Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences最新文献

{"title":"Antidiabetic activities of aerial part of <i>Asparagus racemosus</i> Willd. extract: an <i>in vitro</i>, <i>in vivo</i>, and <i>in silico</i> approach.","authors":"Priya Das, Ankrita Thapa, Suraj Mistri, Gouhar Jahan Ashraf, Sourav Sarkar, Debabrata Modak, Soumen Bhattacharjee, Ravi Kumar Singh, Tarun Kumar Dua, Paramita Paul, Gouranga Nandi, Ranabir Sahu","doi":"10.1515/znc-2024-0142","DOIUrl":"https://doi.org/10.1515/znc-2024-0142","url":null,"abstract":"<p><p><i>Asparagus racemosus</i> Willd., a significant medicinal plant in India's Darjeeling Himalayan region. The current study aims to assess the antidiabetic efficacy of the aerial part of <i>Asparagus racemosus</i> Willd. utilizing a streptozotocin-nicotinamide-induced diabetic rat model. The methanolic extract of plant (ARME) was evaluated for <i>in vitro</i> antidiabetic activity through α-glucosidase and α-amylase enzyme suppression assay and assessed <i>in vivo</i> in a streptozotocin-induced rat model. A 21-day chronic multiple-dose study of ARME was examined. STZ-induced diabetic rats were treated with metformin (70 mg/kg) and ARME at concentrations of 200 and 400 mg/kg. It was discovered that ARME inhibited the activities of α-amylase and α-glucosidase and showed potent therapeutic effects on the rat's model. ARME helps raise body weight, hemoglobin, and other blood counts and normalizes the serum parameters in the diabetic group. In addition, liver tissues' abnormal levels of the antioxidant enzymes glutathione and lipid peroxides were returned to those of control animals. HPTLC study revealed the presence of stigmasterol, which showed a strong affinity for the proteins linked to diabetes mellitus through in silico study. As a result of these findings, ARME inhibits the activity of digestive enzymes and has antioxidant and antihyperglycemic effects in STZ-nicotinamide-induced diabetic rats.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143374867","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":"Biogenic selenium nanoparticles: a comprehensive update on the multifaceted application, stability, biocompatibility, risk, and opportunity.","authors":"Pooja V Nagime, Vinay Kumar Pandey, Charu Rajpal, Titilope John Jayeoye, Ashwini Kumar, Vijay R Chidrawar, Sudarshan Singh","doi":"10.1515/znc-2024-0176","DOIUrl":"https://doi.org/10.1515/znc-2024-0176","url":null,"abstract":"<p><p>Biogenic selenium nanoparticles (SeNPs) have emerged as promising area of research due to their unique properties and potential multifaceted applications. The biosynthesis of SeNPs through biological methods, such as using microorganism, plant extracts, etc., offers a safe, eco-friendly, and biocompatible approach, compared to traditional chemical synthesis. Recent several studies demonstrated that multifaceted application of SeNPs includes a broad area such as antibacterial, anticancer, antioxidant, antiviral, anti-inflammatory, antidiabetic, and excellent wound healing activity. On the other hand, SeNPs have also shown promising application in sensing of inorganic toxic metals, electrochemistry, agro-industries, aqua-cultures, and in fabrication of solar panels. Additionally, SeNPs capability to enhance the efficacy of traditional antibiotics and act as effective agents against multidrug-resistant pathogens has shown their potential in addressing critical health challenges. Although, the SeNPs exhibit wide applicability, the potential toxicity of Se, particularly in its various oxidative states, necessitates careful assessment of the environmental and health impacts associated with their use. Therefore, understanding the balance between their beneficial properties and potential risks is crucial for its safe applications. This review focuses exclusively on SeNPs synthesized via eco-friendly process, excluding research utilizing other synthesis processes. Moreover, this review aims to offer an overview of the diverse applications, potential risks, stability requirement, and cytocompatibility requirement, and multifaceted opportunities associated with SeNPs. Ultimately, the review bridges a gap in knowledge by providing an updated details of multifaceted applications of SeNPs.