RESUMEN
BACKGROUND: The present study aimed to compare the intravenous bolus effect of oxycodone and fentanyl on hemodynamic response after endotracheal intubation and postoperative pain in patients undergoing closed reduction of nasal bone fracture. METHODS: In this prospective randomized double-blinded study, 64 patients undergoing closed reduction of nasal bone fracture were randomized into one of two groups: the fentanyl group (Group F) or the oxycodone group (Group O). Each drug (fentanyl 2 mcg/kg in Group F and oxycodone 0.2 mg/kg in Group O) was administered prior to the induction of general anesthesia. Hemodynamic changes after endotracheal intubation and postoperative pain were then measured in both groups. RESULTS: There was no significant difference in the change in mean arterial pressure and heart rate between pre-induction and post-intubation in both Groups F and O (P > 0.05). Postoperative pain in Group O was milder than that in Group F (P < 0.001); however, time to awakening from the end of operation was shorter in Group F (P = 0.012). CONCLUSION: In patients undergoing closed reduction of nasal bone fracture, oxycodone attenuates hemodynamic response to endotracheal intubation similar to fentanyl. However, oxycodone is more effective than fentanyl in improving postoperative pain. TRIAL REGISTRATION: Clinical Research Information Service (Trial registry number: KCT0001153 ) on 3 July, 2014.
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Fentanilo/uso terapéutico , Hemodinámica/efectos de los fármacos , Intubación Intratraqueal/métodos , Oxicodona/uso terapéutico , Dolor Postoperatorio/tratamiento farmacológico , Adulto , Analgésicos Opioides/uso terapéutico , Anestesia General/métodos , Femenino , Fracturas Óseas/tratamiento farmacológico , Fracturas Óseas/cirugía , Humanos , Masculino , Adulto JovenRESUMEN
Aldose reductase (AR) inhibitors have considerable therapeutic potential against diabetic complications and do not increase the risk of hypoglycemia. Through bioassay-guided fractionation of the 70% acetone extract obtained from Paulownia coreana seeds, phenylpropanoid glycosides (compounds 1-4) and 5 phenolic compounds were isolated (compounds 5-9). Their structures were determined on the basis of spectroscopic analysis and comparison with reported data. All the isolates were subjected to in vitro bioassays to evaluate their inhibitory activities against recombinant human aldose reductase (rhAR) and sorbitol formation in human erythrocytes. Phenylethanoid glycosides showed more effective than the phenolic compounds in inhibiting rhAR. Among the compounds, isocampneoside II (3) was found to significantly inhibit rhAR with an IC(50) value of 9.72 µM. In kinetic analyses performed using Lineweaver-Burk plots of 1/velocity and 1/concentration of substrate, isocampneoside II (3) showed uncompetitive inhibition against rhAR. Furthermore, it inhibited sorbitol formation in a rat lens incubated with a high concentration of glucose; this finding indicated that isocampneoside II (3) may effectively prevent osmotic stress in hyperglycemia. Thus, the P. coreana-derived phenylethanoid glycoside isocampneoside II (3) may have a potential therapeutics against diabetic complications.
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Aldehído Reductasa/antagonistas & inhibidores , Glicósidos/farmacología , Semillas/química , Animales , Eritrocitos/efectos de los fármacos , Eritrocitos/enzimología , Glicósidos/química , Humanos , Cinética , Cristalino/efectos de los fármacos , Cristalino/metabolismo , Masculino , Estructura Molecular , Ratas , Sorbitol/metabolismoRESUMEN
INTRODUCTION: Isoflavonoids from Belamcanda chinensis are known to have a number of physiological benefits including anti-inflammatory, anti-angiogenic and anti-mutagenic properties. However, there have been no reports on the effective isolation and purification of isoflavonoids from B. chinensis. OBJECTIVE: To develop an efficient method for the preparative isolation and purification of isoflavones from B. chinensis by high-speed counter-current chromatography (HSCCC). METHODOLOGY: A two-step HSCCC isolation method was developed using solvent system of n-hexane-ethyl acetate-2-propanol-methanol-water (5:6:2:3.5:6, v/v) and of ethyl acetate-methanol-water (10:2:9, v/v). FLASH purification system (45% methanol, isocratic) was also used for further purification. The purities and chemical structures of the isolated compounds were determined by high-performance liquid chromatography-photodiode array detection (HPLC-PDA), electrospray ionisation-mass spectrometry (ESI-MS), ¹H- and ¹³C-nuclear magnetic resonance spectrometry (NMR) and nuclear overhauser enhancement (NOE). RESULTS: HSCCC was successfully used for the preparative separation and purification of seven isoflavones, including tectoridin (145.4 mg, 97.5%), iridin (77.9 mg, 94.0%), irilin D (42.0 mg, 92.0%), tectorigenin (294.1 mg, 98.6%), iristectorigenin A (86.8 mg, 93.4%), irigenin (141.8 mg, 95.8%) and irisflorentin (73.4 mg, 94.7%) from the rhizomes of B. chinensis. CONCLUSION: Two isoflavone glycosides and five isoflavone derivatives were successfully isolated and purified from the crude methanol extract of dried rhizomes of the B. chinensis by HSCCC.
