Antiinflamm Antiallergy Agents Med Chem [JOURNAL]
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200 papers
Resveratrol as a Regulator of Inflammation, Oxidative Stress, and Glucose Stability in Diabetes.
M Hasbullah A, Binesh A, Venkatachalam K
Antiinflamm Antiallergy Agents Med Chem · 2025 Oct · PMID 41169130 · Publisher ↗
Diabetes mellitus, a complex metabolic disorder, proves to be a challenge for the population around the world, as it includes chronic inflammation, oxidative stress, and glucose dysregulation. Resveratrol is a naturally...
Diabetes mellitus, a complex metabolic disorder, proves to be a challenge for the population around the world, as it includes chronic inflammation, oxidative stress, and glucose dysregulation. Resveratrol is a naturally occurring compound that acts as a diabetes complication- mitigating agent through complex cellular maneuvers and acts specifically to remedy diabetes complications. This review focuses on the action of resveratrol, underlining its vital impact in the alteration of significant pathophysiological pathways in diabetes. Besides, the activation of the AMPK and SIRT1 pathways also greatly improved cellular stress responses as well as insulin sensitivity. Numerous clinical studies have validated that the implementation of natural polyphenols' supplementation enhances glucose control, diabetes, inflammation, and insulin sensitivity, which supports these study findings. Its clear safety profile and flexible bioavailability also enhance its position as an adjunct diabetes therapy. As promising as that is, some issues still need to be addressed, including tackling standardized challenges like dosage issues and bioavailability.
Isolation, Characterization, Molecular Docking, and Antioxidant Evaluation of Esculetin Derived from Cichorium intybus Seeds.
Naina, Chandra P
Antiinflamm Antiallergy Agents Med Chem · 2025 Oct · PMID 41051045 · Publisher ↗
INTRODUCTION: Cichorium intybus, a biennial plant belonging to the Asteraceae family, has been widely utilized in traditional Indian medicine for its tonic, anti-acne, anti-inflammatory, antioxidant, and hepatoprotective...
INTRODUCTION: Cichorium intybus, a biennial plant belonging to the Asteraceae family, has been widely utilized in traditional Indian medicine for its tonic, anti-acne, anti-inflammatory, antioxidant, and hepatoprotective properties. Despite its known medicinal benefits, the bioactive compounds responsible for these activities require further exploration to validate their therapeutic potential. Our aim is to investigate the molecular docking interactions and antioxidant potential of an isolated bioactive compound from Cichorium intybus seeds, with a focus on its role in mitigating oxidative stress and inflammation in the liver. METHODS: The compound was isolated using ethanol extraction, followed by phytochemical screening, TLC, column chromatography, and identification through FTIR, NMR, and mass spectroscopy. Molecular docking studies were conducted using Schrödinger Suite to analyze interactions with PPARα. Antioxidant activity was evaluated using DPPH and ABTS radical scavenging assays, with results compared through Trolox Equivalent Antioxidant Capacity (TEAC) values. RESULTS: Esculetin, the isolated compound, exhibited strong binding affinity with PPARα (XP GScore: -7.0 kcal/mol). Antioxidant assays showed moderate activity, with DPPH radical scavenging activity (RSA) of 10.37% and ABTS RSA of 7.445%. The TEAC values were 13.23 μmol/mg and 21.930 μmol/mg, respectively, indicating its potential antioxidant efficacy. DISCUSSION: Esculetin from Cichorium intybus showed moderate antioxidant activity and strong PPARα binding, indicating its potential as a therapeutic agent. These findings align with existing research but require validation through in vivo studies to confirm efficacy and elucidate biological mechanisms. CONCLUSION: Esculetin demonstrates significant potential as a bioactive antioxidant and antiinflammatory agent, supporting its relevance for further pharmacological and therapeutic investigations.
Analytical Techniques for the Quantification and Validation of Resveratrol: A Review.
