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Evaluation for in vitro Photodynamic Activity of Chlorin e6-Artesunate Conjugates by Irradiation with Different Wavelengths of Light Source

Xiuhan Guo,a,b Yueqing Li,a Shisheng Wang,a,b@ Liu Wang,a Rui Cai,c Guangzhe Li,a and Weijie Zhaoa,b
aSchool of Pharmaceutical Science and Technology, Dalian University of Technology, 116023 Dalian, P. R. China
bState Key Laboratory of Fine Chemicals, Dalian University of Technology, 116023 Dalian, P. R. China
cSchool of Chemical Engineering, Dalian University of Technology, 116023 Dalian, P. R. China
@Corresponding author E-mail: wangss@dlut.edu.cn
 
DOI: 10.6060/mhc181115w
Macroheterocycles 2018 11(4) 378-382
 
In the development of new photosensitizers for cancer therapy, increasing the capacity of intracellular reactive oxygen species (ROS) production is an important strategy. In this paper, artesunate as a ROS generation group was regioselectively introduced to the chlorin e6 scaffold to obtain four conjugates of chlorin e6 and artesunate. By irradiation with 440 nm, 630 nm and 660 nm of light source the four conjugates exhibited significantly improved phototoxicity against HepG2 cells compared with chlorin e6 and artesunate. Irradiation with 440 nm or 660 nm light source gave higher phototoxicity as well as intracellular ROS level.

 

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