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Métodos Terapéuticos y Terapias MTCI
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1.
J Biomed Sci ; 24(1): 18, 2017 Feb 28.
Artículo en Inglés | MEDLINE | ID: mdl-28245819

RESUMEN

BACKGROUND: Sarcosine, a glycine transporter type 1 inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site, potentiates NMDA receptor function. Structurally similar to sarcosine, N,N-dimethylglycine (DMG) is also N-methyl glycine-derivative amino acid and commonly used as a dietary supplement. The present study compared the effects of sarcosine and DMG on NMDA receptor-mediated excitatory field potentials (EFPs) in mouse medial prefrontal cortex brain slices using a multi-electrode array system. RESULTS: Glycine, sarcosine and DMG alone did not alter the NMDA receptor-mediated EFPs, but in combination with glutamate, glycine and its N-methyl derivatives significantly increased the frequency and amplitude of EFPs. The enhancing effects of glycine analogs in combination with glutamate on EFPs were remarkably reduced by the glycine binding site antagonist 7-chlorokynurenate (7-CK). However, DMG, but not sarcosine, reduced the frequency and amplitude of EFPs elicited by co-application of glutamate plus glycine. D-cycloserine, a partial agonist at the glycine binding site on NMDA receptors, affected EFPs in a similar manner to DMG. Furthermore, DMG, but not sarcosine, reduced the frequencies and amplitudes of EFPs elicited by glutamate plus D-serine, another endogenous ligand for glycine binding site. CONCLUSIONS: These findings suggest that sarcosine acts as a full agonist, yet DMG is a partial agonist at glycine binding site of NMDA receptors. The molecular docking analysis indicated that the interactions of glycine, sarcosine, and DMG to NMDA receptors are highly similar, supporting that the glycine binding site of NMDA receptors is a critical target site for sarcosine and DMG.


Asunto(s)
Potenciales de la Membrana/efectos de los fármacos , Receptores de N-Metil-D-Aspartato/agonistas , Receptores de N-Metil-D-Aspartato/metabolismo , Sarcosina/análogos & derivados , Sarcosina/farmacología , Animales , Masculino , Ratones , Ratones Endogámicos ICR
2.
PLoS One ; 9(7): e96006, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24984066

RESUMEN

Deep-sea water (DSW), which is rich in micronutrients and minerals and with antioxidant and anti-inflammatory qualities, may be developed as marine drugs to provide intestinal protection against duodenal ulcers. We determined several characteristics in the modified DSW. We explored duodenal pressure, oxygenation, microvascular blood flow, and changes in pH and oxidative redox potential (ORP) values within the stomach and duodenum in response to tap water (TW, hardness: 2.48 ppm), DSW600 (hardness: 600 ppm), and DSW1200 (hardness: 1200 ppm) in Wistar rats and analyzed oxidative stress and apoptosis gene expressions by cDNA and RNA microarrays in the duodenal epithelium. We compared the effects of drinking DSW, MgCl2, and selenium water on duodenal ulcers using pathologic scoring, immunohistochemical analysis, and Western blotting. Our results showed DSW has a higher pH value, lower ORP value, higher scavenging H2O2 and HOCl activity, higher Mg2+ concentrations, and micronutrients selenium compared with TW samples. Water infusion significantly increased intestinal pressure, O2 levels, and microvascular blood flow in DSW and TW groups. Microarray showed DSW600, DSW1200, selenium water upregulated antioxidant and anti-apoptotic genes and downregulated pro-apoptotic gene expression compared with the TW group. Drinking DSW600, DSW1200, and selenium water but not Mg2+ water significantly enhanced Bcl-2 and thioredoxin reductase 1 expression. Bax/Bcl-2/caspase 3/poly-(ADP-ribose)-polymerase signaling was activated during the pathogenesis of duodenal ulceration. DSW drinking reduced ulcer area as well as apoptotic signaling in acetic acid-induced duodenal ulcers. DSW, which contains selenium, provides intestinal protection against duodenal ulcers through the upregulation of Bcl-2 and thioredoxin reductase 1.


