Current pharmaceutical biotechnology最新文献

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Protective Effects of Curcumin and Nanomicelle Curcumin on Chlorpyrifos-induced Oxidative Damage and Inflammation in the Uterus, Ovary and Brain of Rats. 姜黄素和纳米姜黄素对毒死蜱诱导的大鼠子宫、卵巢和脑氧化损伤和炎症的保护作用
IF 2.2 4区 医学
Current pharmaceutical biotechnology Pub Date : 2025-01-01 DOI: 10.2174/0113892010297408240319073735
Maryam Nazarian, Hamed Aramjoo, Babak Roshanravan, Saeed Samarghandian, Tahereh Farkhondeh
{"title":"Protective Effects of Curcumin and Nanomicelle Curcumin on Chlorpyrifos-induced Oxidative Damage and Inflammation in the Uterus, Ovary and Brain of Rats.","authors":"Maryam Nazarian, Hamed Aramjoo, Babak Roshanravan, Saeed Samarghandian, Tahereh Farkhondeh","doi":"10.2174/0113892010297408240319073735","DOIUrl":"10.2174/0113892010297408240319073735","url":null,"abstract":"<p><strong>Background and aims: </strong>Chlorpyrifos (CPF), which is classified as an Organophosphorus Pesticide (OP), has been identified as a toxic agent for the reproductive system due to its capacity to induce oxidative stress and inflammation. Curcumin (CUR) has been reported as a natural antioxidant and anti-inflammatory agent that could combat toxicity in various tissues. This study aims to examine the protective effects of CUR and its nanoformulation against reproductive impairment induced by CPF.</p><p><strong>Methods: </strong>Forty-eight female Wistar albino rats were randomly allocated to six groups (n=8): control (0.5 mL of corn oil, the solvent for CPF), CPF (10 mg/kg), CPF + CUR 100 mg/kg/day, CPF + CUR 300 mg/kg/day, CPF + nano-micelle curcumin (NMC) 2.5 mg/kg/day, and CPF + NMC 5 mg/kg/day. The experimental treatment was performed for 30 days. Then, brain, ovary and uterus tissues were collected for measuring oxidative stress and inflammatory indices.</p><p><strong>Results: </strong>MDA, NO, IL-6, and TNF-α concentrations significantly increased in the brain, ovary and uterus of the CPF group versus the control group (p < 0.001). The levels of GSH and SOD in the uterus, ovaries, and brain exhibited a significant decrease in the CPF group compared to the control group (p < 0.05). However, CUR (300 mg/kg) and NMC (5 mg/kg) significantly decreased MDA, NO, TNF-α, and Il-6 and increased SOD and GSH levels in the uterus, ovaries and brain of the CPF-exposed animals versus the CPF-exposed non-treated animals (p < 0.001).</p><p><strong>Conclusion: </strong>Our findings indicated that CUR and NMC could be effective in alleviating CPFinduced reproductive toxicity.</p>","PeriodicalId":10881,"journal":{"name":"Current pharmaceutical biotechnology","volume":" ","pages":"490-496"},"PeriodicalIF":2.2,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140335068","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
TP508 Promotes Bone Regeneration on Distraction Osteogenesis via the Activation of Wnt/β-catenin Signaling Pathway. TP508通过激活Wnt/β-catenin信号通路促进牵引性成骨过程中的骨再生
IF 2.2 4区 医学
Current pharmaceutical biotechnology Pub Date : 2025-01-01 DOI: 10.2174/0113892010289575240306033011
Kehan Li, Linan Liu, Jingyi Zhang, Chenyu Liao, Jian Hu, Jian Song
{"title":"TP508 Promotes Bone Regeneration on Distraction Osteogenesis <i>via</i> the Activation of Wnt/β-catenin Signaling Pathway.","authors":"Kehan Li, Linan Liu, Jingyi Zhang, Chenyu Liao, Jian Hu, Jian Song","doi":"10.2174/0113892010289575240306033011","DOIUrl":"10.2174/0113892010289575240306033011","url":null,"abstract":"<p><strong>Introduction: </strong>TP508 is a thrombin peptide that participates in the inflammatory response and wound healing. Its role in the molecular mechanism of distraction osteogenesis remains unclear. This study established a tibia distraction osteogenesis (DO) model in rats and investigated the role and mechanism of TP508 in bone regeneration during DO.