Glycyrrhetinic acid derivatives: a novel class of inhibitors of gap-junctional intercellular communication. Structure-activity relationships

J Pharmacol Exp Ther. 1988 Sep;246(3):1104-7.

Abstract

Glycyrrhetinic acid was shown previously to inhibit intercellular gap-junctional communication between human fibroblasts. In the present study 31 derivatives of glycyrrhetinic acid were tested for their ability to inhibit communication. Eight of the compounds inhibited communication with high potency (IC50 less than 3 microM) and showed low toxicity, properties which suggest they may be useful pharmacological probes for studies of gap-junction function.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Communication / drug effects*
  • Cell Line
  • Fibroblasts / cytology
  • Glycyrrhetinic Acid / analogs & derivatives*
  • Glycyrrhetinic Acid / pharmacology
  • Humans
  • Intercellular Junctions / drug effects*
  • Structure-Activity Relationship

Substances

  • Glycyrrhetinic Acid