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组蛋白去乙酰化酶抑制剂CG-745与伏立诺他在非小细胞肺癌中的抗癌效果比较

Comparison of Anticancer Effects of Histone Deacetylase Inhibitors CG-745 and Suberoylanilide Hydroxamic Acid in Non-small Cell Lung Cancer.

作者信息

Kim Hyo Jin, An Ui Ri, Yoon Han Jee, Lim Hyun, Hwang Ki Eun, Kim Young Suk, Kim Hak Ryul

机构信息

Division of Pulmonary Medicine, Department of Internal Medicine, Wonkwang University School of Medicine, Iksan, Republic of Korea.

出版信息

Tuberc Respir Dis (Seoul). 2025 Apr;88(2):342-352. doi: 10.4046/trd.2024.0090. Epub 2025 Feb 13.

DOI:10.4046/trd.2024.0090
PMID:39947744
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12010713/
Abstract

BACKGROUND

Histone deacetylase (HDAC) inhibition offers potential anticancer effects across diverse cancers due to HDAC's significant role in cancer development and progression. Consequently, we demonstrated the therapeutic efficacy of the novel HDAC inhibitor, CG-745, in comparison with existing inhibitors such as suberoylanilide hydroxamic acid (SAHA) in non-small cell lung cancer (NSCLC) cells.

METHODS

CG-745's effect on apoptosis and reactive oxygen species (ROS)-dependent mitochondrial dysfunction was investigated using annexin V assay, MitoSoX, and Western blot in human A549 and H460 cells. Additionally, HDAC expression was analyzed through real-time polymerase chain reaction. We also evaluated the inhibitory effect of CG-745 on epithelial-mesenchymal transition (EMT) induced by transforming growth factor β1 (TGF-β1) via Western blot, scratch analysis, and matrigel invasion analysis.

RESULTS

Compared to SAHA, CG-745 inhibited cell viability and mRNA expression of HDACs such as HDAC1, HDAC2, HDAC3, and HDAC8. It also induced apoptosis, ROS, and mitochondrial dysfunction in a concentration-dependent manner. CG-745 reversed EMT triggered by TGF-β1 in A549 and H460 cells, and curtailed the migration and invasion enhanced by TGF-β1. CG-745 has demonstrably inhibited EMT and induced apoptosis in NSCLC cells.

CONCLUSION

CG-745 may represent a novel therapeutic strategy for NSCLC treatment.

摘要

背景

由于组蛋白去乙酰化酶（HDAC）在癌症发生和发展中起重要作用，HDAC抑制作用对多种癌症具有潜在的抗癌效果。因此，我们展示了新型HDAC抑制剂CG - 745与诸如伏立诺他（SAHA）等现有抑制剂相比，在非小细胞肺癌（NSCLC）细胞中的治疗效果。

方法

使用膜联蛋白V检测法、MitoSoX和蛋白质免疫印迹法，在人A549和H460细胞中研究CG - 745对凋亡和活性氧（ROS）依赖性线粒体功能障碍的影响。此外，通过实时聚合酶链反应分析HDAC表达。我们还通过蛋白质免疫印迹法、划痕分析和基质胶侵袭分析，评估了CG - 745对转化生长因子β1（TGF - β1）诱导的上皮-间质转化（EMT）的抑制作用。

结果

与SAHA相比，CG - 745抑制了HDAC1、HDAC2、HDAC3和HDAC8等HDAC的细胞活力和mRNA表达。它还以浓度依赖性方式诱导凋亡、ROS和线粒体功能障碍。CG - 745逆转了A549和H460细胞中由TGF - β1触发的EMT，并减少了TGF - β1增强的迁移和侵袭。CG - 745已明显抑制NSCLC细胞中的EMT并诱导凋亡。

结论

CG - 745可能代表一种用于NSCLC治疗的新型治疗策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cd1/12010713/18f8a48e26af/trd-2024-0090f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cd1/12010713/fd39076ad542/trd-2024-0090f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cd1/12010713/6435396e0207/trd-2024-0090f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cd1/12010713/06ef6e75c44b/trd-2024-0090f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cd1/12010713/4c6b2a81589d/trd-2024-0090f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cd1/12010713/29ea99f50e70/trd-2024-0090f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cd1/12010713/18f8a48e26af/trd-2024-0090f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cd1/12010713/fd39076ad542/trd-2024-0090f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cd1/12010713/6435396e0207/trd-2024-0090f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cd1/12010713/06ef6e75c44b/trd-2024-0090f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cd1/12010713/4c6b2a81589d/trd-2024-0090f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cd1/12010713/29ea99f50e70/trd-2024-0090f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cd1/12010713/18f8a48e26af/trd-2024-0090f6.jpg

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