大戟烷二萜酯类化合物作为多药耐药逆转剂从大飞扬中分离得到。
Jatrophane diterpenoid esters from Euphorbia sororia serving as multidrug resistance reversal agents.
机构信息
The Key Laboratory of Plant Resources and Chemistry of Arid Zone, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China; State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Urumqi 830011, China; University of the Chinese Academy of Sciences, Beijing 100039, China.
The Key Laboratory of Plant Resources and Chemistry of Arid Zone, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China; State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Urumqi 830011, China.
出版信息
Fitoterapia. 2014 Jan;92:244-51. doi: 10.1016/j.fitote.2013.11.008. Epub 2013 Nov 27.
Six (1-6) new jatrophane diterpenoid esters together with four known compounds (7-10) were isolated from the acetone extract of fructus Euphorbia sororia. Their structures were elucidated by the spectral technology, including the 2D NMR experiments (HMQC, HMBC and NOESY). The absolute configuration of compound 1 and compound 7 were first confirmed by X-ray crystallographic analysis. Compounds 1-7 were assayed for their antiproliferative activity in human cancer cell lines: human mammary adenocarcinoma (MCF-7) and human lung adenocarcinoma (A549). All the compounds were inactive for the cell lines. The multidrug-resistance reversal activity was also tested on KBv200 cells and compound 2 displayed strong multidrug resistance reversal activity, outperforming verapamil at 10 μM.
从大戟属植物Euphorbia sororia 的丙酮提取物中分离得到了六个（1-6）新的 Jatrophane 二萜酯类化合物和四个已知化合物（7-10）。通过光谱技术，包括 2D NMR 实验（HMQC、HMBC 和 NOESY）确定了它们的结构。化合物 1 和化合物 7 的绝对构型是通过 X 射线晶体学分析首次确定的。对化合物 1-7 进行了在人癌细胞系中的抗增殖活性测定：人乳腺腺癌（MCF-7）和人肺腺癌（A549）。所有化合物对细胞系均无活性。还对 KBv200 细胞进行了多药耐药逆转活性测试，化合物 2 显示出较强的多药耐药逆转活性，在 10 μM 时优于维拉帕米。
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