title: Cellular pharmacology studies of shikonin derivatives.
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.
authors.affiliation: Laboratory of Molecular Immunoregulation, Division of Basic Sciences, National Cancer Institute-Frederick, MD 21702-1201, USA.
authors.forename: Xin
authors.initials: X
authors.lastname: Chen
authors.forename: Lu
authors.initials: L
authors.lastname: Yang
authors.forename: Joost J
authors.initials: JJ
authors.lastname: Oppenheim
authors.forename: M Zack
authors.initials: MZ
authors.lastname: Howard
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000494:pharmacology; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology; D006099:Granuloma / Q000188:drug therapy; D006801:Humans; D007249:Inflammation / Q000188:drug therapy; D029684:Lithospermum; D008407:Mast Cells / Q000187:drug effects; D009285:Naphthoquinones / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D009369:Neoplasms / Q000188:drug therapy; D009504:Neutrophils / Q000187:drug effects; D008517:Phytotherapy; D010936:Plant Extracts / Q000493:pharmacokinetics / Q000494:pharmacology; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology; D011451:Prostaglandin-Endoperoxide Synthases / Q000187:drug effects; D016897:Respiratory Burst / Q000187:drug effects; D015398:Signal Transduction / Q000187:drug effects; D014945:Wound Healing / Q000187:drug effects
chemical_list: D000890:Anti-Infective Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000972:Antineoplastic Agents, Phytogenic; D009285:Naphthoquinones; D010936:Plant Extracts; D010975:Platelet Aggregation Inhibitors; C016101:shikonin; D011451:Prostaglandin-Endoperoxide Synthases