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| dc.contributor.author | Huang, Shang-En | |
| dc.contributor.author | Sulistyowati, Erna | |
| dc.contributor.author | Chao, Yu-Ying | |
| dc.contributor.author | Wu, Bin-Nan | |
| dc.contributor.author | Dai, Zen-Kong | |
| dc.contributor.author | Hsu, Jong-Hau | |
| dc.contributor.author | Yeh, Jwu-Lai | |
| dc.date.accessioned | 2021-11-18T02:52:20Z | |
| dc.date.available | 2021-11-18T02:52:20Z | |
| dc.date.issued | 2021-05-28 | |
| dc.identifier.uri | https://pubmed.ncbi.nlm.nih.gov/34071594/ | |
| dc.identifier.uri | http://repository.unisma.ac.id/handle/123456789/2578 | |
| dc.description | [ARCHIVES] Copyright Article from : Biomedicines 2021 | en_US |
| dc.description.abstract | Osteoarthritis is a degenerative arthropathy that is mainly characterized by dysregulation of inflammatory responses. KMUP-1, a derived chemical synthetic of xanthine, has been shown to have anti-inflammatory and antioxidant properties. Here, we aimed to investigate the in vitro anti-inflammatory and in vivo anti-osteoarthritis effects of KMUP-1. Protein and gene expressions of inflammation markers were determined by ELISA, Western blotting and microarray, respectively. RAW264.7 mouse macrophages were cultured and pretreated with KMUP-1 (1, 5, 10 µM). The productions of TNF-α, IL-6, MMP-2 and MMP- 9 were reduced by KMUP-1 pretreatment in LPS induced inflammation of RAW264.7 cells. The expressions of iNOS, TNF-α, COX-2, MMP-2 and MMP-9 were also inhibited by KMUP-1 pretreatment. The gene expression levels of TNF and COX families were also downregulated. In addition, KMUP-1 suppressed the activations of ERK, JNK and p38 as well as phosphorylation of IκBα/NF-κB signaling pathways. Furthermore, SIRT1 inhibitor attenuated the inhibitory effect of KMUP-1 in LPS-induced NF-κB activation. In vivo study showed that KMUP-1 reduced mechanical hyperalgesia in monoiodoacetic acid (MIA)-induced rats OA. Additionally, KMUP-1 pretreatment reduced the serum levels of TNF-α and IL-6 in MIA-injected rats. Moreover, macroscopic and histological observation showed that KMUP-1 reduced articular cartilage erosion in rats. Our results demonstrated that KMUP-1 inhibited the inflammatory responses and restored SIRT1 in vitro, alleviated joint-related pain and cartilage destruction in vivo. Taken together, KMUP-1 has the potential to improve MIA-induced articular cartilage degradation by inhibiting the levels and expression of inflammatory mediators suggesting that KMUP-1 might be a potential therapeutic agent for OA. | en_US |
| dc.language.iso | en | en_US |
| dc.publisher | National Library of Medicine | en_US |
| dc.relation.ispartofseries | Biomedicines 2021;Vol. 28, No. 9(6) | |
| dc.subject | Xanthine-derived KMUP-1 | en_US |
| dc.subject | Anti-inflammation | en_US |
| dc.subject | NF-κB | en_US |
| dc.subject | SIRT1 | en_US |
| dc.subject | Osteoarthritis | en_US |
| dc.title | In Vitro Evaluation of the Anti-Inflammatory Effect of KMUP-1 and In Vivo Analysis of Its Therapeutic Potential in Osteoarthritis | en_US |
| dc.type | Article | en_US |
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Publikasi Ilmiah Dosen Program Studi Pendidikan Dokter