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Endomorphins in rheumatoid arthritis, osteoarthritis, and experimental arthritis
Author(s) -
Jessop David S.,
Fassold Alexander,
Wolff Christine,
Hofbauer Rafael,
ChoverGonzalez Antonio,
Richards Louise J.,
Straub Rainer H.
Publication year - 2010
Publication title -
annals of the new york academy of sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.712
H-Index - 248
eISSN - 1749-6632
pISSN - 0077-8923
DOI - 10.1111/j.1749-6632.2009.05294.x
Subject(s) - rheumatoid arthritis , medicine , osteoarthritis , arthritis , physical therapy , dermatology , alternative medicine , pathology
The opioid tetrapeptides endomorphins (EM)‐1 and EM‐2 are widely expressed in central nervous system and immune tissues of rats and humans. Their analgesic properties are well characterized but they also have anti‐inflammatory properties. EM‐1 significantly attenuated the onset of hindpaw inflammation in adjuvant‐induced arthritis in rats. Immunohistochemical staining demonstrated the presence of EMs in T cells, macrophages, and fibroblasts in synovial tissues from patients with osteo‐ or rheumatoid arthritis (RA). In an ex vivo superfusion system, EM‐1 potently inhibited the release of proinflammatory cytokines interleukin (IL)‐6 and IL‐8 from synovial tissues from patients with osteo‐ or RA. These results demonstrate that EMs are endogenously synthesized within human immune cells and have the potential to act as potent therapeutic agents in the treatment of chronic inflammatory disease. We discuss the clinical potential for EM analogues chemically modified to resist proteolytic degradation and identify modified protease‐resistant analogues with enhanced bioactivity.