Current Research in Pharmacology and Drug Discovery最新文献

{"title":"Optimizing ibrutinib bioavailability: Formulation and assessment of hydroxypropyl-β-cyclodextrin-based nanosponge delivery systems","authors":"Sunitha Sampathi ,&nbsp;Nitiraj Kulkarni ,&nbsp;D.V.R.N. Bhikshapathi ,&nbsp;Jagadish V. Tawade ,&nbsp;Nainaru Tarakaramu ,&nbsp;Rzgar Farooq Rashid ,&nbsp;Aziz Kubaev","doi":"10.1016/j.crphar.2025.100213","DOIUrl":"10.1016/j.crphar.2025.100213","url":null,"abstract":"<div><h3>Background</h3><div>The current research aims to improve the oral bioavailability of ibrutinib (IBR), a class II drug with low solubility, through the formulation of nanosponges (NSPs) that incorporate IBR, utilizing Hydroxypropyl β-cyclodextrin (HPβCD) and 1,1′-carbonyldiimidazole (CDI) as cross-linking agent.</div></div><div><h3>Methods</h3><div>IBR-loaded HPβCD-NSPs were formulated by optimizing the molar proportion of HPβCD to CDI, as well as stirring rate and duration using a design-based methodology. The synthesized nanoparticles (NSPs) were examined for size, potential, and entrapment of drug. Characterization was performed by X-ray diffraction analysis, Fourier Transform Infrared Spectroscopy (FT-IR), and Differential Scanning Calorimetry (DSC), to assess compatibility. Permeability studies were conducted, followed by in vitro and in vivo assessments.</div></div><div><h3>Results</h3><div>The optimized IBR-loaded HPβCD NSPs demonstrated a mean particle size of 145.6 ± 6.8 nm, a PDI of 0.170 ± 0.036, and an EE of 71.04 ± 2.40%. Further validation through zeta sizing, microscopic and spectral analysis, release studies, and pharmacokinetic assessments confirmed the optimization. The HPβCD NSPs demonstrated 14.96 times higher AUC0-t (area under the curve) with a Cmax increase of 6.45 times compared to the free drug, indicating a substantial improvement in bioavailability.</div></div><div><h3>Conclusion</h3><div>IBR-loaded HPβCD NSPs offer a promising strategy for improved drug release and bioavailability, which could significantly benefit melanoma treatment.</div></div>","PeriodicalId":10877,"journal":{"name":"Current Research in Pharmacology and Drug Discovery","volume":"8 ","pages":"Article 100213"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143180668","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Exploring the role of sex in asthma and COPD pharmacological treatment","authors":"Luigino Calzetta ,&nbsp;Shima Gholamalishahi ,&nbsp;Elena Pistocchini ,&nbsp;Bartolomeo Zerillo ,&nbsp;Maria Gabriella Matera ,&nbsp;Paola Rogliani","doi":"10.1016/j.crphar.2025.100234","DOIUrl":"10.1016/j.crphar.2025.100234","url":null,"abstract":"<div><div>Sex is a fundamental determinant in pharmacology, influencing disease prevalence, severity, and therapeutic responses. Differences in pharmacokinetics and pharmacodynamics between men and women contribute to variations in drug efficacy and safety profiles. While sex refers to biological and physiological characteristics, gender encompasses social and behavioral factors. Despite their distinct meanings, these terms are often used interchangeably in medical research, potentially leading to misinterpretations. Historically, female and intersex individuals have been underrepresented in clinical studies, resulting in biased treatment approaches. Acknowledging these disparities, researchers now emphasize the importance of sex-specific differences to enhance therapeutic outcomes.</div><div>This review explores the impact of sex on the pharmacological treatment of chronic obstructive respiratory diseases, particularly asthma and chronic obstructive pulmonary disease (COPD).</div><div>Asthma is more prevalent in women, whereas COPD severity is rising among female patients. Sex influences the response to bronchodilators, inhaled corticosteroids (ICS), and combination therapies. Studies suggest that men exhibit a greater response to β₂-adrenoceptor agonists and sex differences in muscarinic acetylcholine receptor (mAChR) expression may influence bronchodilator response to muscarinic antagonists. Moreover, women display stronger immune responses and higher corticosteroid receptor expression, potentially modulating the efficacy of ICS. Women are also more likely to experience adverse drug reactions and face challenges in correct inhaler device use, impacting treatment adherence and clinical outcomes. Despite these differences between men and women, sex-specific approaches remain insufficiently integrated into clinical practice. Addressing sex disparities in pharmacotherapy is crucial to optimize treatment strategies. Further research is needed to elucidate sex-related differences and incorporate them into evidence-based guidelines for asthma and COPD management.