中介二芳基卟吩衍生物的合成及光动力抗肿瘤作用研究  

Synthesis of meso-diarylporphyrin derivatives and evaluation oftheir antitumor effects in photodynamic therapy

作　　者：丁雅馨 刘银 糜乐 邱彦 G.Lavanya 金辉[2] 陈志龙[1] DING Ya-Xin;LIU Yin;MI Le;QIU YAN;GLavanya;JIN Hui;CHEN Zhi-long(Department of Pharmaceutical Science and Technology,College of Chemistry and Biology,Donghua University,Shanghai 201620,China;Pudong New Area People’s Hospital,Shanghai 201200,China)

机构地区：[1]东华大学化学化工与生物学院生物医药研究中心,上海201620 [2]上海市浦东新区人民医院,上海201200

出　　处：《应用化工》2022年第S02期1-6,共6页Applied Chemical Industry

基　　金：国家自然科学基金(21977016);上海市科委基金(18430731600,19411970600,19410711000,20430730900,20490740400,21430730100);浦东新区科委基金(PKJ2019-Y31,PKJ2020-Y42);中国博士后基金资助(2020M681126)。

摘　　要：以二芳基卟吩环结构为基础,设计并制备了4个二芳基卟吩衍生物(P1、P2、P3和P4)。采用^(1)H NMR、^(13)C NMR和HR-MS对其结构进行了表征。通过紫外-可见吸收光谱确定其最长吸收波长位于630 nm左右;荧光发射光谱表明其最大发射波长位于630 nm左右;化合物P4的单线态氧生成速率最高(K=0.0314 min^(-1));MTT法检测对人食管癌细胞(ECA-109)的体外细胞抗增殖能力,结果显示4个化合物对ECA-109均具有光动力抑制作用。化合物P4在635 nm光照条件下,对ECA-109细胞抑制率高达70%,光毒性效果明显,值得进一步开发。Here a series of 5,15-diarylporphyrin derivatives(P1-4)were designed and synthesized.Their structures were characterized by ^(1)H NMR,^(13)C NMR and HR-MS.The UV-Vis spectra of P1-4 showed that the maximum absorption were around 630 nm.The maximum emission wavelength was located at 630 nm in fluorescence emission spectrum.The in vitro anti-proliferation ability of these four compounds against human esophageal carcinoma cell line(ECA-109)was evaluated by MTT assay and flow cytometry.The test results showed that all these compounds had photodynamic inhibitory effects on ECA-109.Upon light-irradiation at 635 nm,compound P4 exhibited the most obvious photodynamic anti-tumor effect,with an inhibition rate of 70%,and compound P4 was deserved further exploration in drug discovery.

关 键 词：光敏剂 光动力疗法 二芳基卟吩 抗肿瘤活性 

分 类 号：R914.4[医药卫生—药物化学]