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The protective effect of phloretin in osteoarthritis: a in vitro and in vivo study.

Abstract

Osteoarthritis (OA) is a degenerative joint disease characterized by cartilage degradation and inflammation. Phloretin, a type of dihydrochalcone mainly found in apples and apple-derived products, has been reported to possess various potent biological effects, such as as antioxidant, anti-cancer, anti-inflammatory and immunomodulatory activities. However, the anti-inflammatory effects of phloretin on OA have not been reported. This study aimed to assess the effects of phloretin on human OA chondrocytes. Human OA chondrocytes were pretreated with phloretin (10, 30, 100μM) for 2 h and subsequently stimulated with IL-1β for 24 h. Production of NO, PGE2, TNF-α and IL-6 was evaluated by the Griess reagent and ELISAs. The mRNA expression of COX-2, iNOS, MMP-3, MMP-13 and ADAMTS-5 was measured by real-time PCR. Changes in the protein expression of COX-2, iNOS, MMPs, ADAMTS, aggrecan, collagen-II, NF-κB and PI3K/AKT signal pathway was detected by Western blot. In this study, we found that phloretin significantly inhibited the IL-1β-induced production of NO, PGE2, TNF-α and IL-6, expression of COX-2, iNOS, MMP-3, MMP-13 and ADAMTS-5, degradation of aggrecan and collagen-II in human OA chondrocytes. Furthermore, phloretin dramatically suppressed IL-1β-stimulated PI3K/Akt phosphorylation and NF-kB activation in human OA chondrocytes. In addition, treatment of phloretin not only prevented the destruction of cartilage and the thickening of subchondral bone but also relieved synovitis in mice OA models. Also, the immunohistochemistry results showed that phloretin significantly decreased the expression of MMP-13 and ADAMTS-5 and increased the expression of collagen-II and aggrecan in mice OA. Taken together, these results suggest that phloretin may be a potential agent in the treatment of OA.

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Publication details

The article was received on 03 Aug 2017, accepted on 06 Nov 2017 and first published on 07 Nov 2017


Article type: Paper
DOI: 10.1039/C7FO01199G
Citation: Food Funct., 2017, Accepted Manuscript
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    The protective effect of phloretin in osteoarthritis: a in vitro and in vivo study.

    W. Zheng, C. Chen, C. Zhang, L. Cai and H. Chen, Food Funct., 2017, Accepted Manuscript , DOI: 10.1039/C7FO01199G

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