Biotechnology and applied biochemistry最新文献

{"title":"Carboxymethyl Chitosan and Chitosan as a Bioactive Delivery System: A Review.","authors":"Parinaz Sadat Alemi, Marjan Mohamadali, Samira Arabahmadi, Shiva Irani, Fereshteh Sharifi","doi":"10.1002/bab.2758","DOIUrl":"https://doi.org/10.1002/bab.2758","url":null,"abstract":"<p><p>The functionality and mechanism of bioactive agents (BA) in treating various diseases have been studied as a progressive route. Designing an effective delivery system for transferring these molecules and components is a major challenge. For that reason, a wide range of biomaterials has been introduced to deliver BA to the target tissue or cells. Chitosan (CTS) is a nontoxic, biocompatible, biodegradable, and notable point low-cost polymer, and, as a result, can be effectively utilized in the formulation of diverse delivery systems, in biomedical applications. However, CTS has some limitations, such as poor solubility in aqueous and alkaline media, rapid swelling and degradation, and consequence fast release agent. The CTS derivative carboxymethyl chitosan (CMC) is an acceptable candidate for overcoming these limitations. CMC is a high-impact grade for pharmaceutical and biomedical applications because of its nontoxic, biocompatible, biodegradable, gelation, mucoadhesive, antibacterial, and antifungal. CMC bioactivity potentials are related to carboxyl and methyl groups added through chemical modification in the CTS backbone. In this review, the physical and chemical properties of CTS and CMC have been introduced and discussed. Afterward, its biomedical applications with delivery approaches for various BA (drugs, genes, proteins), microfluidic, and cancer have been considered.</p>","PeriodicalId":9274,"journal":{"name":"Biotechnology and applied biochemistry","volume":" ","pages":"e2758"},"PeriodicalIF":3.2,"publicationDate":"2025-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143984026","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Exploiting Self-Immobilized Fungi for Biovalorization of Oil Palm Sap to Organic Acids Through Repeated-Batch Fermentation.","authors":"Benjamas Chiersilp, Asma Billateh, Ketsara Sriklab, Chutima Thongsongkaew","doi":"10.1002/bab.2730","DOIUrl":"https://doi.org/10.1002/bab.2730","url":null,"abstract":"<p><p>This study focused on utilizing agricultural waste, oil palm sap (OPS) as a sole nutrient source for organic acid production by self-immobilized fungi. Among the fungi cultured in OPS, Rhizopus oryzae TISTR 3336 was selected as it could form compact and adequate-size pellets (3-5 mm) and gave the highest total acid production yield of 0.31 ± 0.02 g/g-sugar under pH control. The optimal conditions were as follows: inoculum size of 10⁶ spores/mL and shaking speed of 120 rpm. Using concentrated OPS gave higher final concentration of organic acids but reduced the production yield. The repeated-batch fermentation of OPS by self-immobilized fungi was successfully carried out for four cycles. The optimal initial sugar concentration was 40 g/L, giving the organic acid productions ranging of 19 to 35 g/L, with yields ranging of 0.47 to 0.87 g/g-sugar. This study has shown the efficient bioconversion of agricultural wastes into organic acids using self-immobilized fungi in the repeated-batch fermentation.</p>","PeriodicalId":9274,"journal":{"name":"Biotechnology and applied biochemistry","volume":" ","pages":""},"PeriodicalIF":3.2,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143972021","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design and Synthesis of Triazole-Based p-tert-Butylcalix[4]Arene Conjugates and Evaluation of Their Antimicrobial, Antibiofilm, and Anti-Quorum-Sensing Activities.","authors":"Alfred Ngenge Tamfu, Selahattin Bozkurt, Ozgur Ceylan","doi":"10.1002/bab.2761","DOIUrl":"https://doi.org/10.1002/bab.2761","url":null,"abstract":"<p><p>Macrocyclic calix[n]arenes have many applications, with diverse structures that can easily be functionalized either on upper or lower rims, mostly to impart solubility and improve biological activities. In this study, triazole-based p-tert-butylcalix[4]arene conjugates (AT10a and AT10b) and their p-tert-butylphenol analogs (AT10b and AT11b) were synthesized in good yields and characterized using ¹³C NMR and ¹H NMR experiments. The compounds were evaluated for their antimicrobial (AM) activity against Gram-positive bacteria (Staphylococcus aureus, Enterococcus faecalis, Listeria