XQ2, a Novel TPZ Derivative, Induced G2/M Phase Arrest and Apoptosis under Hypoxia in Non-Small Cell Lung Cancer Cells
XQ2, a Novel TPZ Derivative, Induced G2/M Phase Arrest and Apoptosis under Hypoxia in Non-Small Cell Lung Cancer Cells
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XQ2，一种新型 TPZ 衍生物，在缺氧条件下诱导非小细胞肺癌细胞 G2/M 期阻滞和凋亡
DOI：
10.1271/bbb.90889
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发表时间：
2010
期刊：
影响因子：
--
通讯作者：
P. Luo
中科院分区：
文献类型：
--
作者：
Jian;Xing;Qinjie Weng;Duo;Q. Xia;Yongzhou Hu;Qiaojun He;Bo Yang;P. Luo
缺氧是各种肿瘤的必然情况之一。它控制肿瘤进展的各种水平的调节，并导致肿瘤对放疗和化疗的抵抗。本文研究了TPZ衍生物N-乙氧甲基-3-氨基-1，2，4-苯并三嗪-1，4-二氧化物（XQ 2）在常氧和缺氧条件下的抗肿瘤作用，细胞增殖实验发现XQ 2在常氧和缺氧条件下对受试癌细胞株均表现出较强的抑制作用。流式细胞术和western blot研究表明XQ 2诱导A549细胞G2/M期阻滞和caspase依赖性凋亡。此外，细胞内活性氧（ROS）似乎在缺氧时XQ 2的抗癌作用中起关键作用。总之，我们的数据表明，XQ 2通过抑制ROS水平并触发细胞周期停滞和与凋亡相关的半胱天冬酶依赖性途径来发挥抗癌作用。
Hypoxia is one of the inevitable circumstances of various tumors. It controls various levels of regulation in tumor progression and results in tumor resistance to radiotherapy and chemotherapy. Here we investigated a synthetic TPZ derivative, N-ethoxymethyl-3-amino-1,2,4-benzotriazine-1,4-dioxide (XQ2), a novel compound that induced anti-cancer effects both in normoxia and in hypoxia, cell proliferation assay found that XQ2 exhibited a potent inhibitory effect on the tested cancer cell lines both in normoxia and in hypoxia. Flow cytometry and western blot studies indicated that XQ2 induces G2/M arrest and a caspase-dependent apoptosis in A549 cells. Additionally, intracellular reactive oxygen species (ROS) appear to play a key role in the anticancer effect of XQ2 in hypoxia. Taken together, our data suggest that XQ2 exerted anticancer action by suppressing the ROS level and triggering cell-cycle arrest and the caspase-dependent pathway, which is associated with apoptosis.
影响因子：
11.2
作者：
S. Krajewski;S. Tanaka;S. Takayama;M. J. Schibler;W. Fenton;John Calvin Reed
通讯作者：
S. Krajewski;S. Tanaka;S. Takayama;M. J. Schibler;W. Fenton;John Calvin Reed
影响因子：
29
作者：
Guzy, RD;Hoyos, B;Schumacker, PT
通讯作者：
Schumacker, PT