RESUMEN
The expression of matrix metalloproteinase (MMPs)-9 is critical for cell migration and can lead to invasion and metastasis of cancer cells. In the present study, we examined the inhibitory effects of JNP3, a new compound which was isolated from traditional Chinese medicine, on cell invasion and MMP-9 activation in phorbol myristate acetate (PMA)-induced MCF-7 cells. Treatment with JNP3 significantly and selectively inhibited PMA-induced MMP-9 secretion, mRNA expression and protein levels, and these results led to reduction of cell invasion and migration in PMA-induced MCF-7 cells. The results of MMP-9 promoter assay and EMSA showed that JNP3 specifically inhibited PMA-induced MMP-9 gene expression by blocking NF-κB-dependent transcriptional activity. In addition, PMA-induced phosphorylation of ERK1/2 and JNK were suppressed by JNP3 treatment, whereas the phosphorylation of p38 MAPK was not affected by JNP3. These results suggest that JNP3 can be potential anti-cancer agents through specific inhibition of NF-κB-dependent MMP-9 gene expression.
Asunto(s)
Antineoplásicos/farmacología , Neoplasias de la Mama/metabolismo , Neoplasias de la Mama/patología , Inhibidores de la Metaloproteinasa de la Matriz , FN-kappa B/antagonistas & inhibidores , Triterpenos/farmacología , Línea Celular Tumoral , Regulación hacia Abajo , Femenino , Expresión Génica/efectos de los fármacos , Regulación Enzimológica de la Expresión Génica/efectos de los fármacos , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Humanos , MAP Quinasa Quinasa 4/metabolismo , Sistema de Señalización de MAP Quinasas/efectos de los fármacos , Metaloproteinasa 9 de la Matriz/genética , Invasividad Neoplásica , Fosforilación/efectos de los fármacos , Acetato de Tetradecanoilforbol/farmacología , Triterpenos/químicaRESUMEN
A previously unidentified gene encoding ubiquitin-conjugating enzyme was isolated from leaves of wild rice plant treated with wounding and microbe-associated molecular patterns. The OgUBC1 gene was composed of 148 amino acids and contained a typical active site and 21 ubiquitin thioester intermediate interaction residues and 4 E3 interaction residues. Both exogenous application of salicylic acid and UV-B irradiation triggered expression of OgUBC1 in leaves of wild rice. Recombinant OgUBC1 proteins bound to ubiquitins in vitro, proposing that the protein might act as E2 enzyme in planta. Heterologous expression of the OgUBC1 in Arabidopsis thaliana protected plants from cellular damage caused by an excess of UV-B radiation. A stable expression of chalcone synthase gene was detected in leaves of OgUBC1-expressing Arabidopsis, resulting in producing higher amounts of anthocyanin than those in wild-type Col-0 plants. Additionally, both pathogenesis-related gene1 and 5 were transcribed in the transgenic Arabidopsis in the absence of pathogen infection. The OgUBC1-expressing plants were resistant to the infection of Botrytis cinerea. Taken together, we suggested that the OgUBC1 is involved in ubiquitination process important for cellular response against biotic and abiotic stresses in plants.
Asunto(s)
Arabidopsis/microbiología , Arabidopsis/efectos de la radiación , Botrytis , Expresión Génica , Oryza/enzimología , Enfermedades de las Plantas/genética , Tolerancia a Radiación/genética , Enzimas Ubiquitina-Conjugadoras/genética , Arabidopsis/genética , Oryza/genética , Enfermedades de las Plantas/microbiología , Rayos UltravioletaRESUMEN
The ubiquitin-26S proteasome system is important in the quality control of intracellular proteins. The ubiquitin-26S proteasome system includes the E1 (ubiquitin activating), E2 (ubiquitin conjugating), and E3 (ubiquitin ligase) enzymes. U-box proteins are a derived version of RING-finger domains, which have E3 enzyme activity. Here, we present the isolation of a novel U-box protein, U-box containing E3 ligase induced by phosphate starvation (OsUPS), from rice (Oryza sativa). The cDNA encoding the O. sativa U-box protein (OsUPS) comprises 1338 bp, with an open reading frame of 445 amino acids. The amino acid sequence of OsUPS cDNA shows 41-79% identity with other plant U-box homologous genes. The open reading frame of the OsUPS protein is comprised of notable domains: a single ~70-amino acid domain and a GKL domain that contains conserved glycine, lysine/arginine residues and leucine-rich feature. We found that full-length expression of OsUPS was up-regulated in both rice plants and cell culture in the absence of inorganic phosphate (P(i)). A self-ubiquitination assay indicated that the bacterially expressed OsUPS protein had E3 ligase activity, and subcellular localization results showed that OsUPS was located in the chloroplast. These results support the notion that OsUPS plays an important role in the P(i) signaling pathway through the ubiquitin-26S proteasome system.
