Russian Journal of Bioorganic Chemistry最新文献

{"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}

{"title":"Synthesis and Cytotoxicity Evaluation of Maleopimaric and Dihydroquinopimaric Esters and Amides","authors":"E. V. Tretyakova,&nbsp;S. R. Sharafutdinova","doi":"10.1134/S1068162024060256","DOIUrl":"10.1134/S1068162024060256","url":null,"abstract":"<p><b>Objective:</b> The increasing social significance of antitumor drugs is associated with the high prevalence of oncological diseases and determines the need to search for and create new effective drugs. This study aims to synthesize, characterize, and evaluate the cytotoxicity potential of diterpene esters and amides (<b>I</b>–<b>XIII</b>) and (<b>XVII–XIX</b>). <b>Methods:</b> The acid chloride method was used to synthesize 1-, 1,4-, and 1,4,20- derivatives of methyl dihydroquinopimarate containing furan and indoleacetyl fragments (<b>I</b>–<b>V</b>) and C²⁰-amides of dihydroquinopimaric and maleopimaric acids containing linear, heterocyclic, and aromatic amine fragments (<b>VI</b>–<b>XIII</b>). The reaction of diethyl chlorophosphite with dihydroquinopimaric alcohols proceeds in the presence of dimethylaminopyridine in pyridine to give diethoxyphosphoryl derivatives (<b>XVII</b>–<b>XIX</b>). The structures of the synthesized compounds were confirmed by mass spectrometry and one- and two-dimensional NMR spectroscopy. Primary assessment of the <i>in vitro</i> cytotoxic activity of 16 synthesized compounds against a panel of 60 tumor cell lines was performed. <b>Results and Discussion:</b> It was found that the introduction of a diethoxyphosphoryl substituent in the C¹ position of the <i>E</i> ring of methyl dihydroquinopimarate and of a benzylamine fragment in the C²⁰ position of maleopimaric acid resulted in the preparation of compounds that showed a pronounced cytotoxic activity. <b>Conclusions:</b> Diethoxyphosphoryl derivatives (<b>XIX</b>) and (<b>XVII</b>), and benzylamide (<b>IX</b>) were found to be cytotoxic against one, seven, and four breast cancer, leukemia, nonsmall cell lung cancer, and melanoma and prostate cancer cell lines, respectively. The highest activity was demonstrated by maleopimaric acid benzylamide (<b>XIII</b>), which effectively inhibited the growth of 19 cell lines of eight cancer types and had a significant cytotoxic effect against all the studied leukemia cell lines. The resulting data show that the synthesized derivatives can be recommended for in-depth study and development of a promising group of cytotoxic drugs.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2618 - 2626"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826108","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":"Ultrasound Assisted Synthesis of Pyran Derivatives Catalysed by Uranyl Nitrate and Their Molecular Docking Against Glycogen Synthase Kinase-3 Beta Receptor","authors":"K. Venkatesan,&nbsp;T. Srinivasa Rao,&nbsp;V. Sridhar,&nbsp;J. Yacobe,&nbsp;T. V. V. Satyanarayana,&nbsp;M. Pasupathi","doi":"10.1134/S1068162024060050","DOIUrl":"10.1134/S1068162024060050","url":null,"abstract":"<p><b>Objective:</b> Green and medicinal chemistry share the common objective of creating easy-to-use, cost-effective catalytic systems using commonly available materials. To synthesize 4<i>H</i>-pyrans derivatives by one-pot chemical reaction of cycloalkanones, substituted aldehyde with malononitrile at conventional, and ultrasonic method using uranyl nitrate hexahydrate acting as a catalyst were produced pyrans derivatives (<b>IVa–IVj</b>) in good to high yields. <b>Methods:</b> The main benefits of this eco-friendly approach are its high efficiency, solvent-free or low solvent reaction conditions, ease of operation, and utilization of readily available catalysts. After conducting additional research on the binding manner of the contacts between the most active frameworks and the α-glucosidase active sites, docking analysis was carried out to investigate the α-glucosidase enzyme’s active cavity. <b>Results and Discussion:</b> Upon interpreting the data, it became evident that scaffolds (<b>IVa</b>) and (<b>IVc</b>) were the most effective inhibitors of α-glucosidase, exhibiting excellent binding contacts with the enzyme’s active region. <b>Conclusions:</b> We propose a simple and green synthetic methodology for the synthesis of pyran derivatives and the molecular docking experiments showed that these compounds are strongly bound to the protein-binding sites of glycogen synthase kinase-3 beta receptor.