Cellular pharmacology studies of shikonin derivatives

Authors

  • Xin Chen,

    1. Laboratory of Molecular Immunoregulation, Division of Basic Sciences, National Cancer Institute-Frederick, Frederick, MD 21702-1201, USA
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  • Lu Yang,

    1. Laboratory of Molecular Immunoregulation, Division of Basic Sciences, National Cancer Institute-Frederick, Frederick, MD 21702-1201, USA
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  • Joost J. Oppenheim,

    1. Laboratory of Molecular Immunoregulation, Division of Basic Sciences, National Cancer Institute-Frederick, Frederick, MD 21702-1201, USA
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  • O. M. Zack Howard

    Corresponding author
    1. Laboratory of Molecular Immunoregulation, Division of Basic Sciences, National Cancer Institute-Frederick, Frederick, MD 21702-1201, USA
    • Laboratory of Molecular Immunoregulation, Division of Basic Sciences, National Cancer Institute-Frederick, Frederick, MD 21702-1201, USA
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  • The content of this publication does not necessarily reflect the views or policies of the Department of Health and Human Services, nor does mention of trade names, commercial products, or organization imply endorsement by the US Government.

Abstract

The naphthoquinone pigment, shikonin, isolated from Lithospermum erythrorhizon Sieb. et Zucc.(Boraginaceae) and its derivatives are the active components isolated from the Chinese herbal therapeutic, Zicao. Historically, Zicao root extracts have been used to treat macular eruption, measles, sore-throat, carbuncles and burns. Multiple pharmacological actions have been attributed to shikonin, e.g. antiinflammatory, antigonadotropic and anti-HIV-1 activity. In this review, several therapeutic applications of shikonin will be summarized including its pleiotropic, antiinflammatory and antitumour effects. Widely diverse and sometimes conflicting activities have been attributed to shikonin, e.g. wound healing, enhanced granuloma formation, suppression of local acute inflammatory reactions, inhibition of angiogenesis, inhibition of select chemokine ligands, inhibition of DNA topoisomerase activity, inhibition of platelet activation and antimicrobial activity. Comparison of the various reported mechanisms of action for shikonin lead us to hypothesize that shikonin is an effective inhibitor of protein–protein interaction with multiple targets in both the intracellular and extracellular compartments. This general inhibitory effect can account for the broad spectrum of shikonin biological and pharmacological activities. Published in 2002 by John Wiley & Sons, Ltd.

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