monocytogenes), Gram-negative bacteria (Escherichia coli, Salmonella typhi, Pseudomonas aeruginosa), and fungi (Candida albicans, Candida tropicalis), and minimal/minimum inhibitory concentration (MIC) values varied from 19 to 2500 µg/mL. The AM activities of the compounds were good against most of the strains, with S. aureus, L. monocytogenes, and C. albicans being the most susceptible. The compounds inhibited violacein synthesis in Chromobacterium violaceum CV12472 and MIC and sub-MIC concentrations. AT10a and AT11a all showed 100% inhibition at MIC and 1/2 MIC concentrations, whereas compound AT10b and compound AT11b had 85.1% ± 2.1% and 90.7% ± 1.2% inhibitions at 1/2 MIC. The compounds inhibited quorum sensing (QS) against C. violaceum CV026 at MIC and 1/2 MIC, with AT11a being the most active with inhibition diameters of 18.50 ± 0.75 mm (MIC) and 11.50 ± 0.47 mm (1/2 MIC). QS inhibition indicates that the compounds could disrupt communication and coordinated behavior in bacteria. The compounds inhibited swarming and swimming motilities against P. aeruginosa PA01 at MIC and sub-MIC concentrations, implying that they can reduce spread of bacteria and cross-infections through surface colonization. The compounds showed concentration-dependent biofilm inhibition against a range of pathogenic bacteria at MIC and sub-MIC. S. aureus, L. monocytogenes, and S. typhi biofilms were most susceptible to the compounds compared to the others. Inhibition of biofilm is an indication of possible eradication of resistance in bacteria. The results suggest that triazole-based calixarene derivatives are suitable scaffolds for the development of good AMs, which could quench cell-to-cell signaling and attenuate virulence factors in bacteria.</p>","PeriodicalId":9274,"journal":{"name":"Biotechnology and applied biochemistry","volume":" ","pages":"e2761"},"PeriodicalIF":3.2,"publicationDate":"2025-04-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143966264","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Senkyunolide I Improves Septicemia-Induced Brain Dysfunction via Regulating Nrf2 and Astrocyte Activity.","authors":"Haohao Cao, Tao Liu, Meixia Xu","doi":"10.1002/bab.2748","DOIUrl":"https://doi.org/10.1002/bab.2748","url":null,"abstract":"<p><p>Senkyunolide I (Sen I) has a protective effect on the blood-brain barrier (BBB) in rats with sepsis-associated encephalopathy (SAE). This study investigated whether Sen I regulates Nrf2 to ameliorate sepsis-induced brain dysfunction (SIBD). Sixty rats were randomly assigned into Sham group, SAE group (Model group), SAE + Sen I group (72 mg/kg, Sen I group), and SAE+ positive control group (RTA 402, Nrf2 receptor agonist, RTA 402 group), with 15 rats in each group. The cecal ligation and puncture (CLP) method was applied to induce sepsis in rats. SAE modeling was verified 6 h after operation. The drug was administered 24 h after surgery. Six rats in each group were sacrificed 24 h after administration, with brains extracted. The remaining rats would continue to be observed for their survival status until 72 h post-surgery. Brain cell apoptosis was measured using TUNEL. We detected the expression of glial fibrillary acidic protein (GFAP) by immunofluorescence, Nrf2 gene expression by RT-qPCR, and the protein expression of Nrf2, MMP-9, AQP-4, and occludin by Western blot. TNF-α and IL-1β levels were tested by ELISA, and malondialdehyde (MDA) and glutathione peroxidase (GSH-Px) by biochemical tests. Survival rate at 72 h post-surgery, Sham group was 100%. The survival rate of the Sen I group (44.4%) and the RTA 402 group (55.6%) is significantly higher than that of the Model group (11.1%). Both Sen I and RTA 402 can improve the brain tissue damage in rats caused by sepsis, specifically by reducing apoptosis and GFAP expression, reducing TNF-α, IL-1β, and MDA levels, increasing the activity of GSH-Px, downregulating the protein expression of MMP-9 and AQP-4, and upregulating the protein expression of Nrf2 and occludin. Moreover, Sen I significantly increased the expression of Nrf2 in rat brain tissues. Sen I ameliorates SIBD in rats by regulating the expression of Nrf2 and astrocyte activation.