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

{"title":"Inhibition of Fenton Reaction-driven Lipid Peroxidation and Anti-inflammatory Activity of Extracts from Roots of Debregeasia Longifolia.","authors":"Faruk Alam, Moidul Islam Judder, Sumi Barman, Md Moidul Islam, Mohidul Islam, Atul Adhikari, Sarbanga Bezbaruah","doi":"10.2174/0118715230437161260331073929","DOIUrl":"https://doi.org/10.2174/0118715230437161260331073929","url":null,"abstract":"<p><strong>Introduction: </strong>Debregeasia longifolia has been used traditionally in treating inflammatory and oxidative stress-associated disorders, but the potential of this herb in redox modulation has not been fully defined. Lipid peroxidation in biological substrates sensitive to oxygen acts as a good biomarker to determine antioxidant potential. The objective of this paper was to assess the antioxidant and anti-inflammatory properties of D. longifolia root extracts and to determine the connection between those properties and the levels of polyphenols and flavonoids.</p><p><strong>Methods: </strong>The roots of D. longifolia that were collected in Meghalaya, India, were authentic and extracted sequentially with increased polarity of the solvents. The antioxidant activity was determined by the inhibition of lipid peroxidation of brain lipid substrates by the Fe2+/H2O2 (Fenton reaction)- induced lipid peroxidation through the TBARS technique. Anti-inflammatory activity was assessed through carrageenan-induced swelling of paws in rats and protein denaturation inhibition. The polyphenols and flavonoids were totaled, and correlation analysis was conducted.</p><p><strong>Results: </strong>The lipid peroxidation inhibition of the ethanol extract was the highest (49.55%) and followed by the hydroalcoholic extract (45.17%). Antioxidant activity had strong positive relations with polyphenol (r = 0.9784) and flavonoid (r = 0.9624) contents. Extracts at 250 mg/kg were both found to be effective in reducing carrageenan-induced paw edema and as effective as indomethacin. Phytochemical analysis was performed, identifying compounds such as 2-propylphenol, quercetin glycosides, and atrazine-desethyl.</p><p><strong>Discussion: </strong>The ability to exert strong antioxidant and anti-inflammatory effects is probably due to the high content of polyphenols and flavonoids, which could be mediated by COX-2 and 5-LOX inhibitors.</p><p><strong>Conclusion: </strong>This paper confirms the traditional application of D. longifolia and demonstrates ethanolic root extracts as potential natural antioxidants and anti-inflammatory agents with therapeutic benefits.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-04-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147680134","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":"PREFACE.","authors":"Claudiu T Supuran","doi":"10.2174/0118715230495733260325093041","DOIUrl":"https://doi.org/10.2174/0118715230495733260325093041","url":null,"abstract":"","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147597384","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":"Anti-inflammatory Potential of Pongamia pinnata: A Comprehensive Review on Molecular Mechanisms and Therapeutic Implications.","authors":"Bhumika Dudhatra, Kashyap Thummar, Jigna Vadalia, Vaibhav Bhatt","doi":"10.2174/0118715230426226260126161153","DOIUrl":"https://doi.org/10.2174/0118715230426226260126161153","url":null,"abstract":"<p><p>Pongamia pinnata (L.) has long been used in both the Ayurvedic and Siddha systems of medicine. It belongs to the leguminous family and shows significant potential for antiinflammatory activity, further supported by growing pharmacological and mechanistic evidence. This paper discusses recent advances in the study of its phytochemistry and the molecular mechanisms underlying its anti-inflammatory effects. Flavonoids, furanoflavonoids, terpenoids, and sterols are the main bioactive compounds, which modulate key inflammatory pathways such as NF- κB, COX-2, iNOS, and the expression of proinflammatory cytokines. Antioxidant, immunomodulatory, and membrane-stabilising activities help reduce oxidative stress and inflammation. Diseasespecific evidence highlights potential roles in arthritis, metabolic inflammation, neurodegeneration, and skin disorders. Emerging formulation approaches, including nanoparticles, ethosomes, and hydrogels, have improved the bioavailability, stability, and targeted delivery of various constituents of P. pinnata. Although preclinical studies have demonstrated a favourable safety profile, inadequate clinical validation and the need for standardised formulations remain two major barriers to therapeutic translation. This review aims to guide future research towards standardisation, pharmacokinetics, and formulation development to position P. pinnata as an attractive candidate for anti-inflammatory drug development.