Cellular pharmacology studies of shikonin derivatives

• Published in: Phytotherapy research 2002-05, Vol.16 (3), p.199-209
• Main Authors: Chen, Xin, Yang, Lu, Oppenheim, Joost J., Howard, O. M. Zack
• Format: Article
• Language: English
• Subjects: Animals; anti tumour; Anti-Infective Agents - pharmacology; Anti-Inflammatory Agents, Non-Steroidal - chemistry; Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics; Anti-Inflammatory Agents, Non-Steroidal - pharmacology; antiinflammatory; Antineoplastic Agents, Phytogenic - pharmacology; Biological and medical sciences; cellular pharmacology; General pharmacology; Granuloma - drug therapy; Humans; Inflammation - drug therapy; Lithospermum; Mast Cells - drug effects; Medical sciences; Naphthoquinones - chemistry; Naphthoquinones - pharmacokinetics; Naphthoquinones - pharmacology; Neoplasms - drug therapy; Neutrophils - drug effects; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; Phytotherapy; Plant Extracts - pharmacokinetics; Plant Extracts - pharmacology; Platelet Aggregation Inhibitors - pharmacology; Prostaglandin-Endoperoxide Synthases - drug effects; Respiratory Burst - drug effects; shikonin; Signal Transduction - drug effects; Wound Healing - drug effects; Zicao
• ISSN: 0951-418X; 1099-1573
• 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. Published in 2002 by John Wiley & Sons, Ltd.