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乌龙茶二氢黄酮 B 通过抑制 p38MAPK 激活抑制破骨细胞生成。

Inhibitory effect of oolonghomobisflavan B on osteoclastogenesis by suppressing p38 MAPK activation.

机构信息

Department of Oral Pathology and Regenerative Medicine, School of Dentistry, IHBR, Kyungpook National University, Daegu 41940, Republic of Korea.

Department of Food Science and Biotechnology, Daegu University, Gyeongsan 38453, Republic of Korea.

出版信息

Bioorg Med Chem Lett. 2020 Sep 15;30(18):127429. doi: 10.1016/j.bmcl.2020.127429. Epub 2020 Jul 21.

Abstract

Suppression of differentiation and/or function of osteoclasts is considered an effective therapeutic strategy for osteolytic bone diseases such as periodontitis and osteoporosis. Evidence regarding the health benefits of oolong tea consumption is accumulating, and tea polyphenols have various pharmacological properties such as anti-cancer and anti-diabetes effects. In this study, we investigated the effect of oolonghomobisflavan B (OFB), a polyphenolic compound in oolong tea, on osteoclast differentiation. OFB suppressed receptor activator of nuclear factor-κB (RANKL)-induced formation of tartate-resistant acid phosphatase-positive multinuclear cells without cytotoxicity. OFB also significantly attenuated p38 phosphorylation, which is essential for RANKL-induced osteoclastogenesis, and inhibited the expressions of nuclear factor of activated T cells, cytoplasmic 1 (NFATc1) and osteoclast-specific target genes, including dendritic cell-specific transmembrane protein and cathepsin K. Our findings suggest that OFB exhibits an anti-osteoclastogenic activity by inhibiting RANKL-mediated p38 activation, which is useful for the prevention and treatment of osteolytic bone diseases.

摘要

抑制破骨细胞的分化和/或功能被认为是治疗牙周炎和骨质疏松症等溶骨性骨病的有效策略。关于乌龙茶消费对健康益处的证据正在不断积累,茶多酚具有多种药理作用,如抗癌和抗糖尿病作用。在这项研究中,我们研究了乌龙茶同源双黄烷 B(OFB)对破骨细胞分化的影响。OFB 抑制核因子-κB 受体激活剂(RANKL)诱导的抗酒石酸酸性磷酸酶阳性多核细胞的形成,而没有细胞毒性。OFB 还显著抑制了 p38 磷酸化,p38 磷酸化对于 RANKL 诱导的破骨细胞生成至关重要,并抑制了核因子活化 T 细胞、细胞质 1(NFATc1)和破骨细胞特异性靶基因的表达,包括树突状细胞特异性跨膜蛋白和组织蛋白酶 K。我们的研究结果表明,OFB 通过抑制 RANKL 介导的 p38 激活表现出抗破骨细胞生成活性,这对于预防和治疗溶骨性骨病是有用的。

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