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线粒体在新合成查耳酮诱导的肝癌细胞内源性凋亡中的作用

Mitochondrial Role in Intrinsic Apoptosis Induced by a New Synthesized Chalcone in Hepatocellular Carcinoma Cells.

作者信息

Santarsiero Anna, Pappalardo Ilaria, Rosa Gabriella Margherita, Pisano Isabella, Superchi Stefano, Convertini Paolo, Todisco Simona, Scafato Patrizia, Infantino Vittoria

机构信息

Department of Science, University of Basilicata, Viale dell'Ateneo Lucano 10, 85100 Potenza, Italy.

Department of Biosciences, Biotechnologies and Biopharmaceutics, University of Bari, Via Orabona 4, 70125 Bari, Italy.

出版信息

Biomedicines. 2022 Dec 2;10(12):3120. doi: 10.3390/biomedicines10123120.

DOI:10.3390/biomedicines10123120
PMID:36551876
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9775964/
Abstract

Hepatocellular carcinoma (HCC) is the most common type of liver cancer and the fourth cause of cancer-related deaths worldwide. Presently, a few drugs are available for HCC treatment and prevention, including both natural and synthetic compounds. In this study, a new chalcone, ()-1-(2,4,6-triethoxyphenyl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (ETTC), was synthesized and its effects and mechanisms of action over human hepatoma cells were investigated. Cytotoxic activity was revealed in HCC cells, while no effects were observed in normal hepatocytes. In HCC cells, ETTC caused subG1 cell cycle arrest and apoptosis, characterized by nuclear fragmentation. The activation of caspases 3/7 and 9, the increase in pro-apoptotic BAX, and the decrease in anti-apoptotic BCL-2 suggest the activation of the intrinsic pathway of apoptosis. ETTC mitochondrial targeting is confirmed by the reduction in mitochondrial membrane potential and Complex I activity together with levels of superoxide anion increasing. Our outcomes prove the potential mitochondria-mediated antitumor effect of newly synthesized chalcone ETTC in HCC.

摘要

肝细胞癌（HCC）是最常见的肝癌类型，也是全球癌症相关死亡的第四大原因。目前，有几种药物可用于HCC的治疗和预防，包括天然和合成化合物。在本研究中，合成了一种新的查尔酮，（）-1-（2,4,6-三乙氧基苯基）-3-（3,4,5-三甲氧基苯基）丙-2-烯-1-酮（ETTC），并研究了其对人肝癌细胞的作用及其作用机制。在肝癌细胞中显示出细胞毒性活性，而在正常肝细胞中未观察到作用。在肝癌细胞中，ETTC导致亚G1期细胞周期停滞和凋亡，其特征为核碎裂。半胱天冬酶3/7和9的激活、促凋亡BAX的增加以及抗凋亡BCL-2的减少表明凋亡的内在途径被激活。线粒体膜电位降低、复合体I活性降低以及超氧阴离子水平升高证实了ETTC的线粒体靶向作用。我们的结果证明了新合成的查尔酮ETTC在肝癌中潜在的线粒体介导的抗肿瘤作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/67c8750697c5/biomedicines-10-03120-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/7c1973e69263/biomedicines-10-03120-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/c81dba07c5c5/biomedicines-10-03120-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/a7db783dcec0/biomedicines-10-03120-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/23393e3f820b/biomedicines-10-03120-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/08dbdbe0db38/biomedicines-10-03120-g004a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/787d21e2a5dd/biomedicines-10-03120-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/67c8750697c5/biomedicines-10-03120-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/7c1973e69263/biomedicines-10-03120-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/c81dba07c5c5/biomedicines-10-03120-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/a7db783dcec0/biomedicines-10-03120-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/23393e3f820b/biomedicines-10-03120-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/08dbdbe0db38/biomedicines-10-03120-g004a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/787d21e2a5dd/biomedicines-10-03120-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c7b/9775964/67c8750697c5/biomedicines-10-03120-g006.jpg

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2
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Pharmaceuticals (Basel). 2022 Oct 11;15(10):1250. doi: 10.3390/ph15101250.
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Cancers (Basel). 2024 Mar 8;16(6):1092. doi: 10.3390/cancers16061092.
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