</p><p><strong>Method: </strong>Micro-computed tomography (Micro-CT) and hematoxylin-eosin (HE) staining were used to track osteogenesis. Western blot and quantitative real-time polymerase chain reaction (qRT-PCR) were performed to measure the expression of osteoblast-related factors, Wnt/β- catenin signaling-related proteins and genes. Immunohistochemistry was used to measure the expression of β-catenin in the cytoplasm and nucleus.</p><p><strong>Results: </strong>TP508 accelerated bone regeneration increased the expression of the osteoblast-related factors Alkaline phosphatase (ALP), runt-related transcription factor 2 (RUNX2), and osteocalcin (OCN). After the Wnt signaling was inhibited by LGK974, the expression of osteoblastrelated factors was downregulated, leading to a decrease in bone regeneration ability. More importantly, TP508 upregulated β-catenin and its target CYCLIN-D1 and could reverse the decreased osteogenic ability caused by LGK974.</p><p><strong>Conclusion: </strong>In conclusion, TP508 promotes bone regeneration in DO by activating the Wnt/β- catenin signaling pathway.</p>","PeriodicalId":10881,"journal":{"name":"Current pharmaceutical biotechnology","volume":" ","pages":"402-410"},"PeriodicalIF":2.2,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140101238","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Recent Developments in Nanotechnology and Immunotherapy for the Diagnosis and Treatment of Pancreatic Cancer. 用于诊断和治疗胰腺癌的纳米技术和免疫疗法的最新发展。
IF 2.2 4区 医学
Current pharmaceutical biotechnology Pub Date : 2025-01-01 DOI: 10.2174/0113892010284407240212110745
Komal Sindhi, Abhishek Kanugo
{"title":"Recent Developments in Nanotechnology and Immunotherapy for the Diagnosis and Treatment of Pancreatic Cancer.","authors":"Komal Sindhi, Abhishek Kanugo","doi":"10.2174/0113892010284407240212110745","DOIUrl":"10.2174/0113892010284407240212110745","url":null,"abstract":"<p><p>Pancreatic cancer kills millions of people worldwide each year and is one of the most prevalent causes of mortality that requires prompt therapy. A large number of people suffering from pancreatic cancer are detected at an advanced stage, with incurable and drug-resistant tumor, hence the overall survival rate of pancreatic cancer is less. The advance phase of this cancer is generated because of expression of the cancer-causing gene, inactivation of the tumorsuppressing gene, and deregulation of molecules in different cellular signalling pathways. The prompt diagnosis through the biomarkers significantly evades the progress and accelerates the survival rates. The overexpression of Mesothelin, Urokinase plasminogen activator, IGFR, Epidermal growth factor receptor, Plectin-1, Mucin-1 and Zinc transporter 4 were recognized in the diagnosis of pancreatic cancer. Nanotechnology has led to the development of nanocarriersbased formulations (lipid, polymer, inorganic, carbon based and advanced nanocarriers) which overcome the hurdles of conventional therapy, chemotherapy and radiotherapy which causes toxicity to adjacent healthy tissues. The biocompatibility, toxicity and large-scale manufacturing are the hurdles associated with the nanocarriers-based approaches. Currently, Immunotherapybased techniques emerged as an efficient therapeutic alternative for the prevention of cancer. Immunological checkpoint targeting techniques have demonstrated significant efficacy in human cancers. Recent advancements in checkpoint inhibitors, adoptive T cell therapies, and cancer vaccines have shown potential in overcoming the immune evasion mechanisms of pancreatic cancer cells. Combining these immunotherapeutic approaches with nanocarriers holds great promise in enhancing the antitumor response and improving patient survival.</p>","PeriodicalId":10881,"journal":{"name":"Current pharmaceutical biotechnology","volume":" ","pages":"143-168"},"PeriodicalIF":2.2,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139982543","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
