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从艾叶中通过活性导向分离得到东莨菪素和异东莨菪素,这两种物质是对CCRF-CEM白血病细胞和多药耐药CEM/ADR5000细胞具有抑制活性的成分。

Activity-guided isolation of scopoletin and isoscopoletin, the inhibitory active principles towards CCRF-CEM leukaemia cells and multi-drug resistant CEM/ADR5000 cells, from Artemisia argyi.

作者信息

Adams Michael, Efferth Thomas, Bauer Rudolf

机构信息

Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz, Graz, Austria.

出版信息

Planta Med. 2006 Jul;72(9):862-4. doi: 10.1055/s-2006-947165.

Abstract

The ethyl acetate extract of Artemisia argyi leaves showed substantial inhibition in a cell proliferation assay using human CCRF-CEM leukaemia cells. Bioassay-guided fractionation of the extract led to the isolation of scopoletin and isoscopoletin as the active principles. Their IC50 values were 2.6 and 4.0 microM, respectively. Additionally the two substances were tested against the multidrug resistant subline, CEM/ADR5000 where they both showed IC50 values of 1.6 microM. In contrast to the standard cytostatic drugs doxorubicin, vincristine, and paclitaxel, CEM/ADR5000 cells therefore did not exhibit cross-resistance to scopoletin and isoscopoletin.

摘要

艾叶的乙酸乙酯提取物在使用人CCRF - CEM白血病细胞的细胞增殖试验中显示出显著抑制作用。对该提取物进行生物测定导向的分级分离,得到了东莨菪素和异东莨菪素作为活性成分。它们的IC50值分别为2.6和4.0微摩尔。此外,还对这两种物质针对多药耐药亚系CEM/ADR5000进行了测试,它们在该亚系中的IC50值均为1.6微摩尔。因此,与标准细胞毒性药物阿霉素、长春新碱和紫杉醇不同,CEM/ADR5000细胞对东莨菪素和异东莨菪素没有表现出交叉耐药性。

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