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James E. Polli - One of the best experts on this subject based on the ideXlab platform.

  • In Vivo Performance of a Novel Fluorinated Magnetic Resonance Imaging Agent for Functional Analysis of Bile Acid Transport
    2015
    Co-Authors: Diana Vivian, Kunrong Cheng, Sandeep Khurana, Edwin H. Kriel, Paul A. Dawson, Jean-pierre Raufman, James E. Polli
    Abstract:

    A novel trifluorinated Cholic Acid Derivative, CA-lys-TFA, was designed and synthesized for use as a tool to measure bile Acid transport noninvasively using magnetic resonance imaging (MRI). In the present study, the in vivo performance of CA-lys-TFA for measuring bile Acid transport by MRI was investigated in mice. Gallbladder CA-lys-TFA content was quantified using MRI and liquid chromatography/tandem mass spectrometry. Results in wild-type (WT) C57BL/6J mice were compared to those in mice lacking expression of Asbt, the ileal bile Acid transporter. 19F signals emanating from the gallbladders of WT mice 7 h after oral gavage with 150 mg/kg CA-lys-TFA were reproducibly detected by MRI. Asbt-deficient mice administered the same dose had undetectable 19F signals by MRI, and gallbladder bile CA-lys-TFA levels were 30-fold lower compared to WT animals. To our knowledge, this represents the first report of in vivo imaging of an orally absorbed drug using 19F MRI. Fluorinated bile Acid analogues have potential as tools to measure and detect abnormal bile Acid transport by MRI

  • In vivo performance of a novel fluorinated magnetic resonance imaging agent for functional analysis of bile Acid transport.
    Molecular pharmaceutics, 2014
    Co-Authors: Diana Vivian, Kunrong Cheng, Sandeep Khurana, Edwin H. Kriel, Paul A. Dawson, Jean-pierre Raufman, James E. Polli
    Abstract:

    A novel trifluorinated Cholic Acid Derivative, CA-lys-TFA, was designed and synthesized for use as a tool to measure bile Acid transport noninvasively using magnetic resonance imaging (MRI). In the present study, the in vivo performance of CA-lys-TFA for measuring bile Acid transport by MRI was investigated in mice. Gallbladder CA-lys-TFA content was quantified using MRI and liquid chromatography/tandem mass spectrometry. Results in wild-type (WT) C57BL/6J mice were compared to those in mice lacking expression of Asbt, the ileal bile Acid transporter. (19)F signals emanating from the gallbladders of WT mice 7 h after oral gavage with 150 mg/kg CA-lys-TFA were reproducibly detected by MRI. Asbt-deficient mice administered the same dose had undetectable (19)F signals by MRI, and gallbladder bile CA-lys-TFA levels were 30-fold lower compared to WT animals. To our knowledge, this represents the first report of in vivo imaging of an orally absorbed drug using (19)F MRI. Fluorinated bile Acid analogues have potential as tools to measure and detect abnormal bile Acid transport by MRI.

  • Su2017 In Vivo Performance of a Novel Fluorinated Magnetic Resonance Imaging Agent for Functional Analysis of Bile Acid Transport
    Gastroenterology, 2014
    Co-Authors: Diana Vivian, Kunrong Cheng, Sandeep Khurana, Edwin H. Kriel, Paul A. Dawson, James E. Polli, Jean-pierre Raufman
    Abstract:

    A novel trifluorinated Cholic Acid Derivative, CA-lys-TFA, was designed and synthesized for use as a tool to measure bile Acid transport noninvasively using magnetic resonance imaging (MRI). In the present study, the in vivo performance of CA-lys-TFA for measuring bile Acid transport by MRI was investigated in mice. Gallbladder CA-lys-TFA content was quantified using MRI and liquid chromatography/tandem mass spectrometry. Results in wild-type (WT) C57BL/6J mice were compared to those in mice lacking expression of Asbt, the ileal bile Acid transporter. 19F signals emanating from the gallbladders of WT mice 7 h after oral gavage with 150 mg/kg CA-lys-TFA were reproducibly detected by MRI. Asbt-deficient mice administered the same dose had undetectable 19F signals by MRI, and gallbladder bile CA-lys-TFA levels were 30-fold lower compared to WT animals. To our knowledge, this represents the first report of in vivo imaging of an orally absorbed drug using 19F MRI. Fluorinated bile Acid analogues have potential...