</div></div>","PeriodicalId":10877,"journal":{"name":"Current Research in Pharmacology and Drug Discovery","volume":"9 ","pages":"Article 100234"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145094964","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":"Real-world clinical utility (effectiveness) of omalizumab as add-on therapy in patient with difficult-to-treat severe allergic asthma","authors":"Rowshne Jahan,&nbsp;Ziaul Huq","doi":"10.1016/j.crphar.2025.100218","DOIUrl":"10.1016/j.crphar.2025.100218","url":null,"abstract":"<div><h3>Background</h3><div>Severe allergic asthma (SAA) requires high-dose inhaled corticosteroids and additional medications. It poses a substantial health and financial burden. Omalizumab, an antibody that targets IgE, has improved symptoms and quality of life in severe allergic asthma (SAA) patients. Its impact in Bangladeshi patients is unknown, and this study aimed to evaluate its effectiveness in improving lung function in severe allergic asthma (SAA) patients.</div></div><div><h3>Methods</h3><div>This single-centre, real-world study aimed to assess omalizumab's effectiveness in 131 Bangladeshi patients with SAA. Information regarding demographics, BMI, and IgE levels, were collected from patients &gt;12 years with poorly controlled SAA before and 3 months after omalizumab treatment. Pulmonary function tests (PFTs), including Forced Vital Capacity (FVC), Forced Expiratory Volume in 1 s (FEV1 %), FEV1/FVC (%), and Fractional Exhaled Nitric Oxide (FeNO), were performed according to established guidelines. A structured questionnaire was used for data collection. Ethical measures were taken in accordance with the current Declaration of Helsinki.</div></div><div><h3>Results</h3><div>The mean age of study population was 42.7 ± 16.15 (SD) years with majority being female (67.9 %). The mean BMI and IgE level was 28 ± 5.37 kg/m² and 594.3 ± 679.9 IU/mL respectively. The mean baseline FVC, FEV₁ and FEV₁/FVC ratio was 63.5 % ± 19.2, 61.3 % ± 21.8 and 80.4 % ± 12.6 respectively. The mean post-omalizumab FVC, FEV₁ and FEV₁/FVC ratio was 72.5 % ± 25.6, 68.3 % ± 28.2 and 79.1 % ± 13.8 respectively. The FeNO reading revealed that number of patients with &lt;25 ppb reading increased post omalizumab treatment (70.2 % vs 84 %).FEV₁ expressed was significantly higher in patients post-omalizumab treatment than at the baseline (p = 0.019) and percentage of patients with FEV₁ below the predicted 50 % was higher at baseline compared to after omalizumab treatment (31.3 % vs 23.7 %). Similarly, the FVC was significantly higher post-omalizumab treatment compared to baseline (p = 0.001). The FEV₁/FVC ratio was not significantly different post omalizumab treatment (p = 0.758).</div></div><div><h3>Conclusion</h3><div>Our study finding have suggested that omalizumab as add on therapy achieved an adequate asthma control in patients with severe allergic asthma.</div></div>","PeriodicalId":10877,"journal":{"name":"Current Research in Pharmacology and Drug Discovery","volume":"8 ","pages":"Article 100218"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143824426","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":"Probing into the chemopreventive properties of synthetic 1,3,6-tri-O-galloyl-α-D-glucose (α-TGG) against glioblastoma and triple-negative breast cancer-derived cell models","authors":"Carolane Veilleux ,&nbsp;Jihane Khalifa ,&nbsp;Alain Zgheib ,&nbsp;Angélique Sabaoth Konan ,&nbsp;Roger Gaudreault ,&nbsp;Borhane Annabi","doi":"10.1016/j.crphar.2025.100219","DOIUrl":"10.1016/j.crphar.2025.100219","url":null,"abstract":"<div><div>Inflammation plays a significant role in cancer progression. Chemopreventive strategies against cellular response to pro-inflammatory cues may therefore contribute to inhibit the acquisition of an invasive phenotype. 1,3,6-Tri-O-Galloyl-β-D-Glucose (β-TGG) is a type of gallotannin naturally found in plants like <em>Paeonia lactiflora</em> and <em>Terminalia chebula.