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1.
Medicine (Baltimore) ; 98(20): e15695, 2019 May.
Artículo en Inglés | MEDLINE | ID: mdl-31096512

RESUMEN

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.


Asunto(s)
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 Tratamiento
2.
Medicine (Baltimore) ; 97(12): e0141, 2018 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-29561417

RESUMEN

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.


Asunto(s)
Anestesia General/efectos adversos , Mioclonía/etiología , Adulto , Analgesia Controlada por el Paciente , Anticonvulsivantes/uso terapéutico , Artroscopía , Femenino , Cadera/cirugía , Humanos , Mioclonía/tratamiento farmacológico , Extremidad Superior
3.
BMC Anesthesiol ; 16(1): 115, 2016 11 17.
Artículo en Inglés | MEDLINE | ID: mdl-27855660

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.


Asunto(s)
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 Joven
4.
J Clin Anesth ; 34: 327-35, 2016 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-27687403

RESUMEN

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.


Asunto(s)
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 Tiempo
5.
Phytochem Anal ; 22(5): 468-73, 2011.
Artículo en Inglés | MEDLINE | ID: mdl-21465599

RESUMEN

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.


Asunto(s)
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 Ultravioleta
6.
Arch Pharm Res ; 34(2): 211-5, 2011 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-21380803

RESUMEN

A flavanol glycoside, glucodistylin (1) and three polyphenol derivatives, gallate (2), (+)-catechin (3) and (+)-gallocatechin (4) were isolated from an aqueous acetone extract of the bark of Quercus acutissima. Of these compounds, glucodistylin exhibited uncompetitive inhibitory activity against recombinant human aldose reductase with an IC(50) value of 7.2 µM. Furthermore, glucodistylin inhibited sorbitol accumulation by 48.84% at 50 µM. This flavonoid showed therapeutic potential in the prevention and treatment of diabetes-related complications.


Asunto(s)
Aldehído Reductasa/antagonistas & inhibidores , Catequina/análogos & derivados , Catequina/farmacología , Flavonoides/farmacología , Flavonoles/farmacología , Glicósidos/farmacología , Fenoles/farmacología , Quercus , Sorbitol/metabolismo , Aldehído Reductasa/metabolismo , Catequina/química , Catequina/aislamiento & purificación , Complicaciones de la Diabetes/tratamiento farmacológico , Complicaciones de la Diabetes/prevención & control , Evaluación Preclínica de Medicamentos , Flavonoides/química , Flavonoides/aislamiento & purificación , Flavonoles/química , Flavonoles/aislamiento & purificación , Glicósidos/química , Glicósidos/aislamiento & purificación , Humanos , Terapia Molecular Dirigida , Fenoles/química , Fenoles/aislamiento & purificación , Corteza de la Planta , Polifenoles , Proteínas Recombinantes/antagonistas & inhibidores
7.
Biol Pharm Bull ; 34(1): 160-3, 2011.
Artículo en Inglés | MEDLINE | ID: mdl-21212537

RESUMEN

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.


Asunto(s)
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/metabolismo
8.
J Ethnopharmacol ; 131(1): 56-62, 2010 Aug 19.
Artículo en Inglés | MEDLINE | ID: mdl-20554007

RESUMEN

AIM OF THE STUDY: The aim of the present study was to investigate the effects of MeOH extract of PL (PLME) and its fractions on angiogenesis. MATERIALS AND METHODS: PLME and its subsequent fractions (methylene chloride, ethyl acetate, n-butanol and aqueous fractions) were evaluated in vitro. Specifically, the anti-angiogenic activities of PLME and its fractions were investigated by measuring their effects on the proliferation, migration, tube formation and phosphorylation of vascular endothelial growth factor receptor (VEGFR)-2 in human umbilical vein endothelial cells (HUVECs). In addition, the in vivo Matrigel plug model was applied to evaluate new vessel formation. RESULTS: The results revealed that PLME and its subsequent fractions, except for the aqueous fraction, led to significant inhibition of the proliferation, migration, tube formation and VEGFR-2 phosphorylation of HUVECs as well as in vivo angiogenesis. CONCLUSIONS: These findings indicate the potential for the use of PLME in pathological situations involving stimulated angiogenesis, such as inflammation and tumor development.


