首页> 外国专利> Composition for prevention or treatment of bone disease containing skullcapflavone derivatives or pharmaceutically acceptable salts thereof as an active ingredient

Composition for prevention or treatment of bone disease containing skullcapflavone derivatives or pharmaceutically acceptable salts thereof as an active ingredient

机译:包含头骨黄酮衍生物或其药学上可接受的盐作为有效成分的预防或治疗骨病的组合物

摘要

The present invention relates to a pharmaceutical composition for preventing or treating bone diseases, comprising skullcapflavone derivatives or pharmaceutically acceptable salts thereof as an active ingredient. According to the present invention, it was confirmed that when BMM cells are treated with RANKL in the presence of the skullcapflavone derivatives, the differentiation of osteoclasts is significantly suppressed, and the expressions of the following members are suppressed: NFATc1 related to the differentiation of osteoclasts and target genes thereof; c-Fos which is known to be an upstream regulator of NFATc1; MAPKs and Src-AKT which are activated by RANKL; CREB-PGC-1 which is involved in mitochondrial biogenesis and target genes thereof; and caveolin-1 which promotes the differentiation of osteoclasts. Additionally, as the expressions of a redox-sensitive transcriptional factor, Nrf2 and target protein thereof which is an antioxidant enzyme, and FOXO1 and catalase are increased, the production of active oxygen species is decreased, bone resorption function of osteoclasts is reduced, and inflammation-induced bone damage is suppressed. Accordingly, the skullcapflavone derivatives of the present invention can be beneficially used in preventing or treating bone diseases.
机译:本发明涉及一种用于预防或治疗骨疾病的药物组合物,该药物组合物包含黄褐黄酮衍生物或其药学上可接受的盐作为活性成分。根据本发明,证实了当在头骨黄酮衍生物存在下用RANKL处理BMM细胞时,破骨细胞的分化被显着抑制,并且以下成员的表达被抑制:与破骨细胞的分化有关的NFATc1。及其靶基因; c-Fos,已知是NFATc1的上游调节剂; RANKL激活的MAPK和Src-AKT;与线粒体生物发生有关的CREB-PGC-1及其靶基因;和Caveolin-1促进破骨细胞的分化。另外,随着氧化还原敏感性转录因子,作为抗氧化酶的Nrf2及其靶蛋白,以及FOXO1和过氧化氢酶的表达增加,活性氧的产生减少,破骨细胞的骨吸收功能降低,并且炎症诱导的骨损伤被抑制。因此,本发明的黄芪黄酮衍生物可以有益地用于预防或治疗骨疾病。

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