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2580 - 2588"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826164","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":"Production and Refolding of the Ligand-Binding Domain of TrkA Receptor with the Extracellular Juxtamembrane Region","authors":"D. R. Bedanokova,&nbsp;M. V. Goncharuk,&nbsp;A. V. Shabalkina,&nbsp;V. A. Lushpa,&nbsp;A. S. Arseniev,&nbsp;E. V. Bocharov,&nbsp;K. S. Mineev,&nbsp;S. A. Goncharuk","doi":"10.1134/S1068162024060232","DOIUrl":"10.1134/S1068162024060232","url":null,"abstract":"<p><b>Objective:</b> One of the major problems in the field of neurotrophin signaling is the role of Trk juxtamembrane regions. Here we present the production protocol of the d5 ligand-binding domain of TrkA with the full-length extracellular juxtamembrane region for structural studies. <b>Methods:</b> The protein was produced in <i>E. coli</i> cells. Protein purification included immobilized metal affinity and size-exclusion chromatography in the presence of urea. Refolding was performed using three approaches: dialysis, pulse and flash dilution. The quality of the final protein was assessed by gel filtration and NMR. <b>Results and Discussion:</b> We demonstrated that the obtained strain allows the production of milligram quantities of the target protein, including its isotope-labeled derivatives. A comparison of several refolding protocols revealed that dialysis and flash dilution are optimal, with the latter option being more economically feasible. <b>Conclusions:</b> Analysis of the final protein preparation showed that the proposed protein expression, purification, and refolding scheme allows the production of a highly purified protein suitable for structural and functional studies.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2589 - 2595"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826116","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 and Synthesis of Some New Quinoxaline-Thiazole-Benzamide Hybrids: In Vitro Anticancer Activity and Their Molecular Docking Studies","authors":"Gouthami Dasari,&nbsp;Madhuri Pandiri,&nbsp;Vinitha Badithapuram,&nbsp;Rajender Reddy Karnekanti,&nbsp;Jyothi Mandala,&nbsp;Srinivas Bandari","doi":"10.1134/S1068162024060104","DOIUrl":"10.1134/S1068162024060104","url":null,"abstract":"<p><b>Objective:</b> The quinoxaline compound with molecular formula C₈H₆N₂O, which shows a wide range of biological activities including antiviral, anticancer, antimicrobial, antituberculosis, and antileishmanial. <b>Methods:</b> As a part of our efforts to design new anticancer agents, in this study, we develop quinoxaline-thiazole-benzamide hybrids. The anticancer evolution of these hybrids was studied using the MTT assay method. <b>Results and Discussion:</b> The anticancer activity results exhibit that three compounds, 3,5-dimethoxy-<i>N</i>-(4-(2-oxo-1,2-dihydroquinoxaline-1-carbonyl)thiazol-2-yl)benzamide, 4-methoxy-<i>N-</i>(4-(2-oxo-1,2-dihydroquinoxa line-1-carbonyl)thiazol-2-yl)benzamide, and 3,4-dimethoxy-<i>N</i>-(4-(2-oxo-1,2-dihydroquinoxaline-1-carbonyl)thiazol-2-yl)benzamide were shown remarkable anticancer activity ranging from 1.23 to 1.96 µM, demonstrating greater potency than the standard drug. <b>Conclusions:</b> Finally, the <i>in silico</i> results are strongly supported by <i>in vitro</i> anticancer activity data and tyrosine kinase EGFR inhibitory activity assay results.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2171 - 2181"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826174","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":"Vitamin B12 in Drug Delivery Systems (A Review)","authors":"A. A. Skuredina,&nbsp;D. E. Ialama,&nbsp;I. M. Le-Deygen","doi":"10.1134/S1068162024060372","DOIUrl":"10.1134/S1068162024060372","url":null,"abstract":"<p>Vitamin B₁₂ is a vital biologically active compound for human and is involved in a wide range of metabolic processes. The widespread vitamin B₁₂ deficiency and vitamin’s low penetrating ability into cells determine the urgency of delivery systems development for the design of formulations with improved biopharmaceutical properties. This work provides a brief discussion of the main chemical and biochemical properties of the vitamin B₁₂, as well as considers oral, injectable and transdermal multicomponent dosage forms of vitamin B₁₂ that are aimed at solving the issue. Moreover, the literature analysis of the prospects of using vitamin B₁₂ as an auxiliary component for both passive and active delivery of other drug molecules, for example, peptide nucleic acids and antitumor drugs, is presented. The review describes in detail the types of proposed delivery systems for biologically active compounds, in which vitamin B₁₂ is one of the components.