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Discovery of selective ROCK2 inhibitors with free radical scavenging ability for the treatment of gouty arthritis.
Mol Divers
January 2025
Key Laboratory of Structure-Based Drugs Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, PR China.
ROCK inhibitors can inhibit IL-1β and NLRP3, and their therapeutic potential for osteoarthritis and rheumatoid arthritis has been confirmed, but their impact on gouty arthritis has not been reported yet. By hybridization the structure of Edaravone, a series of ROCK inhibitors with pyrazolone scaffold were designed and synthesized. RM-04 has acceptable selective ROCK2 inhibitory activity with an IC of 4.
View Article and Find Full Text PDFThe Role of the Toll-Like Receptor Signaling Pathway in Autoimmune Diseases and Treatment with Traditional Chinese Medicine: A Literature Review.
Endocr Metab Immune Disord Drug Targets
January 2025
Department of Endocrinology, Affiliated Hospital of Shandong University of Traditional Chinese Medicine, Jinan, China.
Toll-Like Receptors (TLRs) is a pattern recognition receptor that connects innate and adaptive immunity and participates in inflammatory responses play a key role in common autoimmune diseases such as Rheumatoid Arthritis (RA), systemic lupus erythematosus (SLE), psoriasis, and Sjögren's syndrome (SS) by participating in antigen recognition, immune cell activation, and inflammatory factor release. Due to the multi-component and multi-target characteristics of traditional Chinese medicine (TCM), the role of TCM active ingredients acting on TLRs has been widely studied. This article describes the relationship between TLR and four autoimmune diseases, as well as a review of the efficacy of TLR intervention by active ingredients of traditional Chinese medicine.
View Article and Find Full Text PDFHerb-Drug Interaction of Total Glucosides of Paeony and Tripterygium Glycoside with Celecoxib in Beagle Dogs by UPLC-MS/MS.
Eur J Drug Metab Pharmacokinet
January 2025
College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, 471023, China.
Background And Objective: Total glucosides of paeony (TGP) capsules, tripterygium glycoside tablets (TGT), and celecoxib are commonly used drugs in clinical practice for the treatment of Rheumatoid arthritis (RA). An UPLC-MS/MS method for the analysis of celecoxib in beagle dogs was developed, the herb-drug interactions (HDIs) between TGP and TGT with celecoxib were studied based on pharmacokinetics.
Methods: The method of acetonitrile precipitation was applied to process plasma samples.
Development and In-Vitro Tuning of Piperine Containing Solid Lipid Microparticles for the Treatment of Rheumatoid Arthritis.
AAPS PharmSciTech
January 2025
Department of Pharmaceutics, College of Pharmacy, King Saud University, PO Box 2457, 11451, Riyadh, Saudi Arabia.
The current project was designed to develop piperine-loaded solid lipid microparticles (SLMs) to assess the anti-arthritic potential of piperine (PIP). Variable proportions of carnauba wax, beeswax, and tween 80 were employed for preparing SLMs by using the solvent evaporation technique. The developed formulations were subjected to particle size measurements, entrapment efficiency (EE), and zeta potential (ZP) determination.
View Article and Find Full Text PDFSwitching to biological DMARDs versus cycling among JAK inhibitors in patients with rheumatoid arthritis and with inadequate response to JAK inhibitors: from FIRST registry.
RMD Open
January 2025
First Department of Internal Medicine, University of Occupational and Environmental Health Japan, Kitakyushu, Japan
Objectives: This study aimed to identify characteristics of patients with rheumatoid arthritis (RA) with an inadequate response to Janus kinase inhibitors (JAKi-IR) and evaluate the efficacy and safety of subsequent treatments.
Methods: This study included 434 patients with RA who started JAKi treatment. JAKi-IR patients were those who switched to another drug due to inadequate response or did not reach low disease activity within 26 weeks of beginning JAKi.
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