Jin Meihua, Zhao Wennan, Zhang Yanwen, Kobayashi Motomasa, Duan Hongquan, Kong Dexin
Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmaceutical Sciences and Research Center of Basic Medical Sciences, Tianjin Medical University, Tianjin 300070, China; E-Mails:
Int J Mol Sci. 2011;12(11):7352-9. doi: 10.3390/ijms12117352. Epub 2011 Oct 26.
We previously isolated aaptamine, a benzonaphthyridine alkaloid, from marine sponge Aaptos suberitoids. In this study, we investigated the anti-proliferative effect of aaptamine on chronic myeloid leukemia (CML) K562 cells. Aaptamine inhibited growth of K562 with a GI50 as 10 μM, and arrested cell cycle at G2/M phase. Western blot analysis indicated that aaptamine induced p21 expression in K562 cells. Moreover, p21 promoter was activated by aaptamine treatment in p21 transfected K562 cells. Since K562 is p53 negative, aaptamine was demonstrated to be a p53-independent p21 inducer in CML cells.
我们之前从海洋海绵类软海绵属中分离出了aaptamine，一种苯并萘啶生物碱。在本研究中，我们调查了aaptamine对慢性髓性白血病（CML）K562细胞的抗增殖作用。Aaptamine以10 μM的半数生长抑制浓度（GI50）抑制K562细胞的生长，并使细胞周期停滞在G2/M期。蛋白质免疫印迹分析表明，aaptamine在K562细胞中诱导p21表达。此外，在转染p21的K562细胞中，aaptamine处理激活了p21启动子。由于K562细胞p53呈阴性，因此aaptamine被证明是CML细胞中一种不依赖p53的p21诱导剂。
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