Research articles
ScienceAsia 52 (2026): 1-12 |doi:
10.2306/scienceasia1513-1874.2026.036
Zinc porphyrin photosensitizers incorporated with
heavy-atom halogens for in vitro photodynamic therapy
Gui-chen Lia,*, Yan-yan Lib,c,*, Wen-le Zhangd, Neng-zhi Jine, Xiao-xia Fengb, Jia-cheng Liub,*
ABSTRACT: In this study, three halogenated porphyrins were synthesized through the incorporation of heavy atoms
(F, Cl, and Br). Subsequently, to enhance their solubility and bioavailability, zinc atoms were introduced via N-pyridyl
substituted alkylation. This approach culminated in the development of three water-soluble, zinc-containing porphyrins
(ZnP1?ZnP3), which were employed as photosensitizers (PSs) for photodynamic therapy (PDT). Our findings indicate
that ZnP1?ZnP3 can consistently generate singlet oxygen (1O2
) at concentrations significantly higher than that of
the reference compound, tetraphenylporphyrin (TPP), under light irradiation at wavelengths of 600?610 nm. This
result is in concordance with the outcomes of the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT)
assay, and the cytotoxicity profile reveals that the inhibition rate of human umbilical vein endothelial cells (HUVECs)
is virtually negligible. Furthermore, cell staining or cycle analysis, and Reactive Oxygen Species (ROS) detection
experiments collectively demonstrate that light-activated PSs can induce apoptosis in cancer cells and produce ROS,
which are instrumental in the eradication of these cells. Under dark conditions, these complexes exhibit negligible
cytotoxicity. In contrast, they reliably produce 1O2
under light irradiation. Furthermore, due to the heavy atom effect,
bromine-containing ZnP3 achieves the highest in vitro photocytotoxic efficacy among the three photosensitizers.
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| a |
State Key Laboratory of Aridland Crop Science, Gansu Agricultural University, Lanzhou 730070 China |
| b |
Key Laboratory of Eco-Environment-Related Polymer Materials of Ministry of Education, Key Laboratory of Polymer
Materials of Gansu Province, College of Chemistry and Chemical Engineering, Northwest Normal University,
Lanzhou 730070 China |
| c |
Tianzhu No.1 Middle School, Wuwei 733299 China |
| d |
China National Petroleum Corporation Tarim Oilfield Branch, Korla 841000 China |
| e |
Key Laboratory of Advanced Computing, Gansu Computing Center, Lanzhou 730099 China |
* Corresponding author, E-mail: lguchen@163.com, jcliu8@nwnu.edu.cn
Received 8 Dec 2025, Accepted 9 Apr 2026
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