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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...

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Autores principales: Chen, Zhihao, Cho, Eunjin, Ding, Mina, Seong, Jihyoun, Che, Xiangguo, Lee, Sunwoo, Park, Byung‐Ju, Choi, Je‐Yong, Lee, Tae‐Hoon
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2020
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.
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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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