Wang Jianwu, Yu Yuanjing, Hashimoto Fumio, Sakata Yusuke, Fujii Makoto, Hou De-Xing
Department of Biochemical Science and Technology, Faculty of Agriculture, Kagoshima University, Korimoto 1-21-24, Kagoshima 890-0065, Japan.
Int J Mol Med. 2004 Oct;14(4):627-32.
Baicalein is one component of the dried root of Scutellaria Baicalensis Georgi. (Huang Qin) which is widely used in the traditional Chinese herbal medicine. In this study, we report that baicalein was able to induce apoptosis in human promyelocytic leukemia cells (HL-60), as characterized by poly-(ADP-ribose) polymerase (PARP) cleavage and DNA fragmentation. The efficacious induction of apoptosis was observed at 100 microM for 6 h. Mechanistic analysis demonstrated that baicalein induced the cleavage of Bid protein, cytochrome c release from mitochondria into cytosol, and activation of caspase-3, -8 and -9. Moreover, baicalein caused elevation of intracellular hydrogen peroxide level. Catalase could effectively block baicalein-induced DNA fragmentation. These data indicate that baicalein may trigger an apoptotic death program through reactive oxygen species (ROS)-mediated mitochondrial dysfunction pathway. The findings enhance our understanding of anticancer function of baicalein in herbal medicine.
黄芩素是黄芩（Huang Qin）干燥根的一种成分，黄芩在传统中药中广泛应用。在本研究中，我们报道黄芩素能够诱导人早幼粒细胞白血病细胞（HL-60）凋亡，其特征为聚（ADP-核糖）聚合酶（PARP）裂解和DNA片段化。在100微摩尔浓度处理6小时时观察到有效诱导凋亡。机制分析表明，黄芩素诱导Bid蛋白裂解、细胞色素c从线粒体释放到细胞质中以及半胱天冬酶-3、-8和-9的激活。此外，黄芩素导致细胞内过氧化氢水平升高。过氧化氢酶可有效阻断黄芩素诱导的DNA片段化。这些数据表明，黄芩素可能通过活性氧（ROS）介导的线粒体功能障碍途径触发凋亡死亡程序。这些发现增进了我们对黄芩素在草药中的抗癌功能的理解。
