title: Shikonin and its derivatives: a patent review.
abstract: BACKGROUND
  Shikonin and its derivatives are the main components of red pigment extracts from Lithospermum erythrorhizon, whose medicinal properties have been confirmed for a long history, and have aroused great interest as the hallmark molecules responsible for their significant biological activities, especially for their striking anticancer effects.
  
  
  METHODS
  Areas covered in this paper include a review of the total synthesis, biological effects and mechanisms of shikonin and its derivatives for their anticancer activities in the past decade, basing on literature and patents. The current state and problems are also discussed.
  
  
  CONCLUSIONS
  At present, screening for anticancer shikonin derivatives is based on cellular level to find compounds with stronger cytotoxicity. Though several compounds have been discovered with striking cytotoxicity in vitro, however, no selectivity was observed and undoubtedly, the further outcomes have been disappointing because of their great damage to normal cells. Meanwhile, the presumed mechanisms of action are also established in terms of their cytotoxicity. From a pharmacological point of view, most of the shikonin derivatives are at an early stage of their development, and thus it is difficult to determine the exact effectiveness in cancer treatment. With research in this field going deeper, it can be expected that, despite the difficulties, shikonin derivatives as potential anticancer agents will soon follow.
authors: Shanghai Jiaotong University, School of Pharmacy, 800 Dongchun Road, Shanghai 200240, PR China. ssli@sjtu.edu.cn
authors: Rubing
authors: R
authors: Wang
authors: Runting
authors: R
authors: Yin
authors: Wen
authors: W
authors: Zhou
authors: Defeng
authors: D
authors: Xu
authors: Shaoshun
authors: S
authors: Li
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000302:isolation & purification / Q000494:pharmacology*; D015195:Drug Design; D006801:Humans; D029684:Lithospermum / Q000737:chemistry*; D009285:Naphthoquinones / Q000302:isolation & purification / Q000494:pharmacology*; D009369:Neoplasms / Q000188:drug therapy; D010330:Patents as Topic; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D009285:Naphthoquinones; D010936:Plant Extracts; C016101:shikonin