Goel H, Nagarajan K, Nainwal LM … +1 more , Bhardwaj S
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 40993954 · Publisher ↗
INTRODUCTION: Trans-resveratrol is a bioactive polyphenol that has been widely studied for its antioxidant, anti-inflammatory, and chemoprotective properties. It holds promise in pharmaceutical and nutraceutical formulat...
INTRODUCTION: Trans-resveratrol is a bioactive polyphenol that has been widely studied for its antioxidant, anti-inflammatory, and chemoprotective properties. It holds promise in pharmaceutical and nutraceutical formulations but is limited by poor bioavailability and stability. METHODS: This review synthesizes validated analytical methods for quantifying trans-resveratrol across various matrices. A comprehensive literature search (2000-2024) was conducted using PubMed, Scopus, and Google Scholar, focusing on RP-HPLC, HPTLC, GC, and UV spectroscopy. Method validation follows ICH guidelines. and nutraceutical formulations but is limited by poor bioavailability and stability. RESULTS: Thirty-seven validated analytical methods were reviewed. RP-HPLC using C18 columns with acetonitrile-water mobile phases dominated the literature. The most sensitive technique identified was LC-MS/MS (LOD = 0.001 μg/mL), particularly effective in biological samples. Matrix types included wine, serum, and nanoparticle formulations. and nutraceutical formulations but is limited by poor bioavailability and stability. DISCUSSION: RP-HPLC and LC-MS/MS have emerged as robust techniques for resveratrol quantification due to their sensitivity and specificity. Emerging tools like biosensors and UPLC offer rapid analysis with lower solvent consumption. Challenges such as isomerization, photodegradation, and matrix interferences necessitate stringent sample-handling protocols. and nutraceutical formulations but is limited by poor bioavailability and stability. CONCLUSION: Advanced chromatographic methods, especially RP-HPLC and LC-MS/MS, are essential for the reliable quantification of trans-resveratrol. Future research should focus on analytical standardization and the development of novel delivery systems to enhance resveratrol's pharmacokinetic profile.
Developments in the Management Strategies for Allergy: Advances in Artificial Intelligence and Future Perspectives.
Kumar S, Malviya R, Sridhar SB … +2 more , Shareef J, Wadhwa T
Antiinflamm Antiallergy Agents Med Chem · 2025 Sep · PMID 40965022 · Publisher ↗
INTRODUCTION: Artificial intelligence (AI) is rapidly transforming biomedical research by offering advanced tools to analyse complex datasets. In the field of allergy studies, however, the translation of AI-generated ins...
INTRODUCTION: Artificial intelligence (AI) is rapidly transforming biomedical research by offering advanced tools to analyse complex datasets. In the field of allergy studies, however, the translation of AI-generated insights into clinical practice remains limited and underutilised. METHOD: This review critically discussed the current applications of AI in allergy studies. It focuses on the methodological foundations of AI, including machine learning and clustering algorithms, and assesses their practical benefits and limitations. Representative case studies are explored to demonstrate real-world applications, and challenges in data quality, integration, and algorithmic fairness are examined. RESULTS: AI techniques have shown promise in tasks such as disease phenotyping and patient stratification within allergy research. Case studies reveal that AI can uncover immunological insights and support precision medicine approaches. However, the field faces challenges, including fragmented data sources, algorithmic bias, and the limited presence of therapeutic AI tools in clinical practice. DISCUSSION: Despite the demonstrated potential, several barriers hinder the broader adoption of AI in allergy care. These include the need for high-quality, standardised datasets, ethical oversight, and transparent methodologies. The review highlights the importance of these factors in ensuring the reliability, reproducibility, and equity of AI-driven interventions in allergy research. CONCLUSION: AI holds significant promise for improving diagnostic accuracy and enabling personalised treatment strategies in allergy care. Realising its full potential will require robust frameworks, ethical governance, and interdisciplinary collaboration to overcome current limitations and drive clinical translation.
Preparation and Evaluation of Amorphous Solid Dispersion of Etoricoxib, Employing A Fast Approach for Polymer Selection.