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143371160","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":"Assessing the molecular interaction between a COVID-19 drug, nirmatrelvir, and human serum albumin: calorimetric, spectroscopic, and microscopic investigations.","authors":"Mujaheed Abubakar, Ahmad Fadhlurrahman Ahmad Hidayat, Adyani Azizah Abd Halim, Kushagra Khanna, Mohammed Suleiman Zaroog, Mogana Sundari Rajagopal, Saad Tayyab","doi":"10.1515/znc-2024-0223","DOIUrl":"https://doi.org/10.1515/znc-2024-0223","url":null,"abstract":"<p><p>The research examined the molecular interaction between nirmatrelvir (NIR), a drug used to treat COVID-19, and human serum albumin (HSA) using various techniques, <i>viz.</i>, isothermal titration calorimetry (ITC), absorption, fluorescence, CD spectroscopy, and atomic force microscopy (AFM). ITC analysis showed that the NIR-HSA system possessed a moderate binding affinity, with a <i>K</i> _<i>a</i> value of 6.53 ± 0.23 × 10⁴ M^-1 at a temperature of 300 K. The thermodynamic values demonstrated that the NIR-HSA complex was stabilized by hydrophobic contacts, hydrogen bonds, and van der Waals forces. The research also discovered modifications in the UV-Vis absorption spectrum of the protein as well as swelling of the HSA molecule when exposed to NIR, based on AFM results. The three-dimensional fluorescence spectral data indicated changes in the microenvironment around HSA's Trp and Tyr residues. Alterations in the protein structure (both secondary and tertiary structures) of HSA after NIR binding were verified using CD spectral studies in the far-UV and near-UV regions. The identification of the NIR binding site in subdomain IB (Site III) of HSA was predicted through competitive displacement experiments.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143374804","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":"Insight into <i>in vitro</i> thymidine phosphorylase and <i>in silico</i> molecular docking studies: identification of hybrid thiazole bearing Schiff base derivatives.","authors":"Sundas Mumtaz, Fazal Rahim, Rafaqat Hussain, Shoaib Khan, Obaid Ur Rahman Abid, Asma Sardar, Tayyiaba Iqbal, Mohammad Shahidul Islam, Tahani Mazyad Almutairi","doi":"10.1515/znc-2024-0214","DOIUrl":"https://doi.org/10.1515/znc-2024-0214","url":null,"abstract":"<p><p>In pursuit of effective thymidine phosphorylase inhibitors, a series of hybrid analogs of thiazole-hydrazone derivatives (1-15) were synthesized and evaluated for their enzyme inhibitory potential using 7-deazaxanthine as a positive control. The goal was to determine these derivatives' effectiveness in suppressing thymidine phosphorylase activity, a target relevant to antitumor strategies due to the enzyme's role in angiogenesis and tumor growth. Biological evaluations indicated that all synthesized analogs displayed significant to moderate inhibitory activity, with IC₅₀ values between 3.93 ± 0.90 and 25.75 ± 4.30 µM. Particularly, compounds 12, 9, and 28 exhibited superior potency, with IC₅₀ values of 3.93 ± 0.90, 4.10 ± 1.10, and 4.50 ± 1.10 µM, respectively, surpassing the standard inhibitor 7-deazaxanthine (IC₅₀ = 16.8 ± 2.20 µM). Additionally, molecular docking studies were performed to elucidate the binding interactions of the synthesized thiazole-hydrazone derivatives with the active site of thymidine phosphorylase. The docking results aligned well with experimental data, revealing favorable binding conformations and significant interactions that support the observed inhibitory activities, particularly in the most potent compounds. These findings underscore the promise of thiazole-hydrazone derivatives as effective thymidine phosphorylase inhibitors, suggesting that targeted structural modifications could further enhance their activity. Further investigations, including <i>in vivo</i> studies, are warranted to explore their potential applications in anticancer therapies. This study highlights the valuable role of molecular docking in understanding the structure-activity relationship (SAR) of thiazole-hydrazone derivatives, emphasizing the potential of these compounds in advancing thymidine phosphorylase inhibition strategies for therapeutic purposes.