Non-invasive glucagon-like peptide-1 receptor imaging in pancreas with ¹⁸F-Al labeled Cys³⁹-exendin-4

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• 作者：Baoming Mi^a ; ^c ; ¹ ; Yuping Xu^b ; ^d ; ¹ ; Donghui Pan^b ; Lizhen Wang^b ; Runlin Yang^b ; Chunjing Yu^c ; Weixing Wan^c ; Yiwei Wu^a ; ^{wuyiwei3988@gmail.com" class="auth_mail" title="E-mail the corresponding author} ; Min Yang^b ; ^d ; ^{ymzfk@yahoo.com.hk" class="auth_mail" title="E-mail the corresponding author}
• 关键词：GLP-1R Imaging ; Pancreas ; PET ; 18F-Al-NOTA-MAL-Cys39-exendin-4
• 刊名：Biochemical and Biophysical Research Communications
• 出版年：2016
• 出版时间：26 February 2016
• 年：2016
• 卷：471
• 期：1
• 页码：47-51
• 全文大小：898 K

文摘

Glucagon-like peptide-1 receptor (GLP-1R) is abundantly expressed on beta cells and may be an ideal target for the pancreas imaging. Monitoring the GLP-1R of pancreas could be benefit for understanding the pathophysiology of diabetes. In the present study, ¹⁸F-Al labeled exendin-4 analog, ¹⁸F-Al-NOTA-MAL-Cys³⁹-exendin-4, was evaluated for PET imaging GLP-1R in the pancreas.

4 id="absSec_2">Methods4>

The targeting of ¹⁸F-Al labeled exendin-4 analog was examined in healthy and streptozotocin induced diabetic rats. Rats were injected with ¹⁸F-Al-NOTA-MAL-Cys³⁹-exendin-4 and microPET imaging was performed at 1 h postinjection, followed by ex vivo biodistribution. GLP-1R expression in pancreas was determined through post mortern examinations.

4 id="absSec_3">Results4>

The pancreas of healthy rats was readily visualized after administration of ¹⁸F-Al-NOTA-MAL-Cys³⁹-exendin-4, whereas the pancreas of diabetic rats, as well as those from rats co-injected with excess of unlabeled peptides, was barely visible by microPET. At 60 min postinjection, the pancreatic uptakes were 1.02 ± 0.15%ID/g and 0.23 ± 0.05%ID/g in healthy and diabetic rats respectively. Under block, the pancreatic uptakes of non-diabetic rats reduced to 0.21 ± 0.07%ID/g at the same time point. Biodistribution data and IHC staining confirmed the findings of the microPET imaging.

4 id="absSec_4">Conclusion4>

The favorable preclinical data indicated that ¹⁸F-Al-NOTA-MAL-Cys³⁹-exendin-4may be suitable for non-invasive monitoring functional pancreatic beta cells.