Combinatorial chemistry & high throughput screening最新文献

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Therapeutic Effects and Molecular Mechanism of Banxia Xiexin Decoction on Intestinal Mucosal Barrier Function in Sepsis. 半夏泻心汤对脓毒症患者肠黏膜屏障功能的影响及分子机制。
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-04-29 DOI: 10.2174/0113862073349597250410111941
Wen Dai, Lei Zhou, Hao Hao, Diankui Wang, Feihu Zhang, Peng Wang, Lin Wang, Li Kong
{"title":"Therapeutic Effects and Molecular Mechanism of Banxia Xiexin Decoction on Intestinal Mucosal Barrier Function in Sepsis.","authors":"Wen Dai, Lei Zhou, Hao Hao, Diankui Wang, Feihu Zhang, Peng Wang, Lin Wang, Li Kong","doi":"10.2174/0113862073349597250410111941","DOIUrl":"https://doi.org/10.2174/0113862073349597250410111941","url":null,"abstract":"<p><strong>Aim: </strong>This study aims to investigate therapeutic effects and involved molecular mechanisms of Banxia Xiexin Decoction (BXD) in reducing gastrointestinal complications associated with sepsis.</p><p><strong>Background: </strong>Sepsis is a common critical illness that threatens patient survival and costs society a lot. This syndrome is a prominent cause of death in ICUs due to its high mortality rate, which exceeds 30% after 28 days and 35.5% after 90 days. Sepsis remains a major medical challenge despite a 20%-30% drop in fatality rates due to a better understanding of its physiological and pathological features and better therapeutic techniques. There is no pharmacological treatment for sepsis, highlighting the need for more study.</p><p><strong>Objective: </strong>We explored the protecting effects of BXD on intestinal functionality in sepsis by investigating its roles in the regulation of mitochondrial autophagy and mitochondrial functioning in small intestinal epithelial cells, primarily via the PINK1/Parkin signaling pathway.</p><p><strong>Method: </strong>We established a cell model of Human Intestinal Epithelial Cell (HIEC) injury induced by lipopolysaccharide (LPS) and a cecal ligation and perforation (CLP) sepsis model in Sprague Dawley (SD) rats. The cell model and animal model of sepsis were divided into control groups and different treatment groups that received different doses of BXD. We utilized HIECs with PINK1 knockdown to assess BXD's protective effects on the sepsis intestinal barrier and its regulatory mechanism both on the PINK1/Parkin signaling pathway, exploring both its facilitative and inhibitory effects. ELISA method was used to measure inflammatory markers IL-6, IL-1β, and intestinal injury-related molecules IFABP and DAO. Pathological assessments were performed with H&E staining, and tight junction proteins ZO-1 and Occludin were detected using immunohistochemical staining. Mitochondrial membrane protein TOM20 was detected through immunofluorescence staining. Mitochondrial membrane potential and autophagy were assessed via flow cytometry. The expression levels of PINK1, Park, LC3, and p62 proteins and mRNA, integral to the PINK1/Parkin autophagy pathway, were evaluated using Western Blot and RT-PCR.</p><p><strong>Results: </strong>Compared to the control group, BXD therapy significantly lowered serum DAO, IFABP, and DA. The BXD therapy group showed a more significant and sustained drop in IL-6 and IL-1β levels than the control group. The BXD therapy reduced intestinal mucosa damage by lowering DAO and IFABP. BXD also restored tight junction proteins ZO-1 and Occludin, improving intestinal mucosal barrier function. In septic rats, BXD therapy lowered serum IL-6 and IL-1β levels, avoiding inflammation and reducing intestinal damage. BXD enhanced TOM20, which protected intestinal epithelial cell mitochondria against decreasing mitochondrial membrane potential. BXD increased the PINK1/Parkin mitochondrial ","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143991563","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
Unlocking the Potential of Ketamine: A Systematic Review and Meta-analysis of its Safety and Efficacy in Acute Pain Management. 解锁氯胺酮的潜力:其在急性疼痛管理中的安全性和有效性的系统回顾和荟萃分析。
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-04-29 DOI: 10.2174/0113862073377616250404101442
