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Anticancer and antimetastatic activity of copper(II)-tropolone complex against human breast cancer cells, breast multicellular spheroids and mammospheres.
Journal of Inorganic Biochemistry ( IF 3.8 ) Pub Date : 2019-12-26 , DOI: 10.1016/j.jinorgbio.2019.110975
Lucia M Balsa 1 , Maria C Ruiz 1 , Lucia Santa Maria de la Parra 1 , Enrique J Baran 1 , Ignacio E León 1
Affiliation  

The goal of this work was to display the anticancer and antimetastatic activity of a copper(II) with tropolone (trp), complex [Cu(trp)2] toward human breast cancer cells in monolayer (2D) and spheroids (3D). Cytotoxicity assays against MCF7 (IC50(complex) = 5.2 ± 1.8 μM, IC50(CDDP) = 19.3 ± 2.1 μM) and MDA-MB-231 (IC50(complex) = 4.0 ± 0.2 μM, IC50(CDDP) = 27.0 ± 1.9 μM) demonstrate that [Cu(trp)2] exert greater antitumor potency than cisplatin (CDDP) on 2D and 3D human breast cancer cell models. Besides, [Cu(trp)2] inhibits cell migration by reducing the metalloproteinases activities and the compound undergoes the breast cancer cells to apoptosis at lower concentrations (2.5-10 μM). Moreover, [Cu(trp)2] overcame CDDP presenting an IC50 value 26-fold more lower against breast multicellular spheroids ((IC50(complex) = 4.9 μM, IC50(CDDP) = 130 μM)). Also, our results showed that [Cu(trp)2] inhibited the cell migration and cell invasion of breast multicellular spheroids, showing that [Cu(trp)2] exhibited antimetastatic properties. On the other hand, [Cu(trp)2] reduced mammosphere forming capacity affecting the size and number of mammospheres. Taken together, [Cu(trp)2] exhibited anticancer and antimetastatic properties on monolayer (2D) and spheroids (3D) derived from human breast cancer cells.

中文翻译:

铜(II)-马酚酮复合物对人乳腺癌细胞,乳房多细胞球体和乳腺球的抗癌和抗转移活性。

这项工作的目的是展示铜(II)与曲托酮(trp),复合物[Cu(trp)2]对单层(2D)和球形(3D)中人乳腺癌细胞的抗癌和抗转移活性。针对MCF7(IC50(复合物)= 5.2±1.8μM,IC50(CDDP)= 19.3±2.1μM)和MDA-MB-231(IC50(复合物)= 4.0±0.2μM,IC50(CDDP)= 27.0±1.9)的细胞毒性测定μM)证明[Cu(trp)2]在2D和3D人乳腺癌细胞模型上比顺铂(CDDP)发挥更大的抗肿瘤作用。此外,[Cu(trp)2]通过降低金属蛋白酶活性抑制细胞迁移,并且该化合物以较低的浓度(2.5-10μM)经历乳腺癌细胞的凋亡。此外,[Cu(trp)2]克服了CDDP,相对于乳房多细胞球体,IC50值降低了26倍((IC50(复合物)= 4.9μM,IC50(CDDP)= 130μM))。此外,我们的结果表明[Cu(trp)2]抑制了乳腺癌多细胞球体的细胞迁移和细胞侵袭,表明[Cu(trp)2]表现出抗转移特性。另一方面,[Cu(trp)2]降低了乳球形成能力,影响了乳球的大小和数量。两者合计,[Cu(trp)2]在源自人乳腺癌细胞的单层(2D)和球体(3D)上显示出抗癌和抗转移特性。
更新日期:2019-12-27
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