Combinatorial chemistry & high throughput screening最新文献

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Resveratrol Reduces Cisplatin-induced Cochlear Hair Cell Pyroptosis by Inhibiting the mtROS/TXNIP/NLRP3 Pathway.
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-01-22 DOI: 10.2174/0113862073354456241219065512
Andi Peng, Jiahui Peng, Ruosha Lai, Wei Liu, Xubo Chen, Bing Hu, Yingying Xu, Lihua Li
{"title":"Resveratrol Reduces Cisplatin-induced Cochlear Hair Cell Pyroptosis by Inhibiting the mtROS/TXNIP/NLRP3 Pathway.","authors":"Andi Peng, Jiahui Peng, Ruosha Lai, Wei Liu, Xubo Chen, Bing Hu, Yingying Xu, Lihua Li","doi":"10.2174/0113862073354456241219065512","DOIUrl":"https://doi.org/10.2174/0113862073354456241219065512","url":null,"abstract":"<p><strong>Background: </strong>Cisplatin is an effective anti-cancer drug with limited clinical applications due to ototoxicity. Resveratrol, known for its antioxidant and anti-inflammatory properties, has been reported to mitigate these adverse effects, although the underlying mechanism remains under-researched.</p><p><strong>Objective: </strong>This study aimed to investigate the effects and underlying mechanisms of resveratrol on cisplatin-induced ototoxicity.</p><p><strong>Methods: </strong>Ototoxicity was modeled in House Ear Institute-Organ of Corti 1 (HEI-OC1) cells by cisplatin exposure, followed by interventions using thioredoxin-interacting protein (TXNIP) siRNA transfection, MitoQ, or resveratrol. Apoptosis and proliferation were quantitatively assessed using terminal deoxynucleotidyl transferase (TdT)-mediated dUTP nick-end labeling (TUNEL) and Ki67 immunostaining. Quantitative real-time PCR (qRT-PCR) and western blotting were used to measure the changes in mRNA and protein levels. Flow cytometry and enzyme- linked immunosorbent assay (ELISA) were used to analyze pyroptotic cells and inflammatory responses. Reactive oxygen species (ROS) production was tracked using 2', 7'- dichlorofluorescein diacetate (DCFH-DA) staining and flow cytometry. Mitochondrial Membrane Potential (MMP) and mitochondrial permeability transition pore (MPTP) opening levels were analyzed through tetramethylrhodamine ethyl ester (TMRE) staining and specific reagent kits, respectively. Lastly, immunofluorescence staining and co-immunoprecipitation were employed to investigate the co-localization and interactions between TXNIP and thioredoxin (TRX)/NOD-like receptor family pyrin domain-containing 3 (NLRP3) proteins.</p><p><strong>Results: </strong>Cisplatin exacerbated apoptosis, suppressed cell proliferation, and upregulated NLRP3, pro-Caspase-1, cleaved Caspase-1, Gasdermin D (GSDMD), GSDMD-N, and TXNIP expression. Concurrently, cisplatin resulted in increased pyroptotic cells and increased interleukin-6 (IL-6), IL-18, IL-1β, and tumor necrosis factor-α (TNF-α) levels. These effects were mitigated by TXNIP knockdown. Furthermore, cisplatin led to elevated cellular ROS and mitochondrial ROS (mtROS), decreased MMP, and inhibited MPTP opening. Cisplatin reduced the colocalization and interaction between TRX and TXNIP while enhancing those between TXNIP and NLRP3. These changes were attenuated by MitoQ. Resveratrol displayed effects similar to those of TXNIP knockdown and MitoQ treatment.</p><p><strong>Conclusion: </strong>Resveratrol alleviated the toxic effects of cisplatin on cochlear hair cells by inhibiting cell pyroptosis process mediated by the mtROS/TXNIP/NLRP3 pathway.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143022475","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
Investigation of the Mechanism of Pachyman against Gout Arthritis with Network Pharmacology Analysis and Verification In Vivo.
