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1.
Int J Biol Macromol ; 168: 676-685, 2021 Jan 31.
Artículo en Inglés | MEDLINE | ID: mdl-33220373

RESUMEN

Egletes viscosa is a plant with therapeutic value due to its antibacterial, antinociceptive and gastroprotective properties. This study aimed to purify, characterize, and evaluate the cytotoxicity of a lectin (EgviL) from the floral capitula of E. viscosa. The lectin was isolated from saline extract through precipitation with ammonium sulfate followed by Sephadex G-75 chromatography. The molecular mass and isoelectric point (pI) of EgviL were determined as well as its temperature and pH stability. Physical-chemical parameters of interaction between EgviL and carbohydrates were investigated by fluorescence quenching and 1H nuclear magnetic resonance (NMR). Cytotoxicity was investigated against human peripheral blood mononuclear cells (PBMCs) and neoplastic cells. EgviL (28.8 kDa, pI 5.4) showed hemagglutinating activity stable towards heating until 60 °C and at the pH range 5.0-7.0. This lectin is able to interact through hydrophobic and electrostatic bonds with galactose and glucose, respectively. EgviL reduced the viability of PBMCs only at the highest concentration tested (100 µg/mL) while was toxic to Jurkat E6-1 cells with IC50 of 24.1 µg/mL,inducing apoptosis. In summary, EgviL is a galactose/glucose-binding protein with acidic character, stable to heating and with cytotoxic effect on leukemic cells.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Asteraceae/química , Leucocitos Mononucleares/citología , Lectinas de Plantas/farmacología , Antineoplásicos Fitogénicos/química , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Precipitación Química , Estabilidad de Medicamentos , Galactosa/metabolismo , Glucosa/metabolismo , Pruebas de Hemaglutinación , Humanos , Interacciones Hidrofóbicas e Hidrofílicas , Concentración 50 Inhibidora , Punto Isoeléctrico , Células Jurkat , Leucocitos Mononucleares/efectos de los fármacos , Células MCF-7 , Lectinas de Plantas/química
2.
Int J Biol Macromol ; 136: 1034-1041, 2019 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-31233796

RESUMEN

Many skin disorders and diseases are related to tyrosinase activity, in particular, due to the vital role played by this enzyme in the melanogenic process. Although numerous natural and synthetic tyrosinase inhibitors have been published, substantial efforts have been made to understand the influence of tyrosinase inhibition on the viability of melanoma cells. Here, we assess the impact of two keto-derivatives: 2-acetyl-furan (F1), furfural-acetone (F2), and two carboxyl-derivatives: 2-furan-acrylic acid (F3), 5-methyl-2-furan-acrylic acid (F4), on the mushroom tyrosinase (mTYR) activity, by applying spectroscopic, kinetic and theoretical techniques. From an exploratory and theoretical point of view, results indicated that albeit all furans bind tightly to and inhibit mTYR very efficient, carboxyl-furan derivatives presented best inhibitory activities than keto- derivatives and performed the inhibition competitively and reversible. Moreover, we examined the influence of carboxyl derivative on the viability of melanoma cells. Results expose differential toxicity of these furan derivatives, which indicates a piece of evidence that furan inhibition activity may be related to its toxicity against B16F10 cells.


Asunto(s)
Antineoplásicos/farmacología , Inhibidores Enzimáticos/farmacología , Furanos/farmacología , Melanoma/patología , Monofenol Monooxigenasa/antagonistas & inhibidores , Agaricales/enzimología , Animales , Antineoplásicos/metabolismo , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Inhibidores Enzimáticos/metabolismo , Furanos/metabolismo , Humanos , Ratones , Simulación del Acoplamiento Molecular , Monofenol Monooxigenasa/química , Monofenol Monooxigenasa/metabolismo , Conformación Proteica
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