Jean-pierre Raufman - One of the best experts on this subject based on the ideXlab platform.

  • In Vivo Performance of a Novel Fluorinated Magnetic Resonance Imaging Agent for Functional Analysis of Bile Acid Transport
    2015
    Co-Authors: Diana Vivian, Kunrong Cheng, Sandeep Khurana, Edwin H. Kriel, Paul A. Dawson, Jean-pierre Raufman, James E. Polli
    Abstract:

    A novel trifluorinated Cholic Acid Derivative, CA-lys-TFA, was designed and synthesized for use as a tool to measure bile Acid transport noninvasively using magnetic resonance imaging (MRI). In the present study, the in vivo performance of CA-lys-TFA for measuring bile Acid transport by MRI was investigated in mice. Gallbladder CA-lys-TFA content was quantified using MRI and liquid chromatography/tandem mass spectrometry. Results in wild-type (WT) C57BL/6J mice were compared to those in mice lacking expression of Asbt, the ileal bile Acid transporter. 19F signals emanating from the gallbladders of WT mice 7 h after oral gavage with 150 mg/kg CA-lys-TFA were reproducibly detected by MRI. Asbt-deficient mice administered the same dose had undetectable 19F signals by MRI, and gallbladder bile CA-lys-TFA levels were 30-fold lower compared to WT animals. To our knowledge, this represents the first report of in vivo imaging of an orally absorbed drug using 19F MRI. Fluorinated bile Acid analogues have potential as tools to measure and detect abnormal bile Acid transport by MRI

  • In vivo performance of a novel fluorinated magnetic resonance imaging agent for functional analysis of bile Acid transport.
    Molecular pharmaceutics, 2014
    Co-Authors: Diana Vivian, Kunrong Cheng, Sandeep Khurana, Edwin H. Kriel, Paul A. Dawson, Jean-pierre Raufman, James E. Polli
    Abstract:

    A novel trifluorinated Cholic Acid Derivative, CA-lys-TFA, was designed and synthesized for use as a tool to measure bile Acid transport noninvasively using magnetic resonance imaging (MRI). In the present study, the in vivo performance of CA-lys-TFA for measuring bile Acid transport by MRI was investigated in mice. Gallbladder CA-lys-TFA content was quantified using MRI and liquid chromatography/tandem mass spectrometry. Results in wild-type (WT) C57BL/6J mice were compared to those in mice lacking expression of Asbt, the ileal bile Acid transporter. (19)F signals emanating from the gallbladders of WT mice 7 h after oral gavage with 150 mg/kg CA-lys-TFA were reproducibly detected by MRI. Asbt-deficient mice administered the same dose had undetectable (19)F signals by MRI, and gallbladder bile CA-lys-TFA levels were 30-fold lower compared to WT animals. To our knowledge, this represents the first report of in vivo imaging of an orally absorbed drug using (19)F MRI. Fluorinated bile Acid analogues have potential as tools to measure and detect abnormal bile Acid transport by MRI.

  • Su2017 In Vivo Performance of a Novel Fluorinated Magnetic Resonance Imaging Agent for Functional Analysis of Bile Acid Transport
    Gastroenterology, 2014
    Co-Authors: Diana Vivian, Kunrong Cheng, Sandeep Khurana, Edwin H. Kriel, Paul A. Dawson, James E. Polli, Jean-pierre Raufman
    Abstract:

    A novel trifluorinated Cholic Acid Derivative, CA-lys-TFA, was designed and synthesized for use as a tool to measure bile Acid transport noninvasively using magnetic resonance imaging (MRI). In the present study, the in vivo performance of CA-lys-TFA for measuring bile Acid transport by MRI was investigated in mice. Gallbladder CA-lys-TFA content was quantified using MRI and liquid chromatography/tandem mass spectrometry. Results in wild-type (WT) C57BL/6J mice were compared to those in mice lacking expression of Asbt, the ileal bile Acid transporter. 19F signals emanating from the gallbladders of WT mice 7 h after oral gavage with 150 mg/kg CA-lys-TFA were reproducibly detected by MRI. Asbt-deficient mice administered the same dose had undetectable 19F signals by MRI, and gallbladder bile CA-lys-TFA levels were 30-fold lower compared to WT animals. To our knowledge, this represents the first report of in vivo imaging of an orally absorbed drug using 19F MRI. Fluorinated bile Acid analogues have potential...