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Glicósidos/aislamiento & purificación , Iridaceae/química , Isoflavonas/aislamiento & purificación , Cromatografía Líquida de Alta Presión/métodos , Distribución en Contracorriente/métodos , Glicósidos/química , Isoflavonas/química , Resonancia Magnética Nuclear Biomolecular , Rizoma/química , Espectrometría de Masa por Ionización de Electrospray , Espectrofotometría UltravioletaRESUMEN
We evaluated the inhibitory effects of components from the root of Glycyrrhiza uralensis (G. uralensis) on aldose reductase (AR) and sorbitol formation in rat lenses with high levels of glucose as part of our ongoing search of natural sources for therapeutic and preventive agents for diabetic complications. In order to identify the bioactive components of G. uralensis, 5 prenylated flavonoids (semilicoisoflavone B, 7-O-methylluteone, dehydroglyasperin C, dehydroglyasperin D, and isoangustone A), three flavonoids (liquiritigenin, isoliquiritigenin, and licochalcone A), and two triterpenoids (glycyrrhizin and glycyrrhetinic acid) were isolated; their chemical structures were then elucidated on the basis of spectroscopic evidence and comparison with published data. The anti-diabetic complication activities of 10 G. uralensis-derived components were investigated via inhibitory assays using rat lens AR (rAR) and human recombinant AR (rhAR). From the 10 isolated compounds, semilicoisoflavone B showed the most potent inhibition, with the IC(50) values of rAR and rhAR at 1.8 and 10.6microM, respectively. In the kinetic analyses using Lineweaver.Burk plots of 1/velocity and 1/concentration of substrate, semilicoisoflavone B showed noncompetitive inhibition against rhAR. The results clearly indicated that the presence of a gamma,gamma-dimethylchromene ring is partly responsible for the AR inhibitory activity of isoprenoid-type flavonoids. Further, semilicoisoflavone B inhibited sorbitol formation of rat lens incubated with a high concentration of glucose, indicating that this compound may be effective for preventing osmotic stress in hyperglycemia.
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Aldehído Reductasa/antagonistas & inhibidores , Complicaciones de la Diabetes/tratamiento farmacológico , Inhibidores Enzimáticos/farmacología , Flavonoides/farmacología , Glycyrrhiza uralensis/química , Cristalino/efectos de los fármacos , Extractos Vegetales/farmacología , Sorbitol/metabolismo , Animales , Complicaciones de la Diabetes/metabolismo , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/aislamiento & purificación , Flavonoides/química , Flavonoides/aislamiento & purificación , Glucosa/metabolismo , Humanos , Cristalino/metabolismo , Masculino , Estructura Molecular , Presión Osmótica/efectos de los fármacos , Fitoterapia , Extractos Vegetales/química , Ratas , Ratas Wistar , Proteínas Recombinantes , Rizoma , Triterpenos/química , Triterpenos/aislamiento & purificación , Triterpenos/farmacologíaRESUMEN
This study employed the online HPLC-2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonate radical cation (ABTS(+*)) bioassay to rapidly determine antioxidant compounds occurring in the licorice extract of Glycyrrhiza uralensis. The negative peaks of the ABTS(+*) radical scavenging detection system, which indicated the presence of antioxidant activity, were monitored by measuring the decrease in absorbance at 734 nm. The ABTS(+)-based antioxidant activity profile showed that three peaks exhibited antioxidant activity, and then the high-speed counter-current chromatography technique of preparative scale was successfully applied to separate the three peaks I-III in one step from the licorice extract. The high-speed counter-current chromatography was performed using a two-phase solvent system composed of n-hexane-ethyl acetate-methanol-water (6.5:5.5:6:4, v/v). Yields of the three peaks, dehydroglyasperin C (I, 95.1% purity), dehydroglyasperin D (II, 96.2% purity), and isoangustone A (III, 99.5% purity), obtained were 10.33, 10.43, and 6.7% respectively. Chemical structures of the purified dehydroglyasperin C (I), dehydroglyasperin D (II), and isoangustone A (III) were identified by ESI-MS and (1)H- and (13)C-NMR analysis.
