Silibinin inhibits LPS-induced macrophage activation by blocking p38 MAPK in RAW 264.7 cells

Cha Kyung Youn, Seon Joo Park, Min Young Lee, Man Jin Cha, Ok Hyeun Kim, Ho Jin You, In Youp Chang, Sang Pil Yoon, Young Jin Jeon

Research output: Contribution to journalArticlepeer-review

46 Scopus citations


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 silib-inin 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.

Original languageEnglish (US)
Pages (from-to)258-263
Number of pages6
JournalBiomolecules and Therapeutics
Issue number4
StatePublished - 2013
Externally publishedYes


  • Macrophages
  • Nitric oxide
  • P38 MAPK
  • Silibinin


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