rosiglitazone / Generic mfg. - LARVOL DELTA

Mechanistic Insights of BPA Alternatives on PPARγ Binding and the Consequence on Adipocyte Differentiation. (PubMed, Environ Sci Technol) - "Crystallography revealed distinct binding modes for BPPH and BPS4BE compared to rosiglitazone, indicating partial agonism. These findings raise significant concerns about the safety of BPA alternatives and underscore the need for structure-based risk assessment to ensure safer substitutes."

Journal • Genetic Disorders • Obesity • PPARG

Patient-derived organoid xenografts model esophageal cancer cachexia and enable assessment of anti-inflammatory drug repositioning. (PubMed, iScience) - "Using this platform, we tested two macrophage-targeting interventions: 10 mg/kg/day rosiglitazone, a PPAR-γ agonist, and 40 mg/kg/day pexidartinib (PLX3397), a CSF1R inhibitor. Transcriptomic analyses confirmed suppression of pro-cachectic cytokine signaling. This study presents a clinically relevant platform for preclinical cachexia research and supports macrophage modulation as a potential anti-cachexia strategy."

Journal • Cachexia • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Oncology • Squamous Cell Carcinoma

Elevated asprosin expression exacerbates synovial inflammation by PPAR-γ-dependent mechanisms in rheumatoid arthritis. (PubMed, Clin Immunol) - "TNF-α led to a marked downregulation of PPAR-γ, which was associated with increased asprosin levels, treatment with rosiglitazone effectively attenuated asprosin overproduction. Elevated circulating asprosin levels serve as an independent risk factor for RA and demonstrate promising diagnostic potential. PPAR-γ-mediated overexpression of asprosin contributes to synovial fibroblast dysfunction, suggesting a pathogenic role in RA development."

Journal • Immunology • Inflammation • Inflammatory Arthritis • Metabolic Disorders • Rheumatoid Arthritis • Rheumatology • TNFA

In vitro model of human subcutaneous adipocyte spheroids for studying mitochondrial dysfunction and mitochondria activating compounds. (PubMed, iScience) - "Post-differentiation treatment with rosiglitazone, a peroxisome proliferator-activated receptor γ agonist, improved mitochondrial bioenergetics and adiponectin secretion in lipid mixture-administered adipocyte spheroids. Our model enables precise measurement of adipocyte mitochondria metabolism, providing a platform for mitochondria-focused research and drug discovery in obesity."

Journal • Preclinical • Genetic Disorders • Metabolic Disorders • Obesity

PPARγ agonism ameliorates acute kidney injury by inhibiting neutrophil extracellular trap formation-mediated renal tubular epithelial cell PANoptosis. (PubMed, Cell Commun Signal) - "PPARγ is a pivotal checkpoint in CP-AKI by inhibiting ROS-NETosis-driven AIM2-mediated PANoptosis. This protective mechanism is also applicable to IRI-induced AKI, highlighting its broad relevance. HD-1L confers renoprotection through PPARγ activation, providing a novel therapeutic strategy against AKI."

Journal • Acute Kidney Injury • Cardiovascular • Inflammation • Nephrology • Renal Disease • Reperfusion Injury • CASP3 • PPARG

Study on the Characteristics and Cellular Origins of the Sebaceous Gland (ChiCTR) - P4 | N=20 | Not yet recruiting | Sponsor: WUHAN UNIVERSITY; WUHAN UNIVERSITY

New P4 trial • Atopic Dermatitis • Dermatitis • Dermatology • Immunology

An integrated drug repositioning analysis identifies rosiglitazone as a treatment for sarcopenia. (PubMed, Commun Biol) - "Genetic analyses further support the causal role of Clostridiaceae/Clostridium in grip strength. Our findings nominate rosiglitazone as a promising intervention for sarcopenia, warranting further clinical investigation."

