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鱼藤素,一种天然的鱼藤酮类化合物,通过诱导凋亡在体外抑制小鼠骨髓瘤细胞生长。

Deguelin, a natural rotenoid, inhibits mouse myeloma cell growth in vitro via induction of apoptosis.

作者信息

Li Zhengguang, Wu Jun, Wu Changping, Jiang Jingting, Zheng Xiao, Xu Bin, Li Min

机构信息

Department of Oncology, The Third Affiliated Hospital of Soochow University, Changzhou 213003, P.R. China.

出版信息

Oncol Lett. 2012 Oct;4(4):677-681. doi: 10.3892/ol.2012.790. Epub 2012 Jul 6.

Abstract

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.

摘要

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。

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