人参皂苷Compound K衍生物作为新型LXRα激活剂的合成及生物学评价
Synthesis and Biological Evaluation of Ginsenoside Compound K Derivatives as a Novel Class of LXRα Activator.
作者信息
Huang Yan, Liu Hongmei, Zhang Yingxian, Li Jin, Wang Chenping, Zhou Li, Jia Yi, Li Xiaohui
机构信息
Institute of Materia Medica and Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Shapingba, Chongqing 400038, China.
Department of Pharmacy, Xinqiao Hospital & The Second Affiliated Hospital, Third Military Medical University, Shapingba, Chongqing 400037, China.
出版信息
Molecules. 2017 Jul 24;22(7):1232. doi: 10.3390/molecules22071232.
Compound K is one of the active metabolites of 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 exhibited the best potency (cholesteryl ester content: 41.51%; expression of ABCA1 mRNA: 319%) and low cytotoxicity.
化合物K是皂苷的活性代谢产物之一，其可通过激活肝X受体α（LXRα）减轻小鼠模型中动脉粥样硬化的形成。我们合成并评估了一系列用短链脂肪酸修饰的人参皂苷化合物K衍生物。这类人参皂苷化合物K衍生物的所有结构均表现出与人参皂苷化合物K相当或更好的生物活性。特别是结构表现出最佳效力（胆固醇酯含量：41.51%；ABCA1 mRNA表达：319%）且细胞毒性低。
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