Xiaojuan Chou, Wenhua Zha, Jian Hu, Chen Chen, Rajesh K Singh, Geng Liu
{"title":"Unlocking the Potential of Ketamine: A Systematic Review and Meta-analysis of its Safety and Efficacy in Acute Pain Management.","authors":"Xiaojuan Chou, Wenhua Zha, Jian Hu, Chen Chen, Rajesh K Singh, Geng Liu","doi":"10.2174/0113862073377616250404101442","DOIUrl":"https://doi.org/10.2174/0113862073377616250404101442","url":null,"abstract":"<p><strong>Background: </strong>The management of acute pain is a crucial and challenging component of emergency care. The pursuit of an ideal drug that alleviates pain rapidly and with fewer side effects is an ongoing endeavor.</p><p><strong>Objective: </strong>This meta-analysis reviews the safety and efficacy of ketamine in adult emergency department (ED) patients experiencing acute pain.</p><p><strong>Methodology: </strong>This study was limited to randomized controlled trials (RCTs). The comparative group was morphine or other opioids or placebo, whereas the experimental group was ketamine. The primary outcome measures, in addition to adverse events, were the numeric rating scale (NRS). The included studies were subjected to analysis using the Review Manager Database. The non-significant changes in pain score were observed in the ketamine group at 10 minutes [- 0.46 (-2.03, 1.10)], 30 minutes [-0.13 (-0.62, 0.37)], and 60 minutes [-0.18 (-0.97, 0.61)] as compared to the control group.</p><p><strong>Results: </strong>The significant changes were observed at 15 minutes [-4.11 (-7.91, -0.31)] in the ketamine group as compared to the control group. The overall risk ratio (1.20 [95% Confidence interval (CI), 0.93 to 1.55] indicated a non-significant difference in adverse events in the control group as compared to the ketamine group. The heterogeneity among included studies was found to be higher, as indicated by the I2 statistics.</p><p><strong>Conclusion: </strong>There were no significant differences in adverse events between the ketamine and the control groups. More randomized clinical trials are needed to determine ketamine's involvement in acute pain at 10, 30, and 60 minutes.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143980520","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
Exploring the Active Ingredients and Core Targets of Erxia Decoction in the Treatment of Sleep Disorder by Integration of Network Pharmacology and Proteomics. 网络药理学与蛋白质组学相结合探讨二夏汤治疗睡眠障碍的有效成分及核心靶点。
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-04-29 DOI: 10.2174/0113862073348555250320035548
Bo Jiang, Huiran Yang, Fei Zhou, Huijun Qu, Xueqian Hu, Zhanwen Liu
{"title":"Exploring the Active Ingredients and Core Targets of Erxia Decoction in the Treatment of Sleep Disorder by Integration of Network Pharmacology and Proteomics.","authors":"Bo Jiang, Huiran Yang, Fei Zhou, Huijun Qu, Xueqian Hu, Zhanwen Liu","doi":"10.2174/0113862073348555250320035548","DOIUrl":"https://doi.org/10.2174/0113862073348555250320035548","url":null,"abstract":"<p><strong>Aims: </strong>For clarifying the \"multi genes and multi targets\" characteristic of the treatment of Erxia Decoction (EXD), the aim of this study was to employ network pharmacology technology to perform cluster analysis on selected EXD targets.</p><p><strong>Background: </strong>EXD, a famous Chinese herbal prescription, consisting of Pinelliae Rhizoma (PR) and Prunellae Spica (PS), was mainly used to treat sleep disorder (SLD).</p><p><strong>Objective: </strong>Using network pharmacology combined with proteomics to find out the main active components and core targets of EXD in the treatment of SLD.</p><p><strong>Method: </strong>By constructing the network of drug-component-target, the key protein targets of EXD for the treatment of SLD were screened. Then the interaction of the main active components of EXD and predicted candidate targets were verified. Then the proteomic analysis was used to screen the core targets in BV2 cells treated with EXD or the chemical ingredients, and the expression level was validated by Western blotting. Finally, molecular docking was used to further evaluate the mechanism of the action of the main ingredients and the core targets.