从朝鲜小檗树干中活性导向分离细胞毒性三萜。
Bioactivity-guided isolation of cytotoxic triterpenoids from the trunk of Berberis koreana.
机构信息
Natural Products Laboratory, School of Pharmacy, Sungkyunkwan University, Jangan-ku, Suwon, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2010 Mar 15;20(6):1944-7. doi: 10.1016/j.bmcl.2010.01.156. Epub 2010 Feb 4.
A bioassay-guided fractionation and chemical investigation of the trunk of Berberis koreana resulted in the isolation and characterization of two new triterpenoids, 23-trans-p-coumaroyloxy-2alpha,3alpha-dihydroxyolean-12-en-28-oic acid (1), and 23-cis-p-coumaroyloxy-2alpha,3alpha-dihydroxyolean-12-en-28-oic acid (2), along with seven known triterpenoids (3-9). The structures of the new compounds were determined on the basis of spectroscopic analyses including 2D NMR. The cytotoxic activities of the triterpenes (1-9) were evaluated by determining their inhibitory effects on human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15) using the SRB assay. Compounds 5 and 6 showed potent cytotoxicity against A549, SK-OV-3, SK-MEL-2, and HCT-15 cell lines (IC(50) (5): 4.37, 7.04, 9.72, and 5.83 microM, and IC(50) (6): 5.57, 7.84, 13.29, and 5.61 microM, respectively).
从朝鲜小檗的树干中进行基于生物测定的分离和化学研究，导致分离和鉴定出两种新的三萜类化合物，23-反式-对香豆酰氧基-2α，3α-二羟基齐墩烷-12-烯-28-酸（1）和 23-顺式-对香豆酰氧基-2α，3α-二羟基齐墩烷-12-烯-28-酸（2），以及七种已知的三萜类化合物（3-9）。新化合物的结构是基于包括 2D NMR 在内的光谱分析确定的。通过 SRB 测定法测定它们对人肿瘤细胞系（A549、SK-OV-3、SK-MEL-2 和 HCT-15）的抑制作用，评估三萜类化合物（1-9）的细胞毒性。化合物 5 和 6 对 A549、SK-OV-3、SK-MEL-2 和 HCT-15 细胞系表现出很强的细胞毒性（IC50（5）：4.37、7.04、9.72 和 5.83 μM，IC50（6）：5.57、7.84、13.29 和 5.61 μM，分别）。
Zotero 插件