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溴结构域抑制剂 -N- 甲基吡咯烷酮可预防破骨细胞骨吸收和骨形成蛋白诱导的骨细胞中骨硬化蛋白的表达。

The Bromodomain Inhibitor -Methyl pyrrolidone Prevents Osteoporosis and BMP-Triggered Sclerostin Expression in Osteocytes.

机构信息

Center of Dental Medicine, Oral Biotechnology & Bioengineering, University of Zurich, Plattenstrasse 11, 8032 Zürich, Switzerland.

Department of Pharmacology, Faculty of Dentistry, Mahidol University, Bangkok 10400, Thailand.

出版信息

Int J Mol Sci. 2018 Oct 25;19(11):3332. doi: 10.3390/ijms19113332.


DOI:10.3390/ijms19113332
PMID:30366476
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6275050/
Abstract

(1) Background: In an adult skeleton, bone is constantly renewed in a cycle of bone resorption, followed by bone formation. This coupling process, called bone remodeling, adjusts the quality and quantity of bone to the local needs. It is generally accepted that osteoporosis develops when bone resorption surpasses bone formation. Osteoclasts and osteoblasts, bone resorbing and bone forming cells respectively, are the major target in osteoporosis treatment. Inside bone and forming a complex network, the third and most abundant cells, the osteocytes, have long remained a mystery. Osteocytes are responsible for mechano-sensation and -transduction. Increased expression of the osteocyte-derived bone inhibitor sclerostin has been linked to estrogen deficiency-induced osteoporosis and is therefore a promising target for osteoporosis management. (2) Methods: Recently we showed in vitro and in vivo that NMP (-Methyl-2-pyrrolidone) is a bioactive drug enhancing the BMP-2 (Bone Morphogenetic Protein 2) induced effect on bone formation while blocking bone resorption. Here we tested the effect of NMP on the expression of osteocyte-derived sclerostin. (3) Results: We found that NMP significantly decreased sclerostin mRNA and protein levels. In an animal model of osteoporosis, NMP prevented the estrogen deficiency-induced increased expression of sclerostin. (4) Conclusions: These results support the potential of NMP as a novel therapeutic compound for osteoporosis management, since it preserves bone by a direct interference with osteoblasts and osteoclasts and an indirect one via a decrease in sclerostin expression by osteocytes.

摘要

(1) 背景:在成人骨骼中,骨在骨吸收和骨形成的循环中不断更新。这种耦联过程称为骨重建,它根据局部需要调整骨的质量和数量。当骨吸收超过骨形成时,一般认为会发生骨质疏松症。破骨细胞和成骨细胞分别是骨吸收和骨形成的主要细胞,是骨质疏松症治疗的主要靶点。在骨骼内部形成复杂的网络中,第三丰富的细胞——骨细胞,长期以来一直是个谜。骨细胞负责机械感觉和转导。骨细胞衍生的骨抑制剂硬骨素的表达增加与雌激素缺乏诱导的骨质疏松症有关,因此是骨质疏松症管理的一个有希望的靶点。(2) 方法:最近我们在体外和体内研究表明,NMP(N-甲基-2-吡咯烷酮)是一种具有生物活性的药物,可增强 BMP-2(骨形态发生蛋白 2)对骨形成的作用,同时阻断骨吸收。在这里,我们测试了 NMP 对骨细胞衍生的硬骨素表达的影响。(3) 结果:我们发现 NMP 显著降低了硬骨素 mRNA 和蛋白水平。在骨质疏松症动物模型中,NMP 可预防雌激素缺乏诱导的硬骨素表达增加。(4) 结论:这些结果支持 NMP 作为一种治疗骨质疏松症的新型治疗化合物的潜力,因为它通过直接干扰成骨细胞和破骨细胞以及通过降低骨细胞中硬骨素的表达来间接保护骨骼。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cbf3/6275050/17a6d569fa3d/ijms-19-03332-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cbf3/6275050/c8715fb96668/ijms-19-03332-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cbf3/6275050/d964d11fc04e/ijms-19-03332-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cbf3/6275050/207f12aef49b/ijms-19-03332-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cbf3/6275050/89a1f801be37/ijms-19-03332-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cbf3/6275050/17a6d569fa3d/ijms-19-03332-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cbf3/6275050/c8715fb96668/ijms-19-03332-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cbf3/6275050/d964d11fc04e/ijms-19-03332-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cbf3/6275050/207f12aef49b/ijms-19-03332-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cbf3/6275050/89a1f801be37/ijms-19-03332-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cbf3/6275050/17a6d569fa3d/ijms-19-03332-g005.jpg

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引用本文的文献

[1]
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J Orthop Translat. 2025-5-16

[2]
CGK733 alleviates ovariectomy-induced bone loss through blocking RANKL-mediated Ca oscillations and NF-κB/MAPK signaling pathways.

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[3]
Linagliptin in Combination With Metformin Ameliorates Diabetic Osteoporosis Through Modulating BMP-2 and Sclerostin in the High-Fat Diet Fed C57BL/6 Mice.

Front Endocrinol (Lausanne). 2022

[4]
The regulatory roles of miR-26a in the development of fracture and osteoblasts.

Ann Transl Med. 2022-1

[5]
Effect of N-Vinyl-2-Pyrrolidone (NVP), a Bromodomain-Binding Small Chemical, on Osteoblast and Osteoclast Differentiation and Its Potential Application for Bone Regeneration.

Int J Mol Sci. 2021-10-13

[6]
Potential Functions of the BMP Family in Bone, Obesity, and Glucose Metabolism.

J Diabetes Res. 2021

[7]
The Role of Macrophage in the Pathogenesis of Osteoporosis.

Int J Mol Sci. 2019-4-28

本文引用的文献

[1]
Investigational anabolic agents for the treatment of osteoporosis: an update on recent developments.

Expert Opin Investig Drugs. 2017-8-29

[2]
Sclerostin's role in bone's adaptive response to mechanical loading.

Bone. 2017-3

[3]
BET protein bromodomain inhibitor-based combinations are highly active against post-myeloproliferative neoplasm secondary AML cells.

Leukemia. 2017-3

[4]
Acetylation Reader Proteins: Linking Acetylation Signaling to Genome Maintenance and Cancer.

PLoS Genet. 2016-9-15

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JQ1, a small molecule inhibitor of BRD4, suppresses cell growth and invasion in oral squamous cell carcinoma.

Oncol Rep. 2016-8-24

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The sclerostin-neutralizing antibody AbD09097 recognizes an epitope adjacent to sclerostin's binding site for the Wnt co-receptor LRP6.

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J Leukoc Biol. 2016-10

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Osteocyte differentiation and the formation of an interconnected cellular network in vitro.

Eur Cell Mater. 2016-5-24

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Strontium ranelate increases osteoblast activity.

Tissue Cell. 2016-6

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The epigenetically active small chemical N-methyl pyrrolidone (NMP) prevents estrogen depletion induced osteoporosis.

Bone. 2015-9

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