</p>","PeriodicalId":9274,"journal":{"name":"Biotechnology and applied biochemistry","volume":" ","pages":"e2748"},"PeriodicalIF":3.2,"publicationDate":"2025-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143971948","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Metolazone and Azosemide, Clinically Utilized Diuretics, Exhibit Inhibitory Activity for Glyoxalase I.","authors":"Masahiro Watanabe, Takao Toyomura, Hidenori Wake, Takashi Nishinaka, Omer Faruk Hatipoglu, Hideo Takahashi, Masahiro Nishibori, Shuji Mori","doi":"10.1002/bab.2760","DOIUrl":"https://doi.org/10.1002/bab.2760","url":null,"abstract":"<p><p>Methylglyoxal (MGO), a byproduct produced in the process of glycolysis, has cytotoxicity and forms advanced glycation endproducts (AGEs), which cause cell failure in several tissues. Because MGO is mainly removed by the action of glyoxalase I (GLO1), the activity of this enzyme contributes to the accumulation of MGO. We recently found that quinetazone, a diuretic pharmaceutical agent, has the potential to inhibit GLO1 activity. Therefore, we explored whether diuretics that have a similar structure to quinetazone inhibit GLO1. The inhibitory characteristics of diuretics with recombinant GLO1 were spectrophotometrically determined. Cell proliferation and accumulation of MGO-derived AGEs were evaluated by MTT assay and Western blotting. Among the thiazide, thiazide-like, and loop diuretics, metolazone and azosemide were found to inhibit GLO1 activity by 97% at 100 µM. Furthermore, we examined whether the substructures of these diuretics have inhibitory activity, quinazolinone or phenyltetrazole were determined to be the minimal structures of metolazone or azosemide required for inhibition of GLO1, respectively. In proximal renal tubule-like HK-2 and vascular endothelial cell-like EA.hy926 cells, these diuretics were shown to inhibit cell proliferation and induce accumulation of MGO-derived AGEs. In contrast, the substructures of these diuretics that did not affect GLO1 activity did not cause these changes. Metolazone and azosemide have inhibitory effects against GLO1. Considering that these diuretics are clinically employed as pharmaceutical agents, high or prolonged dosages may contribute to pathogenesis through GLO1 inhibition, followed by MGO and/or AGE accumulation.</p>","PeriodicalId":9274,"journal":{"name":"Biotechnology and applied biochemistry","volume":" ","pages":"e2760"},"PeriodicalIF":3.2,"publicationDate":"2025-04-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143810488","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Low RYR2 Level Relates to Poor Prognosis of Patients With Lung Adenocarcinoma by Promoting Tumor Cell Proliferation and Inhibiting Immune Cell Infiltration.","authors":"Tao Wang, Baozhen Wang, Zhongting Lu, Tao Li","doi":"10.1002/bab.2759","DOIUrl":"https://doi.org/10.1002/bab.2759","url":null,"abstract":"<p><p>Ryanodine receptor type 2 (RYR2) is a large calcium channel that has been identified as one of the most frequently mutated genes in lung adenocarcinoma (LUAD). Despite its potential significance, the role of RYR2 in LUAD remains poorly understood. In this study, we obtained transcriptomic data (normal n = 59, tumor n = 541) from TCGA portal and RYR2 protein abundance data from cProSite, which includes 86 normal and 91 tumor samples. Additionally, we assembled a cohort of 38 patients with LUAD and collected paired tumor and adjacent non-tumor control samples. To investigate the functional impact of RYR2, we employed 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and flow cytometry analysis to assess cell viability and apoptosis, respectively. While mitochondria function was evaluated via measuring oxygen consumption rate. The relationship between RYR2 expression level and immune cell infiltration was analyzed by immunohistochemistry and flow cytometry analysis. Furthermore, RT-qPCR and enzyme-linked immunosorbent assay were used to quantify the expression levels of CCL14 and CXCL12. Our findings demonstrated that both the mRNA and protein levels of RYR2 were significantly downregulated in LUAD samples, and lower RYR2 levels are associated with the poor patient prognosis. Overexpression of RYR2 in A549 and H1299 cells resulted in impaired mitochondrial function, decreased cell viability, and increased apoptosis. Notably, RYR2 levels exhibited a negative correlation with tumor purity, and tumors with lower RYR2 levels showed diminished infiltration of T cells and dendritic cells. Knockdown of RYR2 in LUAD cells inhibited the production of chemokines, particularly CCL14 and CXCL12. In conclusion, our study reveals that RYR2 functions as a tumor suppressor in LUAD by inducing mitochondrial dysfunction and promoting immune cell infiltration.