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

{"title":"Exploring Anti-Inflammatory Compounds from Kappaphycus Alvarezii in High Cholesterol-Induced Zebrafish Larvae: Revealing Cardiovascular Potential.","authors":"Rabika Ramalingam, Kaliyamurthi Venkatachalam, Ambika Binesh","doi":"10.2174/0118715230342356250611114954","DOIUrl":"https://doi.org/10.2174/0118715230342356250611114954","url":null,"abstract":"<p><strong>Introduction: </strong>The study investigated the anti-inflammatory properties of Kappaphycus alvarezii by employing zebrafish larvae as a model system.</p><p><strong>Materials and methods: </strong>The seaweed extract was subjected to phytochemical screening, uncovering the presence of alkaloids, terpenoids, proteins, and cardiac glycosides. UV-visible, FTIR, and GC-MS were employed to identify the presence of bioactive compounds. The western blotting method was used to confirm the target proteins.</p><p><strong>Results: </strong>Analysis through GC-MS revealed the presence of specific organic bioactive compounds, including 4-chlorobuten-3-yne, Methane-D, trichloro, and 1-propanol, 2-(1-methylethoxy), each with distinct retention times. In the group induced with a high-cholesterol diet (HCD), the activities of antioxidant enzymes (SOD, CAT, GPx, and GST) were elevated, and K. alvarezii treatment successfully reversed this effect. Additionally, the HCD group exhibited upregulation in the protein expression of MMP-9, MMP-13, MPO, IL-6, TNFα, and NFκB due to inflammation, whereas K. alvarezii therapy reversed the inflammatory process in the treated group. These findings indicate the potential of K. alvarezii to counteract inflammatory responses induced by a high-cholesterol diet through modulation of antioxidant enzyme activities and downregulation of pro-inflammatory markers.</p><p><strong>Conclusion: </strong>Kappaphycus alvarezii shows promise for developing natural sources for antiradicals, food supplements, nutraceuticals, and various functional foods with therapeutic applications.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-06-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144532485","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}

{"title":"Chronic Treatment with Angiotensin-(1-7) Improves Metabolism by Modulating Adipose Tissue and Oxidative Stress in Mice.","authors":"Alanna Fernandes Paraíso, Jaciara Neves Sousa, João Marcus Oliveira Andrade, Eloá Mangabeira Santos, Débora de Farias Lelis, Charles Santos Da Costa, Jones Bernardes Graceli, Bruna Kaicy Barbosa, Lucyana Conceição Farias, Alfredo Mauricio Batista de Paula, André Luiz Sena Guimarães, Daniele Teixeira Alves, Maik Gollasch, Robson Augusto Souza Santos, Sérgio Henrique Sousa Santos","doi":"10.2174/0118715230367867250613134043","DOIUrl":"https://doi.org/10.2174/0118715230367867250613134043","url":null,"abstract":"<p><strong>Background: </strong>Angiotensin-(1-7) is a crucial endocrine modulatory peptide that can enhance conditions like diabetes, obesity, and other features of metabolic syndrome. However, there is a lack of data on its long-term effects.</p><p><strong>Aim: </strong>This study aimed to assess the impact of chronic oral administration of Angiotensin- (1-7) on adipose tissue modulation and metabolic processes in mice.</p><p><strong>Methods: </strong>The Angiotensin-(1-7) peptide oral formulation was encapsulated within the hydroxypropyl-β-cyclodextrin oligosaccharide (HPβCD) matrix. Male Swiss mice were divided into 4 groups: standard diet (ST)+HPßCD; ST+Ang-(1-7); high-fat diet HFD+HPßCD, and HFD+Ang-(1-7). The treatment lasted for 12 months, during which body weight, food intake, glycemic and lipid profiles, visceral adiposity, oxidative stress indicators, histological parameters, quantitative real-time PCR assessments, and comprehensive in silico bioinformatics analyses were conducted.</p><p><strong>Results: </strong>Prolonged treatment with Ang-(1-7) led to improvements in glucose levels, visceral body adiposity, decreased cholesterol and triglyceride levels, and reduced oxidative stress. Bioinformatics analysis revealed that AKT1, an insulin signaling effector (INS), and key inflammatory markers like IL-6 and VEGF may be potential molecular mediators of Angiotensin-(1-7) effects. Non-obese animals treated with Angiotensin-(1-7) showed increased expression levels of AKT1, supporting the findings from the bioinformatics analysis.</p><p><strong>Conclusion: </strong>This study demonstrates that chronic oral use of Ang-(1-7) enhances adipose and metabolic parameters, suggesting its potential as a long-term therapeutic agent for regulating metabolic disorders.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-06-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144510227","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}

