RESUMEN
High-density poly(ethylene glycol) (PEG) molecules are grafted onto Si surfaces in a brush-like configuration. We demonstrate that this surface is an excellent substrate for oligonucleotide immobilization. p-Maleimidophenyl isocyanate is used as a heterobifunctional cross-linker to tether thiol-modified oligonucleotides to terminal OH groups on the PEG brush. This approach gives excellent immobilization specificity and low background. The immobilized oligonucleotides show high sensitivity for the detection of complementary targets.
Asunto(s)
Oligonucleótidos/química , Polietilenglicoles/química , Silicio/química , Secuencia de Bases , Reactivos de Enlaces Cruzados/química , Cianatos/química , Maleimidas/química , Microscopía Fluorescente , Hibridación de Ácido Nucleico , Sensibilidad y Especificidad , Espectrometría por Rayos X , Compuestos de Sulfhidrilo/química , Propiedades de Superficie , Xantenos/químicaRESUMEN
OBJECTIVE: To investigate the effects of musk-1, a glucoprotein component isolated from the water extract of musk, on some functions of rat polymorphonuclear leukocytes activated by IL-8 in vitro. METHOD: An in vitro incubation system was used. Superoxide anion production was determined by cytochrome C reduction. beta-glucuronidase and lysozyme release was quantitated by enzyme reactions in which phenolph-thaleinglucuronic acid and Micrococcus Lysodeikticus were as the substrates, respectively. RESULTS: In comparison with control, musk-1 at concentration 1-100 micrograms.ml-1 can increase superoxide anion production by 91.7%-291%, and decrease beta-glucuronidase and lysozyme release by 2.2%-58.1% and 3.9%-39.8%, respectively. CONCLUSION: Inhibition of lysosomel enzyme release might be considered as one of mechanisms of antiinflammatory action of musk.
Asunto(s)
Antiinflamatorios no Esteroideos/farmacología , Ácidos Grasos Monoinsaturados/farmacología , Glucuronidasa/metabolismo , Materia Medica/farmacología , Neutrófilos/metabolismo , Animales , Femenino , Masculino , Muramidasa/metabolismo , Oxígeno/metabolismo , Ratas , Ratas WistarRESUMEN
AIM: To study the protective effect of Gn-3 (a stilbene polymer isolated from Gnetum parvifolium) against liver injury induced by CCl4, N-acetyl-p-aminophenol (APAP) and Bacillus Calmette-Guerin (BCG) plus bacterial lipopolysaccharide (LPS) in mice. METHODS: The experimental model of liver injury were induced by 0.1% CCl4 i.p. (10 mL.kg-1.d-1 for 3d), APAP i.p. (150 mg.kg-1) or BCG (5 mg) plus LPS (7.5 micrograms) in mice. The levels of ALT in serum, MDA and GSH in liver tissues were detected. The histopathologic changes were observed by light microscope. RESULTS: Gn-3 was shown to markedly reduce the elevated serum ALT levels, liver tissue MDA and improve the histopathological changes in all the three experimental liver injury models. No effect of Gn-3 was observed on the liver GSH level in liver injury mice. CONCLUSION: Gn-3 was found to inhibit the development of liver injury caused by CCl4, APAP, or BCG plus LPS. This means that Gn-3 has liver protective effects.
Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas/patología , Hígado/patología , Sustancias Protectoras/farmacología , Estilbenos/farmacología , Acetaminofén , Alanina Transaminasa/sangre , Animales , Intoxicación por Tetracloruro de Carbono , Enfermedad Hepática Inducida por Sustancias y Drogas/metabolismo , Gnetum/química , Lipopolisacáridos , Hígado/metabolismo , Masculino , Malondialdehído/metabolismo , Ratones , Mycobacterium bovis , Plantas Medicinales/química , Distribución Aleatoria , Estilbenos/aislamiento & purificaciónRESUMEN
OBJECTIVE: To investigate the effects of Musk glucoprotein on platelet activating factor (PAF) production and the concentration of cytosolic free Ca2+ in polymorphonuclear leukocytes of rat. METHODS: An in vitro incubation system was used, production of PAF and activity of acetyl transferase were measured by isotope incorporation, the concentration of cytosolic free Ca2+ was quantitated using the fluorescent Ca2+ indicator Fura-2. RESULTS: Musk-1 at concentration of 1-100 micrograms.ml-1 can significantly inhibit production of PAF, activity of acetyl transferase and the increase of cytosolic Ca2+ concentration in polymorphonuclear leukocytes of rat. CONCLUSION: Part of mechanisms underlying antiinflammatory action of Musk-1 is through inhibiting the synthesis of PAF and the increase of cytosolic Ca2+ level.
