Nocardioazines: A Novel Bridged Diketopiperazine Scaffold from a Marine-Derived Bacterium Inhibits P-Glycoprotein
Nocardioazines: A Novel Bridged Diketopiperazine Scaffold from a Marine-Derived Bacterium Inhibits P-Glycoprotein
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DOI：
10.1021/ol200904v
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发表时间：
2011-05-20
期刊：
影响因子：
5.2
通讯作者：
Capon, Robert J.
中科院分区：
文献类型：
--
作者：
Raju, Ritesh;Piggott, Andrew M.;Capon, Robert J.
一种来自澳大利亚海洋沉积物的分离物Nocardiopsis sp. （CMB-M0232）产生了一类新的二酮哌嗪，表明其具有独特的区域选择性二酮哌嗪吲哚戊烯基转移酶的作用。nocardioazine A桥接支架被证明是膜蛋白外排泵p糖蛋白的非细胞毒性抑制剂，逆转了多药耐药结肠癌细胞的阿霉素耐药。
An Australian marine sediment-derived Isolate, Nocardiopsis sp. (CMB-M0232), yielded a new class of prenylated diketopiperazine, Indicative of the action of a uniquely regioselective diketopiperazine indole prenyltransferase. The bridged scaffold of nocardioazine A proved to be a noncytotoxic inhibitor of the membrane protein efflux pump P-glycoprotein, reversing doxorubicin resistance in a multidrug resistant colon cancer cell.