Pharmaceuticals最新文献

{"title":"Investigating the Mechanism of Yiqi Huoxue Jieyu Granules Against Ischemic Stroke Through Network Pharmacology, Molecular Docking and Experimental Verification.","authors":"Ying Chen, Huifen Zhou, Ting Zhang, Haitong Wan","doi":"10.3390/ph18091332","DOIUrl":"10.3390/ph18091332","url":null,"abstract":"<p><p><b>Background:</b> Ischemic stroke (IS) is a significant cause of global mortality and disability. Yiqi Huoxue Jieyu granules (YHJGs) show therapeutic potential for IS, but their mechanisms remain unclear. This study investigated YHJGs' effects through network pharmacology, molecular docking, and experimental validation. <b>Methods:</b> Active YHJG components and IS targets were identified from TCMSP, GeneCards, and DisGeNET databases. Network analysis and molecular docking (AutoDock Vina) were performed. In vivo studies used 72 male Sprague-Dawley rats (MCAO model) divided into sham, model, nimodipine (10.8 mg/kg), and three YHJG dose groups (0.72, 1.44, 2.88 g/kg). Assessments included neurological scores, TTC staining, histopathology, and molecular analyses (qPCR/Western blot). <b>Results:</b> Network analysis identified 256 shared targets between YHJG and IS, with PI3K-AKT and MAPK as key pathways. Molecular docking showed strong binding between YHJG compounds (e.g., quercetin) and core targets (AKT1, ERK1/2). YHJG treatment significantly improved neurological function (<i>p</i> < 0.01), reduced infarct volume (<i>p</i> < 0.01), and attenuated neuronal damage. The expression of IL-1β, TNF-α, IL-6, AKT1, and pERK1/2/ERK1/2 significantly increased in the MCAO group (<i>p</i> < 0.01), while YHJG treatment significantly reduced their expression (<i>p</i> < 0.01). PPAR-γ expression significantly increased in the YHJG-H group (<i>p</i> < 0.01). <b>Conclusions:</b> The expression of IL-1β, TNF-α, IL-6, AKT1, and pERK1/2/ERK1/2 significantly increased in the MCAO group, while YHJG treatment significantly reduced their expression. PPAR-γ expression significantly increased in the YHJG-H group. YHJGs could treat IS through diverse ingredients, targets, and pathways by inhibiting inflammatory indices and AKT1 expression, and reducing ERK1/2 phosphorylation.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472206/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177486","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"<i>Moringa</i> (<i>Moringa oleifera</i>) Leaf Attenuates the High-Cholesterol Diet-Induced Adverse Events in Zebrafish: A 12-Week Dietary Intervention Resulted in an Anti-Obese Effect and Blood Lipid-Lowering Properties.","authors":"Kyung-Hyun Cho, Ashutosh Bahuguna, Yunki Lee, Ji-Eun Kim, Sang Hyuk Lee, Krismala Djayanti","doi":"10.3390/ph18091336","DOIUrl":"10.3390/ph18091336","url":null,"abstract":"<p><p><b>Objective:</b> The study investigates the dietary effects of <i>Moringa oleifera</i> leaf powder on obesity, blood biochemical parameters, and organ health in hyperlipidemic zebrafish (<i>Danio rerio</i>). <b>Methodology</b>: Adult hyperlipidemic zebrafish (n = 56/group) were fed for 12 weeks either with a high-cholesterol diet (HCD, 4% <i>w</i>/<i>w</i>) or HCD supplemented with 0.5% (<i>w</i>/<i>w</i>) <i>M. oleifera</i> leaf powder (0.5% MO) or HCD with 1.0% (<i>w</i>/<i>w</i>) <i>M. oleifera</i> leaf powder (1.0% MO). At different time points (0 to 12 weeks), the survivability and body weight (BW) of zebrafish were measured, while various biochemical and histological evaluations were performed after 12 weeks of feeding the respective diets. Additionally, an in silico approach was used to assess the binding interactions of MO phytoconstituents with 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. <b>Results</b>: Following 12-week supplementation, higher zebrafish survivability was observed in the MO-supplemented groups compared to the survivability of the HCD group. Relative to the initial BW, only 4% BW enhancement was observed post 12 weeks of dietary intake of 1.0% MO, in contrast to 27% BW gain in the HCD group. MO supplementation at both (0.5% and 1.0%) effectively mitigates the HCD-induced dyslipidemia and significantly minimizes the atherogenic coefficient and atherogenic index. Similarly, MO reduces elevated blood glucose levels, the ALT/AST ratio, and augments ferric ion reduction (FRA) and paraoxonase (PON) activity in a dose-dependent manner. Likewise, MO (particularly at 1.0%) effectively restrained HCD-induced steatosis, hepatic interleukin (IL)-6 production, and protected the kidneys, testes, and ovaries from oxidative stress and cellular senescence. The in silico findings underscore that the six phytoconstituents (chlorogenic acid, isoquercetin, kaempferol 3-<i>O</i>-rutinoside, astragalin, apigetrin, and myricetin) of MO exhibited a strong interaction with HMG-CoA reductase active and binding site residues via hydrogen and hydrophobic interactions. <b>Conclusions</b>: The findings demonstrated an antioxidant, anti-inflammatory, and hypoglycemic effect of MO, guiding the events to prevent HCD-induced metabolic stress and safeguard vital organs.