酞菁光敏剂与聚酰胺-胺树枝状大分子的缀合：提高了对 HepG2 细胞的溶解性、分散性和光活性。
Conjugation of Phthalocyanine Photosensitizer with Poly(amidoamine) Dendrimer: Improved Solubility, Disaggregation and Photoactivity Against HepG2 Cells.
机构信息
Biopharmaceutical Photocatalysis, State Key Laboratory of Photocatalysis on Energy and Environment, Cancer Metastasis Alert and Prevention Center, Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, College of Chemistry, Fuzhou University, Fuzhou, China.
Ministry of Education Key Laboratory of Analysis and Detection for Food Safety, Fujian Provincial Key Laboratory of Analysis and Detection for Food Safety, Fuzhou University, Fuzhou, China.
出版信息
Curr Cancer Drug Targets. 2019;19(4):312-320. doi: 10.2174/1568009618666180706164046.
OBJECTIVE
To improve solubility and to reduce aggregation, ZnPcC4 was conjugated to a third-generation poly-amidoamine dendrimer with amino end group (G3-PAMAM-NH2), which acts as a novel photodynamic therapy (PDT) drug carrier system.
METHODS
The phthalocyanines were synthesized by construction reaction. The nano drug was obtained from the conjugation of ZnPcC4 to G3-PAMAM-NH2, using EDC and NHS as coupling agents. The ZnPcC4@G3-PAMAM-NH2 conjugation was characterized by UV-Vis and MS. The 1O2 quantum yield of ZnPcC4@G3-PAMAM-NH2 in water was measured by the chemiluminescence method. The in vitro PDT responses of the studied photosensitizers were studied in hepatocellular carcinoma cell line HepG2 by MTT assay.
RESULTS
At ZnPcC4/G3-PAMAM-NH2 raw ratio of 100/1, the ZnPcC4 conjugate had improved solubility and reduced aggregation tendency in aqueous solution. At this optimum molar ratio, ZnPcC4- G3-PAMAM-NH2 inhibited HepG2 cells, with a half-maximal inhibitory concentration of 1.67 µg/mL upon infrared light exposure. The controls, including dark conditions, or media as well as G3-PAMAM-NH2 exposure, exhibited no inhibitory response.
CONCLUSION
The conjugation of phthalocyanine photosensitizer ZnPcC4 to poly-amidoamine dendrimer G3-PAMAM-NH2 improved the PDT outcomes, in which the optimized binding ratio of ZnPcC4 to G3-PAMAM-NH2 was 6:1.
目的
提高溶解性并减少聚集，将锌酞菁 C4 与具有氨基末端基团的第三代聚酰胺胺树状大分子（G3-PAMAM-NH2）偶联，用作新型光动力疗法（PDT）药物载体系统。
方法
通过构建反应合成酞菁。通过 EDC 和 NHS 作为偶联剂，将 ZnPcC4 偶联到 G3-PAMAM-NH2 上，得到纳米药物。通过紫外可见光谱和质谱对 ZnPcC4@G3-PAMAM-NH2 进行了表征。通过化学发光法测量了 ZnPcC4@G3-PAMAM-NH2 在水中的 1O2 量子产率。通过 MTT 测定法研究了研究的光敏剂在肝癌细胞系 HepG2 中的体外 PDT 反应。
结果
在 ZnPcC4/G3-PAMAM-NH2 原始比例为 100/1 的情况下，ZnPcC4 缀合物在水溶液中具有改善的溶解性和降低的聚集倾向。在这个最佳摩尔比下，ZnPcC4-G3-PAMAM-NH2 抑制 HepG2 细胞，在红外光照射下的半最大抑制浓度为 1.67 µg/mL。对照物，包括黑暗条件或培养基以及 G3-PAMAM-NH2 暴露，均未显示出抑制反应。
结论
将光敏剂锌酞菁 C4 与聚酰胺胺树状大分子 G3-PAMAM-NH2 偶联可改善 PDT 效果，其中 ZnPcC4 与 G3-PAMAM-NH2 的最佳结合比为 6:1。
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