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

{"title":"Antiurolithiatic Potential of Colocasia esculenta Tubers: An Integrative In Silico, In Vitro, and In Vivo Evaluation.","authors":"Vishal Chanalia, Gurvirender Singh, Smita Narwal, Ashwani K Dhingra, Dushyant, Khushbu, Ashutosh","doi":"10.2174/0118715230431617251204215745","DOIUrl":"https://doi.org/10.2174/0118715230431617251204215745","url":null,"abstract":"<p><strong>Introduction: </strong>Colocasia esculenta has been traditionally used in Persian medicine for treating kidney ailments, with its rhizome juice reportedly effective in dissolving kidney stones. Building upon this ethnomedicinal background, the present study investigated the antiurolithiatic potential of ethanolic extracts derived from the tubers of Colocasia esculenta using a comprehensive approach encompassing in silico, in vitro, and in vivo methodologies.</p><p><strong>Methods: </strong>In vitro assays included nucleation, aggregation, and titrimetric assays. The in vivo antiurolithiatic activity was assessed using an ethylene glycol (0.75% v/v)-induced urolithiasis model in female Wistar rats, divided into six groups (n = 6). The extract was administered orally at doses of 100, 200, and 400 mg/kg body weight/day, with Cystone serving as the standard reference drug.</p><p><strong>Results: </strong>Phytochemical screening of the ethanolic extract confirmed the presence of bioactive constituents such as flavonoids, tannins, and phenolics, known for their antioxidant and therapeutic properties. The extract demonstrated significant antioxidant activity in DPPH, hydrogen peroxide, and FRAP assays, indicating a potential role in mitigating oxidative stress-related renal damage. In silico docking indicated strong protein-ligand affinities for key phytoconstituents with targets implicated in stone regulation, including vitexin binding to 1PU0, catechin binding to 7P8W and 2ETE, and quercetin binding to 5ZJF and 2NZL. These compounds exhibited superior inhibitory potential compared to standard antiurolithiatic agents such as potassium citrate, indicating their role in preventing crystal aggregation and nucleation. In vitro assays showed that the extract effectively inhibited calcium oxalate crystal formation, an essential step in preventing kidney stone growth. In vivo studies demonstrated dose-dependent improvements, including significant reductions in serum urea, creatinine, and uric acid levels, along with decreased renal crystal deposition. Histopathological analysis confirmed reduced kidney inflammation and crystal accumulation, particularly at the highest dose.</p><p><strong>Discussion: </strong>Collectively, these findings suggest that ethanolic extracts of Colocasia esculenta tubers possess promising antiurolithiatic activity. The observed effects may be attributed to their antioxidant potential, enzyme inhibition properties, and direct interference with calcium oxalate crystal formation.</p><p><strong>Conclusion: </strong>This study supports the traditional use of Colocasia esculenta in kidney disorders and highlights its potential for development into a natural therapeutic agent for urolithiasis.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148611541","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":"Pentacyclic Triterpenoids as Multitarget Ligands Bridging Inflammation, Metabolic Dysfunction, and Cancer: Mechanistic Insights and Translational Perspectives.","authors":"Siva Prasad Panda, Navneet Pachauri, Srishti Mishra, Vikrant Singh","doi":"10.2174/0118715230474288260703044805","DOIUrl":"https://doi.org/10.2174/0118715230474288260703044805","url":null,"abstract":"<p><p>Pentacyclic Triterpenoids (PTs) such as oleanolic acid, ursolic acid, and betulinic acid are a large family of natural products with considerable diversity and have excellent therapeutic potential in the treatment of inflammatory and metabolic diseases. PTs have substantial efficacy against both critical pathways in inflammation and glucose regulation. The anti-inflammatory effects are mainly achieved by inhibiting nuclear factor-κB (NF-κB) activation, downregulating pro-inflammatory cytokines, and attenuating oxidative stress. At the same time, the anti-diabetic effects are related to the regulation/modulation of insulin signaling, activation of AMP-activated protein kinase (AMPK), modulation of peroxisome proliferator-activated receptor-gamma (PPAR-γ), and improvement of glucose homeostasis. Cross-talk between inflammation and metabolism explains the dual biological effects of PTs on inflammation and on patients with metabolic disorders. The Structure-Activity Relationship (SAR) studies show that certain structural modifications could improve each activity, indicating potential for rational drug design. The clinical translation of these agents, although supported by encouraging data in preclinical models, has been limited by issues regarding bioavailability, standardization, and the full assessment of safety. This review discusses the role of PTs in distinct pathological conditions (inflammation, diabetes, and cancer) and the integrated examination of inflammation-metabolism crosstalk via common molecular mediators (e.g., NF-κB, Nrf2, PPAR-γ, and PTP1B). This analysis bridges Structure-Activity Relationship (SAR) trends with translational and clinical insights. The resulting framework provides a mechanistically unified, forward-looking perspective designed to guide targeted therapeutic development. In contrast to single-target synthetic drugs, PTs simultaneously drive complexity in multifactorial diseases, including diabetes, metabolic syndrome, and inflammation-associated cancer, by modulating inflammatory, metabolic, and oxidative pathways.