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Δ8(14)-Ergostenol Glycoside Derivatives Inhibit the Expression of Inflammatory Mediators and Matrix Metalloproteinase
Authors:Hyejin Moon  Myoungsil Ko  Yujin Park  Jeonguk Kim  Dowon Yoon  Eunjoohwang Lee  Taehoon Lee  Hakwon Kim
Affiliation:1.Global Center for Pharmaceutical Ingredient Materials, Department of Applied Chemistry, Kyung Hee University, Yongin 17104, Korea; (H.M.); (M.K.); (J.K.); (D.Y.);2.Graduate School of East-West Medicinal Science, Kyung Hee University, Yongin 17104, Korea; (Y.P.); (E.L.)
Abstract:Arthritis is a chronic inflammatory disease accompanied by pathological reactions such as swelling, redness, fever, and pain in various joint areas. The drugs currently available to treat arthritis are associated with diverse side-effects. Therefore, there is a need for safer and more effective treatments to alleviate the inflammation of arthritis with fewer side-effects. In this study, a new sterol, Δ8(14)-ergostenol, was discovered, and its glycosides were synthesized and found to be more efficient in terms of synthesis or anti-inflammatory activity than either spinasterol or 5,6-dihydroergosterol is. Among these synthetic glycosides, galactosyl ergostenol inhibited the expression of inflammatory mediators in TNF-α-stimulated FLS and TNF-α-induced MMPs and collagen type II A1 degradation in human chondrocytes. These results suggest the new galactosyl ergostenol as a treatment candidate for arthritis.
Keywords:ergostenol   ergostenol glycosides   arthritis   matrix metalloproteinase   collagen type II A1
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