</em> Unfortunately, the overall yields of β-TGG extraction require complex purification protocols from plant sources and are relatively low. Here, a new synthetic α-anomer of TGG (α-TGG) was characterized for anti-inflammatory and anticancer biological properties. <em>In vitro</em> pro-inflammatory and epithelial-to-mesenchymal transition (EMT) cues, triggered by phorbol 12-myristate 13-acetate (PMA), concanavalin A (ConA), tumor necrosis factor (TNF) α, and transforming growth factor (TGF) β, were used to screen α-TGG in two highly aggressive human cancer cell models, namely the U87 glioblastoma and the MDA-MB-231 triple-negative breast cancer (TNBC)-derived cells. α-TGG dose-dependently inhibited ConA-mediated activation of the latent matrix metalloproteinase pro-MMP-2 into its active MMP-2 form as well as the ConA- and PMA-mediated cyclooxygenase (COX)-2 expression, two biomarkers of inflammation, in U87 cells. In MDA-MB-231, α-TGG inhibited PMA- and TNFα-mediated induction of pro-MMP-9, a marker of inflammation and invasive phenotype. Finally, in both cell lines, α-TGG further inhibited TGFβ-induced chemotaxis, as well as TGFβ-induced Smad2 phosphorylation and Snail expression, crucial upstream signaling pathway and downstream biomarkers associated with EMT. Collectively, we confirm that α-TGG retained potent anti-inflammatory and anti-invasive pharmacological properties which support its chemopreventive potential.</div></div>","PeriodicalId":10877,"journal":{"name":"Current Research in Pharmacology and Drug Discovery","volume":"8 ","pages":"Article 100219"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143784989","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Unveiling the mechanisms of synthetic compounds against Candida auris: An integrative review","authors":"Yamini Saini ,&nbsp;Zeeshan Fatima ,&nbsp;Muriel Billamboz ,&nbsp;Saif Hameed","doi":"10.1016/j.crphar.2025.100231","DOIUrl":"10.1016/j.crphar.2025.100231","url":null,"abstract":"<div><div>The multidrug-resistant fungal species <em>Candida auris</em> has drawn attention from across the world due to its capacity to elude traditional therapies and flourish in medical environments. Its resilience, which includes biofilm development and efflux-mediated drug resistance, highlighted the need for novel antifungal approaches. Despite advancements in antifungal therapeutics, the rising prevalence of resistance and limited antifungal arsenal demand ongoing research into novel and more effective treatments. To tackle this rising issue, the available literature suggests several approaches. Among those, the use of synthetic compounds (SCs) appears as first-line option. However, to prove the efficacy of these SCs against <em>C. auris</em> a complete coverage is still elusive in a single study. Thus, in this integrative review, we aimed to summarize the anti-<em>C. auris</em> SCs that are reported in literature. About 47 articles were included in this review using predefined selection criteria. Data were extracted for detailed reviews from PubMed, Google scholar and Science direct. All the included studies tested antifungal activities of the SCs and evaluated their mode of actions. These data highlighted diverse modes of action such as perturbation of biofilm formation, disruption of cell wall and organelles, inhibition of efflux and generation of reactive oxygen species to name few. Taken together, SCs represent viable candidates for effective antifungal treatment. The information gathered in the present study emphasizes the need for further investigations, including preclinical studies and clinical trials, to evaluate the therapeutic potential of these agents against <em>C. auris</em>.</div></div>","PeriodicalId":10877,"journal":{"name":"Current Research in Pharmacology and Drug Discovery","volume":"9 ","pages":"Article 100231"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144988058","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":"Advancing organ-on-chip systems: the role of microfluidics in neuro-cardiac research","authors":"Maria João Ferreira ,&nbsp;Sarah Colombani ,&nbsp;Albin Bernardin ,&nbsp;Alain Lacampagne ,&nbsp;Jean-Luc Pasquié ,&nbsp;Pedro F. Costa ,&nbsp;Benoit Charlot ,&nbsp;Albano C. Meli","doi":"10.1016/j.crphar.2025.100227","DOIUrl":"10.1016/j.crphar.2025.100227","url":null,"abstract":"<div><div>The neuro-cardiac junction is involved in many pathological conditions in humans, but no model currently allows translational studies to investigate its