Shaikh BM, Gajbe JW, Madgulkar AR … +2 more , Bhalekar MR, Shinde MB
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 40908687 · Publisher ↗
BACKGROUND: Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used to manage pain and inflammation but are associated with gastrointestinal and cardiovascular risks, especially with COX-2 inhibitors. Topical del...
BACKGROUND: Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used to manage pain and inflammation but are associated with gastrointestinal and cardiovascular risks, especially with COX-2 inhibitors. Topical delivery systems offer a safer alternative by minimizing systemic exposure; however, poor solubility and limited skin penetration remain challenges. Enhancing solubility through solid dispersion and incorporating it into a gel formulation may improve permeability and therapeutic effectiveness, addressing the need for safer and more efficient topical NSAID delivery. INTRODUCTION: This investigation aimed to enhance the solubility and dissolution rate of poorly water-soluble etoricoxib through the development of solid dispersions using the kneading method. METHODS: A suitable carrier was selected from a pool of candidates based on polarised microscopy analysis. The influence of a solubilizer on amorphization was evaluated. Solid dispersions of Etoricoxib and its corresponding physical mixtures, incorporating or excluding the solubilizer, were prepared at varying drug-to-carrier ratios. Yield, drug content, saturation solubility, and dissolution profiles of these formulations were determined. Solid-state characterization using Fourier Transform-Infrared (FTIR), X-ray diffraction (XRD), Scanning electron microscopy (SEM), and differential scanning calorimetry (DSC) techniques was conducted. RESULTS: FTIR spectra indicated the formation of intermolecular hydrogen bonds within the dispersions. XRD, SEM, and DSC analysis confirmed the amorphous transition of crystalline etoricoxib in all the prepared solid dispersions. In comparison to pure etoricoxib and its physical mixes, the produced solid dispersions showed significantly improved dissolution and solubility, Discussion: Solid dispersion technology effectively enhanced the solubility and dissolution of poorly water-soluble etoricoxib. Polarised microscopy also proved valuable for rapid excipient screening. However, the study was limited by the narrow range of solubilizers tested. While Poloxamer 407 was selected for its availability and untapped potential, broader screening of advanced solubilizers could offer improved outcomes. CONCLUSION: The solubility increased from 99.08 to 296.8 μg/ml and the dissolution rose from 69.32% to 98.07%. These findings suggest that the kneading method and Poloxamer successfully produced amorphous solid dispersions of etoricoxib with significantly enhanced solubility and dissolution properties, potentially improving its bioavailability.
Optimization and Characterization of Tetrahydrocurcumin Loaded Niosome for Psoriasis Management.
Garg A, Chauhan CS, Deshmukh R … +1 more , Agrawal R
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 40873211 · Publisher ↗
INTRODUCTION: The low solubility and permeability of tetrahydrocurcumin act as a barrier in its therapeutic effectiveness, particularly in the topical treatment of skin diseases like psoriasis. METHODS: Niosomes were pre...
INTRODUCTION: The low solubility and permeability of tetrahydrocurcumin act as a barrier in its therapeutic effectiveness, particularly in the topical treatment of skin diseases like psoriasis. METHODS: Niosomes were prepared using thin-film hydration method using span 60, cholesterol as independent variables in Box Behnken design. Particle size, entrapment efficiency and drug loading were taken as dependent variables. In Box Behnken design the levels are -1, 0, and +1. The values for span 60 are 50, 75, and 100mg and for cholesterol 10, 20, and 30mg. RESULTS: The optimized formulation has a particle size of 116.9 nm, entrapment efficiency of 94.7% and, drug loading of 85.23%. The niosomes showed first-order release kinetics property and maintained stability at 4℃ and 25℃ for three months. The desirability score obtained was 0.896. DISCUSSION: The optimized niosomal formulation enhanced THC's solubility, permeability, and stability, supporting its potential for effective topical psoriasis treatment. Future studies will focus on in situ gel incorporation and in vivo validation. CONCLUSION: The developed formulation significantly improves the solubility and permeability of tetrahydrocurcumin which leads to improved therapeutic effectiveness in the formulation for the treatment of psoriasis. Further studies will incorporate these niosomes in in situ gels for the application.
