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ISSN 1998-9539

Tumor Acidic Microenvironment Targeted Pyropheophorbide a Dimer, an Alternative Strategy for Simultaneous Tumor Fluorescence Imaging and PDT Treatment

Lei Cao,a Shisheng Wang,a Liu Wang,a Xiuhan Guo,a Guangzhe Li,a and Weijie Zhaoa,b@ 

aSchool of Pharmaceutical Science and Technology, Dalian University of Technology, 116024 Dalian, P.R. China

bState Key Laboratory of Fine Chemicals, Dalian University of Technology, 116024 Dalian, P.R. China

@Corresponding author E-mail:;


DOI: 10.6060/mhc190336z

Macroheterocycles 2019 12(2) 187-192


Targeting tumor acidic microenvironment, a cis-aconitate linked pyropheophorbide a dimer 3 was designed and prepared. The observed fluorescence quenching of 3 verified our FRET based molecular design. Acid-dependent cleavage in aqueous solution, singlet oxygen generation, and cytotoxicity against HepG2 cell lines of dimer 3 were investigated. The dimer demonstrated different levels of fluorescence recovery when incubated in acidic aqueous environment as well as effective phototoxicity against HepG2 cells.

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