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2540 - 2557"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826222","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":"Covalent Epidermal Growth Factor Receptor (EGFR) Inhibitors in Targeted Therapy of Drug-Resistant Non-Small Cell Lung Cancer (A Review)","authors":"A. B. Shvetsov,&nbsp;A. V. Semenov","doi":"10.1134/S1068162024060347","DOIUrl":"10.1134/S1068162024060347","url":null,"abstract":"<p>Non-small cell lung cancer (NSCLC) is the main subtype of lung cancer and a common cause of cancer-related mortality worldwide. Mutations in the epidermal growth factor receptor (EGFR) gene play a leading role in the pathogenesis of NSCLC, causing its pathological activity. The first generation of EGFR inhibitors, acting reversibly, effectively block the effects of EGFR with activating mutations by competing with adenosine triphosphate for binding to the kinase. However, after several months of treatment, a secondary T790M mutation often occurs, causing resistance to subsequent therapy with these drugs. Effective inhibition of EGFR bearing the T790M mutation was possible due to second-generation inhibitors acting via a covalent mechanism. However, the second generation of covalent inhibitors has received limited use in therapy due to insufficient selectivity for EGFR T790M and a narrow therapeutic window. The discovery of covalent pyrimidine-based inhibitors has led to the emergence of a number of effective and safer third-generation drugs for the treatment of NSCLC with the EGFR T790M mutation. This review contains a brief description of first- and second-generation EGFR inhibitors and a detailed discussion of the main stages in the development of third-generation inhibitors. The main emphasis is placed on the identified “structure–activity” patterns. Data are provided on inhibitors that have received the status of approved drugs for the treatment of NSCLC. Promising directions for the development of novel EGFR inhibitors are indicated.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2283 - 2311"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826374","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":"Exopolysaccharide from Rhizopus nigricans Modulates Antitumor Immune Responses by Promoting Tumor-Associated Macrophage Polarization toward the M1 Phenotype in C57BL/6J Mice","authors":"Guozheng Qin,&nbsp;Ping Li,&nbsp;Mingrui Zhang,&nbsp;Zhengzhi Yu,&nbsp;Xuebin Shen,&nbsp;Wanyun Zhang,&nbsp;Yuyan Zhou,&nbsp;Pingchuan Yuan,&nbsp;Yuhan Yang,&nbsp;Chunyan Liu,&nbsp;Guodong Wang","doi":"10.1134/S1068162024060049","DOIUrl":"10.1134/S1068162024060049","url":null,"abstract":"<p><b>Objective:</b> Exopolysaccharide (EPS1-1) exhibits immunomodulatory and antitumor activities; however, its mechanism of action remains unknown. We determined the antitumor activity and whether EPS1-1 could enhance the shift of tumor-associated macrophages (TAMs) toward the M1 phenotype. <b>Methods:</b> The viability of MC-38 was assessed by the CCK-8 assay. The phagocytic activity of primary peritoneal macrophages (PEMs) was assayed by immunofluorescence microscopy and the levels of TNF-α, IL-6, and NO were tested by ELISA kits, and NO assay kit. M1 polarization was analyzed by flow cytometry and Immunofluorescence staining. <b>Results and Discussion:</b> The viability of MC-38 cells did not exhibit a significant difference (<i>p</i> &gt; 0.05). EPS1-1 significantly upregulated IL-6, TNF-α, and NO production as well as phagocytic activity. Furthermore, it significantly inhibited tumor growth (85.32%), increased the spleen and thymus indices, and elevated the proportion of M1 cells <i>in vitro</i> and <i>in vivo</i>. <b>Conclusions:</b> It indicated that EPS1-1 had no direct inhibitory effect on MC-38 cell viability, exhibited remarkable anti-tumor activity against MC-38 transplanted tumors, reduced the volume of transplanted tumors, and significantly activated TAMs polarization to an immunostimulatory M1 phenotype to modulate antitumor immune responses in C57BL/6J mice.