Asunto(s)
Genes de Plantas/genética , Oryza/enzimología , Oryza/genética , Fosfatos/deficiencia , Proteínas de Plantas/genética , Ubiquitina-Proteína Ligasas/genética , Arabidopsis/efectos de los fármacos , Arabidopsis/genética , Arabidopsis/metabolismo , Bioensayo , Cloroplastos/efectos de los fármacos , Cloroplastos/enzimología , Clonación Molecular , Regulación Enzimológica de la Expresión Génica , Regulación de la Expresión Génica de las Plantas/efectos de los fármacos , Proteínas Fluorescentes Verdes/metabolismo , Datos de Secuencia Molecular , Hibridación de Ácido Nucleico , Oryza/efectos de los fármacos , Fosfatos/farmacología , Proteínas de Plantas/metabolismo , Plantas Modificadas Genéticamente , Transporte de Proteínas/efectos de los fármacos , Proteínas Recombinantes de Fusión/metabolismo , Fracciones Subcelulares/efectos de los fármacos , Fracciones Subcelulares/enzimología , Ubiquitina-Proteína Ligasas/metabolismo , Ubiquitinación/efectos de los fármacosRESUMEN
Salinity stress severely affects plant growth and development causing crop loss worldwide. Suaeda asparagoides is a salt-marsh euhalophyte widely distributed in southwestern foreshore of Korea. To isolate salt tolerance genes from S. asparagoides, we constructed a cDNA library from leaf tissues of S. asparagoides that was treated with 200 mM NaCl. A total of 1,056 clones were randomly selected for EST sequencing, and 932 of them produced readable sequence. By sequence analysis, we identified 538 unigenes and registered each in National Center for Biotechnology Information. The 80 salt stress related genes were selected to study their differential expression. Reverse transcription-PCR and Northern blot analysis revealed that 23 genes were differentially expressed under the high salinity stress conditions in S. asparagoides. They are functionally diverse including transport, signal transduction, transcription factor, metabolism and stress associated protein, and unknown function. Among them dehydrin (SaDhn) and RNA binding protein (SaRBP1) were examined for their abiotic stress tolerance in yeast (Saccharomyces cerevisiae). Yeast overexpressing SaDhn and SaRBP1 showed enhanced tolerance to osmotic, freezing and heat shock stresses. This study provides the evidence that SaRBP1 and SaDhn from S. asparagoides exert abiotic stress tolerance in yeast. Information of salt stress related genes from S. asparagoides would contribute for the accumulating genetic resources to improve osmotic tolerance in plants.
Asunto(s)
Chenopodiaceae/genética , Proteínas de Plantas/genética , Tolerancia a la Sal/genética , Plantas Tolerantes a la Sal/genética , Adaptación Biológica , Secuencia de Aminoácidos , ADN Complementario , Etiquetas de Secuencia Expresada , Regulación de la Expresión Génica de las Plantas , Corea (Geográfico) , Datos de Secuencia Molecular , Hojas de la Planta/genética , Proteínas de Unión al ARN/genética , Salinidad , Homología de Secuencia de Aminoácido , Transducción de Señal/genética , Factores de Transcripción/genéticaRESUMEN
Oleifolioside A, a new triterpenoid compound isolated from Dendropanax morbifera Leveille (D. morbifera), was shown in this study to have potent inhibitory effects on lipopolysaccharide (LPS-)stimulated nitric oxide (NO) and prostaglandin E(2) (PGE(2)) production in RAW 264.7 macrophages. Consistent with these findings, oleifolioside A was further shown to suppress the expression of LPS-stimulated inducible nitric oxide synthase (iNOS) and cyclooxigenase-2 (COX-2) in a dose-dependent manner at both the protein and mRNA levels and to significantly inhibit the DNA-binding activity and transcriptional activity of NF-κB in response to LPS. These results were found to be associated with the inhibition of the degradation and phosphorylation of IκB-α and subsequent translocation of the NF-κB p65 subunit to the nucleus. Inhibition of NF-κB activation by oleifolioside A was also shown to be mediated through the prevention of p38 MAPK and ERK1/2 phosphorylation. Taken together, our results suggest that oleifolioside A has the potential to be a novel anti-inflammatory agent capable of targeting both the NF-κB and MAPK signaling pathways.
