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1.
Org Biomol Chem ; 17(22): 5533-5537, 2019 06 05.
Artículo en Inglés | MEDLINE | ID: mdl-31090781

RESUMEN

Taking inspiration from the assembly of so-called peptoids (N-alkylglycine oligomers) we present a new synthetic methodology whereby N-heterocyclic carbene (NHC) based Pd ligands were assembled using a sub-monomer approach and loaded with Pd via solid-phase synthesis. This allowed the rapid generation a library of NHC-palladium catalysts that were readily functionalised to allow bioconjugation. These catalysts were able to rapidly activate a caged fluorophore and 'switch-on' an anticancer prodrug in 3D cell culture.


Asunto(s)
Materiales Biocompatibles/síntesis química , Compuestos Heterocíclicos/síntesis química , Metano/análogos & derivados , Paladio/química , Técnicas de Síntesis en Fase Sólida , Materiales Biocompatibles/química , Materiales Biocompatibles/farmacología , Catálisis , Supervivencia Celular/efectos de los fármacos , Compuestos Heterocíclicos/química , Compuestos Heterocíclicos/farmacología , Humanos , Ligandos , Células MCF-7 , Metano/síntesis química , Metano/química , Metano/farmacología , Estructura Molecular
2.
Int J Biol Macromol ; 258(Pt 1): 128838, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38128798

RESUMEN

Pseudomonas aeruginosa is one of the leading causes of opportunistic infections such as chronic wound infection that could lead to multiple organ failure and death. Gallium (Ga3+) ions are known to inhibit P. aeruginosa growth and biofilm formation but require carrier for localized controlled delivery. Lactoferrin (LTf), a two-lobed protein, can deliver Ga3+ at sites of infection. This study aimed to develop a Ga-LTf complex for the treatment of wound infection. The characterisation of the Ga-LTf complex was conducted using differential scanning calorimetry (DSC), Infra-Red (FTIR) and Inductive Coupled Plasma Optical Emission Spectrometry (ICP-OES). The antibacterial activity was assessed by agar disc diffusion, liquid broth and biofilm inhibition assays using the colony forming units (CFUs). The healing capacity and biocompatibility were evaluated using a P.aeruginosa infected wound in a rat model. DSC analyses showed thermal transition consistent with apo-lactoferrin; FTIR confirmed the complexation of gallium to lactoferrin. ICP-OES confirmed the controlled local delivery of Ga3+. Ga-LTf showed a 0.57 log10 CFUs reduction at 24 h compared with untreated control in planktonic liquid broth assay. Ga-LTf showed the highest antibiofilm activity with a 2.24 log10 CFUs reduction at 24 h. Furthermore, Ga-LTf complex is biocompatible without any adverse effect on brain, kidney, liver and spleen of rats tested in this study. Ga-LTf can be potentially promising novel therapeutic agent to treat pathogenic bacterial infections.


Asunto(s)
Galio , Ratas , Animales , Galio/química , Galio/metabolismo , Galio/farmacología , Pseudomonas aeruginosa , Lactoferrina/metabolismo , Antibacterianos/farmacología , Biopelículas
3.
Chem Asian J ; 12(1): 76-85, 2017 Jan 03.
Artículo en Inglés | MEDLINE | ID: mdl-27925415

RESUMEN

Red-light-emitting water-soluble semiconducting quantum dots (QDs) were synthesized by using a wide variety of commercially available thiol-type capping agents. QDs with a negatively charged nanosurface showed excellent selectivity for paraquat (PQ) at pH 7.4 over other commonly encountered pesticides/herbicides, including diquat (DQ). The presence of a 4,4'-bis-pyridinium unit in PQ enabled it to initiate long-range aggregation, thereby leading to the formation of nanostructures with excellent emission-quenching behavior. Precoated quartz plates were developed as a low-cost, portable sensor for the on-site detection of PQ in both natural water and human urine. Estimation of the PQ concentration was performed in different commercial formulations and the detection of PQ contamination in adulterated dairy product was also achieved with excellent sensitivity. Finally, we screened more than 50 different food items, including vegetables, fruits, cereals, and fodders, to construct a generalized marker for any residual PQ in such specimens.


Asunto(s)
Compuestos de Cadmio/química , Productos Agrícolas/química , Análisis de los Alimentos , Contaminación de Alimentos/análisis , Herbicidas/análisis , Luz , Nanopartículas/química , Telurio/química , Compuestos de Cadmio/síntesis química , Tamaño de la Partícula , Propiedades de Superficie
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