¹³¹I-Caerin 1.1 and ¹³¹I-Caerin 1.9 for the treatment of non-small-cell lung cancer

ObjectiveTo investigate the effect of the I-131-labeled high-affinity peptides Caerin 1.1 and Caerin 1.9 for the treatment of A549 human NSCLC cells. Methods 3-[4,5-Dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide (MTT) and plate clone formation assays were performed to confirm the in vitro anti-tumor activity of Caerin 1.1 and Caerin 1.9. Chloramine-T was used to label Caerin 1.1 and Caerin 1.9 with I-131, and the Cell Counting Kit 8 assay was performed to analyze the inhibitory effect of unlabeled Caerin 1.1, unlabeled Caerin 1.9, I-131-labeled Caerin 1.1, and I-131-labeled Caerin 1.9 on the proliferation of NSCLC cells. An A549 NSCLC nude mouse model was established to investigate the in vivo anti-tumor activity of unlabeled Caerin 1.1, unlabeled Caerin 1.9, I-131-labeled Caerin 1.1, and I-131-labeled Caerin 1.9. Results Caerin 1.1 and Caerin 1.9 inhibited the proliferation of NSCLC cells in vitro in a concentration-dependent manner. The half-maximal inhibitory concentration was 16.26 mu g/ml and 17.46 mu g/ml, respectively, with no significant intergroup difference (P>0.05). I-131-labeled Caerin 1.1 and I-131-labeled Caerin 1.9 were equally effective and were superior to their unlabeled versions in their ability to inhibit the proliferation and growth of NSCLC cells (P>0.05). Conclusions(131)I-labeled Caerin 1.1 and I-131-labeled Caerin 1.9 inhibit the proliferation and growth of NSCLC cells and may become potential treatments for NSCLC.