Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 5 de 5
Filter
1.
AAPS PharmSciTech ; 25(7): 196, 2024 Aug 22.
Article in English | MEDLINE | ID: mdl-39174848

ABSTRACT

In this study, N, N '-bis {4- [(α-L- rhamnosyloxy) benzyl]} thiourea (PG-1), a phenolic glycoside compound was purified from Moringa seed. The PG-1 has attracted extensive attention due to its anti-cancer, antioxidant, anti-inflammatory and hypoglycemic properties. However, some of its physicochemical properties such as oral bioavailability has not been studied. Herein, a highly purified PG-1 was extracted and incorporated in multiple layered liposomes (PG-1-L) to avoid its burst release and enhance oral bioavailability. After appropriate characterization, it was discovered that the obtained PG-1-L was stable, homogeneous and well dispersed with the average particle size being 89.26 ± 0.23 nm. Importantly, the in vitro release and in vivo oral bioavailability of PG-1-L were significantly improved compared with PG-1. In addition, MTT results showed that compared with the free PG-1, PG-1-L displayed obvious inhibitory effect on the HepG2 cells, while the inhibitory effect on healthy non-malignant 3T6 and LO-2 cells was not significant, indicating that PG-1-L had high safety. In conclusion, PG-1-L can be used as a promising delivery system and an ideal novel approach to improve the oral bioavailability and anticancer activity of PG-1.


Subject(s)
Biological Availability , Glycosides , Liposomes , Moringa oleifera , Phenols , Seeds , Moringa oleifera/chemistry , Seeds/chemistry , Humans , Glycosides/chemistry , Glycosides/administration & dosage , Glycosides/pharmacology , Glycosides/isolation & purification , Animals , Hep G2 Cells , Phenols/administration & dosage , Phenols/chemistry , Phenols/isolation & purification , Phenols/pharmacokinetics , Particle Size , Drug Delivery Systems/methods , Mice , Male , Rats , Administration, Oral , Chemistry, Pharmaceutical/methods , Rats, Sprague-Dawley
2.
Toxicol In Vitro ; 99: 105886, 2024 Aug.
Article in English | MEDLINE | ID: mdl-38945377

ABSTRACT

Bisphenol S (BPS) was introduced in many industrial and commercial applications as a presumed safer alternative to bisphenol A. However, concerns have been raised surrounding skin absorption and potential persistence of BPS and its related toxic effects in humans. A previous study revealed the likelihood of a reservoir building up in exposed skin. Here, we studied the interactions of BPS solubilized in acetone, ultrapure water, or artificial sebum with freshly excised human skin samples. In vitro tests were performed in static Franz diffusion cells, to explore reservoir and occlusion effects, absorption and metabolism. Most BPS passed through the skin without metabolization - <10% was recovered as glucuronide or sulfate conjugates. Importantly, a substantial amount of BPS persisted in the skin, especially in the stratum corneum. This reservoir could lead to prolonged diffusion into the body after surface cleaning. Occlusion, that may occur with protective clothing, amplified BPS absorption up to six-fold. These findings have implications for occupational settings, highlighting the persistence of BPS contamination even after washing the skin's surface and the need to ensure protective equipment is correctly maintained and used.


Subject(s)
Phenols , Skin Absorption , Skin , Sulfones , Humans , Phenols/pharmacokinetics , Phenols/toxicity , Skin/metabolism , Sulfones/pharmacokinetics , In Vitro Techniques , Female , Male , Adult , Middle Aged
3.
Braz. j. microbiol ; 49(3): 656-661, July-Sept. 2018. tab, graf
Article in English | LILACS | ID: biblio-951809

ABSTRACT

Abstract Hamelia patens, is a plant traditionally used to treat a variety of conditions among the Huastec people of Mexico. The objective of this study is to characterize the phenolic content and critically examine the antimicrobial activity of leaf extracts H. patens, obtained by maceration, Soxhlet and percolation, using ethanol as 70% solvent. Phenolic compounds are characterized by liquid chromatography, coupled to a High Resolution Mass Spectrometry, and the antimicrobial activity was studied from the inhibitory effect of each extract for Escherichia coli, Staphylococcus aureus, Salmonella typhi and S. paratyphi, and by the Minimum Bactericidal Concentration, the percentage of activity and the Index of Bacterial Susceptibility of each extract. The phenolic compound identified in different concentrations in the three extracts was epicatechin. The extracts obtained by the three methods had antimicrobial activity, however, there was no significant difference (p < 0.05) between the Minimum Bactericidal Concentration of the extracts obtained by maceration, percolation and Soxhlet. The results of this study contribute to the body of knowledge on the use of extracts in controlling microorganisms with natural antimicrobials.