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Antioxidantes/análisis , Benzopiranos/análisis , Flavonoides/análisis , Glycyrrhiza/química , Isoflavonas/análisis , Antioxidantes/química , Benzopiranos/química , Cromatografía Líquida de Alta Presión , Flavonoides/química , Isoflavonas/química , Estructura Molecular , Factores de TiempoRESUMEN
RATIONALE: Neuropathy secondary to diabetes mellitus often does not respond well to conventional therapy. Scrambler therapy may be an alternative treatment for otherwise intractable neuropathy. PATIENT CONCERNS: A 45-year-old female complained of bilateral plantar foot pain. She had been treated for diabetes mellitus for 5 years. Oral analgesics did not resolve her pain. Even nerve block therapy did not adequately relieve her pain. DIAGNOSES: Diabetic peripheral neuropathy. INTERVENTION: Scrambler therapy. OUTCOME: Pain reduction; the treatment effect was based around the location of the scrambler patch. LESSONS: Scrambler therapy is effective for the treatment of diabetic peripheral neuropathy. Moreover, effective pain management can be achieved for patients who complain of general pain of the sole, including the toe, by attaching scrambler patches around the ankle.
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Neuropatías Diabéticas/terapia , Pie/inervación , Manejo del Dolor/instrumentación , Dolor/etiología , Complicaciones de la Diabetes/epidemiología , Terapia por Estimulación Eléctrica/métodos , Femenino , Pie/patología , Humanos , Persona de Mediana Edad , Dolor/diagnóstico , Manejo del Dolor/métodos , Dimensión del Dolor/psicología , Resultado del TratamientoRESUMEN
The extract of the root of Acanthopanax chiisanensis Nakai is used for the treatment of inflammation. To analyse the action mechanism of this extract, the effect of hyperin (quercetin-3-O-beta-d-galactose) isolated from the ethyl acetate fraction of the root of A. chiisanensis on nitrite production and induction of inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS, 1 microg/mL)-stimulated rat peritoneal macrophages were examined. The effect of the structurally related compounds, isoquercitrin (quercetin-3-O-beta-d-glucose) and quercetin (an aglycone of the two compounds) isolated from the extract of the leaves of Vaccinium koreanum Nakai was also examined to compare the effect. It was shown that hyperin inhibited the LPS-induced iNOS expression and nitrite production. Of the three compounds, quercetin showed the most potent inhibitory activity. The phosphorylation of p44/42 mitogen activated protein kinase (MAPK), p38 MAPK and c-Jun N-terminal kinase (JNK) were also inhibited by these compounds. These findings suggested that hyperin in the extract of the root of A. chiisanensis inhibits nitric oxide (NO) production through inhibition of the expression of iNOS by attenuation of p44/p42 MAPK, p38 MAPK and JNK, and thus participates in the antiinflammatory activity of the extract.
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Lipopolisacáridos/farmacología , Macrófagos Peritoneales/efectos de los fármacos , Nitritos/metabolismo , Quercetina/análogos & derivados , Animales , Eleutherococcus/química , Proteínas Quinasas JNK Activadas por Mitógenos/metabolismo , Macrófagos Peritoneales/metabolismo , Masculino , Quinasas de Proteína Quinasa Activadas por Mitógenos/metabolismo , Óxido Nítrico/biosíntesis , Óxido Nítrico Sintasa de Tipo II/metabolismo , Extractos Vegetales/farmacología , Raíces de Plantas/química , Quercetina/farmacología , Ratas , Ratas Sprague-DawleyRESUMEN
RATIONALE: Myoclonic movement is a rare side effect after general anesthesia. Since we use various intravenous agents during general anesthesia recently, it is troublesome to find out the exact cause of this neurologic complication. PATIENT CONCERNS: A 31-year-old female patient without any past medical history underwent hip arthroscopic surgery under general anesthesia. DIAGNOSES: Although there was no specific event during the operation, she showed a sudden myoclonic movement confined to left upper extremity in recovery room. INTERVENTIONS: We administered anticonvulsant agents intrvenously, the myoclonus was stopped shortly but recurred over again. As we stopped the patient-controlled analgesia due to nausea, the symptom halted. OUTCOMES: There was no significant abnormality in electroencephalography or brain diffusion magnetic resonance imaging, which was taken after the event. LESSONS: Clinicians should carefully consider the pharmacologic characteristics and neurologic adverse effects of all administered agents when myoclonus occurs after general anesthesia.
