title: Triptolide: progress on research in pharmacodynamics and toxicology.
abstract: BACKGROUND
  Tripterygium wilfordii Hook. f. (Tripterygium wilfordii), also known as Huangteng and gelsemium elegan, is a traditional Chinese medicine that has been marketed in China as Tripterygium wilfordii glycoside tablets. Triptolide (TP), an active component in Tripterygium wilfordii extracts, has been used to treat various diseases, including lupus, cancer, rheumatoid arthritis and nephritic syndrome. This review summarizes recent developments in the research on the pharmacodynamics, pharmacokinetics, pharmacy and toxicology of TP, with a focus on its novel mechanism of reducing toxicity. This review provides insight for future studies on traditional Chinese medicine, a field that is both historically and currently important.
  
  
  METHODS
  We included studies published primarily within the last five years that were available in online academic databases (e.g., PubMed, Google Scholar, CNKI, SciFinder and Web of Science).
  
  
  RESULTS
  TP has a long history of use in China because it displays multiple pharmacological activities, including anti-rheumatism, anti-inflammatory, anti-tumor and neuroprotective properties. It has been widely used for the treatment of various diseases, such as rheumatoid arthritis, nephritic syndrome, lupus, Behcet׳s disease and central nervous system diseases. Recently, numerous breakthroughs have been made in our understanding of the pharmacological efficacy of TP. Although TP has been marketed as a traditional Chinese medicine, its multi-organ toxicity prevents it from being widely used in clinical practice.
  
  
  CONCLUSIONS
  Triptolide, a biologically active natural product extracted from the root of Tripterygium wilfordii, has shown promising pharmacological effects, particularly as an anti-tumor agent. Currently, in anti-cancer research, more effort should be devoted to investigating effective anti-tumor targets and confirming the anti-tumor spectrum and clinical indications of novel anti-tumor pro-drugs. To apply TP appropriately, with high efficacy and low toxicity, the safety and non-toxic dose range for specific target organs and diseases should be determined, the altered pathways and mechanisms of exposure need to be clarified, and an early warning system for toxicity needs to be established. With further in-depth study of the efficacy and toxicity of TP, we believe that TP will become a promising multi-use drug with improved clinical efficacy and safety in the future.
authors.affiliation: Jiangsu Center of Drug Screening, China Pharmaceutical University, Nanjing 210009, China. Electronic address: lixiaojiaoyang@163.com.
authors.forename: Xiao-Jiaoyang
authors.initials: XJ
authors.lastname: Li
authors.affiliation: Jiangsu Center of Drug Screening, China Pharmaceutical University, Nanjing 210009, China; Key Laboratory of Drug Quality Control and Pharmacovigilance, China Pharmaceutical University, Nanjing 210009, China. Electronic address: beaglejiang@cpu.edu.cn.
authors.forename: Zhen-Zhou
authors.initials: ZZ
authors.lastname: Jiang
authors.affiliation: Jiangsu Center of Drug Screening, China Pharmaceutical University, Nanjing 210009, China; Jiangsu Center for Pharmacodynamics Research and Evaluation, China Pharmaceutical University, Nanjing 210009, China. Electronic address: lyonzhang@163.com.
authors.forename: Lu-yong
authors.initials: LY
authors.lastname: Zhang
mesh_terms: D000818:Animals; D004224:Diterpenes / Q000009:adverse effects / Q000302:isolation & purification / Q000494:pharmacology*; D004365:Drugs, Chinese Herbal / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D004852:Epoxy Compounds / Q000009:adverse effects / Q000302:isolation & purification / Q000494:pharmacology; D020834:Ethnopharmacology; D006801:Humans; D008516:Medicine, Chinese Traditional / Q000379:methods; D010616:Phenanthrenes / Q000009:adverse effects / Q000302:isolation & purification / Q000494:pharmacology*; D029757:Tripterygium / Q000737:chemistry*
chemical_list: D004224:Diterpenes; D004365:Drugs, Chinese Herbal; D004852:Epoxy Compounds; D010616:Phenanthrenes; C001899:triptolide
keywords: Anti-tumor; Metabolism; Toxicity; Tripterygium wilfordii Hook. f.; Triptolide; Triptolide (PubChem CID: 107985)