RESUMEN
The study evaluated the anticomplement effects from organic solvent extracts of five Compositae plants (Ligularia fischeri (Ledeb.) Turez, Ligularia taquetii (H.Lev. & Vaniot) Nakai, Ainsliaea acerifolia Sch.Bip, Aster scaber Thunb, Aster koraiensis Nakai, Synurus deltoides Aiton) from South Korea on the classical pathway complement system. We have evaluated organic solvent extracts from five Compositae with regard to its anticomplement activity. Chloroform extracts from L. taquetii showed inhibitory activity against complement system with 50% inhibitory concentrations (IC50) values of 73.2 µg/mL. This is the first report of anticomplement activity from L. taquetii.
Asunto(s)
Asteraceae/química , Vía Clásica del Complemento/efectos de los fármacos , Metanol/química , Extractos Vegetales/farmacología , Solventes/química , Animales , Relación Dosis-Respuesta a Droga , Humanos , Extractos Vegetales/química , Conejos , OvinosRESUMEN
The present study evaluated the anticomplement effects from isolated compounds of Sorghum bicolor in classical pathway complement system. Using column chromatograph, three compounds; Sorgoleone-362 (1), Sorgoleone-360 (2) and Sorgoleone-386 (3) were isolated and evaluated for in vitro anticomplement activity. Sorgoleone-386 showed inhibitory activity against complement system with 50% inhibitory concentrations (IC(50)) values of 148.3µg/ml. This is the first report of anticomplement activity of isolated compounds from Sorghum bicolor.
Asunto(s)
Benzoquinonas/farmacología , Inactivadores del Complemento/farmacología , Vía Clásica del Complemento/efectos de los fármacos , Lípidos/farmacología , Extractos Vegetales/química , Raíces de Plantas/química , Sorghum/química , Animales , Benzoquinonas/aislamiento & purificación , Cromatografía Líquida de Alta Presión , Cromatografía en Capa Delgada , Cinamatos/farmacología , Inactivadores del Complemento/aislamiento & purificación , Depsidos/farmacología , Flavonoides/farmacología , Hemólisis/inmunología , Concentración 50 Inhibidora , Lípidos/aislamiento & purificación , Estructura Molecular , Conejos , Ovinos , Ácido RosmarínicoRESUMEN
The study evaluated the anticomplement activity from various solvent extracts of eight Artemisia plants (Artemisia capillaris Thunb., Artemisia fukudo Makino., Artemisia japonica Thunb., Artemisia montana (Nakai) Pamp., Artemisia keiskeana Miq., Artemisia rubripes Nakai., Artemisia stolonifera (Maxim.) Kom., and Artemisia sylvatica Max.) from South Korea on the classical pathway (CP). We have evaluated various organic solvent extract from eight Artemisia plants with regard to its anticomplement activity on the CP. A. rubripes and A. montana chloroform extracts showed inhibitory activity against complement system with 50% inhibitory concentrations (IC50) values of 54.3 and 64.2 µg/mL. This is the first report of anticomplement activity from Artemisia plants.
Asunto(s)
Artemisia/química , Vía Clásica del Complemento/efectos de los fármacos , Proteínas del Sistema Complemento/metabolismo , Extractos Vegetales/farmacología , Animales , Humanos , Extractos Vegetales/química , Conejos , República de Corea , Ovinos , Solventes/químicaRESUMEN
The study evaluated the anticomplement activity from isolated compounds from Artemisia montana (Nakai) Pamp. from South Korea on the classical pathway. In a previous work, A. montana (Nakai) Pamp. chloroform extracts showed inhibitory activity against complement system. The chromatographic separation of a chloroform chloride extract of A. montana (Nakai) Pamp. led to the isolation of four compounds. Their structures were characterized to be ezoartemin, yamayomoginin, ezomontanin and 11,13-dihydroezomontanin by spectroscopic data. This is the first report of anticomplement activity of isolated compounds from A. montana (Nakai) Pamp.