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-01-22 DOI: 10.2174/0113862073330896241211155436
Qing-Xin Kong, Wei-Ping Xu, Cheng Fan, Bi-Lin Liu, Li-Ping Reng, Qiao Ruan
{"title":"Investigation of the Mechanism of Pachyman against Gout Arthritis with Network Pharmacology Analysis and Verification In Vivo.","authors":"Qing-Xin Kong, Wei-Ping Xu, Cheng Fan, Bi-Lin Liu, Li-Ping Reng, Qiao Ruan","doi":"10.2174/0113862073330896241211155436","DOIUrl":"https://doi.org/10.2174/0113862073330896241211155436","url":null,"abstract":"<p><strong>Purpose: </strong>Pachyman, derived from Poria cocos, has been used to treat gouty arthritis (GA) for thousands of years, although its precise role and mechanisms remain unclear. Herein, we investigate the therapeutic effects of pachyman on GA and explore their underlying mechanisms.</p><p><strong>Methods: </strong>Network pharmacology and experimental methods were employed to investigate the therapeutic mechanisms of pachyman against GA. The protein-protein interaction network of shared targets between pachyman and gout was constructed. Furthermore, we elucidated the functions and mechanisms of pachyman against GA. Subsequently, we validated the predicted mechanisms from an experiment on rats.</p><p><strong>Results: </strong>The treatment of GA with pachyman primarily related to tumor necrosis factor (TNF), matrix metalloproteinases (MMP), and relaxation factor signaling pathways. In the experimental validation, pachyman were found to regulate the expression of IL-1β, TNF-α, TGF-β, superoxide dismutase, and glutathione peroxidase of hyperuricemic rats.</p><p><strong>Conclusion: </strong>These collective findings suggest that pachyman holds promise as an alternative treatment for GA.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143022348","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
Cellulose and Cellulose Nanomaterials: Recent Research and Applications in Medical Field.
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-01-22 DOI: 10.2174/0113862073334330241105095235
Murtaza Ahmad Khanday, Danish Ahmad Shergujri, Aisha Noor, Shahid Fayaz, Syed Naiem Raza, Reyaz Hassan Mir, Nisar Ahmad Khan
{"title":"Cellulose and Cellulose Nanomaterials: Recent Research and Applications in Medical Field.","authors":"Murtaza Ahmad Khanday, Danish Ahmad Shergujri, Aisha Noor, Shahid Fayaz, Syed Naiem Raza, Reyaz Hassan Mir, Nisar Ahmad Khan","doi":"10.2174/0113862073334330241105095235","DOIUrl":"https://doi.org/10.2174/0113862073334330241105095235","url":null,"abstract":"<p><p>Cellulose, the most prevalent biopolymer in the world, is comprehensively reviewed. Cellulose occurs in fibrillar patterns with alternating crystalline and amorphous regions. The non-toxic and -friendly nature of cellulose has made it beneficial in many fields, such as pharmaceuticals, biomedical, nanotechnology, etc. Numerous sources, including the plant cell wall and wood, some types of bacteria, algae, and tunicates can provide cellulose. This polysaccharide is composed of a straight chain of d-glucose units attached by β (1 → 4) that extend in number from several hundred to thousands. This review details the recent progress in the synthesis of cellulose nanofibers or nanofibrillated cellulose, cellulose nanocrystals, commonly referred to as nanocellulose, and bacterial cellulose. The methodologies and procedures for evaluating the morphology, purity, crystallinity, mechanical, rheological, and other characteristics of cellulose micro/nanomaterials are covered in this review. The current study also discusses several ways to functionalize CNFs, CNCs, and BC. Finally, a guide to the synthesis of cellulose nanocomposites is provided, along with possible uses in the biomedical field, such as wound healing, bone tissue engineering, and artificial blood vessel production. Additionally, applications related to the pharmaceutical industry are also highlighted.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143022347","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
Ir-Catalyzed Intermolecular Arylthiocyanation of Alkenes.
