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1.
Colloids Surf B Biointerfaces ; 147: 151-160, 2016 Nov 01.
Article in English | MEDLINE | ID: mdl-27500358

ABSTRACT

There are requirements for surfaces with antibacterial properties in various technological fields. U-PEO hybrids with antibacterial properties were synthesized by the sol-gel process, incorporating combinations of cerium and silver salts at different silver molar fractions (0, 0.02, 0.05, 0.10, and 1) relative to the total amount of doped cations. The loaded hybrids were characterized by TGA, XRD, and Raman spectroscopy. Release tests were performed using UV-vis spectroscopy, and the antibacterial properties of the hybrids were studied in agar tests and turbidimetry assays. The nanostructural evolution of the hybrids during the release of the antibacterial agents was investigated by in situ SAXS. XRD results showed the presence of the AgCl crystalline phase in the loaded hybrids from a silver molar fraction of 0.05. Raman spectroscopy evidenced the interaction of silver cations with the polymeric part of the hybrid. SAXS results confirmed these interactions and showed that cerium species interacted with both organic and inorganic parts of the hybrids. The loaded U-PEO hybrids were found to release all the incorporated cerium in 1h, while the hybrid containing 100% of silver released only 78% of the incorporated silver. All the loaded hybrids displayed antibacterial activity against the Pseudomonas aeruginosa bacterium. The antibacterial activity was found to increase with silver molar fraction. Due to its high antibacterial activity and low silver molar fraction, the loaded hybrid with silver molar fraction of 0.10 seemed to be a good compromise between efficiency, esthetic transparency, and photostability.


Subject(s)
Anti-Bacterial Agents/pharmacology , Cerium/pharmacology , Pseudomonas aeruginosa/drug effects , Silver Compounds/pharmacology , Anti-Bacterial Agents/chemistry , Cerium/chemistry , Microbial Sensitivity Tests , Scattering, Small Angle , Silver Compounds/chemistry
2.
Bioorg Med Chem Lett ; 24(7): 1707-10, 2014 Apr 01.
Article in English | MEDLINE | ID: mdl-24630563

ABSTRACT

Trypanosoma brucei and Trypanosoma cruzi are the etiologic agents of sleeping sickness and Chagas disease, respectively, two of the 17 preventable tropical infectious diseases (NTD) which have been neglected by governments and organizations working in the health sector, as well as pharmaceutical industries. High toxicity and resistance are problems of the conventional drugs employed against trypanosomiasis, hence the need for the development of new drugs with trypanocidal activity. In this work we have evaluated the trypanocidal activity of a series of N1,N2-dibenzylethane-1,2-diamine hydrochlorides (benzyl diamines) and N1-benzyl,N2-methyferrocenylethane-1,2-diamine hydrochlorides (ferrocenyl diamines) against T. brucei and T. cruzi parasite strains. We show that incorporation of the ferrocenyl group into the benzyl diamines increases the trypanocidal activity. The molecules exhibit potential trypanocidal activity in vitro against all parasite strains. Cytotoxicity assay was also carried out to evaluate the toxicity in HepG2 cells.


Subject(s)
Benzyl Compounds/pharmacology , Diamines/pharmacology , Ferrous Compounds/pharmacology , Trypanocidal Agents/pharmacology , Trypanosoma brucei brucei/drug effects , Trypanosoma cruzi/drug effects , Benzyl Compounds/chemical synthesis , Benzyl Compounds/chemistry , Cell Survival/drug effects , Diamines/chemical synthesis , Diamines/chemistry , Dose-Response Relationship, Drug , Ferrous Compounds/chemical synthesis , Ferrous Compounds/chemistry , Hep G2 Cells , Humans , Metallocenes , Molecular Structure , Parasitic Sensitivity Tests , Structure-Activity Relationship , Trypanocidal Agents/chemical synthesis , Trypanocidal Agents/chemistry
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