| 张震.3,5-二氨基苯甲酸缩邻香草醛席夫碱镉配合物的合成及抗肿瘤活性研究[J].济宁医学院学报,2014,(3):153-157,161 |
| 3,5-二氨基苯甲酸缩邻香草醛席夫碱镉配合物的合成及抗肿瘤活性研究 |
| Synthesis and anti-tumor activity of cadmium complex with 3,5-diaminobenzoic acid o-vanillin Schiff base |
| 投稿时间：2014-05-03 |
| DOI：10.3969/j.issn.1000-9760.2014.03.001 |
| 中文关键词: 席夫碱;镉配合物;抗肿瘤活性7 |
| 英文关键词: Schiff base;Cd complex;Anti-tumor activity |
| 基金项目: |
| 作者 | 单位 | | 张震 | 济宁医学院药学院, 山东日照 276826 |
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| 中文摘要: |
| 目的 合成新的席夫碱配体及其金属配合物并对其抗肿瘤活性进行研究。方法 合成了3,5-二氨基苯甲酸席夫碱配体及其Cd(Ⅱ)的配合物,经元素分析、红外光谱、核磁共振谱、热重分析及摩尔电导率等手段进行表征。通过细胞增殖分析、蛋白酶体活性分析、免疫蛋白印迹分析及细胞形态分析研究了配合物的体外抗肿瘤活性。结果 制备了席夫碱配体L和配合物CdL,解析得其分子式分别为(C7H4N2O2)(C8H6O2)2和[Cd(C7H4N2O2)(C8H6O2)2]·2H2O。活性研究显示,CdL可以有效地抑制肿瘤细胞增殖且具有良好的蛋白酶体抑制活性,其IC50值为 3.3 μM;在设定的时间条件下,CdL对乳腺癌MDA-MB-231细胞蛋白酶体CT活性的抑制作用和细胞凋亡的诱导能力,均呈浓度和时间依赖方式;乳腺癌MDA-MB-231细胞比正常MCF-10A 细胞对CdL的敏感性高得多。结论 配合物CdL能够抑制肿瘤细胞内蛋白酶体CT活性,从而诱导肿瘤细胞凋亡,且对正常细胞的毒性较小。 |
| 英文摘要: |
| Objective To synthesize new Schiff base ligands and its metal complex and explore their anti-tumor activity.Methods 3,5-diaminobenzoic acid o-vanillin Schiff base and its Cd(Ⅱ) complexes were prepared and characterized by elemental analyses,IR,1HNMR,TG analysis and molar conductance.Its anti-tumor activity in vitro was studied by cell proliferation assay,proteasomal activity assay,western blot and cellular morphology analysis in human breast cancer cells.Results The Schiff base and its Cd(II) complexes were successfully prepared,and their molecular formula were(C7H4N2O2)(C8H6O2)2和[Cd(C7H4N2O2)(C8H6O2)2]·2H2O.CdL was found to effectively inhibit the CT-like activity of purified 20S proteasome with IC50 values of 3.3 μM.Moreover,inhibition of cancer cell proliferation also correlated with this effect.CdL possessed proteasome inhibition capability and induced apoptosis in a concentration-and time-dependent manner in the ER-negative MDA-MB-231 human breast cancer cells.At the same time,MCF-10A cells were much less sensitive to the CdL complexes when compared to MDA-MB-231 breast cancer cells.Conclusion Organic complexes CdL is capable of inhibiting tumor cellular proteasome activity and consequently inducing cancer-cell-specific apoptotic death. |
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