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Updated: May 23, 2026

Using Multi-fluorinated Bile Acids and In Vivo Magnetic Resonance Imaging to Measure Bile Acid Transport
Published on: November 27, 2016
Synthesis, characterization and biological activity of hydroxyl-bisphosphonic analogs of bile acids
Olga Bortolini1, Giancarlo Fantin, Marco Fogagnolo
1Dipartimento di Chimica and SOF-CNR sezione di Ferrara, Università di Ferrara, Via Borsari 46, 44121 Ferrara, Italy. olga.bortolini@unife.it
Abstract:
Bisphosphonates (BPs) are now the most widely used drugs for diseases associated with increased bone resorption, such as osteoporosis, and tumor bone diseases. A significant drawback of the BPs is their poor oral absorption that is enhanced by the presence of bile acid substituents in the bisphosphonate framework, with no toxic effects. A straightforward synthesis of bile acid-containing hydroxy-bisphosphonates and a full characterization of these pharmaceutically important molecules, including an evaluation of affinity and the mechanism of binding to hydroxyapatite, is presented. The biological activity of bile acid-containing bisphosphonate salts was determined using the neutral-red assay on the L929 cell line and primary cultures of osteoclasts. The bioactivity of the new compounds was found superior than bisphosphonates of established activity.
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