</p><p><strong>Result: </strong>The 24 components of EXD mainly participate in the SLD treatment process by acting on 15 important key genes, and the core signal pathways were identified in the process of the action of EXD in treating SLD. Four key ingredients and five core targets were revealed from the results of network pharmacological analysis combination with proteomics, and then the AKT1 protein as a key target was validated by PCR and Western blotting.</p><p><strong>Conclusion: </strong>This study preliminarily revealed EXD, morin (MOR) and quercetin (QUE) mainly inhibited the AKT1 core targets for the treatment of SLD using the network pharmacological analysis, proteomics, Western blotting, and molecular docking. The results elucidated partly the molecular mechanism and provided clues and a basis for further research.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143971709","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
Effectiveness and Safety of Butyphthalide Injection in Treatment of Aphasia after Cerebral Infarction: A Meta-analysis. 丁苯酞注射液治疗脑梗死后失语的有效性和安全性:一项荟萃分析。
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-04-29 DOI: 10.2174/0113862073368524250313053657
Xiongying Huang, Yuan Xie, Yingchen Li
{"title":"Effectiveness and Safety of Butyphthalide Injection in Treatment of Aphasia after Cerebral Infarction: A Meta-analysis.","authors":"Xiongying Huang, Yuan Xie, Yingchen Li","doi":"10.2174/0113862073368524250313053657","DOIUrl":"https://doi.org/10.2174/0113862073368524250313053657","url":null,"abstract":"<p><strong>Objective: </strong>The objective of this study is to evaluate the efficacy and safety of butylphthalide injection in the treatment of aphasia after cerebral infarction.</p><p><strong>Methods: </strong>CNKI, Wanfang database, Duxiu, VIP, CBM, PubMed, Embase, Web of Science, Cochrane, and Socolar databases were searched from the establishment of the database to August 2024. According to the topic of butylphthalide injection treated aphasia after cerebral infarction, the eligible RCT was selected and meta-analysis was performed using RevMan 5.4 software and stata16 software. Two researchers independently screened the study, extracted the basic information in the study, and assessed the risk of bias in the study.</p><p><strong>Results: </strong>A total of 1047 patients were included in 12 articles, including 524 patients in the experimental group (butylphthalide injection + conventional/special speech rehabilitation training) and 523 patients in the control group (conventional/special speech rehabilitation). The results of meta-analysis showed that the total clinical efficacy of the experimental group was better than that of the control group (RR=1.29, 95%CI: 1.17-1.43, Z=4.98, P < 0.0000). The National Institutes of Health Stroke Scale (NIHSS) score of the experimental group was lower than that of the control group (conventional language rehabilitation training group: MD=-4.11,95%CI: -4.44~- 3.78, Z=24.38, P < 0.00001; special language rehabilitation training group: MD=-2.53, 95%CI: - 3.77 ~ -1.28, Z=3.97, P < 0.00001). Aphasia Quotient (AQ) scores of experimental groups were higher than those of control group (conventional language rehabilitation training group: MD=11.10, 95%CI: 10.26 ~ 11.94, Z=25.97, P<0.00001; special language rehabilitation training group: MD=5.23, 95%CI: 3.34~7.11, Z=5.44, P<0.00001); Adverse reactions: P>0.05, no statistical significance.</p><p><strong>Conclusion: </strong>Butylphthalide injection is effective and safe in the treatment of aphasia after cerebral infarction.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143986632","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
Exploring Potential Bifunctional Peptides with Anti-tyrosinase and Antioxidant Activities from Porphyra Protolysate Using in Silico Analysis. 利用硅分析从卟啉水解物中寻找具有抗酪氨酸酶和抗氧化活性的潜在双功能肽。
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-04-29 DOI: 10.2174/0113862073341023250113053959
Si-Bo Huang, Pei-Xia Feng, Liu-Ying Li, Hong-Hui Guo, En-Qin Xia
