本文選題：法尼基硫代水楊酸　切入點：近紅外熒光　出處：《中國實驗動物學報》2017年04期

【摘要】：目的研究法尼基硫代水楊酸(farnesylthiosalicylic Acid,FTS)與七甲川菁(heptamethine carbocyanine)近紅外(near infrared,NIR)熒光染料共軛化合物的腫瘤靶向性及其在活體成像中的應(yīng)用,明確該化合物對腫瘤生長的抑制作用。方法將人乳腺癌細胞MCF-7、膠質(zhì)瘤細胞U251和前列腺癌細胞PC3培養(yǎng)至對數(shù)生長期后,分別加入不同濃度的FTS和FTS-IR783,觀察兩種化合物對腫瘤細胞的生長抑制作用;培養(yǎng)的三種腫瘤細胞中加入FTS-IR783(20μmol/L),熒光顯微鏡下觀察熒光染料在腫瘤細胞中的聚集;將三種腫瘤細胞(每只1×10~6個)皮下移植裸鼠,兩周后荷瘤鼠腹腔注射FTS-IR783(每只10 nmol/L),活體成像分別測定腫瘤部位近紅外熒光信號和腫瘤體積的相關(guān)性。結(jié)果與FTS相比較,FTS-IR783可顯著抑制MCF-7、U251和PC3的生長;三種腫瘤細胞可特異性識別FTS-IR783,呈現(xiàn)近紅外熒光集聚;皮下荷瘤模型注射FTS-IR783后,活體成像顯示腫瘤部位熒光強度與生物發(fā)光強度相關(guān)性分別達到0.987,0.998和0.971。結(jié)論 FTS與近紅外熒光染料IR-783共軛結(jié)合后可特異性識別腫瘤細胞,用于腫瘤模型的活體成像,同時該化合物具有的腫瘤靶向性可顯著抑制腫瘤細胞的生長,有望成為新型的靶向藥物。
[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.
【作者單位】： 第四軍醫(yī)大學實驗動物中心;
【基金】：軍隊實驗動物專項(編號:SYDW2016-006號) 國家自然科學基金(批準編號:31501112)
【分類號】：R-332;R73-3
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本文編號：1722096