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来自秀丽崖白菜的 clerodane 二萜类化合物,可作为 TRAIL 增敏剂发挥协同作用。

Clerodane diterpenes from Casearia arguta that act as synergistic TRAIL sensitizers.

机构信息

Molecular Targets Laboratory, Molecular Discovery Program, Center for Cancer Research, NCI-Frederick, Frederick, MD 21702, USA.

出版信息

J Nat Prod. 2010 Dec 27;73(12):2013-8. doi: 10.1021/np1004455. Epub 2010 Nov 10.

Abstract

Casearia arguta was investigated as part of the ongoing search for synergistic TRAIL (tumor necrosis factor-α-related apoptosis-inducing ligand) sensitizers. As a result of this study, argutins A-H, eight new highly oxygenated clerodane diterpenes, were isolated from the plant Casearia arguta collected in Guatemala. The modified Mosher ester method was utilized to establish the absolute configuration of argutins A and F. Each of the argutins showed varying levels of synergy with TRAIL. Argutin B showed the highest TRAIL sensitization; the synergistic effect of argutin B and TRAIL together was 3-fold greater than argutin B alone.

摘要

作为正在进行的寻找 TRAIL(肿瘤坏死因子相关凋亡诱导配体)增敏剂的一部分,对山香圆进行了研究。作为这项研究的结果,从危地马拉采集的植物山香圆中分离出了 8 种新的高度氧化的 clerodane 二萜类化合物,分别为 argutins A-H。采用改良的 Mosher 酯法确定了 argutins A 和 F 的绝对构型。每种 argutin 均显示出与 TRAIL 不同程度的协同作用。argutin B 显示出最高的 TRAIL 增敏作用;argutin B 和 TRAIL 联合使用的协同作用比单独使用 argutin B 强 3 倍。

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