</p>","PeriodicalId":9274,"journal":{"name":"Biotechnology and applied biochemistry","volume":" ","pages":"e2759"},"PeriodicalIF":3.2,"publicationDate":"2025-04-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143810486","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of a Codetection System Based on STRs and Biofluid-Specific CpG Markers.","authors":"Zeqin Li, Shiqi Liu, Fang Yuan, Mengfan Yu, Shuaikun Zhi, Xingchun Zhao, Gengqian Zhang","doi":"10.1002/bab.2754","DOIUrl":"https://doi.org/10.1002/bab.2754","url":null,"abstract":"<p><p>The detection of body fluids in biological stains at crime scenes and their association with donors is increasingly important for the validity of evidence in case investigations and prosecutions. While autosomal short tandem repeats (STR) and DNA methylation markers can effectively analyze personal identification and body fluid origin, there is currently no integrated system for simultaneous STR typing (subsource level) and biofluid identification (source level). This study has developed a codetection system based on DNA methylation markers (cytosine-phosphate-guanine [CpG]) and an STR amplification system for simultaneous personal identification and biofluid origin determination using capillary electrophoresis. This system integrates a 7-plex amplification system, comprising 5 biofluid-specific CpG markers (cg05261336 for semen, cg04011671 for peripheral blood, cg09107912 for saliva, cg15988970 for vaginal secretion, and cg18069290 for menstrual blood) and 2 control markers, with a 20-plex STR amplification system. The combined system successfully distinguished five types of body fluids from single sources (peripheral blood, semen, saliva, menstrual blood, and vaginal secretion) and generated DNA methylation profiles in mixed samples of two to four body fluids in varying proportions. The cumulative discrimination power for personal identification was calculated to be 1-3.5120 × 10^-25. Additionally, semen and vaginal secretion with 0.1 ng DNA input or kept at room temperature for 5 months could still be efficiently identified. This study provides a promising method for simultaneously identifying body fluids and their donors in forensic science.</p>","PeriodicalId":9274,"journal":{"name":"Biotechnology and applied biochemistry","volume":" ","pages":"e2754"},"PeriodicalIF":3.2,"publicationDate":"2025-04-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143802573","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Rosmanol Suppresses Nasopharyngeal Carcinoma Cell Proliferation and Enhances Apoptosis, the Regulation of MAPK/NF-κB Signaling Pathway.","authors":"Weiping Tao, Chaowu Jiang, Periyannan Velu, Cao Lv, Yan Niu","doi":"10.1002/bab.2750","DOIUrl":"https://doi.org/10.1002/bab.2750","url":null,"abstract":"<p><p>Nasopharyngeal Carcinoma (NPC) is a major public health problem in endemic zones. NPC is correlated with substantial illness and death; thus, superior treatment is desired. Rosmanol (RM) is a phenolic diterpene antioxidant extracted from the medicinal herb Rosemary (Rosmarinus officinalis). RM has been investigated for its anti-inflammatory and anti-tumor properties by numerous signaling cascades. However, the fundamental anticancer latent mechanism of RM persists as unidentified. Hence, this present research proposes to search for the anti-cancer efficacy of RM on human NPC cells CNE2 using an in vitro approach. To assess the possible molecular mechanisms of proliferation, apoptosis, cell-cycle regulatory proteins, and MAPKs/NF-κB signaling of NPC cells were administered RM (20 and 30 µM) and assayed through MTT, DCFH-DA, Rh-123 staining, AO/EB, PI, Rh-123/DAPI merge form staining, RT-PCR, and Western blot. The result was recognized that RM could reduce NPC cell viability by elevated intracellular ROS, MMP damage, and generate apoptosis. RM inhibits the Cyclin-D1, Bax, TNF-α, and NF-κB, and induces BCl-2 analyzed via RT PCR. RM attenuates the cell cycle mechanism by repressing NPC cell cycle-related proteins: CDK4/CDK6, pRB, cyclin-D1, and MAPKs/NF-κB signaling. These data established that the MAPKs/NF-κB pathway is a potential target for the remedial action of RM. In summary, RM may be an effective conventional chemotherapy drug in preventing the progression of NPC.