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472896/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177538","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis, Computational Studies, and Structural Analysis of 1-(3,5-Dimethoxyphenyl)azetidin-2-ones with Antiproliferative Activity in Breast Cancer and Chemoresistant Colon Cancer.","authors":"Azizah M Malebari, Shubhangi Kandwal, Abdirahman Ali, Darren Fayne, Brendan Twamley, Daniela M Zisterer, Mary J Meegan","doi":"10.3390/ph18091330","DOIUrl":"10.3390/ph18091330","url":null,"abstract":"<p><p><b>Background/Objectives</b>: A series of 1-(3,5-dimethoxyphenyl)azetidine-2-ones were synthesised to evaluate their antiproliferative activity in MCF-7 breast cancer cells and HT-29 chemoresistant colon cancer cells. The 1,4-diarylazetidin-2-ones were designed by replacing the characteristic 3,4,5-trimethoxyphenyl Ring A of the antimitotic stilbene combretastatin CA-4 with a 3,5-dimethoxyphenyl substituent at N-1, together with phenyl, hydroxyl, and phenoxy substituents at C-3 of the four-membered ring. <b>Methods</b>: A panel of 12 novel compounds was synthesized and evaluated in estrogen receptor (ER)- and progesterone receptor (PR)-positive MCF-7 breast cancer cells followed with the more potent compounds further evaluated in HT-29 chemoresistant colon cancer cells. Cytotoxicity was determined by LDH assay. The structures of the 1-(3,5-dimethoxyphenyl)azetidine-2-ones <b>12i</b>, <b>12k</b>, <b>12o</b>, <b>12p</b> together with the 1-(3,5-dimethoxyphenyl)azetidine-2-one <b>12s</b> were determined by X-ray crystallography. The <i>trans</i> configuration of the C-3 and C-4 substituents of the <i>β</i>-lactam ring was confirmed for compounds <b>12k</b> and <b>12u</b>. Molecular modelling and molecular dynamics studies examined the molecular interactions of the compounds with the colchicine binding site of tubulin. <b>Results</b>: The 1-(3,5-Dimethoxyphenyl)-4-(4-ethoxyphenyl)-3-hydroxyazetidin-2-one <b>12l</b> was identified as the most potent antiproliferative compound in the series (with an IC₅₀ value of 10 nM in MCF-7 breast cancer cells and 3 nM in HT-29 colon cancer cells) and with greater potency than CA-4 in the chemoresistant HT-29 cells. Computational docking studies predicted binding conformations for <b>12l</b> and the related series of compounds in the colchicine binding site of tubulin and rationalised the impact of the 3,5-dimethoxyphenyl substituent at N-1 of the azetidine-2-one on activity. <b>Conclusions</b>: These findings indicate that the novel 1-(3,5-dimethoxyphenyl)-2-azetidinone <b>12l</b> is a suitable candidate for further investigation as a potential antiproliferative microtubule-targeting agent for breast and chemoresistant colon cancers.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472776/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177840","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacological Effects and Mechanisms of Tanshinone IIA in Bone Injury Repair.","authors":"Weijian Hu, Yameng Si, Xinru Wen, Duan Lin, Zihao Yu, Xin Xie, Jiabin Xu","doi":"10.3390/ph18091338","DOIUrl":"10.3390/ph18091338","url":null,"abstract":"<p><p>Tanshinone IIA (T-IIA), a fat-soluble diterpene quinone extracted from <i>Salvia miltiorrhiza</i>, is widely recognized for its multiple pharmacological properties, including anti-inflammatory, antioxidant, anti-fibrotic, and anti-tumor effects. Recent studies have highlighted its great potential in treating bone metabolic disorders, especially osteoporosis and bone damage repair. Bone health depends on the dynamic balance between osteoblast-mediated bone formation and osteoclast-mediated bone resorption. Disruption of this balance can lead to diseases such as osteoporosis, which is often diagnosed after a fracture, seriously affecting the quality of life and increasing the medical burden. Early identification of high-risk groups