Translational Horizons in Computer-Aided Drug Discovery: Bridging Insights with One Health Challenges.
Vlasiou MC
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 40755098 · Publisher ↗
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Exploring Anti-inflammatory Compounds from in High Cholesterol-induced Zebrafish Larvae: Revealing Cardiovascular Potential.
Ramalingam R, Venkatachalam K, Binesh A
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 40588997 · Publisher ↗
INTRODUCTION: The study investigated the anti-inflammatory properties of Kappaphycus alvarezii by employing zebrafish larvae as a model system. MATERIALS AND METHODS: The seaweed extract was subjected to phytochemical sc...
INTRODUCTION: The study investigated the anti-inflammatory properties of Kappaphycus alvarezii by employing zebrafish larvae as a model system. MATERIALS AND METHODS: The seaweed extract was subjected to phytochemical screening, uncovering the presence of alkaloids, terpenoids, proteins, and cardiac glycosides. UVvisible, FTIR, and GC-MS were employed to identify the presence of bioactive compounds. The western blotting method was used to confirm the target proteins. RESULTS: 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 highcholesterol 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. CONCLUSION: shows promise for developing natural sources for antiradicals, food supplements, nutraceuticals, and various functional foods with therapeutic applications.
Chronic Treatment with Angiotensin-(1-7) Improves Metabolism by Modulating Adipose Tissue and Oxidative Stress in Mice.
Paraiso AF, Sousa JN, Andrade JMO … +12 more , Santos EM, de Farias Lelis D, Da Costa CS, Graceli JB, Barbosa BK, Farias LC, de Paula AMB, Guimaraes ALS, Alves DT, Gollasch M, Santos RAS, Santos SHS
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 40574388 · Publisher ↗
BACKGROUND: 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 effe...
BACKGROUND: 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. AIM: This study aimed to assess the impact of chronic oral administration of Angiotensin-( 1-7) on adipose tissue modulation and metabolic processes in mice. METHODS: 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 bioinformatics analyses were conducted. RESULTS: 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. CONCLUSION: 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.
Novel Mouth Rinse Displaying Analgesic and Anti-inflammatory Properties: An Study.
Reddy SSP, Francis DL, Mondal S … +3 more , Rathi M, Katti N, Chopra SS
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 40511804 · Publisher ↗
INTRODUCTION: 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 propert...
INTRODUCTION: 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 cytotoxic and anti-inflammatory properties of a novel essential oil compound containing nanosilver using HaCaT and THP-1 human leukemia monocytic cell lines. MATERIALS AND METHODS: Neutral red uptake (NRU) assay was used to assess cytotoxicity 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 using ELISA, and COX-2 inhibition assay was performed. RESULTS: Cytotoxicity of the test compound was nearly absent. TNF-α levels decreased in positive control (2.81 pg/ml) and test samples (1.30 pg/ml) compared to control (22.04 pg/ml). COX-2 inhibition assay revealed test compound (0-20%) and positive control (0- 100%), with 25 μM celecoxib as a standard. IC for HaCaT cells was 0.6334% (positive control) and 0.6051% (test group). IC 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. DISCUSSION: This study showed the possibility of novel essential oils and nano-silvercontaining compounds as a medication material in preventing gingivitis. The cytotoxicity 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. CONCLUSION: 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.
Inclusive Drug Designing of Novel Indole Derivatives using Rationale, Pharmacophore Mapping and Molecular Docking.
Mehra A, Mittal A, Sharma R … +2 more , Sangwan R, Mehra A
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 40231509 · Publisher ↗
BACKGROUND: The presence of insufficient insulin signaling in type 2 diabetes arises due to either insulin resistance or impaired insulin secretion, ultimately leading to elevated blood glucose levels, a condition known...
BACKGROUND: The presence of insufficient insulin signaling in type 2 diabetes arises due to either insulin resistance or impaired insulin secretion, ultimately leading 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. Notably, 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. OBJECTIVES: 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. METHODS: 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 compounds. 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. RESULTS: 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 compounds 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 sensitization, and hepatotoxicity. RS43 is the most stable compound as it has high ΔE, η, and χ in DFT analysis. CONCLUSION: 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.