</p>","PeriodicalId":9274,"journal":{"name":"Biotechnology and applied biochemistry","volume":" ","pages":"e2750"},"PeriodicalIF":3.2,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143763042","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Valorization of Pomace Waste for the Production of Cellulose by Komagataeibacter diospyri RSA4.","authors":"Rakshanda Singh, Moniya Katyal, Ritu Mahajan, Ranjan Gupta, Neeraj K Aggarwal, Anita Yadav","doi":"10.1002/bab.2757","DOIUrl":"10.1002/bab.2757","url":null,"abstract":"<p><p>In this study, the mixed extract of pomace waste of sweet lime, apple, and pineapple was used as a culture media for the production of cellulose by Komagataeibacter diospyri RSA4. Maximum cellulose yield was found at an inoculum age (48 h), inoculum size (6% v/v), pH (4.0), temperature (30°C), incubation period (15 days), and media:flask volume (1:2.5). Cellulose yield was about 1.78-fold higher in mixed pomace waste extract (PE)-based medium in comparison to Hestrin-Schramm (HS) media. The maximum yield of cellulose was obtained with mixed PE-based medium, supplemented with 30 g/L glucose, 20 g/L peptone, 20 g/L yeast extract, 1.15 g/L citric acid, and 2.5 g/L disodium hydrogen phosphate. Cellulose yield was nearly 6.03-fold higher in supplemented mixed PE (SPE)-based medium than in standard HS medium. Comparative analysis of purified cellulose produced in mixed PE medium, SPE medium, and standard HS media was done by field emission scanning electron microscopy, energy dispersive spectroscopy, x-ray diffraction, Fourier transform infrared spectroscopy, thermogravimetric study, and derivative of thermogravimetric analysis, and cellulose was found to be similar in all the three media. This study shows that the mixed PE can be utilized as a potentially sustainable and valorizable media for production of bacterial cellulose. This is the first report, showing valorization of mixed pomace waste for the production of cellulose.</p>","PeriodicalId":9274,"journal":{"name":"Biotechnology and applied biochemistry","volume":" ","pages":"e2757"},"PeriodicalIF":2.7,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143763044","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Isoindole-1,3-Dione Sulfonamides as Potent Inhibitors of Glucosidase, Aldose Reductase, and Tyrosinase: A Molecular Docking and Enzyme Inhibition Study.","authors":"Zozan Aslan, Esra Yılmaz, Nurgül Pulat, Amine Şeker, Ayşe Ertem, Musa Demirhan, Saliha Gündoğdu, Mustafa Arslan, Yeliz Demir","doi":"10.1002/bab.2756","DOIUrl":"https://doi.org/10.1002/bab.2756","url":null,"abstract":"<p><p>Diabetes mellitus, especially type 2, is a global health challenge, and effective enzyme inhibitors are essential for its control. Conventional inhibitors have drawbacks such as gastrointestinal side effects and regional availability, examples being acarbose and epalrestat. Moreover, tyrosinase, which controls melanin synthesis which is also a target for reducing hyperpigmentation disorders. In this study, we demonstrate the inhibitory action of novel isoindole-1,3-dione-based sulfonamides against key enzymes associated with diabetes and hyperpigmentation, α-Glucosidase (α-Glu), aldose reductase (ALR2), and tyrosinase. The presynthesized compounds (3, 4a-k) are tested for in vitro inhibition against α-Glu, ALR2, and tyrosinase and compared with reference compounds acarbose, epalrestat, and kojic acid. Kinetic studies showed that both competitive and noncompetitive inhibition modes were observed. Among them, compound 4a displayed the highest ALR2 inhibitory potency (K_i: 0.211 µM) and was superior to epalrestat. In terms of α-Glu, compound 4k was shown to be more potent with a K_i of 0.049 µM, particularly versus acarbose. Compound 4d showed excellent inhibitory activity (K_i: 1.43 µM) in tyrosinase assays, much more potent than kojic acid. Molecular docking studies revealed the details of enzyme-binding interactions, which justify the respective inhibitory mechanisms observed. Structure-activity relationships reflected that compounds with strong hydrogen bonding and hydrophobic interactions led to higher potency. These findings highlight the importance of isoindole-1,3-dione-based sulfonamides as therapeutic agents and will provide valuable leads for developing multifunctional enzyme inhibitors for such diabetic complications and hyperpigmentation.</p>","PeriodicalId":9274,"journal":{"name":"Biotechnology and applied biochemistry","volume":" ","pages":"e2756"},"PeriodicalIF":3.2,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143763036","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}