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Anestesia General/efectos adversos , Mioclonía/etiología , Adulto , Analgesia Controlada por el Paciente , Anticonvulsivantes/uso terapéutico , Artroscopía , Femenino , Cadera/cirugía , Humanos , Mioclonía/tratamiento farmacológico , Extremidad SuperiorRESUMEN
STUDY OBJECTIVE: To compare the effectiveness of streamlined liner of pharyngeal airway (SLIPA) in paralyzed and nonparalyzed, anesthetized patients undergoing gynecological surgery. DESIGN: Prospective randomized double-blind clinical trial. SETTING: Intraoperative. PATIENTS: A total of 80 female patients with American Society of Anesthesiologists class I or II and who were undergoing gynecological surgery. INTERVENTIONS: The patients were randomly allocated to either the nonparalyzed group (group NR, n=40) or the paralyzed group (group R, n=40). MEASUREMENTS: Oropharyngeal leakage pressure was the primary outcome. Insertion time; number of insertion attempts; success rate at first insertion; involuntary movement; peak inspiratory pressure (PIP); leakage fraction; hemodynamic changes; complications, such as blood tinging, regurgitation, and sore throat; and recovery time were also evaluated for secondary outcomes. MAIN RESULTS: Oropharyngeal leakage pressure, which is primary outcome, was no difference among the groups. Insertion time, number of insertion attempts, success rate at first insertion, involuntary movement, leakage fraction, hemodynamic changes, and complications were not statistically different among the groups. The PIP in group NR was significantly increased compared to that of group R (P=.002). Recovery time was significantly longer in group R than in group NR (P<.001). CONCLUSIONS: SLIPA had good performance in both paralyzed and nonparalyzed patients. There was no difference in SLIPA performance or complications irrespective of muscle relaxant use, except decrease in PIP and prolong recovery time in paralyzed patients.
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Manejo de la Vía Aérea/métodos , Procedimientos Quirúrgicos Ginecológicos/métodos , Fármacos Neuromusculares no Despolarizantes/administración & dosificación , Parálisis/inducido químicamente , Adulto , Manejo de la Vía Aérea/instrumentación , Método Doble Ciego , Diseño de Equipo , Femenino , Humanos , Persona de Mediana Edad , Faringe , Estudios Prospectivos , Factores de TiempoRESUMEN
1. The effects of acharan sulphate, a glycosaminoglycan isolated from the giant African snail Achatina fulica, on angiogenesis in the granulation tissue were analysed using an air pouch-type carrageenin-induced inflammation model in rats and a cotton thread-induced inflammation model in mice. 2. In the carrageenin-induced inflammation model in rats, intra-pouch injections of acharan sulphate (5 and 50 micro g) inhibited the pouch fluid accumulation and the granulation tissue formation as well as the angiogenesis in the granulation tissue at day 6 in a dose-dependent manner. 3. The inhibitory effects of acharan sulphate at 50 micro g on the pouch fluid accumulation and the leucocyte infiltration into the pouch fluid was not so effective as that of the cyclo-oxygenase inhibitor indomethacin at 100 micro g, but the inhibitory effects of acharan sulphate at 50 micro g on the granulation tissue formation and angiogenesis in the granulation tissue were almost the same as those of indomethacin at 100 micro g. 4. Acharan sulphate did not affect levels of vascular endothelial growth factor (VEGF) in the granulation tissue and in the pouch fluid at day 6, but indomethacin significantly lowered them. 5. In the cotton thread-induced inflammation model in mice, injections of acharan sulphate (10 micro g) at the site of the cotton thread implantation inhibited the granulation tissue formation and angiogenesis as indomethacin (20 micro g) did. Acharan sulphate (10 micro g) did not affect levels of VEGF in the cotton thread-induced granulation tissue at day 5, but indomethacin (20 micro g) significantly lowered them. 6. In culture of human vascular endothelial cells, acharan sulphate at 10 and 100 micro g ml(-1) inhibited VEGF-induced capillary tube formation. 7. These findings suggest that the inhibitory effect of acharan sulphate on angiogenesis in carrageenin- and cotton thread-induced granulation tissues is not due to the inhibition of VEGF protein induction, but is due to the inhibition of VEGF-induced vascular tube formation.