{"title":"Exploring Potential Bifunctional Peptides with Anti-tyrosinase and Antioxidant Activities from Porphyra Protolysate Using in Silico Analysis.","authors":"Si-Bo Huang, Pei-Xia Feng, Liu-Ying Li, Hong-Hui Guo, En-Qin Xia","doi":"10.2174/0113862073341023250113053959","DOIUrl":"https://doi.org/10.2174/0113862073341023250113053959","url":null,"abstract":"<p><strong>Background: </strong>Extracts from Porphyra have been detected to have antioxidant activity and tyrosinase (TYR) inhibitory activity. However, bioactive peptides (BPs) released from Porphyra proteins (PPs) have not been comprehensively reported.</p><p><strong>Objective: </strong>The aim of this study is to rapidly identify bifunctional peptides with antioxidant and TYR inhibitory activities from a large number of digested peptides from PPs.</p><p><strong>Methods: </strong>In this study, a total of 3,288 proteins from six main species of Porphyra were collected, and the antioxidant potential (AP) was evaluated. Hydrolyzed peptides with 2-8 amino acid lengths were collected and known antioxidants were removed. Next, these peptides were further screened using ADMET analysis. Finally, the DPPH· scavenging potential (IC50) and TYR inhibition potential (TIP) of these peptides were further predicted by QSAR models and molecular docking based pharmacophore models, respectively.</p><p><strong>Results: </strong>The most released antioxidant peptides after digestion of all types of PPs were dipeptides with sequences EL, IR and AY. In addition, 44,689 short non-repeatable peptides were swirled in these hydrolysates, which have not yet been reported to have antioxidant activity. Next, 337 of these digested peptides were predicted to be absorbed without hepato-renal toxicity and had virtual metabolic scores > 0.01%. Finally, 138 peptides were predicted to have AP and TIP.</p><p><strong>Conclusion: </strong>Porphyra is a kind of promising source rich in bifunctional peptides. Present study adopted an innovative method with some free scripts to rapid discovery of bifunctional peptides from a large number of unknown PPs.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143957262","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
Deciphering the Microbiome-Gut-Eye Axis: A Mendelian Randomization Analysis of the Causal Influence of Gut Microbiota on Myopia. 解读微生物群-肠道-眼睛轴:肠道微生物群对近视因果影响的孟德尔随机化分析。
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-04-29 DOI: 10.2174/0113862073385717250415110224
Weicheng Xu, Wei Shi
{"title":"Deciphering the Microbiome-Gut-Eye Axis: A Mendelian Randomization Analysis of the Causal Influence of Gut Microbiota on Myopia.","authors":"Weicheng Xu, Wei Shi","doi":"10.2174/0113862073385717250415110224","DOIUrl":"https://doi.org/10.2174/0113862073385717250415110224","url":null,"abstract":"<p><strong>Background: </strong>The intricate relationship between the gut microbiome and myopia is increasingly recognized, underscoring the need to explore its causal dynamics. Despite emerging evidence, the influence of Gut Microbiota (GM) on ocular development remains underexplored.</p><p><strong>Methods: </strong>This study utilized Mendelian Randomization (MR) to investigate the causal impact of GM on the development of myopia. Instrumental variables (IVs) were identified from Genome- Wide Association Studies (GWAS), focusing on genetic variants significantly associated with microbiome composition. A comprehensive array of MR techniques was applied to ensure a robust estimation of causal effects and to adjust for potential confounders and pleiotropy.</p><p><strong>Results: </strong>The Inverse-Variance Weighted (IVW) method was used to identify significant associations between GM and myopia. Increased risk of myopia was linked to the class Betaproteobacteria (OR=1.01, 95% CI 1.004-1.017, P=0.003), the order Burkholderiales (OR=1.009, 95% CI 1.001-1.016, P=0.02), the family Oxalobacteraceae (OR=1.005, 95% CI 1.001-1.01, P=0.023), and several genera including Eubacterium xylanophilum group (OR=1.007, 95% CI 1.001-1.013, P=0.033), and Bifidobacterium (OR=1.005, 95% CI 1-1.01, P=0.038). Protective effects were noted for the order Mollicutes RF9 (OR=0.994, 95% CI 0.99-0.999, P=0.014), the genus Allisonella (OR=0.996, 95% CI 0.993-0.999, P=0.019), the genus Lachnospiraceae UCG001 (OR=0.994, 95% CI 0.989-1, P=0.045), and the family Enterobacteraceae (OR=0.991, 95% CI 0.982-1, P=0.047) and order Enterobacteriales (OR=0.991, 95% CI 0.982-1, P=0.047). Sensitivity analyses further confirmed the robustness of these findings.