Diana Vivian - One of the best experts on this subject based on the ideXlab platform.

  • In Vivo Performance of a Novel Fluorinated Magnetic Resonance Imaging Agent for Functional Analysis of Bile Acid Transport
    2015
    Co-Authors: Diana Vivian, Kunrong Cheng, Sandeep Khurana, Edwin H. Kriel, Paul A. Dawson, Jean-pierre Raufman, James E. Polli
    Abstract:

    A novel trifluorinated Cholic Acid Derivative, CA-lys-TFA, was designed and synthesized for use as a tool to measure bile Acid transport noninvasively using magnetic resonance imaging (MRI). In the present study, the in vivo performance of CA-lys-TFA for measuring bile Acid transport by MRI was investigated in mice. Gallbladder CA-lys-TFA content was quantified using MRI and liquid chromatography/tandem mass spectrometry. Results in wild-type (WT) C57BL/6J mice were compared to those in mice lacking expression of Asbt, the ileal bile Acid transporter. 19F signals emanating from the gallbladders of WT mice 7 h after oral gavage with 150 mg/kg CA-lys-TFA were reproducibly detected by MRI. Asbt-deficient mice administered the same dose had undetectable 19F signals by MRI, and gallbladder bile CA-lys-TFA levels were 30-fold lower compared to WT animals. To our knowledge, this represents the first report of in vivo imaging of an orally absorbed drug using 19F MRI. Fluorinated bile Acid analogues have potential as tools to measure and detect abnormal bile Acid transport by MRI

  • In vivo performance of a novel fluorinated magnetic resonance imaging agent for functional analysis of bile Acid transport.
    Molecular pharmaceutics, 2014
    Co-Authors: Diana Vivian, Kunrong Cheng, Sandeep Khurana, Edwin H. Kriel, Paul A. Dawson, Jean-pierre Raufman, James E. Polli
    Abstract:

    A novel trifluorinated Cholic Acid Derivative, CA-lys-TFA, was designed and synthesized for use as a tool to measure bile Acid transport noninvasively using magnetic resonance imaging (MRI). In the present study, the in vivo performance of CA-lys-TFA for measuring bile Acid transport by MRI was investigated in mice. Gallbladder CA-lys-TFA content was quantified using MRI and liquid chromatography/tandem mass spectrometry. Results in wild-type (WT) C57BL/6J mice were compared to those in mice lacking expression of Asbt, the ileal bile Acid transporter. (19)F signals emanating from the gallbladders of WT mice 7 h after oral gavage with 150 mg/kg CA-lys-TFA were reproducibly detected by MRI. Asbt-deficient mice administered the same dose had undetectable (19)F signals by MRI, and gallbladder bile CA-lys-TFA levels were 30-fold lower compared to WT animals. To our knowledge, this represents the first report of in vivo imaging of an orally absorbed drug using (19)F MRI. Fluorinated bile Acid analogues have potential as tools to measure and detect abnormal bile Acid transport by MRI.

