研究目的
To evaluate the potential of a novel 68Ga labeled PSMA probe 68Ga-PSMA-BCH for PSMA over-expression tumor imaging.
研究成果
68Ga-PSMA-BCH was successfully synthesized with high purity and specific activity, demonstrating high stability, specific uptake in PSMA-expressing tumors, and comparable performance to 68Ga-PSMA-617 in imaging properties. It is a promising candidate for prostate cancer diagnosis and guiding peptide radioligand therapy, warranting further clinical investigations.
研究不足
The study is preclinical, conducted in animal models and cell lines, which may not fully translate to human applications. The specific activity calculation is crude, and the comparison with 68Ga-PSMA-617 is based on limited data points. Potential optimizations include further clinical trials and refinement of synthesis methods.
1：Experimental Design and Method Selection:
The study involved synthesizing a NOTA-conjugated precursor (NOTA-PSMA) using a peptide synthesizer, radiolabeling it with 68GaCl3 under mild conditions (pH 4.2 sodium acetate buffers at room temperature for 10 min), and evaluating its properties through in vitro and in vivo assays including stability tests, cell uptake studies, biodistribution, and micro-PET imaging. Theoretical models include affinity comparisons based on log Kd values for chelators.
2：2 sodium acetate buffers at room temperature for 10 min), and evaluating its properties through in vitro and in vivo assays including stability tests, cell uptake studies, biodistribution, and micro-PET imaging. Theoretical models include affinity comparisons based on log Kd values for chelators. Sample Selection and Data Sources:
2. Sample Selection and Data Sources: Samples included the synthesized NOTA-PSMA precursor, 68GaCl3, cell lines (22Rv1 with light PSMA expression and PC-3 as negative control), and animal models (BALB/c mice and nude mice bearing 22Rv1 and PC-3 tumors). Data were acquired from laboratory experiments.
3：List of Experimental Equipment and Materials:
Equipment includes peptide synthesizer, HPLC system, radio-HPLC, radio-TLC, micro-PET scanner, incubator, and Sep-pak C18 Cartridge. Materials include NOTA-PSMA, 68GaCl3, sodium acetate buffers, ethanol, saline, human serum albumin (HSA), PBS, octanol, ZJ-43 inhibitor, and cell culture reagents.
4：Experimental Procedures and Operational Workflow:
Steps include synthesis and purification of NOTA-PSMA, radiolabeling with 68Ga, purification using Sep-pak cartridge, stability tests in saline and HSA, log P measurement, cell uptake assays with blocking studies, biodistribution in mice, and micro-PET imaging at specified time points.
5：Data Analysis Methods:
Data were analyzed using radio-HPLC and radio-TLC for purity, statistical tests (e.g., P-values for significance), and imaging analysis with ROI drawing for uptake ratios.
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peptide synthesizer
Used for synthesizing the NOTA-PSMA precursor.
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HPLC system
Used for chemical purity analysis of NOTA-PSMA and radiochemical purity analysis of 68Ga-PSMA-BCH.
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radio-HPLC
Used for analyzing radiochemical purity of 68Ga-PSMA-BCH.
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radio-TLC
Used for analyzing radiochemical purity and stability of 68Ga-PSMA-BCH, with methanol and 1 M NH4Ac solution as eluant.
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Sep-pak C18 Cartridge
Used for purification of 68Ga-PSMA-BCH after radiolabeling.
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micro-PET scanner
Used for imaging studies in mice to visualize tumor uptake.
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68Ge-68Ga generator
Source of 68Ga radionuclide for labeling.
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