Synthesis and Biological Evaluation of Ginsenoside Compound K Derivatives as a Novel Class of LXRα Activator

Molecules. 2017 Jul 24;22(7):1232. doi: 10.3390/molecules22071232.

Abstract

Compound K is one of the active metabolites of Panaxnotoginseng saponins, which could attenuate the formation of atherosclerosis in mice modelsvia activating LXRα. We synthesized and evaluated a series of ginsenoside compound K derivatives modified with short chain fatty acids. All of the structures of this class of ginsenoside compound K derivative exhibited comparable or better biological activity than ginsenoside compound K. Especially structure 1 exhibited the best potency (cholesteryl ester content: 41.51%; expression of ABCA1 mRNA: 319%) and low cytotoxicity.

Keywords: LXRα; atherosclerosis; derivatives; ginsenoside compound K; reverse cholesterol transport.

MeSH terms

  • ATP Binding Cassette Transporter 1 / metabolism
  • Animals
  • Atherosclerosis / drug therapy*
  • Atherosclerosis / metabolism
  • Ginsenosides / therapeutic use*
  • Liver X Receptors / metabolism
  • Mice

Substances

  • ATP Binding Cassette Transporter 1
  • Ginsenosides
  • Liver X Receptors
  • ginsenoside M1