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-01-22 DOI: 10.2174/0113862073347918241209052708
Jie Xu, Jing Leng, Hao Huang, Yanan Li, Ying Qi Chen
{"title":"Ir-Catalyzed Intermolecular Arylthiocyanation of Alkenes.","authors":"Jie Xu, Jing Leng, Hao Huang, Yanan Li, Ying Qi Chen","doi":"10.2174/0113862073347918241209052708","DOIUrl":"https://doi.org/10.2174/0113862073347918241209052708","url":null,"abstract":"<p><strong>Aims: </strong>Organic thiocyanates are important pharmaceutical intermediates. This study aimed to develop a selective and efficient approach for synthesizing organic thiocyanates.</p><p><strong>Methods: </strong>Under mild reaction conditions, an array of alkenes, KSCN, and diaryliodonium salts are considered good substrates, providing various aryl-substituted alkylthiocyanates with modest to excellent yield. Radical trapping and nucleophilic trapping experiments were carried out to explore the mechanistic pathways. The experiments indicated the involvement of free-radical and carbenium ion intermediate processes. Diaryliodonium salts were used as the radical arylating reagent, and KSCN was the electrophilic cyanating reagent. Under irradiation, the excited photocatalyst reduced aryldiazonium salt to aryl radical. Then, the radical was added to olefin to generate a new radical. Finally, the generated radical was further oxidized and arrested by SCN anion.</p><p><strong>Conclusion: </strong>This coupling reaction provides a straightforward and practical route to construct various aryl-substituted alkylthiocyanates.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143022416","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
Mechanisms of the Compound of Magnoliae Flos and Xanthii Fructus Essential Oils for the Treatment of Allergic Rhinitis based on the Integration of Network Pharmacology, Molecular Docking, and Animal Experiment.
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-01-22 DOI: 10.2174/0113862073333657241216040227
Tao Lu, Yuqin Yang, Zhenlin Yang, Ziyi Liu, Miao Li, Ziman Lu, Ting Gong, Jincheng Zhang
{"title":"Mechanisms of the Compound of Magnoliae Flos and Xanthii Fructus Essential Oils for the Treatment of Allergic Rhinitis based on the Integration of Network Pharmacology, Molecular Docking, and Animal Experiment.","authors":"Tao Lu, Yuqin Yang, Zhenlin Yang, Ziyi Liu, Miao Li, Ziman Lu, Ting Gong, Jincheng Zhang","doi":"10.2174/0113862073333657241216040227","DOIUrl":"https://doi.org/10.2174/0113862073333657241216040227","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Aim and objective: &lt;/strong&gt;Magnoliae Flos (Chinese name: Xin-Yi) and Xanthii Fructus (Chinese name: Cang-Er-Zi) are Chinese herbal medicines and have been used to treat allergic rhinitis (AR). However, the therapeutic effect, active ingredients, and probable processes of a compound of Magnoliae Flos and Xanthii Fructus in the form of essential oils (CMFXFEO) in treating AR have not been reported. This study aims to determine the efficacy of the CMFXFEO on ovalbumin (OVA)-induced AR in a rat model and to use network pharmacology and molecular docking to reveal the hub genes, biological functions, and signaling pathways of CMFXFEO against AR.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;Animal experiments were applied to validate the role of CMFXFEO in the treatment of AR. 20 rats were randomly divided into four groups: control group (CON, n=5), positive control group (AR, n=5), CMFXFEO-treated group (AR+CMFXFEO, n=5), and budesonide-treated group (AR+Budesonide, n=5). Rats were stimulated with OVA to induce AR. Symptom scores assessment and histo-pathomorphological evaluation was performed. The serum level of OVA-specific immunoglobulin (Ig) E was measured. Gas Chromatograph-Mass Spectrometer analysis (GC-MS) was used to identify the monomer chemical composition of CMFXFEO. The target genes of CMFXFEO were obtained by using PubChem and SwissTargetPrediction databases. The target genes of AR were screened using GeneCards, DisGeNET, and OMIM databases. The target genes were intersected using the venny2.1 website to obtain the potential therapeutic targets of CMFXFEO for treating AR and to construct the PPI network. Gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses were used to reveal associated signaling pathways. The Sybyl tool was used to dock the CMFXFEO with key therapeutic targets molecularly.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;Intranasal CMFXFEO administration significantly suppressed the allergic symptoms, reduced the inflammatory cell infiltration, and the serum level of OVA-specific immunoglobulin (Ig) E. The main components of CMFXFEO obtained through the GC-MS analysis, listed as γ-terpinene (9.4908%), limonene (7.2693%), menthol (7.1821%), β-pinene (7.1190%), β-caryophyllene (7.0396%), eucalyptol (6.1367%), linalool(5.9686%), eugenol (5.0776%). A total of 398 CMFXFEO targets and 488 AR-related targets were screened, of which 42 were common targets. The GO and KEGG pathway analyses unveiled that CMFXFEO were strongly associated with several signaling pathways, including the AGE-RAGE signaling pathway, TNF signaling pathway, and Chemokine signaling pathway. PPI network construction screened six hub genes as therapeutic targets, including STAT3, IL1B, TLR4, PTGS2, ICAM1, and VCAM1. The molecular docking verification indicated that CMFXFEO have good binding activity with therapeutic targets, and β-Pinene's docking ability with TLR4 is particularly prominent.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;The anti-infl","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143022474","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
Mechanism of HJ11 Decoction in the Treatment of Atherosclerosis Based on Network Pharmacology and Experimental Validation.
