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Objective <p>To explore and compare the value of <sup>131</sup>I-TFMP-Y4 and <sup>131</sup>I-Caerin 1.1 in internal irradiation therapy for hepatocellular carcinoma.</p> Methods <p>(1) 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) analysis revealed the inhibitory effects of Caerin 1.1 and TFMP-Y4 on Hepg2 and LO2 cell growth. (2) The chloramine-T method was used to prepare <sup>131</sup>I-Caerin 1.1 and <sup>131</sup>I-TFMP-Y4. (3) Uptake and elution assays revealed that Hepg2 cells bound and retained <sup>131</sup>I-Caerin 1.1 and <sup>131</sup>I-TFMP-Y4, and the inhibitory effects on Hepg2 cells were verified with cellular proliferation/toxicity assays. (4) A hormonal nude mouse model was established to study the in vivo therapeutic effects of the peptides alone, <sup>131</sup>I-Caerin 1.1 and <sup>131</sup>I-TFMP-Y4.</p> Results <p>(1) Caerin 1.1 inhibited Hepg2 and LO2 cell proliferation in a concentration-dependent manner, and the half-maximal inhibitory concentrations (IC<sub>50</sub>) were 9.34&#xa0;µg/mL and 22.16&#xa0;µg/mL, respectively. Moreover, TFMP-Y4 did not inhibit these two cell lines. (2) The labeling rates of <sup>131</sup>I-Caerin 1.1 and <sup>131</sup>I-TFMP-Y4 were high and stable. Both could significantly reduce the activity of Hepg2 cells and inhibit tumor growth in vitro and in vivo.</p> Conclusion <p><sup>131</sup>I-Caerin 1.1 and <sup>131</sup>I-TFMP-Y4 significantly inhibited the proliferation of Hepg2 cells in vitro and in vivo. In addition, <sup>131</sup>I-TFMP-Y4 can reduce adverse reactions during treatment.</p>

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Experimental study of iodine-131 labeling of a novel tumor-targeting peptide, TFMP-Y4, in the treatment of hepatocellular carcinoma with internal irradiation

  • 期刊论文

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  • 发表日期：

    2025年2月12日

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  • Juan Du,
  • Weiwei Ren,
  • Wenjie Liu,
  • Yixuan Zhou,
  • Yushan Li,
  • Qingyi Lai,
  • Xiongying Liu,
  • Tongsheng Chen,
  • Wenjuan Liu,
  • Zhuanming Chen,
  • Jinhe Zhang,
  • Peipei Zhang,
  • Jianwei Yuan

摘要

Objective

To explore and compare the value of 131I-TFMP-Y4 and 131I-Caerin 1.1 in internal irradiation therapy for hepatocellular carcinoma.

Methods

(1) 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) analysis revealed the inhibitory effects of Caerin 1.1 and TFMP-Y4 on Hepg2 and LO2 cell growth. (2) The chloramine-T method was used to prepare 131I-Caerin 1.1 and 131I-TFMP-Y4. (3) Uptake and elution assays revealed that Hepg2 cells bound and retained 131I-Caerin 1.1 and 131I-TFMP-Y4, and the inhibitory effects on Hepg2 cells were verified with cellular proliferation/toxicity assays. (4) A hormonal nude mouse model was established to study the in vivo therapeutic effects of the peptides alone, 131I-Caerin 1.1 and 131I-TFMP-Y4.

Results

(1) Caerin 1.1 inhibited Hepg2 and LO2 cell proliferation in a concentration-dependent manner, and the half-maximal inhibitory concentrations (IC50) were 9.34 µg/mL and 22.16 µg/mL, respectively. Moreover, TFMP-Y4 did not inhibit these two cell lines. (2) The labeling rates of 131I-Caerin 1.1 and 131I-TFMP-Y4 were high and stable. Both could significantly reduce the activity of Hepg2 cells and inhibit tumor growth in vitro and in vivo.

Conclusion

131I-Caerin 1.1 and 131I-TFMP-Y4 significantly inhibited the proliferation of Hepg2 cells in vitro and in vivo. In addition, 131I-TFMP-Y4 can reduce adverse reactions during treatment.