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Isoliquiritigenin Derivatives Inhibit RANKL-Induced Osteoclastogenesis by Regulating p38 and NF-κB Activation in RAW 264.7 Cells

Bone diseases may not be imminently life-threatening or a leading cause of death such as heart diseases or cancers. However, as aging population grows in almost every part of the world, they surely impose significant socioeconomic burden on the society, not to mention the patients and their families...

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Autores principales: Jeong, Seongtae, Lee, Seahyoung, Kim, Kundo, Lee, Yunmi, Lee, Jiyun, Oh, Sena, Choi, Jung-Won, Kim, Sang Woo, Hwang, Ki-Chul, Lim, Soyeon
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7504656/
https://www.ncbi.nlm.nih.gov/pubmed/32867185
http://dx.doi.org/10.3390/molecules25173908
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author Jeong, Seongtae
Lee, Seahyoung
Kim, Kundo
Lee, Yunmi
Lee, Jiyun
Oh, Sena
Choi, Jung-Won
Kim, Sang Woo
Hwang, Ki-Chul
Lim, Soyeon
author_facet Jeong, Seongtae
Lee, Seahyoung
Kim, Kundo
Lee, Yunmi
Lee, Jiyun
Oh, Sena
Choi, Jung-Won
Kim, Sang Woo
Hwang, Ki-Chul
Lim, Soyeon
author_sort Jeong, Seongtae
collection PubMed
description Bone diseases may not be imminently life-threatening or a leading cause of death such as heart diseases or cancers. However, as aging population grows in almost every part of the world, they surely impose significant socioeconomic burden on the society, not to mention the patients and their families. Osteoporosis is the most common type of bone disease, which frequently develops in seniors, especially in postmenopausal women. Although currently several anti-osteoclastic drugs designed to suppress excessive osteoclast activation, a major cause of osteoporosis, are commercially available, accompanying adverse effects ranging from mild to severe have been reported as well. Natural products have become increasingly popular because of their effectiveness with fewer side effects. Isoliquiritigenin (ILG), a natural flavonoid from licorice, has been reported to suppress osteoclast differentiation and activation. In the present study, newly synthesized ILG derivatives were screened for their anti-osteoporotic activity as more potent substitute candidates to ILG. Out of the 12 ILG derivatives tested, two compounds demonstrated significantly improved bone loss in vitro by inhibiting both osteoclastogenesis and osteoclast activity. The results of the present study indicate that these compounds may serve as a potential drug for osteoporosis and warrant further studies to evaluate their in vivo efficacy.
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spelling pubmed-75046562020-09-26 Isoliquiritigenin Derivatives Inhibit RANKL-Induced Osteoclastogenesis by Regulating p38 and NF-κB Activation in RAW 264.7 Cells Jeong, Seongtae Lee, Seahyoung Kim, Kundo Lee, Yunmi Lee, Jiyun Oh, Sena Choi, Jung-Won Kim, Sang Woo Hwang, Ki-Chul Lim, Soyeon Molecules Article Bone diseases may not be imminently life-threatening or a leading cause of death such as heart diseases or cancers. However, as aging population grows in almost every part of the world, they surely impose significant socioeconomic burden on the society, not to mention the patients and their families. Osteoporosis is the most common type of bone disease, which frequently develops in seniors, especially in postmenopausal women. Although currently several anti-osteoclastic drugs designed to suppress excessive osteoclast activation, a major cause of osteoporosis, are commercially available, accompanying adverse effects ranging from mild to severe have been reported as well. Natural products have become increasingly popular because of their effectiveness with fewer side effects. Isoliquiritigenin (ILG), a natural flavonoid from licorice, has been reported to suppress osteoclast differentiation and activation. In the present study, newly synthesized ILG derivatives were screened for their anti-osteoporotic activity as more potent substitute candidates to ILG. Out of the 12 ILG derivatives tested, two compounds demonstrated significantly improved bone loss in vitro by inhibiting both osteoclastogenesis and osteoclast activity. The results of the present study indicate that these compounds may serve as a potential drug for osteoporosis and warrant further studies to evaluate their in vivo efficacy. MDPI 2020-08-27 /pmc/articles/PMC7504656/ /pubmed/32867185 http://dx.doi.org/10.3390/molecules25173908 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Jeong, Seongtae
Lee, Seahyoung
Kim, Kundo
Lee, Yunmi
Lee, Jiyun
Oh, Sena
Choi, Jung-Won
Kim, Sang Woo
Hwang, Ki-Chul
Lim, Soyeon
Isoliquiritigenin Derivatives Inhibit RANKL-Induced Osteoclastogenesis by Regulating p38 and NF-κB Activation in RAW 264.7 Cells
title Isoliquiritigenin Derivatives Inhibit RANKL-Induced Osteoclastogenesis by Regulating p38 and NF-κB Activation in RAW 264.7 Cells
title_full Isoliquiritigenin Derivatives Inhibit RANKL-Induced Osteoclastogenesis by Regulating p38 and NF-κB Activation in RAW 264.7 Cells
title_fullStr Isoliquiritigenin Derivatives Inhibit RANKL-Induced Osteoclastogenesis by Regulating p38 and NF-κB Activation in RAW 264.7 Cells
title_full_unstemmed Isoliquiritigenin Derivatives Inhibit RANKL-Induced Osteoclastogenesis by Regulating p38 and NF-κB Activation in RAW 264.7 Cells
title_short Isoliquiritigenin Derivatives Inhibit RANKL-Induced Osteoclastogenesis by Regulating p38 and NF-κB Activation in RAW 264.7 Cells
title_sort isoliquiritigenin derivatives inhibit rankl-induced osteoclastogenesis by regulating p38 and nf-κb activation in raw 264.7 cells
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7504656/
https://www.ncbi.nlm.nih.gov/pubmed/32867185
http://dx.doi.org/10.3390/molecules25173908
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