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Glicosaminoglicanos/uso terapéutico , Inflamación/tratamiento farmacológico , Neovascularización Patológica/tratamiento farmacológico , Animales , Relación Dosis-Respuesta a Droga , Factores de Crecimiento Endotelial/metabolismo , Inflamación/metabolismo , Inflamación/patología , Péptidos y Proteínas de Señalización Intercelular/metabolismo , Linfocinas/metabolismo , Masculino , Ratones , Neovascularización Patológica/metabolismo , Neovascularización Patológica/patología , Ratas , Caracoles , Factor A de Crecimiento Endotelial Vascular , Factores de Crecimiento Endotelial VascularRESUMEN
In cultures of the murine macrophage cell line RAW 264.7, effects of four 2'-hydroxychalcone derivatives, 2'-hydroxy-4'-methoxychalcone (compound 1), 2',4-dihydroxy-4'-methoxychalcone (compound 2), 2',4-dihydroxy-6'-methoxychalcone (compound 3) and 2'-hydroxy-4,4'-dimethoxychalcone (compound 4), on lipopolysaccharide (LPS)-induced production of nitric oxide (NO) and tumor necrosis factor (TNF)-alpha were examined. Compounds 1, 2 and 3 at 3-30microM inhibited the production with almost the same potency. Compound 4 showed no inhibitory activity. Compounds 1, 2 and 3 at 3-30microM inhibited the LPS-induced expression of inducible nitric oxide synthase (iNOS) and TNF-alpha mRNA. To clarify the mechanism involved, effects of compounds 1, 2 and 3 on the activation of nuclear factor (NF)-kappaB and activator protein-1 (AP-1) were examined. Both the LPS-induced activation of NF-kappaB and AP-1 were blocked by compounds 1, 2 and 3 at 3-30microM. Moreover, the three compounds at such concentrations inhibited the LPS-induced IkappaB degradation and the phosphorylation of c-jun N-terminal kinase (JNK) and c-jun. These findings suggest that the inhibition of the LPS-induced production of NO and TNF-alpha by the 2'-hydroxychalcone derivatives is due to the inhibition of NF-kappaB and AP-1 activations.
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Chalcona/análogos & derivados , Chalcona/farmacología , Lipopolisacáridos/farmacología , Macrófagos/efectos de los fármacos , Óxido Nítrico Sintasa/biosíntesis , Factor de Necrosis Tumoral alfa/biosíntesis , Animales , Línea Celular , Chalconas , Interacciones Farmacológicas , Expresión Génica/efectos de los fármacos , Proteínas I-kappa B/metabolismo , Proteínas Quinasas JNK Activadas por Mitógenos , Macrófagos/metabolismo , Ratones , Proteínas Quinasas Activadas por Mitógenos/metabolismo , Inhibidor NF-kappaB alfa , FN-kappa B/metabolismo , Nitratos/metabolismo , Óxido Nítrico Sintasa de Tipo II , Fosforilación , ARN Mensajero/biosíntesis , ARN Mensajero/efectos de los fármacos , Transducción de Señal , Factor de Transcripción AP-1/metabolismoRESUMEN
Acharan sulfate is a new type of glycosaminoglycan from the giant African snail, Achatina fulica. Acharan sulfate, which has a primary repeating disaccharide structure of alpha-D-N-acetylglucosaminyl-2-O-sulfo-alpha-L-iduronic acid, was studied as a potential antitumor agent in both in vivo and in vitro assays. The antiangiogenic activity of acharan sulfate was evaluated in the chorioallantoic membrane assay and by measuring its effect on the proliferation of calf pulmonary artery endothelial cells. In vivo, a matrigel plug assay showed that acharan sulfate suppressed basic fibroblast growth factor (bFGF)-stimulated angiogenesis and lowered the hemoglobin (Hb) content inside the plug. Acharan sulfate was administered s.c. at two doses for 15 days to C57BL/6 mice implanted with murine Lewis lung carcinoma in the back. It was also administered i.p. to ICR mice bearing sarcoma 180 at a dose of 30 mg/kg. Subcutaneous injection of acharan sulfate at doses of 10 and 30 mg/kg decreased tumor weight and tumor volume by 40% without toxicity or resistance. Intraperitoneal injection of acharan sulfate also decreased tumor weight and volume by 40% in sarcoma 180-bearing mice. These results suggest that the antitumor activity of acharan sulfate may be related to the inhibition of angiogenesis.
