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1.
Biomolecules ; 11(2)2021 01 29.
Artigo em Inglês | MEDLINE | ID: mdl-33572889

RESUMO

Lectins are a class of proteins responsible for several biological roles such as cell-cell interactions, signaling pathways, and several innate immune responses against pathogens. Since lectins are able to bind to carbohydrates, they can be a viable target for targeted drug delivery systems. In fact, several lectins were approved by Food and Drug Administration for that purpose. Information about specific carbohydrate recognition by lectin receptors was gathered herein, plus the specific organs where those lectins can be found within the human body.


Assuntos
Carboidratos/química , Lectinas/química , Receptor de Asialoglicoproteína/química , Sistemas de Liberação de Medicamentos , Humanos , Ligação de Hidrogênio , Imunidade Inata , Ligantes , Proteínas/química , Transdução de Sinais , Estados Unidos , United States Food and Drug Administration
2.
Molecules ; 25(7)2020 Apr 10.
Artigo em Inglês | MEDLINE | ID: mdl-32290160

RESUMO

Polymeric nanoparticles can be used for drug delivery systems in healthcare. For this purpose poly(lactic-co-glycolic acid) (PLGA) and poly(ethylene glycol) (PEG) offer an excellent polymeric matrix. In this work, PLGA and PEG polymers were functionalized with coumarin and carbohydrate moieties such as thymidine, glucose, galactose, and mannose that have high biological specificities. Using a single oil in water emulsion methodology, functionalized PLGA nanoparticles were prepared having a smooth surface and sizes ranging between 114-289 nm, a low polydispersity index and a zeta potential from -28.2 to -56.0 mV. However, for the corresponding PEG derivatives the polymers obtained were produced in the form of films due to the small size of the hydrophobic core.


Assuntos
Carboidratos/química , Nanopartículas/química , Polímeros/química , Técnicas de Química Sintética , Portadores de Fármacos/química , Ligantes , Nanopartículas/ultraestrutura , Polietilenoglicóis/química , Ácido Poliglicólico/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/química
3.
Polymers (Basel) ; 12(1)2020 Jan 04.
Artigo em Inglês | MEDLINE | ID: mdl-31947904

RESUMO

Doxorubicin-loaded PLGA nanoparticles conjugated with a new galactose-based ligand for the specific recognition by human hepatoma cellular carcinoma cells (Hep G2) were successfully produced. The new targeting compound was selected using molecular docking combined with quantum chemical calculations for modelling and comparing molecular interactions among the H1 subunit of the asialoglycoprotein receptor containing the carbohydrate recognition domain and the ligand. The ligand, bis(1-O-ethyl-ß-D-galactopyranosyl)amine, was synthetized, characterized, and subsequently linked to PLGA. Unloaded (PLGA-di-GAL NP) and doxorubicin-loaded (DOX-PLGA-di-GAL NP) nanoparticles were prepared using an emulsion method and characterized. The produced DOX-PLGA-di-GAL NP are spherical in shape with a size of 258 ± 47 nm, a zeta potential of -62.3 mV, and a drug encapsulation efficiency of 83%. The in vitro drug release results obtained show a three-phase release profile. In vitro cell studies confirmed the interaction between Hep G2 cells and PLGA-di-GAL NP. Cell cytotoxicity tests showed that unloaded NP are nontoxic and that DOX-PLGA-di-GAL NP caused a decrease of around 80% in cellular viability. The strategy used in this work to design new targeting compounds represents a promising tool to develop effective hepatocyte targeting drug delivery systems and can be applied to other tissues/organs.