  • Su2017 In Vivo Performance of a Novel Fluorinated Magnetic Resonance Imaging Agent for Functional Analysis of Bile Acid Transport
    Gastroenterology, 2014
    Co-Authors: Diana Vivian, Kunrong Cheng, Sandeep Khurana, Edwin H. Kriel, Paul A. Dawson, James E. Polli, Jean-pierre Raufman
    Abstract:

    A novel trifluorinated Cholic Acid Derivative, CA-lys-TFA, was designed and synthesized for use as a tool to measure bile Acid transport noninvasively using magnetic resonance imaging (MRI). In the present study, the in vivo performance of CA-lys-TFA for measuring bile Acid transport by MRI was investigated in mice. Gallbladder CA-lys-TFA content was quantified using MRI and liquid chromatography/tandem mass spectrometry. Results in wild-type (WT) C57BL/6J mice were compared to those in mice lacking expression of Asbt, the ileal bile Acid transporter. 19F signals emanating from the gallbladders of WT mice 7 h after oral gavage with 150 mg/kg CA-lys-TFA were reproducibly detected by MRI. Asbt-deficient mice administered the same dose had undetectable 19F signals by MRI, and gallbladder bile CA-lys-TFA levels were 30-fold lower compared to WT animals. To our knowledge, this represents the first report of in vivo imaging of an orally absorbed drug using 19F MRI. Fluorinated bile Acid analogues have potential...

Luciano Galantini - One of the best experts on this subject based on the ideXlab platform.

  • Twisted nanoribbons from a RGD-bearing Cholic Acid Derivative
    Colloids and surfaces. B Biointerfaces, 2017
    Co-Authors: Leana Travaglini, Cesare Giordano, Andrea D'annibale, Marta Gubitosi, Maria Chiara Di Gregorio, Karin Schillén, Azzurra Stefanucci, Adriano Mollica, Nicolae Viorel Pavel, Luciano Galantini
    Abstract:

    Abstract In light of the biomedical interest for self-assembling amphiphiles bearing the tripeptide Arg-Gly-Gly (RGD), a Cholic Acid Derivative was synthesized by introducing an aromatic moiety on the steroidal skeleton and the RGD sequence on the carboxylic function of its chain 17–24, thus forming a peptide amphiphile with the unconventional rigid amphiphilic structure of bile salts. In aqueous solution, the compound self-assembled into long twisted ribbons characterized by a very low degree of polydispersity in terms of width (≈25 nm), thickness (≈4.5 nm) and pitch (≈145 nm). It was proposed that in the ribbon the molecules are arranged in a bilayer structure with the aromatic moieties in the interior, strongly involved in the intermolecular interaction, whereas the RGD residues are located at the bilayer-water interface. The nanostructure is significantly different from those generally provided by RGD-containing amphiphiles with the conventional peptide-tail structure, for which fibers with a circular cross-section were observed, and successfully tested as scaffolds for tissue regeneration. From previous work on the use of this kind of nanostructures, it is known that features like morphology, rigidity, epitope spacing and periodicity are important factors that dramatically affect cell adhesion and signaling. Within this context, the reported results demonstrate that bile salt-based peptide surfactants are promising building blocks in the preparation of non-trivial RGD-decorated nanoaggregates with well-defined morphologies and epitope distributions.

  • Multi stimuli response of a single surfactant presenting a rich self-assembly behavior
    RSC Advances, 2015
    Co-Authors: M. C. Di Gregorio, Leana Travaglini, Marta Gubitosi, Nicolae Viorel Pavel, Francisco Meijide, Maxim Varenik, Aida Jover, Oren Regev, Luciano Galantini
    Abstract:

    This work reports on the multi stimuli sensitivity of a Cholic Acid Derivative in a buffer. The molecules self-organize in single walled tubules at room temperature and pH 8.0–9.5. By increasing the pH to 10.0–12.0, these tubules open up and form scrolls, which transform by aging into different tubular structures. A further evolution from scrolls or tubules into ribbons is induced by increasing the temperature. Moreover, a transition into rolled lamellae can be triggered by adding NaCl. All transitions are reversible and accompanied by drastic molecular rearrangements, manifested by spectroscopic and imaging techniques. Such rich multi stimuli responsiveness is usually accomplished by block copolymers or peptides and seldom by pure surfactants. The reported surfactant provides in addition an uncommon variety of structures. The sharpness of the spectroscopic response suggests that the system could be employed in physico-chemical sensors with a rather narrow dynamic range.

Leana Travaglini - One of the best experts on this subject based on the ideXlab platform.