Metabolic Evaluation of a Novel Hydroxyfuranone Compound: Adiposity Reduction in Obese Mice by Increasing SIRT1 Gene Expression.
Silva Moraes D, Rodrigues Pereira S, Duque Esteves T … +9 more , Correia ACA, Dantas Guimaraes VH, Alves Pereira U, do Couto Tavares E, de Paula AMB, Jeane Aguiar C, Conceicao Farias L, Sena Guimaraes AL, Santos SHS
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 40017255 · Publisher ↗
BACKGROUND: 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. OBJECTIVES: The pr...
BACKGROUND: 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. OBJECTIVES: The present study aimed to synthesize a novel molecule containing the moieties hydroxybutenolide and sulfonamide [3-chloro-4-(p-chlorophenylsulfonylamino)-5- hydroxyfuran-2(5H)-one] (FS) and evaluate its metabolic effects in an obese mice model with metabolic syndrome. METHODS: 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 hydroxybutenolide (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, highdensity lipoprotein cholesterol, triacylglycerol, histological analyses, and gene expression by RT-PCR for the adipose tissue genes SIRT1, SIRT3, SIRT5, and NFKβ, were evaluated. RESULTS: 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. CONCLUSION: Treatment with FS 3-chloro-4-(p-chlorophenylsulfonylamino)-5-hydroxyfuran- 2(5H)-one improved metabolic profile and increased the SIRT1 expression.
Evaluation of the Synergistic Anti-inflammatory Activities of the Combined Hydroalcoholic Extracts from L. and L.
Zatla AT, Hammoudi A, Dib MEA … +1 more , Perard J
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 39976097 · Publisher ↗
BACKGROUND: Chronic inflammatory diseases are rising, driving the search for effective natural treatments. L. and Pimpinella anisum L. (anise) exhibit notable anti-inflammatory properties individually, but their combine...
BACKGROUND: Chronic inflammatory diseases are rising, driving the search for effective natural treatments. 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. INTRODUCTION: The rise in chronic inflammatory diseases has increased interest in natural anti-inflammatory treatments. L. and Pimpinella anisum L. are wellknown 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 antiinflammatory activity of hydroalcoholic extracts from these plants, aiming to offer an effective natural therapeutic alternative. METHODS: Hydroalcoholic extracts were prepared by maceration of both plants. Anti-inflammatory activity was assessed using the protein denaturation method with Diclofenac as a standard. RESULTS: Phytochemical analysis identified flavonoids, alkaloids, tannins, glycosides, and polyphenols in , 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%). CONCLUSION: The combination of and extracts significantly enhanced anti-inflammatory activity compared to individual extracts, underscoring their potential as natural therapeutic alternatives to conventional treatments.
Leveraging Underutilized Sri Lankan Fruits in the Fight against Autoimmune Disorders.
Virajini MPT, Bandara MD, Jayasooriya PT … +2 more , Samarakoon KW, Kuruppu AI
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 39835566 · Publisher ↗
The potential of underutilized plant species to improve food security, health, economic output, and the environment has not been fully realized. Sri Lanka an island on the Indian Ocean is home to numerous plant species w...
The potential of underutilized plant species to improve food security, health, economic 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, including many underutilized plants that could help meet the growing demand for food, energy, 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 managing immune related conditions. This review will explore underutilized fruit crops from Sri Lanka that could be used against inflammation, including autoimmune diseases.
Toxicity and Anti-inflammatory Effects of (Miller) Urb, Ethanolic Extract, in Zebrafish .
Ferreira DP, Holanda FH, Borges SF … +7 more , da S Ramos R, Shinkai VMT, de Souza GC, Carvalho JCT, Pimenta RS, do Nascimento JLM, Ferreira IM
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 39757604 · Publisher ↗
INTRODUCTION: Eleutherine bulbosa (Miller) Urb, popularly known as "marupazinho", is frequently used in traditional medicine for treating various diseases, including hypertension, ulcers, constipation, and intestinal inf...
