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A化合物性质的研究进展：乳腺癌细胞系中的细胞毒性活性及己糖激酶II的下调

Advances in the Properties of Incomptine A: Cytotoxic Activity and Downregulation of Hexokinase II in Breast Cancer Cell Lines.

作者信息

Arietta-García Angel Giovanni, Calzada Fernando, Ramírez-Sánchez Israel, Bautista Elihú, García-Hernandez Normand, Ordoñez-Razo Rosa María

机构信息

Unidad de Investigación Médica en Genética Humana, UMAE Hospital de Pediatría 2° Piso, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Mexico City CP 06725, Mexico.

Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades, 2° Piso CORSE, Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Mexico City CP 06725, Mexico.

出版信息

Int J Mol Sci. 2023 Aug 3;24(15):12406. doi: 10.3390/ijms241512406.

DOI:10.3390/ijms241512406
PMID:37569780
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10419048/
Abstract

Breast cancer treatments are limited by the cancer subtype and its selectivity towards tumor cells, hence the importance of finding compounds that increase the survival of healthy cells and target any subtype. Incomptine A (IA) is a sesquiterpene lactone with demonstrated cytotoxic activity. In this study, through assays, it was observed that IA has similar cytotoxic activity between the subtypes triple negative, HER2+, and luminal A of the breast cancer cell lines. IA cytotoxic activity is higher in cancer than in nontumorigenic cells, and its selectivity index for cancer cells is more than that of the drug doxorubicin. Molecular docking and its comparison with the 2-Deoxyglucose inhibitor suggest that IA could bind to Hexokinase II (HKII), decreasing its expression. Since we did not find changes in the expression of the glycolytic pathway, we suppose that IA could affect the antiapoptotic function of HKII in cancer cells. The IA-HKII union would activate the voltage-gated anion channel 1 (VDAC1), resuming apoptosis. Therefore, we suggest that IA could be used against almost any subtype and that its cytotoxic effect could be due to the reactivation of apoptosis in breast cancer cells.

摘要

乳腺癌治疗受到癌症亚型及其对肿瘤细胞的选择性限制，因此找到能提高健康细胞存活率并靶向任何亚型的化合物至关重要。茵陈炔内酯A（IA）是一种具有细胞毒性活性的倍半萜内酯。在本研究中，通过实验观察到IA在三阴性、HER2 +和腔面A型乳腺癌细胞系亚型之间具有相似的细胞毒性活性。IA在癌细胞中的细胞毒性活性高于非致瘤细胞，其对癌细胞的选择性指数高于阿霉素。分子对接及其与2-脱氧葡萄糖抑制剂的比较表明，IA可能与己糖激酶II（HKII）结合，降低其表达。由于我们未发现糖酵解途径表达的变化，我们推测IA可能影响HKII在癌细胞中的抗凋亡功能。IA与HKII的结合会激活电压门控阴离子通道1（VDAC1），恢复细胞凋亡。因此，我们认为IA可用于对抗几乎任何亚型，其细胞毒性作用可能是由于乳腺癌细胞中细胞凋亡的重新激活。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05f3/10419048/5e1a7ba5c2a9/ijms-24-12406-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05f3/10419048/099f11b0b754/ijms-24-12406-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05f3/10419048/c9ec9bbedef5/ijms-24-12406-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05f3/10419048/1950184444cf/ijms-24-12406-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05f3/10419048/95eecb9ac55f/ijms-24-12406-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05f3/10419048/5e1a7ba5c2a9/ijms-24-12406-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05f3/10419048/099f11b0b754/ijms-24-12406-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05f3/10419048/c9ec9bbedef5/ijms-24-12406-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05f3/10419048/1950184444cf/ijms-24-12406-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05f3/10419048/95eecb9ac55f/ijms-24-12406-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05f3/10419048/5e1a7ba5c2a9/ijms-24-12406-g005.jpg

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2
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Genes (Basel). 2022 Mar 20;13(3):549. doi: 10.3390/genes13030549.
3
Expanding the Study of the Cytotoxicity of Incomptines A and B against Leukemia Cells.研究不完整化合物 A 和 B 对白血病细胞的细胞毒性。
使用纳米载体靶向三阴性乳腺癌干细胞
Discov Nano. 2024 Mar 7;19(1):41. doi: 10.1186/s11671-024-03985-y.
Molecules. 2022 Mar 4;27(5):1687. doi: 10.3390/molecules27051687.
4
Glucose deprivation using 2-deoxyglucose and acarbose induce metabolic oxidative stress and apoptosis in female mice bearing breast cancer.葡萄糖剥夺使用 2-脱氧葡萄糖和阿卡波糖诱导患有乳腺癌的雌性小鼠发生代谢性氧化应激和细胞凋亡。
Biochimie. 2022 Apr;195:59-66. doi: 10.1016/j.biochi.2022.01.007. Epub 2022 Jan 20.
5
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6
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