and appropriate treatment are essential for preventing fracture recurrence. Studies have shown that T-IIA can promote osteoblast differentiation and inhibit osteoclast activity, targeting key signaling pathways such as NF-κB, PI3K/Akt, and Wnt/β-catenin, all of which are closely related to bone metabolism. T-IIA has a dual role in regulating bone formation and bone resorption, making it a potential drug for the treatment of osteoporosis. In addition, T-IIA has neuroprotective, hepatic, renal, cardiac, and cerebral effects, which enhance its therapeutic effect. Despite the remarkable efficacy of T-IIA, its clinical application is limited due to poor solubility and low bioavailability. Recent advances in drug delivery systems, such as liposome formulations and nanocarriers, have improved their pharmacokinetics, increased absorption rate, and bioavailability. Combination therapy with growth factors or stem cells can further enhance its efficacy. Future studies should focus on optimizing the delivery system of T-IIA and exploring its combined application with other therapeutic strategies to expand its clinical application range.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472646/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177761","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fused Imidazotriazole-Based Therapeutics: A Multidisciplinary Study Against Diabetes-Linked Enzymes Alpha-Amylase and Alpha-Glucosidase Using In Vitro and In Silico Methods.","authors":"Manal M Khowdiary, Shifa Felemban","doi":"10.3390/ph18091333","DOIUrl":"10.3390/ph18091333","url":null,"abstract":"<p><p><b>Background/Objective:</b> The present study reports the design, synthesis, and biological evaluation of novel imidazo-triazole derivatives as potential antidiabetic agents. <b>Methods:</b> The novel series was synthesized by treating amino-triazole bearing carboxylic acid with substituted 2-bromo acetophenone and was biologically compared with acarbose under in vitro analysis. <b>Results:</b> Structure-activity relationship (SAR) analysis revealed that among these compounds, remarkable activity was shown by compound <b>5</b> (having three hydroxyl substituents) with IC₅₀ value of 6.80 ± 0.10 and 7.10 ± 0.20 µM for α-amylase and α-glucosidase in comparison to reference drug acarbose. To support experimental findings, computational investigations including molecular docking, pharmacophore modeling, molecular dynamics simulations, density functional theory (DFT), and absorption distribution metabolism excretion and toxicity (ADMET) profiling were employed. These studies confirmed the stability of ligand-protein interactions and provided insights into electronic and reactivity features governing enzyme inhibition. <b>Conclusions:</b> Collectively, the integration of in vitro and in silico approaches underscores the potential of novel imidazo-triazole scaffolds as promising leads for the development of safer and more effective therapeutics against diabetes mellitus.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472753/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177660","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Repurposing Cofilin-Targeting Compounds for Ischemic Stroke Through Cheminformatics and Network Pharmacology.","authors":"Saleh I Alaqel, Abida Khan, Mashael N Alanazi, Naira Nayeem, Hayet Ben Khaled, Mohd Imran","doi":"10.3390/ph18091323","DOIUrl":"10.3390/ph18091323","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Cofilin, a key regulator of actin cytoskeleton dynamics, contributes to neuroinflammation, synaptic damage, and blood-brain barrier disruption in ischemic stroke. Despite its established role in stroke pathology, cofilin remains largely untargeted by existing therapeutics. This study aimed to identify potential cofilin-binding molecules by repurposing <i>LIMK1</i> inhibitors through an integrated computational strategy. <b>Methods</b>: A cheminformatics pipeline combined QSAR modeling with four molecular fingerprint sets and multiple machine learning algorithms. The best-performing QSAR model (substructure-Random Forest) achieved R²_train = 0.8747 and R²_test = 0.8078, supporting the reliability of compound prioritization. Feature importance was assessed through SHAP analysis. Top candidates were subjected to molecular docking against cofilin, followed by 300 ns molecular dynamics simulations, MM-GBSA binding energy calculations, principal component analysis (PCA), and dynamic cross-correlation matrix (DCCM) analyses. Network pharmacology identified overlapping targets between selected compounds and stroke-related genes. <b>Results</b>: Three compounds, CHEMBL3613624, ZINC000653853876, and Gandotinib, were prioritized based on QSAR performance, binding affinity (-6.68, -6.25, and -5.61 Kcal/mol, respectively), and structural relevance. Docking studies confirmed key interactions with Asp98 and His133 on cofilin. Molecular dynamics simulations supported the stability of these interactions, with Gandotinib showing the highest conformational stability, and ZINC000653853876 exhibiting the most favorable energetic profile. Network pharmacology analysis revealed eight intersecting targets, including <i>MAPK1</i>, <i>PRKCB</i>, <i>HDAC1</i>, and serotonin receptors, associated with neuroinflammatory and vascular pathways in strokes. <b>Conclusions</b>: This study presents a rational, integrative repurposing framework for identifying cofilin-targeting compounds with potential therapeutic relevance in ischemic stroke. The selected candidates warrant further experimental validation.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472226/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177633","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Anti-Oxidant, Anti-Inflammatory and Antiviral Properties of Luteolin Against SARS-CoV-2: Based on Network Pharmacology.","authors":"Xin Li, Yunmei Fu, Tong Yu, Ruizhe Song, Hongguang Nie, Yan Ding","doi":"10.3390/ph18091329","DOIUrl":"10.3390/ph18091329","url":null,"abstract":"<p><p>Luteolin is a natural flavonoid compound with multifaceted pharmacological properties, including anti-oxidant, anti-inflammatory, antiviral, and anti-tumor activities. Network pharmacology analysis has been utilized to decipher the underlying mechanisms and multitargets of luteolin against coronavirus disease 2019 (COVID-19). This review aims to provide a systematic and comprehensive summary of luteolin, as a potential novel remedy with anti-severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) activity, as well as its anti-oxidant mechanisms. We systematically delineate the epidemiological profile, genomic architecture, and replicative dynamics of SARS-CoV-2, thereby constructing a multiscale framework to decode its pathogenic mechanisms. Employing a multi-level network pharmacology analytical strategy, we identify 46 core targets through protein interaction network construction, followed by Gene Ontology and Kyoto Encyclopedia of Genes and Genomes enrichment analysis. Molecular investigations reveal luteolin's dual antiviral mechanisms, including direct targeting of SARS-CoV-2 proteins and host-directed intervention through suppression of angiotensin-converting enzyme 2 receptor engagement/transmembrane protease serine 2-mediated viral priming. The polypharmacological profile of luteolin demonstrates synergistic effects in blocking viral entry, replication, and host inflammatory cascades. This phytochemical repurposing study of luteolin provides a novel mechanistic paradigm for developing multitarget antiviral agents, highlighting the translational value of natural compounds in combating emerging viral variants.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472728/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145176676","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design, Synthesis, In Silico Docking, Multitarget Bioevaluation and Molecular Dynamic Simulation of Novel Pyrazolo[3,4-<i>d</i>]Pyrimidinone Derivatives as Potential In Vitro and In Vivo Anti-Inflammatory Agents.","authors":"Mostafa Roshdi, Mamdouh F A Mohamed, Eman A M Beshr, Hossameldin A Aziz, Sahar M Gebril, Stefan Bräse, Aliaa M Mohassab","doi":"10.3390/ph18091326","DOIUrl":"10.3390/ph18091326","url":null,"abstract":"<p><p><b>Background:</b> A novel series of pyrazolo[3,4-<i>d</i>]pyrimidinone derivatives were synthesized, characterized, and examined for their anti-inflammatory effects. <b>Results:</b> The findings indicated that compounds <b>5d</b>, <b>5j</b>, <b>5k</b>, and <b>5m</b> demonstrated significant anti-inflammatory effects through the selective inhibition of the COX-2 isozyme, with IC₅₀ values ranging from 0.27 to 2.34 μM, compared to celecoxib (IC₅₀ = 0.29 μM). Compound <b>5k</b> emerged as the most potent, exhibiting a selectivity index (SI) of 95.8 for COX-2 relative to COX-1. In vivo tests additionally validated that compounds <b>5j</b> and <b>5k</b> demonstrated significant anti-inflammatory efficacy, exhibiting