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2519 - 2528"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826359","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":"Adjuvant Effect of Benzo(a)pyrene on Specific IgE Production and B-Cell Subpopulations in Lungs, Regional Lymph Nodes, and Spleen in Mouse Allergy Model","authors":"D. B. Chudakov,&nbsp;O. A. Shustova,&nbsp;M. A. Strel’tsova,&nbsp;A. A. Generalov,&nbsp;R. A. Velichinskii,&nbsp;O. D. Kotsareva,&nbsp;G. V. Fattakhova","doi":"10.1134/S106816202406030X","DOIUrl":"10.1134/S106816202406030X","url":null,"abstract":"<p><b>Objective:</b> Despite a large number of works focused on the search for the mechanisms of formation of IgE-producing B-cells, the question of the relative contribution of germinal centers and extrafollicular foci B-cells in this process still remains controversial. Of particular interest is the study of the mechanisms of stimulation of the allergic immune response under the influence of air pollutants. The aim of the work was to study the connection between the adjuvant effect of benzo(<i>a</i>)pyrene (BaP) on the production of specific IgE in a novel low-dose allergy model with changes in the subpopulation composition of B-cells in the tissue of the immunization site and secondary lymphoid organs. <b>Methods:</b> Antigen without any stimuli was administrated to one group of BALB/c mice for 9 weeks in a low (0.3 μg) dose. BaP was administrated to another group of mice along with antigens at a dose of 4 ng. B-cell subpopulations were analyzed by flow cytometry. <b>Results and discussion:</b> BaP significantly stimulated the production of allergen-specific IgG₁ at early (3 weeks) time point, and allergen-specific IgE at late (9 weeks) time point. The aeropollutant increased the content of CD19⁺CD38^–CD95⁺B220⁺ germinal center B-cells with the phenotype and their precursors (CD19⁺CD38⁺CD95⁺B220⁺) with the phenotype in the spleen at early and late time points, but not in the lungs or regional lymph nodes. Under its influence, the content of CD19⁺CD38^–CD95⁺B220^– and CD19⁺CD38⁺CD95⁺B220⁺ extrafollicular plasmablasts in the spleen at an early time point and in lung tissue at a later time point also increases. In the spleen, BaP increased the content of CD138⁺CD19^–B220⁺ and CD138⁺CD19^–B220^– mature plasma cells, and in regional lymph nodes the content of CD138⁺CD19⁺B220^– immature plasma cells at a later time point. <b>Conclusions:</b> The adjuvant effect of BaP on the production of specific IgE was largely associated with stimulation of the formation of germinal centers in the spleen and with extrafollicular activation of B-cells in lung tissue.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2269 - 2282"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826256","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":"Coumarin Backbone as a Door-Opening Key for Investigating Chloroxylenol as Oral Antimicrobial Agents: an In Vitro–In Silico Study","authors":"Atyaf Talal Mahmood,&nbsp;Islam Khalid Kamal,&nbsp;Yasser Fakri Mustafa","doi":"10.1134/S1068162024060013","DOIUrl":"10.1134/S1068162024060013","url":null,"abstract":"<p><b>Objective:</b> Formulations containing chloroxylenol (COL), particularly Dettol, are commonly used in homes and hospitals for its antiseptic activity. Many studies documented the toxicity of this COL when human accidentally intake it in concentration less than 5%. <b>Methods:</b> The aim of this work is to use COL as a building block to create seven coumarin-based chemicals. Their structural frameworks were confirmed by various spectrophotometric methods. Also, these chemicals were submitted into two kinds of studies: <i>in vitro</i> and <i>in silico</i>. For the former one, the antimicrobial activity of these chemicals was specified against ten strains of infectious aerobes, anaerobes, and fungi. To explore the biocompatibility, the exploratory chemicals were studied using two normal bacteria and three healthy cellular lines. The <i>in silico</i> study include checking the theoretical capacity of the exploratory chemicals to oral-administrated and their toxicity-anticipated profiles. <b>Results and Discussion:</b> The gathered findings indicated that these chemicals has outstanding potential to inhibit the growth of infectious aerobes and fungi, and (<b>AA4</b>) being the best of their growth-inhibitor. Also, the same potential was observed against the infectious anaerobes, but here (<b>AA1</b>) was the superior growth-inhibitor. These wide-spectrum antimicrobial activities were coupled with great biocompatibilities with normal species under study. On the other hand, the results gathered from <i>in silico</i> study demonstrated that the exploratory chemicals have a powerful potential to oral-administrated with minimal anticipated toxicity. <b>Conclusions:</b> From these findings, the authors concluded that it is possible to use COL as a building unit to create biocompatible, wide-spectrum, low toxicity, oral-administrated antimicrobial prospects.</p>","PeriodicalId":758,"journal":{"name":"Russian Journal of Bioorganic Chemistry","volume":"50 6","pages":"2252 - 2268"},"PeriodicalIF":1.1,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142826383","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}