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目的利用前期制备的超微超顺磁性氧化铁(USPIO)标记的含有精氨酸-甘氨酸-天冬氨酸(RGD)序列的环肽探针(RGD-USPIO分子探针)进行MR成像,评价壁虎活性单体BH1273209对人肺腺癌SPC细胞的作用效果。方法将SPC细胞接种于6孔板中培养24h,分为实验组和对照组,分别加入1mg/ml的BH1273209和培养液,培养48h后加入含铁浓度25μg/ml的RGD-USPIO培养1h,进行普鲁士蓝染色。将细胞重悬于1%琼脂糖凝胶中,置于Eppendorf管内进行MR扫描。结果随浓度增加,BH1273209对SPC细胞的抑制作用增强,1 mg/ml时抑瘤率最高;铁浓度为25μg/ml时RGD-USPIO探针对SPC细胞活性无明显影响。对照组SPC细胞内可见较多蓝染颗粒,实验组SPC细胞内未见明显的蓝染颗粒。T2WI中,实验组的SNR(132.26±17.24)较对照组(4.89±3.35)明显增高(P<0.01)。结论MR分子成像可简便、准确地评价BH1273209对SPC细胞的作用效果;BH1273209使SPC细胞结合RGD-USPIO明显减少,推测其通过抑制整合素配体-受体结合而发挥抗肿瘤作用。
OBJECTIVE: MR imaging was performed using a cyclic peptide probe (RGD-USPIO molecular probe) containing arginine-glycine-aspartic acid (RGD) sequence labeled with ultrapure superparamagnetic iron oxide (USPIO) Effect of gecko active monomer BH1273209 on human lung adenocarcinoma SPC cells. Methods SPC cells were seeded in 6-well plates and cultured for 24h. The cells were divided into experimental group and control group. BH1273209 (1mg / ml) and culture medium were added respectively. After culturing for 48h, RGCs were cultured in RGD-USPIO containing 25μg / Prussian blue staining. The cells were resuspended in 1% agarose gel and placed in an Eppendorf tube for MR scanning. Results With increasing concentration, the inhibitory effect of BH1273209 on SPC cells was enhanced, and the inhibition rate was highest at 1 mg / ml. No significant effect of RGD-USPIO probe on the activity of SPC was observed when the concentration of iron was 25μg / ml. In the control group, more blue staining particles were observed in the SPC cells and no obvious blue staining particles were observed in the SPC cells in the experimental group. In T2WI, the SNR of the experimental group (132.26 ± 17.24) was significantly higher than that of the control group (4.89 ± 3.35) (P <0.01). Conclusions MR imaging can be used to evaluate the effect of BH1273209 on SPC cells easily and accurately. BH1273209 can significantly reduce the binding of RGC-USPIO to SPC cells, suggesting that it exerts anti-tumor effect by inhibiting integrin ligand-receptor binding.