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Shikonin, a component of Chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type 1
Chen X.5; Yang L.2; Zhang N.1; Turpin J.A.3; Buckheit R.W.2; Osterling C.4; Oppenheim J.J.1; Howard O.M.Z.1
2003-09-01
Source PublicationAntimicrobial Agents and Chemotherapy
ISSN00664804
Volume47Issue:9Pages:2810-2816
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 1α], and CCL5 [regulated upon activation, normal T-cell expressed and secreted protein]), the CXC chemokine (CXCL12 [stromal cell-derived factor 1α]), 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 (ICs) ranging from 96 to 366 nM. Shikonin also effectively inhibited the replication of the HIV Ba-L isolate in monocytes/macrophages, with an IC 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.

DOI10.1128/AAC.47.9.2810-2816.2003
URLView the original
Indexed BySCI
WOS Research AreaMicrobiology ; Pharmacology & Pharmacy
WOS SubjectMicrobiology ; Pharmacology & Pharmacy
WOS IDWOS:000184988000014
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Cited Times [WOS]:150   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.National Cancer Institute at Frederick
2.TherImmune Research Corporation
3.Howpin International Consulting
4.Southern Research Institute Birmingham
5.SAIC-Frederick
Recommended Citation
GB/T 7714
Chen X.,Yang L.,Zhang N.,et al. Shikonin, a component of Chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type 1[J]. Antimicrobial Agents and Chemotherapy,2003,47(9):2810-2816.
APA Chen X..,Yang L..,Zhang N..,Turpin J.A..,Buckheit R.W..,...&Howard O.M.Z..(2003).Shikonin, a component of Chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type 1.Antimicrobial Agents and Chemotherapy,47(9),2810-2816.
MLA Chen X.,et al."Shikonin, a component of Chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type 1".Antimicrobial Agents and Chemotherapy 47.9(2003):2810-2816.
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