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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Remarkable enhancement in photocytotoxicity and hydrolytic stability of curcumin on binding to an oxovanadium(IV) moiety
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Remarkable enhancement in photocytotoxicity and hydrolytic stability of curcumin on binding to an oxovanadium(IV) moiety

机译：姜黄素结合氧杂钒（IV）部分后，光细胞毒性和水解稳定性显着增强

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摘要

Oxovanadium(IV) complexes of polypyridyl and curcumin-based ligands, viz. [VO(cur)(L)Cl] (1, 2) and [VO(scur)(L)Cl] (3, 4), where L is 1,10-phenanthroline (phen in 1 and 3), dipyrido[3,2-a:2',3'-c]phenazine (dppz in 2 and 4), Hcur is curcumin and Hscur is diglucosylcurcumin, were synthesized and characterized and their cellular uptake, photocytotoxicity, intracellular localization, DNA binding, and DNA photo-cleavage activity studied. Complex [VO(cur)(phen)Cl] (1) has (VN2O3Cl)-N-IV distorted octahedral geometry as evidenced from its crystal structure. The sugar appended complexes show significantly higher uptake into the cancer cells compared to their normal analogues. The complexes are remarkably photocytotoxic in visible light (400-700 nm) giving an IC50 value of <5 mu M in HeLa, HaCaT and MCF-7 cells with no significant dark toxicity. The green emission of the complexes was used for cellular imaging. Predominant cytosolic localization of the complexes 1-4 to a lesser extent into the nucleus was evidenced from confocal imaging. The complexes as strong binders of calf thymus DNA displayed photocleavage of supercoiled pUC19 DNA in red light by generating (OH)-O-center dot radicals as the ROS. The cell death is via an apoptotic pathway involving the ROS. Binding to the VO2+ moiety has resulted in stability against any hydrolytic degradation of curcumin along with an enhancement of its photocytotoxicity.
机译：聚吡啶基和姜黄素基配体的氧钒（IV）配合物，即。 [VO（cur）（L）Cl]（1、2）和[VO（scur）（L）Cl]（3、4），其中L为1,10-菲咯啉（1和3中的phen），双吡啶[ 3,2-a：2'，3'-c]吩嗪（dppz在2和4中），Hcur是姜黄素，Hscur是二葡萄糖基姜黄素，已合成并表征，其细胞摄取，光细胞毒性，细胞内定位，DNA结合和DNA研究了光裂解活性。配合物[VO（cur）（phen）Cl]（1）具有（VN2O3Cl）-N-IV扭曲的八面体几何形状，从其晶体结构证明。与它们的正常类似物相比，添加糖的复合物对癌细胞的摄取明显更高。该复合物在可见光（400-700 nm）下具有明显的光细胞毒性，在HeLa，HaCaT和MCF-7细胞中的IC50值<5μM，无明显的暗毒性。配合物的绿色发射用于细胞成像。共聚焦成像证明复合物1-4在细胞核中的定位较小。作为小牛胸腺DNA的强结合物的复合物通过产生（OH）-O-中心点自由基作为ROS在红光下显示出超螺旋pUC19 DNA的光裂解。细胞死亡是通过涉及ROS的凋亡途径。与VO 2+部分的结合已导致针对姜黄素的任何水解降解的稳定性以及其光细胞毒性的增强。

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