In Vitro and In Vivo Anti-Osteoarthritis Effects of 2,3,5,4'-Tetrahydroxystilbene-2-O-β-d-Glucoside from Polygonum Multiflorum.

Po-Wei Tsai,Yi-Hui Lee,Lih-Geeng Chen,Chia-Jung Lee,Ching-Chiung Wang

doi:10.3390/molecules23030571

Abstract

Polygonum multiflorum Thunb. is a traditional herbal medicine that is rich in polyphenols. The major compound, 2,3,5,4′-tetrahydroxystilbene-2-O-β-d-glucoside (THSG) has many pharmacological activities, such as antioxidative and free radical-scavenging properties, and the abilities to reduce hyperlipidemia, prevent lipid peroxidation, and protect the cardiovascular system. In this study, the anti-osteoarthritis (OA) effects of THSG were explored using in vitro and in vivo models. THSG inhibited nitric oxide (NO) and prostaglandin E2 (PGE2) production and inducible NO synthase (iNOS) and cyclooxygenase-2 expressions by lipopolysaccharide-stimulated RAW 264.7 cells. On the other hand, THSG inhibited PGE2 production and iNOS and matrix metalloproteinase-13 expressions by interleukin-1β-stimulated primary rat chondrocytes. Through a mono-iodoacetate-induced rat OA model assay, THSG reduced paw edema and improved the weight-bearing distribution. Therefore, THSG has anti-inflammatory activity and could be applied as a lead compound for the development as an OA drug.

Highlights

Osteoarthritis (OA) is a chronic degenerative bone and joint disease mostly in the elderly, with main pathological features of articular cartilage degeneration, mild synovitis, meniscus injury, bone remodeling, subchondral bone sclerosis, and osteophyte formation [1,2,3]
In the isolation system focused on THSG, we excluded other compounds and efficiently gained the active compound, with a 1.2% yield
nitric oxide (NO) from from arginine, arginine, and and it it plays plays an important role in many body functions

Summary

Introduction

Osteoarthritis (OA) is a chronic degenerative bone and joint disease mostly in the elderly, with main pathological features of articular cartilage degeneration, mild synovitis, meniscus injury, bone remodeling, subchondral bone sclerosis, and osteophyte formation [1,2,3]. It was thought that articular cartilage was the main cause of OA degradation, and it has been confirmed that. The major pathogenic factors of articular cartilage degenerative lesions are joint load conduction disorder, joint nutrition reduction, and free radical damage. All kinds of pathogenic factors can lead to cartilage degeneration, which is caused by different routes of articular chondrocytes and cartilage matrix degradation of the body, in which the death of chondrocytes is the key to cartilage lesions [5,6]

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Discussion

Conclusion