Asunto(s)
Úlcera Duodenal/metabolismo , Úlcera Duodenal/prevención & control , Proteínas Proto-Oncogénicas c-bcl-2/biosíntesis , Agua de Mar/química , Selenio , Tiorredoxina Reductasa 1/biosíntesis , Regulación hacia Arriba/efectos de los fármacos , Animales , Modelos Animales de Enfermedad , Úlcera Duodenal/patología , Femenino , Ratas , Ratas Wistar , Selenio/química , Selenio/farmacología
3.
Life Sci ; 81(13): 1071-8, 2007 Sep 08.
Artículo en Inglés | MEDLINE | ID: mdl-17826802

RESUMEN

The antinociceptive actions of honokiol and magnolol, two major bioactive constituents of the bark of Magnolia officinalis, were evaluated using tail-flick, hot-plate and formalin tests in mice. The effects of honokiol and magnolol on the formalin-induced c-Fos expression in the spinal cord dorsal horn as well as motor coordination and cognitive function were examined. Data showed that honokiol and magnolol did not produce analgesia in tail-flick, hot-plate paw-shaking and neurogenic phase of the overt nociception induced by intraplantar injection of formalin. However, honokiol and magnolol reduced the inflammatory phase of formalin-induced licking response. Consistently, honokiol and magnolol significantly decreased formalin-induced c-Fos protein expression in superficial (I-II) laminae of the L4-L5 lumbar dorsal horn. However, honokiol and magnolol did not elicit motor incoordination and memory dysfunction at doses higher than the analgesic dose. These results demonstrate that honokiol and magnolol effectively alleviate the formalin-induced inflammatory pain without motor and cognitive side effects, suggesting their therapeutic potential in the treatment of inflammatory pain.


Asunto(s)
Antiinflamatorios no Esteroideos/farmacología , Compuestos de Bifenilo/farmacología , Depresores del Sistema Nervioso Central/farmacología , Lignanos/farmacología , Dolor/tratamiento farmacológico , Animales , Antiinflamatorios no Esteroideos/efectos adversos , Antiinflamatorios no Esteroideos/química , Compuestos de Bifenilo/efectos adversos , Compuestos de Bifenilo/química , Depresores del Sistema Nervioso Central/efectos adversos , Depresores del Sistema Nervioso Central/química , Modelos Animales de Enfermedad , Evaluación Preclínica de Medicamentos , Fijadores/toxicidad , Formaldehído/toxicidad , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Lignanos/efectos adversos , Lignanos/química , Región Lumbosacra , Magnolia/química , Memoria/efectos de los fármacos , Ratones , Dolor/inducido químicamente , Dolor/metabolismo , Células del Asta Posterior/metabolismo , Células del Asta Posterior/patología , Proteínas Proto-Oncogénicas c-fos/biosíntesis
4.
Planta Med ; 69(6): 532-6, 2003 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-12865972

RESUMEN

Magnolol and honokiol are the two major phenolic constituents of the plant medicine "Houpo" ( Magnolia obovata), which is used in the treatment of chest tightness and asthma. The aim of this study was to investigate the influence of magnolol and honokiol on smooth muscle tone in porcine trachea. Magnolol and honokiol (0.1 - 100 microM) inhibited carbachol- and high K +-induced muscle contractions in a concentration-dependent fashion, but did not affect basal muscle tension. After washout of these pretreatments, carbachol- and high K +-evoked muscle contractions were still abolished, suggesting that the inhibition was irreversible. Magnolol and honokiol also concentration-dependently decreased the Ca 2+-dependent muscle contraction induced by high K + depolarization. Ca 2+ channel antagonists attenuated carbachol-induced muscular response by approximately 30 %, but did not further potentiate the inhibitory actions of magnolol and honokiol on muscle contraction. However, the inhibitory effects of magnolol and honokiol on carbachol-evoked muscular contractile response were partially reversed after removal of Ca 2+ channel antagonist pretreatment. Alternatively, caffeine-elicited muscle contractions were not altered by magnolol, honokiol, and verapamil. In conclusion, the relaxant effects of magnolol and honokiol on porcine tracheal smooth muscle suggest an association with the blockade of Ca 2+ influx through voltage-operated Ca 2+ channels instead of Ca 2+ release from intracellular Ca 2+ stores. The magnolol- and honokiol-induced inhibitions on tracheal smooth muscle contraction may be relevant to the claimed therapeutic effects of the extract from magnolia bark and contribute to their pharmacological effects by acting as anti-asthmatic agents.


Asunto(s)
Compuestos de Bifenilo/farmacología , Broncodilatadores/farmacología , Lignanos , Magnolia , Contracción Muscular/efectos de los fármacos , Fitoterapia , Tráquea/efectos de los fármacos , Animales , Asma/tratamiento farmacológico , Compuestos de Bifenilo/administración & dosificación , Compuestos de Bifenilo/uso terapéutico , Broncodilatadores/administración & dosificación , Broncodilatadores/uso terapéutico , Calcio/metabolismo , Carbacol , Relación Dosis-Respuesta a Droga , Masculino , Músculo Liso/efectos de los fármacos , Cloruro de Potasio , Porcinos , Verapamilo/farmacología
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