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Inhibition of MDA-MB-231 cell proliferation by pHLIP(Var7)-P1AP and SPECT imaging of MDA-MB-231 breast cancer-bearing
Yue Hua Chen1, Ming Ming Yu2, Zhen Guang Wang2
1Intensive Care Unit, The Affiliated Hospital of Qingdao University, Qingdao, China.
Aim:
To observe the effect of pHLIP(Var7)-P1AP on the proliferation of MDA-MB-231 triple-negative breast cancer cells and the small-animal single-photon-emission computed tomography (SPECT) imaging of breast cancer-bearing mice carrying MDA-MB-231 cells.
Methods:
Peptide pHLIP(Var7)-P1AP was synthesized by solid-phase peptide synthesis. The binding of fluorescently labeled pHLIP(Var7)-P1AP to MDA-MB-231 cells under various pH conditions and its effect on MDA-MB-231 cell proliferation were analyzed. pHLIP(Var7)-P1AP was labeled with 125I, and the biological distribution of 125I-pHLIP(Var7)-P1AP in the breast cancer mouse model carrying MDA-MB-231 cells as well as the outcome of small-animal SPECT imaging were evaluated.
Results:
pHLIP(Var7)-P1AP was successfully synthesized. Under pH 6.0, fluorescently labeled pHLIP(Var7)-P1AP had a higher binding ability to MDA-MB-231 cells and significantly inhibited the proliferation of MDA-MB-231 cells. The labeling efficiency of pHLIP(Var7)-P1AP with 125I was 33.1 ± 2.7 %, and the radiochemical purity was 98.5 ± 1.8 %. 125I-pHLIP(Var7)-P1AP showed a high concentration in tumors. Small-animal SPECT imaging showed clearly visible tumors at 4 h after injection.
Conclusions:
In the acidic environment, pHLIP(Var7)-P1AP can efficiently target MDA-MB-231 cells and inhibit their growth. Small-animal SPECT of 125I-pHLIP(Var7)-P1AP can clearly image tumors.
Insights
The peptide pHLIP(Var7)-P1AP effectively targets and inhibits triple-negative breast cancer cells in acidic environments. Small-animal SPECT imaging with 125I-pHLIP(Var7)-P1AP clearly visualizes tumors, aiding in breast cancer diagnosis.
Area of Science:
- Biomedical Imaging
- Cancer Biology
- Peptide Therapeutics
Background:
- Triple-negative breast cancer (TNBC) presents a significant therapeutic challenge due to its aggressive nature and lack of targeted treatments.
- The tumor microenvironment is often acidic, a characteristic that can be exploited for targeted drug delivery.
Purpose of the Study:
- To evaluate the efficacy of pHLIP(Var7)-P1AP in inhibiting MDA-MB-231 triple-negative breast cancer cell proliferation.
- To assess the utility of radiolabeled pHLIP(Var7)-P1AP for small-animal single-photon-emission computed tomography (SPECT) imaging of breast cancer.
Main Methods:
- Peptide synthesis of pHLIP(Var7)-P1AP via solid-phase peptide synthesis.
- Analysis of fluorescently labeled pHLIP(Var7)-P1AP binding to MDA-MB-231 cells at varying pH and its antiproliferative effects.
- Radiolabeling of pHLIP(Var7)-P1AP with Iodine-125 (125I) and evaluation of its biodistribution and SPECT imaging performance in a mouse model.
Main Results:
- Successful synthesis of pHLIP(Var7)-P1AP.
- Enhanced binding and significant inhibition of MDA-MB-231 cell proliferation observed at pH 6.0.
- 125I-pHLIP(Var7)-P1AP demonstrated high tumor uptake and enabled clear visualization of tumors via small-animal SPECT imaging within 4 hours post-injection.
Conclusions:
- pHLIP(Var7)-P1AP exhibits efficient targeting of MDA-MB-231 cells in acidic conditions, leading to growth inhibition.
- 125I-pHLIP(Var7)-P1AP is a promising radiotracer for effective small-animal SPECT imaging of breast tumors.
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