</p><p><strong>Conclusions: </strong>The findings support the \"Microbiome-Gut-Eye Axis\" as a potential factor in myopia pathogenesis and highlight microbiota-targeted interventions as novel therapeutic strategies for managing myopia. This study lays the groundwork for further research on how modifying GM can influence eye health and offers new perspectives on preventive health strategies.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143982771","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
Mutation Mapping of PD-L1 Expression in Advanced Non-small Cell Lung Cancer: A Real-world Retrospective Cohort Study. PD-L1表达在晚期非小细胞肺癌中的突变定位:一项真实世界的回顾性队列研究。
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-04-25 DOI: 10.2174/0113862073368808250416035054
Fang Hao, Qing Ma, Diansheng Zhong
{"title":"Mutation Mapping of PD-L1 Expression in Advanced Non-small Cell Lung Cancer: A Real-world Retrospective Cohort Study.","authors":"Fang Hao, Qing Ma, Diansheng Zhong","doi":"10.2174/0113862073368808250416035054","DOIUrl":"https://doi.org/10.2174/0113862073368808250416035054","url":null,"abstract":"<p><strong>Background: </strong>The duration of response to immune checkpoint inhibitors (ICIs) varies because of tumor immune heterogeneity, and employing programmed death receptor ligand 1 (PD-L1) expression to evaluate the efficacy of anti-programmed cell death-1 (PD-1)/PD-L1 antibodies remains controversial.</p><p><strong>Method: </strong>A total of 138 advanced non-small cell lung cancer (NSCLC) patients were subdivided into 2 groups - 52 patients with a PD-L1 Expression≥50% and 86 patients with a PD-L1 Expression <50% - based on next-generation sequencing (NGS) to analyze multiple-dimensional data types, including tumor mutation burden (TMB), gene alterations, gene enrichment analysis, therapy response, and immune-related adverse events (irAEs).</p><p><strong>Results: </strong>High levels of PD-L1 expression were significantly associated with advanced age and TMB status. The PD-L1≥50% cohort presented mutations of KRAS, NOTCH1, and FAT, while the PD-L1<50% group exhibited mutations of EGFR, PTEN, or LATS1/2. Except for the ascertained DNA damage response regulation. Even though there was no significant difference between PD-L1≥50% and PD-L1<50% cohorts on therapy response, patients with a PD-L1 Expression≥ 50% elicited a high irAEs incidence rate and increased plasma interleukin 6 (IL-6) concentration.</p><p><strong>Conclusion: </strong>This real-world retrospective study suggested that high expression of PD-L1 exhibited inappropriate activation of different pathways and collaborated with anti-cytokines and chemokines therapy may optimize clinical therapy efficacy.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-04-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143986880","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
HuangE Capsules Improve Bladder Function in BOO-induced Overactive Bladder Rats: Network Pharmacology and Experimental Validation. 黄歌胶囊改善boo诱导膀胱过度活动大鼠膀胱功能:网络药理学及实验验证。
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-04-25 DOI: 10.2174/0113862073373430250415070358
Peizhe Li, Yuewen Pang, Shiyu Zhao, Heyang Liu, Siyu Han, Ran Zhong, Shuang He, Jing Shi, Haisheng Cheng, Yongji Yan, Junyao Duan, Huijie Gong
