表环氧愈创木薁内酯通过抑制 ERK1/2 和 NFATc1 信号通路抑制破骨细胞生成并抵抗 OVX 诱导的骨质疏松症。

Epoxymicheliolide inhibits osteoclastogenesis and resists OVX-induced osteoporosis by suppressing ERK1/2 and NFATc1 signaling.

机构信息

Research Centre for Regenerative Medicine, Orthopaedic Department, the First Affiliated Hospital of Guangxi Medical University, Guangxi, China; Collaborative Innovation Centre of Regenerative Medicine and Medical BioResource Development and Application, Guangxi Medical University, Nanning, Guangxi 530021, China.

Guangzhou Medical University, Guangzhou, Guangdong 510120, China.

出版信息

Int Immunopharmacol. 2022 Jun;107:108632. doi: 10.1016/j.intimp.2022.108632. Epub 2022 Mar 3.

Abstract

The hyperactivity of osteoclasts caused by postmenopausal estrogen deficiency plays an imperative role in the progression of osteoporosis. Although osteoporosis-related drugs have been widely used to alleviate this disorder, there is an urgent need for drugs with fewer side effects. In this study, we found that epoxymicheliolide (EMCL), a derivative of parthenolide, has a high affinity to ERK1/2, but the treatment and mechanism of osteoporosis using EMCL have not been explored. Therefore, we intended to figure out the effects and potential mechanisms of EMCL on RANKL-stimulated osteoclast formation and function in vitro, construct an OVX murine model to simulate the therapeutic effects of EMCL on estrogen-deficient bone loss subsequently. EMCL restrained the phosphorylation of ERK1/2 in the RANKL-stimulated MAPK pathway, which in sequence inhibited the transcription and expression of the main osteoclast transcription factor NFATc1, resulting in the suppression of osteoclastogenesis and bone resorption. However, the same concentration of EMCL did not affect the proliferation and differentiation of osteoblasts. In vivo experiments showed that EMCL can significantly resist osteoporosis caused by estrogen deficiency, alleviate bone loss, and reduce the number of osteoclasts. These results suggest that EMCL can reduce osteoclast production and bone resorption by inhibiting ERK1/2 phosphorylation and NFATc1 entering the nucleus, and could be used in the treatment of osteoporosis caused by estrogen deficiency and hyperactivity of osteoclasts.

摘要

破骨细胞的过度活跃是绝经后雌激素缺乏导致骨质疏松症进展的重要原因。尽管已经广泛使用骨质疏松相关药物来缓解这种疾病,但仍迫切需要副作用更少的药物。在这项研究中,我们发现,来源于小白菊内酯的环氧小白菊内酯(EMCL)对 ERK1/2 具有很高的亲和力,但尚未探索 EMCL 治疗和治疗骨质疏松症的机制。因此,我们旨在研究 EMCL 对体外 RANKL 刺激的破骨细胞形成和功能的影响及其潜在机制,随后构建 OVX 小鼠模型模拟 EMCL 对雌激素缺乏性骨丢失的治疗作用。EMCL 抑制了 RANKL 刺激的 MAPK 通路中 ERK1/2 的磷酸化,从而依次抑制了主要破骨细胞转录因子 NFATc1 的转录和表达,导致破骨细胞生成和骨吸收受到抑制。然而,相同浓度的 EMCL 并不影响成骨细胞的增殖和分化。体内实验表明,EMCL 能显著抵抗雌激素缺乏引起的骨质疏松症,减轻骨丢失,减少破骨细胞数量。这些结果表明,EMCL 可通过抑制 ERK1/2 磷酸化和 NFATc1 进入细胞核来减少破骨细胞的产生和骨吸收,可用于治疗雌激素缺乏和破骨细胞过度活跃引起的骨质疏松症。

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