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Molecules 2017, 22(7), 1232; doi:10.3390/molecules22071232

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

1
Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China
2
Department of Pharmacy, Xinqiao Hospital & The Second Affiliated Hospital, Third Military Medical University, Shapingba, Chongqing 400037, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Received: 25 June 2017 / Revised: 17 July 2017 / Accepted: 18 July 2017 / Published: 24 July 2017
(This article belongs to the Section Medicinal Chemistry)
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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. View Full-Text
Keywords: atherosclerosis; LXRα; ginsenoside compound K; derivatives; reverse cholesterol transport atherosclerosis; LXRα; ginsenoside compound K; derivatives; reverse cholesterol transport
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Huang, Y.; Liu, H.; Zhang, Y.; Li, J.; Wang, C.; Zhou, L.; Jia, Y.; Li, X. Synthesis and Biological Evaluation of Ginsenoside Compound K Derivatives as a Novel Class of LXRα Activator. Molecules 2017, 22, 1232.

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