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Glicosaminoglicanos/farmacología , Neoplasias Experimentales/prevención & control , Caracoles/química , Alantoides/irrigación sanguínea , Alantoides/efectos de los fármacos , Inhibidores de la Angiogénesis/farmacología , Animales , Bovinos , División Celular/efectos de los fármacos , Células Cultivadas , Embrión de Pollo , Corion/irrigación sanguínea , Corion/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Endotelio Vascular/citología , Endotelio Vascular/efectos de los fármacos , Glicosaminoglicanos/aislamiento & purificación , Masculino , Ratones , Ratones Endogámicos C57BL , Ratones Endogámicos ICR , Neoplasias Experimentales/patología , Sarcoma Experimental/patología , Sarcoma Experimental/prevención & control , Organismos Libres de Patógenos Específicos , Análisis de Supervivencia , Células Tumorales Cultivadas , Ensayos Antitumor por Modelo de XenoinjertoRESUMEN
The anti-oxidant activities of the various fractions from the herbs of Artemisia apiacea were investigated. The n-hexane and n-butanol fractions were found to cause significant free radical scavenging effects on DPPH, their scavenging potencies as indicated in IC(50) values, being 230.1 and 183.7 microg/ml, respectively. The n-butanol fraction exhibited a significant decrease in serum transaminase activities elevated by hepatic damage induced by CCl(4)-intoxication in rats. All fractions tested exhibited a lipid peroxidation causing a significant decrease in MDA production in TBA-reactant assay. The n-butanol fraction was the strongest in the increase in the anti-oxidant enzymes such as hepatic cytosolic superoxide dismutase (SOD), catalase and glutathione peroxidase (GSH-px) activities in CCl(4)-intoxicated rats. These results suggest that the herbs of A. apiacea possess not only the anti-oxidant, but also the activities in CCl(4)-intoxicated rats. Especially, the n-butanol extract was found to cause significant increases in the rat liver cytosolic SOD, catalase, GSH-px activities as well as a significant decrease in the MDA production.
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Antioxidantes/farmacología , Artemisia , Alanina Transaminasa/sangre , Animales , Antioxidantes/química , Antioxidantes/uso terapéutico , Aspartato Aminotransferasas/sangre , Compuestos de Bifenilo , Intoxicación por Tetracloruro de Carbono/tratamiento farmacológico , Intoxicación por Tetracloruro de Carbono/metabolismo , Depuradores de Radicales Libres/química , Técnicas In Vitro , Peroxidación de Lípido/efectos de los fármacos , Hígado/efectos de los fármacos , Hígado/metabolismo , Hígado/ultraestructura , Masculino , Malondialdehído/metabolismo , Fitoterapia , Picratos/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Ratas , Ratas Sprague-Dawley , SolventesRESUMEN
Fucosterol isolated from Pelvetia siliquosa was tested for its anti-diabetic activity in vivo. Fucosterol, when administered orally at 30 mg/kg in streptozotocin-induced diabetic rats, was caused a significant decrease in serum glucose concentrations, and exhibited an inhibition of sorbitol accumulations in the lenses. Fucosterol, when administered orally at 300 mg/kg in epinephrine-induced diabetic rats, was also caused an inhibition of blood glucose level and glycogen degradation. These results demonstrated that fucosterol is a main anti-diabetic principle from the marine algae P. siliquosa.
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Diabetes Mellitus Experimental/prevención & control , Phaeophyceae/química , Rodanina/análogos & derivados , Estigmasterol/análogos & derivados , Estigmasterol/farmacología , Animales , Glucemia/efectos de los fármacos , Glucemia/metabolismo , Diabetes Mellitus Experimental/sangre , Relación Dosis-Respuesta a Droga , Hígado/efectos de los fármacos , Hígado/metabolismo , Glucógeno Hepático/metabolismo , Masculino , Ratones , Ratas , Ratas Sprague-Dawley , Rodanina/farmacología , Estigmasterol/química , Estigmasterol/aislamiento & purificación , TiazolidinasRESUMEN
Four compounds were isolated from Salicornia herbacea by repeated column chromatography. Their structures were identified as beta-sitosterol (1), stigmasterol (2), uracil (3), and isorhamnetin-3-O-beta-D-glucopyranoside (4) by spectral analysis and comparison with the published data.
