ArticleSignal transduction and targeted therapy2023
Metabolic reprogramming of proinflammatory macrophages by target delivered roburic acid effectively ameliorates rheumatoid arthritis symptoms.
Article in Signal transduction and targeted therapy, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 77 papers.
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Who cites it
77 citing papers in PubMed, 125 citations in OpenAlex.
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- Stimuli-responsive structural transformation of adaptive peptide nanomaterials toward biomedical applications.Materials today. Bio · 2026Review
- Integrated LC-Orbitrap-MS and network pharmacology decipher the pharmacological basis of Eucommiae folium in treating rheumatoid arthritis.Molecular diversity · 2026Article
- Assembled Hyaluronic Acid Therapeutics for Targeting M1 Macrophages and Regulating Immune Homeostasis for Ulcerative Colitis Treatment.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Mitochondria-Targeted Multimodal Nanotherapeutics Suppress Oxidized mtDNA-Driven Inflammation at the Source.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Advances in Living Cell-Mediated Nanodrug Delivery Systems: Construction Strategies, Applications and Challenges.Pharmaceutics · 2026Review
- SPP1+ macrophages contribute to silica-induced pulmonary inflammation and fibrosis via the ERK/JNK signaling pathway.American journal of respiratory cell and molecular biology · 2026Article
- Review
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- Advances in Nano-Drug Delivery Systems for Chronic Autoimmune Diseases: A Focus on Diabetes Mellitus, Inflammatory Bowel Disease, and Rheumatoid Arthritis.Molecules (Basel, Switzerland) · 2026Review
- Nanoparticles isolated from the Gubi Zhitong formula alleviate knee osteoarthritis by reprogramming macrophages.Materials today. Bio · 2026Article
- The vicious cycle from inflammation to pyroptosis: the core role of macrophage polarization imbalance in the pathogenesis of knee osteoarthritis.Molecular biology reports · 2026Review
- Dual itaconate delivery systems modulate macrophage Acod1-Hif-1α-glycolysis axis for immunotherapy of bioprosthetic heart valve calcification.Bioactive materials · 2026Article
- Erxian Decoction Ameliorates Myocardial Damage in Ovariectomized Rats by Regulating the Gut Microbiota and TMAO-Mediated NLRP3 Inflammatory Pathway.Journal of microbiology and biotechnology · 2026Article
- Traditional Chinese Medicine Modernization in Diagnosis and Treatment: Utilizing Artificial Intelligence and Nanotechnology.MedComm · 2026Review
- 4D-printed Fe3O4-PLLA scaffolds modulate osteoimmune microenvironment for oral bone repair.Materials today. Bio · 2026Article
- Amino acid metabolism modulates macrophage polarization: implications for autoimmune-related diseases.Frontiers in immunology · 2026Review
- ROS scavenging nanoengineered bioactive glass interfaces reprogram macrophage immunity for tendon-bone regeneration.Regenerative biomaterials · 2026Article
- GM-CSF promotes pro-inflammatory macrophage activation associated with Akt/mTOR signaling during experimental colitis.Frontiers in immunology · 2026Article
- Succinate-mediated metabolic alterations and signaling in RA: mechanisms and therapeutic implications.Frontiers in immunology · 2026Review
17 more citing papers are in PubMed but not listed here.
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Authors and funding
14 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Rheumatoid arthritis (RA) is a common chronic inflammatory disorder that usually affects joints. It was found that roburic acid (RBA), an ingredient from anti-RA herb Gentiana macrophylla Pall., displayed strong anti-inflammatory activity. However, its medical application is limited by its hydrophobicity, lack of targeting capability and unclear functional mechanism. Here, we constructed a pH responsive dual-target drug delivery system hitchhiking RBA (RBA-NPs) that targeted both CD44 and folate receptors, and investigated its pharmacological mechanism. In rat RA model, the nanocarriers effectively delivered RBA to inflammatory sites and significantly enhanced the therapeutic outcomes compared with free RBA, as well as strongly reducing inflammatory cytokine levels and promoting tissue repair. Following analysis revealed that M1 macrophages in the joints were reprogrammed to M2 phenotype by RBA. Since the balance of pro- and anti-inflammatory macrophages play important roles in maintaining immune homeostasis and preventing excessive inflammation in RA, this reprogramming is likely responsible for the anti-RA effect. Furthermore, we revealed that RBA-NPs drove M1-to-M2 phenotypic switch by down-regulating the glycolysis level via blocking ERK/HIF-1α/GLUT1 pathway. Thus, our work not only developed a targeting delivery system that remarkably improved the anti-RA efficiency of RBA, but also identified a potential molecular target to reversely reprogram macrophages though energy metabolism regulation.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.