INTRODUCTION: Eleutherine bulbosa (Miller) Urb, popularly known as "marupazinho", 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. METHODS: 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. RESULTS: 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. CONCLUSION: Molecular docking studies revealed that the eleutherol molecule isolated from E. bulbosa has a dual inhibition profile against cyclooxygenase-1 and 2.
Formulation, Characterization and Cytotoxic Effect of Indomethacin-loaded Nanoparticles.
Yalcınkaya K, Senel B, Akyıl E
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 39757603 · Full text
BACKGROUND: 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 treatmen...
BACKGROUND: 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. OBJECTIVES: 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). METHODS: 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 Dynasan116 (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 H NMR; cumulative drug release rates were assessed using HPLC and cytotoxicities were examined by the MTT assay. RESULTS: 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. CONCLUSION: 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.
Antioxidant and Analgesics and Anti-inflammatory Activity of Leaf Extract in Rats.
Vyas A, Gupta R, Jatav R
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 39681830 · Publisher ↗
OBJECTIVES: This study assessed the In-vitro Antioxidant and In-vivo Analgesics and Anti-inflammatory Activity of Leaf Extract in Rats. INTRODUCTION: Diverse pharmacological applications of plants from the Apocynaceae f...
OBJECTIVES: This study assessed the In-vitro Antioxidant and In-vivo Analgesics and Anti-inflammatory Activity of Leaf Extract in Rats. INTRODUCTION: Diverse pharmacological applications of plants from the Apocynaceae family are reported in the literature. ; an ornamental species belonging to the Apocynaceae family, is characterized by diverse biological activities, i.e. antioxidant, cytotoxic, thrombolytic, membrane-stabilizing, antimicrobial, and anti-proliferative effects. This species represents a perennial flora that thrives in tropical and subtropical climates. MATERIALS AND METHODS: Ultrasonication-assisted method used for plant extraction. The extracts were subjected to phytochemical screening tests, followed by total phenolic content analysis, using gallic acid as a standard. The antioxidant activity was examined by DPPH scavenging and FRAP assays. The acetic acid-induced writhing test, tail flick, and Hot plate method were used for the determination of analgesic activity. Anti-inflammatory activity by following carrageenan-induced paw edema. RESULTS: ABLE treatments show analgesic effectiveness against the acid-induced pain source, tail flick, and hot plate methods at different doses of ABLE 400,200,100 mg/kg results showed respectively- 55.32, 38.67, and 22.85 (% inhibition), 89.47%, 62.57 %, 49.57%, and 100%, 92.40%, 65.33% response after 180 min of drug administration. ABLE 400 and 200 mg/kg exhibit effective results (1.43± 0.005 and 1.50± 0.008) against carrageenan- induced intoxication. DISCUSSION: The fundamental components of antioxidants that can aid in the reduction of free radicals include phenol, flavonoids, and polyphenols. Applying DPPH and FRAP, ABLE exhibits remarkable antioxidant activity. When it comes to both centrally and peripherally acting analgesics, ABLE exhibits highly effective activity. Methanolic ABLE had a noticeable impact on paw edema caused by carrageenan. Antioxidants, alkaloids, and glycosides were present in methanolic ABLE, which allowed it to efficiently combat inflammatory mediators and the cause of pain. CONCLUSION: Ultrasonic assistance is beneficial in isolating active metabolites in plants, with phenolic compounds exhibiting antioxidant activity. ABLE, a plant with 55% squalene, effectively combats inflammatory mediators and pain. Further investigation is needed to identify biomarkers in the plant.
Discovery and Chemical Exploration of Spiro[Benzofuran-3,3'-Pyrroles] Derivatives as Innovative FLT3 Inhibitors for Targeting Acute Myeloid Leukemia.
