Nuclear Techniques ›› 2017, Vol. 40 ›› Issue (12): 120301-120301.doi: 10.11889/j.0253-3219.2017.hjs.40.120301

• NUCLEAR CHEMISTRY, RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE • Previous Articles     Next Articles

The killing effect of 131I-labeled B2-S22-AFA on breast cancer cells with high HER-2 expression

LI Yamei, GUAN Yanxing, CHEN Xuezhong, ZHANG Qing, ZHANG Qing, ZHANG Mengzhi   

  1. Department of Nuclear Medicine, the First Affiliated Hospital of Nanchang University, Nanchang 330006, China
  • Received:2017-03-21 Revised:2017-10-19 Online:2017-12-10 Published:2017-12-08
  • Supported by:
    Supported by Ganpo Excellence 555 Project and Natural Science Fund Project of Jiangxi Province (No.2007GZY1419)

Abstract: Background: B2-S22-AFA is a kind of small molecule mimetic polypeptide that can conjugate to epidermal growth factor receptor 2 (HER-2) specifically and has obvious depressant effect on breast cancer cells with overexpressing HER-2. Purpose: This study aims to investigate the specific killing effect of 131I-labeled B2-S22-AFA on breast cancer cell with overexpressing HER-2. Methods: 131I-B2-S22-AFA was prepared by using N-bromosuccinimide method to measure the labeling efficiency, radiochemical purity, stability, and immunocompetence. The expression levels of HER-2 in SKBR3 and MDA-MB-231 cells were detected by Immunohistochemistry and Western Blot. The inhibitory rate of B2-S22-AFA on cell growth was observed with epidermal growth factors (EGF) at different concentrations. Five groups i.e, B2-S22-AFA group (B2-S22-AFA final concentration:1 μg·mL-1), 131I-B2-S22-AFA group (131I-B2-S22-AFA final concentration:144 kBq/1 μg·mL-1), 131I group (131I final concentration:144 kBq·mL-1), negative control group and reagent blank group, were selected for contrast tests with the final concentration of EGF in each group at 5.0 pg·mL-1. The proliferation and activity of cells were measured by Methyl thiazolyl tetrazolium assay. The inhibitory rates were compared among 131I-B2-S22-AFA group, B2-S22-AFA group and 131I group in the growth of the two kinds of cells at different time. Results: 1) HER-2 receptors were strongly expressed in SKBR3 cells while weakly (low) or no expressed in MDA-MB-231 cells. The radiochemical purity, labeling rate and specific activity of 131I-B2-S22-AFA were 95.0%-97.6%, 64.8%-79.6% and 151.7 MBq·mg-1, respectively. Radiochemical purity of 131I-B2-S22-AFA was 95.4%, 93.5%, 91.4%, 88.2% and 77.4% when it was placed at 37℃ in serum for 4 h, 12 h, 24 h, 48 h and 72 h, respectively. The maximum binding rates of SKBR3 and MDA-MB-231 cells were (66.47±3.24)% and (3.89±0.81)% (tested for 3 times) respectively. 2) The inhibitory effect of B2-S22-AFA on the growth of SKBR3 cells only in the presence of EGF. 3) The killing effect of 131I-B2-S22-AFA on SKBR3 cells was significantly stronger than that of B2-S22-AFA and 131I (p<0.05), and the inhibitory effect of B2-S22-AFA on the growth of SKBR3 cells was significantly higher than that of 131I (p<0.05). 131I-B2-S22-AFA and B2-S22-AFA had no obvious killing effect on MDA-MB-231 cells. Conclusion: 131I-B2-S22-AFA can significantly enhance and accelerate the specific killing effect of B2-S22-AFA on breast cancer cells with high HER-2 expression.

Key words: Breast cancer, Isotope labeling, 131I-B2-S22-AFA, Epidermal growth factor receptor 2

CLC Number: 

  • R817.8