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Chenopodiaceae/química , Cromatografía por Intercambio Iónico , Etanol , Hexanos , Hidrólisis , Indicadores y Reactivos , Corea (Geográfico) , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Metanol , Solventes , Espectrometría de Masa por Ionización de ElectrosprayRESUMEN
The anti-oxidant activities of fucosterol isolated from the marine algae Pelvetia siliquosa were investigated. Fucosterol exhibited a significant decrease in serum transaminase activities elevated by hepatic damage induced by CCl4-intoxication in rats. Fucosterol inhibited the sGOT and sGPT activities by 25.57 and 63.16%, respectively. Fucosterol showed the increase in the anti-oxidant enzymes such as hepatic cytosolic superoxide dismutase (SOD), catalase and glutathione peroxidase (GSH-px) activities by 33.89, 21.56 and 39.24%, respectively, in CCl4-intoxicated rats. These results suggest that fucosterol possess not only the anti-oxidant, but also the hepatoprotective activities in rats.
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Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Eucariontes/química , Estigmasterol/aislamiento & purificación , Estigmasterol/farmacología , Administración Oral , Animales , Antioxidantes/química , Tetracloruro de Carbono/administración & dosificación , Tetracloruro de Carbono/efectos adversos , Intoxicación por Tetracloruro de Carbono/diagnóstico , Catalasa/biosíntesis , Catalasa/farmacología , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Enfermedad Hepática Inducida por Sustancias y Drogas/patología , Pruebas Enzimáticas Clínicas , Esquema de Medicación , Glutatión Peroxidasa/biosíntesis , Glutatión Peroxidasa/farmacología , Hexanos , Inyecciones Intraperitoneales , Corea (Geográfico) , Hígado/efectos de los fármacos , Hígado/enzimología , Masculino , Extractos Vegetales/administración & dosificación , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacocinética , Premedicación , Ratas , Ratas Sprague-Dawley , Silimarina/administración & dosificación , Silimarina/farmacocinética , Estigmasterol/análogos & derivados , Estigmasterol/química , Superóxido Dismutasa/biosíntesis , Superóxido Dismutasa/farmacología , Transaminasas/antagonistas & inhibidores , Transaminasas/biosíntesis , Transaminasas/efectos de los fármacosRESUMEN
The present study was carried out to clarify whether tectorigenin and tectoridin isolated from the rhizomes of Belamcanda chinensis (Iridaceae) inhibit hepatic damage induced by carbon tetrachloride (CCl4)-intoxication in rats by the experimental methods in vitro and in vivo. Tectorigenin and tectoridin exhibited a significant decrease in serum transaminase activities elevated by hepatic damage induced by CCl4-intoxication in rats, as well as in a lipid peroxidation causing a significant decrease in malondialdehyde (MDA) production by thiobarbituric acid (TBA)-reactant assay. Both compounds also showed strong increase in the antioxidant enzymes such as hepatic cytosolic superoxide dismutase (SOD), catalase and glutathione peroxidase (GSH-px) activities in CCl4-intoxicated rats. These results suggested that tectorigenin and tectoridin isolated from the rhizomes of B. chinensis possess not only the antioxidative, but also the hepatoprotective activities in CCl4-intoxicated rats.
Asunto(s)
Antioxidantes/uso terapéutico , Intoxicación por Tetracloruro de Carbono/tratamiento farmacológico , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Iridaceae/química , Isoflavonas/uso terapéutico , Alanina Transaminasa/sangre , Animales , Aspartato Aminotransferasas/sangre , Intoxicación por Tetracloruro de Carbono/patología , Enfermedad Hepática Inducida por Sustancias y Drogas/patología , Citosol/metabolismo , Isoflavonas/farmacología , Peroxidación de Lípido/efectos de los fármacos , Hígado/metabolismo , Hígado/patología , Masculino , Extractos Vegetales/química , Extractos Vegetales/farmacología , Raíces de Plantas/química , Ratas , Ratas Sprague-Dawley , Superóxido Dismutasa/metabolismoRESUMEN
The chloroform and the ethyl acetate fractions from the roots of Acanthopanax chiisanensis exhibited a significant inhibition of prostaglandin E2 (PGE2) production in rat peritoneal macrophages stimulated by the protein kinase C activator, 12-O-tetradecanoylphorbol 13-acetate (TPA). Hyperin was isolated as an active principle from the ethyl acetate fraction. It suppressed not only PGE2 production but also nitric oxide (NO) production in vitro in a concentration dependent manner, their IC50, being 24.3 and 32.9 microM, respectively. Hyperin also caused a significant inhibition of increase in acetic acid-induced vascular permeability in mice in vivo.
