来自山茱萸的肝脏X受体和过氧化物酶体增殖物激活受体激动剂。
Liver X receptor and peroxisome proliferator-activated receptor agonist from Cornus alternifolia.
作者信息
He Yang-Qing, Ma Guo-Yi, Peng Jiang-nan, Ma Zhan-Ying, Hamann Mark T
机构信息
Department of Applied Chemistry, Xi'an University of Technology, Xi'an 710048, China.
出版信息
Biochim Biophys Acta. 2012 Jul;1820(7):1021-6. doi: 10.1016/j.bbagen.2012.02.004. Epub 2012 Feb 13.
BACKGROUND
Peroxisome proliferator-activated receptors (PPARs) belong to the nuclear receptors superfamily and are transcription factors activated by specific ligands. Liver X receptors (LXR) belong to the nuclear hormone receptors and have been shown to play an important role in cholesterol homeostasis. From the previous screening of several medicinal plants for potential partial PPARγ agonists, the extracts of Cornus alternifolia were found to exhibit promising bioactivity. In this paper, we report the isolation and structural elucidation of four new compounds and their potential as ligands for PPAR.
METHODS
The new compounds were extracted from the leaves of C. alternifolia and fractionated by high-performance liquid chromatography. Their structures were elucidated on the basis of spectroscopic evidence and analysis of their hydrolysis products.
RESULTS
Three new iridoid glycosides including an iridolactone, alternosides A-C (1-3), a new megastigmane glycoside, cornalternoside (4) and 10 known compounds, were obtained from the leaves of C. alternifolia. Kaempferol-3-O-β-glucopyranoside (5) exhibited potent agonistic activities for PPARα, PPARγ and LXR with EC50 values of 0.62, 3.0 and 1.8 μM, respectively.
CONCLUSIONS
We isolated four new and ten known compounds from C. alternifolia, and one known compound showed agonistic activities for PPARα, PPARγ and LXR.
GENERAL SIGNIFICANCE
Compound 1 is the first example of a naturally occurring iridoid glycoside containing a β-glucopyranoside moiety at C-6.
背景
过氧化物酶体增殖物激活受体（PPARs）属于核受体超家族，是由特定配体激活的转录因子。肝X受体（LXR）属于核激素受体，已被证明在胆固醇稳态中起重要作用。通过先前对几种药用植物进行潜在的PPARγ部分激动剂筛选，发现山茱萸提取物具有良好的生物活性。本文报道了四种新化合物的分离、结构解析及其作为PPAR配体的潜力。
方法
从山茱萸叶中提取新化合物，并用高效液相色谱法进行分离。根据光谱证据及其水解产物分析确定其结构。
结果
从山茱萸叶中获得了三种新的环烯醚萜苷，包括一种环烯醚萜内酯，alternosides A - C（1 - 3），一种新的巨大戟烷苷，cornalternoside（4）以及10种已知化合物。山奈酚 - 3 - O - β - 吡喃葡萄糖苷（5）对PPARα、PPARγ和LXR表现出强效激动活性，其EC50值分别为0.62、3.0和1.8 μM。
结论
我们从山茱萸中分离出四种新化合物和十种已知化合物，其中一种已知化合物对PPARα、PPARγ和LXR表现出激动活性。
一般意义
化合物1是在C - 6位含有β - 吡喃葡萄糖苷部分的天然环烯醚萜苷的首个实例。
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