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

被引：22
|
作者：
Huang, Yan [1 ,2 ]
Liu, Hongmei [1 ,2 ]
Zhang, Yingxian [1 ,2 ]
Li, Jin [1 ,2 ]
Wang, Chenping [1 ,2 ]
Zhou, Li [3 ,4 ]
Jia, Yi [1 ,2 ]
Li, Xiaohui [1 ,2 ]
机构：
[1] Third Mil Med Univ, Coll Pharm, Inst Mat Med, Chongqing 400038, Peoples R China
[2] Third Mil Med Univ, Coll Pharm, Dept Pharmaceut, Chongqing 400038, Peoples R China
[3] Third Mil Med Univ, Xinqiao Hosp, Dept Pharm, Chongqing 400037, Peoples R China
[4] Third Mil Med Univ, Affiliated Hosp 2, Chongqing 400037, Peoples R China
来源：
MOLECULES | 2017年 / 22卷 / 07期
关键词：
atherosclerosis; LXR alpha; ginsenoside compound K; derivatives; reverse cholesterol transport; SAPONINS ATTENUATE ATHEROSCLEROSIS; LIVER X-RECEPTORS; GENE-EXPRESSION; APOE(-/-) MICE; IN-VITRO; METABOLITE; CANCER; CELLS; PROLIFERATION; DISCOVERY;
D O I：
10.3390/molecules22071232
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Compound K is one of the active metabolites of Panaxnotoginseng saponins, which could attenuate the formation of atherosclerosis in mice modelsvia activating LXR alpha. 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.
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页数：13
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