Fan S, Duba D E, O'Connor P M
Department of Radiation Oncology, Long Island Jewish Medical Center, New Hyde Park, NY 11042, USA.
Chemotherapy. 1999 Nov-Dec;45(6):437-45. doi: 10.1159/000007237.
Olomoucine, a purine derivative, inhibits multiple cyclin-dependent kinases that play important roles in regulating the G1/S and G2/M transitions of the cell cycle. In this study we investigated the cellular effects of olomoucine in two human Burkitt's lymphoma cell lines, WMN (containing wild-type p53) and CA46 (containing mutant p53), and found that in consistency with its ability to block the activity of cyclin E/Cdk2 and cyclin B1/Cdc2 kinases, olomoucine caused cell cycle arrest at both G1/S and G2/S boundaries. Moreover, cell cycle arrest occurred equally well in these two cell lines bearing different p53 gene status, suggesting that p53 was not responsible for the cell cycle arrest by olomoucine. A similar p53-independent fashion was also observed in the cytotoxic potency and apoptosis induction of olomoucine, in contrast to ionizing radiation which caused more cytotoxic activity and apoptosis in the WMN cell line bearing wild-type p53 compared with CA46 cells bearing mutant p53. Such p53-independent cytotoxicity of olomoucine was also confirmed in other human Burkitt's lymphoma and lymphoid cell lines containing wild-type and mutant p53. Therefore, our results give an impetus to continued research into olomoucine that might be a very useful chemotherapeutic strategy in the treatment of patients with mutant p53 tumors, at least in lymphoma patients.
奥洛莫辛是一种嘌呤衍生物,可抑制多种细胞周期蛋白依赖性激酶,这些激酶在调节细胞周期的G1/S和G2/M转换中发挥重要作用。在本研究中,我们研究了奥洛莫辛对两种人类伯基特淋巴瘤细胞系WMN(含野生型p53)和CA46(含突变型p53)的细胞作用,发现与其阻断细胞周期蛋白E/Cdk2和细胞周期蛋白B1/Cdc2激酶活性的能力一致,奥洛莫辛导致细胞周期在G1/S和G2/S边界处停滞。此外,在这两种具有不同p53基因状态的细胞系中,细胞周期停滞的情况同样良好,这表明p53与奥洛莫辛引起的细胞周期停滞无关。在奥洛莫辛的细胞毒性效力和诱导凋亡方面也观察到类似的不依赖p53的方式,与之形成对比的是,与含突变型p53的CA46细胞相比,电离辐射在含野生型p53的WMN细胞系中引起了更强的细胞毒性活性和凋亡。奥洛莫辛这种不依赖p53的细胞毒性在其他含野生型和突变型p53的人类伯基特淋巴瘤和淋巴细胞系中也得到了证实。因此,我们的结果推动了对奥洛莫辛的持续研究,奥洛莫辛可能是治疗突变型p53肿瘤患者(至少在淋巴瘤患者中)非常有用的化疗策略。