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-03-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147629684","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":"The Structural Analogy of MASP-2 with Thrombin and MASP-1 Reveals Strong Binding with PAR4.","authors":"Uzma Saqib, Mridul Madhuri, Sumati Hajela, Sadhana Sharma, Krishnan Hajela","doi":"10.2174/0118715230411505251126063432","DOIUrl":"https://doi.org/10.2174/0118715230411505251126063432","url":null,"abstract":"<p><strong>Introduction: </strong>The historical discovery that thrombin activates Protease-Activated Receptor 4 (PAR4) has paved the way for several novel findings. Besides thrombin, the complement lectin pathway protease Mannose-Binding Lectin-Associated Serine Protease-1 (MASP-1) also binds to PAR4, albeit with lower affinity. Similar to thrombin, MASP-1 activates Ca²⁺ signaling pathways in endothelial cells. MASP-2, a homolog of MASP-1, plays an important role in complement activation; however, its direct interaction with PAR4 has not yet been elucidated. In this study, we performed structural investigations of thrombin, MASP-1, and MASP-2 to evaluate their binding affinities toward the PAR4 peptide.</p><p><strong>Methods: </strong>We employed in silico docking, binding affinity calculations, molecular dynamics simulations, and mutagenesis studies to test our hypothesis.</p><p><strong>Results: </strong>For the first time, we demonstrate that, like thrombin and MASP-1, MASP-2 binds to PAR4 with appreciable affinity and could serve as a potential agonist of the PAR4 receptor and its associated inflammatory signaling pathways.</p><p><strong>Discussion: </strong>The high sequence similarity of MASP-2 with MASP-1 and thrombin is an important factor in attaining comparable binding with the PAR4 peptide.</p><p><strong>Conclusion: </strong>Our findings may pave the way for future investigations into the signaling mechanisms and therapeutic potential of PAR4-mediated inflammatory diseases.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146055681","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":"Pyrazole Derivatives as Selective COX-2 Inhibitors: An Updated Review.","authors":"Rajarshi Nath, Bikram Nandi, Arindam Maity, Sourav Maiti, Indrajit Maity, Sourasish Mallick, Shah Alam Khan, Samiran Paul, Biplab Debnath, Md Jawaid Akhtar","doi":"10.2174/0118715230435505251027113148","DOIUrl":"https://doi.org/10.2174/0118715230435505251027113148","url":null,"abstract":"<p><p>Inflammation is a defensive mechanism in the pathophysiology of many chronic diseases, including cancer, gastrointestinal problems, arthritis, cardiovascular disease, chronic wounds, and lesions, which may lead to death worldwide. Research over several decades has resulted in many non-steroidal anti-inflammatory drugs (NSAIDs), but they are associated with adverse drug reactions. As a result, the need for new anti-inflammatory drugs has significantly increased. A key target of NSAIDs, cyclooxygenase (COX) catalyses the synthesis of prostanoids, a broad family of arachidonic acid metabolites including prostacyclin, thromboxane, and prostaglandins. The inhibition of COX is implicated in gastrointestinal toxicities and ulceration. The inducible isoform of COX-2 is quickly expressed in various cell types in response to proinflammatory chemicals, cytokines, growth factors, and diseases related to inflammation. Thus, avoidance strategies for the nonselective COX inhibition and targeting COX-2 selectively are studied for COX-2 inhibitors for the treatment of inflammation, free from side effects. The scaffolds present in known inhibitors are important to achieve the goals. Pyrazole is the most noticeable and familiar heterocyclic scaffold. The prominent anti-inflammatory properties of pyrazole derivatives make them an important family of drugs. This article provides a comprehensive overview of new pyrazole derivatives synthesis and inhibitory activity against COX-2 for the past 5 years. The structure-activity relationship (SAR) and docking insights from this article could be helpful for the medicinal chemist in the development of next-generation COX-2 inhibitors.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147313928","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":"Design, Spectral Insights, and Enhanced Antioxidant Potential of Novel Phenothiazine Derivatives-1.","authors":"Shamsher Singh, Himanchal Sharma, Smiriti Gohri, Dhananjay Taumer","doi":"10.2174/0118715230378846251009082148","DOIUrl":"https://doi.org/10.2174/0118715230378846251009082148","url":null,"abstract":"<p><strong>Introduction: </strong>Phenothiazine derivatives represent an important class of heterocyclic compounds known for a wide range of pharmacological activities. Their antioxidant potential has drawn considerable interest for therapeutic applications against oxidative stress-related disorders. This study focused on synthesizing a new series of phenothiazine derivatives and evaluating their antioxidant activity.