4.
Front Physiol ; 9: 1844, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30622481

RESUMO

The quality of fish flesh depends on the skeletal muscle's energetic state and delaying energy depletion through diets supplementation could contribute to the preservation of muscle's quality traits and modulation of fish allergens. Food allergies represent a serious public health problem worldwide with fish being one of the top eight more allergenic foods. Parvalbumins, have been identified as the main fish allergen. In this study, we attempted to produce a low allergenic farmed fish with improved muscle quality in controlled artificial conditions by supplementing a commercial fish diet with different creatine percentages. The supplementation of fish diets with specific nutrients, aimed at reducing the expression of parvalbumin, can be considered of higher interest and beneficial in terms of food safety and human health. The effects of these supplemented diets on fish growth, physiological stress, fish muscle status, and parvalbumin modulation were investigated. Data from zootechnical parameters were used to evaluate fish growth, food conversion ratios and hepatosomatic index. Physiological stress responses were assessed by measuring cortisol releases and muscle quality analyzed by rigor mortis and pH. Parvalbumin, creatine, and glycogen concentrations in muscle were also determined. Comparative proteomics was used to look into changes in muscle and liver tissues at protein level. Our results suggest that the supplementation of commercial fish diets with creatine does not affect farmed fish productivity parameters, or either muscle quality. Additionally, the effect of higher concentrations of creatine supplementation revealed a minor influence in fish physiological welfare. Differences at the proteome level were detected among fish fed with different diets. Differential muscle proteins expression was identified as tropomyosins, beta enolase, and creatine kinase among others, whether in liver several proteins involved in the immune system, cellular processes, stress, and inflammation response were modulated. Regarding parvalbumin modulation, the tested creatine percentages added to the commercial diet had also no effect in the expression of this protein. The use of proteomics tools showed to be sensitive to infer about changes of the underlying molecular mechanisms regarding fish responses to external stimulus, providing a holistic and unbiased view on fish allergens and muscle quality.

5.
J Microencapsul ; 33(4): 315-22, 2016 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-27189857

RESUMO

The objective of this work is to produce doxorubicin-loaded galactose-conjugated poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) to be specifically recognised by human hepatoma cellular carcinoma (Hep G2) cells and assess NPs cytotoxicity. Doxorubicin-unloaded and doxorubicin-loaded galactose-conjugated PLGA NPs were prepared using an emulsion method and characterised for morphology, size, drug release behaviour, Hep G2 recognition and cell cytotoxicity. The produced doxorubicin-loaded PLGA-galactose-conjugate nanoparticles (PLGA-GAL NPs) are spherical in shape with a size of 365 ± 74 nm, a drug encapsulation efficiency of 69% and released in a biphasic pattern with higher release rates at pH 5. In vitro cell studies confirmed the specific interaction between the receptors of Hep G2 and the PLGA-GAL NPs. Cell cytotoxicity tests showed that unloaded NPs are non-toxic and that doxorubicin-loaded NPs caused a cellular viability decrease of around 80%, therefore representing a promising approach to improve liver-specific drug delivery.


Assuntos
Doxorrubicina , Portadores de Fármacos , Galactose/química , Hepatócitos/metabolismo , Nanopartículas/química , Poliglactina 910/química , Animais , Células CHO , Cricetinae , Cricetulus , Doxorrubicina/química , Doxorrubicina/farmacocinética , Doxorrubicina/farmacologia , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Portadores de Fármacos/farmacologia , Células Hep G2 , Humanos
6.
Med Chem ; 12(1): 22-9, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26256586

RESUMO

Sucrose octa(N-ethyl)carbamate was synthesized directly from sucrose and ethyl isocyanate, and its structure was confirmed by various analytical methods, such as (1)H and (13)C NMR, FTIR, m.p., MS, and optical rotation. Its antibacterial, antifungal and cytotoxic activities were investigated. It exhibited strong inhibition against all bacteria tested, namely S. aureus (MIC 0.18±0.006), B. cereus (MIC 0.094±0.000), M. flavus (MIC 0.28±0.01), L. monocytogenes (MIC 0.18±0.006), P. aeruginosa (MIC 0.094±0.002), S. typhimurium (MIC 0.094±0.002), E. coli (MIC 0.18±0.006) and E. cloacae (MIC 0.18±0.006) and strong antifungal activity towards T. viride (MIC 0.09 ± 0.006), A. versicolor (MIC 0.18 ± 0.01), A. ochraceus (MIC 0.375 ± 0.01) and P. ochrochloron (MIC 0.375 ± 0.04). Furthermore, it showed moderate antitumor potential against human breast (GI50 357.20±14.12), colon (GI50 332.43±11.19) and cervical (GI50 282.67±3.97) cell lines and, more important, without hepatotoxicity.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antineoplásicos/farmacologia , Carbamatos/farmacologia , Sacarose/análogos & derivados , Ampicilina/farmacologia , Animais , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Antineoplásicos/síntese química , Antineoplásicos/química , Aspergillus/efeitos dos fármacos , Carbamatos/síntese química , Carbamatos/química , Linhagem Celular Tumoral , Bactérias Gram-Negativas/efeitos dos fármacos , Humanos , Penicillium/efeitos dos fármacos , Sacarose/síntese química , Sacarose/química , Sacarose/farmacologia , Suínos , Trichoderma/efeitos dos fármacos
7.
Homeopatia (Buenos Aires) ; 62(3): 207-9, 1997.
Artigo em Espanhol | HomeoIndex - Homeopatia | ID: hom-4871

