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.

引用

页数：13

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