Asunto(s)
Artemisia/química , Vía Clásica del Complemento/efectos de los fármacos , Proteínas del Sistema Complemento/química , Adulto , Animales , Humanos , Masculino , OvinosRESUMEN
The study evaluated the anticomplement activity from various solvent extracts of nine Amarantaceae plants (Achyranthes japonica (Miq.) Nakai, Amaranthus mangostanus L., Amaranthus retroflexus L., Amaranthus spinosus L., Celosia argentea var. spicata., Amaranthus lividus L., Celosia cristata L., Amaranthus viridis L., Gomphrena globosa L.) from South Korea on the classical pathway. We have evaluated various organic solvent extract from nine Amarantaceae plants with regard to its anticomplement activity on the classical pathway. Achyranthes japonica chloroform extracts showed inhibitory activity against complement system with 50% inhibitory concentrations (IC(50)) value of 73.1µg/ml. This is the first report of anticomplement activity from Amarantaceae plants.
Asunto(s)
Amaranthaceae/química , Inactivadores del Complemento/farmacología , Vía Clásica del Complemento/efectos de los fármacos , Compuestos Orgánicos/química , Extractos Vegetales/farmacología , Solventes/química , Animales , Inactivadores del Complemento/aislamiento & purificación , Vía Clásica del Complemento/inmunología , Hemólisis/inmunología , Concentración 50 Inhibidora , Extractos Vegetales/aislamiento & purificación , Conejos , República de Corea , OvinosRESUMEN
The present study evaluated the anticomplement effects of isolated compounds from Achyranthes japonica in the classical pathway of the complement system. Using column chromatography, three compounds: achyranthoside C dimethyl ester, achyranthoside C butyl dimethyl ester, and achyranthoside E dimethyl ester were isolated and evaluated for in vitro anticomplement activity. Achyranthoside C dimethyl ester showed the most potent inhibitory activity against the complement system, with 50% inhibitory concentrations (IC(50)) values of 26.2 µg/mL. This is the first report of anticomplement activity of isolated compounds from A. japonica.
Asunto(s)
Achyranthes/química , Inactivadores del Complemento/farmacología , Vía Clásica del Complemento/efectos de los fármacos , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/farmacología , Saponinas/farmacología , Animales , Cloroformo/química , Cromatografía Líquida de Alta Presión , Cromatografía en Capa Delgada , Inactivadores del Complemento/aislamiento & purificación , Vía Clásica del Complemento/inmunología , Hemólisis/inmunología , Concentración 50 Inhibidora , Ácido Oleanólico/aislamiento & purificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Conejos , Saponinas/aislamiento & purificación , OvinosRESUMEN
The study evaluated the anticomplement activity from isolated compounds from Artemisia rubripes Nakai from South Korea on the classical pathway. In the previous works, Artemisia rubripes chloroform extracts showed inhibitory activity against complement system. The chromatographic separation of a chloroform chloride extract of Artemisia rubripes led to the isolation of three compounds. Their structures were characterized to be scopoletin (1), 11,(13)-triene-6,12-olide (2), and 1ß,6α-dihydroxy-4(15)-eudesmene (3) by spectroscopic data. This is the first report of anticomplement activity of isolated compounds from Artemisia rubripes.
