Please use this identifier to cite or link to this item: http://hdl.handle.net/1822/49052

TitlePreparation and biological evaluation of ethionamide-mesoporous silicon nanoparticles against Mycobacterium tuberculosis
Author(s)Vale, Nuno
Correia, Alexandra
Silva, Sara
Figueiredo, Patrícia
Mäkilä, , Ermei
Salonen, Jarno
Hirvonen, Jouni
Pedrosa, Jorge
Santos Hélder A.
Fraga, Alexandra
KeywordsEthionamide
Porous silicon nanoparticles
Mycobacterium tuberculosis
Strain H37Rv
MIC50
Issue date1-Feb-2017
PublisherElsevier
JournalBioorganic & Medicinal Chemistry Letters
CitationVale, N., Correia, A., Silva, S., Figueiredo, P., Mäkilä, E., Salonen, J., ... & Fraga, A. (2017). Preparation and biological evaluation of ethionamide-mesoporous silicon nanoparticles against Mycobacterium tuberculosis. Bioorganic & medicinal chemistry letters, 27(3), 403-405
Abstract(s)Ethionamide (ETH) is an important second-line antituberculosis drug used for the treatment of patients infected with multidrug-resistant Mycobacterium tuberculosis. Recently, we reported that the loading of ETH into thermally carbonized-porous silicon (TCPSi) nanoparticles enhanced the solubility and permeability of ETH at different pH-values and also increased its metabolization process. Based on these results, we synthesized carboxylic acid functionalized thermally hydrocarbonized porous silicon nanoparticles (UnTHCPSi NPs) conjugated with ETH and its antimicrobial effect was evaluated against Mycobacterium tuberculosis strain H37Rv. The activity of the conjugate was increased when compared to free-ETH, which suggests that the nature of the synergy between the NPs and ETH is likely due to the weakening of the bacterial cell wall that improves conjugate-penetration. These ETH-conjugated NPs have great potential in reducing dosing frequency of ETH in the treatment of multidrug-resistant tuberculosis (MDR-TB). (C) 2016 Elsevier Ltd. All rights reserved.
TypeArticle
URIhttp://hdl.handle.net/1822/49052
DOI10.1016/j.bmcl.2016.12.060
ISSN0960-894X
Publisher versionhttp://www.sciencedirect.com/science/article/pii/S0960894X16313397
Peer-Reviewedyes
AccessOpen access
Appears in Collections:ICVS - Artigos em Revistas Internacionais com Referee

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