</p><p><strong>Methods: </strong>A series of phenothiazine derivatives [5a-5h] was synthesized by conjugating phenothiazine with various aryl amines via an acetyl linker using standard organic synthesis techniques. The structures of the synthesized compounds were confirmed using spectroscopic techniques, including FT-IR, ^1H NMR, ^13C NMR, and mass spectrometry (MS). Antioxidant activity was assessed using two in vitro assays: the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method and the low-density lipoprotein (LDL) oxidation inhibition assay.</p><p><strong>Results: </strong>All synthesized compounds were successfully characterized by the aforementioned spectroscopic techniques. The antioxidant assays revealed that most of the derivatives exhibited notable antioxidant activity. Among them, Compound 5e, bearing a 4-amino-2-methoxyphenol moiety, demonstrated the highest activity, surpassing the standard antioxidants Vitamin C and butylated hydroxyanisole (BHA). Conversely, compound 5h showed comparatively lower activity.</p><p><strong>Discussion: </strong>The findings indicate that structural variations, particularly the presence of electrondonating groups on the phenothiazine ring, significantly influence antioxidant potential. The superior performance of Compound 5e highlights the importance of specific substituent patterns in enhancing biological activity. However, further investigation into pharmacokinetics and in vivo efficacy is necessary to support potential therapeutic use.</p><p><strong>Conclusion: </strong>The study successfully synthesized and characterized a novel series of phenothiazine derivatives, several of which exhibited potent antioxidant properties. Structure- activity relationship (SAR) analysis suggested that electron-donating substituents enhance activity, pointing to promising future applications in treating oxidative stress-related conditions.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145902158","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":"Clinical Applications of Ligand Traps Targeting Activin Type II Receptors.","authors":"Kunihiro Tsuchida","doi":"10.2174/0118715230416604251029062751","DOIUrl":"https://doi.org/10.2174/0118715230416604251029062751","url":null,"abstract":"<p><p>This review summarizes recent advances in ligand trap therapies targeting activin type II receptors [ActRIIA/ACVR2A and ActRIIB/ACVR2B], which serve as shared receptors for members of the TGF-β family, including activins, GDF11, and myostatin [MSTN]. These receptors mediate Smad2/3 signaling and play critical roles in hematopoiesis, vascular homeostasis, and muscle regulation. Two peptide-based ligand traps have recently received clinical approval: luspatercept [ActRIIB-Fc], an erythroid maturation agent, and sotatercept [ActRIIA-Fc], a novel therapeutic agent for pulmonary arterial hypertension [PAH]. Luspatercept primarily inhibits activin B and GDF11, thereby promoting late-stage erythropoiesis and demonstrating efficacy in anemia associated with conditions such as myelodysplastic syndromes [MDS] and β-thalassemia. Sotatercept binds activins and GDFs to rebalance Smad2/3 and Smad1/5/8 signaling, thereby improving vascular remodeling in PAH. Although both agents have failed to increase skeletal muscle mass in clinical trials consistently, they represent significant advances in the treatment of hematopoietic and vascular disorders. Future studies should focus on optimal dosing strategies, long-term safety, and potential synergistic effects when combined with other therapeutic modalities.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145902179","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":"Visfatin as a Potential Inflammatory Biomarker and Therapeutic Target in Osteoarthritis: A Narrative Review.","authors":"Utpal Bhui, Ashutosh Sengar, Bimlesh Kumar, Shantanu Bandopadhyay","doi":"10.2174/0118715230409497251105102359","DOIUrl":"https://doi.org/10.2174/0118715230409497251105102359","url":null,"abstract":"<p><p>Osteoarthritis (OA) is a common, chronic degenerative joint disease that leads to the progressive degeneration of articular cartilage, subchondral bone, and synovium. In short, it is characterized primarily by inflammation, cartilage breakdown, and subchondral bone remodeling leading to joint pain, stiffness, and severe functional limitations. OA pathogenesis results from complex reciprocal interactions between genetic, mechanical, and environmental factors that culminate in the activation of pro-inflammatory mediators such as Interleukin 1β (IL 1β) and Tumor Necrosis Factor alpha (TNF α), which stimulate Matrix Metalloproteinases (MMPs) and break down the cartilage extracellular matrix. Additionally, oxidative stress, mitochondrial dysfunction, and chondrocyte senescence play crucial roles in disease progression. Consequently, adipokines have become important contributors to OA pathophysiology, with special emphasis on visfatin. These molecules released from adipose tissue also represent a systemic proinflammatory signal, found at higher concentrations in OA synovial fluid, and contribute to cartilage degradation and worsening of clinical symptoms. Visfatin participates in various signaling pathways to further amplify inflammatory cascades and cartilage destruction. In this review, we explore the role of visfatin and its possible mechanisms contributing to the progression of OA.