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N‐[2‐(4‐benzoyl‐1‐piperazinyl)phenyl]‐2‐(4‐chlorophenoxy) acetamide is a novel inhibitor of resorptive bone loss in mice
The dynamic balance between bone formation and bone resorption is vital for the retention of bone mass. The abnormal activation of osteoclasts, unique cells that degrade the bone matrix, may result in many bone diseases such as osteoporosis. Osteoporosis, a bone metabolism disease, occurs when extre...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
John Wiley and Sons Inc.
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7875930/ https://www.ncbi.nlm.nih.gov/pubmed/33369010 http://dx.doi.org/10.1111/jcmm.16228 |
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author | Chen, Zhihao Cho, Eunjin Ding, Mina Seong, Jihyoun Che, Xiangguo Lee, Sunwoo Park, Byung‐Ju Choi, Je‐Yong Lee, Tae‐Hoon |
author_facet | Chen, Zhihao Cho, Eunjin Ding, Mina Seong, Jihyoun Che, Xiangguo Lee, Sunwoo Park, Byung‐Ju Choi, Je‐Yong Lee, Tae‐Hoon |
author_sort | Chen, Zhihao |
collection | PubMed |
description | The dynamic balance between bone formation and bone resorption is vital for the retention of bone mass. The abnormal activation of osteoclasts, unique cells that degrade the bone matrix, may result in many bone diseases such as osteoporosis. Osteoporosis, a bone metabolism disease, occurs when extreme osteoclast‐mediated bone resorption outstrips osteoblast‐related bone synthesis. Therefore, it is of great interest to identify agents that can regulate the activity of osteoclasts and prevent bone loss‐induced bone diseases. In this study, we found that N‐[2‐(4‐benzoyl‐1‐piperazinyl)phenyl]‐2‐(4‐chlorophenoxy) acetamide (PPOAC‐Bz) exerted a strong inhibitory effect on osteoclastogenesis. PPOAC‐Bz altered the mRNA expressions of several osteoclast‐specific marker genes and blocked the formation of mature osteoclasts, suppressing F‐actin belt formation and bone resorption activity in vitro. In addition, PPOAC‐Bz prevented OVX‐induced bone loss in vivo. These findings highlighted the potential of PPOAC‐Bz as a prospective drug for the treatment of osteolytic disorders. |
format | Online Article Text |
id | pubmed-7875930 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | John Wiley and Sons Inc. |
record_format | MEDLINE/PubMed |
spelling | pubmed-78759302021-02-18 N‐[2‐(4‐benzoyl‐1‐piperazinyl)phenyl]‐2‐(4‐chlorophenoxy) acetamide is a novel inhibitor of resorptive bone loss in mice Chen, Zhihao Cho, Eunjin Ding, Mina Seong, Jihyoun Che, Xiangguo Lee, Sunwoo Park, Byung‐Ju Choi, Je‐Yong Lee, Tae‐Hoon J Cell Mol Med Original Articles The dynamic balance between bone formation and bone resorption is vital for the retention of bone mass. The abnormal activation of osteoclasts, unique cells that degrade the bone matrix, may result in many bone diseases such as osteoporosis. Osteoporosis, a bone metabolism disease, occurs when extreme osteoclast‐mediated bone resorption outstrips osteoblast‐related bone synthesis. Therefore, it is of great interest to identify agents that can regulate the activity of osteoclasts and prevent bone loss‐induced bone diseases. In this study, we found that N‐[2‐(4‐benzoyl‐1‐piperazinyl)phenyl]‐2‐(4‐chlorophenoxy) acetamide (PPOAC‐Bz) exerted a strong inhibitory effect on osteoclastogenesis. PPOAC‐Bz altered the mRNA expressions of several osteoclast‐specific marker genes and blocked the formation of mature osteoclasts, suppressing F‐actin belt formation and bone resorption activity in vitro. In addition, PPOAC‐Bz prevented OVX‐induced bone loss in vivo. These findings highlighted the potential of PPOAC‐Bz as a prospective drug for the treatment of osteolytic disorders. John Wiley and Sons Inc. 2020-12-23 2021-02 /pmc/articles/PMC7875930/ /pubmed/33369010 http://dx.doi.org/10.1111/jcmm.16228 Text en © 2020 The Authors. Journal of Cellular and Molecular Medicine published by Foundation for Cellular and Molecular Medicine and John Wiley & Sons Ltd. This is an open access article under the terms of the http://creativecommons.org/licenses/by/4.0/ License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Original Articles Chen, Zhihao Cho, Eunjin Ding, Mina Seong, Jihyoun Che, Xiangguo Lee, Sunwoo Park, Byung‐Ju Choi, Je‐Yong Lee, Tae‐Hoon N‐[2‐(4‐benzoyl‐1‐piperazinyl)phenyl]‐2‐(4‐chlorophenoxy) acetamide is a novel inhibitor of resorptive bone loss in mice |
title |
N‐[2‐(4‐benzoyl‐1‐piperazinyl)phenyl]‐2‐(4‐chlorophenoxy) acetamide is a novel inhibitor of resorptive bone loss in mice |
title_full |
N‐[2‐(4‐benzoyl‐1‐piperazinyl)phenyl]‐2‐(4‐chlorophenoxy) acetamide is a novel inhibitor of resorptive bone loss in mice |
title_fullStr |
N‐[2‐(4‐benzoyl‐1‐piperazinyl)phenyl]‐2‐(4‐chlorophenoxy) acetamide is a novel inhibitor of resorptive bone loss in mice |
title_full_unstemmed |
N‐[2‐(4‐benzoyl‐1‐piperazinyl)phenyl]‐2‐(4‐chlorophenoxy) acetamide is a novel inhibitor of resorptive bone loss in mice |
title_short |
N‐[2‐(4‐benzoyl‐1‐piperazinyl)phenyl]‐2‐(4‐chlorophenoxy) acetamide is a novel inhibitor of resorptive bone loss in mice |
title_sort | n‐[2‐(4‐benzoyl‐1‐piperazinyl)phenyl]‐2‐(4‐chlorophenoxy) acetamide is a novel inhibitor of resorptive bone loss in mice |
topic | Original Articles |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7875930/ https://www.ncbi.nlm.nih.gov/pubmed/33369010 http://dx.doi.org/10.1111/jcmm.16228 |
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