{"title":"HuangE Capsules Improve Bladder Function in BOO-induced Overactive Bladder Rats: Network Pharmacology and Experimental Validation.","authors":"Peizhe Li, Yuewen Pang, Shiyu Zhao, Heyang Liu, Siyu Han, Ran Zhong, Shuang He, Jing Shi, Haisheng Cheng, Yongji Yan, Junyao Duan, Huijie Gong","doi":"10.2174/0113862073373430250415070358","DOIUrl":"https://doi.org/10.2174/0113862073373430250415070358","url":null,"abstract":"<p><strong>Aims: </strong>Our objective is to assess the therapeutic impact of HEC on OAB rats and investigate potential mechanisms.</p><p><strong>Background: </strong>Overactive bladder (OAB) is a syndrome of urinary storage symptoms characterized by \"urinary urgency with or without urinary acute incontinence, usually accompanied by increased daytime and nocturnal urination\", which impacts patients' quality of life. We found the potential therapeutic impact of HuangE capsules (HEC) on OAB patients through clinical practice. However, the exact effect and mechanism of action remain unclear.</p><p><strong>Methods: </strong>We developed a \"drugs- active ingredients- targets- diseases\" network and employed the pathway enrichment analysis to identify the potential mechanisms of HEC on OAB. Bladder outlet obstruction (BOO) models and sham-operated ones were established in healthy male Wistar rats through surgical procedures. Following 28 days of continuous gavage administration of HEC, saturated copper sulfate test paper was utilized to quantify the frequency of urination over a 24- hour period. Subsequently, cystostomy was conducted to perform cystometry, and Masson staining was applied to a portion of the bladder tissue. Finally, we investigated the Rho/Rho-kinase pathway's expression and assessed the oxidative stress and inflammatory factor levels in the rat bladder through western blotting and ELISA techniques.</p><p><strong>Results: </strong>Through network pharmacological analysis, we identified RhoA/Rho-kinase pathway and cytokine including TNF-α, IL-6, SOD and MDA as potential mechanisms of HEC on OAB. The rats in the 2× HuangE group exhibited significantly enhanced urodynamic outcomes and decreased 24-hour urination frequency compared to the model group. Masson staining indicated a decrease in the proportion of collagenous tissue and an improvement in histomorphology. We observed a decrease expression of RhoA, ROCK1, and ROCK2 protein in the bladder tissue of 2× HuangE group rats, along with elevated SOD levels and decreased levels of TNF-α, IL-6, and MDA.</p><p><strong>Conclusion: </strong>HEC could improve bladder function and morphology in BOO-induced OAB rats by reducing the expression of RhoA, ROCK1, and ROCK2 and lowering levels of oxidative stress and inflammation.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-04-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143966841","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
Shenhuang Liuwei Powder Alleviates Streptozotocin-Induced Diabetic Ulcers in Rats through the Inhibition of the AGE/RAGE Signaling Pathway and Promotion of Antibacterial Activity and Angiogenesis via Activation of the PI3K/Akt/eNOS/HIF-1α Pathway. 参黄六味散通过激活PI3K/Akt/eNOS/HIF-1α通路,抑制AGE/RAGE信号通路,促进抗菌活性和血管生成,减轻链脲佐菌素诱导的大鼠糖尿病溃疡。
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-04-24 DOI: 10.2174/0113862073370028250326071104
Jun Li, Qian Zhang, Shengnan Li, Shu Wang, Fengye Zhou, Haifeng Zhang, Jianping Chen
{"title":"Shenhuang Liuwei Powder Alleviates Streptozotocin-Induced Diabetic Ulcers in Rats through the Inhibition of the AGE/RAGE Signaling Pathway and Promotion of Antibacterial Activity and Angiogenesis via Activation of the PI3K/Akt/eNOS/HIF-1α Pathway.","authors":"Jun Li, Qian Zhang, Shengnan Li, Shu Wang, Fengye Zhou, Haifeng Zhang, Jianping Chen","doi":"10.2174/0113862073370028250326071104","DOIUrl":"https://doi.org/10.2174/0113862073370028250326071104","url":null,"abstract":"<p><strong>Aims and objective: </strong>Shenhuang Liuwei powder (SHLWP) is frequently used to treat diabetic ulcers (DUs), but its mechanism of action remains poorly understood. This study aimed to identify the active compounds and mechanisms by which SHLWP alleviates DUs.</p><p><strong>Methods: </strong>The chemical components of SHLWP were analyzed using high-resolution mass spectrometry (HRMS). Network pharmacology based on HRMS data identified SHLWP-associated targets and signaling pathways. Its antibacterial activity was assessed using Kirby-Bauer disc diffusion and minimum inhibitory concentration (MIC) tests. Its in vivo pharmacological effects were evaluated in a streptozotocin-induced diabetic ulcer model in Sprague-Dawley (SD) rats.