Synthesis and cytotoxic activities of usnic acid derivatives
Synthesis and cytotoxic activities of usnic acid derivatives
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DOI：
10.1016/j.bmc.2008.05.069
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发表时间：
2008-07-15
影响因子：
3.5
通讯作者：
Tomasi, Sophie
中科院分区：
文献类型：
--
作者：
Bazin, Marc-Antoine;Le Lamer, Anne-Cecile;Tomasi, Sophie
在鼠和人癌细胞系上评价了九种松萝酸-胺缀合物。多胺衍生物在L1210细胞中显示出显著的细胞毒性。它们的活性似乎是独立的多胺运输系统（PTS）。实际上，它们在中国仓鼠卵巢（CHO）和PTS缺陷型CHO-MG细胞中的活性相似。此外，α-二氟甲基鸟氨酸，一种已知间接增强PTS活性并因此增加通过PTS进入细胞的细胞毒性药物的细胞毒性的鸟氨酸脱羧酶抑制剂，对多胺衍生物的活性没有影响。活性更高的衍生物（1，8-二氨基辛烷衍生物）在所有研究的癌细胞系上显示出相似的活性并诱导细胞凋亡。(c)2008爱思唯尔有限公司保留所有权利。
Nine usnic acid-amine conjugates were evaluated on murine and human cancer cell lines. The polyamine derivatives showed significant cytotoxicity in L1210 cells. Their activities appeared to be independent of the polyamine transport system (PTS). Indeed, their activities were similar in chinese hamster ovary (CHO) and in the PTS deficient CHO-MG cells. In addition, alpha-difluoromethylornithine, an ornithine decarboxylase inhibitor known to indirectly enhance the activity of the PTS and consequently increase the cytotoxicity of cytotoxic drugs entering cells via the PTS, had no effect on the activity of the polyamine derivatives. The more active derivative (1,8-diaminooctane derivative) displayed similar activities on all cancer cell lines studied and induced apoptosis. (c) 2008 Elsevier Ltd. All rights reserved.