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

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.

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.

Method: 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 in vitro 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.

Result: 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.

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.

Method: 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.

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. UV-visible, FTIR, and GC-MS were employed to identify the presence of bioactive compounds. The western blotting method was used to confirm the target proteins.

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 high-cholesterol diet (HCD), the activities of antioxidant enzymes (SOD, CAT, GPx, and GST) were elevated, and K. alvarezii treatment successfully reversed this effect. Additionally, the HCD group exhibited upregulation in the protein expression of MMP-9, MMP-13, MPO, IL-6, TNFα, and NFκB due to inflammation, whereas K. alvarezii therapy reversed the inflammatory process in the treated group. These findings indicate the potential of K. alvarezii to counteract inflammatory responses induced by a high-cholesterol diet through modulation of antioxidant enzyme activities and downregulation of pro-inflammatory markers.

Conclusion: Kappaphycus alvarezii shows promise for developing natural sources for antiradicals, food supplements, nutraceuticals, and various functional foods with therapeutic applications.

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 in silico 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.

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 cy-totoxic and anti-inflammatory properties of a novel essential oil compound contain-ing nanosilver using HaCaT and THP-1 human leukemia monocytic cell lines.

Materials and methods: Neutral red uptake (NRU) assay was used to assess cyto-toxicity and ELISA to evaluate the inflammatory cytokines. The test compound was compared to 0.12% chlorhexidine gluconate (CHX). Cytotoxicity was determined in HaCaT and THP-1 cell lines using NRU assay. TNF-α expression was measured us-ing ELISA, and COX-2 inhibition assay was performed.

Results: Cytotoxicity of the test compound was nearly absent. TNF-α levels de-creased in positive control (2.81pg/ml) and test samples (1.30 pg/ml) compared to control (22.04pg/ml). COX-2 inhibition assay revealed test compound (0-20%) and positive control (0-100%), with 25 μM celecoxib as a standard. IC50 for HaCaT cells was 0.6334% (positive control) and 0.6051% (test group). IC50 using THP-1 cells was not converged for the test and 424.6% for positive control. IC-50 for COX-2 inhibition was 1.469% in the test and 8.801% in the positive control.

Discussion: This study showed the possibility of novel essential oils and nano-sil-ver-containing compounds as a medication material in preventing gingivitis. The cy-totoxicity was negligible, while the level of TNF- α was much decreased, and COX-2 activity assays indicated its efficiency in anti-inflammatory properties. The results encourage the therapeutic potential of the compound for periodontitis, and further studies are required to demonstrate therapeutic efficiency and safety.

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.

Background: Chronic inflammatory diseases are rising, driving the search for effective natural treatments. Mentha pulegium L. and Pimpinella anisum L. (anise) exhibit notable anti-inflammatory properties individually, but their combined effects are less studied. This research evaluates the in vitro synergistic anti-inflammatory activities of their hydroalcoholic extracts. Phytochemical analysis confirmed the presence of flavonoids, tannins, and polyphenols in both extracts. Individually, they demonstrated significant activity (78.5% and 72.3%, respectively, at 10 g/L) compared to Diclofenac (62.3%). Their combination achieved 88.6% inhibition at the same concentration. These findings highlight their potential as natural anti-inflammatory agents.

Introduction: The rise in chronic inflammatory diseases has increased interest in natural anti-inflammatory treatments. Mentha pulegium 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 Mentha pulegium, with an absence of saponins. Pimpinella anisum contained flavonoids, tannins, heterosides, and polyphenols. The extracts exhibited strong anti-inflammatory activity individually (78.5% and 72.3%, respectively, at 10 g/L) and even higher inhibition (88.6%) when combined, surpassing Diclofenac (62.3%).

Conclusion: The combination of Mentha pulegium and Pimpinella anisum extracts significantly enhanced anti-inflammatory activity compared to individual extracts, underscoring their potential as natural therapeutic alternatives to conventional treatments.

Plant-based repellents have been used for generations as personal protection against mosquitoes. Ethnobotanical studies provide valuable knowledge for developing natural products. Commercial repellents with plant-based ingredients are popular, but insufficient studies follow Pesticide Evaluation Scheme WHO guidelines. Further standardized studies are needed to evaluate repellent compounds and develop high-repellency and safe products. Essential Oils (EOs) from aromatic plants have gained popularity as low-risk insecticides due to their low toxicity and short environmental persistence. These plant-derived EOs, produced through steam distillation, have repellent, insecticidal, and growth-reducing effects on various insects. They control phytophagous insects, bite flies, and home and garden insects. US registration is the main hurdle for new EOs. This review explores the use of essential oils from plants as a natural repellent, focusing on their effectiveness and synergistic effects. Essential oils are volatile mixtures of hydrocarbons with diverse functional groups, and their effectiveness is linked to monoterpenes and sesquiterpenes. Synergistic effects can improve their effectiveness, and the use of other natural products, like vanillin, can increase protection time. Cymbopogon spp., Ocimum spp., and Eucalyptus spp. are among the most promising plant families.

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 Dynasan^®116 (DYN) was used as the solid lipid for SLN. Prepared formulations were characterized for Particle Size (PS), Polydispersity Index (PDI), Zeta Potential (ZP), Encapsulation Efficiency (%EE), and drug-excipient compatibility using DSC, FT-IR, and ¹H NMR; cumulative drug release rates were assessed using HPLC and in vitro 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.