{"title":"Novel Mouth Rinse Displaying Analgesic and Anti-inflammatory Properties: An in vitro Study.","authors":"Saravanan Sampoornam Pape Reddy, Delfin Lovelina Francis, Soumi Mondal, Manish Rathi, Neelima Katti, Sukhbir Singh Chopra","doi":"10.2174/0118715230384352250526103643","DOIUrl":"https://doi.org/10.2174/0118715230384352250526103643","url":null,"abstract":"<p><strong>Introduction: </strong>Periodontitis is a chronic inflammatory disease requiring effective anti-inflammatory treatments. Nano-silver and essential oils have shown potential due to their antimicrobial and anti-inflammatory properties. Combining these agents offers a promising therapeutic approach. This study investigated the cy-totoxic and anti-inflammatory properties of a novel essential oil compound contain-ing nanosilver using HaCaT and THP-1 human leukemia monocytic cell lines.</p><p><strong>Materials and methods: </strong>Neutral red uptake (NRU) assay was used to assess cyto-toxicity and ELISA to evaluate the inflammatory cytokines. The test compound was compared to 0.12% chlorhexidine gluconate (CHX). Cytotoxicity was determined in HaCaT and THP-1 cell lines using NRU assay. TNF-α expression was measured us-ing ELISA, and COX-2 inhibition assay was performed.</p><p><strong>Results: </strong>Cytotoxicity of the test compound was nearly absent. TNF-α levels de-creased in positive control (2.81pg/ml) and test samples (1.30 pg/ml) compared to control (22.04pg/ml). COX-2 inhibition assay revealed test compound (0-20%) and positive control (0-100%), with 25 μM celecoxib as a standard. IC50 for HaCaT cells was 0.6334% (positive control) and 0.6051% (test group). IC50 using THP-1 cells was not converged for the test and 424.6% for positive control. IC-50 for COX-2 inhibition was 1.469% in the test and 8.801% in the positive control.</p><p><strong>Discussion: </strong>This study showed the possibility of novel essential oils and nano-sil-ver-containing compounds as a medication material in preventing gingivitis. The cy-totoxicity was negligible, while the level of TNF- α was much decreased, and COX-2 activity assays indicated its efficiency in anti-inflammatory properties. The results encourage the therapeutic potential of the compound for periodontitis, and further studies are required to demonstrate therapeutic efficiency and safety.</p><p><strong>Conclusion: </strong>Results demonstrate the inhibitory effect of the test compound on COX-2 activity. The potential of a novel test compound containing essential oils and nano-silver as a promising anti-inflammatory agent warrants further investigation for its therapeutic applications in periodontitis.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-06-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144287973","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}

