8-羟基喹啉衍生物镍(Ⅱ)配合物的合成、晶体结构、抗肿瘤活性及其与BSA作用研究  

Synthesis,Crystal Structure,Antitumor Activity and Interaction with BSA of Nickel(Ⅱ)Complex with 8-Hydroxyquinoline Derivative

作　　者：袁涛 覃姣兰 黄如川 姚鹏飞 范歆晨 谢亚茹 YUAN Tao;QIN Jiao-lan;HUANG Ru-chuan;YAO Peng-fei;FAN Xin-chen;XIE Ya-ru(Guangxi Key Laboratory of Urban Water Environment,College of Chemistry and Environmental Engineering,Baise University,Baise 533000,China)

机构地区：[1]百色学院化学与环境工程学院广西城市水环境重点实验室,广西百色533000

出　　处：《化学试剂》2023年第5期51-58,共8页Chemical Reagents

基　　金：广西省部共建药用资源化学与药物分子工程国家重点实验室开放课题项目(CMEMR2019-B11);广西自然科学青年基金项目(2018GXNSFBA281197);广西大学生创新创业训练计划项目(202110609138)。

摘　　要：以8-羟基喹啉-2-甲醛和2-肼基-4,6-二甲基嘧啶缩合得到席夫碱配体L,配体L与NiCl_(2)·6H_(2)O反应得到配合物[Ni(L)Cl 2](简称L-Ni),X-单晶衍射表明配合物L-Ni属于三斜晶系,空间群P-1。MTT实验表明,配合物L-Ni对肿瘤细胞MGC-803、NCI-H460、T-24、Skov-3的生长均有抑制作用,对T-24的抑制作用最强,IC_(50)=(16.65±0.18)μmol/L,细胞毒性大于顺铂。从荧光光谱结果看,配合物L-Ni能使牛血清白蛋白(BSA)的荧光发生静态猝灭,两者间主要作用力为氢键和范德华力。配合物L-Ni与BSA间有一个结合位点,紫外-可见光谱、同步荧光光谱及位点竞争实验表明,配合物L-Ni与BSA亚结构域ⅡA的位点Ⅰ结合,使BSA微环境极性减小,而疏水性增加,推测配合物L-Ni使BSA的二级结构发生了改变。The schiff base ligand L was synthesized by the condensation of 8-hydroxyquinoline-2-formaldehyde and 2-hydrazino-4,6-dimethylpyrimidine,L then reacted with NiCl 2·6H 2O to obtain the complex[Ni(L)Cl_(2)](L-Ni),X-single crystal diffraction showed that L-Ni belongs to the triclinic system,and the spatial group P-1.MTT tests showed that L-Ni could inhibit the growth of tumor cells(MGC-803,NCI-H460,T-24 and Skov-3),and have the strongest inhibition on T-24,IC_(50)=(16.65±0.18)μmol/L.Such cytotoxicity is greater than that of cisplatin.According to the fluorescence spectroscopy results,L-Ni can statically quench the fluorescence of bovine serum albumin(BSA),and the main binding forces between them are hydrogen bonding and Van der Waals force.The UV-Vis spectra,synchronous fluorescence spectra and site tests indicated there is a binding site between L-Ni and BSA,which is L-Ni binding to the site I of BSA subdomainⅡA.This binding force could cause the polarity decrease and thus the hydrophobicity increase of BSA microenvironment,inferring the secondary structure changes of BSA by L-Ni.

关 键 词：镍配合物 抗肿瘤 光谱研究 静态猝灭 相互作用 

分 类 号：O657[理学—分析化学]