Devine, R, Martin, DSD, Kinsella, GK et al. (2 more authors) (2020) Characterization of an aryl piperazine/2-hydroxypropyl-β-cyclodextrin association, a complex with antidiabetic potential. Results in Chemistry, 2. 100026. ISSN 2211-7156
Abstract
This study explores the molecular association between 4-(thiophen-2-yl)-1-(4-(4-(trifluoromethyl)phenyl)piperazin-1-yl)butan-1-one (RTC1), an antidiabetic compound recently reported by our research group with challenging aqueous solubility, and 2-hydroxypropyl-β-cyclodextrin (HPBCD). The formation of a RTC1/HPBCD complex resulted in improved solubility. A phase-solubility diagram was used to determine the complex stability constant and stoichiometric ratio. 2D 1H NMR spectroscopy was utilized to study the molecular interaction between RTC1 and HPBCD in the complex. Differential scanning calorimetry and scanning electron microscopy was also employed to confirm complex formation. In vitro biological evaluation, using a glucose uptake assay, showed that the homogeneous RTC1/HPBCD complex solution showed the same activity to that of RTC1 alone, with no reduction in activity due to the presence of HPBCD.
Metadata
Item Type: | Article |
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Authors/Creators: |
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Copyright, Publisher and Additional Information: | © 2020 Published by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/). |
Keywords: | Diabetes; Aryl piperazine; 2-Hydroxypropyl-β-cyclodextrin |
Dates: |
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Institution: | The University of Leeds |
Academic Units: | The University of Leeds > Faculty of Biological Sciences (Leeds) > School of Biomedical Sciences (Leeds) |
Depositing User: | Symplectic Publications |
Date Deposited: | 28 Jun 2021 10:17 |
Last Modified: | 28 Jun 2021 10:17 |
Status: | Published |
Publisher: | Elsevier |
Identification Number: | 10.1016/j.rechem.2020.100026 |
Open Archives Initiative ID (OAI ID): | oai:eprints.whiterose.ac.uk:175575 |