Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 27, Issue 3, Pages 403-405Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.12.060
Keywords
Ethionamide; Porous silicon nanoparticles; Mycobacterium tuberculosis; Strain H37Rv; MIC50
Categories
Funding
- Fundacao para a Ciencia e Tecnologia (FCT, Portugal)
- FEDER (European Union) [UID/MULTI/04378/2013, IF/00092/2014, IF2014]
- Comissao de Coordenacao e Desenvolvimento Regional do Norte (CCDR-N)/NORTE/Portugal [Norte-01-0145-FEDER-000024]
- Academy of Finland [252215, 281300]
- University of Helsinki Research Funds
- Biocentrum Helsinki
- European Research Council under the European Union's Seventh Framework Programme (FP) [310892]
Ask authors/readers for more resources
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.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available
Share Paper
