Inhibition of human ether-à-go-go-related gene K+ currents expressed in HEK293 cells by three gingerol components from ginger

J Pharm Pharmacol. 2022 Aug 19;74(8):1133-1139. doi: 10.1093/jpp/rgac029.

Abstract

Objectives: Gingerols are bioactive compounds derived from ginger, our experiment investigates the effects of 6-, 8- and 10-Gin on the human ether-à-go-go-related gene (hERG) K+ channels by using patch clamp technology.

Key findings: hERG K+ currents were suppressed by 6-, 8- and 10-Gin in a concentration-dependent manner. The IC50 values of 6-, 8- and 10-Gin were 41.5, 16.1 and 86.5 μM for the hERG K+ currents, respectively. The maximum inhibitory effects caused by 6-, 8- and 10-Gin were 44.3% ± 2.0%, 88.6% ± 1.3% and 63.1% ± 1.1%, respectively, and the effects were almost completely reversible.

Conclusion: These findings suggest that 8-Gin is the most potent hERG K+ channel inhibitor among gingerol components and may offer a new approach for understanding and treating cancer.

Keywords: active components; cancer; gingerol; hERG K+ channels; patch clamp.

MeSH terms

  • Catechols
  • Ether-A-Go-Go Potassium Channels* / genetics
  • Ethers
  • Fatty Alcohols
  • HEK293 Cells
  • Humans
  • Potassium Channel Blockers / pharmacology
  • Zingiber officinale*

Substances

  • Catechols
  • Ether-A-Go-Go Potassium Channels
  • Ethers
  • Fatty Alcohols
  • Potassium Channel Blockers
  • gingerol