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Silibinin Inhibits LPS-Induced Macrophage Activation by Blocking p38 MAPK in RAW 264.7 Cells

We demonstrate herein that silibinin, a polyphenolic flavonoid compound isolated from milk thistle (Silybum marianum), inhibits LPS-induced activation of macrophages and production of nitric oxide (NO) in RAW 264.7 cells. Western blot analysis showed silibinin inhibits iNOS gene expression. RT-PCR s...

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Autores principales: Youn, Cha Kyung, Park, Seon Joo, Lee, Min Young, Cha, Man Jin, Kim, Ok Hyeun, You, Ho Jin, Chang, In Youp, Yoon, Sang Pil, Jeon, Young Jin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Korean Society of Applied Pharmacology 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3819897/
https://www.ncbi.nlm.nih.gov/pubmed/24244809
http://dx.doi.org/10.4062/biomolther.2013.044
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author Youn, Cha Kyung
Park, Seon Joo
Lee, Min Young
Cha, Man Jin
Kim, Ok Hyeun
You, Ho Jin
Chang, In Youp
Yoon, Sang Pil
Jeon, Young Jin
author_facet Youn, Cha Kyung
Park, Seon Joo
Lee, Min Young
Cha, Man Jin
Kim, Ok Hyeun
You, Ho Jin
Chang, In Youp
Yoon, Sang Pil
Jeon, Young Jin
author_sort Youn, Cha Kyung
collection PubMed
description We demonstrate herein that silibinin, a polyphenolic flavonoid compound isolated from milk thistle (Silybum marianum), inhibits LPS-induced activation of macrophages and production of nitric oxide (NO) in RAW 264.7 cells. Western blot analysis showed silibinin inhibits iNOS gene expression. RT-PCR showed that silibinin inhibits iNOS, TNF-α, and IL1β. We also showed that silibinin strongly inhibits p38 MAPK phosphorylation, whereas the ERK1/2 and JNK pathways are not inhibited. The p38 MAPK inhibitor abrogated the LPS-induced nitrite production, whereas the MEK-1 inhibitor did not affect the nitrite production. A molecular modeling study proposed a binding pose for silibinin targeting the ATP binding site of p38 MAPK (1OUK). Collectively, this series of experiments indicates that silibinin inhibits macrophage activation by blocking p38 MAPK signaling.
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spelling pubmed-38198972013-11-15 Silibinin Inhibits LPS-Induced Macrophage Activation by Blocking p38 MAPK in RAW 264.7 Cells Youn, Cha Kyung Park, Seon Joo Lee, Min Young Cha, Man Jin Kim, Ok Hyeun You, Ho Jin Chang, In Youp Yoon, Sang Pil Jeon, Young Jin Biomol Ther (Seoul) Articles We demonstrate herein that silibinin, a polyphenolic flavonoid compound isolated from milk thistle (Silybum marianum), inhibits LPS-induced activation of macrophages and production of nitric oxide (NO) in RAW 264.7 cells. Western blot analysis showed silibinin inhibits iNOS gene expression. RT-PCR showed that silibinin inhibits iNOS, TNF-α, and IL1β. We also showed that silibinin strongly inhibits p38 MAPK phosphorylation, whereas the ERK1/2 and JNK pathways are not inhibited. The p38 MAPK inhibitor abrogated the LPS-induced nitrite production, whereas the MEK-1 inhibitor did not affect the nitrite production. A molecular modeling study proposed a binding pose for silibinin targeting the ATP binding site of p38 MAPK (1OUK). Collectively, this series of experiments indicates that silibinin inhibits macrophage activation by blocking p38 MAPK signaling. The Korean Society of Applied Pharmacology 2013-07-30 /pmc/articles/PMC3819897/ /pubmed/24244809 http://dx.doi.org/10.4062/biomolther.2013.044 Text en Copyright ©2013, The Korean Society of Applied Pharmacology http://creativecommons.org/licenses/by-nc/3.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0/) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Articles
Youn, Cha Kyung
Park, Seon Joo
Lee, Min Young
Cha, Man Jin
Kim, Ok Hyeun
You, Ho Jin
Chang, In Youp
Yoon, Sang Pil
Jeon, Young Jin
Silibinin Inhibits LPS-Induced Macrophage Activation by Blocking p38 MAPK in RAW 264.7 Cells
title Silibinin Inhibits LPS-Induced Macrophage Activation by Blocking p38 MAPK in RAW 264.7 Cells
title_full Silibinin Inhibits LPS-Induced Macrophage Activation by Blocking p38 MAPK in RAW 264.7 Cells
title_fullStr Silibinin Inhibits LPS-Induced Macrophage Activation by Blocking p38 MAPK in RAW 264.7 Cells
title_full_unstemmed Silibinin Inhibits LPS-Induced Macrophage Activation by Blocking p38 MAPK in RAW 264.7 Cells
title_short Silibinin Inhibits LPS-Induced Macrophage Activation by Blocking p38 MAPK in RAW 264.7 Cells
title_sort silibinin inhibits lps-induced macrophage activation by blocking p38 mapk in raw 264.7 cells
topic Articles
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3819897/
https://www.ncbi.nlm.nih.gov/pubmed/24244809
http://dx.doi.org/10.4062/biomolther.2013.044
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