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Data for Hydrolyzable poly[poly(ethylene glycol) methyl ether acrylate]–colistin prodrugs through copper-mediated photoinduced living radical polymerization
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Zhu, Chongyu, Schneider, Elena K., Nikolaou, Vasiliki, Klein, Tobias, Li, Jian, Davis, Thomas P., Whittaker, Michael R., Wilson, Paul, Kempe, Kristian, Velkov, Tony and Haddleton, David M. (2017) Data for Hydrolyzable poly[poly(ethylene glycol) methyl ether acrylate]–colistin prodrugs through copper-mediated photoinduced living radical polymerization. [Dataset]
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Archive (ZIP) (Experimental details for the measurement data including NMR, HPLC, GPC, MALDI-ToF MS, Disk Diffusion Assay, Minimum Inhibitory Concentration and Time Kill assays)
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Official URL: https://doi.org/10.1021/acs.bioconjchem.7b00242
Abstract
Through the recently developed copper-mediated photoinduced living radical polymerization (CP-LRP), a novel and well-defined polymeric prodrug of the antimicrobial lipopeptide colistin has been developed. A colistin initiator (Boc5-col-Br2) was synthesized through the modification of colistin on both of its threonine residues using a cleavable initiator linker, 2-(2-bromo-2-methylpropanoyloxy) acetic acid (BMPAA), and used for the polymerization of acrylates via CP-LRP. Polymerization proceeds from both sites of the colistin initiator, and through the polymerization of poly(ethylene glycol) methyl ether acrylate (PEGA480), three water-soluble polymer-colistin conjugates (col-PPEGA, having degrees of polymerization of 5, 10, and 20) were achieved with high yield (conversion of ≥93%) and narrow dispersities (Đ < 1.3) in 2-4 h. Little or no effect on the structure and activity of the colistin was observed during the synthesis, and most of the active colistin can be recovered from the conjugates in vitro within 2 days. Furthermore, in vitro biological analyses including disk diffusion, broth microdilution, and time-kill studies suggested that all of the conjugates have the ability to inhibit the growth of multidrug-resistant (MDR) Gram-negative bacteria, of which col-PPEGA DP5 and DP10 showed similar or better antibacterial performance compared to the clinically relevant colistin prodrug CMS, indicating their potential as an alternative antimicrobial therapy. Moreover, considering the control over the polymerization, the CP-LRP technique has the potential to provide an alternative platform for the development of polymer bioconjugates.
| Item Type: | Dataset | |||||||||||||||||||||||||||
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| Subjects: | Q Science > QD Chemistry Q Science > QR Microbiology R Medicine > RM Therapeutics. Pharmacology |
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| Divisions: | Faculty of Science > Chemistry | |||||||||||||||||||||||||||
| SWORD Depositor: | Library Publications Router | |||||||||||||||||||||||||||
| Type of Data: | Individual files: Excel, Word, PowerPoint, Origin, GPC software (from Agilent), MALDI ToF software (from Bruker), NMR software (from Bruker), HPLC software (from Agilent), PDF viewer, Photo viewer, Text viewer | |||||||||||||||||||||||||||
| Library of Congress Subject Headings (LCSH): | Prodrugs, Polymerization, Multidrug resistance, Gram-negative bacteria | |||||||||||||||||||||||||||
| Journal or Publication Title: | Bioconjugate Chemistry | |||||||||||||||||||||||||||
| Publisher: | Department of Chemistry, University of Warwick | |||||||||||||||||||||||||||
| ISSN: | 1043-1802 | |||||||||||||||||||||||||||
| Official Date: | 26 July 2017 | |||||||||||||||||||||||||||
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| DOI: | 10.1021/acs.bioconjchem.7b00242 | |||||||||||||||||||||||||||
| Status: | Peer Reviewed | |||||||||||||||||||||||||||
| Publisher Statement: | ** From PubMed via Jisc Publications Router. | |||||||||||||||||||||||||||
| Access rights to Published version: | Restricted or Subscription Access | |||||||||||||||||||||||||||
| Description: | Experimental details for the measurement data including NMR, HPLC, GPC, MALDI-ToF MS, Disk Diffusion Assay, Minimum Inhibitory Concentration and Time Kill assays |
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