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-01-21 DOI: 10.2174/0113862073356770241218065012
Fei Lu, Jiaxi Zou, Weiming Xu, Fangyuan Zhang, Wenyi Nie, Yue Zhao, Lijie Jiang, Lizhe Liang, Jingqing Hu
{"title":"Mechanism of HJ11 Decoction in the Treatment of Atherosclerosis Based on Network Pharmacology and Experimental Validation.","authors":"Fei Lu, Jiaxi Zou, Weiming Xu, Fangyuan Zhang, Wenyi Nie, Yue Zhao, Lijie Jiang, Lizhe Liang, Jingqing Hu","doi":"10.2174/0113862073356770241218065012","DOIUrl":"https://doi.org/10.2174/0113862073356770241218065012","url":null,"abstract":"<p><strong>Background: </strong>HJ11 (HJ11 decoction), which is based on the traditional prescription Si-Miao-Yong-An decoction, has exerted a remarkable effect on atherosclerosis (AS). Nevertheless, the main components and underlying mechanisms of HJ11 for treating AS remain unclear.</p><p><strong>Aim of the study: </strong>This study was designed to elucidate the mechanism of HJ11 in the treatment of AS through network pharmacology and in vivo experimental validation.</p><p><strong>Methods: </strong>Network pharmacology was employed to explore the primary bioactive components and targets of HJ11. AS-related genes were obtained from the GeneCards and DisGeNET databases and screened for intersections with HJ11. A herb-compound-target interaction network was constructed by Cytoscape 3.9.1, and molecular docking analyses were constructed on key targets. By using a mouse model, the mechanism of action of HJ11 was further confirmed.</p><p><strong>Results: </strong>A total of 231 active components of HJ11, 1681 AS-related genes, and 156 common targets were identified. Through the establishment of numerous networks, it was discovered that the main association of the mechanism of HJ11 in AS therapy pertained to anti-inflammation. Important substances included quercetin, kaempferol, and luteolin, while TNF-α, AKT1, IL-6, and VEGFA were the main targets. Molecular docking demonstrated that there were favorable binding interactions between active drugs (quercetin, kaempferol, and luteolin) and targets (TNF-α, AKT1, IL-6, and VEGFA). In the in vivo study, HJ11 reduced the expression of TNF-α, AKT1, IL-6, and VEGFA at both the mRNA and protein levels, inhibited atherosclerotic lesions in AS mouse models, and retarded the development of retroarterioid sclerosis.</p><p><strong>Conclusions: </strong>HJ11 can inhibit inflammation and the progression of AS, and the mechanism might involve downregulating the expression of TNF-α, AKT1, IL-6, and VEGFA.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-01-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143022418","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
FOLR1 Regulates the Malignant Progression of Glioblastoma through the SRC/ERK1/2 Axis. FOLR1通过SRC/ERK1/2轴调控胶质母细胞瘤的恶性进展。
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-01-20 DOI: 10.2174/0113862073335351241226070841
Xueshan Jia, Weihang Liang, Junya Yang, Xuejiao Chen, Yi Bin, Zhikun Cao, Qingfeng Tian
{"title":"FOLR1 Regulates the Malignant Progression of Glioblastoma through the SRC/ERK1/2 Axis.","authors":"Xueshan Jia, Weihang Liang, Junya Yang, Xuejiao Chen, Yi Bin, Zhikun Cao, Qingfeng Tian","doi":"10.2174/0113862073335351241226070841","DOIUrl":"https://doi.org/10.2174/0113862073335351241226070841","url":null,"abstract":"<p><strong>Background: </strong>GBM is an aggressive brain tumor with limited treatment options. Prior research has indicated FOLR1 as a pivotal gene involved in cancer pathogenesis.</p><p><strong>Aim: </strong>This study aimed to explore the involvement of folate receptor alpha (FOLR1) in glioblastoma (GBM) and evaluate its potential as a therapeutic target.</p><p><strong>Objective: </strong>This study investigated the expression pattern of FOLR1 in GBM, its impact on patient prognosis, and its role in GBM cell growth and the SRC/ERK1/2 signaling axis.