AI Article Synopsis
- Researchers developed improved inhibitors for MMP-12, which could help treat lung and heart diseases, by adding an ionic liquid structure to increase their water solubility.
- Four new biologically active salts were created by connecting a sulfonamide part of the MMP-12 inhibitor to different ionic liquids, showing promising activity and solubility.
- One of the new salts, based on imidazolium, was used to create gold nanoparticles that can target MMP-12, allowing for advanced studies on its location within cells using electron microscopy.
Article Abstract
Selective and potent matrix metalloproteinase 12 (MMP-12) inhibitors endowed with improved hydrophilicity are highly sought for potential use in the treatment of lung and cardiovascular diseases. In the present paper, we modified the structure of a nanomolar MMP-12 inhibitor by incorporating an ionic liquid (IL) moiety to improve aqueous solubility. Four biologically active salts were obtained by linking the sulfonamide moiety of the MMP-12 inhibitor to imidazolium-, pyrrolidinium-, piperidinium-, and DABCO-based ILs. The imidazolium-based bioactive salt was tested on human recombinant MMPs and on monocyte-derived dendritic cells, showing activity similar to that of the parent compound, but improved water solubility. The imidazolium-based bioactive salt was then used to prepare electrostatically stabilized MMP inhibitor-coated gold nanoparticles (AuNPs) able to selectively bind MMP-12. These AuNPs were used to study subcellular localization of MMP-12 in monocyte-derived dendritic cells by transmission electron microscopy analysis.
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| http://dx.doi.org/10.1002/cmdc.201800733 | DOI Listing |
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