Journal • Diabetes • Metabolic Disorders • Sarcopenia • Targeted Protein Degradation • FBXO32 • IGF1

Optimization of Adipogenic Differentiation Protocol for Murine and Human Cell Culture Models. (PubMed, Bio Protoc) - "We show that high cell density, rosiglitazone supplementation, and an extended primary induction phase combine to promote lipid accumulation...Key features • Extend a robust, standardized adipogenic differentiation protocol from 3T3-L1 preadipocytes to clinically relevant models, including hADSCs and the heterogeneous SVF. • Identify key optimized parameters-cell density, induction timing, and inducer composition-enabling highly reproducible differentiation across species."

Journal • Preclinical

Macrophage-biomimetic nanomedicine for targeted therapy of abdominal aortic aneurysm via Nrf2/NF-κB pathway. (PubMed, Theranostics) - " Leveraging the multi-pore property of mesoporous Prussian blue nanoparticles (MPB NPs), we encapsulated the rosiglitazone (RLZ) into MPB NPs to synthesize MPB-RLZ NPs... MPB-RLZ@MM NPs exhibited excellent biosafety and therapeutic efficacy against AAA. This macrophage-biomimetic strategy presents a promising therapeutic approach for AAA treatment."

Journal • Cardiovascular

Repurposing Rosiglitazone Induces Apoptosis Accompanied by Impaired Antioxidant Defense in Cholangiocarcinoma Cells: Findings from Proteomic and Functional Analyses. (PubMed, Pharmaceuticals (Basel)) - "Its apoptosis-inducing effect is independent of PPARγ activation. These findings underscore the therapeutic potential of RSG for CCA treatment."

Journal • Biliary Cancer • Cholangiocarcinoma • Oncology • Solid Tumor • ANXA1 • CASP3 • CASP7 • PPARG

Hyperoside ameliorates NAFLD in rats via remodeling gut microbiota and reprogramming serum metabolic networks. (PubMed, Front Nutr) - "The SD rats were divided into five groups (normal control, NAFLD model, low-dose hyperoside [0.6 mg/kg/day], high-dose hyperoside [1.5 mg/kg/day], and rosiglitazone positive control [5 mg/kg/day]) and treated for 12 weeks...Beneficial bacteria were negatively correlated with pro-inflammatory metabolites like lysophosphatidylcholine. Hyperoside ameliorates NAFLD, which is associated with gut microbiota remodeling and modulation of host metabolic networks, supporting its potential as a multi-target therapeutic agent for NAFLD."

Journal • Preclinical • Addiction (Opioid and Alcohol) • Fibrosis • Hepatology • Immunology • Liver Cirrhosis • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease • TLR4 • TNFA

The Identification of Mitochondrial-Related Biomarkers of Ruptured Intracranial Aneurysms Based on Bioinformatics Analysis and Machine Learning. (PubMed, J Neurosci Res) - "Finally, potential therapeutic drugs such as rosiglitazone were identified by drug prediction, and the molecular docking of ME2 with cryptotanshinone suggested a new therapeutic approach. This study may provide a new strategy for the diagnosis and treatment of RIA targeting mitochondria."

Biomarker • Journal • Cardiovascular • Vascular Neurology • BCL2A1 • VAV1

Trigonelline regulates glycolysis and energy metabolism during hepatic fibrosis via Glut-1-HIF-1α axis: Focusing the interaction of macrophages and HSCs. (PubMed, Phytomedicine) - "TRG could ameliorate hepatic fibrosis through inhibiting ECM excessive deposition and inflammatory response. Inhibiting Glut-1-HIF-1α axis and glycolysis was a potential therapeutic strategy for TRG ameliorating liver microenvironment, further against hepatic fibrosis."

Journal • Fibrosis • Hepatology • Immunology • Inflammation • Liver Cirrhosis • HIF1A • IL1R1 • IL6 • SLC2A1 • TGFB1 • TRG

Protective Effect and Mechanism of Rosiglitazone in α-amanitin-induced Hepatotoxicity Via Activation of PPAR-γ/Nrf2 Signaling Pathway. (PubMed, J Biochem Mol Toxicol) - "Early RSG intervention can thereby effectively mitigate α-AMA-induced acute liver injury by upregulating the PPAR-γ/Nrf2 signaling pathway. Future studies should focus on exploring the clinical potential of RSG as a therapeutic agent for amanita mushroom poisoning."

