摘要
为了发现高效的光动力药物。以焦脱镁叶绿酸a衍生物为母体,通过酰胺反应引入氨基苯并吩噁嗪盐酸盐,制得苯并吩噁嗪叶绿素衍生物(PTM);采用^(1)H NMR、MS对其结构进行表征;用紫外-可见光谱、荧光发射光谱对其光学性能进行表征;用DPBF法测定了单线态氧生成速率;用MTT法测定了化合物光动力抗肿瘤活性。该化合物的紫外-可见最长吸收波长位于669 nm、最大荧光发射波长位于673 nm;其单线态氧生成速率为K=0.005 5 s^(-1);MTT法测试表明当浓度为8μg/mL、激光波长669 nm、光照强度为6 J/cm^(2)时,人食管癌细胞存活率仅为26.27%。上述研究表明该化合物光学性质优良、单线态氧生成速率高、对肿瘤细胞有明显的光动力抑制作用,值得进一步研究开发。
To find more effective photodynamic drug. Benzophenoxazine chlorophyll derivative(PTM) was prepared by combination of pyropheophorbide-a with benzophenoxazine through condensation reaction. Its structure was characterized with^(1)HNMR and MS. Its Photophysical properties was characterized by ultraviolet-visible absorption spectrum, fluorescence emission spectrum. The singlet oxygen generation rate was detected with DPBF method, and anti-tumor activity was tested with MTT assay. It has obvious absorption at about 669 nm in the ultraviolet-visible absorption spectrum, has emission at about 673 nm in the fluorescence emission spectrum, and the singlet oxygen generation rate K is 0.005 5 s^(-1). MTT assay showed the survival rate of esophageal cancer cells was only 26.27% after incubation with this compound 8 μg/mL, irradiation with light 6 J/cm^(2)and 690 nm. The excellent photophysical properties, high singlet oxygen generation rate and obvious photodynamic antitumor effect made PTM a promising new photosensitizer for cancer treatment in PDT.
作者
韩广辉
江颖
曹宁
王金海
王来兴
韩一平
ODonal
陈志龙
HAN Guanghui;JIANG Yin;CAO Ning;WANG Jinhai;WANG Laixing;HAN Yiping;ODonal;CHEN Zhilong(Department of Pharmaceutical Science and Technology,College of Chemistry and Biology,Donghua University,Shanghai 201620,China;Shanghai Changhai Hospital,Shanghai 200433,China)
出处
《激光杂志》
CAS
北大核心
2022年第1期197-201,共5页
Laser Journal
基金
国家自然科学基金(No.21977016)
上海市科委基金(No.18411968000,18410721700,19411970600)。
关键词
吩噁嗪
叶绿素衍生物
光敏剂
光动力疗法
肿瘤
phenoxazine
chlorophyll derivative
photosensitizer
photodynamic therapy
tumor
