萘酚醛席夫碱过渡金属配合物的合成、晶体结构及抗肿瘤活性 |
Synthesis, crystal structures, and antitumor activities of transition metal complexes incorporating a naphthol-aldehyde Schiff base ligand |
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摘要: 合成了3种萘酚醛缩色胺席夫碱过渡金属配合物[Cu (L)2(DMF)2](1)、[Ni (L)2(DMF)2](2)和[Zn (L)2](3),其中HL=N-[(2-hydroxy-1-naphthalenyl) methylene]-[(1H-indol-3-yl) ethyl]imine。利用红外光谱、元素分析和单晶X射线衍射等测试手段对配合物1~3进行了结构表征。采用MTT法对该系列配合物进行了体外抗肿瘤活性初筛,结果表明配合物1~3对人胃癌细胞MGC-803、人非小细胞肺癌细胞A549和人乳腺癌细胞MDA-MB-231都有较好的抑制作用。通过流式细胞术检测配合物1诱导肿瘤细胞凋亡的情况,结果显示配合物1诱导MGC-803细胞发生晚期凋亡;随后,细胞刮板实验表明随着配合物1浓度的增加,其对MGC-803细胞的杀伤作用增强,且杀伤作用呈剂量依赖性。 |
关键词: 萘酚醛席夫碱 过渡金属配合物 合成 晶体结构 抗肿瘤活性 |
基金项目: 安徽省高校自然科学研究项目(No.2024AH051920,2023AH051762)和国家级大学生创新创业训练计划项目(No.202310368050)资助。 |
Abstract: To study the synthesis and antitumor activities of the transition metal complexes incorporating a novel naphthol-aldehyde Schiff base ligand, three transition metal complexes [Cu(L)2(DMF)2] (1), [Ni(L)2(DMF)2] (2), and [Zn(L)2] (3) were synthesized using a Schiff base of N-[(2-hydroxy-1-naphthalenyl)methylene]-[(1H-indol-3-yl)ethyl] imine (HL) by liquid diffusion method. The complexes 1-3 were characterized by IR analysis, elemental analysis, and single-crystal X-ray diffraction. Moreover, their antitumor activities in vitro were screened through three human cancer cell lines (MGC-803, A549, MDA-MB-231) by the MTT assay. It revealed that complexes 1-3 showed high antitumor activities. Complex 1 showed much higher antitumor activities than complexes 2 and 3, and even than cisplatin. Among them, complex 1 had the highest inhibitory effects on tumor cells with its IC50 value (half-inhibitory concentration) being (4.8±0.2) μmol·L-1 against MGC-803 cells. These demonstrated a potential anti-cancer candidate for complex 1, which induced MGC-803 cancer cells' late apoptosis by flow cytometry. Subsequently, the cell scraper experiment showed that the killing effect of MGC-803 cells was enhanced with the increase in the concentration of complex 1. |
Keywords: naphthol-aldehyde Schiff base transition metal complex synthesis crystal structure antitumor activity |
投稿时间:2024-07-23 修订日期:2024-09-30 |
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吴静,惠朴真,郑慧林,袁平川,汪春飞,王慧,谷晓霞.萘酚醛席夫碱过渡金属配合物的合成、晶体结构及抗肿瘤活性[J].无机化学学报,2024,40(12):2422-2428. |
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