Important note: Information in this article was accurate in October 2003. The state of the art may have changed since the publication date. |
AIDSWEEKLY Plus; Monday, October 20, 2003
Staff Medical Writers
"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)," researchers in the United States explained. "G protein-coupled chemokine receptors are used by HIV-1 as coreceptors to enter the host cells."
In a recent study, X. Chen and coauthors at the National Cancer Institute "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)," they wrote in the journal Antimicrobial Agents and Chemotherapy.
"Shikonin downregulated 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)," published data indicated. "CCR5 mRNA expression was also downregulated 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 (IC50s) 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," according to the report.
"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," the researchers concluded. "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."
Chen and colleagues published their study in Antimicrobial Agents and Chemotherapy (Shikonin, a component of Chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2003 Sep;47(9):2810-6.
For additional information, contact O.M.Z. Howard, NCI, Molecular Immunoregulation Laboratory, P.O. Box B, Bldg. 560 Room 31-19, Frederick, MD 21702, USA.
The publisher of the journal Antimicrobial Agents and Chemotherapy can be contacted at: American Society for Microbiology, 1752 N St. NW, Washington, DC 20036-2904, USA.
The information in this article comes under the major subject areas of AIDS & HIV, Herbal Medicine and Pharmaceutical & Drug Development.
This article was prepared by AIDS Weekly editors from staff and other reports.
Reference
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", Antimicrob Agents Chemother. 2003 Sep;47(9):2810-6
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