Journal • Hepatology • Inflammation • Liver Failure • CASP3 • CAT • CXCL8 • IL6 • TNFA

Establishment of Mouse Meibomian Gland Organoids for In Vitro Modeling of Meibomian Gland Dysfunction. (PubMed, Invest Ophthalmol Vis Sci) - "IL-1β exposure arrested organoid development, inhibited lipid accumulation, and induced hyperkeratinization of MG organoids, which was reversed by SB203580, an inhibitor of the p38 mitogen-activated protein kinase (MAPK) signaling pathway, or rosiglitazone, an agonist of the PPARγ signaling pathway...Organoids modeled key features of MGD through exposure to IL-1β and can respond to targeted therapy. The system offered a promising platform for MGD research."

Journal • Preclinical • Transplantation • IL1B • KRT5 • LRIG1 • PPARG

Thiazolidine-2,4-Dione: Bridging the Gap Between Synthesis, SAR, and Biological Activities, and Computational Predictions. (PubMed, Zhongguo Ying Yong Sheng Li Xue Za Zhi) - "This review highlights the significance of the TZD scaffold as a multifunctional pharmacophore in drug discovery. By integrating synthetic strategies, SAR analysis, and advanced computational tools, TZD derivatives continue to show great potential for the development of new therapeutic agents for various diseases. The combined understanding of chemistry and biological activities of TZDs paves the way for innovative research and future drug design."

Journal • Review • Oncology

Early-in-life inhalation of ferrocene-derived diesel exhaust-induced metabolic and small intestinal toxicities: Roles of peroxisome proliferator-activated receptor gamma and ferroptosis. (PubMed, Ecotoxicol Environ Saf) - "Again, PPARγ silencing mimicked the observed effects, while rosiglitazone alleviated such effects. In conclusion, early-in-life inhalation exposure to FDE resulted in metabolic and small intestinal toxicities in 1- or 3-month-old chickens, such effects were associated with PPARγ/PGC1α-ferroptosis signaling."

Journal • GPX4 • PPARG • SLC7A11

Mechanistic insights into Gwt1-substrate interactions and antifungal drug discovery via molecular dynamics and virtual screening. (PubMed, J Biomol Struct Dyn) - "Leveraging these structural insights, we performed virtual screening targeting the hydrophobic pocket formed by Tyr129, Tyr400, Phe404, and Tyr408, which identified two approved drugs, tivozanib and rosiglitazone, as potential Gwt1 inhibitors. Experimental validation confirmed their antifungal activities against pathogenic fungi, including Cryptococcus neoformans, Candida albicans, and Aspergillus fumigatus. This work provides dynamic mechanistic insights into Gwt1 function and offers a rational strategy for repurposing existing drugs as antifungals targeting the GPI pathway."

Journal

Myricanol modulates PPARγ/ACSL1/SCD1 metabolic signaling pathway to promote mitochondria biogenesis and fatty acid β-oxidation in high-fat diet-induced obese mice. (PubMed, J Ethnopharmacol) - "This study reveals a novel cellular mechanism through which myricanol reduces lipid levels via the PPARγ/ACSL1/SCD1 signaling pathway. Myricanol also promotes mitochondrial biogenesis and fatty acid β-oxidation; therefore, it holds great promise as a phytotherapeutic agent for hyperlipidemia."

Journal • Preclinical • Dyslipidemia • Inflammation • Obesity • ACACA • ACSL1 • CPT1A • MIR184 • MIR203A • MIR205 • MUTYH • PPARG

Toward Efficient Beige Adipogenesis: Protocol Optimization Using Adipose-Derived Stem Cells. (PubMed, Cells) - "Among the key adipogenic factors, rosiglitazone proved more effective than indomethacin. Extending the induction phase from 4 to 8 days and maintaining dexamethasone throughout the culture markedly enhanced differentiation efficiency...The optimized protocol successfully induced beige adipogenesis in ADSCs from eight independent donors, though efficiency varied considerably which could be attributed to individual donor variability. These findings provide a robust in vitro model for studying beige fat biology and highlight the relevance of personalized approaches in metabolic research."