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143256473","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":"Essential oil composition, <i>in vitro</i> antidiabetic, cytotoxicity, antimicrobial, antioxidant activity, and <i>in silico</i> molecular modeling analysis of secondary metabolites from <i>Justicia schimperiana</i>.","authors":"Getachew Tegegn, Yadessa Melaku, Muhdin Aliye, Abiy Abebe, Sileshi Degu, Rajalakshmanan Eswaramoorthy, Mo Hunsen, Milkyas Endale","doi":"10.1515/znc-2024-0124","DOIUrl":"https://doi.org/10.1515/znc-2024-0124","url":null,"abstract":"<p><p><i>Justicia schimperiana</i>, known as \"Dhumuugaa\" in Afan Oromo and \"Sensel\" or \"Smiza\" in Amharic, is traditionally used to treat ailments such as scabies, fever, asthma, diarrhea, malaria, and more. This study explored the chemical composition and biological activity of its extracts and isolated compounds. The essential oils were extracted using the hydrodistillation method, and their chemical composition was evaluated using GC-MS. GC-MS analysis identified 54 and 52 chemical components in the essential oils (EOs) from roots and leaves, respectively. The structures of the isolated compounds have been identified using 1D and 2D-NMR techniques. Six compounds - β-sitosterol (<b>1</b>), 5-methoxy durmillone (<b>2</b>), <i>trans</i>-resveratrol (<b>3</b>), tricuspidatol A (<b>4</b>), kaempferol-3-O-α-rhamnopyranoside (<b>5</b>), and kaempferol-3-O-rutinoside (<b>6</b>) - were isolated from the root extracts and reported for the first time in this species. The antimicrobial activity was evaluated using the broth microdilution technique. EOs extracts showed significant antibacterial activity, particularly against <i>Staphylococcus aureus</i>, <i>Streptococcus agalactiae</i>, while compound <b>6</b> showed potent activity with an MIC of 0.25 μg/mL. The antioxidant activity revealed strong radical scavenging for compounds <b>5</b> and <b>6</b>, with extracts also demonstrating significant α-amylase inhibitory effects and moderate cytotoxicity against the MCF-7 cell line. Molecular docking and ADMET analysis highlighted compounds <b>5</b> and <b>6</b> as promising therapeutic agent. These findings highlight the medicinal potential of <i>J. schimperiana</i> roots, warranting further exploration.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143054019","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":"French marigold (<i>Tagetes patula</i>) flavonoid extract-based priming ameliorates initial drought stress on <i>Oryza sativa</i> var <i>indica</i>, cultivar Satabdi (IET4786): a sustainable approach to avoid initial drought stress.","authors":"Arunima Saha, Suraj Kumar, Sanjukta Dey, Chiranjib Bhattacharyya, Ranabir Sahu, Gouhar Jahan Ashraf, Somnath Bhattacharyya, Pritam Das, Subhendu Bandyopadhyay, Saikat Dewanjee, Moumita Gangopadhyay","doi":"10.1515/znc-2024-0093","DOIUrl":"https://doi.org/10.1515/znc-2024-0093","url":null,"abstract":"<p><p>Drought stress remains a serious concern in <i>Oryza sativa</i> L. var <i>indica</i>, cultivar Satabdi (IET4786) production, particularly during the earliest growth phases, ultimately affecting yield due to the recent trend of delayed rain arrival in West Bengal, India. This study aimed to develop a cost-effective strategy to improve the drought tolerance capacity of rice seedlings by priming the seeds with flavonoid-enriched extract (FEE) of French marigold (<i>Tagetes patula</i>) petals to withstand the initial drought milieu. The morpho-physiological and biochemical responses of rice seedlings were evaluated to perceive the priming efficacy in alleviating water stress-induced untoward effects. The findings revealed that mechanical priming of the IET4786 seeds with FEE (50 mg/mL for 30 min) significantly improved seedling survival against initial drought stress for 14 days. After 24 h of recovery from drought stress, the primed seed-derived seedlings exhibited significantly improved morphological, physiological, biochemical, and redox parameters compared to the seedlings derived from unprimed seeds under net house conditions. In search of mechanistic insights, seed priming significantly increased proline content by endorsing Δ¹-pyrroline-5-carboxylate synthetase activities, endorsed methylglyoxal clearance homeostasis by improving glyoxalase I and II activities through restoring glutathione (GSH) level, and enhanced polyamine accumulation in the leaves of seedlings to endure drought stress.