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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Antibacterial AZT derivative regulates metastasis of breast cancer cells
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Antibacterial AZT derivative regulates metastasis of breast cancer cells

机译：抗菌AZT衍生物调节乳腺癌细胞的转移

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摘要

Antimicrobial peptides (AMP) with anticancer activity have drawn remarkable attention in modern treatments. However, long peptide length and protease instability are the most addressing factors, which hampers their further development as therapeutic agents. In view of this, herein, we designed and synthesized a series of AZT-based cationic small molecule incorporating a variety of hydrophobic groups and cationic charges, including amine and guanidine groups to mimic the amphipathic structure of AMPs. These compounds were evaluated for their antibacterial activity against Gram-positive and Gram-negative bacteria. Through an extensive structure activity relationship study (SAR), we identified ADG-2e as the most potent antibacterial agent, which exhibited remarkable potency against drug resistant bacterial strains such as MRSA and MDRPA. Further, ADG-2e was examined for their anti-metastatic ability by investigating the cancer cell migration and invasiveness through scratch wound-healing assay and transwell invasive assay, respectively. In addition, time-lapse cell tracking analysis also performed for analyzing the cell movement pattern. Treatment of ADG-2e against metastatic breast cancer cells (MDA-MB-231) suppressed tumor cell migration by multi-directional lamellipodium formation, indicating their anti-metastatic potential. Thus, our cationic AZT based small molecules may evolve as an appealing class of antibacterial agents with anti-metastasis potential. (c) 2020 Elsevier Masson SAS. All rights reserved.
机译：抗微生物肽（AMP）抗癌活性在现代治疗中具有显着的关注。然而，长期肽长度和蛋白酶不稳定性是最多的寻址因子，其妨碍了它们作为治疗剂的进一步发展。鉴于此，我们设计和合成了一种基于AZT的阳离子小分子，其包含各种疏水基团和阳离子电荷，包括胺和胍基团以模拟AMPS的两亲结构。评估这些化合物对革兰氏阳性和革兰氏阴性细菌的抗菌活性。通过广泛的结构活动关系研究（SAR），我们将ADG-2E鉴定为最有效的抗菌剂，这表现出抗毒性细菌菌株如MRSA和MDRPA的显着效力。此外，通过分别通过划伤伤口愈合测定和Transwell侵袭测定来研究癌细胞迁移和侵袭来检查ADG-2E的抗转移能力。此外，还执行时间流逝小区跟踪分析，用于分析细胞运动模式。治疗转移性乳腺癌细胞的ADG-2E（MDA-MB-231）抑制了多向层层形成的肿瘤细胞迁移，表明它们的抗转移性潜力。因此，我们的阳离子基于基于的小分子可以作为具有抗转移潜力的抗菌剂的吸引力类别。 （c）2020 Elsevier Masson SAS。版权所有。

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