</p><p><strong>Methods: </strong>Initially, we conducted an expression analysis of FOLR1 based on public databases and examined its expression pattern in GBM and its impact on patient prognosis. Subsequently, cell experiments were carried out to evaluate the regulation of GBM cells by differential FOLR1 expression. We then downloaded 100 FOLR1 co-expressed genes from the Linkedomics data repository and performed an enrichment analysis. Finally, the role of FOLR1 and SRC/ERK1/2 axis in GBM was analyzed again by cell experiments.</p><p><strong>Results: </strong>FOLR1 was found to be substantially expressed in GBM patients and was linked to a poor prognosis. Cell experiments showed that overexpression of FOLR1 promoted GBM cell growth, while low expression of FOLR1 inhibited cell growth. Additionally, genes related to FOLR1 were enriched in the lysosome, toxoplasmosis, and other pathways. This study further indicated that FOLR1 facilitates the activation of the SRC/ERK1/2 signaling pathway in GBM cells, and the attenuation of these pathways can effectively impede the malignancy-promoting effects triggered by FOLR1 in GBM cells.</p><p><strong>Conclusions: </strong>We revealed that FOLR1 orchestrates the malignant advancement of GBM by stimulating the SRC/ERK1/2 signaling axis, underscoring its pivotal role in the pathogenesis of GBM.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143001389","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
Herbal Mucoadhesive Gels for Canker Sores: Analysis of Physicochemical Properties, Efficacy, and Safety. 用于口腔溃疡的草药黏附凝胶:理化性质、疗效和安全性分析。
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-01-20 DOI: 10.2174/0113862073341539241223195855
Evren Algın Yapar, Ebrar İnal, Bilge Ahsen Kara, Tuana Seray Yıldırım, Fatıma Nur Yılmaz, Cemre Özkanca, Meryem Sedef Erdal, Sibel Döşler, Murat Kartal
{"title":"Herbal Mucoadhesive Gels for Canker Sores: Analysis of Physicochemical Properties, Efficacy, and Safety.","authors":"Evren Algın Yapar, Ebrar İnal, Bilge Ahsen Kara, Tuana Seray Yıldırım, Fatıma Nur Yılmaz, Cemre Özkanca, Meryem Sedef Erdal, Sibel Döşler, Murat Kartal","doi":"10.2174/0113862073341539241223195855","DOIUrl":"https://doi.org/10.2174/0113862073341539241223195855","url":null,"abstract":"<p><strong>Aim: </strong>The goal of this research was to formulate mucoadhesive gels using hydroglyceric extracts of Cistus creticus L. and Inula viscosa (L.) Aiton, either separately or in combination, utilizes carboxymethyl cellulose and detects their physicochemical characteristics and safety for oromucosal cells and antimicrobial (antibacterial, antifungal, and antiviral) efficacy to assess their performance.</p><p><strong>Methods: </strong>Using LC-HRMS, the extracts of C. creticus and I. viscosa were examined. Evaluations were conducted on the formulations' viscosity, cytotoxicity-cell proliferation controls, texture, antibacterial activity, pH, and organoleptic properties. The minimal inhibitory concentrations and microbroth dilution tests were used to assess the effectiveness of the formulations.</p><p><strong>Results: </strong>The pH, organoleptic, and physical characteristics of each formulation have been determined to be appropriate. The research results demonstrated that I. viscosa contributed antiviral efficacy to the formulations linked to dose-dependent activities against all examined mouth pathogens, whereas C. creticus provided antibacterial and antifungal efficacy. The formulation containing C. creticus extract alone was the most cytotoxic, whereas the formulation including I. viscosa extract alone was the least cytotoxic against gingival fibroblast cells, according to the findings of tests on cell proliferation and cytotoxicity.</p><p><strong>Conclusion: </strong>The formulation contained a 32% 1:1 mixture of I. viscosa and C. creticus hydroglyceric extracts was detected as safe with acceptable cytotoxicity along with antibacterial and antiviral effectiveness, were encouraging for future investigations.</p>","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143001409","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 Mechanism of Acupuncture in Improving Ovarian Function in Rats with Poor Ovarian Response Using High-Throughput Sequencing. 利用高通量测序技术探索针刺改善卵巢反应差大鼠卵巢功能的机制。
