Iodine-125 labeled Australian frog tree host-defense peptides caerin 1.1 and 1.9 better inhibit human breast cancer cells growth than the unlabeled peptides. 125 I-caerin 1.9 may better be used for the treatment of breast cancer.

Objectives: We recently showed that host defense caerin peptides isolated from Australian frog tree were able to inhibit cervical cancer tumour cell growth in vitro. We wished to determine if radioactive isotope iodine-125 (1(25)I) can be labeled to caerin 1.9 peptide and if this peptide is bioactive for breast cancer cells treatment. Materials and Methods: The biological function of caerin (1.1 and 1.9) peptides were investigated by in vitro 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The anti-cancer effect of I-125 labeled caerin 1.9 was compared with unlabeled caerin 1.9 peptide. The tissue distribution of I-125 labeled caerin 1.9 peptide was further studied in mice. Results: In the current paper, we demonstrated that caerin peptides (1.1 and 1.9) were separately able to inhibit the viability of two breast cancer cell lines in vitro and this inhibition was more profound when these peptides were simultaneously applied. Moreover, I-125 can be stably attached to caerin 1.9 peptide with high efficiency. Iodine-125 labeled caerin 1.9 inhibited 125 breast cancer cells line MCF-7 viability more efficiently than free I-125 and also than unlabeled caerin 1.9. Additionally, iodine-125 labeled caerin 1.9 in vivo imaging demonstrated that although slightly, it could be accumulated in tumor tissue. Conclusion: Our results from this totally original study indicated that radioactive isotope I-125 labeled to caerin peptide 1.9 may be used to treat breast cancer while at the same time the response to treatment may be monitored by simultaneous imaging.