{"title":"Inclusive Drug Designing of Novel Indole Derivatives using Rationale, Pharmacophore Mapping and Molecular Docking.","authors":"Anuradha Mehra, Amit Mittal, Rahul Sharma, Rekha Sangwan, Aryan Mehra","doi":"10.2174/0118715230352441250309014403","DOIUrl":"https://doi.org/10.2174/0118715230352441250309014403","url":null,"abstract":"<p><p>Introductions/Background: The presence of insufficient insulin signaling in type 2 diabetes arises due to either insulin resistance or impaired insulin secretion, ultimately lead-ing to elevated blood glucose levels, a condition known as hyperglycemia. Diabetes poses a pervasive worldwide challenge, with its prevalence steadily surging in both developed and developing nations. A promising avenue for improving the management of diabetes type 2 involves the exploration of glucokinase activators as an innovative therapeutic target. Nota-bly, a recent breakthrough in this area has been the market approval granted by the Japanese FDA for the use of the innovative GKA, Dorzagliatin, in the treatment of diabetes type 2.</p><p><strong>Objective: </strong>To augment the management of diabetes type 2 and mitigate the undesirable side effects linked to prolonged use of conventional medications, this research endeavor sought to create innovative glucokinase activators.</p><p><strong>Methods: </strong>The ZINC database yielded a collection of 56 compounds, each showcasing a 40% structural similarity to 1-(phenylsulfonyl)-1H-indole-2-carboxylic acid. These compounds, all featuring the distinctive indole core, were meticulously selected for further investigation. Structural illustrations were crafted using ChemBioDraw Ultra, and 1.5.6 AutoDock Vina was for molecular docking. The Swiss ADME algorithm facilitated online log P predictions, while the software PKCSM was utilized to forecast the toxicity profiles of the leading com-pounds. DFT analysis was done to ensure the stability of compounds by using Gaussian 16 quantum chemistry software and Mulliken charge distributions used to optimize molecular geometries.</p><p><strong>Results: </strong>Among all the compounds, RS33 and RS37 exhibited the highest affinities for GK receptors, with the docking scores of -8.93 and -8.44 kcal/mol, respectively. These com-pounds follow Lipinski's Rule, indicating promising absorption and excretion profiles through the gastrointestinal tract. Compared to standard drugs Dorzagliatin (GKA) and MRK (co-crystallized ligand), both RS33 and RS37 demonstrate no AMES toxicity, skin sensitiza-tion, and hepatotoxicity. RS43 is the most stable compound as it has high ΔE, η, and χ in DFT analysis.</p><p><strong>Conclusion: </strong>The novel-designed lead molecules demonstrate an enhanced pharmacokinetic profile, superior binding affinity, and minimal toxicity, based on computational study. These attributes make them promising candidates for further optimization as glucokinase activators.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144060506","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}

{"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}

{"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}

{"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}

{"title":"A Comprehensive Review on Insect Repellent Agents: Medicinal Plants and Synthetic Compounds.","authors":"Deepak K Yadav, Sunny Rathee, Versha Sharma, Umesh K Patil","doi":"10.2174/0118715230322355240903072704","DOIUrl":"10.2174/0118715230322355240903072704","url":null,"abstract":"<p><p>Plant-based repellents have been used for generations as personal protection against mosquitoes. Ethnobotanical studies provide valuable knowledge for developing natural products. Commercial repellents with plant-based ingredients are popular, but insufficient studies follow Pesticide Evaluation Scheme WHO guidelines. Further standardized studies are needed to evaluate repellent compounds and develop high-repellency and safe products. Essential Oils (EOs) from aromatic plants have gained popularity as low-risk insecticides due to their low toxicity and short environmental persistence. These plant-derived EOs, produced through steam distillation, have repellent, insecticidal, and growth-reducing effects on various insects. They control phytophagous insects, bite flies, and home and garden insects. US registration is the main hurdle for new EOs. This review explores the use of essential oils from plants as a natural repellent, focusing on their effectiveness and synergistic effects. Essential oils are volatile mixtures of hydrocarbons with diverse functional groups, and their effectiveness is linked to monoterpenes and sesquiterpenes. Synergistic effects can improve their effectiveness, and the use of other natural products, like vanillin, can increase protection time. <i>Cymbopogon spp., Ocimum spp</i>., and <i>Eucalyptus spp.</i> are among the most promising plant families.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"84-102"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142485100","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}

