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Design, Synthesis, and Biological Activity of Releasable m-THPC-PEGfolate Conjugate Using a Disulfide-containing Linker

[ Vol. 16 , Issue. 3 ]

Author(s):

Li Peng Xi*, Li Dong Hong, Wan Chuan and Chen Ben Shou   Pages 165 - 169 ( 5 )

Abstract:


The present study reported the preparation of a novel mutual prodrug containing meso-tetra (m-hydroxy phenyl) chlorin (m-THPC), PEG and folate. The folate receptor (FR) targeting compound is a water-soluble chemical incorporating a hydrophilic PEG spacer unit and a reducible selfimmolative disulfide-based linker system between the FR-targeting ligand and the chlorin. The m- THPC-s-s-PEG-Folate was proved to release the parent drug and exhibited significant targeting effects on HeLa cells. In addition, the redox-responsive folate targeting photosensitizer m-THPC-s-s-PEG-Folate showed slightly higher phototoxicity than m-THPC-PEG-Folate for HeLa cells.

Keywords:

m-THPC, folate, disulfide, tumor, PEG, releasable.

Affiliation:

Chongqing Chemical Industry Vocational College, Chongqing 400020, State Key Laboratory of Trauma, Burn and Combined Injury, The 2nd Department of Research Institute of Surgery, Third Military Medical University, Chongqing 400042, Chongqing Chemical Industry Vocational College, Chongqing 400020, Chongqing Chemical Industry Vocational College, Chongqing 400020

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