Anti-inflammatory & anti-allergy agents in medicinal chemistry最新文献

筛选
英文 中文
Metabolic Evaluation of a Novel Hydroxyfuranone Compound: Adiposity Reduction in Obese Mice by Increasing SIRT1 Gene Expression.
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2025-02-27 DOI: 10.2174/0118715230349902250203060705
Daniel Silva Moraes, Suely Rodrigues Pereira, Tulio Duque Esteves, Ana Carolina Americo Correia, Victor Hugo Dantas Guimarães, Ulisses Alves Pereira, Eder do Couto Tavares, Alfredo Maurício Batista de Paula, Carla Jeane Aguiar, Lucyana Conceição Farias, André Luiz Sena Guimarães, Sérgio Henrique Sousa Santos
{"title":"Metabolic Evaluation of a Novel Hydroxyfuranone Compound: Adiposity Reduction in Obese Mice by Increasing SIRT1 Gene Expression.","authors":"Daniel Silva Moraes, Suely Rodrigues Pereira, Tulio Duque Esteves, Ana Carolina Americo Correia, Victor Hugo Dantas Guimarães, Ulisses Alves Pereira, Eder do Couto Tavares, Alfredo Maurício Batista de Paula, Carla Jeane Aguiar, Lucyana Conceição Farias, André Luiz Sena Guimarães, Sérgio Henrique Sousa Santos","doi":"10.2174/0118715230349902250203060705","DOIUrl":"https://doi.org/10.2174/0118715230349902250203060705","url":null,"abstract":"<p><strong>Background: </strong>Obesity is one of the main health problems worldwide and is associated with type 2 diabetes mellitus. In this context, butenolides and sulfonamides are known for their anti-obesity effects.</p><p><strong>Objective: </strong>The present study aimed to synthesize a novel molecule containing the moieties hydroxybutenolide and sulfonamide [3-chloro-4-(p-chlorophenylsulfonylamino)-5-hy-droxyfuran-2(5H)-one] (FS) and evaluate its metabolic effects in an obese mice model with metabolic syndrome.</p><p><strong>Methods: </strong>4 groups of mice were divided into standard diet (ST), standard diet with added hydroxybutenolide (ST+FS), high-fat diet (HF), and high-fat diet with added hydroxy-butenolide (HF+FS). Over 30 days, FS was administered by gavage at a dose of 70 mg/kg/day. Body weight, food consumption, glycemic tests, total serum cholesterol, high-density lipoprotein cholesterol, triacylglycerol, histological analyses, and gene expression by RT-PCR for the adipose tissue genes SIRT1, SIRT3, SIRT5, and NFKβ, were evaluated.</p><p><strong>Results: </strong>A decrease in body weight was observed after FS administration (ST+FS: -7.81±4.39 and HF+FS: -11.77±9.59), reducing glucose and fasting blood glucose in the treated group. Adipose tissue mass (ST+FS: 0.017 ±0.011; HF+FS: 0.062±0.017), white epididymal adipose tissue volume, triglycerides, as well as the adipocyte area, were lower for the HF+FS group. SIRT1 and SIRT3 expressions were higher in groups that received hydroxybutenolide.</p><p><strong>Conclusion: </strong>Treatment with FS 3-chloro-4-(p-chlorophenylsulfonylamino)-5-hydroxy-furan-2(5H)-one improved metabolic profile and increased the SIRT1 expression.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-02-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143525762","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","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 Evaluation of the Synergistic Anti-inflammatory Activities of the Combined Hydroalcoholic Extracts from Mentha Pulegium L. and Pimpinella Anisum L.