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-01-20 DOI: 10.2174/0113862073365843241223093834
Yunzhu Liu, Wanqiu Yang, Rongli Yuan, Zimeng Li, Tianyu Wang, Bin Yang, Zhi Li, Mengjing Wang, Jie Wu
{"title":"Exploring the Mechanism of Acupuncture in Improving Ovarian Function in Rats with Poor Ovarian Response Using High-Throughput Sequencing.","authors":"Yunzhu Liu, Wanqiu Yang, Rongli Yuan, Zimeng Li, Tianyu Wang, Bin Yang, Zhi Li, Mengjing Wang, Jie Wu","doi":"10.2174/0113862073365843241223093834","DOIUrl":"https://doi.org/10.2174/0113862073365843241223093834","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Objective: &lt;/strong&gt;This study aimed to investigate the possible mechanism through which acupuncture protects ovaries with Poor Ovarian Response (POR) in rats based on microRNA (miRNA).&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;Thirty-six SPF SD female non-pregnant rats aged 8 weeks were randomly divided into the blank group, model group, and acupuncture group, with 12 rats in each group. According to the group, the rats were given gavage of Tripterygium wilfordii polyglycosides suspension for 14 days to establish the model of POR, and then the rats were treated with acupuncture for 2 weeks, once a day, for 20 minutes. Afterward, their hormone levels were measured, and HE staining was performed on the ovaries after the intervention. Three rats from each group were randomly selected for ovarian tissue miRNA sequencing, and differential miRNAs were subjected to Gene Ontology (GO) enrichment analysis, Kyoto Encyclopedia of Genes and Genomes (KEGG) signaling pathway analysis, and Quantitative Polymerase Chain Reaction (QPCR) verification. By using TargetScan to predict the target genes of differential miRNAs, we validated the results with a dual luciferase reporter gene assay.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;Compared with the blank group, the estrus cycle of the model group was significantly prolonged (P&lt;0.01). Anti-Müllerian Hormone (AMH) (P&lt;0.01) and Estrogen (E2) were significantly decreased (P&lt;0.05). Follicle-Stimulating Hormone (FSH)(P&lt;0.05) and Luteinizing Hormone (LH) increased sharply (P&lt;0.01). Compared with the model group, the estrus cycle was significantly shortened in the acupuncture group (P&lt;0.01). AMH and E2 were markedly raised (P&lt;0.05). FSH (P&lt;0.05) and LH (P&lt;0.01) were significantly declined. miRNA sequencing showed that there were 23 miRNAs significantly different between the model group and the blank group (P&lt;0.05), and 30 miRNAs significantly different between the acupuncture group and the model group (P&lt;0.05). GO demonstrated that the network was mainly involved in cellular components, cells, cellular metabolic processes, binding, and single biological processes; KEGG signaling pathway enrichment showed that it was mainly related to MAPK, adhesion junction, calcium signaling pathways, etc. Q-PCR results showed that after modeling, the expression rose, and after acupuncture, the expression of the following miRNA decreased: miR-154-5p (P&lt;0.01), miR-300-5p (P &lt; 0.05), miR-376c-5p (P&lt;0.05). The dual luciferase reporter assay showed that the relative luciferase activity of the miR-300-5p mimics+MAP3K1-WT group was significantly lower than that of the NC+MAP3K1-WT group (P&lt;0.01). HE results demonstrated that the number of primordial follicles and primary follicles in the model group was significantly lower than that in the blank group (P&lt;0.05). Moreover, the morphology was poorer, and the granulosa cell layer was thinner. Compared with the model group, the number of primary follicles in the acupuncture group increased (P&lt;0.05); the mo","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143001383","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
