RESUMO
It is essential to develop novel catalysts with high catalytic activity, strong durability, and good stability for further application in methanol fuel cells. In this work, we present for the first time the effect of the chemical functional groups (thiol and amine) with different electron affinity in reduced graphene oxide supports on the morphology and catalytic activity of platinum nanoparticles for the methanol oxidation reaction. Hydroxyl groups on graphene oxide were initially brominated and then transformed to the desired functional groups. The good dispersion of metal nanoparticles over functionalized carbon substrates (particle size less than 5 nm) with good durability, even at a limited functionalization degree (less than 7%) has been demonstrated by morphological and structural studies. The durability of the catalysts was much improved via strong coordination between the metal and nitrogen or sulfur atoms. Impressively, the catalytic activity of platinum nanoparticles on aminated reduced graphene oxide was found to be much better than that on thiolated graphene oxide despite the weaker affinity between amine and noble metals. These findings support further developing new graphene derivatives with the desired functionalization for electronics and energy applications..
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The use of metal-organic framework materials in electrochemical sensors has been gaining more attention in the last few years due to their highly porous structure and electrocatalytic activity. In this work, a novel paracetamol electrochemical sensor based on a Cu-BTC microporous film electrochemically grown onto glassy carbon electrode was introduced. The Cu-BTC film was deposited directly onto the electrode surface via an electrochemical approach using a Et3N probase to accelerate the growth of Cu-BTC. The fast growth enables the formation of a microporous structure with better adsorption of targeted molecules. The two-dimensional arrangement of units made of dimeric copper cations coordinated to carboxylate anions helped to improve the electrochemical conductivity and electron transfer rate at the electrode surface (charge transfer resistance was dramatically decreased from 2173 Ω to 86 Ω). The electrocatalytic activity of copper ion centers in Cu-BTC was studied with peak separation between oxidation and reduction peaks of pseudo-redox paracetamol molecules much shortened (from 629 mV to 87 mV). Consequently, the sensing parameters (sensitivity and detection limit) of the as-prepared paracetamol sensor were considerably improved. Further works need to be conducted on tailoring ligand structure in order to much improve the electrical conductivity of metal-organic frameworks for sensing purposes.
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Acute lymphoblastic leukemia (ALL) is the hematologic malignancy characterized by the aberrant proliferation of immature lymphoid cells. A20 is a deubiquitinase gene that inhibits functional activation of immune cells mediated through NF-κB/STAT pathways and frequently found inactivated in lymphoma. IL-6 is a pro-inflammatory cytokine secreted by immune cells under the pathogenic conditions and regulated by STAT signaling. Little is known about the role of A20 in regulating the function of ALL blasts and underlying molecular mechanisms. The present study, therefore, explored whether A20 expression contributes to IL-6 induced cell migration and activation of myeloid cells in ALL. To this end, blood samples of thirty-five adult ALL patients were examined. Gene expression profile was determined by quantitative RT-PCR, immunophenotype by flow cytometry, secretion of inflammatory cytokines by ELISA, and cell migration by a transwell migration assay. As a result, the expression of A20 was inactivated in ALL. Immunophenotypic analysis indicated that percent of CD11b+CD40+ expressing cells present in ALL was significantly reduced when transfected with PEM-T easy A20. Importantly, IL6-induced CXCL12-mediated migration of ALL blasts was dependent on the presence of A20. The inhibitory effects of A20 on activated myeloid cells and migration of ALL blasts were mediated through the STAT pathway upon IL-6 challenge. In addition, the CA-125 level was much higher in elderly females than either young female or male ALL patients or healthy donors. In conclusion, the inhibitory effects of A20 on activation of ALL blasts are expected to affect the immune response to treatment for adult ALL patients.