In vitro Antileishmanial Activity and In silico Molecular Modeling Studies of Novel Analogs of Dermaseptins S4 and B2. Dermaseptins S4 和 B2 的新型类似物的体外抗利什曼活性和硅分子模型研究。
IF 2.2 4区 医学
Current pharmaceutical biotechnology Pub Date : 2025-01-01 DOI: 10.2174/0113892010296038240427050421
Houda Haddad, Klinger Antonio da Franca Rodrigues, Houcemeddine Othman, Leiz Maria Costa Veras, Raiza Raianne Luz Rodrigues, Ines Ouahchi, Bouraoui Ouni, Amira Zaϊri
{"title":"<i>In vitro</i> Antileishmanial Activity and <i>In silico</i> Molecular Modeling Studies of Novel Analogs of Dermaseptins S4 and B2.","authors":"Houda Haddad, Klinger Antonio da Franca Rodrigues, Houcemeddine Othman, Leiz Maria Costa Veras, Raiza Raianne Luz Rodrigues, Ines Ouahchi, Bouraoui Ouni, Amira Zaϊri","doi":"10.2174/0113892010296038240427050421","DOIUrl":"10.2174/0113892010296038240427050421","url":null,"abstract":"<p><strong>Background: </strong>Leishmaniasis is responsible for approximately 65,000 annual deaths. Various Leishmania species are the predominant cause of visceral, cutaneous, or mucocutaneous leishmaniasis, affecting millions worldwide. The lack of a vaccine, emergence of resistance, and undesirable side effects caused by antileishmanial medications have prompted researchers to look for novel therapeutic approaches to treat this disease. Antimicrobial peptides (AMPs) offer an alternative for promoting the discovery of new drugs.</p><p><strong>Methods: </strong>In this study, we detail the synthesis process and investigate the antileishmanial activity against <i>Leishmania (Viannia) braziliensis</i> for peptides belonging to the dermaseptin (DS) family and their synthetic analogs. The MTT assay was performed to investigate the cytotoxicity of these peptides on the murine macrophage cell line RAW 264.7. Subsequently, we performed molecular modeling analysis to explore the structure-function correlation of the derivatives interacting with the parasitic membrane.</p><p><strong>Results: </strong>All examined derivatives displayed concentration-dependent antileishmanial effect at low concentrations. Their effectiveness varied according to the peptide's proprieties. Notably, peptides with higher levels of charge demonstrated the most pronounced activities. Cytotoxicity assays showed that all the tested peptides were not cytotoxic compared to the tested conventional drug. The structure-function relationships demonstrated that the charged N-terminus could be responsible for the antileishmanial effect observed on promastigotes.</p><p><strong>Conclusion: </strong>Collectively, these results propose that dermaseptins (DS) might offer potential as promising candidates for the development of effective antileishmanial therapies.</p>","PeriodicalId":10881,"journal":{"name":"Current pharmaceutical biotechnology","volume":" ","pages":"276-288"},"PeriodicalIF":2.2,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142281697","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Development and Characterization of Polymeric-based Biomaterial from Agro-food Waste: A Sustainable and Eco-friendly Approach Towards Plastic Pollution. 从农业食品废弃物中开发聚合物生物材料并确定其特性:应对塑料污染的可持续和生态友好型方法。
IF 2.2 4区 医学
Current pharmaceutical biotechnology Pub Date : 2025-01-01 DOI: 10.2174/0113892010304507240528064315
Rabbia Hussain, Athar Aziz, Rashid Amin, Asma Khurshid