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148521762","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":"Preparation, Characterization, Optimization, and In vitro Anti-inflammatory Evaluation of Epigallocatechin Gallate (EGCG)-loaded Nanostructured Lipid Carriers.","authors":"Neelesh Singh, Rajesh Choudhary, Shilpi Prasad, Swarnali Das Paul","doi":"10.2174/0118715230462416260630105245","DOIUrl":"10.2174/0118715230462416260630105245","url":null,"abstract":"<p><strong>Introduction: </strong>Sustained joint inflammation and oxidative stress are symptoms of Rheumatoid Arthritis (RA), an autoimmune disorder characterized by chronic inflammation. The present study was designed to prepare Epigallocatechin Gallate (EGCG)-loaded Nanostructured Lipid Carriers (NLCs) for enhanced therapeutic benefits in inflammatory conditions like RA.</p><p><strong>Methods: </strong>The NLCs were prepared using lecithin using a modified hot homogenizationultrasonication approach containing an aqueous-to-lipid phase ratio of 3:1 (v/v), where the lipid phase consisted of stearic acid and oleic acid (70:30 ratio), while the aqueous phase contained Tween 80 (2% w/v) and soy lecithin (1% w/v). The effect of drug concentration, lipid-to-drug ratio, or stirring time on particle size, zeta potential, and entrapment efficiency was investigated and optimized using a Box-Behnken design. Solubility profiles and partition coefficients were analyzed by spectrophotometric methods. The antioxidant and anti-inflammatory activity of the optimized EGCG-loaded NLCs was evaluated using an in vitro DPPH, H2O2, and protein denaturation assay as a preliminary screening model.</p><p><strong>Results: </strong>The optimum EGCG-NLCs showed 82.78% DPPH radical scavenging, 92% H2O2 radical scavenging, and 97.23% inhibition of protein denaturation at high concentration (100 µg/ml).</p><p><strong>Discussion: </strong>The antioxidant and anti-inflammatory activity of EGCG-NLCs demonstrated their therapeutic acceptability for the topical treatment of inflammatory conditions.</p><p><strong>Conclusion: </strong>In conclusion, EGCG-loaded NLCs demonstrated enhanced stability, bioactivity, and applicability for targeted inflammatory conditions such as rheumatoid arthritis therapy. This nanocarrier holds great promise as a phytochemical vehicle delivery system, which can also be integrated with other sophisticated drug delivery structures and undergo in vivo testing in the future.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-07-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148431911","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":"Hypoxia-inducible Factors in Macrophage Polarization and Metabolic Reprogramming Under Stress: Implications for Inflammation and Tissue Repair.","authors":"Shawna Yadav, Kaliyamurthi Venkatachalam, Ambika Binesh","doi":"10.2174/0118715230462552260701063409","DOIUrl":"10.2174/0118715230462552260701063409","url":null,"abstract":"<p><p>Hypoxia-inducible Factors (HIFs) are the transcriptional regulators of the cellular response to low oxygen tension and metabolic changes. The transition of macrophages and their adaptability to environmental stressors, such as hypoxia and nutrient deprivation, serve as the central regulators of immune responses. This review covers the role of Hypoxia-Inducible Factors (HIFs), chiefly HIF-1α and HIF-2α, in stress-mediated macrophage polarization and metabolic reprogramming. HIF-1α drives glycolytic activity and inflammatory gene expression, resulting in the development of an M1 - like pro-inflammatory activation state, while HIF-2α enables alternatively activated (M2- like) macrophages to support tissue remodeling, angiogenesis, and resolution of inflammation through oxidative metabolism and tissue repair. The two proteins HIF-1α and HIF-2α maintain a balance that controls whether macrophages develop inflammatory diseases or repair damaged tissues; therefore, this balance serves as a potential target for medical treatments. The balance between HIF-1α and HIF-2α determines how macrophages respond to inflammation versus tissue repair, representing a new area for potential treatment development. Additional modulation of these responses is achieved through interaction with the NF-κB, mTOR, and STAT3 signaling pathways. Any metabolic changes downstream of the HIFs can alter the functional outcome of macrophages in diseases such as obesity, cancer, atherosclerosis, and chronic inflammation. Inflammation resolution and angiogenesis, probably facilitated via HIFs, follow efficient wound healing and tissue regeneration. With the refinement in emerging technologies and future therapeutic opportunities in molecular technologies such as CRISPR and single-cell multi-omics, it has become possible to unravel the finely regulated, context-dependent roles of HIFs, thus opening exciting vistas for immune therapeutics.