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2025-02-19 DOI: 10.2174/0118715230363843250122051332
Amina Tabet Zatla, Amina Hammoudi, Mohammed El Amine Dib, Joëlle Perard
{"title":"In vitro Evaluation of the Synergistic Anti-inflammatory Activities of the Combined Hydroalcoholic Extracts from Mentha Pulegium L. and Pimpinella Anisum L.","authors":"Amina Tabet Zatla, Amina Hammoudi, Mohammed El Amine Dib, Joëlle Perard","doi":"10.2174/0118715230363843250122051332","DOIUrl":"https://doi.org/10.2174/0118715230363843250122051332","url":null,"abstract":"<p><strong>Background: </strong>Chronic inflammatory diseases are rising, driving the search for effective natural treatments. Mentha pulegium L. and Pimpinella anisum L. (anise) exhibit notable anti-inflammatory properties individually, but their combined effects are less studied. This research evaluates the in vitro synergistic anti-inflammatory activities of their hydroalcoholic extracts. Phytochemical analysis confirmed the presence of flavonoids, tannins, and polyphenols in both extracts. Individually, they demonstrated significant activity (78.5% and 72.3%, respectively, at 10 g/L) compared to Diclofenac (62.3%). Their combination achieved 88.6% inhibition at the same concentration. These findings highlight their potential as natural anti-inflammatory agents.</p><p><strong>Introduction: </strong>The rise in chronic inflammatory diseases has increased interest in natural anti-inflammatory treatments. Mentha pulegium L. and Pimpinella anisum L. are well-known for their anti-inflammatory potential, attributed to their bioactive compounds like flavonoids and polyphenols. While the individual effects of these plants are established, their combined use is underexplored. This study evaluates the in vitro synergistic anti-inflammatory activity of hydroalcoholic extracts from these plants, aiming to offer an effective natural therapeutic alternative.</p><p><strong>Methods: </strong>Hydroalcoholic extracts were prepared by maceration of both plants. Anti-in-flammatory activity was assessed using the protein denaturation method with Diclofenac as a standard.</p><p><strong>Results: </strong>Phytochemical analysis identified flavonoids, alkaloids, tannins, glycosides, and polyphenols in Mentha pulegium, with an absence of saponins. Pimpinella anisum contained flavonoids, tannins, heterosides, and polyphenols. The extracts exhibited strong anti-inflammatory activity individually (78.5% and 72.3%, respectively, at 10 g/L) and even higher inhibition (88.6%) when combined, surpassing Diclofenac (62.3%).</p><p><strong>Conclusion: </strong>The combination of Mentha pulegium and Pimpinella anisum extracts significantly enhanced anti-inflammatory activity compared to individual extracts, under-scoring their potential as natural therapeutic alternatives to conventional treatments.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-02-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143461549","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Leveraging Underutilized Sri Lankan Fruits in the Fight against Autoimmune Disorders. 利用未充分利用的斯里兰卡成果抗击自身免疫性疾病。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2025-01-17 DOI: 10.2174/0118715230353359241211215415
M P Theja Virajini, Mithila Bandara, Prasad Jayasooriya, Kalpa W Samarakoon, Anchala I Kuruppu
{"title":"Leveraging Underutilized Sri Lankan Fruits in the Fight against Autoimmune Disorders.","authors":"M P Theja Virajini, Mithila Bandara, Prasad Jayasooriya, Kalpa W Samarakoon, Anchala I Kuruppu","doi":"10.2174/0118715230353359241211215415","DOIUrl":"https://doi.org/10.2174/0118715230353359241211215415","url":null,"abstract":"<p><p>The potential of underutilized plant species to improve food security, health, eco-nomic output, and the environment has not been fully realized. Sri Lanka an island on the Indian Ocean is home to numerous plant species with significant medicinal potential, in-cluding many underutilized plants that could help meet the growing demand for food, en-ergy, medicines, and industrial resources. Globally, there are over a thousand known and unknown phytochemicals derived from plants. Although these compounds are primarily produced by plants for self-defence, in vitro and in vivo studies have demonstrated their anti-inflammatory properties. Recent research indicates that several phytochemicals can also protect humans from disease by regulating key inflammatory pathways, such as NF-κB, MAPK, JAK/STAT and Nrf-2, which are involved in autoimmune diseases. Thus, these bioactive compounds are vital for managing autoimmune disorders. This review will ex-plore underutilized fruit crops from Sri Lanka that could be used against inflammation, in-cluding autoimmune diseases.