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

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.

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Calcitonin directly attenuates collagen type II degradation by inhibition of matrix metalloproteinase expression and activity in articular chondrocytes

Osteoarthritis and Cartilage ◽

10.1016/j.joca.2006.01.014 ◽

2006 ◽

Vol 14 (8) ◽

pp. 759-768 ◽

Cited By ~ 68

Author(s):

B.C. Sondergaard ◽

H. Wulf ◽

K. Henriksen ◽

S. Schaller ◽

S. Oestergaard ◽

...

Keyword(s):

Matrix Metalloproteinase ◽

Collagen Type ◽

Articular Chondrocytes ◽

Type Ii ◽

Collagen Type Ii ◽

Expression And Activity

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Role of mitogen-activated protein kinases and NFκB on IL-1β-induced effects on collagen type II, MMP-1 and 13 mRNA expression in normal articular human chondrocytes

Rheumatology International ◽

10.1007/s00296-006-0114-7 ◽

2006 ◽

Vol 26 (10) ◽

pp. 900-903 ◽

Cited By ~ 50

Author(s):

Zhiyong Fan ◽

Huiqing Yang ◽

Brigitte Bau ◽

Stephan Söder ◽

Thomas Aigner

Keyword(s):

Mrna Expression ◽

Protein Kinases ◽

Collagen Type ◽

Human Chondrocytes ◽

Type Ii ◽

Collagen Type Ii ◽

Mitogen Activated Protein Kinases ◽

Mitogen Activated Protein

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Curcumin protects human chondrocytes from IL-1β-induced inhibition of collagen type II and β1-integrin expression and activation of caspase-3: An immunomorphological study

Annals of Anatomy - Anatomischer Anzeiger ◽

10.1016/j.aanat.2005.06.007 ◽

2005 ◽

Vol 187 (5-6) ◽

pp. 487-497 ◽

Cited By ~ 85

Author(s):

Mehdi Shakibaei ◽

Gundula Schulze-Tanzil ◽

Thilo John ◽

Ali Mobasheri

Keyword(s):

Caspase 3 ◽

Collagen Type ◽

Human Chondrocytes ◽

Β1 Integrin ◽

Integrin Expression ◽

Type Ii ◽

Collagen Type Ii ◽

Immunomorphological Study

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In Vitro Effects of Low Doses of β-Caryophyllene, Ascorbic Acid and d-Glucosamine on Human Chondrocyte Viability and Inflammation

Pharmaceuticals ◽

10.3390/ph14030286 ◽

2021 ◽

Vol 14 (3) ◽

pp. 286

Author(s):

Elena Mattiuzzo ◽

Alessia Faggian ◽

Rina Venerando ◽

Andrea Benetti ◽

Elisa Belluzzi ◽

...

Keyword(s):

Ascorbic Acid ◽

Collagen Type ◽

Protective Action ◽

Human Chondrocytes ◽

Low Doses ◽

Type Ii ◽

Collagen Type Ii ◽

Human Chondrocyte ◽

Anti Inflammatory

β-caryophyllene (BCP), a plant-derived sesquiterpene, has been reported to have anti-inflammatory and antioxidant effects. The purpose of this study is to evaluate the effects of BCP in combination with ascorbic acid (AA) and d-glucosamine (GlcN) against macrophage-mediated inflammation on in vitro primary human chondrocytes. Changes in cell viability, intracellular ROS generation, gene expression of pro-inflammatory mediators, metalloproteinases (MMPs), collagen type II and aggrecan were analyzed in primary human chondrocytes exposed to the conditioned medium (CM) of activated U937 monocytes and subsequently treated with BCP alone or in combination with AA and GlcN. The CM-induced chondrocyte cytotoxicity was reduced by the presence of low doses of BCP alone or in combination with AA and GlcN. The exposure of cells to CM significantly increased IL-1β, NF-κB1 and MMP-13 expression, but when BCP was added to the inflamed cells, alone or in combination with AA and GlcN, gene transcription for all these molecules was restored to near baseline values. Moreover, chondrocytes increased the expression of collagen type II and aggrecan when stimulated with AA and GlcN alone or in combination with BCP. This study showed the synergistic anti-inflammatory and antioxidative effects of BCP, AA and GlcN at low doses on human chondrocyte cultures treated with the CM of activated U937 cells. Moreover, the combination of the three molecules was able to promote the expression of collagen type II and aggrecan. All together, these data could suggest that BCP, AA and GlcN exert a chondro-protective action.

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