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碘 - 125标记的澳大利亚树蛙宿主防御肽caerin 1.1和1.9比未标记的肽更能有效抑制人乳腺癌细胞的生长。碘 - caerin 1.9可能更适合用于治疗乳腺癌。

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. I-caerin 1.9 may better be used for the treatment of breast cancer.

作者信息

Yuan Jianwei, You Xinchao, Ni Guoying, Wang Tianfang, Cavezza Shelley, Pan Xuan, Liu Xiaosong

机构信息

The First Affiliated Hospital/School of Clinical Medicine, Guangdong Pharmaceutical University, Guangzhou, Guangdong 510080, China.

出版信息

Hell J Nucl Med. 2018 May-Aug;21(2):115-120. doi: 10.1967/s002449910803. Epub 2018 Jul 12.

Abstract

OBJECTIVE

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 (I) can be labeled to caerin 1.9 peptide and if this peptide is bioactive for breast cancer cells treatment.

SUBJECTS 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 labeled caerin 1.9 was compared with unlabeled caerin 1.9 peptide. The tissue distribution of I 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 can be stably attached to caerin 1.9 peptide with high efficiency. Iodine-125 labeled caerin 1.9 inhibited breast cancer cells line MCF-7 viability more efficiently than free I 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 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.

摘要

目的

我们最近发现,从澳大利亚树蛙中分离出的宿主防御凯林肽能够在体外抑制宫颈癌细胞的生长。我们希望确定放射性同位素碘 - 125(I)是否可以标记到凯林1.9肽上,以及该肽对乳腺癌细胞治疗是否具有生物活性。

受试者与方法

通过体外3 -(4,5 - 二甲基噻唑 - 2 - 基)- 2,5 - 二苯基四氮唑溴盐(MTT)法研究凯林(1.1和1.9)肽的生物学功能。将碘标记的凯林1.9的抗癌效果与未标记的凯林1.9肽进行比较。进一步在小鼠中研究碘标记的凯林1.9肽的组织分布。

结果

在本论文中,我们证明凯林肽(1.1和1.9)分别能够在体外抑制两种乳腺癌细胞系的活力,并且当同时应用这些肽时,这种抑制作用更显著。此外,碘可以高效稳定地连接到凯林1.9肽上。碘 - 125标记的凯林1.9比游离碘以及未标记的凯林1.9更有效地抑制乳腺癌细胞系MCF - 7的活力。此外,碘 - 125标记的凯林1.9的体内成像表明,虽然含量较少,但它可以在肿瘤组织中积累。

结论

我们这项全新研究的结果表明,放射性同位素碘标记的凯林肽1.9可用于治疗乳腺癌,同时可通过同步成像监测治疗反应。

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