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143019592","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Dry-feed Added Quercetin Mitigates Cyclophosphamide-induced Oxidative Stress, Inflammation and Gonadal Fibrosis in Adult Male Rats. 干饲料添加槲皮素可减轻环磷酰胺诱导的成年雄性大鼠氧化应激、炎症和性腺纤维化
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0118715230316410240821105658
Anthony T Olofinnade, Oladotun B Ajifolawe, Olakunle J Onaolapo, Adejoke Y Onaolapo
{"title":"Dry-feed Added Quercetin Mitigates Cyclophosphamide-induced Oxidative Stress, Inflammation and Gonadal Fibrosis in Adult Male Rats.","authors":"Anthony T Olofinnade, Oladotun B Ajifolawe, Olakunle J Onaolapo, Adejoke Y Onaolapo","doi":"10.2174/0118715230316410240821105658","DOIUrl":"10.2174/0118715230316410240821105658","url":null,"abstract":"<p><strong>Background: </strong>Cyclophosphamide (CYP), a widely used cancer chemotherapeutic agent has been linked with male gonadotoxicity, resulting in infertility. The notion that potent antioxidants could be beneficial in mitigating CYP-induced gonadotoxicity necessitated this research. Therefore, we examined the effects of feed-added quercetin on CYP-induced gonadotoxicity in male rats.</p><p><strong>Methods: </strong>Male postpubertal rats were randomly assigned into six groups of 10 rats each. The normal control (fed standard rodent diet) and two groups fed quercetin-supplemented diet at 100 and 200 mg/kg of feed received normal saline intraperitoneally at 2 ml/kg daily. A fourth group which served as the CYP control (fed standard rodent diet) and the last two groups fed quercetin at 100 and 200 mg/kg of feed were administered CYP at 150 mg/kg/day. Rats were administered normal saline or CYP intraperitoneally on days 1 and 2, while standard diet or feed-added quercetin was administered daily for 21 days. On day 22, half of the animals were either sacrificed or paired with age-matched females for fertility assessment. Estimation of testosterone levels, antioxidant, anti-inflammatory markers, and histomorphological examination of the testis and epididymis was also assessed.</p><p><strong>Results: </strong>The administration of CYP was associated with weight loss, decreased food intake, decreased antioxidant capacity, increased gonadosomatic index, increased lipid peroxidation, sub-fertility, and histological evidence of gonadal injury. However, administration of quercetin reversed CYP-induced changes.</p><p><strong>Conclusion: </strong>The result of this study suggests that dietary quercetin supplementation has the ability to mitigate CYP induced gonadotoxicity and mitigate subfertility in male rats. However, further studies are required to assess its possible use in humans.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"43-56"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142335924","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Topical Administration of Nanostructured Lipid Carriers as a Viable Approach to Reduce Inflammation: A Review. 纳米结构脂质载体的局部给药是减少炎症的可行方法:综述。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0118715230311633240708075738
Prakash Rajak, Arka Karmakar, Santa Sarma, Biman Bhuyan
{"title":"Topical Administration of Nanostructured Lipid Carriers as a Viable Approach to Reduce Inflammation: A Review.","authors":"Prakash Rajak, Arka Karmakar, Santa Sarma, Biman Bhuyan","doi":"10.2174/0118715230311633240708075738","DOIUrl":"10.2174/0118715230311633240708075738","url":null,"abstract":"<p><p>This review seeks to assess the potential of nanomaterials, specifically Nano-structured Lipid Carriers (NLCs), in mitigating challenges associated with inflammation-related disorders, with a particular emphasis on chronic ailments like arthritis. A comprehensive literature review spanning Web of Science, PubMed, and other scholarly repositories from 2000 to 2023 is conducted. Articles are selected based on their focus on NLCs and inflammation management, utilizing keywords, such as \"nanomaterials,\" \"targeted drug delivery,\" and \"arthritis.