Al-Mahadeen MM, Jaber AM, Zahra JA … +3 more , Al-Najjar BO, El-Abadelah MM, Khanfar MA
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 39648426 · Publisher ↗
AIMS: This study aimed at the synthesis of several spiro[benzofuran-3,3'-pyrroles] derivatives by a three-component reaction conducted by mixing DMAD, -bridgehead heterocycles, and benzofuran-2,3-diones in dichloromethan...
AIMS: This study aimed at the synthesis of several spiro[benzofuran-3,3'-pyrroles] derivatives by a three-component reaction conducted by mixing DMAD, -bridgehead heterocycles, and benzofuran-2,3-diones in dichloromethane at room temperature for 24 h. Moreover, evaluation of their cytotoxicity affinities against FMS-like tyrosine kinase 3 was carried out. OBJECTIVES: 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. METHODS: 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, -bridgehead heterocycles and benzofuran-2,3-diones in dichloromethane at room temperature for 24 h. The compounds were analyzed using NMR H, C, 2D-NMR (COSY, HMQC, HMBC), and HRMS. Docking simulations were conducted to elucidate the anticancer activity of synthesized compounds on FLT3 protein, with Gilteritinib as a reference for comparison. RESULTS: 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 (IC = 2.5 μM). CONCLUSION: Fifteen new synthetic spiro[benzofuran-3,3'-pyrroles] were prepared, characterized, and evaluated for cytotoxicity affinities against FMS-like tyrosine kinase 3. Compound 12e showed strong binding affinity and potent inhibitory activity (IC = 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[benzofuran-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.
Genistein Enhances the Beneficial Effects of Exercise on Antioxidant and Anti-inflammatory Balance and Cardiomyopathy in Ovariectomized Diabetic Rats.
Mohammadi M, Salehi AM, Azadi SM … +3 more , Khajvand-Abedini M, Nazari-Serenjeh F, Habibi P
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 39482917 · Publisher ↗
AIMS: 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. BACKGROUND: It is wel...
AIMS: 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. BACKGROUND: 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. OBJECTIVES: 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. METHODS: 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. RESULTS: 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. CONCLUSION: Genistein or/and exercise as a natural replacement therapy could improve diabeticinduced cardiac complications in ovariectomized rats' hearts.
A Review on Phytochemical Constituents used as Current Treatment Strategies for Neurodegenerative Disease.
Jee K, Gaur R, Kadian JP … +5 more , Meenu K, Murtaza M, Verma SK, Malik B, Shilpa K
Antiinflamm Antiallergy Agents Med Chem · 2025 · PMID 39415572 · Publisher ↗
In today's time, a diversity of neurodegenerative diseases that widely affect the CNS causing insufficiency in particular brain processes such as memory, mobility, and cognition due to the moderate loss of CNS neurons. T...
In today's time, a diversity of neurodegenerative diseases that widely affect the CNS causing insufficiency in particular brain processes such as memory, mobility, and cognition due to the moderate loss of CNS neurons. This review emphasizes different phytochemical constituents used widely for the prevention or treatment of various neurodegenerative diseases such as Alzheimer's disease (AD) and Parkinson's disease (PD). Berberin (BBR), which is an isoquinoline class of alkaloid and isolated from the plant and , has both acetylcholine esterase (AChE) inhibiting properties as well as monoamine oxidase (MAO) inhibiting properties involved in the betterment of AD by decreasing the production of reactive oxygen species (ROS). Like BBR, Physostigmine, isolated from the / and belongs to the family Leguminosae, and Morphine, isolated from the plant , also has a significant impact on the management and treatment of AD and PD by reducing both neuroinflammation and pro-inflammatory cytokines production. Morphine bineurodegenerative diseases with μ-opioid receptor (MOR) in CNS elevate GABA levels in the synaptic cleft of the brain and reduces the neurotoxicity via stimulation of MOR. It has been discovered that physostigmine improves cognitive function in AD patients and reduces α-synuclein expression in PD neural cell lines. Isorhyncophylline (IRN) is a Chinese herbal medicine isolated from the plant Uncaria rhyncophylla which provides neuroprotective efficiency against neurotoxicity that occurs by amyloid β (the main component of amyloid plaques) found in the brain of people with AD.
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