Shikonin extracted from medicinal Chinese herbs exerts anti-inflammatory effect via proteasome inhibition

Li Lu, Aiping Qin, Hongbiao Huang, Ping Zhou, Chuanyin Zhang, Ningning Liu, Shujue Li, Guanmei Wen, Change Zhang, Weihua Dong, Xuejun Wang, Q. Ping Dou, Jinbao Liu

Research output: Contribution to journalArticlepeer-review

143 Scopus citations


Shikonin, extracted from medicinal Chinese herb (Lithospermum erythrorhizo), was reported to exert anti-inflammatory and anti-cancer effects both in vitro and in vivo. We have found that proteasome was a molecular target of shikonin in tumor cells, but whether shikonin targets macrophage proteasome needs to be investigated. In the current study, we report that shikonin inhibited inflammation in mouse models as efficiently as dexamethasone. Shikonin at 4 μM reduced the Lipopolysaccharides (LPS)-mediated TNFα release in rat primary macrophage cultures, and blocked the translocation of p65-NF-κB from the cytoplasm to the nucleus, associated with decreased proteasomal activity. Consistently, shikonin accumulated IκB-α, an inhibitor of NF-κB, and ubiquitinated proteins in rat primary macrophage cultures, demonstrating that the proteasome is a target of shikonin under inflammatory conditions. Shikonin also induced macrophage cell apoptosis and cell death. These results demonstrate for the first time that proteasome inhibition by shikonin contributes to its anti-inflammatory effect. The novel finding about macrophage proteasome as a target of shikonin suggests that this medicinal compound has great potential to be developed into an anti-inflammatory agent.

Original languageEnglish (US)
Pages (from-to)242-247
Number of pages6
JournalEuropean Journal of Pharmacology
Issue number2-3
StatePublished - May 11 2011
Externally publishedYes


  • Inflammation
  • Macrophage
  • Proteasome inhibitor
  • Shikonin

ASJC Scopus subject areas

  • Pharmacology


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