Triptolide: pharmacological spectrum, biosynthesis, chemical synthesis and derivatives

Theranostics. 2021 May 24;11(15):7199-7221. doi: 10.7150/thno.57745. eCollection 2021.

Abstract

Triptolide, an abietane-type diterpenoid isolated from Tripterygium wilfordii Hook. F., has significant pharmacological activity. Research results show that triptolide has obvious inhibitory effects on many solid tumors. Therefore, triptolide has become one of the lead compounds candidates for being the next "blockbuster" drug, and multiple triptolide derivatives have entered clinical research. An increasing number of researchers have developed triptolide synthesis methods to meet the clinical need. To provide new ideas for researchers in different disciplines and connect different disciplines with researchers aiming to solve scientific problems more efficiently, this article reviews the research progress made with analyzes of triptolide pharmacological activity, biosynthetic pathways, and chemical synthesis pathways and reported in toxicological and clinical studies of derivatives over the past 20 years, which have laid the foundation for subsequent researchers to study triptolide in many ways.

Keywords: Biological activities; Biosynthesis; Chemical synthesis; Tripterygium wilfordii; Triptolide.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Agents, Phytogenic* / biosynthesis
  • Antineoplastic Agents, Phytogenic* / chemical synthesis
  • Antineoplastic Agents, Phytogenic* / therapeutic use
  • Diterpenes* / chemical synthesis
  • Diterpenes* / metabolism
  • Diterpenes* / therapeutic use
  • Epoxy Compounds / chemical synthesis
  • Epoxy Compounds / metabolism
  • Epoxy Compounds / therapeutic use
  • Humans
  • Phenanthrenes* / chemical synthesis
  • Phenanthrenes* / metabolism
  • Phenanthrenes* / therapeutic use
  • Tripterygium* / chemistry
  • Tripterygium* / metabolism

Substances

  • Antineoplastic Agents, Phytogenic
  • Diterpenes
  • Epoxy Compounds
  • Phenanthrenes
  • triptolide