Anti-inflammatory and PPAR Subtypes Transactivational Activities of Phenolics and Lignans from the Stem Bark of Kalopanax pictus
Anti-inflammatory and PPAR Subtypes Transactivational Activities of Phenolics and Lignans from the Stem Bark of Kalopanax pictus
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DOI：
10.5012/bkcs.2011.32.11.4049
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发表时间：
2011-11
影响因子：
1.7
通讯作者：
T. Quang;N. Ngan;C. Minh;P. Kiem;N. X. Nhiem;B. H. Tai;N. Thao;B. Luyen;S. Song;Y. Kim
中科院分区：
文献类型：
--
作者：
T. Quang;N. Ngan;C. Minh;P. Kiem;N. X. Nhiem;B. H. Tai;N. Thao;B. Luyen;S. Song;Y. Kim
从红刺楸（Kalopanax pictus）茎皮中分得一个新化合物Kalopanaxin F（3）和11个已知化合物（1，2，4-12）。根据化学和光谱方法鉴定了它们的结构。其中5种化合物（2、3、5、6和12）以剂量依赖性方式显著抑制HepG 2细胞中TNFα诱导的NF-κB转录活性，IC 50值范围为6.2 - 9.1 µM。此外，基于HepG 2细胞中考克斯-2和iNOS基因表达的降低，证实了这些化合物的转录抑制功能。化合物3-7、9和12剂量依赖性地显著激活PPARs的转录活性，EC 50值范围为4.1-12.7 μM。化合物4和5以剂量依赖性方式表现出PPARα、PPARγ和PPARβ（δ）反式激活活性，EC 50值分别为16.0和17.0、8.7和16.5、26.2和26.3 µM。
A new compound, kalopanaxin F (3), and 11 known compounds (1, 2, 4-12), were isolated from the stem bark of Kalopanax pictus. Their structures were elucidated on the basis of chemical and spectroscopic methods. Five of the compounds (2, 3, 5, 6, and 12) significantly inhibited TNFα-induced NF-κB transcriptional activity in HepG2 cells in a dose-dependent manner, with IC50 values ranging from 6.2 to 9.1 µM. Furthermore, the transcriptional inhibitory function of these compounds was confirmed based on decreases in COX-2 and iNOS gene expression in HepG2 cells. Compounds 3-7, 9, and 12 significantly activated the transcriptional activity of PPARs dose-dependently, with EC50 values ranging from 4.1-12.7 µM. Compounds 4 and 5 exhibited PPARα, PPARγ, and PPARβ(δ) transactivational activities in a dose-dependent manner, with EC50 values of 16.0 and 17.0, 8.7 and 16.5, 26.2 and 26.3 µM, respectively.