Cellular pharmacology studies of shikonin derivatives

Phytother Res. 2002 May;16(3):199-209. doi: 10.1002/ptr.1100.


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.

Publication types

  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Animals
  • Anti-Infective Agents / pharmacology
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Antineoplastic Agents, Phytogenic / pharmacology
  • Granuloma / drug therapy
  • Humans
  • Inflammation / drug therapy
  • Lithospermum*
  • Mast Cells / drug effects
  • Naphthoquinones / chemistry
  • Naphthoquinones / pharmacokinetics
  • Naphthoquinones / pharmacology*
  • Neoplasms / drug therapy
  • Neutrophils / drug effects
  • Phytotherapy
  • Plant Extracts / pharmacokinetics
  • Plant Extracts / pharmacology
  • Platelet Aggregation Inhibitors / pharmacology
  • Prostaglandin-Endoperoxide Synthases / drug effects
  • Respiratory Burst / drug effects
  • Signal Transduction / drug effects
  • Wound Healing / drug effects


  • Anti-Infective Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Antineoplastic Agents, Phytogenic
  • Naphthoquinones
  • Plant Extracts
  • Platelet Aggregation Inhibitors
  • shikonin
  • Prostaglandin-Endoperoxide Synthases