Subject(s)
Phenols/isolation & purification , Phenols/pharmacokinetics , Plant Extracts/isolation & purification , Plant Extracts/pharmacokinetics , Hamelia/chemistry , Chemical Fractionation/methods , Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/pharmacology , Phenols/chemistry , Staphylococcus aureus/drug effects , Plant Extracts/chemistry , Microbial Sensitivity Tests , Escherichia coli/drug effects , Mexico , Anti-Bacterial Agents/chemistry
4.
Rev. chil. nutr ; 37(3): 377-385, Sept. 2010. tab
Article in Spanish | LILACS | ID: lil-577404

ABSTRACT

Consumption of fruit and vegetables has the potential to reduce non-transmissible diseases (NTD), such as cardiovascular diseases (CVD) and cancer, which are major public health concerns. Chile is a major apple producer and exporter in the world. Its production is concentrated in the sixth (O'Higgins) and seventh (Maule) regions of Central Chile. Phenolics and flavonoids are responsible for apple's high antioxidant activity. Many epidemiologic studies have shown that a diet rich in apples can reduce cardiovascular events (myocardial infarct and stroke) and some type of cancers. The mechanisms involved are not well understood. Nevertheless, antioxidants are key-players. Some of their in-vitro activities are inhibition of low-density lipoprotein (LDL) oxidation, cholesterol levels reduction, endothelium protection, reduction of neoplastic cells proliferation and apoptosis activation. Consequently, daily apple consumption campaigns in the country should be implemented, as well as funding research focused on molecular mechanisms involved in its antioxidant activity.


Las enfermedades no transmisibles (ENT), especialmente las cardiovasculares (ECV) y el cáncer, representan un grave problema de salud pública. Es conocido que el consumo de frutas y hortalizas disminuye el riesgo de sufrir dichas enfermedades. El manzano (Malus domestica Borkh.) se cultiva en Chile en una amplia zona geográfica, concentrándose principalmente en las regiones sexta y séptima. La actividad antioxidante de la manzana se debe principalmente a su contenido en fenoles y flavonoides. Varios estudios epidemiológicos han mostrado que el consumo de manzanas puede prevenir el desarrollo de ECV (infarto agudo de miocardio y enfermedad cerebro vascular) y ciertos tipos de cáncer. Los mecanismos por los cuales se producen dichos efectos, no están totalmente aclarados, sin embargo la participación de los antioxidantes es fundamental. Entre los principales hallazgos se han descrito, en relación a ECV: inhibición de la oxidación de low-density lipoprotein (LDL), disminución de colesterol total y protección de endotelio; y en relación a cáncer: disminución de la proliferación de células neoplásicas y activación de la apoptosis de las mismas. Debido al incuestionable efecto protector para la salud humana que presenta la ingesta de manzana, se deben impulsar estrategias que apunten a incentivar su consumo diario en el país. Asimismo, se deben seguir estudiando los principios activos y los mecanismos moleculares.


Subject(s)
Humans , Diet , Cardiovascular Diseases/prevention & control , Fruit/chemistry , Malus/chemistry , Neoplasms/prevention & control , Antioxidants , Cholesterol, LDL , Cardiovascular Diseases/epidemiology , Phenols/administration & dosage , Phenols/pharmacokinetics , Flavonoids/administration & dosage , Flavonoids/pharmacokinetics , Neoplasms/epidemiology , Cell Proliferation
5.
Invest. med. int ; 19(3): 123-7, nov. 1992. tab
Article in Spanish | LILACS | ID: lil-117798

ABSTRACT

En el estudio se valoró y ratificó la eficacia antiespasmódica-analgésica de los trifenoles en la dismenorrea mediante estudio comparativo doble ciego y randomizado, vs piroxicam en pacientes entre 18 y 35 años de edad seleccionadas en la consulta externa del Hospital General con manifestaciones bien definidas de disfunción uterina ocasionada por dismenorrea primaria y tratadas en forma ambulatoria a base exclusiva de trifenoles y piroxicam (cápsulas) con dosis promedio de 3 cápsulas de 20 mg al día por tres días y con seguimiento posterior por tres ciclos. El dolor para su estudio fue considerado como espástico (cólico) y marcado en una tabla como intenso, moderado, ligero y nulo, con localizacioón clásica en hipogastrio, valorado con escala visual del 1 al 10 como variable discontinua, con tabla comparativa en variable Método de Mann Whitney.


Subject(s)
Humans , Female , Adolescent , Adult , Dysmenorrhea/drug therapy , Phenols/pharmacokinetics , Phenols/therapeutic use , Piroxicam/pharmacokinetics , Piroxicam/therapeutic use
SELECTION OF CITATIONS
SEARCH DETAIL