\" Exclusion criteria involve non-English studies or those lacking adequate detail on NLCs. Synthesized data provide an overview of the advantages, challenges, and prospects of NLCs in addressing chronic inflammatory disorders. This review also examines the therapeutic applications of nanotechnology, including targeted drug delivery and tissue engineering, particularly focusing on the intricate biological responses in chronic inflammation, often involving Non-steroidal Anti-inflammatory Drugs (NSAIDs). Moreover, the exploration extends to topical delivery methods to enhance control over medication concentration, with a review of lipid nanoparticles, such as liposomes and solid-lipid nanoparticles, highlighting their potential in augmenting drug permeation while addressing challenges like inadequate drug loading. NLCs have emerged as promising candidates for overcoming drug delivery challenges, particularly in arthritis treatment, with a focus on their advantages across diverse lipid compositions. The review underscores significant strides in inflammation management through NLC utilization, offering insights into future research directions. Moreover, it contributes to ongoing advancements in nanomedicine, emphasizing the pivotal role of NLCs in developing innovative therapeutic approaches for inflammation-related disorders, particularly arthritis. NLCs represent a promising avenue for effective interventions, signaling progress in nanotechnology-enabled therapeutics.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"26-42"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141857545","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Naringenin: A Promising Immunomodulator for Anti-inflammatory, Neuroprotective and Anti-cancer Applications. "柚皮素:一种有望用于抗炎、神经保护和抗癌的免疫调节剂"。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0118715230320007240708074939
Sarita Solanki, Himangi Vig, Nidhi Khatri, Bhanu Pratap Singh, Mohammad Shahid Khan, Manish Devgun, Pranay Wal, Ankita Wal
{"title":"Naringenin: A Promising Immunomodulator for Anti-inflammatory, Neuroprotective and Anti-cancer Applications.","authors":"Sarita Solanki, Himangi Vig, Nidhi Khatri, Bhanu Pratap Singh, Mohammad Shahid Khan, Manish Devgun, Pranay Wal, Ankita Wal","doi":"10.2174/0118715230320007240708074939","DOIUrl":"10.2174/0118715230320007240708074939","url":null,"abstract":"<p><strong>Background: </strong>Inflammatory, immune, and neurodegenerative diseases constitute a category of persistent and debilitating conditions affecting millions worldwide, with intertwined pathophysiological pathways. Recent research has spotlighted naturally occurring compounds like naringenin for potential therapeutic applications across multiple ailments.</p><p><strong>Objectives: </strong>This review offers an encompassing exploration of naringenin's anti-inflammatory, immune-protective, and neuroprotective mechanisms, elucidating its pharmacological targets, signal transduction pathways, safety profile, and insights from clinical investigations.</p><p><strong>Methods: </strong>Data for this review were amassed through the scrutiny of various published studies <i>via</i> search engines such as PubMed and Google Scholar. Content from reputable publishers including Bentham Science, Taylor and Francis, Nature, PLOS ONE, among others, was referenced.</p><p><strong>Results: </strong>Naringenin exhibits substantial anti-inflammatory effects by restraining the NF-κB signaling pathway. It activates Nrf2, renowned for its anti-inflammatory properties, inducing the release of hemeoxynase-1 by macrophages. Furthermore, naringenin treatment downregulates the expression of Th1 cytokines and inflammatory mediators. It also impedes xanthine oxidase, counteracts reactive oxygen species (ROS), scavenges superoxide radicals, mitigates the accessibility of oxygen-induced K+ erythrocytes, and reduces lipid peroxidation. Naringenin's antioxidant prowess holds promise for addressing neurological conditions.