[1]张金平,段降龙,杨欣悦,等.胃癌荷瘤小鼠应用四苯乙烯金属双环化合物靶向光敏剂进行光动力治疗的实验研究[J].现代检验医学杂志,2026,41(05):26-30.[doi:10.3969/j.issn.1671-7414.2026.05.005]
　ZHANG Jinping,DUAN Xianglong,YANG Xinyue,et al.Experimental Study on Photodynamic Therapy of Gastric Tumor-Bearing Mice Using Tetraphenylethylene-Based Metallabicyclic Compounds as Targeted Photosensitizers[J].Journal of Modern Laboratory Medicine,2026,41(05):26-30.[doi:10.3969/j.issn.1671-7414.2026.05.005]
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胃癌荷瘤小鼠应用四苯乙烯金属双环化合物靶向光敏剂进行光动力治疗的实验研究()

《现代检验医学杂志》[ISSN:/CN:]

卷:
第41卷
期数:
2026年05期
页码:
26-30
栏目:
论著
出版日期:
2026-09-15

文章信息/Info

Title:
Experimental Study on Photodynamic Therapy of Gastric Tumor-Bearing Mice Using Tetraphenylethylene-Based Metallabicyclic Compounds as Targeted Photosensitizers
文章编号:
1671-7414 （2026） 05-026-05
作者:
张金平1，段降龙2，杨欣悦3，王佳宁4，吴玉玲1
（1.西安交通大学，西安710049；2.陕西省人民医院，西安710068；3.西北工业大学，西安710072；4.西藏民族大学，陕西咸阳712082）
Author(s):
ZHANG Jinping1, DUAN Xianglong2, YANG Xinyue3, WANG Jianing4, WU Yuling1
(1. Xi’an Jiaotong University, Xi’an 710049, China; 2.Shaanxi Provincial People’s Hospital, Xi’an 710068, China; 3. Northwestern Polytechnical University, Xi’an 710072, China; 4. Xizang Minzu University, Shannxi Xianyang 712082, China)
关键词:
胃癌;  荷瘤小鼠;  四苯乙烯金属双环化合物;  靶向光敏剂;  光动力治疗
分类号:
R-332； R735.2； R730.5
DOI:
10.3969/j.issn.1671-7414.2026.05.005
文献标志码:
A
摘要:
目的 验证四苯乙烯金属双环化合物靶向光敏剂的低暗毒性、 高活性氧 （ROS） 产率等特性， 为胃癌光动力治疗 （PDT） 提供高效低毒的新型候选靶向光敏剂。 方法 采用多组分配位驱动自组装策略构建四苯乙烯金属双环化合物靶向光 敏剂； 以人胃癌 AGS、 HGC-27 细胞为体外研究对象， 设光照组 （50mW/cm2 ， 10min） 和避光组， 通过CCK-8法检测细胞毒性， 活/死细胞染色观察细胞杀伤性能， 荧光显微镜检测细胞内ROS生成水平； 建立裸鼠胃癌荷瘤模型， 评估该靶向光敏剂的 体内抑瘤效果及生物安全性。 结果 成功构建四苯乙烯金属双环化合物靶向光敏剂， 合成产率达94%。 与避光组相比， 光照 组细胞IC50 降低[AGS细胞 (7.58±0.40 μmol/L vs 37.05±3.67 μmol/L)、 HGC-27细胞 (5.70±0.34 μmol/L vs 35.16±4.05 μmol/L)]， 差异具有统计学意义 （t=13.85、 12.55， 均P＜ 0.05） ， 确定6.5μmol/L为后续试验适宜浓度。 活/死细胞染色结果 显示， 光照组细胞死亡率显著高于避光组[AGS细胞(45.00%±0.40% vs 6.86%±0.84%)、 HGC-27细胞 （85.98%±0.51% vs 8.63%±0.31%） ]， 差异具有统计学意义 （t=67.74、 218.70， 均P<0.05） 。 与避光组相比， 光照组细胞内ROS平均荧光强度更高 [AGS细胞 （123.63±3.65 a.u. vs 48.89±3.22 a.u.） 、 HGC-27细胞(154.54±12.31 a.u. vs 50.88±5.22 a.u.)]， 差异具有统计学意 义 （t=26.33、 13.29， 均P＜0.05） 。 体内实验中， 与对照组相比， 单纯光敏剂组小鼠肿瘤体积差异无显著统计学意义 （t=0.56， P>0.05） ， 光敏剂+光照组肿瘤体积显著降低 （t=3.04， P<0.05） ； 各实验组小鼠治疗期间体重无明显变化 （F=0.02， P>0.05） 。 结 论 四苯乙烯金属双环化合物靶向光敏剂具有高合成产率、 低暗毒性、 高ROS产率的特性， 可在胃癌细胞中实现高效光动 力杀伤， 且在动物体内具备显著抑瘤效果与良好生物安全性， 有望成为胃癌PDT的新型候选靶向光敏剂。
Abstract:
