Karahan Emrah, Gençoğlu Katmerlikaya Tuğba, Önal Emel, Dağ Aydan, Gürek Ayşe Gül, Ahsen Vefa
Department of Chemistry, Gebze Technical University, Kocaeli, Turkiye.
Department of Biotechnology, Institute of Health Sciences, Bezmiâlem Vakıf University, İstanbul, Turkiye.
Turk J Chem. 2024 Jan 22;48(4):582-596. doi: 10.55730/1300-0527.3681. eCollection 2024.
Breast cancer is one of the most common types of cancer worldwide and has the most lethality ratio for females among all cancers. Although current cancer therapeutics have made considerable advancements, there is still room for improvement in terms of efficacy. Many anticancer drugs have a risk of causing serious adverse effects due to their nonspecific cytotoxic effects on both tumor and healthy cells. New therapeutics might have a greater ability to kill cancer cells, reduce the volume of tumors, and improve overall therapy response rates. Herein, we report the efficient synthesis and characterization of three amphi -dioximes and their six novel mono-, which are extremely rare in platinum chemistry, and bisplatinum(II) complexes for breast cancer treatment. Antitumoral activities of Pt(II) complexes have been investigated on CCD-1079Sk healthy fibroblast cell line, MCF-7 and MDA-MB-231 human breast cancer cell lines. Cytotoxicity, cell cycle, and apoptotic assays were performed. All new Pt(II) complexes exhibited selective antiproliferative effects on breast cancer cells by showing less cytotoxicity to healthy cells than known anticancer drugs cisplatin and bicalutamide. In vitro studies show that these new Pt complexes have high anticancer and antiproliferative effects and may be new alternatives to existing anticancer drugs.
乳腺癌是全球最常见的癌症类型之一,在所有癌症中,女性乳腺癌的致死率最高。尽管目前的癌症治疗方法已经取得了显著进展,但在疗效方面仍有改进空间。许多抗癌药物由于对肿瘤细胞和健康细胞都具有非特异性细胞毒性作用,存在引起严重不良反应的风险。新型治疗方法可能具有更强的杀死癌细胞、缩小肿瘤体积以及提高总体治疗反应率的能力。在此,我们报告了三种两性二肟及其六种新型单肟(在铂化学中极为罕见)和双铂(II)配合物的高效合成与表征,用于乳腺癌治疗。对Pt(II)配合物的抗肿瘤活性在CCD - 1079Sk健康成纤维细胞系、MCF - 7和MDA - MB - 231人乳腺癌细胞系上进行了研究。进行了细胞毒性、细胞周期和凋亡分析。所有新的Pt(II)配合物对乳腺癌细胞均表现出选择性抗增殖作用,与已知抗癌药物顺铂和比卡鲁胺相比,对健康细胞的细胞毒性更小。体外研究表明,这些新的Pt配合物具有较高的抗癌和抗增殖作用,可能成为现有抗癌药物的新替代品。