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145703563","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":"Microsponge Drug Delivery Systems: Advancing the Therapeutic Efficacy of Anti-Inflammatory Medications.","authors":"Akshay Kumar, Rakesh, Rajesh Gautam, Vir Vikram","doi":"10.2174/0118715230401202251106104630","DOIUrl":"https://doi.org/10.2174/0118715230401202251106104630","url":null,"abstract":"<p><p>Microsponge drug delivery systems represent an innovative approach to enhancing the therapeutic efficacy of anti-inflammatory drugs through controlled release, improved bioavailability, and targeted delivery. These porous polymeric microspheres, ranging from 5 to 300 μm, encapsulate active pharmaceutical ingredients (APIs) to achieve sustained drug release, minimizing systemic side effects and dosing frequency. Chronic inflammatory conditions, such as rheumatoid arthritis, inflammatory bowel disease (IBD), and psoriasis, often require prolonged treatment, but conventional therapies such as nonsteroidal anti-inflammatory drugs (NSAIDs) and corticosteroids are limited by systemic toxicity and frequent administration. Microsponges address these challenges by enhancing drug stability, increasing retention at the target site, and reducing systemic exposure. Advanced fabrication techniques, including emulsion solvent diffusion, liquid-liquid suspension polymerization, and electrohydrodynamic atomization, allow precise control over microsponge properties, optimizing drug loading and release kinetics. In arthritis, microsponges extend anti-inflammatory activity; in IBD, they enable colon-specific delivery; and in psoriasis, they enhance drug penetration through keratinized plaques. These systems improve patient compliance by reducing dosing frequency and minimizing adverse effects. Despite their promise, further research is needed to optimize formulations, evaluate long-term safety, and fully explore their potential in managing chronic inflammatory diseases. Microsponge technology offers a transformative platform for improving therapeutic outcomes, paving the way for innovative treatments in pharmaceutical and clinical applications.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145703584","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":"Next-Generation Probiotics in Allergy Therapy: Scientific Evidence and Clinical Applications.","authors":"Vatan Chaudhary, Atul Pratap Singh, Himanchal Sharma, Dhananjay Taumar","doi":"10.2174/0118715230407403251105101126","DOIUrl":"https://doi.org/10.2174/0118715230407403251105101126","url":null,"abstract":"<p><p>The global increase in allergic diseases, such as atopic dermatitis, allergic rhinitis, asthma, and food allergies, has become a major public health issue. These diseases typically involve immune dysregulation, including a Th1/Th2 imbalance, increased IgE levels, regulatory T cell (Treg) dysfunction, and epithelial barrier dysfunction. New research has recognised an important role for the gut and mucosal microbiome in regulating immune responses and has prompted interest in the therapeutic utility of probiotics. Probiotics are live microbes that, when given in adequate amounts, confer health benefits, generally such as immunomodulation or restoration of gut barrier function. Traditional probiotics (i.e., Lactobacillus and Bifidobacterium species) reduce allergic inflammation through promotion of Treg differentiation, increases in antiinflammatory cytokines (e.g., IL-10), suppression of Th2 cytokines (e.g., IL-4), and modification of IFNγ. Traditional probiotics also support mucosal barrier function and restore microbial composition by producing short-chain fatty acids (SCFAs), like butyrate, which act directly on Gprotein- coupled receptors and histone deacetylases to suppress inflammation. Next-generation probiotics (NGPs), such as Akkermansia muciniphila, Faecalibacterium prausnitzii, Bacteroides fragilis, and some clusters of Clostridia, can provide more targeted effects. These NGPs can secrete anti-inflammatory metabolite compounds, such as polysaccharide A (PSA), which modulate dendritic cells and increase Treg activity, and can promote mucin production to improve gut barrier function. Overall, there are key issues with strain specificity, dose, safety in immunocompromised individuals, and possible regulatory classification issues. Future opportunities may include precision microbiome profiling, synthetic biology, and artificial intelligence-driven strain discovery to develop personalised approaches to allergy immunotherapy.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145703534","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}