2. Academic Validation
  3. Synthesis and Biological Evaluation of Ginsenoside Compound K Derivatives as a Novel Class of LXRα Activator

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

Affiliations

  • 1 Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China. huangyanoo8@126.com.
  • 2 Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China. hongmeiliu0819@126.com.
  • 3 Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China. 15095839731@163.com.
  • 4 Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China. ioulj@tmmu.edu.cn.
  • 5 Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China. wangchenping.0219@aliyun.com.
  • 6 Department of Pharmacy, Xinqiao Hospital & The Second Affiliated Hospital, Third Military Medical University, Shapingba, Chongqing 400037, China. zhouli1007@126.com.
  • 7 Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China. jy@tmmu.edu.cn.
  • 8 Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China. xhl@tmmu.edu.cn.
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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