Δ⁸⁽¹⁴⁾-Ergostenol Glycoside Derivatives Inhibit the Expression of Inflammatory Mediators and Matrix Metalloproteinase

• Main Authors: Hyejin Moon, Myoungsil Ko, Yujin Park, Jeonguk Kim, Dowon Yoon, Eunjoohwang Lee, Taehoon Lee, Hakwon Kim
• Format: Article
• Language: English
• Published: MDPI AG 2021-07-01
• Series: Molecules
• Subjects: ergostenol; ergostenol glycosides; arthritis; matrix metalloproteinase; collagen type II A1
• Online Access: https://www.mdpi.com/1420-3049/26/15/4547

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.