三萜类化合物抑制 AP-1 功能与细胞毒性或蛋白质合成抑制无关。
Quassinoid inhibition of AP-1 function does not correlate with cytotoxicity or protein synthesis inhibition.
机构信息
Molecular Targets Development Program and Laboratory of Cancer Prevention, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, USA.
出版信息
J Nat Prod. 2009 Mar 27;72(3):503-6. doi: 10.1021/np800732n.
Abstract
Several quassinoids were identified in a high-throughput screening assay as inhibitors of the transcription factor AP-1. Further biological characterization revealed that while their effect was not specific to AP-1, protein synthesis inhibition and cell growth assays were inconsistent with a mechanism of simple protein synthesis inhibition. Numerous plant extracts from the plant family Simaroubaceae were also identified in the same screen; bioassay-guided fractionation of one extract (Ailanthus triphylla) yielded two known quassinoids, ailanthinone (3) and glaucarubinone (4), which were also identified in the pure compound screening procedure.
摘要
在高通量筛选实验中，几种苦木苦味素被鉴定为转录因子 AP-1 的抑制剂。进一步的生物学特性分析表明，虽然它们的作用并非特异性针对 AP-1，但蛋白合成抑制和细胞生长测定结果与单纯的蛋白合成抑制机制不一致。在同一筛选中还鉴定了来自苦木科植物家族的许多植物提取物；一种提取物（臭椿）的生物活性导向分离得到两种已知的苦木苦味素，苦木酮（3）和考布他汀酮（4），这两种化合物在纯化合物筛选过程中也被鉴定出来。
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