Abstract
Fibroblast-like synoviocytes are a key effector cell type involved in the pathogenesis of rheumatoid arthritis. The major green tea catechin, epigallocatechin-3-O-gallate (EGCG), has attracted significant interest for rheumatoid arthritis therapy because of its ability to suppress the proliferation and interleukin-6 secretion of synoviocytes. However, therapeutic efficacy of EGCG has been limited by a lack of target cell specificity. Herein we report hyaluronic acid–EGCG (HA–EGCG) conjugates as an anti-arthritic agent that is capable of targeting fibroblast-like synoviocytes via HA–CD44 interactions. These conjugates exhibited superior anti-proliferative and anti-inflammatory activities compared with EGCG under simulated physiological conditions. Near-infrared fluorescence imaging revealed preferential accumulation of the conjugates at inflamed joints in a collagen-induced arthritis rat model, and their anti-arthritic efficacy was investigated by measuring a change in the edema and histopathological scores. Our findings suggest the potential of HA–EGCG conjugates as an anti-arthritic agent for the treatment of rheumatoid arthritis.
Highlights
Rheumatoid arthritis (RA) is an autoimmune joint disease affecting approximately 0.5–1% of the world's adult population.[1]
We report hyaluronic acid–EGCG (HA–EGCG) conjugates as an anti-arthritic agent that is capable of targeting fibroblast-like synoviocytes via Hyaluronic acid (HA)–CD44 interactions
Blocker), but not with excess dextran (Fig. 2C and D). These results demonstrated that the intracellular entry of HA–EGCG–AF conjugates was mainly through CD44-mediated endocytosis
Summary
Rheumatoid arthritis (RA) is an autoimmune joint disease affecting approximately 0.5–1% of the world's adult population.[1]. With the earlier nding in PBS, HA–EGCG conjugates produced smaller amounts of H2O2 (74 mM) than EGCG (165 mM) when incubated in RPMI medium for 90 min (Fig. 3C).
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