Bazin Marc-Antoine, Le Lamer Anne-Cécile, Delcros Jean-Guy, Rouaud Isabelle, Uriac Philippe, Boustie Joël, Corbel Jean-Charles, Tomasi Sophie
EA 4090 Substances lichéniques et photoprotection, UFR des Sciences Pharmaceutiques et Biologiques, Université de Rennes 1, 2 Avenue du Professeur Léon Bernard, 35043 Rennes Cedex, France.
Bioorg Med Chem. 2008 Jul 15;16(14):6860-6. doi: 10.1016/j.bmc.2008.05.069. Epub 2008 Jun 14.
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.
对九种扁枝衣酸-胺缀合物在小鼠和人类癌细胞系上进行了评估。多胺衍生物在L1210细胞中表现出显著的细胞毒性。它们的活性似乎与多胺转运系统（PTS）无关。实际上，它们在中华仓鼠卵巢（CHO）细胞和缺乏PTS的CHO-MG细胞中的活性相似。此外，α-二氟甲基鸟氨酸是一种鸟氨酸脱羧酶抑制剂，已知可间接增强PTS的活性，从而增加通过PTS进入细胞的细胞毒性药物的细胞毒性，但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表现出相似的活性并诱导细胞凋亡。
