The Influence of Betulin and Its Derivatives on Selected Colorectal Cancer Cell Lines' Viability and Their Antioxidant Systems

Cells. 2024 Aug 17;13(16):1368. doi: 10.3390/cells13161368.

Abstract

Oxidative stress is considered one of the main reasons for the development of colorectal cancer (CRC). Depending on the stage of the disease, variable activity of the main antioxidant enzymes, i.e., superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx), is observed. Due to limited treatment methods for CRC, new substances with potential antitumor activity targeting pathways related to oxidative stress are currently being sought, with substances of natural origin, including betulin, leading the way. The betulin molecule is chemically modified to obtain new derivatives with improved pharmacokinetic properties and higher biological activity. The aim of this study was to evaluate the effects of betulin and its new derivatives on viability and major antioxidant systems in colorectal cancer cell lines. The study showed that betulin and its derivative EB5 affect the antioxidant enzyme activity to varying degrees at both the protein and mRNA levels. The SW1116 cell line is more resistant to the tested compounds than RKO, which may be due to differences in the genetic and epigenetic profiles of these lines.

Keywords: CAT; GPx; SOD; betulin; cell lines; colorectal cancer; cytotoxicity; derivatives; oxidative stress; synthesis.

MeSH terms

  • Antioxidants* / pharmacology
  • Betulinic Acid
  • Catalase* / metabolism
  • Cell Line, Tumor
  • Cell Survival* / drug effects
  • Colorectal Neoplasms* / drug therapy
  • Colorectal Neoplasms* / metabolism
  • Colorectal Neoplasms* / pathology
  • Glutathione Peroxidase / genetics
  • Glutathione Peroxidase / metabolism
  • Humans
  • Oxidative Stress / drug effects
  • Superoxide Dismutase / metabolism
  • Triterpenes* / chemistry
  • Triterpenes* / pharmacology

Substances

  • betulin
  • Antioxidants
  • Triterpenes
  • Catalase
  • Glutathione Peroxidase
  • Superoxide Dismutase
  • Betulinic Acid