Assuntos
Regulação Leucêmica da Expressão Gênica , Leucemia-Linfoma Linfoblástico de Células Precursoras/metabolismo , Fatores de Transcrição STAT/metabolismo , Transdução de Sinais , Proteína 3 Induzida por Fator de Necrose Tumoral alfa/metabolismo , Idoso , Movimento Celular , Quimiocina CXCL12/metabolismo , Citocinas/metabolismo , Células Dendríticas/citologia , Feminino , Perfilação da Expressão Gênica , Humanos , Sistema Imunitário , Imunofenotipagem , Inflamação , Interleucina-6/metabolismo , Masculino , Pessoa de Meia-Idade , Células Mieloides/metabolismo , NF-kappa B/metabolismoRESUMO
Five new oleanane-type saponins, hirsutosides A - E, were isolated from the leaves of Glochidion hirsutum (Roxb.) Voigt. Their structures were elucidated as 21ß-benzoyloxy-3ß,16ß,23,28-tetrahydroxyolean-12-ene 3-O-ß-d-glucopyranoside (1), 21ß-benzoyloxy-3ß,16ß,23,28-tetrahydroxyolean-12-ene 3-O-ß-d-glucopyranosyl-(1 â 3)-ß-d-glucopyranoside (2), 21ß-benzoyloxy-3ß,16ß,23,28-tetrahydroxyolean-12-ene 3-O-6-acetyl-[ß-d-glucopyranosyl-(1 â 3)]-ß-d-glucopyranoside (3), 21ß-benzoyloxy-3ß,16ß,23,28-tetrahydroxyolean-12-ene 3-O-ß-d-glucopyranosyl-(1 â 3)-ã-l-arabinopyranoside (4), and 21ß-benzoyloxy-3ß,16ß,23-trihydroxyolean-12-ene-28-al 3-O-ß-d-glucopyranosyl-(1 â 3)-α-l-arabinopyranoside (5). All isolated compounds were evaluated for cytotoxic activities on four human cancer cell lines, HepG-2, A-549, MCF-7, and SW-626 using the SRB assay. Compounds 1, 2, 4, and 5 showed significant cytotoxic activities against all human cancer cell lines with IC50 values ranging from 3.4 to 10.2 µm. Compound 3 containing acetyl group at glc C(6â³) exhibited weak cytotoxic activity with IC50 values ranging from 47.0 to 54.4 µm.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Magnoliopsida/química , Saponinas/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Ácido Oleanólico/análogos & derivados , Folhas de Planta/químicaRESUMO
Two new lignans (7S,7'R,8S,8'R)-3,3'-dimethoxy-7,7'-epoxylignan-4,4',9-triol 4-O-ß-D-glucopyranoside (1) and 9-O-formylaviculin (2) together with other thirteen known secondary metabolites were isolated from the leaves of Antidesma hainanensis. Their chemical structures were determined using NMR, electrospray ionization (ESI)-MS, circular dichroism (CD) spectroscopic methods, and as well as by comparison with those reported in the literature. Neuro-inflammatory activity of isolated compounds was evaluated by their inhibition on nitric oxide (NO) production in activated BV2 microglial cells. At concentration of 40 µM, compounds 1-3, 5, 7, 8, 9, 14, and 15 exhibited inhibitory effects over 50%, suggesting that they could be potential candidate drugs for the cure of neuro-inflammation. In addition, compounds 1, 8, 14, and 15 significantly inhibited 16.23, 27.76, 21.23, and 29.44% NO production at diluted concentration as low as 2.5 µM.
Assuntos
Lignanas/farmacologia , Microglia/efeitos dos fármacos , Microglia/metabolismo , Óxido Nítrico/biossíntese , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Relação Dose-Resposta a Droga , Humanos , Lignanas/química , Lignanas/isolamento & purificação , Lipopolissacarídeos/farmacologia , Microglia/citologia , Estrutura Molecular , Folhas de Planta/química , Relação Estrutura-AtividadeRESUMO
Chemical investigation of the EtOAc extracts of marine-derived fungal isolates Aspergillus sp. SF-5974 and Aspergillus sp. SF-5976 yielded a new dihydroisocoumarin derivative (1) and 12 known metabolites. The structures of the isolated metabolites were established by extensive spectroscopic analyses, including 1D and 2D NMR spectra and MS data. Among the metabolites, the absolute configuration of 5'-hydroxyasperentin (6) was determined by single-crystal X-ray diffraction analysis. The in vitro antineuroinflammatory effects of the metabolites were also evaluated in lipopolysaccharide (LPS)-stimulated microglial cells. Among the isolated metabolites, dihydroisocoumarin derivatives 1-6 (10-80 µM) were shown to inhibit LPS-induced nitric oxide (NO) and prostaglandin E2 (PGE2) production by suppressing the expression of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2), respectively, in LPS-stimulated BV2 microglia. Further, 1 (20-80 µM) was found to suppress the phosphorylation of the inhibitor of nuclear factor kappa B-α (IκB-α), interrupt the nuclear translocation of nuclear factor kappa B (NF-κB), and decrease the activation of p38 mitogen-activated protein kinase (MAPK).
