Li Zhengguang, Wu Jun, Wu Changping, Jiang Jingting, Zheng Xiao, Xu Bin, Li Min
Department of Oncology, The Third Affiliated Hospital of Soochow University, Changzhou 213003, P.R. China.
Oncol Lett. 2012 Oct;4(4):677-681. doi: 10.3892/ol.2012.790. Epub 2012 Jul 6.
Deguelin is a naturally occurring rotenoid with strong cancer chemopreventive and antitumor activities. In the present study, we investigated the antitumor activity of deguelin against MPC-11 murine myeloma cells and the possible mechanism of action in vitro. Our results revealed that deguelin inhibited the proliferation of MPC-11 cells in a concentration- and time-dependent manner and caused the apoptotic death of MPC-11 cells. Following exposure to deguelin, the phosphorylation of Akt was decreased. The inhibition of cell growth may be associated with decreased levels of phosphorylated Akt. Deguelin-induced apoptosis was characterized by the upregulation of Bax, downregulation of Bcl-2 and activation of caspase-3. In conclusion, deguelin inhibits murine myeloma cell proliferation by inducing apoptosis via regulation of the Bax/Bcl-2 ratio and by inhibition of the activation of Akt. Its potential as an anticancer agent against multiple myeloma warrants further investigation.
鱼藤素是一种天然存在的鱼藤酮类化合物,具有很强的癌症化学预防和抗肿瘤活性。在本研究中,我们研究了鱼藤素对MPC - 11小鼠骨髓瘤细胞的抗肿瘤活性及其体外可能的作用机制。我们的结果表明,鱼藤素以浓度和时间依赖性方式抑制MPC - 11细胞的增殖,并导致MPC - 11细胞凋亡死亡。暴露于鱼藤素后,Akt的磷酸化水平降低。细胞生长的抑制可能与磷酸化Akt水平的降低有关。鱼藤素诱导的凋亡表现为Bax上调、Bcl - 2下调和caspase - 3激活。总之,鱼藤素通过调节Bax/Bcl - 2比值诱导凋亡并抑制Akt激活来抑制小鼠骨髓瘤细胞增殖。其作为抗多发性骨髓瘤抗癌剂的潜力值得进一步研究。