Hepatoprotective Potential of Indian Medicinal Plants. 印度药用植物的保肝潜能。
IF 1.6 4区 医学
Combinatorial chemistry & high throughput screening Pub Date : 2025-01-17 DOI: 10.2174/0113862073346295250107070310
Arti Kumari, Nisha Chandila, Rubina Bhutani, Inderjeet Yadav
{"title":"Hepatoprotective Potential of Indian Medicinal Plants.","authors":"Arti Kumari, Nisha Chandila, Rubina Bhutani, Inderjeet Yadav","doi":"10.2174/0113862073346295250107070310","DOIUrl":"https://doi.org/10.2174/0113862073346295250107070310","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Introduction: &lt;/strong&gt;The liver is essential for both the body's removal of waste materials and the metabolism of nutrients, it is critical for sustaining general health. However, a number of factors, including viral infections, immune system malfunctions, cancer, alcohol intake, and drug toxicity, are contributing to the rising prevalence of liver problems. Alternative approaches to liver disease treatment are being investigated due to the potential limitations of conventional medical treatments. In this regard, the possible hepatoprotective effects of medicinal plants containing bioactive chemicals high in antioxidants have drawn attention.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Method: &lt;/strong&gt;This review's objective is to provide an overview of the Indian medicinal plants' therapeutic value. A variety of databases, including PubMed, Web of Science, Scopus, Academic Journals Embase, Google Scholar, and Science Direct, were searched for relevant literature using keywords such as \"hepatoprotective,\" \"hepatotoxins,\" \"medicinal plants,\" and \"phytoconstituents\".&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Result: &lt;/strong&gt;This article focuses on plant-based medicines that guard against oxidative stress and pollutants, highlighting the potential of herbal remedies as alternatives to traditional liver disease treatments. Reviewing the hepatoprotective qualities of a number of medicinal plants, such as Ginkgo biloba, Woodfordia fruticosa, Thymus quinquecostatus, and Terminalia arjuna, offer more details about their effectiveness. Terminalia arjuna: Preclinical research demonstrates a 30-40% decrease in liver enzyme levels and a 50-60% rise in antioxidant indicators; clinical trials reveal a 25-30% decrease in liver enzyme levels. Thymus quinquecostatus: Research on animals shows a 35-45% decrease in liver enzymes, and preliminary clinical findings indicate a 20-30% improvement in liver function. Woodfordia fruticosa: Although clinical evidence is not as strong as preclinical trials, early investigations indicate a 25-35% improvement in liver enzymes and a 50-60% reduction in liver damage indicators. Ginkgo biloba: Shown enhanced liver function and a 40-50% decrease in liver enzymes; clinical trials have also shown improvements in liver enzymes and a 20-30% decrease in fibrosis markers in NAFLD patients.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;In conclusion, the increased prevalence of liver diseases emphasizes the necessity for nonconventional therapeutic options. Medicinal plants, as opposed to conventional medicines, have promising hepatoprotective effects with fewer adverse effects since they include bioactive substances such as sterols, anthocyanins, terpenoids, saponin glycosides, and polyphenolics. Clinical trials have shown the potential of some plant medications to support liver health. For example, clinical trials have demonstrated the effectiveness of Picrorhiza kurroa in treating liver disorders including viral hepatitis, with a notable decrease in liver enzyme levels. Xanthones found i","PeriodicalId":10491,"journal":{"name":"Combinatorial chemistry & high throughput screening","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143001405","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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