Asunto(s)
Inhibidores de la Angiogénesis/farmacología , Proliferación Celular/efectos de los fármacos , Metanol/farmacología , Extractos Vegetales/farmacología , Polisacáridos/farmacología , Agaricales , Inhibidores de la Angiogénesis/aislamiento & purificación , Animales , Movimiento Celular/efectos de los fármacos , Movimiento Celular/fisiología , Células Cultivadas , Células Endoteliales/efectos de los fármacos , Células Endoteliales/fisiología , Endotelio Vascular/efectos de los fármacos , Endotelio Vascular/fisiología , Humanos , Masculino , Ratones , Ratones Endogámicos ICR , Phellinus , Extractos Vegetales/aislamiento & purificación , Polisacáridos/aislamiento & purificación , Receptor 2 de Factores de Crecimiento Endotelial Vascular/antagonistas & inhibidores , Receptor 2 de Factores de Crecimiento Endotelial Vascular/metabolismo
9.
Biol Pharm Bull ; 33(5): 917-21, 2010.
Artículo en Inglés | MEDLINE | ID: mdl-20460778

RESUMEN

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.


Asunto(s)
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/farmacología
10.
J Agric Food Chem ; 58(3): 1603-8, 2010 Feb 10.
Artículo en Inglés | MEDLINE | ID: mdl-20088509

RESUMEN

Our preliminary experiment demonstrated that a n-hexane/EtOH (9:1, volume) extract of Glycyrrhiza uralensis (licorice) caused a significant induction of NAD(P)H:oxidoquinone reductase (NQO1), one of the well-known phase 2 detoxifying enzymes. We isolated dehydroglyasperin C (DGC) as a potent phase 2 enzyme inducer from licorice. DGC induced NQO1 both in wild-type murine hepatoma Hepa1c1c7 and ARNT-lacking BPRc1 cells, indicating that the compound is a monofunctional inducer. The compound induced not only NQO1 but also some other phase 2 detoxifying/antioxidant enzymes, such as glutathione S-transferase, gamma-glutamylcysteine synthase, glutathione reductase, and heme oxygenase 1. Similar to most monofunctional inducers, DGC caused the accumulation of Nrf2 in the nucleus in dose- and time-dependent manners and thereby activated expression of phase 2 detoxifying enzymes. It also resulted in a dose-dependent increase in the luciferase activity in the reporter assay, in which HepG2-C8 cells transfected with antioxidant response element (ARE)-luciferase construct were used, suggesting that the induction of phase 2 detoxifying and antioxidant enzymes could be achieved through the interaction of Nrf2 with the ARE sequence in the promoter region of their genes.


Asunto(s)
Benzopiranos/farmacología , Regulación Enzimológica de la Expresión Génica/efectos de los fármacos , Glycyrrhiza/química , Fase II de la Desintoxicación Metabólica , NAD(P)H Deshidrogenasa (Quinona)/metabolismo , Factor 2 Relacionado con NF-E2/metabolismo , Extractos Vegetales/farmacología , Animales , Benzopiranos/química , Benzopiranos/aislamiento & purificación , Línea Celular Tumoral , Glutatión Transferasa/genética , Glutatión Transferasa/metabolismo , Humanos , Ratones , NAD(P)H Deshidrogenasa (Quinona)/genética , Factor 2 Relacionado con NF-E2/genética , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Activación Transcripcional/efectos de los fármacos
11.
J Sep Sci ; 33(4-5): 664-71, 2010 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-20112307

RESUMEN

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.


Asunto(s)
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 Tiempo
12.
Nat Prod Commun ; 5(12): 1927-30, 2010 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-21299122

RESUMEN

Protein tyrosine phosphatase 1beta (PTP1beta) acts as a negative regulator of insulin signaling. Selective inhibition of PTP1beta has served as a potential drug target for the treatment of type 2 diabetes mellitus. We evaluated the inhibitory effect of Phellinus linteus against PTP1beta as part of our ongoing search for natural therapeutic and preventive agents for diabetes mellitus. Fractions of the P. linteus extract were found to exhibit significant inhibitory activities against PTP1beta. In an attempt to identify bioactive components, we isolated, from the most active ethyl acetate fraction, five hispidin derivatives (phelligridimer A, davallialactone, hypholomine B, interfungins A, and inoscavin A) and four phenolic compounds (protocatechuic acid, protocatechualdehyde, caffeic acid, and ellagic acid). The chemical structures of these compounds were elucidated from spectroscopic evidence and by comparison with published data. All the compounds strongly inhibited PTP1beta activity in an in vitro assay; their IC50 values ranged from 9.0 +/- 0.01 to 58.2 +/- 0.3 microM. Our results indicated that the hispidin skeleton may be an important moiety for inhibitory activity of the above compounds against PTP1beta. Thus, hispidin derivatives could be a potent new class of natural PTP1beta inhibitors.