</p><p><strong>Conclusion: </strong>Extensive research has been undertaken to establish the anti-inflammatory, immunomodulatory, and neuroprotective attributes of naringenin across various medical domains, lending credence to its pharmacological utility. The principal obstacle to naringenin's adoption as a therapeutic agent remains the dearth of in vivo data. Efforts should focus on rendering naringenin delivery patient-friendly, economically viable, and technologically advanced.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"1-25"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141794486","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Molecular Docking, Pharmacophore Modeling and ADMET Prediction of Novel Heterocyclic Leads as Glucokinase Activators. 作为葡萄糖激酶激活剂的新型杂环先导化合物的分子对接、药理模型和 ADMET 预测。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0118715230325278240821053346
Anuradha Mehra, Amit Mittal, Shivangi Singh
{"title":"Molecular Docking, Pharmacophore Modeling and ADMET Prediction of Novel Heterocyclic Leads as Glucokinase Activators.","authors":"Anuradha Mehra, Amit Mittal, Shivangi Singh","doi":"10.2174/0118715230325278240821053346","DOIUrl":"10.2174/0118715230325278240821053346","url":null,"abstract":"<p><strong>Background: </strong>A pivotal impetus has driven the development of numerous small molecules aiming to improve therapeutic strategies for type 2 diabetes. Glucokinase (GK) activation has been offered a new realm of therapeutic antidiabetic activity with novel heterocyclic derivatives. In the context of antidiabetic drug design, GK is an interesting and newly validated target. A key enzyme needed for blood glucose homeostasis is Glucokinase, which is dysfunctional in individuals with type 2 diabetes. Heterocyclic derivatives are utilized in this innovative approach to activate GK enzymes as medicinal agents that will significantly improve type 2 diabetes management.</p><p><strong>Objectives: </strong>To address type 2 diabetes, as well as minimize unwanted side effects, this research endeavor aimed to develop activators of glucokinase.</p><p><strong>Methods: </strong>A rigorous scrutiny was conducted of the Maybridge online repository, which houses a formidable collection of 53,000 lead compounds. A collection of 125 compounds that contain the thiazolidinedione core was selected from this extensive collection. The structures were generated using ChemDraw 2D, stabilized conformation with ChemBioDraw Ultra, and docked using Auto Dock Vina 1.5.6 in this methodology. In addition, log P was predicted online using the Swiss ADME algorithm. The PKCSM software was used to predict the toxicity of the leading compounds.</p><p><strong>Results: </strong>The highest binding affinity was found for AS72 and AS108 to GK receptors. GI absorption and excretion of these compounds were efficient due to Lipinski's Rule of Five compliance. When compared with the standard drugs Dorzagliatin (GKA) and MRK (co-crystallized ligand), these substances demonstrated a notable lack of AMES toxicity, skin sensitization, and hepatotoxicity.</p><p><strong>Conclusion: </strong>In recent studies, lead molecules that possess enhanced pharmacokinetic profiles, increased binding affinity, and lower toxicity were developed to act as glucokinase activators.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"57-74"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142335936","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Formulation, Characterization, and Cytotoxic Effect of Indomethacin-Loaded Nanoparticles. 吲哚美辛纳米颗粒的制备、表征和细胞毒性作用。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2024-12-27 DOI: 10.2174/0118715230348349241126053733
Kaan Yalçınkaya, Behiye Şenel, Evrim Akyıl
{"title":"Formulation, Characterization, and Cytotoxic Effect of Indomethacin-Loaded Nanoparticles.","authors":"Kaan Yalçınkaya, Behiye Şenel, Evrim Akyıl","doi":"10.2174/0118715230348349241126053733","DOIUrl":"https://doi.org/10.2174/0118715230348349241126053733","url":null,"abstract":"<p><strong>Background: </strong>Indomethacin (IND), classified as class 2 in the Biopharmaceutical Classification System (BCS), has emerged as an anti-inflammatory agent with low solubility and high permeability. Widely used in the treatment of various diseases, such as rheumatoid arthritis and ankylosing spondylitis, this drug is well-known for its adverse effects, particularly in the stomach, and a short biological half-life, which is around 1.5-2 hours.