Asunto(s)
Calcio/metabolismo , Materia Medica/farmacología , Neutrófilos/metabolismo , Factor de Activación Plaquetaria/biosíntesis , alfa-Macroglobulinas/farmacología , Acetiltransferasas/metabolismo , Animales , Separación Celular , Ácidos Grasos Monoinsaturados , Femenino , Masculino , Ratas , Ratas WistarRESUMEN
AIM: To investigate the effect of baicalin on liver microsomal cytochrome P450 system and the mechanism of liver protective action of baicalin. METHODS: Liver microsomal cytochrome P450, b5, aminopyrin N-demethylase (ADM), 7-ethoxycoumarin O-deethylase (ECD) and benzopyrene hydroxylase (AHH) activity were quantitated by UV chromatography. Activities of six cytochrome P450 isoforms were assayed with Western Blotting. RESULTS: Baicalin increased liver microsomal cytochrome. P450 level and ADM, ECD and AHH activity significantly. The three P450 isoforms, 1A1, 2B1 and 2C11, were also induced selectively by baicalin, but the b5 level, 3A2, 2D1 and 2E1 were not induced. CONCLUSION: Baicalin increases liver microsomal cytochrome P450 level and induces selectively 1A1, 2B1 and 2C11 of P450 isoforms in mice.
Asunto(s)
Sistema Enzimático del Citocromo P-450/metabolismo , Flavonoides/farmacología , Microsomas Hepáticos/efectos de los fármacos , Animales , Antioxidantes/farmacología , Flavonoides/aislamiento & purificación , Isoenzimas/metabolismo , Masculino , Ratones , Microsomas Hepáticos/enzimología , Plantas Medicinales/química , Distribución Aleatoria , Scutellaria/químicaRESUMEN
The effect of Glycyrrhiza uralensis Fisch (GRZ) aqueous extract and one of its active principles Glycyrrhetinic acid (GRT) on hepatic cytochrome P450 in mice were investigated. Oral administration of GRZ at 10 g/kg/d or GRT at 50 mg/kg/d for 7 days was found to increase the P450 contents up to 4.6 fold compared with the controls. The activities of aryl hydrocarbon hydroxylase (AHH, 3.1 and 3.3 fold), aminopyrine N-demethylase (ADM, 4.2 and 3.2 folds), and 7-ethoxycumarin O-deethylase (ECOD, 2.8 and 2.5 fold) were also shown to be increased. Western blot analysis showed that the subtypes of P450 isoforms induced selectively by GRZ and GRT included CYP1A1 (1.8 and 1.5 fold over that of the control, respectively), CYP2B1 (both 1.3 fold), and CYP2C11 (3.2 and 3.0 fold). Moreover, significant positive correlation between the P450 content or the isoforms and the corresponding enzyme activities mentioned above was observed.
Asunto(s)
Sistema Enzimático del Citocromo P-450/biosíntesis , Ácido Glicirretínico/farmacología , Isoenzimas/biosíntesis , Microsomas Hepáticos/enzimología , Plantas Medicinales , Animales , Western Blotting , Inducción Enzimática , Masculino , Ratones , Microsomas Hepáticos/efectos de los fármacosRESUMEN
In the present investigation, interleukin 6 (IL-6) activity in the supernatant of cultured mouse peritoneal macrophages was monitored using a sensitive bioassay involving the IL-6-dependent murine hybridoma B9 cell line. The effects of resveratrol on Il-6 release by mouse peritoneal macrophages stimulated with calcium ionophore A23187 and fMLP were explored. Resveratrol, at a concentration range from 5 x 10(-6) to 4 x 10(-5) mol.l-1, was found to dose-dependently inhibit IL-6 release by cultured macrophages induced by A23187 and fMLP, and showed no direct cytotoxic effect, but induced proliferation of cultured mouse thymus cells. Resveratrol, at a concentration range from 10(-8) to 10(-5) mol.l-1, was shown to dose-dependently inhibit calcium ion influx into the cells with the stimulation of fMLP (10(-6) mol.l-1). These results suggest that the blocking of calcium ion influx into cells by reveratrol is one of the possible mechanisms of the IL-6 biosynthesis inhibitory action of resveratrol.
