Yılmaz Ismail, Akar Okan Remzi, Erkisa Merve, Selvi Selin, Şengül Abdurrahman, Ulukaya Engin
Department of Chemistry, Faculty of Science, Karabük University, 78050 Karabük, Turkey.
Department of Cancer Biology and Pharmacology Institute of Medical Sciences, Istinye University, 34010 Istanbul, Turkey.
ACS Med Chem Lett. 2020 Mar 12;11(5):940-948. doi: 10.1021/acsmedchemlett.9b00676. eCollection 2020 May 14.
A new mononuclear cationic platinum(II) coordination compound with 6,6'-bis(NH-benzimidazol-2-yl)-2,2'-bipyridine () ligand having N-tetradentate binding pocket [Pt()]Cl·2HO () was synthesized and characterized by FT-IR(ATR), UV-vis, H NMR, APCI and MALDI MS, and CHN analysis. The antigrowth effect of was tested in breast cancer (MDA-MB-231), lung cancer (A549), colorectal cancer (HCT-116), prostate cancer (PC-3) cell lines, and bronchial epithelial cell line (BEAS-2B) by the SRB and ATP cell viability assays. Apoptosis was detected with Annexin V, mitopotential, BCL-2 inactivation, and γH2AX assays by flow cytometry. was found to have cytotoxic activity of MDA-MB-231, A549, HCT-116, and PC-3 cancer cell lines in a dose-dependent manner for 48 h. has been found to cause cell death through different mechanisms depending on the type of cancer. The findings indicated that complex induced intrinsic apoptosis with the increased mitochondrial membrane depolarization level, Bcl-2 inactivation, and DNA damage in PC-3 and A549 cell lines.
合成了一种具有N-四齿结合口袋的新型单核阳离子铂（II）配位化合物，该化合物带有6,6'-双（NH-苯并咪唑-2-基）-2,2'-联吡啶（）配体[Pt（）]Cl·2HO（），并通过傅里叶变换红外光谱（衰减全反射）、紫外可见光谱、核磁共振氢谱、大气压化学电离和基质辅助激光解吸电离质谱以及元素分析对其进行了表征。通过磺酰罗丹明B和ATP细胞活力测定法，在乳腺癌（MDA-MB-231）、肺癌（A549）、结肠直肠癌（HCT-116）、前列腺癌（PC-3）细胞系以及支气管上皮细胞系（BEAS-2B）中测试了的抗生长作用。通过流式细胞术用膜联蛋白V、线粒体电位、BCL-2失活和γH2AX测定法检测细胞凋亡。发现对MDA-MB-231、A549、HCT-116和PC-3癌细胞系具有48小时剂量依赖性的细胞毒活性。已发现根据癌症类型通过不同机制导致细胞死亡。研究结果表明，该配合物在PC-3和A549细胞系中通过增加线粒体膜去极化水平、Bcl-2失活和DNA损伤诱导内源性凋亡。
