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Shikonin, a component of antiinflammatory Chinese herbal medicine, selectively blocks chemokine binding to CC chemokine receptor-1
Chen X.; Oppenheim J.; Howard O.M.Z.
2001-03-12
Source PublicationInternational Immunopharmacology
ISSN15675769
Volume1Issue:2Pages:229-236
Abstract

Shikonin is a chemically characterized component of traditional Chinese herbal medicine and has been shown to possess antiinflammatory activities. We ascertained that shikonin blocked radiolabelled Regulated on Activation, Normal T cell Expressed and Secreted (RANTES) and macrophage inflammatory protein-1 (MIP-1 α) binding to human monocytes with IC values of 3.58 × 10 and 2.57 × 10 M, respectively. In contrast, up to 1.7 × 10 M of shikonin failed to inhibit stromal cell-derived factor-1 (SDF-1 α) binding to the cells. Additionally, shikonin blocked RANTES and MIP-1 α binding to stable CC chemokine receptor-1 (CCR1) transfected human embryonic kidney (HEK)/293 cells with IC values of 2.63 × 10 and 2.57 × 10 M, respectively. However, shikonin inhibited neither RANTES nor MIP-1 α binding to CCR5 transfected HEK/293 cells. Shikonin also did not inhibit monocyte chemoattractant protein-1 (MCP-1) binding to CCR2 cells, eotaxin binding to CCR3 cells, interferon-inducible T cell α-chemoattractant (I-TAC) binding to CXCR3 cells and SDF-1 α binding to CXCR4 cells. Additionally, shikonin inhibited RANTES-induced CCR1 cell migration, but did not inhibit CCR1 cell migration induced by epidermal growth factor (EGF). Our study suggests shikonin may be a target for the future design of more potent, highly selective therapeutics that could be useful antiinflammatory agents for selectively blocking the binding of CCR1 ligands. © 2001 Published by Elsevier Science B.V.

KeywordAntagonist Ccr1 Receptor Binding Shikonin
DOI10.1016/S1567-5769(00)00033-3
URLView the original
Indexed BySCI
WOS Research AreaImmunology ; Pharmacology & Pharmacy
WOS SubjectImmunology ; Pharmacology & Pharmacy
WOS IDWOS:000168328800006
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Cited Times [WOS]:52   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
AffiliationNational Cancer Institute at Frederick
Recommended Citation
GB/T 7714
Chen X.,Oppenheim J.,Howard O.M.Z.. Shikonin, a component of antiinflammatory Chinese herbal medicine, selectively blocks chemokine binding to CC chemokine receptor-1[J]. International Immunopharmacology,2001,1(2):229-236.
APA Chen X.,Oppenheim J.,&Howard O.M.Z..(2001).Shikonin, a component of antiinflammatory Chinese herbal medicine, selectively blocks chemokine binding to CC chemokine receptor-1.International Immunopharmacology,1(2),229-236.
MLA Chen X.,et al."Shikonin, a component of antiinflammatory Chinese herbal medicine, selectively blocks chemokine binding to CC chemokine receptor-1".International Immunopharmacology 1.2(2001):229-236.
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