Abstract
The water-soluble vitamin biotin is essential for cellular growth, development, and well-being, but its absorption, distribution, metabolism, and excretion are poorly understood. This paper describes the radiolabeling of biotin with the positron emission tomography (PET) radionuclide carbon-11 ([11C]biotin) to enable the quantitative study of biotin trafficking in vivo. We show that intravenously administered [11C]biotin is quickly distributed to the liver, kidneys, retina, heart, and brain in rodents - consistent with the known expression of the biotin transporter - and there is a surprising accumulation in the brown adipose tissue (BAT). Orally administered [11C]biotin was rapidly absorbed in the small intestine and swiftly distributed to the same organs. Preadministration of nonradioactive biotin inhibited organ uptake and increased excretion. [11C]Biotin PET imaging therefore provides a dynamic in vivo map of transporter-mediated biotin trafficking in healthy rodents. This technique will enable the exploration of biotin trafficking in humans and its use as a research tool for diagnostic imaging of obesity/diabetes, bacterial infection, and cancer.
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CITATION STYLE
Bongarzone, S., Sementa, T., Dunn, J., Bordoloi, J., Sunassee, K., Blower, P. J., & Gee, A. (2020). Imaging Biotin Trafficking in Vivo with Positron Emission Tomography. Journal of Medicinal Chemistry, 63(15), 8265–8275. https://doi.org/10.1021/acs.jmedchem.0c00494
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