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阿斯特拉球酮，一种细胞周期蛋白依赖性激酶抑制剂，通过诱导细胞凋亡的作用介导 HeLa 细胞毒性。

Alsterpaullone, a Cyclin-Dependent Kinase Inhibitor, Mediated Toxicity in HeLa Cells through Apoptosis-Inducing Effect.

机构信息

College of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, China.

出版信息

J Anal Methods Chem. 2013;2013:602091. doi: 10.1155/2013/602091. Epub 2013 Mar 12.

DOI:10.1155/2013/602091
PMID:23577282
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3610382/
Abstract

Alsterpaullone, a small molecule cyclin-dependent kinase (CDK) inhibitor, regulates the cell cycle progression. Beyond death-inducing properties, we identified the effect of alsterpaullone on cycle procedure and apoptosis of HeLa cell. It was found that alsterpaullone inhibited HeLa cells in a time-dependent (0-72 h) and dose-dependent (0-30  μ M) manner. In the presence of alsterpaullone, HeLa cells were arrested in G2/M prior to undergoing apoptosis via a mechanism that is involved in the regulation of various antiapoptotic genes, DNA-repair, transcription, and cell cycle progression. Compared to controls, alsterpaullone effectively prevented HeLa cells from entering S-phase. These potential therapeutic efficacies could be correlated with the activation of caspase-3.

摘要

阿尔斯特泊酮是一种小分子细胞周期蛋白依赖性激酶 (CDK) 抑制剂，可调节细胞周期进程。除了诱导死亡的特性外，我们还确定了阿尔斯特泊酮对 HeLa 细胞周期过程和细胞凋亡的影响。结果发现，阿尔斯特泊酮以时间依赖性（0-72 h）和剂量依赖性（0-30 μM）方式抑制 HeLa 细胞。在阿尔斯特泊酮存在的情况下，HeLa 细胞在经历凋亡之前被阻滞在 G2/M 期，该机制涉及多种抗凋亡基因、DNA 修复、转录和细胞周期进程的调节。与对照组相比，阿尔斯特泊酮能有效阻止 HeLa 细胞进入 S 期。这些潜在的治疗效果可能与 caspase-3 的激活有关。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/000b/3610382/41020e2e90a2/JAMC2013-602091.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/000b/3610382/2c6b2a4923fe/JAMC2013-602091.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/000b/3610382/6d653009f139/JAMC2013-602091.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/000b/3610382/0605d7864a0b/JAMC2013-602091.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/000b/3610382/3289692aa5cb/JAMC2013-602091.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/000b/3610382/41020e2e90a2/JAMC2013-602091.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/000b/3610382/2c6b2a4923fe/JAMC2013-602091.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/000b/3610382/6d653009f139/JAMC2013-602091.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/000b/3610382/0605d7864a0b/JAMC2013-602091.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/000b/3610382/3289692aa5cb/JAMC2013-602091.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/000b/3610382/41020e2e90a2/JAMC2013-602091.005.jpg

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