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Cellular pharmacology studies of shikonin derivatives†
Article first published online: 15 MAY 2002
Copyright © 2002 John Wiley & Sons, Ltd.
Volume 16, Issue 3, pages 199–209, May 2002
How to Cite
Chen, X., Yang, L., Oppenheim, J. J. and Howard, O. M. Z. (2002), Cellular pharmacology studies of shikonin derivatives. Phytother. Res., 16: 199–209. doi: 10.1002/ptr.1100
- Issue published online: 15 MAY 2002
- Article first published online: 15 MAY 2002
- Manuscript Accepted: 8 FEB 2002
- Manuscript Revised: 29 NOV 2001
- Manuscript Received: 15 AUG 2001
- National Cancer Institute
- Complementary and Alternative Medicine Program of National Institutes of Health. Grant Number: Y2-AT-9002
- cellular pharmacology;
- anti tumour;
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.