FTS与NIRF共轭化合物用于小鼠肿瘤模型的成像和治疗

发布时间：2018-04-08 14:54

  本文选题：法尼基硫代水杨酸　切入点：近红外荧光　出处：《中国实验动物学报》2017年04期

【摘要】：目的研究法尼基硫代水杨酸(farnesylthiosalicylic Acid,FTS)与七甲川菁(heptamethine carbocyanine)近红外(near infrared,NIR)荧光染料共轭化合物的肿瘤靶向性及其在活体成像中的应用,明确该化合物对肿瘤生长的抑制作用。方法将人乳腺癌细胞MCF-7、胶质瘤细胞U251和前列腺癌细胞PC3培养至对数生长期后,分别加入不同浓度的FTS和FTS-IR783,观察两种化合物对肿瘤细胞的生长抑制作用;培养的三种肿瘤细胞中加入FTS-IR783(20μmol/L),荧光显微镜下观察荧光染料在肿瘤细胞中的聚集;将三种肿瘤细胞(每只1×10~6个)皮下移植裸鼠,两周后荷瘤鼠腹腔注射FTS-IR783(每只10 nmol/L),活体成像分别测定肿瘤部位近红外荧光信号和肿瘤体积的相关性。结果与FTS相比较,FTS-IR783可显著抑制MCF-7、U251和PC3的生长;三种肿瘤细胞可特异性识别FTS-IR783,呈现近红外荧光集聚;皮下荷瘤模型注射FTS-IR783后,活体成像显示肿瘤部位荧光强度与生物发光强度相关性分别达到0.987,0.998和0.971。结论 FTS与近红外荧光染料IR-783共轭结合后可特异性识别肿瘤细胞,用于肿瘤模型的活体成像,同时该化合物具有的肿瘤靶向性可显著抑制肿瘤细胞的生长,有望成为新型的靶向药物。
[Abstract]:Methods Human breast cancer cell line MCF-7, glioma cell line U251 and prostate cancer cell line PC3 were cultured to logarithmic growth stage, and different concentrations of FTS and FTS-IR783 were added to observe the inhibitory effect of the two compounds on the growth of tumor cells.Three kinds of tumor cells were cultured with FTS-IR783(20 渭 mol 路L ~ (-1), fluorescence microscope was used to observe the aggregation of fluorescent dyes in tumor cells, and three kinds of tumor cells (1 脳 10 ~ 6 each) were subcutaneously transplanted into nude mice.Two weeks later, FTS-IR783 (10 nmol / L) was injected intraperitoneally to the tumor-bearing mice, and the correlation between NIR fluorescence signal and tumor volume was measured by in vivo imaging.Results compared with FTS, FTS-IR783 could significantly inhibit the growth of MCF-7U251 and PC3, the three kinds of tumor cells could specifically recognize FTS-IR783and present near infrared fluorescence agglomeration.In vivo imaging showed that the correlation between fluorescence intensity and bioluminescence intensity was 0.9870.998 and 0.971respectively.Conclusion the conjugation of FTS with near infrared fluorescent dye IR-783 can specifically identify tumor cells and be used in the imaging of tumor models in vivo, and the tumor targeting property of the compound can significantly inhibit the growth of tumor cells.It is expected to be a new target drug.
【作者单位】： 第四军医大学实验动物中心;
【基金】：军队实验动物专项(编号:SYDW2016-006号) 国家自然科学基金(批准编号:31501112)
【分类号】：R-332;R73-3
，

本文编号：1722096