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-07-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148431866","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":"Management of Rheumatoid Arthritis and Oxidative Stress and the Role of Drug Delivery System.","authors":"Zulfa Nooreen, Harshita Sachan, Akshada Amit Koparde, Sharad R Manapure, Vipinchandra B Pande, Ameeduzzafar Zafar, Abida","doi":"10.2174/0118715230387199251002042359","DOIUrl":"https://doi.org/10.2174/0118715230387199251002042359","url":null,"abstract":"<p><p>A systemic inflammatory illness called rheumatoid arthritis (RA), characterized by persistent joint inflammation, results in early mortality and severe disability. Around 1% of people worldwide have it, with women experiencing two to three times the rate of men. The pathophysiology and factors involved in the pathogenesis of RA are covered in this review. The previous 20 years have seen noticeable progress in understanding the mechanisms behind the onset of RA, improving early diagnosis. The most well-known medications used to treat RA are still disease- modifying anti-rheumatic drugs (DMARDs), non-steroidal anti-inflammatory drugs (NSAIDs), and corticosteroids. Oxidative stress, a state in which the concentration of reactive oxygen species (ROS) rises due to increased production, decreased antioxidant defenses, or a combination of the two, has been associated with rheumatoid arthritis. This suggests a breakdown in redox signaling. It is yet unknown exactly how oxidative stress may contribute to the development and maintenance of systemic and locally inflamed rheumatoid arthritis, especially in the early stages. The present review discusses the management of rheumatoid arthritis and oxidative stress, with an emphasis on phytomolecules and novel approaches. Most importantly, we go into detail about newly developed drug delivery systems, including liposomes, dendrimers, micelles, nanoparticles, and microspheres. These techniques show great promise for the management of RA and help overcome the drawbacks of conventional drug delivery systems.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148400367","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":"Comparative Study of Bioactive Potential and Antifungal Susceptibility in H. undatus and H. polyrhizus Stem Extracts.","authors":"V V Chandana Mahanti, Dwarapureddy Anupama Kavya Priya","doi":"10.2174/0118715230463013260623093710","DOIUrl":"https://doi.org/10.2174/0118715230463013260623093710","url":null,"abstract":"<p><strong>Introduction: </strong>Hylocereus species, an economically valuable crop cultivated in tropical and subtropical regions, are increasingly affected by fungal pathogens, leading to reduced yield. Understanding the phytochemical profile and bioactivity of Hylocereus stem extracts may support plant protection and therapeutic applications.</p><p><strong>Methods: </strong>Stem extracts of Hylocereus undatus and Hylocereus polyrhizus were subjected to phytochemical screening and evaluated for antioxidant activity using 2,2-Diphenyl-1-picrylhydrazyl and hydrogen peroxide assays, anti-inflammatory activity by protein denaturation inhibition, and antimicrobial efficacy against bacterial and fungal pathogens. The agar well diffusion assay was conducted using Fluconazole and Itraconazole to determine antifungal effectiveness.</p><p><strong>Results: </strong>Phytochemical profiling revealed the presence of alkaloids, phenols, saponins, tannins, and terpenoids in both species. Hylocereus polyrhizus demonstrated markedly higher antioxidant and anti-inflammatory activity, with an IC50 value of 170.88 μg/mL, compared to Hylocereus undatus, which had an IC50 value of 257.72 μg/mL. Antibacterial assays showed significant inhibition against Neisseria meningitidis and Streptococcus pneumoniae. Agar well diffusion assay indicated dosedependent antifungal activity, with fluconazole exhibiting a maximum ZOI of 16.5 mm, which was higher than that of itraconazole.</p><p><strong>Discussion: </strong>The enhanced bioactivity of Hylocereus polyrhizus is linked to its richer phytochemical composition, indicating its potential as a natural source of multifunctional bioactive molecules. Although crude extracts lacked direct antifungal activity, the strong performance of commercial antifungals highlights the potential complementary application of plant-derived compounds in integrated disease management strategies.</p><p><strong>Conclusion: </strong>This in vitro study presents the first comparative evaluation of Hylocereus undatus and Hylocereus polyrhizus stem extracts, confirming the superior therapeutic potential of Hylocereus polyrhizus and identifying fluconazole as the most effective antifungal agent for managing dragon fruit fungal infections against the tested species.