Molecular Targets Laboratory, Molecular Discovery Program, Center for Cancer Research, NCI-Frederick, Frederick, MD 21702, USA.
J Nat Prod. 2010 Dec 27;73(12):2013-8. doi: 10.1021/np1004455. Epub 2010 Nov 10.
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.
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。