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-01-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142972943","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":"Antidiabetic phytochemicals: an overview of medicinal plants and their bioactive compounds in diabetes mellitus treatment.","authors":"Yenework Nigussie Ashagrie, Kundan Kumar Chaubey, Mesfin Getachew Tadesse, Deen Dayal, Rakesh Kumar Bachheti, Nishant Rai, Atreyi Pramanik, Sorabh Lakhanpal, Anuj Kandwal, Archana Bachheti","doi":"10.1515/znc-2024-0192","DOIUrl":"https://doi.org/10.1515/znc-2024-0192","url":null,"abstract":"<p><p>Diabetes mellitus (DM) is a group of metabolic disorders characterized by hyperglycemia due to insufficient insulin secretion or action. Contributing factors include genetic predisposition, obesity, family history, inactivity, and environmental risks. Type 2 diabetes mellitus (T2DM), the most common form, involves impaired insulin secretion by pancreatic β-cells, leading to insulin resistance. By 2045, it is projected that India and China will have approximately 134.3 and 110.8 million diabetic individuals, respectively. Although synthetic drugs are effective in managing DM, they often come with side effects. Consequently, plant-based phytochemicals with antidiabetic properties are gaining attention. Research indicates that around 115 medicinal plants (MPs) have antidiabetic effects, particularly those from the Fabaceae, Liliaceae, and Lamiaceae families. Bioactive compounds like alkaloids, triterpenoids, flavonoids, and phenolics are known to combat DM. Traditional medicinal systems, particularly in developing countries, offer effective DM management. This review highlights the importance of MPs and their bioactive compounds in treating diabetes and underscores the need for further research to commercialize plant-based antidiabetic drugs.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-01-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142957771","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":"Essential oil of <i>Daucus carota</i> (L.) ssp. <i>carota</i> (Apiaceae) flower: chemical composition, antimicrobial potential, and insecticidal activity on <i>Sitophilus oryzae</i> (L.).","authors":"Mohammed Elhourri, Zakya M'hamdi, Yasmine Ghouati, Ouafae Benkhnigue, Wafaa M Hikal, Hussein A H Said-Al Ahl, Miroslava Kačániová, Mohamed Fawzy Ramadan, Ali Amechrouq","doi":"10.1515/znc-2024-0246","DOIUrl":"https://doi.org/10.1515/znc-2024-0246","url":null,"abstract":"<p><p>In order to search for new chemotypes and to carry out a comparative study with the literature, the current study investigated the chemical composition of the essential oil of the flowers of <i>Daucus carota</i> (L.) ssp. <i>carota</i> using gas chromatography coupled with mass spectrometry (GC-MS). Moreover, the antimicrobial and insecticidal potentials of essential oil were studied. Hydrodistillation was used to extract the essential oil. Due to the immiscibility of essential oils in water and, therefore, in the culture medium, emulsification was carried out using a 0.2 % agar solution to promote germ/composite contact. Fumigation with the oil phase of the essential oil was carried out in airtight and transparent plastic boxes, with a capacity of 1 L as an exposure chamber to test the lightness of essential oils against adults of <i>Sitophilus oryzae</i> (L.). In each box, five <i>Petri</i> dishes were placed. Each replicate consisted of five adults of <i>S. oryzae</i> (L.). The essential oils were spread on Wathman filter paper and placed inside the exposure chamber. Mortality control was carried out by counting insect deaths from the first day of treatment until the death of all individuals. α-Pinene (22.2 %) was the major compound in the essential oil of the oil phase of <i>D. carota</i> (L.) ssp. <i>carota</i> followed by β-asarone (15.1 %), sabinene (12.4 %), and α-himachalene (10.1 %), as well as the crystallized phase containing β-asarone. In terms of antimicrobial activity, the essential oils showed significant inhibition of the six bacteria and seven molds studied at a concentration of 0.45 mg/mL. The essential oils were found to be highly effective against <i>S. oryzae</i> (L.). This approach can help reduce the amount of synthetic antibiotics applied and, therefore, decrease the negative impact of artificial agents, such as residues, resistance, and environmental pollution.