{"title":"Formulation, Characterization and Cytotoxic Effect of Indomethacin-loaded Nanoparticles.","authors":"Kaan Yalcınkaya, Behiye Senel, Evrim Akyıl","doi":"10.2174/0118715230348349241126053733","DOIUrl":"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>Objectives: </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), Polydispersity Index (PDI), Zeta Potential (ZP), Encapsulation Efficiency (%EE), and drug-excipient compatibility using DSC, FT-IR, and ¹H NMR; cumulative drug release rates were assessed using HPLC and <i>in vitro</i> 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":"139-148"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","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}

{"title":"Genistein Enhances the Beneficial Effects of Exercise on Antioxidant and Anti-inflammatory Balance and Cardiomyopathy in Ovariectomized Diabetic Rats.","authors":"Mohammad Mohammadi, Amir Mohammad Salehi, Samaneh Mohassel Azadi, Maryam Khajvand-Abedini, Farzaneh Nazari-Serenjeh, Parisa Habibi","doi":"10.2174/0118715230305886240916105248","DOIUrl":"10.2174/0118715230305886240916105248","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Aims: &lt;/strong&gt;This study aimed to investigate the effects of genistein, swimming exercise, and their co-treatment on heart oxidative stress, inflammation, and cardiomyopathy in ovariectomized diabetic rats.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Background: &lt;/strong&gt;It is well-established that diabetes is a major risk factor for cardiovascular disease in both young and postmenopausal women. Genistein is a natural phytoestrogen that has estrogenic effects. Studies have shown that genistein has a positive impact on menopause, cardiovascular disease, and diabetes in women. However, the impact of genistein treatment alone and in combination with exercise training on the management of cardiac disease in diabetic women after ovarian hormone deprivation has not been fully explored.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Objectives: &lt;/strong&gt;The objective of this study was to evaluate the effect of genistein alone or in combination with exercise training on the cardiac expression of oxidative/inflammation biomarkers (MDA, OSI, TOS, TNF- α, and NF-κB) and miRNA-133, IGF-1, and Bcl-2 in the diabetic ovariectomized rats.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;A group of Wistar rats were randomly divided into seven groups, with eight rats in each group. The groups were named control, sham, ovariectomized group (OVX), OVX +diabetes (OD), OD+ genistein (1 mg/kg, eight weeks; daily SC), OD+exercise (eight weeks), and OD+ genistein+exercise (eight weeks). The rats were given a high-fat diet and low-dose streptozotocin injection to induce diabetes. After eight weeks, the rats were anesthetized, and their hearts were removed. The study assessed the effects of treatment by measuring the expression of miRNA-133 using Real-time Polymerase Chain Reaction (PCR) and the protein levels of Bcl-2, Bax, and IGF- 1 using Western blotting. The study also evaluated the levels of inflammation and oxidative stress markers using ELISA. Pathological changes were also assessed using periodic acid Schiff and hematoxylin & eosin.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;After ovariectomy, the levels of cardiac miRNA-133, IGF-1, and Bcl-2 expression were down-regulated, and the levels of MDA, OSI, TOS, TNF-α, and NF-κB were increased, with a reduced total antioxidant capacity. Diabetes had an additive effect on these factors. Genistein was found to have a positive impact on oxidative and inflammation levels, and it also increased the expression of miRNA-133, Bcl-2, and IGF-1 in rats with OD. Furthermore, the combination of genistein and exercise had a positive effect on miRNA-133, Bcl-2, and IGF-1 expression in the heart, leading to a decrease in Bax levels. The combined intervention showed a noticeable improvement in oxidative and inflammation conditions. Histological examination revealed some abnormalities in cardiac tissue, which were found to be improved with genistein and/or exercise treatments.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;Genistein or/and exercise as a natural replacement therapy could improve diabeticinduced cardiac complic","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"103-113"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142559990","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}