role. Animal models fail to accurately represent this interaction. This review explores the role of microfluidic technologies in advancing organ-on-chip systems that simulate neuro-cardiac interactions in a controlled environment. By offering precise control over cellular environments, microfluidic platforms significantly enhance the modeling of dynamic cardiac-neural cell interactions. These systems allow the development of more accurate and functional neuro-cardiac junctions, vital for investigating cardiovascular diseases and the neuronal impact in these pathologies. While traditional animal models and co-culture techniques have their merits, they are limited in replicating human-specific physiology. Recent innovations in microfluidics, in combination with human-induced pluripotent stem cell technology, provide more physiologically relevant models and address ethical concerns regarding animal use. This review emphasizes the potential of these advanced microfluidic models in improving disease modeling, drug screening, and therapeutic strategies, ultimately advancing personalized medicine.</div></div>","PeriodicalId":10877,"journal":{"name":"Current Research in Pharmacology and Drug Discovery","volume":"9 ","pages":"Article 100227"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144572190","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The simultaneous activation of μ- and δ-opioid receptors by (−)-2S-LP2 rescues allodynia with the contribution of TGF-β1 signaling in a rat chronic constriction injury model","authors":"Fidilio A. ,&nbsp;Grasso M. ,&nbsp;Spoto S. ,&nbsp;Varrasi S. ,&nbsp;Al-Khrasani M. ,&nbsp;Caraci F. ,&nbsp;Parenti C. ,&nbsp;Pasquinucci L.","doi":"10.1016/j.crphar.2025.100229","DOIUrl":"10.1016/j.crphar.2025.100229","url":null,"abstract":"<div><div>In neuropathic pain (NP), a dysregulation of glial functions in the central and peripheral nervous systems has been described, and the balance between pro-inflammatory and anti-inflammatory mediators is lost in the transition from acute to chronic pain. This raises the possibility to resolve pain via the induction of anti-inflammatory cytokines that have a protective role against neuroinflammatory events. Transforming growth factor-β1 (TGF-β1), an anti‐inflammatory cytokine is able to counteract the development of chronic NP. Given the correlation between opioid agonists and TGF-β1 pathway, here we describe the pharmacological profile of the dual-target μ-opioid receptor (MOR)/δ-opioid receptor (DOR) agonist (−)-2<em>S</em>-LP2. (−)-2<em>S</em>-LP2, given intraperitoneally at a dose of 0.7 mg/kg, significantly mitigated mechanical allodynia induced by chronic constriction injury in rats. This antiallodynic effect was sensitive to subcutaneous (s.c.) injection of either the MOR-selective antagonist naloxonazine (NLX, 10 mg/kg) or the DOR-selective antagonist naltrindole (NTD, 3 mg/kg), alone or when combined, demonstrating that (−)-2<em>S</em>-LP2 interacted simultaneously with both MOR and DOR. At mRNA or protein level, a positive effect on TGF-β1 and its receptor TGFβ-R2 expression were found and (−)-2<em>S</em>-LP2 also modulated the expression of spinal TGF-β1 pathway via co‐targeting MOR/DOR. Thus, the dual‐target profile of the MOR/DOR agonist (−)-2<em>S</em>-LP2 exerts its analgesic efficacy by rescue of TGF-β1 and could represent a novel pharmacological tool able to increase anti-inflammatory cytokines in pain conditions such as NP associated with an imbalance between inflammatory and anti-inflammatory cytokines.</div></div>","PeriodicalId":10877,"journal":{"name":"Current Research in Pharmacology and Drug Discovery","volume":"9 ","pages":"Article 100229"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144890365","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":"Gallic acid serves as an effective therapeutic agent of inflammatory bowel disease: Pharmacological impacts on tight junction-dependent intestinal permeability in vivo and its related intracellular signaling","authors":"Apiwan Arinno ,&nbsp;Pichayapa Sukmak ,&nbsp;Purisha Kulworasreth ,&nbsp;Thaniya Sricharunrat ,&nbsp;Chutima S. Vaddhanaphuti ,&nbsp;Pawin Pongkorpsakol","doi":"10.1016/j.crphar.2025.100223","DOIUrl":"10.1016/j.crphar.2025.100223","url":null,"abstract":"<div><div>Intestinal tight junction disruption contributes to the pathogenesis of inflammatory bowel diseases (IBD). We have recently