscopy. <b>Methods:</b> Antimicrobial assessment was conducted against a panel of bacterial strains including <i>E. coli</i>, <i>S. aeruginosa</i>, <i>S. aureus</i>, and <i>B. subtilis</i>, as well as fungal strains <i>A. niger</i> and <i>C. albicans</i>. Molecular docking studies were employed to further validate the results. Anticancer activity was evaluated using the sulforhodamine B (SRB) assay on the HEPG2 cell line. <b>Results and Discussion:</b> The synthesized compounds demonstrated significant antibacterial activity against <i>E. coli</i>, <i>S. aeruginosa</i>, <i>S. aureus</i>, and <i>B. subtilis</i>. Furthermore, notable antifungal activity was observed against <i>A. niger</i> and <i>C. albicans</i>. Compound (<b>Vd</b>) displayed exceptional performance in both aspects, confirmed by molecular docking. Additionally, (<b>IVc</b>), (<b>Vc</b>), (<b>IVh</b>), and (<b>Vh</b>) exhibited significant anticancer activity, while (<b>IVd</b>) exhibited moderate activity at varying concentrations. <b>Conclusions:</b> The newly synthesized compounds exhibit promising antimicrobial and anticancer properties, indicating their potential for pharmaceutical applications. This research represents a significant advancement in medicinal chemistry, offering avenues for further drug development and exploration in the field.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2219 - 2239"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826172","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":"Blood Erythrocytes—a Biological Model for Evaluating Antioxidant Activity of Chemical Compounds (A Review)","authors":"O. G. Shevchenko","doi":"10.1134/S1068162024060323","DOIUrl":"10.1134/S1068162024060323","url":null,"abstract":"<p>This review presents an analysis of literature, including our own work, on various aspects of using red blood cells (RBCs) as an <i>in vitro</i> model in the comprehensive evaluation of antioxidant activity of a wide range of natural and synthetic compounds, their mixtures, and plant extracts. The characteristics of the most commonly used initiators of oxidative stress in such studies, 2,2′-azobis(2-amidinopropane) dihydrochloride (AAPH) and H₂O₂, as well as the mechanisms underlying the development of the hemolytic process are discussed. A critical analysis of methodological approaches to assessing the level of hemolysis is provided. The review further discusses the evaluation of erythrocyte survival under oxidative stress conditions and the ability of the tested compounds to act as membrane protectors. The review considers the criteria for a comprehensive assessment of erythrocytes, facilitating the study of cellular, and molecular mechanisms underlying antioxidant activity of a wide range of substances in a model of oxidative hemolysis of erythrocytes. Traditional methods include assessment of the intensity of membrane lipid peroxidation (LPO) processes through measurement of concentration of products that react with 2-thiobarbituric acid, as well assessment of relative content of oxidized forms of hemoglobin in erythrocytes. The use of modern fluorescent methods is another promising approach. In particular, the fluorescence of heme degradation products, the decrease in intensity of which can indicate antioxidant activity in the investigated compounds, is a sensitive marker of oxidative stress in erythrocytes. Another prominent fluorescent method is the assessment of oxidative stress level by measuring the intracellular concentration of ROS in erythrocytes. Analysis of our own and literature data allows us to recommend to use the method of oxidative hemolysis of erythrocytes to screen newly developed compounds in order to select the most interesting candidates for further in-depth studies. This method is appropriate for establishing the structure-activity relationship and developing a strategy for the targeted synthesis of new biologically active compounds combining high hemocompatibility and antioxidant activity, which are promising for biomedical applications.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2191 - 2208"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826212","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}