Journal • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus

Multi-omic integration identifies broad drug resistance mechanisms and strategies to therapeutically reprogram cancer cells. (PubMed, iScience) - "Computational perturbagen screening identified compounds predicted to counteract these transcriptional signatures, converging on regulators of NFE2L2 activity. Experimental testing confirmed that rosiglitazone reduced NFE2L2-associated gene expression and re-sensitized resistant cells to chemotherapy, demonstrating a scalable strategy for rational phenotypic reprogramming."

Journal • Oncology

1,8-Cineole ameliorates vascular endothelial senescence in diabetes mellitus by directly targeting and deubiquitinating PPAR-γ in vivo and in vitro. (PubMed, J Pharm Anal) - "Accordingly, experiments with the PPAR-γ agonist rosiglitazone, the PPAR-γ inhibitor GW9662, and PPAR-γ siRNA were performed to validate the pharmacological characteristics of 1,8-cineole. Finally, we clarified that 1,8-cineole can directly target PPAR-γ protein, as verified by cellular thermal shift assay, drug affinity responsive target stability, and surface plasmon resonance analyses. Taken together, these results provide the first evidence that 1,8-cineole ameliorates DM-induced vascular endothelial ageing via stabilising PPAR-γ protein by promoting deubiquitination at the Lys-466 site."

Journal • Preclinical • Cardiovascular • Diabetes • Metabolic Disorders • Targeted Protein Degradation

Rbbp7-mediated deacetylation of Acsl4 promotes ovarian aging by enhancing ferroptosis. (PubMed, Int J Biol Macromol) - "We also found that the ferroptosis inhibitor Deferoxamine (DFO), Ferrostatin-1 (Fer-1) or the Acsl4 inhibitor Rosiglitazone (Rosi) inhibited ovarian aging and granulosa cell damage in vivo and in vitro. Inhibiting ferroptosis or Acsl4 can alleviate ovarian aging. Our research has revealed a new mechanism of ovarian aging and provided potential new targets for alleviating it."

Journal • Cardiovascular • Diabetes • Eye Cancer • Heart Failure • Infertility • Metabolic Disorders • Oncology • Retinal Disorders • Retinoblastoma • Sexual Disorders • Solid Tumor • ACSL4 • RBBP7

Emodin Enhances Rosiglitazone's Therapeutic Profile by Dual Modulation of SREBP1-Mediated Adipogenesis and PPARγ-Driven Thermogenesis. (PubMed, Pharmaceuticals (Basel)) - " EMO selectively enhances RSG's glycemic benefits while attenuating its adipogenic effects in severe obesity by dual PPARγ modulation-inhibiting adipogenic pathways while amplifying thermogenesis. This strategy mitigates RSG's adverse effects while improving insulin sensitivity, supporting the potential of EMO as a PPARγ adjunct therapy."

Journal • Diabetes • Genetic Disorders • Metabolic Disorders • Nephrology • Obesity • Renal Disease • Type 2 Diabetes Mellitus • FASN • PPARG • PPARGC1A

miR-205-5p Promotes Hepatic Fat Accumulation as a Downstream Effector of PPARγ Signaling. (PubMed, Genes Cells) - "miR-205-5p was significantly upregulated in the ob/ob mouse livers and induced by treatment with the PPARγ-specific agonist rosiglitazone...These findings suggest that the PPARγ-miR-205-5p axis plays a key role in the promotion of hepatic fat accumulation. Collectively, our data indicate that miR-205-5p has potential as a downstream effector of hepatic PPARγ signaling and may serve as a biomarker and therapeutic target for nonalcoholic fatty liver disease."

Journal • Addiction (Opioid and Alcohol) • Hepatology • Leptin Receptor Deficiency Obesity • Metabolic Dysfunction-Associated Steatohepatitis • Metabolic Dysfunction-Associated Steatotic Liver Disease • ACOX1 • HNF1A • LEP • MIR205 • PPARG