Schools of Dentistry, Chung Shan Medical University, 110, Section 1, Chien-Kuo North Road, Taichung, Taiwan 40201, ROC.
Anticancer Res. 2012 Jul;32(7):2727-34.
Eleven derivatives from Antrodia camphorata were isolated in order to evaluate their selective cytotoxicity toward 14 types of human cancer cell and two non-transformed cell types. Among these triterpenoids, methyl antcinate A (MAA) exhibited the most potent spectrum of anticancer effects in KB cells, four different oral cancer cell lines (TSCCa, GNM, OC-2, and OEC-M1), Panc-1, BT474, PC-3, OVCAR-3, HeLa, and U2OS cells with high selectivity indices (CC(50)/IC(50)). The expression of B-cell lymphoma 2 (Bcl-2), Bcl-2-associated X protein (Bax), and poly(ADP-ribose) polymerase (PARP) of PC-3 cells tested by western blotting suggested that MAA exerts cell death through the caspase-dependent cascade and the Bax-mediated mitochondrial apoptotic pathway, not only on liver and oral cancer cells but on other types as well, including prostate cancer, in a dose-dependent manner. In addition to MAA, methyl antcinate B, dehydroeburicoic acid, and 15α-acetyl-dehydrosulfurenic acid also exhibited significant selective cytotoxic effects to respective cancer cells. Modifications of these triterpenoids may lead to the development of more potent anticancer drugs.
为了评估 11 种来自于暗皮线菌的衍生物对 14 种人类癌细胞和两种非转化细胞类型的选择性细胞毒性，我们对其进行了分离。在这些三萜类化合物中，甲基茵陈色酮 A（MAA）在 KB 细胞、四种不同的口腔癌细胞系（TSCCa、GNM、OC-2 和 OEC-M1）、Panc-1、BT474、PC-3、OVCAR-3、HeLa 和 U2OS 细胞中表现出最有效的广谱抗癌作用，具有高选择性指数（CC（50）/IC（50））。Western blot 检测到 PC-3 细胞中 B 细胞淋巴瘤 2（Bcl-2）、Bcl-2 相关 X 蛋白（Bax）和聚（ADP-核糖）聚合酶（PARP）的表达表明，MAA 通过 caspase 依赖性级联和 Bax 介导的线粒体凋亡途径发挥细胞死亡作用，不仅在肝癌和口腔癌细胞中，而且在其他类型的细胞中，包括前列腺癌，都具有剂量依赖性。除了 MAA 之外，甲基茵陈色酮 B、去氢埃博霉素酸和 15α-乙酰去磺基硫色酮酸对各自的癌细胞也表现出显著的选择性细胞毒性作用。对这些三萜类化合物的修饰可能会导致更有效的抗癌药物的开发。