{"title":"Development and Characterization of Polymeric-based Biomaterial from Agro-food Waste: A Sustainable and Eco-friendly Approach Towards Plastic Pollution.","authors":"Rabbia Hussain, Athar Aziz, Rashid Amin, Asma Khurshid","doi":"10.2174/0113892010304507240528064315","DOIUrl":"10.2174/0113892010304507240528064315","url":null,"abstract":"<p><strong>Introduction: </strong>Commercial plastics are potentially hazardous and can be carcinogenic due to the incorporation of chemical additives along with other additional components utilized as brominated flame retardants and phthalate plasticizers during production that excessively produce large numbers of gases, litter, and toxic components resulting in environmental pollution.</p><p><strong>Methods: </strong>Biodegradable plastic derived from natural renewable resources is the novel, alternative, and innovative approach considered to be potentially safe as a substitute for traditional synthetic plastic as they decompose easily without causing any harm to the ecosystem and natural habitat. The utilization of undervalued compounds, such as by-products of fruits and vegetables in the production of biodegradable packaging films, is currently a matter of interest because of their accessibility, affordability, ample supply, nontoxicity, physiochemical and nutritional properties. Industrial food waste was processed under controlled conditions with appropriate plasticizers to extract polymeric materials. Biodegradability, solubility, and air test analysis were performed to examine the physical properties of polymers prior to the characterization of the biofilm by Fourier-transformed infrared spectroscopy (FTIR) for the determination of polymeric characteristics.</p><p><strong>Results: </strong>The loss of mass examined in each bioplastic film was in the range of 0.01g to 0.20g. The dimension of each bioplastic was recorded in the range of 4.6 mm to 28.7 mm. The existence of -OH, C=C, C=O stretching, and other crucial functional groups that aid in the creation of a solid polymeric material are confirmed by FTIR analysis. This study provides an alternative approach for sustainable and commercially value-added production of polymeric-based biomaterials from agro-industrial waste as they are rich in starch, cellulose, and pectin for the development of bio-plastics.</p><p><strong>Conclusion: </strong>The rationale of this project is to achieve a straightforward, economical, and durable method for the production of bio-plastics through effective utilization of industrial and commercial fruit waste, ultimately aiding in revenue generation.</p>","PeriodicalId":10881,"journal":{"name":"Current pharmaceutical biotechnology","volume":" ","pages":"550-563"},"PeriodicalIF":2.2,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141283236","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Integrated Serum Pharmacochemistry, Network Pharmacology, and Molecular Docking to Study the Mechanism of Rhubarb against Atherosclerosis. 综合血清药理化学、网络药理学和分子对接研究大黄抗动脉粥样硬化的机制
IF 2.2 4区 医学
Current pharmaceutical biotechnology Pub Date : 2025-01-01 DOI: 10.2174/0113892010296117240531071301
Zhi-Yan Cai, Shu-Jiao Li, Yu-Qing Wang
{"title":"Integrated Serum Pharmacochemistry, Network Pharmacology, and Molecular Docking to Study the Mechanism of Rhubarb against Atherosclerosis.","authors":"Zhi-Yan Cai, Shu-Jiao Li, Yu-Qing Wang","doi":"10.2174/0113892010296117240531071301","DOIUrl":"10.2174/0113892010296117240531071301","url":null,"abstract":"<p><strong>Background: </strong>Atherosclerosis (AS) is a chronic inflammatory disease characterized by the accumulation of lipids, the formation of lesion plaques, and the narrowing of arterial lumens. Rhubarb has significant effects against AS, but there is a lack of analysis and exploration of the mechanism of action of the transitional components in serum containing rhubarb.</p><p><strong>Objective: </strong>This work aims to combine serum pharmacochemistry, network pharmacology, and molecular docking to explore active ingredients and mechanism of rhubarb against AS.