reported that gallic acid was able to enhance intestinal tight junction assembly via CaMKK-β/AMPK/SIRT-1/ERK-dependent mechanisms with unknown possible therapeutic applications in IBD. The main aims of this study are to investigate the <em>in vivo</em> effects of gallic acid in experimental colitis mice and to search for feasible mechanisms of action. Here, we found that gallic acid attenuated weight loss, reduced disease activity index, and reversed colon length shortening in DSS-induced colitis mice. Importantly, gallic acid also significantly increased survival rates of DSS-induced colitis mice. Based on histopathological analyses, gallic acid diminished immune cell infiltration and neutrophil activity in colitis tissues. Of particular interest, gallic acid significantly reduced gene expressions of proinflammatory cytokines, including TNF, IFN-γ, IL-1β, IL-6, and IL-8. In addition, gallic acid suppressed MLCK gene transcription and protein expression in DSS-induced colitis mice. Furthermore, gallic acid also enhanced the expression of tight junction proteins, including ZO-1 and occludin. Consistently, gallic acid reduced tight junction-dependent leak pathway permeability and was shown to increase SIRT-1 activity, AMPK, and ERK phosphorylation in colon tissues of DSS-induced colitis mice. This study not only explores anti-colitogenic impacts of gallic acid, but also sheds some light on the mechanisms of its action. According to our findings, gallic acid may be useful as an anti-colitogenic nutraceutical.</div></div>","PeriodicalId":10877,"journal":{"name":"Current Research in Pharmacology and Drug Discovery","volume":"8 ","pages":"Article 100223"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144099671","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":"Expression of concern regarding the article titled “Variability in the serum and tissue concentrations of pre-incisional ceftriaxone for surgery in paediatric population and outcome of surgical-site infections; An open labelled, prospective, non-randomized, analytical study”","authors":"Luigino Calzetta","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":10877,"journal":{"name":"Current Research in Pharmacology and Drug Discovery","volume":"8 ","pages":"Article 100211"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143181615","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Carnosine modulates Aβ-induced transcriptional aberrations in murine microglial cells","authors":"Veronica Rivi ,&nbsp;Giuseppe Carota ,&nbsp;Fabio Tascedda ,&nbsp;Johanna M.C. Blom ,&nbsp;Filippo Caraci ,&nbsp;Cristina Benatti ,&nbsp;Giuseppe Caruso","doi":"10.1016/j.crphar.2025.100221","DOIUrl":"10.1016/j.crphar.2025.100221","url":null,"abstract":"<div><div>Carnosine (β-alanyl-L-histidine) is an endogenous dipeptide known for its anti-inflammatory and antioxidant effects, making it a promising agent for neurodegenerative diseases like Alzheimer's disease (AD). Carnosine has shown protective effects against amyloid beta (Aβ)-induced oxidative stress and inflammation in murine microglial cells, yet its full immunomodulatory impact on these cells, particularly in terms of transcriptional regulation and cytokine interplay, remains underexplored. This study examined carnosine's effects on immune response markers in BV-2 cells exposed to Aβ oligomers. Specifically, gene expression changes in anti-inflammatory mediators (CXCL2 and IL-10) and phagocytic markers (CD11b, CD68, TNFα, IL-1β) were assessed. Notably, carnosine increased CXCL2 and IL-10 expression, promoting an anti-inflammatory response and enhancing microglial phagocytosis. Additionally, carnosine restored CX3CR1 expression, a receptor implicated in Aβ- effects in murine macrophages, and upregulated TGF-β1 and its receptor, supporting its neuroprotective role. These results underscore carnosine's potential to modulate immune responses, enhance microglial activity, and provide neuroprotection in Aβ-induced conditions. The findings highlight carnosine's therapeutic promise for AD treatment, offering a pathway for future research on its use in neurodegenerative disease interventions.</div></div>","PeriodicalId":10877,"journal":{"name":"Current Research in Pharmacology and Drug Discovery","volume":"8 ","pages":"Article 100221"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143943643","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}