greater suppression percentages of generated paw edema than indomethacin, comparable to celecoxib, while preserving excellent safety profiles with intact gastric tissue. Mechanistic studies demonstrated that the anti-inflammatory efficacy of the target compounds was associated with a substantial decrease in serum levels of TNF-α and IL-6. Moreover, molecular modeling investigations corroborated the in vitro findings. Compound <b>5k</b> displayed a binding free energy ΔG of -10.57 kcal/mol, comparable to that of celecoxib, which showed a ΔG of -10.19 kcal/mol. The intensified binding contacts in the COX-2 isozyme indicated the augmented inhibitory efficacy of <b>5k</b>. <b>Conclusions:</b> Compound <b>5k</b> exhibited dual activity by inhibiting the COX-2 isozyme and suppressing the pro-inflammatory cytokines TNF-α and IL-6, therefore providing a remarkable anti-inflammatory effect with increased therapeutic potential.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472512/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177765","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Therapeutic Potential of Cannabinoid Receptors Type 1 and 2-Novel Insights for Enhancing the Chance of Clinical Success.","authors":"Uwe Grether","doi":"10.3390/ph18091324","DOIUrl":"10.3390/ph18091324","url":null,"abstract":"<p><p>This Special Issue of <i>Pharmaceuticals</i> presents eight original articles and three reviews, underscoring the ongoing robust interest in research on cannabinoid receptor type 1 (CB₁R) and type 2 (CB₂R) more than 30 years after their discovery [...].</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12473137/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177588","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of Orally Disintegrating Tablets of Standardized <i>Rhodiola rosea</i> Extract.","authors":"Oxana Brante, Rihards Talivaldis Bagons, Santa Niedra, Austris Mazurs, Baiba Mauriņa, Jurga Bernatoniene, Konstantins Logviss","doi":"10.3390/ph18091328","DOIUrl":"10.3390/ph18091328","url":null,"abstract":"<p><p><b>Background/Objectives:</b><i>Rhodiola rosea</i> L. (<i>Crassulaceae</i>), a perennial adaptogenic herb native to Northern Europe, Asia, and North America, is renowned for its therapeutic properties attributed to phenolic compounds including flavonoids, phenylethanoids, phenylpropanoids, and cinnamyl alcohol glycosides. The plant's antioxidant and anti-inflammatory activities align with its traditional use in boosting physical and cognitive performance, reducing fatigue, and improving stress resilience. However, conventional dosage forms present compliance challenges, particularly for vulnerable populations with swallowing difficulties. This study aimed to develop and optimize orally disintegrating tablets (ODTs) containing standardized <i>Rhodiola rosea</i> root and rhizome (<i>RR</i>) dry extract to ensure rapid disintegration and acceptable taste, thereby improving patient compliance. <b>Methods:</b> Dried <i>Rhodiola rosea</i> root and rhizome (particle size 2-3 mm) were extracted using 70% m/m ethanol using the fractionated maceration methodology. The resulting dry <i>RR</i> extract was standardized to 3.0% m/m rosavin content by blending batches of the extract and analyzed using validated chromatographic methods. The standardized dry extract was formulated into ODTs via direct compression technology. Various excipients were evaluated to achieve rapid disintegration while masking the characteristic bitter taste of <i>RR</i> extract. <b>Results:</b> The optimized ODT formulation (500 mg, 11 mm ø, 20% standardized <i>RR</i> dry extract) disintegrated within 3 min and effectively masking the characteristic bitterness of the <i>RR</i> extract. The formulation maintained content uniformity and did not exhibit loss of active compounds during processing, meeting European Pharmacopoeia requirements for ODTs. <b>Conclusions:</b> The developed ODTs containing standardized <i>Rhodiola rosea</i> extract offer a patient-friendly alternative for oro-mucosal administration, supporting improved compliance in populations with swallowing difficulties while retaining the extract's phytochemical integrity and sensory acceptability.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"18 9","pages":""},"PeriodicalIF":4.8,"publicationDate":"2025-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12472554/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145177681","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}