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142907703","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":"Latest developments in biomaterial interfaces and drug delivery: challenges, innovations, and future outlook.","authors":"Saraswati Patel, Samsi D Salaman, Devesh U Kapoor, Richa Yadav, Swapnil Sharma","doi":"10.1515/znc-2024-0208","DOIUrl":"https://doi.org/10.1515/znc-2024-0208","url":null,"abstract":"<p><p>An ideal drug carrier system should demonstrate optimal payload and release characteristics, thereby ensuring prolonged therapeutic index while minimizing adverse effects. The field of drug delivery has undergone significant advancements, particularly within the last two decades, owing to the revolutionary impact of biomaterials. The use of biomaterials presents significant due to their biocompatibility and biodegradability, which must be addressed in order to achieve effective drug delivery. The properties of the biomaterial and its interface are primarily influenced by their physicochemical attributes, physiological barriers, cellular trafficking, and immunomodulatory effects. By attuning these barriers, regulating the physicochemical properties, and masking the immune system's response, the bio interface can be effectively modulated, leading to the development of innovative supramolecular structures with enhanced effectiveness. With a comprehensive understanding of these technologies, there is a growing demand for repurposing existing drugs for new therapeutic indications within this space. This review aims to provide a substantial body of evidence showcasing the productiveness of biomaterials and their interface in drug delivery, as well as methods for mitigating and modulating barriers and physicochemical properties along with an examination of future prospects in this field.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-11-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142683151","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":"Molecular modeling and synthesis of novel benzimidazole-derived thiazolidinone bearing chalcone derivatives: a promising approach to develop potential anti-diabetic agents.","authors":"Shahzad Ahmad Abbasi, Wajid Rehman, Fazal Rahim, Rafaqat Hussain, Mohammed B Hawsawi, Mustafa S Alluhaibi, Majed Alharbi, Muhammad Taha, Shoaib Khan, Liaqat Rasheed, Abdul Wadood, Syed Adnan Ali Shah","doi":"10.1515/znc-2024-0202","DOIUrl":"https://doi.org/10.1515/znc-2024-0202","url":null,"abstract":"<p><p>Diabetes mellitus (DM) is a disorder which is raised at the alarming level and it is characterized by the hyperglycemia results from the impaired action of insulin, production of insulin or both of these simultaneously. Consequently, it causes problems or failure of different body organs such as kidneys, heart, eyes, nerve system. Since this disease cannot be completely cured until now, we aimed to design series of enzymes inhibitors and tested them for DM treatment. In this series, benzimidazole-based thiazolidinone bearing chalcone derivatives completed in a four step reaction and their structures were confirmed through various spectroscopic techniques. A significant efficacy on antidiabetic enzymes was observed, with IC₅₀ values ranging from 25.05 ± 0.04 to 56.08 ± 0.07 μM for α-amylase and 22.07 ± 0.02 to 53.06 ± 0.07 μM for α-glucosidase. The obtained results were compared to those of the standard glimepiride drug (IC₅₀ = 18.05 ± 0.07 µM for α-amylase and IC₅₀ = 15.02 ± 0 .03 µM for α-glucosidase). The synthesized compounds showed promising antidiabetic potency. Moreover, a molecular docking study was conducted on the most active analogs of the compounds to better understand their interactions with the active sites of the targeted enzymes.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142683157","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}