Dimethyl-celecoxib (DMC), a derivative of celecoxib that lacks cyclooxygenase-2-inhibitory function, potently mimics the anti-tumor effects of celecoxib on Burkitt's lymphoma in vitro and in vivo
Dimethyl-celecoxib (DMC), a derivative of celecoxib that lacks cyclooxygenase-2-inhibitory function, potently mimics the anti-tumor effects of celecoxib on Burkitt's lymphoma in vitro and in vivo
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DOI：
10.4161/cbt.4.5.1699
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发表时间：
2005-05-01
影响因子：
3.6
通讯作者：
Schönthal, AH
中科院分区：
文献类型：
--
作者：
Kardosh, A;Wang, WJ;Schönthal, AH
非甾体抗炎药塞来昔布是一种选择性环氧化酶-2 （COX-2）抑制剂，作为抗癌药物已经显示出一些有希望的结果。然而，关于其抗肿瘤特性是否需要cox -2抑制功能的问题出现了。因此，我们采用了二甲基塞来昔布（DMC）来研究这个问题，它是塞来昔布的一种结构类似物，缺乏cox -2抑制功能。通过对伯基特淋巴瘤细胞进行体外和体内联合研究，我们发现DMC有效地模仿塞来昔布的所有抗增殖和抗肿瘤作用。在细胞培养中，DMC通过下调细胞周期蛋白A和B，以及随后丧失细胞周期蛋白依赖性激酶活性，有效抑制细胞增殖。这种效应似乎也发生在体内，并导致显著(p
The nonsteroidal anti-inflammatory drug (NSAID) celecoxib is a selective cyclooxygenose-2 (COX-2) inhibitor that has shown some promising results as an anti-cancer drug. However, the question arose as to whether or not its COX-2-inhibitory function is required for its anti-tumorigenic properties. We therefore employed dimethyl-celecoxib (DMC), which is a close structural analog of celecoxib that lacks COX-2-inhibitory function, to investigate this question. By performing a combination of in vitro and in vivo studies with Burkitt's lymphoma cells, we found that DMC potently mimics all of the anti-proliferative and anti-tumorigenic effects of celecoxib. In cell culture, DMC effectively inhibits cell proliferation through the down-regulation of cyclins A and B and the ensuing loss of cyclin-dependent kinase activity. This effect appears to take place in vivo as well and results in significantly (p