</p><p><strong>Method: </strong>Firstly, the components of rhubarb in blood samples were identified using HPLC-QTOF/ MS. The ingredients-targets-disease interaction network of rhubarb was constructed through network pharmacology. Then, molecular docking between the ingredients and the core targets was carried out using the Autodock Vina software.</p><p><strong>Results: </strong>Eleven active ingredients and five metabolites were preliminarily identified. The network pharmacology results showed that chrysophanol, resveratrol, and emodin might have potential pharmacological effects on AS. The PPI network showed that the key proteins were PTGS2, ESR1, PTGS1, and ELANE. GO analysis revealed that genes were mainly enriched in the inflammatory response and response to exogenous stimuli. Moreover, these genes were related to IL-17 signaling pathways, lipid and atherosclerosis, and other pathways. Molecular docking analyses showed that chrysophanol and emodin have strong binding affinities with the target proteins PTGS2 and PTGS1.</p><p><strong>Conclusion: </strong>A comprehensive strategy combining serum pharmacochemistry with network pharmacology and molecular docking was employed to investigate the active ingredients and the mechanism of rhubarb in treating AS, which provided a basis for studying the pharmacological effects and action mechanisms of rhubarb.</p>","PeriodicalId":10881,"journal":{"name":"Current pharmaceutical biotechnology","volume":" ","pages":"564-575"},"PeriodicalIF":2.2,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141283234","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
DHA and Cancer: The Uncharted Territory of Nutritional Oncology. DHA 与癌症:营养肿瘤学的未知领域。
IF 2.2 4区 医学
Current pharmaceutical biotechnology Pub Date : 2025-01-01 DOI: 10.2174/0113892010305256240422110943
Devank Shekho, Abhishek Chauhan, Ritika Mishra, Ankit Awasthi
{"title":"DHA and Cancer: The Uncharted Territory of Nutritional Oncology.","authors":"Devank Shekho, Abhishek Chauhan, Ritika Mishra, Ankit Awasthi","doi":"10.2174/0113892010305256240422110943","DOIUrl":"10.2174/0113892010305256240422110943","url":null,"abstract":"","PeriodicalId":10881,"journal":{"name":"Current pharmaceutical biotechnology","volume":" ","pages":"313-315"},"PeriodicalIF":2.2,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140847211","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Correlation between Honey Parameters and Wound Healing Properties: The Case of Piedmont (Italy) Samples. 蜂蜜参数与伤口愈合特性之间的相关性:皮埃蒙特(意大利)样本案例。
IF 2.2 4区 医学
Current pharmaceutical biotechnology Pub Date : 2025-01-01 DOI: 10.2174/0113892010328741240828093859
Simona Martinotti, Gregorio Bonsignore, Mauro Patrone, Elia Ranzato
{"title":"Correlation between Honey Parameters and Wound Healing Properties: The Case of Piedmont (Italy) Samples.","authors":"Simona Martinotti, Gregorio Bonsignore, Mauro Patrone, Elia Ranzato","doi":"10.2174/0113892010328741240828093859","DOIUrl":"10.2174/0113892010328741240828093859","url":null,"abstract":"<p><strong>Introduction: </strong>Honey possesses several positive properties, making it effective in wound healing mechanisms. However, very little information is available on the different honey types for wound healing activity.</p><p><strong>Method: </strong>In the first \"Academy of Sciences\", a public engagement project with high school students, we assessed the properties of thirteen kinds of honey from the Piedmont area (Nord West Italy). In particular, we characterized the color intensity (by Pfund scale), total phenolic content (TPC), total flavonoid content (TFC), H<sup>2</sup>O<sup>2</sup> production, and wound closure rate.</p><p><strong>Results: </strong>Then, we tried to verify the presence of a correlation between these parameters, finding a positive correlation between H<sup>2</sup>O<sup>2</sup> and wound closure rate.