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.
Yan Huang  1 ,  Hongmei Liu  2 ,  Yingxian Zhang  3 ,  Jin Li  4 ,  Chenping Wang  5 ,  Li Zhou  6 ,  Yi Jia  7 ,  Xiaohui Li  8
Affiliations
  • 1. Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China. [email protected].
  • 2. Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China. [email protected].
  • 3. Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China. [email protected].
  • 4. Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China. [email protected].
  • 5. Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China. [email protected].
  • 6. Department of Pharmacy, Xinqiao Hospital & The Second Affiliated Hospital, Third Military Medical University, Shapingba, Chongqing 400037, China. [email protected].
  • 7. Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China. [email protected].
  • 8. Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China. [email protected].
PMID: 28737726 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.
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