Asunto(s)
Artemisia/química , Inactivadores del Complemento/farmacología , Vía Clásica del Complemento/efectos de los fármacos , Escopoletina/farmacología , Sesquiterpenos/farmacología , Animales , Cloroformo/química , Cromatografía Líquida de Alta Presión , Cromatografía en Capa Delgada , Cinamatos/farmacología , Inactivadores del Complemento/química , Inactivadores del Complemento/aislamiento & purificación , Depsidos/farmacología , Flavonoides/farmacología , Hemólisis/inmunología , Concentración 50 Inhibidora , Estructura Molecular , Extractos Vegetales/química , Conejos , Escopoletina/química , Escopoletina/aislamiento & purificación , Sesquiterpenos/química , Sesquiterpenos/aislamiento & purificación , Sesquiterpenos de Eudesmano/química , Sesquiterpenos de Eudesmano/aislamiento & purificación , Sesquiterpenos de Eudesmano/farmacología , Ovinos , Ácido RosmarínicoRESUMEN
The leaves of Angelica anomala Lallemant, Angelica cartilagino-marginata var. distans (Nakai) Kitag, Angelica czernevia (Fisch. et Meyer) Kitagawa, Angelica dahurica Benth. et Hooker, Angelica decursiva (Miq.) Franch. & Sav, Angelica fallax Boissieu, Angelica gigas Nakai, Angelica japonica A. gray were essential oil extracted and immunotoxicity effects were studied. The Angelica anomala, A. cartilagino-marginata var. distans, A. czernevia, A. dahurica, A. decursiva, A. fallax, A. gigas, A. japonica essential oil yield were 4.13, 4.83, 4.45, 3.25, 4.11, 4.73, 4.34 and 4.21%. The A. dahurica essential oil had a significant toxic effect against early fourth-stage larvae of Aedes aegypti L with a lethal concentration 50 (LC50) value of 43.12 ppm and an LC90 value of 65.23 ppm. The above indicates that essential oil contents may play a more important role in the toxicity of essential oil.
Asunto(s)
Aedes/crecimiento & desarrollo , Angelica/química , Insecticidas/farmacología , Aceites Volátiles/farmacología , Animales , Insecticidas/química , Larva/crecimiento & desarrollo , Aceites Volátiles/química , República de CoreaRESUMEN
To examine the neuroprotective effects of Glycine max, we tested its protection against the glutamate-induced toxicity in primary cortical cultured neurons. In order to clarify the neuroprotective mechanism(s) of this observed effect, isolation was performed to seek and identify active fractions and components. From such fractionation, two triterpene glycosides, 3-O-[α-l-rhamnopyranosyl(1-2)-ß-d-glucopyranosyl(1-2)-ß-d-glucuronopyranosyl]olean-12-en-3ß,22ß,24-triol (1) and 3-O-[ß-d-glucopyranosyl(1-2)-ß-d-galactopyranosyl(1-2)-ß-d-glucuronopyranosyl]olean-12-en-3ß,22ß,24-triol (2) were isolated with the methanol extracts with of air-dried Glycine max. Among these compounds, compound 2 exhibited significant neuroprotective activities against glutamate-induced toxicity, exhibiting cell viability of about 50% at concentrations ranging from 0.1 µM to 10 µM. Therefore, the neuroprotective effect of Glycine max might be due to the inhibition of glutamate-induced toxicity by triterpene glycosides.
Asunto(s)
Corteza Cerebral/efectos de los fármacos , Glutamatos/toxicidad , Glycine max/química , Glicósidos/farmacología , Neuronas/efectos de los fármacos , Fármacos Neuroprotectores/farmacología , Saponinas/farmacología , Triterpenos/farmacología , Animales , Células Cultivadas , Corteza Cerebral/citología , Neuronas/citología , Extractos Vegetales/farmacología , Ratas , Ratas Sprague-DawleyRESUMEN
We cloned the gene, CdPAL1, from Cistanche deserticola callus using RACE PCR with degenerate primers that were designed based on a multiple sequence alignment of known PAL genes from other plant species. The gene shows high homology to other known PAL genes registered in GenBank. The recombinant protein exhibited Michaelis-Menten kinetics with a Km of 0.1013 mM, Vmax of 4.858 µmol min(-1), Kcat of 3.36 S(-1), and Kcat/Km is 33,168 M(-1) S(-1). The enzyme had an optimal pH of 8.5 and an activation energy of 38.92 kJ mol(-1) when L-Phenylalanine was used as a substrate; L-tyrosine cannot be used as substrate for this protein. The optimal temperature was 55°C, and the thermal stability results showed that, after a treatment at 70°C for 20 min, the protein retained 87% activity, while a treatment at 75°C for 20 min resulted in a loss of over 85% of the enzyme activity. Treatment with heavy metal ions (Hg2+, Pb2+, and Zn2+) showed remarkable inhibitory effects. Among the intermediates from the lignin (cinnamyl alcohol, cinnamyl aldehyde, coniferyl aldehyde, coniferyl alcohol), phenylpropanoid (cinnamic acid, coumaric acid, caffeic acid, and chlorogenic acid) and phenylethanoid (tyrosol and salidroside) biosynthetic pathways, only cinnamic acid showed strong inhibitory effects against CdPAL1 activity with a Ki of 8 µM. Competitive inhibitor AIP exhibited potent inhibition with Ki=0.056 µM.