</p><p><strong>Objective: </strong>The aim of this study was to overcome the challenges of low solubility, short half-life, and serious side effects occurring with the use of IND-loaded formulations of Solid Lipid Nanoparticles (SLNs) and Polymeric Nanoparticles (PNPs).</p><p><strong>Methods: </strong>For PNPs, emulsification/solvent evoporation method was employed, and for SLNs, the hot homogenizaton method was applied. Eudragit® RLPO (RLPO) and Eudragit® RSPO (RSPO) were used as polymers for PNP and Dynasan®116 (DYN) was used as the solid lipid for SLN. Prepared formulations were characterized for Particle Size (PS), Poly-dispersity Index (PDI), Zeta Potential (ZP), Encapsulation Efficiency (%EE), and drug-ex-recipient compatibility using DSC, FT-IR, and 1H NMR; cumulative drug release rates were assessed using HPLC and in vitro cytotoxicities were examined by the MTT assay.</p><p><strong>Results: </strong>Both PNP and SLN formulations' zeta potential, particle size, and PDI results indicated the formulations to have good stability. Encapsulation efficiency values were obtained as desired. Drug-excipient compatibility was proved using DSC, FT-IR, and 1H NMR. In vitro dissolution results have proven both formulations to have longer release than pure indomethacin. In the MTT analysis of indomethacin application for 24 and 48 hours, a linear correlation was observed between drug concentration and cell viability, and it was determined that the PNP formulation exhibited fewer toxic effects among the formulations. This has proven the PNP nanocarrier as safer for normal cells.</p><p><strong>Conclusion: </strong>IND-loaded PNP and SLN formulations have been successfully prepared in this work and they have achieved drug release in the intestine and prolonged the release duration.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142934173","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Toxicity and anti-inflammatory effects of Eleutherine bulbosa (Miller) Urb, ethanolic extract, in zebrafish (Danio rerio). 绿叶葱乙醇提取物对斑马鱼的毒性和抗炎作用。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2024-12-27 DOI: 10.2174/0118715230352701241130053455
Dionisia P Ferreira, Fabrício H Holanda, Swanny F Borges, Ryan da S Ramos, Victoria Mae T Shinkai, Gisele C De Souza, José Carlos T Carvalho, Raphael S Pimenta, José Luiz M Do Nascimento, Irlon M Ferreira
{"title":"Toxicity and anti-inflammatory effects of Eleutherine bulbosa (Miller) Urb, ethanolic extract, in zebrafish (Danio rerio).","authors":"Dionisia P Ferreira, Fabrício H Holanda, Swanny F Borges, Ryan da S Ramos, Victoria Mae T Shinkai, Gisele C De Souza, José Carlos T Carvalho, Raphael S Pimenta, José Luiz M Do Nascimento, Irlon M Ferreira","doi":"10.2174/0118715230352701241130053455","DOIUrl":"https://doi.org/10.2174/0118715230352701241130053455","url":null,"abstract":"<p><strong>Introduction: </strong>Eleutherine bulbosa (Miller) Urb, popularly known as \"marupa-zinho\", is frequently used in traditional medicine for treating various diseases, including hypertension, ulcers, constipation, and intestinal infection. However, there is little scientific knowledge available regarding the pharmacological effects of this species. Thus in vivo and in silico phytochemical studies are required to establish whether this plant has these effects. Further tests were necessary to evaluate the pharmacological activity of the compounds found in this plant, and demonstrate results related to the anti-inflammatory process, which will serve as the basis for future research in this area.</p><p><strong>Methods: </strong>Therefore, our study aimed to determine the acute toxicity levels of the hexanoic fraction of the ethanolic extract of Eleutherine bulbosa (referred to as ExtHF) using adult zebrafish, with the determination of the LD50, behavioral and histopathological evaluations, as well as the anti-inflammatory potential of ExtHF, at different doses, in abdominal edema induced by carrageenan. The acute toxicity study and histopathological analysis in zebrafish showed that ExtHF has a high toxic potential, with an LD50 of 346.74 mg/kg. However, ExtHF showed an anti-inflammatory effect by inhibiting abdominal edema at all doses tested.