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148400386","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":"Benzothiazole Derivatives: Emerging Potential as Anti-Rheumatic Agents and other Pharmacological Effects.","authors":"Dhirendra Kumar, Divya Pathak, Smriti Gohri","doi":"10.2174/0118715230413902251127111500","DOIUrl":"https://doi.org/10.2174/0118715230413902251127111500","url":null,"abstract":"<p><p>Benzothiazole derivatives are receiving considerable attention for their diverse pharmacological properties, particularly as anti-rheumatic agents. Rheumatoid arthritis is a common musculoskeletal disorder associated with chronic inflammation and joint degradation, necessitating the development of novel treatments. Due to its ability to modulate several biological targets involved in inflammatory pathways, benzothiazole, a heterocyclic scaffold, has emerged as a potential pharmacophore. Benzothiazole derivatives are well documented to display analgesic, antiinflammatory, and immunomodulatory effects, making them promising candidates for antirheumatic drugs. These compounds have been shown to inhibit key cytokines such as TNF-α and IL-6, as well as enzymes like cyclooxygenase (COX) and lipoxygenase (LOX) involved in the inflammation activation sequence. In addition, benzothiazole derivatives exhibit low cytotoxicity, which is advantageous for long-term therapy of chronic diseases. They also possess a wide range of medicinal properties, including antimicrobial, anticancer, anticonvulsant, and antioxidant effects, and can be applied in the treatment of rheumatism. Their chemical structures can be readily modified to enhance selectivity and potency at specific targets, highlighting their versatility. In conclusion, benzothiazole derivatives represent a promising class of compounds for antirheumatic drug development. Ongoing studies have increasingly demonstrated their therapeutic benefits in pain relief, inflammation control, and other pharmacological effects, making them valuable targets for further drug development in rheumatic and related diseases.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148280808","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 of pH-responsive Nanocarriers for Controlled Delivery of Anti-allergic Corticosteroid Analogues.","authors":"Sergey Gupalo, Sutha Devaraj, Kyaw Zaw Win, Yuan Seng Wu, Phone Myint Htoo, Wana Hla Shwe, Rohini Karunakaran, Aravinda Wundavalli, Suprava Das, Manglesh Waran Udayah, Nazmul Mhm","doi":"10.2174/0118715230469773260608050414","DOIUrl":"https://doi.org/10.2174/0118715230469773260608050414","url":null,"abstract":"<p><strong>Introduction: </strong>Allergic inflammation has become an important public health issue. If left uncontrolled, it can lead to serious health problems. Mast cells and the drugs that regulate the endosomal compartments in these cells have become central to addressing these problems. The aim of this project was to build a biological model capable of regulating the intracellular delivery of anti-allergic corticosteroids.</p><p><strong>Methods: </strong>The nanocarrier was designed based on micellar swelling and pH-responsive acid-sensitive linkers. The model's functionality was evaluated through a range of physicochemical characterization and in silico tests. Mathematical modeling was incorporated to simulate the nanocarrier's behavior and diffusion control. Models representing mucosal and mast cell-relevant environments were used to evaluate the designed system in a simulated microenvironment.</p><p><strong>Results: </strong>The nanocarriers showed clear micellar swelling and a pronounced positive surface charge, with high drug encapsulation efficiency, and displayed both pH- and time-dependent behavior, as supported by physicochemical characterization and computational modeling. Mathematical modeling showed that charge dissolution was controlled and that drug release was governed by the rate of proton-dependent drug degradation. The system exhibited minimal drug release under physiological pH conditions, ensuring stability, while enabling controlled and enhanced drug release under acidic conditions relevant to mast cell-associated microenvironments. The system has low hemolysis, low cellular epithelial cytotoxicity, prolonged drug diffusive release, and favorable diffusive release.</p><p><strong>Discussion: </strong>The collected data confirm that the design enables both time- and space-controlled release of the drug from the nanocarrier system within endolysosomal compartments associated with the allergic inflammatory response. The noted control of mast cell secretions illustrates immunomodulation and the control of side effects from systemic/extended use of corticosteroids.</p><p><strong>Conclusion: </strong>This study demonstrates that the system is not only safe and effective for the delivery of drugs into cells but also capable of targeting cells involved in the allergic inflammatory pathway. The emerging pH-sensitive nanocarriers have strong therapeutic potential.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-06-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148267724","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":"Antifungal Efficacy of Natural Oils: A Comprehensive Review on Mechanisms and Innovations.","authors":"Piyush Jain, Shashikant Chandrakar, Pushpa Prasad Gupta","doi":"10.2174/0118715230423421251201150456","DOIUrl":"https://doi.org/10.2174/0118715230423421251201150456","url":null,"abstract":"<p><strong>Introduction: </strong>Rising resistance to conventional antifungal agents, along with concerns over toxicity and environmental safety, has intensified the search for more sustainable and safer alternatives. Natural oils, particularly essential oils and certain fixed oils, have drawn attention for their broad-spectrum antifungal properties and favourable safety profiles. This review aims to provide a comprehensive overview of the antifungal potential of natural oils, exploring their mechanisms of action, practical applications, and recent advances in formulation strategies.