  • Twisted nanoribbons from a RGD-bearing Cholic Acid Derivative
    Colloids and surfaces. B Biointerfaces, 2017
    Co-Authors: Leana Travaglini, Cesare Giordano, Andrea D'annibale, Marta Gubitosi, Maria Chiara Di Gregorio, Karin Schillén, Azzurra Stefanucci, Adriano Mollica, Nicolae Viorel Pavel, Luciano Galantini
    Abstract:

    Abstract In light of the biomedical interest for self-assembling amphiphiles bearing the tripeptide Arg-Gly-Gly (RGD), a Cholic Acid Derivative was synthesized by introducing an aromatic moiety on the steroidal skeleton and the RGD sequence on the carboxylic function of its chain 17–24, thus forming a peptide amphiphile with the unconventional rigid amphiphilic structure of bile salts. In aqueous solution, the compound self-assembled into long twisted ribbons characterized by a very low degree of polydispersity in terms of width (≈25 nm), thickness (≈4.5 nm) and pitch (≈145 nm). It was proposed that in the ribbon the molecules are arranged in a bilayer structure with the aromatic moieties in the interior, strongly involved in the intermolecular interaction, whereas the RGD residues are located at the bilayer-water interface. The nanostructure is significantly different from those generally provided by RGD-containing amphiphiles with the conventional peptide-tail structure, for which fibers with a circular cross-section were observed, and successfully tested as scaffolds for tissue regeneration. From previous work on the use of this kind of nanostructures, it is known that features like morphology, rigidity, epitope spacing and periodicity are important factors that dramatically affect cell adhesion and signaling. Within this context, the reported results demonstrate that bile salt-based peptide surfactants are promising building blocks in the preparation of non-trivial RGD-decorated nanoaggregates with well-defined morphologies and epitope distributions.

  • A tryptophan-substituted Cholic Acid: Expanding the family of labelled biomolecules
    Colloids and Surfaces A: Physicochemical and Engineering Aspects, 2015
    Co-Authors: Leana Travaglini, Andrea D'annibale, Marta Gubitosi, Maria Chiara Di Gregorio, Karin Schillén, Francisco Meijide, Mauro Giustini, Simona Sennato, Marc Obiols-rabasa, Nicolae Viorel Pavel
    Abstract:

    The synthesis of a novel Cholic Acid Derivative bearing in the C-3 position a residue of tryptophan linked through an amide bond is herein described. Acidic or basic conditions are needed for the solubilization of the Derivative in water. In alkaline solutions the molecule shows a self-association similar to the one of its natural precursor leading to the formation of ellipsoidal micelles which does not involve significant Trp–Trp interactions. On the contrary, in Acidic conditions strong interactions between the tryptophan moieties occur, leading to the formation of a gel at low temperature. These interactions are broken upon heating and small micelles similar to those observed at high pH are formed. In both cases, fluorescence spectra suggest a polar environment for the amino Acid fluorophore not remarkably affected by the self-assembly.

  • Multi stimuli response of a single surfactant presenting a rich self-assembly behavior
    RSC Advances, 2015
    Co-Authors: M. C. Di Gregorio, Leana Travaglini, Marta Gubitosi, Nicolae Viorel Pavel, Francisco Meijide, Maxim Varenik, Aida Jover, Oren Regev, Luciano Galantini
    Abstract:

    This work reports on the multi stimuli sensitivity of a Cholic Acid Derivative in a buffer. The molecules self-organize in single walled tubules at room temperature and pH 8.0–9.5. By increasing the pH to 10.0–12.0, these tubules open up and form scrolls, which transform by aging into different tubular structures. A further evolution from scrolls or tubules into ribbons is induced by increasing the temperature. Moreover, a transition into rolled lamellae can be triggered by adding NaCl. All transitions are reversible and accompanied by drastic molecular rearrangements, manifested by spectroscopic and imaging techniques. Such rich multi stimuli responsiveness is usually accomplished by block copolymers or peptides and seldom by pure surfactants. The reported surfactant provides in addition an uncommon variety of structures. The sharpness of the spectroscopic response suggests that the system could be employed in physico-chemical sensors with a rather narrow dynamic range.