RESUMO

Este trabajo trata sobre la ruptura del ligamento cruzado anterior y su tratamiento homeopatico. Se presentan dos casos


Assuntos
Relatos de Casos , Animais , Cães , Traumatismos do Joelho/terapia , Ligamento Cruzado Anterior/lesões
8.
Homeopatía [Argent.] ; 62(3): 207-9, 1997.
Artigo em Espanhol | BINACIS | ID: bin-19389

RESUMO

Este trabajo trata sobre la ruptura del ligamento cruzado anterior y su tratamiento homeopático. Se presentan dos casos (AU)


Assuntos
Animais , Cães , Ligamento Cruzado Anterior/lesões , Patologia Veterinária , Materia Medica , Terapêutica Homeopática
9.
Homeopatía (Argent.) ; 62(3): 207-9, 1997.
Artigo em Espanhol | LILACS | ID: lil-207863

RESUMO

Este trabajo trata sobre la ruptura del ligamento cruzado anterior y su tratamiento homeopático. Se presentan dos casos


Assuntos
Animais , Cães , Ligamento Cruzado Anterior/lesões , Materia Medica , Patologia Veterinária , Terapêutica Homeopática
10.
Homeopatia (Buenos Aires) ; 61(3): 99-105, 1996.
Artigo em Espanhol | HomeoIndex - Homeopatia | ID: hom-4116

RESUMO

La presente publicacion trata sobre el uso de Causticum en veterinaria homeopatica. Este remedio es raramente prescripto como medicamento constitucional y frecuentemente es olvidado como remedio local en enfermedades respiratorias, articulares, neurologicas y de piel. Este trabajo tiene por objeto demonstrar la accion de Causticum en desordenes neurologicos, centrales y perifericas. Finalmente, se presentan cierto numero de casos


Assuntos
Relatos de Casos , Animais , Gatos , Cães , Causticum , Matéria Médica Clínica
11.
Homeopatía [Argent.] ; 61(3): 99-105, 1996.
Artigo em Espanhol | BINACIS | ID: bin-19424

RESUMO

La presente publicación trata sobre el uso de Causticum en veterinaria homeopática. Este remedio es raramente prescripto como medicamento constitucional y frecuentemente es olvidado como remedio local en enfermedades respiratorias, articulares, neurológicas y de piel. Este trabajo tiene por objeto demostrar la acción de Causticum en desórdenes neurológicos, centrales y periféricos. Finalmente, se presentan cierto número de casos (AU)


Assuntos
Animais , Cães , Causticum/farmacologia , Prescrição Homeopática , Causticum/uso terapêutico , Potássio/farmacologia , Potássio/uso terapêutico , Paresia/terapia , Paralisia/terapia
12.
Homeopatía (Argent.) ; 61(3): 99-105, 1996.
Artigo em Espanhol | LILACS | ID: lil-207828

RESUMO

La presente publicación trata sobre el uso de Causticum en veterinaria homeopática. Este remedio es raramente prescripto como medicamento constitucional y frecuentemente es olvidado como remedio local en enfermedades respiratorias, articulares, neurológicas y de piel. Este trabajo tiene por objeto demostrar la acción de Causticum en desórdenes neurológicos, centrales y periféricos. Finalmente, se presentan cierto número de casos


Assuntos
Animais , Cães , Causticum/farmacologia , Prescrição Homeopática , Causticum/uso terapêutico , Paralisia/terapia , Paresia/terapia , Potássio/farmacologia , Potássio/uso terapêutico
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