</p><p><strong>Results: </strong>Seventy-three components were identified in SHLWP, with key constituents including caffeic acid (13.11 ± 0.14 μg/g), ferulic acid (20.40 ± 0.24 μg/g), quercetin (8.49 ± 0.18 μg/g), luteolin (36.63 ± 0.19 μg/g), apigenin (82.14 ± 1.60 μg/g), and linoleic acid (507.59 ± 1.46 μg/g). SHLWP exhibited strong antibacterial activity against Staphylococcus aureus (MIC = 7.8125 μg/mL), Streptococcus pyogenes (MIC < 3.90625 μg/mL), and Streptococcus epidermidis (MIC < 3.90625 μg/mL). Network pharmacology revealed significant enrichment of the AGE/RAGE, HIF-1, and PI3K-Akt pathways, which was validated in vivo using qPCR, immunohistochemistry, and Western blot.</p><p><strong>Conclusion: </strong>SHLWP alleviated streptozotocin-induced diabetic ulcers by inhibiting the AGE/RAGE pathway and promoting antibacterial activity and angiogenesis via the PI3K/Akt/eNOS/HIF-1α pathway, providing a biological basis for its therapeutic effects.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143968329","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
Eco-friendly Advancements through Fish Waste: A Review of Therapeutic and Industrial Innovations. 鱼类废弃物的生态友好进步:治疗和工业创新综述。
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-04-24 DOI: 10.2174/0113862073372954250408181058
Saddam Hussain, Aminur Rahman, Pranab Borah, Arlin Sen, Raju Bharalee, Mayuri Chabukdhara, Hrishikesh Upadhyaya, Akalesh Kumar Verma
{"title":"Eco-friendly Advancements through Fish Waste: A Review of Therapeutic and Industrial Innovations.","authors":"Saddam Hussain, Aminur Rahman, Pranab Borah, Arlin Sen, Raju Bharalee, Mayuri Chabukdhara, Hrishikesh Upadhyaya, Akalesh Kumar Verma","doi":"10.2174/0113862073372954250408181058","DOIUrl":"https://doi.org/10.2174/0113862073372954250408181058","url":null,"abstract":"<p><p>Fish waste, a significant by-product of the fisheries industry, presents both an environmental challenge and a valuable resource. This review delves into the innovative approaches to harness the potential of fish waste for various applications, particularly in the biomedical and industrial sectors. Therapeutically, fish waste yields valuable bioactive compounds such as omega-3 fatty acids, collagen peptides, and gelatine, which are known to benefit cardiovascular, skin, and immune health. Fish-derived collagen, for instance, is employed in wound healing, bone regeneration, and cosmetic applications due to its biocompatibility and lower infection risk compared to land-animal sources. Omega-3 fatty acids from fish waste exhibit anti-inflammatory, anticancer adding value to pharmaceutical industries. Industrially, fish waste can be transformed into eco-friendly materials like bioplastics, biofuels, and biofertilizers, contributing to environmental sustainability. Bioplastics synthesized from fish scales and biotextiles developed from collagen-modified polyester exemplify sustainable alternatives to synthetic materials. Additionally, fish-based biofertilizers enhance soil fertility, promoting greener agriculture. Innovations also include the production of fish-based leather, low-cost fish peptones for microbial culture, and fish oil-based biofuel with diesel-like properties, showcasing versatile applications. This review explores the untapped potential of fish waste, emphasizing its underutilized yet high-value therapeutic and industrial applications. Unlike existing studies, it focuses on lesser-explored areas such as fish-derived biofertilizers for precision agriculture and fish-based bioplastics for sustainable packaging. These applications can significantly reduce pollution, promote non-toxic alternatives, and contribute to sustainable industries. By leveraging fish waste, this review aims to address environmental challenges, support global health initiatives, and highlight innovative solutions for a circular economy.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143969440","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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