Asunto(s)
Antiinflamatorios no Esteroideos/farmacología , Eleutherococcus/química , Macrófagos Peritoneales/efectos de los fármacos , Quercetina/análogos & derivados , Quercetina/farmacología , Animales , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/aislamiento & purificación , Western Blotting , Permeabilidad Capilar/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Inyecciones Intraperitoneales , Macrófagos Peritoneales/citología , Macrófagos Peritoneales/metabolismo , Masculino , Ratones , Óxido Nítrico Sintasa/metabolismo , Nitritos/metabolismo , Extractos Vegetales/química , Extractos Vegetales/farmacología , Raíces de Plantas/química , Quercetina/química , Quercetina/aislamiento & purificación , Ratas , Ratas Sprague-DawleyRESUMEN
The antioxidant activities of Acanthopanax senticosus stems were evaluated in CCl4-intoxicated rats. The n-butanol fraction from the water extract of the stems, when pretreated orally at 200 mg/kg/day for 7 consecutive days in rats, was demonstrated to exhibit significant increases in antioxidant enzyme activities such as hepatic cytosolic superoxide dismutase, catalase and glutathione peroxidase by 30.31, 19.82 and 155%, respectively. The n-butanol fraction whereas showed a significant inhibition of serum GPT activity (65.79% inhibition) elevated with hepatic damage induced by CCl4-intoxication. Eleutheroside B, a lignan component, isolated from the n-butanol fraction was found to cause a moderate free radical scavenging effect on DPPH, its scavenging potency as indicated in IC50 value, being 58.5 microM. These results suggested that the stems of A. senticosus possess not only antioxidant but also hepatoprotective activities.
Asunto(s)
Antioxidantes/farmacología , Eleutherococcus/química , Lignanos/farmacología , Tallos de la Planta/química , Administración Oral , Alanina Transaminasa/sangre , Alanina Transaminasa/efectos de los fármacos , Animales , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Aspartato Aminotransferasas/sangre , Aspartato Aminotransferasas/efectos de los fármacos , Compuestos de Bifenilo , Butanoles/administración & dosificación , Butanoles/química , Butanoles/farmacocinética , Intoxicación por Tetracloruro de Carbono/tratamiento farmacológico , Intoxicación por Tetracloruro de Carbono/metabolismo , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos/métodos , Depuradores de Radicales Libres/metabolismo , Depuradores de Radicales Libres/farmacología , Glucósidos/administración & dosificación , Glucósidos/química , Glucósidos/farmacocinética , Hepatocitos/efectos de los fármacos , Hepatocitos/metabolismo , Hepatocitos/patología , Indicadores y Reactivos , Lignanos/química , Lignanos/aislamiento & purificación , Masculino , Fenilpropionatos/administración & dosificación , Fenilpropionatos/química , Fenilpropionatos/farmacocinética , Picratos/antagonistas & inhibidores , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Ratas , Ratas Sprague-Dawley , Silimarina/administración & dosificación , Silimarina/farmacocinética , Silimarina/uso terapéutico , Solubilidad , Agua/químicaRESUMEN
Aldose reductase, the key enzyme of the polyol pathway, is known to play important roles in the diabetic complication. The inhibitors of aldose reductase, therefore, would be potential agents for the prevention of diabetic complications. To evaluate active principles for the inhibition of aldose reductase from the rhizomes of Belamcanda chinensis, twelve phenolic compounds were isolated and tested for their effects on rat lens aldose reductase. As a result, isoflavones such as tectorigenin, irigenin and their glucosides were found to show a strong aldose reductase inhibition. Tectoridin and tectorigenin, exhibited the highest aldose reductase inhibitory potency, their IC50 values, being 1.08 x 10(-6) M and 1.12 x 10(-6) M, respectively, for DL-glyceraldehyde as a substrate. Both compounds, when administered orally at 100 mg/kg for 10 consecutive days to streptozotocin-induced diabetic rats, caused a significant inhibition of sorbitol accumulation in the tissues such as lens, sciatic nerves and red blood cells. Tectorigenin showed a stronger inhibitory activity than tectoridin. From these results, it is suggested that tectorigenin is attributed to be a promising compound for the prevention and/or treatment of diabetic complications.