</p><p><strong>Conclusion: </strong>These data pave the way to characterize different types of Italian honey to completely understand its potential.</p>","PeriodicalId":10881,"journal":{"name":"Current pharmaceutical biotechnology","volume":" ","pages":"302-311"},"PeriodicalIF":2.2,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142139469","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Revolutionizing Rheumatoid Arthritis Care: AI-infused Herbal Treatments and the Road Ahead. 类风湿性关节炎护理的革命:人工智能草药疗法和未来之路。
IF 2.2 4区 医学
Current pharmaceutical biotechnology Pub Date : 2025-01-01 DOI: 10.2174/0113892010305528240506114408
Milan Singh Kahlon, Md Moidul Islam, Abhinav Vashishat, Sarjana Raikwar
{"title":"Revolutionizing Rheumatoid Arthritis Care: AI-infused Herbal Treatments and the Road Ahead.","authors":"Milan Singh Kahlon, Md Moidul Islam, Abhinav Vashishat, Sarjana Raikwar","doi":"10.2174/0113892010305528240506114408","DOIUrl":"10.2174/0113892010305528240506114408","url":null,"abstract":"","PeriodicalId":10881,"journal":{"name":"Current pharmaceutical biotechnology","volume":" ","pages":"316-318"},"PeriodicalIF":2.2,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140956565","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Inhibitory Activity of Quercetin, Rutin, and Hyperoside against Xanthine Oxidase: Kinetics, Fluorescence, and Molecular Docking. 槲皮素、芦丁和金丝桃苷对黄嘌呤氧化酶的抑制活性:动力学、荧光和分子对接。
IF 2.2 4区 医学
Current pharmaceutical biotechnology Pub Date : 2025-01-01 DOI: 10.2174/0113892010297269240427055003
Yali Yu, Yingzhu Xiong, Siman Tong, Yanli Li, Rongcan Cai, Xv Zhang, Feng Gao
{"title":"Inhibitory Activity of Quercetin, Rutin, and Hyperoside against Xanthine Oxidase: Kinetics, Fluorescence, and Molecular Docking.","authors":"Yali Yu, Yingzhu Xiong, Siman Tong, Yanli Li, Rongcan Cai, Xv Zhang, Feng Gao","doi":"10.2174/0113892010297269240427055003","DOIUrl":"10.2174/0113892010297269240427055003","url":null,"abstract":"<p><strong>Introduction: </strong>Quercetin (Qc), rutin (Ru), and hyperoside (Hyp) are three common polyphenols widely distributed in the plant kingdom.</p><p><strong>Methods: </strong>This study explored the inhibition and mechanisms of Qc, Ru, and Hyp against xanthine oxidase (XOD) by enzyme kinetic analysis, fluorescence analysis, and molecular docking. The inhibitory activities of the three polyphenols on XOD showed the following trend: quercetin > hyperoside > rutin, with IC<sub>50</sub> values of 8.327 ± 0.36 μmol/L, 35.215 ± 0.4 μmol/L and 60.811 ± 0.19 μmol/L, respectively. All three polyphenols inhibited xanthine oxidase activity in a mixed-competitive manner. Synchronous fluorescence results demonstrated that three polyphenols binding to XOD were spontaneous and showed static quenching.</p><p><strong>Results: </strong>The binding of the three polyphenols to XOD is mainly driven by hydrogen bonding and van der Waals forces, resulting in the formation of an XOD-XA complex with only one affinity binding site. The binding sites of the three RSFQ phenolic compounds are close to those of tryptophan. Molecular docking showed that all three polyphenols enter the active pocket of XOD and maintain the stability of the complex through hydrogen bonding, hydrophobic interaction, and van der Waals forces.</p><p><strong>Conclusion: </strong>The results provide a theoretical basis for quercetin, rutin, and hyperoside to be used as function factors to prevent hyperuricemia.</p>","PeriodicalId":10881,"journal":{"name":"Current pharmaceutical biotechnology","volume":" ","pages":"513-524"},"PeriodicalIF":2.2,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140956433","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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