</p><p><strong>Methods: </strong>To ensure transparency and reproducibility, this review followed a systematic literature search strategy covering peer-reviewed studies published between 2021 and 2025. The selection focused on research exploring the chemistry, biological activity, and translational applications of natural oils with antifungal potential. Eligible studies were critically analyzed, and findings were narratively synthesized to identify key trends and evidence gaps. Particular emphasis was placed on understanding the effects of these oils on fungal cell structures and functions, as well as their potential applications in healthcare, agriculture, and food preservation.</p><p><strong>Results: </strong>Natural oils exhibit multiple mechanisms of antifungal action, including disruption of fungal cell membranes and walls, inhibition of biofilm formation, interference with virulence factors, and modulation of cellular processes like efflux pump activity and mitochondrial function.</p><p><strong>Discussion: </strong>The use of natural oils extends across topical medical treatments, crop protection, food preservation, and industrial systems. Innovations in nanotechnology and synergistic formulations have further enhanced their efficacy. However, challenges remain in standardization, stability, and delivery optimization, including limited clinical trials demonstrating real-world efficacy against resistant strains like Candida albicans biofilms.</p><p><strong>Conclusion: </strong>Natural oils hold significant promise as effective antifungal agents within integrated approaches to human health, agriculture, and food safety. Continued research and technological innovation are essential to fully harness their potential and address current limitations in formulation and application, such as regulatory hurdles in clinical translation.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-05-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148140563","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":"Developing a Natural Oil-Based Organogel to Improve the Topical Delivery of Sertaconazole Nitrate.","authors":"Piyush Jain, Shashikant Chandrakar, Pushpa Prasad Gupta, Ravindra Kumar Pandey, Beena Gidwani","doi":"10.2174/0118715230426510251215061748","DOIUrl":"https://doi.org/10.2174/0118715230426510251215061748","url":null,"abstract":"<p><strong>Objective: </strong>Conventional topical antifungal therapies often exhibit limited efficacy, poor patient adherence, and inadequate stability. To address these challenges, a microwave-assisted clove oil-based organogel of sertaconazole nitrate was developed to enhance antifungal activity, sustain drug release, and improve long-term stability.</p><p><strong>Methods: </strong>Organogels were prepared using sertaconazole nitrate, clove oil, Carbopol 934, and polyethylene glycol 400. Physicochemical parameters, including pH, viscosity, spreadability, and drug content, were evaluated, followed by in vitro drug release and ex vivo skin permeation studies using Franz diffusion cells. Antifungal activity was tested against Candida albicans and Trichophyton rubrum, while in vivo therapeutic efficacy and skin irritation were assessed in a dermatophytosis rat model. The long-term stability of the formulation was monitored for 24 months.</p><p><strong>Results: </strong>The optimized formulation (F12) showed excellent performance, with a drug content of 99.96%, viscosity of 41.45 Pa.s, and spreadability of 26.81 g.cm/sec. Drug release reached 99.5% within 24 hours, following zero-order kinetics with a non-Fickian release mechanism. Ex vivo permeation was significantly higher (99.2%) than that of the marketed cream (81.7%). Enhanced antifungal activity was observed, with inhibition zones of 1.82 cm (Candida albicans) and 2.01 cm (Trichophyton rubrum). In vivo studies confirmed effective therapeutic action without signs of skin irritation. Notably, the formulation maintained its physicochemical integrity and antifungal potency throughout 24 months of storage.</p><p><strong>Discussion: </strong>The microwave-assisted technique proved to be a simple, reproducible, and efficient approach for organogel fabrication. The inclusion of clove oil contributed to improved antifungal performance and enhanced skin permeation, thereby strengthening the formulation's therapeutic potential.</p><p><strong>Conclusion: </strong>The developed sertaconazole nitrate organogel demonstrated a safe, effective, and stable topical delivery system with superior antifungal efficacy and long-term stability, representing a promising alternative to conventional antifungal therapies.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147985020","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}