Asunto(s)
Interleucina-6/antagonistas & inhibidores , Macrófagos Peritoneales/efectos de los fármacos , Estilbenos/farmacología , Animales , Calcimicina/farmacología , Calcio/metabolismo , Células Cultivadas , Femenino , Interleucina-6/metabolismo , Transporte Iónico , Activación de Macrófagos/efectos de los fármacos , Macrófagos Peritoneales/metabolismo , Ratones , Ratones Endogámicos C57BL , N-Formilmetionina Leucil-Fenilalanina/farmacología , Neutrófilos/efectos de los fármacos , Neutrófilos/metabolismo , Ratas , Resveratrol , Timo/citología , Timo/efectos de los fármacos , Timo/metabolismoRESUMEN
Both bear and pig bile solutions were shown to have anti-inflammatory, anticonvulsion and analgesic effects, and also to prolong the survival time of mice in hypoxic conditions. It is possible that pig gall bladders could be developed as an alternative to bear gall bladders for uses in certain prescriptions of Chinese medicine.
Asunto(s)
Analgésicos/farmacología , Antiinflamatorios/farmacología , Anticonvulsivantes/farmacología , Bilis/química , Vesícula Biliar/metabolismo , Acetatos/toxicidad , Ácido Acético , Analgésicos/uso terapéutico , Animales , Antiinflamatorios/uso terapéutico , Anticonvulsivantes/uso terapéutico , Ácidos y Sales Biliares/farmacología , Ácidos y Sales Biliares/uso terapéutico , Convulsivantes/toxicidad , Aceite de Crotón/toxicidad , Edema/inducido químicamente , Edema/tratamiento farmacológico , Femenino , Hipoxia/tratamiento farmacológico , Hipoxia/mortalidad , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Irritantes/toxicidad , Masculino , Medicina Tradicional China , Ratones , Dolor/tratamiento farmacológico , Pentilenotetrazol/toxicidad , Convulsiones/inducido químicamente , Convulsiones/tratamiento farmacológico , Porcinos , UrsidaeRESUMEN
Shikonin is one of the active components isolated from the dry root of Arnebia euchroma (Royle) Johnst (AERJ). It has been shown to have anti inflammatory activity on formaldehyde induced paw swelling in rats. Preparations of AERJ has been used clinically in curing phlebitis and vascular purpura. In the present study, sc administered shikonin was shown to have significant inhibitory effects on ear edema induced by croton oil in mice and paw swelling induced by yeast in rats. In order to investigate the influence of shikonin on biosynthesis of LTB4 and 5-HETE, an in vitro leukocyte incubation system was adopted. The results showed that shikonin has fairly strong inhibitory effects on LTB4 and 5-HETE biosynthesis. Its effects and concentrations fit a positive relationship within the range of 10(-7)-10(-4) mol.L-1. The equations of inhibition (Y) versus concentration (X, LogC) obtained by linear regression were Y = 166 + 18.7X (r = 0.9319) for LTB4 and Y = 173 + 18.7X (r = 0.9856) for 5-HETE. The IC50 were 6.2 x 10(-7) and 2.6 x 10(-7) mol.L-1, respectively. The results also indicate that natural shikonin derivatives have similar inhibitory effects on LTB4 biosynthesis. These results suggest that inhibition of LTB4 and 5-HETE may play a major role in the mechanism of anti inflammatory effects of shikonin.
Asunto(s)
Antiinflamatorios no Esteroideos/farmacología , Leucotrieno B4/biosíntesis , Naftoquinonas/farmacología , Animales , Antiinflamatorios no Esteroideos/uso terapéutico , Aceite de Crotón , Edema/inducido químicamente , Edema/tratamiento farmacológico , Ácidos Hidroxieicosatetraenoicos/biosíntesis , Masculino , Ratones , Naftoquinonas/uso terapéutico , Ratas , Ratas WistarRESUMEN
Tremulacin was shown to inhibit carrageenan-induced paw edema in rats and croton oil-induced ear edema in mice. It was also found to inhibit peritoneal leucocyte migration in rats and acetic acid-induced writhing responses in mice. Experiments with isolated longitudinal muscle strips of sensitized guinea pig ileum showed that tremulacin decreased the biosynthesis of Slow Reaction Substance of Anaphylaxis. Tremulacin exerted inhibitory effects on leukotriene B4 biosynthesis in intrapleural leucocytes. These results suggest that the mechanism of antiinflammatory actions of tremulacin is relevant to inhibition of 5-lipoxygenase activity. This is quite different from non-steroid antiinflammatory drugs, such as aspirin, which inhibits prostaglandin synthesis and being a cyclooxygenase inhibitor.
