Xanthotoxin (8-methoxypsoralen): A review of its chemistry, pharmacology, pharmacokinetics, and toxicity

Phytother Res. 2022 Oct;36(10):3805-3832. doi: 10.1002/ptr.7577. Epub 2022 Aug 1.

Abstract

Xanthotoxin (XAT) is a natural furanocoumarins, a bioactive psoralen isolated from the fruit of the Rutaceae plant Pepper, which has received increasing attention in recent years due to its wide source and low cost. By collecting and compiling literature on XAT, the results show that XAT exhibits significant activity in the treatment of various diseases, including neuroprotection, skin repair, osteoprotection, organ protection, anticancer, antiinflammatory, antioxidative stress and antibacterial. In this paper, we review the pharmacological activity and potential molecular mechanisms of XAT for the treatment of related diseases. The data suggest that XAT can mechanistically induce ROS production and promote apoptosis through mitochondrial or endoplasmic reticulum pathways, regulate NF-κB, MAPK, JAK/STAT, Nrf2/HO-1, MAPK, AKT/mTOR, and ERK1/2 signaling pathways to exert pharmacological effects. In addition, the pharmacokinetics properties and toxicity of XAT are discussed in this paper, further elucidating the relationship between structure and efficacy. It is worth noting that data from clinical studies of XAT are still scarce, limiting the use of XAT in the clinic, and in the future, more in-depth studies are needed to determine the clinical efficacy of XAT.

Keywords: mechanisms; pharmacokinetics; pharmacological actions; therapeutics; toxicity; xanthotoxin.

Publication types

  • Review

MeSH terms

  • Anti-Bacterial Agents
  • Furocoumarins* / pharmacology
  • Methoxsalen* / pharmacology
  • NF-E2-Related Factor 2 / metabolism
  • NF-kappa B
  • Proto-Oncogene Proteins c-akt / metabolism
  • Reactive Oxygen Species
  • TOR Serine-Threonine Kinases

Substances

  • Anti-Bacterial Agents
  • Furocoumarins
  • NF-E2-Related Factor 2
  • NF-kappa B
  • Reactive Oxygen Species
  • Proto-Oncogene Proteins c-akt
  • TOR Serine-Threonine Kinases
  • Methoxsalen