EC-17(disodiumsalt)是一种叶酸受体α(FRα)的靶向造影剂，在可见光谱中具有荧光特性。EC-17的激发和发射波长为470/520nm。
EC-17 (disodium salt) is a folate receptor alpha (FRα) targeting contrast agent with fluorescent properties in the visible light spectrum. The peak excitation and emission wavelengths of EC-17 are 470/520 nm.
EC-17 contains the fluorescein fluorochrome and has a spectral wavelength of 490-530 nm. EC-17 is synthesized by a folate (vitamin B9) and fluorescein isothiocyanate (FITC) conjugated through an ethylenediamine spacer to produce folate-FITC, with a molecular weight of 917 kDa. FITC is a derivative of fluorescein functionalized with an isothiocyanate reactive group. The folate-FITC conjugate forms a negatively charged fluorescent molecule that specifically targets cell-surface FRα and is subsequently internalized into the cytoplasm. The signal-to-background ratio (SBR) of EC-17 for HeLa cells range from 0.97 to 7.32 depending on the molarity and concentration of cancer cells[1].
The mean fluorescence signal from the animals injected with EC-17 to be 42,234 ± 12,234 au[1]. Fluorescence microscopy for folate-FITC shows a strong signal in all malignant tumors with FR-α expression and no signal in FR-α-negative malignant or benign lesions[2].
[1]. Tummers QR, et al. Intraoperative imaging of folate receptor alpha positive ovarian and breast cancer using the tumor specific agent EC17. Oncotarget. 2016 May 31;7(22):32144-55.
Cell experiment: | KB, HeLa, and TC1 cells are plated on a cell culture treated 6-well plate and incubated for 16 hours. Once confluent, EC-17 is added cells. The cells are incubated and sealed in a light-protected environment for 45 minutes. Cells are then washed 3 times with PBS and plated and underwent fluorescence microscopy[1]. |
Animal experiment: | Mice[1]Mice are injected subcutaneously in the flank with 1.2×106 TC1 cells (C57BL/6 mice), 1.0×106 HeLa cells (NOD.Cg-Prkdcscid??Il2rgtm1Wjl/SzJ mice), or 1.0×106 KB cells (NOD.Cg-Prkdcscid, Il2rgtm1Wjl/SzJ mice). Once tumor volume reached approximately 300?mm3 half of the mice are injected with 0.1?mg/kg of EC-17 and the other half with 0.1?mg/kg of OTL38 via tail vein. Three hours later, the fluorescence of tumors is measured using Flocam[1]. |
参考文献: [1]. Tummers QR, et al. Intraoperative imaging of folate receptor alpha positive ovarian and breast cancer using the tumor specific agent EC17. Oncotarget. 2016 May 31;7(22):32144-55. | |
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