Synthesis and in vitro antitumor activity of photodynamic therapy reagent based on tetraphene skeleton

doi:10.3969/j.issn.1000-1565.2025.02.008

Journal of Hebei University(Natural Science Edition) ›› 2025, Vol. 45 ›› Issue (2): 176-184.DOI: 10.3969/j.issn.1000-1565.2025.02.008

Synthesis and in vitro antitumor activity of photodynamic therapy reagent based on tetraphene skeleton

FANG Kexin, LIU Haitong, WANG Shuxiang

Key Laboratory of Medicinal Chemistry and Molecular Diagnosis Ministry of Education, College of Chemistry and Materials Science, Hebei University, Baoding 071000, China

Received:2024-11-01 Published:2025-03-26

Abstract

Abstract: A photodynamic therapy(PDT)reagent, LT-TPE-DB-BNO₂ for reactive oxygen species(ROS)generation based on tetraphene(TPE), was synthesized from 4-bromobenzoylbenzene, 4,4’-dimethoxybenzophenone, p-nitrobenzyl bromide(Br-BNO₂)and azide lactose(LT)by nucleophilic substitution, suzuki coupling and click reaction. The stability of LT-TPE-DB-BNO₂ in serum and at different pH value, and the ability of ROS generation were investigated by spectrophotometry and confocal fluorescence microscopy. The effects of LT-TPE-DB-BNO₂ on the viability of HeLa and BRL-3A cells were investigated by MTT method and live and dead cell double staining method. The results showed that LT-TPE-DB-BNO₂ was stable in serum and at different pH value. In the dark condition,it had a little effect on the activity of HeLa and BRL-3A cells. Under irradiation by xenon lamp, ROS was produced by LT-TPE-DB-BNO₂, and the activity of HeLa cells was reduced by 88.3%, indicating that LT-TPE-DB-BNO₂ is a highly efficient PDT reagent.

Key words: tetraphene skeleton, photodynamic therapy(PDT)reagent, antitumor activity

CLC Number:

O632.6

FANG Kexin, LIU Haitong, WANG Shuxiang. Synthesis and in vitro antitumor activity of photodynamic therapy reagent based on tetraphene skeleton[J]. Journal of Hebei University(Natural Science Edition), 2025, 45(2): 176-184.

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Synthesis and in vitro antitumor activity of photodynamic therapy reagent based on tetraphene skeleton

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