Cholesterol-derived novel anti-apoptotic agents on the structural basis of ginsenoside Rk1

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7102-5. doi: 10.1016/j.bmcl.2010.09.071. Epub 2010 Oct 21.

Abstract

Design and synthesis of cholesterol-derived anti-apoptotic agents were described. The synthesized cholesterol analogs designed on the structural basis of ginsenoside Rk1 inhibited the undesirable apoptosis of human endothelial cells, which are induced by a vascular injury. In particular, analogue 1 possessing 4,6-di-O-acetyl-2,3-dideoxyhex-2-enopyran linked to hydroxyl group of cholesterol exhibited the most effective anti-apoptotic activities at both 5 and 10 μg/ml.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis / drug effects*
  • Blood Vessels / injuries
  • Blood Vessels / pathology
  • Cholesterol / analogs & derivatives*
  • Cholesterol / chemistry
  • Cholesterol / pharmacology*
  • Dose-Response Relationship, Drug
  • Endothelial Cells / drug effects
  • Endothelial Cells / pathology
  • Ginsenosides / chemistry*
  • Humans
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Ginsenosides
  • ginsenoside Rk1
  • Cholesterol