Asunto(s)
Polisacáridos/química , Proteína Tirosina Fosfatasa no Receptora Tipo 1/antagonistas & inhibidores , Pironas/farmacología , Frutas/química , Phellinus , Extractos Vegetales , Relación Estructura-Actividad
13.
Biol Pharm Bull ; 31(10): 1968-72, 2008 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-18827365

RESUMEN

To characterize active principles for prevention and treatment of diabetic complications, the isolation of protein glycation inhibitors from the fruiting body of Phellinus linteus was conducted in vitro using the model systems of hemoglobin-delta-gluconolactone (early stage), bovine serum albumin-methylglyoxal (middle stage), and N(alpha)-acetyl-glycyl-lysine methyl ester-D-ribose (last stage) assays. Nine compounds were isolated from the active ethylacetate fraction of the fruiting body and identified as protocatechuic acid (1), protocatechualdehyde (2), caffeic acid (3), ellagic acid (4), hispidin (5), davallialactone (6), hypholomine B (7), interfungins A (8), and inoscavin A (9) by spectroscopic analyses. At the early stage of protein glycation, compounds 6, 8, and 9 exhibited inhibitory activity on hemoglobin A(1C) formation. For the middle stage, compounds 2, 6, and 9 showed a significant inhibitory effect on methylglyoxal-medicated protein modification and their IC(50) values were 144.28, 213.15, and 158.66 muM, respectively. At the last stage of glycation, compound 8 was found to be a potent inhibitor of the cross-linking of proteins, which was more effective than that of aminoguanidine, a well-known inhibitor for advanced glycation end products. Consequently, compound 8 showed the most potent inhibitory effects at each stage of protein glycation. This mechanism may help to provide a protective effect against hyperglycemia-mediated protein damage.


Asunto(s)
Basidiomycota/química , Cuerpos Fructíferos de los Hongos/química , Productos Finales de Glicación Avanzada/antagonistas & inhibidores , Hemoglobina Glucada/química , Glicosilación/efectos de los fármacos , Hemoglobinas/metabolismo , Espectroscopía de Resonancia Magnética , Proteínas/química , Piruvaldehído/química , Albúmina Sérica Bovina/química
14.
Phytother Res ; 22(11): 1552-6, 2008 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-18814209

RESUMEN

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.


Asunto(s)
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-Dawley
15.
Biol Pharm Bull ; 31(4): 765-8, 2008 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-18379080

RESUMEN

In an effort to characterize active principles for diabetic complication from medicinal mushroom, aldose reductase inhibitors were isolated from the fruiting body of Phellinus linteus and identified as hispidin (5), phelligridimer A (6), davallialactone (7), methyldavallialactone (8), hypholomine B (9), interfungins A (10), and inoscavin A (11), together with protocatechuic acid (1), protocatechualdehyde (2), caffeic acid (3), and ellagic acid (4). Their structures were elucidated by spectroscopic analyses. Among them, davallialactone (7), hypholomine B (9), and ellagic acid (4) exhibited potent rat lens aldose reductase and human recombinant aldose reductase inhibitory activity with IC50 values of 0.33, 0.82, 0.63 microM and 0.56, 1.28, 1.37 microM, respectively.


Asunto(s)
Aldehído Reductasa/antagonistas & inhibidores , Basidiomycota/química , Inhibidores Enzimáticos/aislamiento & purificación , Inhibidores Enzimáticos/farmacología , Cuerpos Fructíferos de los Hongos/química , Animales , Liofilización , Humanos , Indicadores y Reactivos , Cristalino/enzimología , Espectroscopía de Resonancia Magnética , Ratas , Ratas Sprague-Dawley , Proteínas Recombinantes/química
16.
Planta Med ; 74(2): 114-9, 2008 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-18214814

RESUMEN

In the present study, we investigated effects of the dried, hot-water extract of Cordyceps militaris (CME) and its major metabolite (cordycepin) against ischemic damage. The repeated treatment with CME protected hippocampal CA1 pyramidal neurons from ischemic damage in gerbils. The treatment with CME or cordycepin in gerbils reduced 4-hydroxy-2-nonenal (a marker of lipid peroxidation) immunoreactivity and levels in the ischemic CA1 region. Glial fibrillary acidic protein immunoreactive astrocytes and ionized calcium-binding adapter molecule 1 immunoreactive microglia in the vehicle-treated ischemic group were activated in the CA1 region 4 days after ischemia/reperfusion, whereas in the CME- or cordycepin-treated ischemic group, their activation was significantly decreased. These results suggest that the repeated treatment with CME protects against neuronal damage from ischemia/reperfusion by reducing oxidative damage.