Asunto(s)
Cistanche/enzimología , Cistanche/genética , Genes de Plantas/genética , Fenilanina Amoníaco-Liasa/genética , Cistanche/efectos de los fármacos , Electroforesis en Gel de Poliacrilamida , Estabilidad de Enzimas/efectos de los fármacos , Regulación Enzimológica de la Expresión Génica/efectos de los fármacos , Regulación de la Expresión Génica de las Plantas/efectos de los fármacos , Concentración de Iones de Hidrógeno/efectos de los fármacos , Iones , Cinética , Metales Pesados/farmacología , Datos de Secuencia Molecular , Especificidad de Órganos/efectos de los fármacos , Péptidos/química , Fenoles/metabolismo , Fenilanina Amoníaco-Liasa/metabolismo , Proteínas Recombinantes/metabolismo , Alineación de Secuencia , Análisis de Secuencia de Proteína , Espectrofotometría Ultravioleta , TemperaturaRESUMEN
2-Aminoindan-2-phosphonic acid (AIP), a specific competitive phenylalanine ammonia lyase (PAL) inhibitor was applied to a suspension cell culture of Cistanche deserticola. The effects of AIP treatment on cell growth, PAL activity, contents and yields of total phenolic compound, salidroside and four phenylethanoid glycosides (PheGs) are investigated. The results demonstrated that, 0.5 and 2.0 µM AIP treatments had similar effects on the measurements investigated in this study. AIP treatment resulted in significant decreases in PAL activity, total phenolic compounds content, and PheGs content. Linear regression analysis showed that PAL activity had a high correlation coefficient with the total phenolic compound content and the four PheGs contents. Total PAL activity-time area under curve (AUC) had a high correlation coefficient with the total phenolic compound yield and the yields of five tested compounds in untreated cell samples. In AIP-treated cells, total PAL activity-time AUC retained a high correlation with the total phenolic compound yield and the yields of three tested compounds, echinacoside, acteoside, and tubuloside A, but not salidroside and cistanoside A. The difference could be caused by the different biosynthetic origins of each of the tested compounds. These results demonstrate the important role of PAL in the biosynthesis of PheGs in the suspension cell culture of C. deserticola.
Asunto(s)
Cistanche/efectos de los fármacos , Cistanche/metabolismo , Glucósidos/metabolismo , Glicósidos/metabolismo , Organofosfonatos/farmacología , Fenoles/metabolismo , Catecoles , Cromatografía Líquida de Alta Presión , IndanosRESUMEN
We assessed the effects of chloroform extract of fermented Viola mandshurica (CEFV) on melanogenesis B16 melanoma cells. CEFV treatment significantly decreased melanin content and tyrosinase activity in dose-dependent manners. To elucidate the mechanism of the inhibitory effects of CEFV on melanogenesis, we performed RT-PCR and Western blotting for melanogenesis-related genes such as tyrosinase, tyrosinase-related protein-1 (TRP-1), TRP-2, and microphthalmia-associated transcription factor (MITF). CEFV strongly inhibited mRNA as well as the protein expression of tyrosinase and MITF, but had no significant effect on TRP-1 or TRP-2 expressions. It markedly decreased the phosphorylation of cAMP responsive element binding protein (CREB), and induced the duration of extracellular signal-regulated kinase (ERK) activation, leading to reduction of MITF expression and subsequently that of tyrosinase. Therefore, we suggest that CEFV induces downregulation of melanogenesis through decreased CREB phosphorylation and ERK activation.