Objective To verify the characteristics of tetraphenylethylene-based metallabicyclic compounds as targeted photosen- sitizers, including low dark toxicity and high reactive oxygen species (ROS) yield, and to provide a novel high-e?cacy, low-tox- icity candidate targeted photosensitizer for photodynamic therapy (PDT) of gastric cancer. Methods A tetraphenylethylene-based metallabicyclic compound targeted photosensitizer was constructed using a multi-component coordination-driven self-assembly strategy. Human gastric cancer AGS and HGC-27 cells were used for in vitro experiments and divided into a light irradiation group (50 mW/cm2 , 10 min) and a dark group. The cytotoxicity was detected by CCK-8 assay, the cell killing performance was observed by live/dead cell staining, and intracellular ROS production was detected using ?uorescence microscopy. A nude mouse model bearing gastric cancer xenografts was established to evaluate the in vivo antitumor e?cacy and biosafety of the targeted photosensitizer. Results The tetraphenylethylene-based metallabicyclic compound targeted photosensitizer was success- fully constructed with a synthetic yield of 94%. Compared with the dark group, the light group exhibited signi?cantly reduced IC50 values in AGS cells (7.58±0.40 μmol/L vs 37.05±3.67 μmol/L) and HGC-27 cells (5.70±0.34 μmol/L vs 35.16±4.05 μmol/L), with statistically significant differences (t=13.85, 12.55, both P< 0.05). A concentration of 6.5 μmol/L was selected for subsequent experiments. Live/dead cell staining revealed that cell death rates in the light group were signi?cantly higher than those in the dark group, with values of 45.00%±0.40% vs 6.86%±0.84% in AGS cells and 85.98%±0.51% vs 8.63%±0.31% in HGC-27 cells (t=67.74, 218.70, both P<0.05). Intracellular ROS mean ?uorescence intensity was signi?cantly higher in the light group than in the dark group, with values of 123.63±3.65 a.u. vs 48.89±3.22 a.u. in AGS cells and 154.54 ± 12.31 a.u. vs 50.88 ± 5.22 a.u. in HGC-27 cells (t=26.33, 13.29, both P< 0.05). In vivo, no signi?cant difference in tumor volume was ob- served between the photosensitizer-alone group and the control group (t= 0.56, P> 0.05), while the tumor volume in the photo- sensitizer + light group was signi?cantly reduced compared with that in the control group (t=3.04, P<0.05). There were no signif- icant changes in body weight of mice across all experimental groups during treatment (F=0.02, P>0.05). Conclusions The tetraphenylethylene-based metallabicyclic compound targeted photosensitizer has the characteristics of high synthetic yield, low dark toxicity, and high ROS production e?ciency. It can achieve effective photodynamic killing in gastric cancer cells and has signi?cant tumor inhibitory effect and favorable biosafety in vivo, making it a promising candidate targeted photosensitizer for PDT of gastric cancer.

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备注/Memo

备注/Memo:
基金项目：陕西省博士后科研资助项目（2025BSHSDZZ387）。
作者简介：张金平（1991-），男，博士研究生，主治医师，研究方向：消化道肿瘤，E-mail：zjp6007@163.com。
通讯作者：吴玉玲（1993-），女，博士研究生，主治医师，研究方向：血液病，E-mail：wuyl5280@163.com。
更新日期/Last Update: 2026-09-15