赫拉
细胞毒性
硫氧还蛋白还原酶
倍半萜
胞浆
还原酶
硫氧还蛋白
细胞凋亡
化学
生物化学
活性氧
细胞内
菊粉
细胞培养
分子生物学
酶
生物
体外
立体化学
医学
病理
中医药
替代医学
遗传学
作者
Meili Yang,Junmin Zhang,Ya Li,Xiao Han,Kun Gao,Jianguo Fang
标识
DOI:10.1016/j.abb.2016.08.008
摘要
In a screen for mammalian thioredoxin reductases inhibitors, an MeOH extract from the roots of Saussurea lappa C.B. Clarke (Compositae) inhibited the activity of cytosolic thioredoxin reductase (TrxR1). Bioassay-guided separation of the extract led to the isolation of a new TrxR1 inhibitor, dehydrocostus lactone (DHC), a guaiane-type sesquiterpene. The content of DHC in the extract was determined to be 0.4%. DHC inhibited human cervical carcinoma HeLa cells with an IC50 of ∼12.00 μM but displayed less cytotoxicity to human immortalized normal liver cells L02. We observed that DHC killed HeLa cells through induction of apoptosis. DHC inhibited the activity of TrxR1 in HeLa cells, which elicited an accumulation of reactive oxygen species (ROS) in cells and a collapse of the intracellular redox equilibrium and eventually induced apoptosis of HeLa cells.
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