Asunto(s)
Productos Biológicos/aislamiento & purificación , Lesiones Encefálicas/prevención & control , Cordyceps/química , Desoxiadenosinas/aislamiento & purificación , Hipocampo/lesiones , Hipocampo/fisiología , Neuronas/fisiología , Adenina/farmacología , Adenosina/farmacología , Aldehídos/metabolismo , Animales , Antifúngicos/aislamiento & purificación , Antifúngicos/farmacología , Productos Biológicos/farmacología , Desoxiadenosinas/farmacología , Gerbillinae , Hipocampo/efectos de los fármacos , Peroxidación de Lípido/efectos de los fármacos , Masculino
17.
Biochem Biophys Res Commun ; 351(1): 146-52, 2006 Dec 08.
Artículo en Inglés | MEDLINE | ID: mdl-17049489

RESUMEN

Foods of plant origin, especially fruits and vegetables, draw increased attention because of their potential benefits to human health. The aim of the present study was to determine in vitro anti-inflammatory activity of four different extracts obtained from the fruits of Rubus coreanus (aqueous and ethanol extracts of unripe and ripe fruits). Among the four extracts, the ethanol extract of unripe fruits of R. coreanus (URCE) suppressed nitric oxide (NO) and prostaglandin E(2) (PGE(2)) production in lipopolysaccharide (LPS)-stimulated RAW264.7 murine macrophages. We also demonstrated that URCE by itself is a potent inducer of heme oxygenase-1 (HO-1). Inhibition of HO-1 activity by tin protoporphyrin, a specific HO-1 inhibitor, suppressed the URCE-induced reductions in the production of NO and PGE(2) as well as the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX-2). Our data suggest that URCE exerts anti-inflammatory effects in macrophages via activation of the HO-1 pathway and helps to elucidate the mechanism underlying the potential therapeutic value of R. coreanus extracts.


Asunto(s)
Antiinflamatorios/administración & dosificación , Frutas/metabolismo , Hemo-Oxigenasa 1/efectos de los fármacos , Factores Inmunológicos/inmunología , Activación de Macrófagos/efectos de los fármacos , Macrófagos/inmunología , Extractos Vegetales/administración & dosificación , Rosácea/metabolismo , Animales , Antiinflamatorios/química , Línea Celular , Relación Dosis-Respuesta a Droga , Etanol/química , Frutas/química , Macrófagos/efectos de los fármacos , Ratones , Extractos Vegetales/química
18.
Phytother Res ; 20(10): 825-30, 2006 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-16881021

RESUMEN

Aldose reductase, the principal enzyme of the polyol pathway, has been shown to play an important role in the complications associated with diabetes. A methanol extract of the stamens of Nelumbo nucifera Gaertn. was shown to exert an inhibitory effect on rat lens aldose reductase (RLAR), and thus was fractionated using several organic solvents, including dichloromethane, ethyl acetate and n-butanol. The ethyl acetate-soluble fraction, which manifested potent RLAR-inhibitory properties, was then purified further via repeated measures of silica gel and Sephadex LH-20 column chromatography. Thirteen flavonoids: kaempferol (1) and seven of its glycosides (2-9), myricetin 3',5'-dimethylether 3-O-beta-d-glucopyranoside (10), quercetin 3-O-beta-d-glucopyranoside (11) and two isorhamnetin glycosides (12, 13) were isolated from N. nucifera, as well as four non-flavonoid compounds: adenine (14), myo-inositol (15), arbutin (16) and beta-sitosterol glucopyranoside (17). These compounds were all assessed with regard to their RLAR-inhibitory properties. Among the isolated flavonoids, those harboring 3-O-alpha-l-rhamnopyranosyl-(1-->6)-beta-d-glucopyranoside groups in their C rings, including kaempferol 3-O-alpha-l-rhamnopyranosyl-(1-->6)-beta-d-glucopyranoside (5) and isorhamnetin 3-O-alpha-l-rhamnopyranosyl-(1-->6)-beta-d-glucopyranoside (13), were determined to exhibit the highest degree of rat lens aldose reductase inhibitory activity in vitro, evidencing IC(50) values (concentration required for a 50% inhibition of enzyme activity) of 5.6 and 9.0 microm, respectively.


