氨基酸席夫碱氧钒(Ⅳ)配合物的合成、晶体结构及其抗肿瘤活性（英文）  

Study on the synthesis,crystal structure and in vitro anticancer activities of three novel oxovanadium(Ⅳ) complexes with ligands of amino acid schiff base and 1,10- phenanthroline

作　　者：曹亚萍[1] 易芩兰 刘洪梅[1] 李海霞[1] 左建丽[1] 袁泽利[1] 

机构地区：[1]遵义医学院药学院,贵州遵义563099

出　　处：《遵义医学院学报》2016年第2期122-128,共7页Journal of Zunyi Medical University

基　　金：国家自然科学基金资助项目(NO:81360471);贵州省国际合作项目(NO:[2012]7036);贵州省科技创新人才团队项目(NO:2014GZ 71255);国家大学生创新项目,贵州省大学生创新项目(NO:201510661007);遵义医学院大学生创新项目(NO:[2014]5809)

摘　　要：目的开发具有新生物活性的非铂系前药。方法采用一锅合成法合成3个新的氨基酸席夫碱和1,10-邻菲罗啉(Ⅳ)配合物[VO(o-van-Naph-L-Ana)(Phen)](o-van-Naph-L-Ana为邻香草醛与3-(1-萘基)-L-丙氨酸缩合成的席夫碱,Phen为1,10-邻菲罗啉)(1)、[VO(Hynaph-L-Tyr)(Phen)](Hynaph-L-Tyr为2-羟基-1-萘甲醛与L-色氨酸缩合成的席夫碱,Phen=1,10-邻菲罗啉)(2)和[VO(o-van-L-Trp)(Phen)](o-van-L-Trp为邻香草醛与L-色氨酸缩合成的席夫碱,Phen=1,10-邻菲罗啉)(3),利用高分辨质谱、FT-IR谱及摩尔电导进行了表征研究,并通过X射线单晶衍射测定了其晶体结构。用MTT法测定目标配合物1、2和3对A549(人肺腺癌细胞)和Hep G2(人源肝癌细胞)的体外抗肿瘤活性。结果成功合成了3个新的钒氧氨基酸席夫碱配合物。3个目标配合物的体外抗肿瘤实验结果表明:配合物2和3对两种受试细胞株均表现出一定的细胞毒性,2和3对A549的IC_50分别为58.88和53.08μmol/L,对Hep G2的IC50分别为:83.95和44.74μmol/L。结论探寻了一种具有反应条件温和、后处理简单的一锅合成方法。合成得到的3个目标配合物中,化合物2和3对A549和Hep G2细胞具有中等活性。Objective To discover the novel bioactivities of non- platinum metallic prodrug. Methods Three novel new oxovanadium（ Ⅳ） complex,[VO（ o- van- Naph- L- Ana）（ Phen） ]（ 1）（ o- van- Naph- L-Ana = Schiff base derived from o- vanillin and 3-（ 1- Naphthyl）- L- alanine,phen = 1,10- phenanthroline）,[VO（ Hynaph- L- Tyr）（ Phen） ]（ 2）（ Hynaph- L- Tyr = Schiff base derived from 2- hydroxy- 1-naphthaldehyde and L- tryptophan,phen = 1,10- phenanthroline） and [VO o- van- L- Trp）（ Phen） ]（ 3）（ o- van- L- Trp = Schiff base derived from o- vanillin and L- tryptophan,phen = 1,10- phen- anthroline）,were synthesized by one- pot,and characterized by H RMS,FT- IR spectra,molar conductance and single- crystal XRD. The in vitro anticancer activities of 1,2 and 3 against A- 549 and He Gp2 were tested by MTT assay. Results Three new amino acid Schiff base oxovanadium（ Ⅳ） complexes 1- 3 were synthesized.These results suggested that the complexes 2 and 3 exhibited certain antitumor activities. The IC50 values of the synthetic test complexes 2 and 3 were 58. 88 and 53. 08 μmol / l in A549,83. 95 and 44. 74 μmol / l in Hep G2,respectively. Conclusion An one- pot synthetic protocol with mild reaction conditions and convenient purification was developed. The complexes 2 and 3 have moderate anticancer activities towards A549 cells（ human lung carcinoma cell line） and Hep G2 cells（ human hepatoma cell line）.

关 键 词：氨基酸 席夫碱 氧钒(Ⅳ)配合物 晶体结构 抗肿瘤活性 

分 类 号：R914.5[医药卫生—药物化学]