RESUMEN
Experiments showed that in patients of renal yin deficiency who took orally Liuwei Dihuang granules for 4 weeks, the contents of cAMP, E2, Zn and Cu were found mankedly lower, but the contents of T mankedly higher than before using the drugs. This indicates that the granules are equally effective as pills and decoction.
Asunto(s)
AMP Cíclico/sangre , Medicamentos Herbarios Chinos/administración & dosificación , Enfermedades Renales/sangre , Testosterona/sangre , Deficiencia Yin/sangre , Adulto , Anciano , Cobre/sangre , Estradiol/sangre , Femenino , Humanos , Enfermedades Renales/tratamiento farmacológico , Masculino , Persona de Mediana Edad , Deficiencia Yin/tratamiento farmacológico , Zinc/sangreRESUMEN
The immunosuppressive effect of cultured Cordyceps sinensis (Bei Lin Capsule) was studied in vitro and in vivo. When the drug was added from 0.6 mg/ml to 5 mg/ml a significant dose-dependent inhibition effect was shown in the following immune reactions of mice (P less than 0.05-0.01): phagocytic function of peripheral blood leucocytes assayed by chemiluminescence; mitogenic response of spleen lymphocytes to Con A; mixed lymphocyte culture and LPS induced interleukin-1 release of macrophages. The survival rate of mice spleen lymphocytes cultured with Cordyceps sinensis 5 mg/ml in 37 degrees C 5% CO2 for 5 days was more than 80%. Cordyceps sinensis 4 g/kg daily significantly prolonged the mice skin allograft survival time (12.7 +/- 2.2 days v.s. 8.3 +/- 0.7 days in the control, P less than 0.01) and its immunosuppressive effect was close to that of Cyclosporin A 5 mg/kg daily on skin allograft.
Asunto(s)
Medicamentos Herbarios Chinos/farmacología , Inmunosupresores , Activación de Linfocitos/efectos de los fármacos , Fagocitosis/efectos de los fármacos , Plantas Medicinales/crecimiento & desarrollo , Animales , Supervivencia de Injerto/efectos de los fármacos , Inmunidad Celular/efectos de los fármacos , Interleucina-1/biosíntesis , Macrófagos/inmunología , Ratones , Ratones Endogámicos BALB C , Ratones Endogámicos C57BL , Ratones Endogámicos DBARESUMEN
The water soluble fraction (WSF) of musk was shown to decrease the vitamin C content of the adrenal gland in mice and to increase plasma corticosterone levels in rats. The anti-inflammatory effect of WSF was not affected by hypophysectomy in the rat but was completely abolished by adrenalectomy in mice, indicating that the adrenal gland may play an important role in mediating the anti-inflammatory effect of musk. The WSF was capable of inhibiting ADP or collagen-induced platelet aggregation in rats. In the meantime, there was a potentiation of immunohemolysis in mice and an elevation of the plasma level of cAMP in rats. The implications of these changes in the anti-inflammatory effects of musk are discussed.
Asunto(s)
Antiinflamatorios , Ácidos Grasos Monoinsaturados/farmacología , Glándulas Suprarrenales/metabolismo , Animales , Artritis Experimental/tratamiento farmacológico , Ácido Ascórbico/metabolismo , Ácidos Grasos Monoinsaturados/uso terapéutico , Masculino , Ratones , Ratas , Ratas EndogámicasRESUMEN
Lei Wan, Poliporus mylittae Cook et Mass (Omphalia lapidescens Schraet) is a kind of fungus used in traditional Chinese medicine, as an anthelminthic. From Lei Wan, an active component designated as S-4001 had been isolated. Preliminary results indicate that S-4001 belongs to D, beta, 1-3 glucan with some 1-6 linkages. After administration of S-4001, significant antiinflammatory activity was found in various experimental animal models, including croton oil induced ear edema in mice and agar or yeast induced ankle swelling in rats. An inhibitory action on leucocyte migration induced by intraperitoneal injection of CMC in rats was also observed. The plasma content of corticosterone was significantly increased, but the content of ascorbic acid in the adrenals did not change in rats given S-4001. Apart from these actions, S-4001 showed a number of immunostimulating actions such as increasing the clearance of Congo red from mice blood and potentiating the immunohemolysis reaction in 615 mice.