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Constituents from Entada scandens with TRAIL-resistance Overcoming Activity

机译:来自Entada scandens的具有TRAIL抗性克服活性的成分

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Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) has emerged as a promising anticancer agent because of its ability to selectively kill tumor cells. But TRAIL-resistance is a major problem of its therapy. A search for compounds for abrogating TRAIL-resistance has, thus, become an important strategy for anticancer drug discovery. In search of bioactive natural products for overcoming TRAIL-resistance, we previously reported some compounds with TRAIL-resistance overcoming activity. Bioassay guided fractionation of Entada scandens led to the isolation of four compounds (1-4). Of the isolates, compounds 1 and 3 showed moderate TRAIL-resistance overcoming activity in TRAIL-resistant human gastric adenocarcinoma (AGS) cells.
机译:肿瘤坏死因子(TNF)相关的凋亡诱导配体(TRAIL)已经成为一种有前途的抗癌剂,因为它具有选择性杀死肿瘤细胞的能力。但是抗TRAIL是其治疗的主要问题。因此,寻找用于消除TRAIL抗性的化合物已成为发现抗癌药物的重要策略。为了寻找克服TRAIL抗性的生物活性天然产物,我们先前报道了一些具有TRAIL抗性克服活性的化合物。 Entada scandens的生物测定指导分级分离导致四种化合物的分离(1-4)。在分离株中,化合物1和3在耐TRAIL的人胃腺癌(AGS)细胞中显示出中等的TRAIL抗性克服活性。

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