¹⁹F-heptuloses as tools for the non-invasive imaging of GLUT2-expressing cells

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• 作者：Willy J. Malaisse^a ; ^{malaisse@ulb.ac.be} ; Ying Zhang^a ; Karim Louchami^a ; Sonu Sharma^b ; Tom Dresselaers^b ; Uwe Himmelreich^b ; Guy Wayne Novotny^c ; Thomas Mandrup-Poulsen^c ; ^d ; Daniel Waschke^e ; Yevgeniy Leshch^e ; Julian Thimm^e ; Joachim Thiem^e ; Abdullah Sener^a
• 关键词：19F-heptuloses ; GLUT2-expressing cells ; Rat hepatocytes ; Insulin secretion ; Rat pancreatic islets
• 刊名：Archives of Biochemistry and Biophysics
• 出版年：2012
• 出版时间：15 January 2012
• 年：2012
• 卷：517
• 期：2
• 页码：138-143
• 全文大小：623 K

文摘

Suitable analogs of d-mannoheptulose are currently considered as possible tools for the non-invasive imaging of pancreatic islet insulin-producing cells. Here, we examined whether ¹⁹F-heptuloses could be used for non-invasive imaging of GLUT2-expressing cells. After 20 min incubation, the uptake of ¹⁹F-heptuloses (25 mM) by rat hepatocytes, as assessed by ¹⁹F NMR spectroscopy, ranged from 0.50 (1-deoxy-1-fluoro-d-mannoheptulose and 3-deoxy-3-fluoro-d-mannoheptulose) to 0.25 (1,3-dideoxy-1,3-difluoro-d-mannoheptulose) and 0.13 (1-deoxy-1-fluoro-d-glucoheptulose, 3-deoxy-3-fluoro-d-glucoheptulose and 1,3-dideoxy-1,3-difluoro-d-glucoheptulose) ¦Ìmol per 3 ¡Á 10⁶ cells. ¹⁹F MRI experiments also allowed the detection of 1-deoxy-1-fluoro-d-mannoheptulose in rat hepatocytes. All three ¹⁹F-mannoheptuloses cited above, as well as 7-deoxy-7-fluoro-d-mannoheptulose and 1-deoxy-1-fluoro-d-glucoheptulose inhibited insulin release evoked in rat isolated pancreatic islets by 10 mM d-glucose to the same extent as that observed with an equivalent concentration (10 mM) of d-mannoheptulose, while 3-deoxy-3-fluoro-d-glucoheptulose and 1,3-dideoxy-1,3-difluoro-d-glucoheptulose (also 10 mM) were less potent than d-mannoheptulose in inhibiting insulin release. The 1-deoxy-1-fluoro-d-mannoheptulose and 3-deoxy-3-fluoro-d-mannoheptulose only marginally affected INS-1 cell viability. These findings are compatible with the view that selected ¹⁹F-heptuloses may represent suitable tools for the non-invasive imaging of hepatocytes and insulin-producing cells by ¹⁹F MRI.