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Shikonin, a component of Chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type 1

  1. Author:
    Chen, X.
    Yang, L.
    Zhang, N.
    Turpin, J. A.
    Buckheit, R. W.
    Osterling, C.
    Oppenheim, J. J.
    Howard, O. M. Z.

  2. Author Address

    NCI, Mol Immunoregulat Lab, BO Box B,Bldg 560 Rm 31-19, Frederick, MD 21702 USA NCI, Mol Immunoregulat Lab, Frederick, MD 21702 USA NCI, Basic Res Program, SAIC Frederick Inc, Frederick, MD 21702 USA TherImmune Res Corp, Gaithersburg, MD 20879 USA Howpin Int Consulting, Frederick, MD 21703 USA So Res Inst, Infect Dis Res Dept, Frederick, MD 21701 USA Howard OMZ NCI, Mol Immunoregulat Lab, BO Box B,Bldg 560 Rm 31-19, Frederick, MD 21702 USA
    1. Year: 2003
  2. Journal: Antimicrobial Agents and Chemotherapy
    1. 47
    2. 9
    3. Pages: 2810-2816
  4. Type of Article: Article
  1. Abstract:

    Shikonin is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities, including inhibition of human immunodeficiency virus (HIV) type 1 (HIV- 1). G protein-coupled chemokine receptors are used by HIV-1 as coreceptors to enter the host cells. In this study, we assessed the effects of shikonin on chemokine receptor function and HIV- 1 replication. The results showed that, at nanomolar concentrations, shikonin inhibited monocyte chemotaxis and calcium flux in response to a variety of CC chemokines (CCL2 [monocyte chemoattractant protein 1], CCL3 [macrophage inflammatory protein 1alpha], and CCL5 [regulated upon activation, normal T-cell expressed and secreted protein]), the CXC chemokine (CXCL12 [stromal cell-derived factor 1alpha]), and classic chemoattractants (formylmethionyl-leucine- phenylalanine and complement fraction C5a). Shikonin down- regulated surface expression of CCR5, a primary HIV-1 coreceptor, on macrophages to a greater degree than the other receptors (CCR1, CCR2, CXCR4, and the formyl peptide receptor) did. CCR5 mRNA expression was also down-regulated by the compound. Additionally, shikonin inhibited the replication of a multidrug-resistant strain and pediatric clinical isolates of HIV in human peripheral blood mononuclear cells, with 50% inhibitory concentrations (IC(50)s) ranging from 96 to 366 nM. Shikonin also effectively inhibited the replication of the HIV Ba-L isolate in monocytes/macrophages, with an IC50 of 470 nM. Our results suggest that the anti-HIV and anti-inflammatory activities of shikonin may be related to its interference with chemokine receptor expression and function. Therefore, shikonin, as a naturally occurring, low-molecular-weight pan- chemokine receptor inhibitor, constitutes a basis for the development of novel anti-HIV therapeutic agents.

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