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番荔枝宁,一种单四氢呋喃类乙酰原,可使癌细胞停滞于G1期,并通过与Bax和半胱天冬酶-3相关的途径引起细胞毒性。

Annonacin, a mono-tetrahydrofuran acetogenin, arrests cancer cells at the G1 phase and causes cytotoxicity in a Bax- and caspase-3-related pathway.

作者信息

Yuan Shyng-Shiou F, Chang Hsueh-Ling, Chen Hsiao-Wen, Yeh Yao-Tsung, Kao Ying-Hsien, Lin Kuei-Hsiang, Wu Yang-Chang, Su Jinu-Huang

机构信息

Department of Obstetrics and Gynecology, Kaohsiung Medical University, Kaohsiung, Taiwan 807, ROC.

出版信息

Life Sci. 2003 May 9;72(25):2853-61. doi: 10.1016/s0024-3205(03)00190-5.

DOI:10.1016/s0024-3205(03)00190-5
PMID:12697268
Abstract

Annonaceous acetogenins are a group of potential anti-neoplastic agents isolated from Annonaceae plants. In this study, we purified annonacin, a cytotoxic mono-tetrahydrofuran acetogenin, from the seeds of Annona reticulata and analyzed its biological effects. Herein, we have shown that annonacin caused significant cell death in various cancer cell lines. T24 bladder cancer cells at the S phase were more vulnerable to the cytotoxicity of annonacin. Furthermore, annonacin activated p21 in a p53-independent manner and arrested T24 cells at the G1 phase. It also induced Bax expression, enhanced caspase-3 activity, and caused apoptotic cell death in T24 cells. In summary, these results suggest that annonacin is potentially a promising anti-cancer compound.

摘要

番荔枝乙缩醛内酯是从番荔枝科植物中分离出的一类具有潜在抗肿瘤活性的物质。在本研究中,我们从番荔枝种子中纯化出了具有细胞毒性的单四氢呋喃乙缩醛内酯annonacin,并分析了其生物学效应。在此,我们发现annonacin可导致多种癌细胞系发生显著的细胞死亡。处于S期的T24膀胱癌细胞对annonacin的细胞毒性更为敏感。此外,annonacin以不依赖p53的方式激活p21,并使T24细胞停滞于G1期。它还诱导Bax表达,增强caspase-3活性,并导致T24细胞发生凋亡性细胞死亡。总之,这些结果表明annonacin可能是一种有前景的抗癌化合物。

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