Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 3 de 3
Filtrar
Más filtros












Base de datos
Intervalo de año de publicación
1.
Toxicol Appl Pharmacol ; 307: 130-137, 2016 09 15.
Artículo en Inglés | MEDLINE | ID: mdl-27495897

RESUMEN

The scarcity of studies on boron containing compounds (BCC) in the medicinal field is gradually being remedied. Efforts have been made to explore the effects of BCCs due to the properties that boron confers to molecules. Research has shown that the safety of some BCCs is similar to that found for boron-free compounds (judging from the acute toxicological evaluation). However, it has been observed that the administration of 3-thienylboronic acid (3TB) induced motor disruption in CD1 mice. In the current contribution we studied in deeper form the disruption of motor performance produced by the intraperitoneal administration of 3TB in mice from two strains (CD1 and C57BL6). Disruption of motor activity was dependent not only on the dose of 3TB administered, but also on the DMSO concentration in the vehicle. The ability of 3TB to enter the Central Nervous System (CNS) was evidenced by Raman spectroscopy as well as morphological effects on the CNS, such as loss of neurons yielding biased injury to the substantia nigra and striatum at doses ≥200mg/kg, and involving granular cell damage at doses of 400mg/kg but less injury in the motor cortex. Our work acquaints about the use of this compound in drug design, but the interesting profile as neurotoxic agent invite us to study it regarding the damage on the motor system.


Asunto(s)
Ácidos Borónicos/toxicidad , Encéfalo/efectos de los fármacos , Animales , Encéfalo/metabolismo , Encéfalo/patología , Dimetilsulfóxido/toxicidad , Masculino , Ratones Endogámicos C57BL , Actividad Motora/efectos de los fármacos , Neuronas/efectos de los fármacos , Neuronas/patología , Pruebas de Toxicidad Aguda , Temblor/inducido químicamente
2.
Toxicol Lett ; 258: 115-125, 2016 Sep 06.
Artículo en Inglés | MEDLINE | ID: mdl-27329537

RESUMEN

Boron is ubiquitous in nature, being an essential element of diverse cells. As a result, humans have had contact with boron containing compounds (BCCs) for a long time. During the 20th century, BCCs were developed as antiseptics, antibiotics, cosmetics and insecticides. Boric acid was freely used in the nosocomial environment as an antiseptic and sedative salt, leading to the death of patients and an important discovery about its critical toxicology for humans. Since then the many toxicological studies done in relation to BCCs have helped to establish the proper limits of their use. During the last 15 years, there has been a boom of research on the design and use of new, potent and efficient boron containing drugs, finding that the addition of boron to some known drugs increases their affinity and selectivity. This mini-review summarizes two aspects of BCCs: toxicological data found with experimental models, and the scarce but increasing data about the structure-activity relationship for toxicity and therapeutic use. As is the case with boron-free compounds, the biological activity of BCCs is related to their chemical structure. We discuss the use of new technology to discover potent and efficient BCCs for medicinal therapy by avoiding toxic effects.


Asunto(s)
Compuestos de Boro/toxicidad , Contaminantes Ambientales/toxicidad , Animales , Compuestos de Boro/efectos adversos , Compuestos de Boro/química , Compuestos de Boro/uso terapéutico , Diseño de Fármacos , Drogas en Investigación/efectos adversos , Drogas en Investigación/química , Drogas en Investigación/uso terapéutico , Contaminantes Ambientales/química , Humanos , Estructura Molecular , Mutágenos/química , Mutágenos/toxicidad , Relación Estructura-Actividad , Pruebas de Toxicidad Aguda , Pruebas de Toxicidad Crónica
3.
Mini Rev Med Chem ; 11(12): 1031-8, 2011 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-21861808

RESUMEN

The ligand-gated ion channels and seven transmembrane domain receptors are the greatest families of transmembrane receptors (TMR) expressed in mammalians and the major target of current available drugs. Recently, boron containing compounds (BCC) have shown capability of acting as ligands on these targets. This mini-review is focused on the description of BCC that target TMR which were evaluated under experimental models. The results in experimental models are related with the theoretical interaction studies of these ligands on the target proteins as 3D-models in order to explore the biological effects of BCC in molecular detail.


Asunto(s)
Compuestos de Boro/farmacología , Receptores Ionotrópicos de Glutamato/antagonistas & inhibidores , Receptores de Glutamato Metabotrópico/antagonistas & inhibidores , Animales , Compuestos de Boro/síntesis química , Compuestos de Boro/química , Humanos , Relación Estructura-Actividad
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA
...