</p><p><strong>Results: </strong>The inhibition rate of 66.2% and 62.4%, respectively, was observed with the 2.5 mg/kg dose, respectively, indicating that ExtHF is safe in terms of acute toxicity based on behavioral changes, mortality rate, and histopathological examination. Therefore, ExtHF has an acceptable level of safety for acute toxicity, defined by the analysis of behavioral changes, mortality, and histopathology, showing a significant anti-inflammatory effect in zebrafish at all doses, showing that ExtHF was very efficient in preventing the formation of edema, in addition, it was also revealed that ExtHF has a great effect in reversing the edema which is already installed.</p><p><strong>Conclusion: </strong>Molecular docking studies revealed that the eleutherol molecule isolated from E. bulbosa has a dual inhibition profile against cyclooxygenase-1 and 2.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142934153","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery and Chemical Exploration of Spiro[Benzofuran-3,3'-Pyrroles] Derivatives as Innovative FLT3 Inhibitors for Targeting Acute Myeloid Leukemia. Spiro[苯并呋喃-3,3'-吡咯]衍生物作为新型FLT3抑制剂的发现和化学探索
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2024-12-06 DOI: 10.2174/0118715230343474241009112335
Mohammed M Al-Mahadeen, Areej M Jaber, Jalal A Zahra, Belal O Al-Najjar, Mustafa M El-Abadelah, Monther A Khanfar
{"title":"Discovery and Chemical Exploration of Spiro[Benzofuran-3,3'-Pyrroles] Derivatives as Innovative FLT3 Inhibitors for Targeting Acute Myeloid Leukemia.","authors":"Mohammed M Al-Mahadeen, Areej M Jaber, Jalal A Zahra, Belal O Al-Najjar, Mustafa M El-Abadelah, Monther A Khanfar","doi":"10.2174/0118715230343474241009112335","DOIUrl":"https://doi.org/10.2174/0118715230343474241009112335","url":null,"abstract":"<p><strong>Aims: </strong>This study aimed at the synthesis of several spiro[benzofuran-3,3'-pyrroles] derivatives by a three-component reaction conducted by mixing DMAD, N-bridgehead het-erocycles, and benzofuran-2,3-diones in dichloromethane at room temperature for 24 h. Moreover, in vitro evaluation of their cytotoxicity affinities against FMS-like tyrosine kinase 3 was carried out.</p><p><strong>Objectives: </strong>The objective of this study was to use a one-pot, three-component reaction to synthesize a novel set of spiro[benzofuran-3,3'-pyrroles] derivatives.</p><p><strong>Methods: </strong>A novel set of spiro[benzofuran-3,3'-pyrroles] ((11-13)a-e) was synthesized by a one-pot three-component reaction involving dimethyl acetylenedicarboxylate, N-bridgehead heterocycles and benzofuran-2,3-diones in dichloromethane at room temperature for 24 h. The compounds were analyzed using NMR 1H, 13C, 2D-NMR (COSY, HMQC, HMBC), and HRMS. Docking simulations were conducted to elucidate the anticancer activity of synthe-sized compounds on FLT3 protein, with Gilteritinib as a reference for comparison.</p><p><strong>Results: </strong>This study demonstrated the successful design, synthesis, and biological evaluation of spiro[benzofuran-3,3'-pyrroles] derivatives as FLT3 inhibitors for AML treatment. The synthesized compounds demonstrated promising binding affinities and significant inhibitory activity against FLT3 kinase. The inhibitors (11a, 11b, 11c, 12d, and 12e) exhibited excellent selectivity profiles against FLT3. Particularly, compound 12e showed strong binding affinity and potent inhibitory activity (IC50 = 2.5 μM).</p><p><strong>Conclusion: </strong>Fifteen new synthetic spiro[benzofuran-3,3'-pyrroles] were prepared, character-ized, and evaluated for cytotoxicity affinities against FMS-like tyrosine kinase 3. Compound 12e showed strong binding affinity and potent inhibitory activity (IC50 = 2.5 μM), making it a promising candidate for further development as a therapeutic option for AML treatment. These findings lay the groundwork for further optimization and development of spiro[benzo-furan-3,3'-pyrroles] derivatives as potential therapeutics for AML treatment. Further studies are needed to explore their efficacy and safety profiles in preclinical and clinical settings.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142796772","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
相关产品
×
本文献相关产品
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信