Asunto(s)
Aldehído Reductasa/antagonistas & inhibidores , Cristalino/enzimología , Nelumbo/química , Animales , Flavonoides/química , Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Flores/química , Cristalino/efectos de los fármacos , Extractos Vegetales/química , Extractos Vegetales/farmacología , Ratas , Ratas Sprague-Dawley
19.
Biol Pharm Bull ; 29(5): 1028-31, 2006 May.
Artículo en Inglés | MEDLINE | ID: mdl-16651739

RESUMEN

In the present study, we evaluated the in vitro and in vivo anti-angiogenic and anti-tumor activities of 2'-hydroxy-4'-methoxychalcone (HMC). HMC decreased angiogenesis in both chick embryos in the chorioallantoic membrane assay and basic fibroblast growth factor (bFGF)-induced vessel formation in the mouse Matrigel plug assay. This compound also reduced the proliferation of calf pulmonary arterial endothelial cells and was found to possess relatively weak gelatinase/collagenase inhibitory activity in vitro. HMC, when administered subcutaneously at the dose of 30 mg/kg for 20 d to mice implanted with murine Lewis lung carcinoma, caused a significant inhibition of tumor volume by 27.2%. Intraperitoneal (i.p.) treatment at the same dosage for 10 d to ICR mice bearing sarcoma 180 caused a significant suppression in tumor weight by 33.7%. Taken together, out data demonstrate that the anti-angiogenic activities of HMC might be due to anti-proliferative activity under inhibition of the induction of COX-2 enzyme. Furthermore, the results suggest that the potent anti-angiogenic activity of HMC seems to be the possible mechanism of action in these animal models of solid tumors.


Asunto(s)
Inhibidores de la Angiogénesis/farmacología , Antineoplásicos/farmacología , Chalcona/análogos & derivados , Animales , Anticoagulantes/farmacología , Carcinoma Pulmonar de Lewis/tratamiento farmacológico , Bovinos , Línea Celular , Proliferación Celular/efectos de los fármacos , Chalcona/farmacología , Chalconas , Embrión de Pollo , Colagenasas/metabolismo , Células Endoteliales/efectos de los fármacos , Factores de Crecimiento de Fibroblastos/farmacología , Gelatinasas/metabolismo , Heparina/farmacología , Células LLC-PK1 , Ratones , Ratones Endogámicos C57BL , Sarcoma 180/patología , Porcinos
20.
Phytother Res ; 19(6): 477-80, 2005 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-16114079

RESUMEN

Aldose reductase, the key enzyme of the polyol pathway, is known to play important roles in diabetic complications. Therefore, inhibitors of aldose reductase would be potential agents for the prevention of diabetic complications. To evaluate the inhibitory potential of aldose reductase from Ganoderma applanatum (Polyporaceae), methanol (MeOH) and water extracts were tested for their effects on rat lens aldose reductase (RLAR). The effects of both extracts on streptozotocin (STZ)-induced diabetes in rats were also investigated. The MeOH extract exhibited a potent rat lens aldose reductase (RLAR) inhibition in vitro, and showed a significant inhibition, of not only serum glucose concentrations, but also of sorbitol accumulations in the lens, red blood cells (RBC) and sciatic nerves in STZ-induced diabetic rats. Associated with a reduction in serum glucose concentration in STZ-induced diabetic rats, this extract was found to cause a significant glucose tolerance effect. These results suggested that G. applanatum might possess constituents with antidiabetic and inhibitory effects on diabetic complications.


Asunto(s)
Ganoderma , Hipoglucemiantes/farmacología , Cristalino/efectos de los fármacos , Fitoterapia , Extractos Vegetales/farmacología , Aldehído Reductasa/antagonistas & inhibidores , Aldehído Reductasa/biosíntesis , Aldehído Reductasa/efectos de los fármacos , Animales , Glucemia/efectos de los fármacos , Diabetes Mellitus Experimental/inducido químicamente , Diabetes Mellitus Experimental/prevención & control , Retinopatía Diabética/inducido químicamente , Retinopatía Diabética/prevención & control , Inhibidores Enzimáticos/administración & dosificación , Inhibidores Enzimáticos/farmacología , Inhibidores Enzimáticos/uso terapéutico , Hipoglucemiantes/administración & dosificación , Hipoglucemiantes/uso terapéutico , Cristalino/enzimología , Extractos Vegetales/administración & dosificación , Extractos Vegetales/uso terapéutico , Ratas , Sorbitol/metabolismo , Organismos Libres de Patógenos Específicos , Estreptozocina
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