Asunto(s)
Fermentación , Melaninas/biosíntesis , Melanoma Experimental/metabolismo , Melanoma Experimental/patología , Extractos Vegetales/farmacología , Viola/química , Viola/metabolismo , Animales , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Proteína de Unión a Elemento de Respuesta al AMP Cíclico/metabolismo , Regulación hacia Abajo/efectos de los fármacos , Activación Enzimática/efectos de los fármacos , Quinasas MAP Reguladas por Señal Extracelular/metabolismo , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Espacio Intracelular/efectos de los fármacos , Espacio Intracelular/metabolismo , Melanoma Experimental/enzimología , Melanoma Experimental/genética , Ratones , Factor de Transcripción Asociado a Microftalmía/metabolismo , Monofenol Monooxigenasa/metabolismo , Fosforilación/efectos de los fármacos , Extractos Vegetales/metabolismo , ARN Mensajero/genética , ARN Mensajero/metabolismo , Transducción de Señal/efectos de los fármacosRESUMEN
To evaluate the anti-Helicobacter pylori activity of Hypericum erectum methanol extracts in order to provide the primary evidence for their use in clinical practice. An ethyl acetate fraction of H. erectum suspension-cell cultures inhibited the growth of H. pylori in vitro, with a MIC50 range of 38.7-63.2 µg/mL, comparable to metronidazole (MIC50 = 43.2 µg/mL). To further investigate the involved active compounds of the H. erectum extracts, four phenol glycosides were isolated for the current study: quercetin-3'-O-ß-D-galactopyranoside, quercetin-3'-O-(2''-acetyl)-ß-D-glucopyranoside, 4,6-dihydroxy-2-methoxyphenyl-1-O-ß-D-glucopyranoside and 4-hydroxy-2,6-dimethoxyphenyl-1-O-α-L-rhamnopyranosyl(1-6)-ß-D-glucopyranoside. The MIC50 values of 4,6-dihydroxy-2-methoxyphenyl-1-O-ß-D-glucopyranoside and 4-hydroxy-2,6-dimethoxyphenyl-1-O-α-L-rhamnopyranosyl(1-6)-ß-D-glucopyranoside from ATCC43504 strains were 7.3 and 27.3 µg/mL, respectively. The other two phenol glycosides did not show anti-H. pylori activity. The results of this work suggest that H. erectum has some therapeutic potential against H. pylori infection, which could be explored for patients with gastroduodenal disorders.
Asunto(s)
Glicósidos/farmacología , Helicobacter pylori/efectos de los fármacos , Hypericum/química , Fenoles/farmacología , Extractos Vegetales/farmacología , Galactósidos/farmacología , Pruebas de Sensibilidad Microbiana , Quercetina/análogos & derivados , Quercetina/farmacología , República de CoreaRESUMEN
The present study evaluated the anticomplement effects of isolated compounds from black coloured rice bran in the classical pathway of the complement system. Using column chromatography, three compounds: oryzafuran, quercetin and protocatechuic acid, were isolated and evaluated for in vitro anticomplement activity. Oryzafuran showed the most potent inhibitory activity against the complement system, with 50% inhibitory concentration (IC50) values of 126.2 µg/mL. This is the first report of anticomplement activity of isolated compounds from black coloured rice bran.
Asunto(s)
Vía Clásica del Complemento/efectos de los fármacos , Oryza/química , Extractos Vegetales/farmacología , Animales , Eritrocitos , Hidroxibenzoatos/farmacología , Concentración 50 Inhibidora , Quercetina/farmacología , Conejos , OvinosRESUMEN
To examine the neuroprotective effects of black galingale, its protection was tested against glutamate-induced neurotoxicity in primary cortical cultured neurons. It was found that an aqueous extract of this medicinal plant exhibited significant protection against glutamate-induced toxicity in primary cultured rat cortical cells. In order to clarify the neuroprotective mechanism(s) of this observed effect, isolation was performed to seek and identify active fractions and components. By such fractionation, bioactive methoxyflavone derivatives were isolated from the methanol extracts from the air-dried rhizomes of black galingale. 5-Hydroxy-3,7,3',4'-tetramethoxyflavone exhibited significant neuroprotective activities against glutamate-induced toxicity, exhibiting cell viability of about 60-70%, at concentrations ranging from 0.1 µm to 10 µm. Therefore, the neuroprotective effect of black galingale might be due to the inhibition of glutamate-induced toxicity by the methoxyflavone derivatives it contains.