Assuntos
Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Aspergillus/química , Isocumarinas/isolamento & purificação , Isocumarinas/farmacologia , Lipopolissacarídeos/farmacologia , Microglia/efeitos dos fármacos , Anti-Inflamatórios/química , Ciclo-Oxigenase 2/efeitos dos fármacos , Ciclo-Oxigenase 2/metabolismo , Dinoprostona/metabolismo , Proteínas I-kappa B , Isocumarinas/química , Biologia Marinha , Estrutura Molecular , Inibidor de NF-kappaB alfa , NF-kappa B/antagonistas & inibidores , Óxido Nítrico/biossíntese , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Óxido Nítrico Sintase Tipo II/efeitos dos fármacos , Ressonância Magnética Nuclear Biomolecular , Fosforilação , Proteínas Quinases p38 Ativadas por Mitógeno/antagonistas & inibidoresRESUMO
A chemical investigation of the methanol extract from the roots of Cudrania tricuspidata resulted in the isolation of 16 compounds, including prenylated xanthones 1-9 and flavonoids 10-16. Their structures were identified by NMR spectroscopy and mass spectrometry and comparisons with published data. Compounds 1-9 and 13-16 significantly inhibited PTP1B activity in a dose dependent manner, with IC50 values ranging from 1.9-13.6 µM. Prenylated xanthones showed stronger PTP1B inhibitory effects than the flavonoids, suggesting that they may be promising targets for the future discovery of novel PTP1B inhibitors. Furthermore, kinetic analyses indicated that compounds 1 and 13 inhibited PTP1B in a noncompetitive manner; therefore, they may be potential lead compounds in the development of anti-obesity and -diabetic agents.
Assuntos
Moraceae/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Proteína Tirosina Fosfatase não Receptora Tipo 1/antagonistas & inibidores , Catálise/efeitos dos fármacos , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Humanos , Hidrólise/efeitos dos fármacos , Concentração Inibidora 50RESUMO
Four new cembranoid diterpenes lobocrasols A-D (1-4), were isolated from the methanol extract of the soft coral Lobophytum crassum. Their structures were elucidated by spectroscopic analysis and by comparison of the spectroscopic data with those of similar compounds previously reported in literature. The anti-inflammatory effects of isolated compounds were evaluated using NF-κB luciferase and reverse transcription polymerase chain reaction (RT-PCR). Compounds 1 and 2 significantly inhibited TNFα-induced NF-κB transcriptional activity in HepG2 cells in a dose-dependent manner, with IC50 values of 6.30±0.42 and 6.63±0.11µM, respectively. Furthermore, the transcriptional inhibition of these compounds was confirmed by a decrease in cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) gene expression levels in HepG2 cells.
Assuntos
Antozoários/química , Anti-Inflamatórios não Esteroides/farmacologia , Diterpenos/farmacologia , NF-kappa B/antagonistas & inibidores , Translocação Genética/efeitos dos fármacos , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Diterpenos/química , Diterpenos/isolamento & purificação , Relação Dose-Resposta a Droga , Células Hep G2 , Humanos , Estrutura Molecular , NF-kappa B/genética , NF-kappa B/metabolismo , Relação Estrutura-Atividade , Translocação Genética/genética , Fator de Necrose Tumoral alfa/farmacologiaRESUMO
Chemical investigation of a marine-derived fungus Penicillium sp. SF-6013 resulted in the discovery of a new tanzawaic acid derivative, 2E,4Z-tanzawaic acid D (1), together with four known analogues, tanzawaic acids A (2) and D (3), a salt form of tanzawaic acid E (4), and tanzawaic acid B (5). Their structures were mainly determined by analysis of NMR and MS data, along with chemical methods. Preliminary screening for anti-inflammatory effects in lipopolysaccharide (LPS)-activated microglial BV-2 cells showed that compounds 1, 2, and 5 inhibited the production of nitric oxide (NO) with IC50 values of 37.8, 7.1, and 42.5 µM, respectively. Compound 2 also inhibited NO production in LPS-stimulated RAW264.7 murine macrophages with an IC50 value of 27.0 µM. Moreover, these inhibitory effects correlated with the suppressive effect of compound 2 on inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression in LPS-stimulated RAW264.7 and BV2 cells. In addition, compounds 2 and 5 significantly inhibited the activity of protein tyrosine phosphatase 1B (PTP1B) with the same IC50 value (8.2 µM).
Assuntos
Anti-Inflamatórios/química , Inibidores Enzimáticos/química , Ácidos Graxos Insaturados/química , Penicillium/metabolismo , Proteína Tirosina Fosfatase não Receptora Tipo 1/antagonistas & inibidores , Tetra-Hidronaftalenos/química , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Linhagem Celular , Ciclo-Oxigenase 2/metabolismo , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/farmacologia , Ácidos Graxos Insaturados/isolamento & purificação , Ácidos Graxos Insaturados/farmacologia , Lipopolissacarídeos/toxicidade , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Espectroscopia de Ressonância Magnética , Camundongos , Conformação Molecular , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Penicillium/química , Ligação Proteica , Proteína Tirosina Fosfatase não Receptora Tipo 1/metabolismo , Tetra-Hidronaftalenos/isolamento & purificação , Tetra-Hidronaftalenos/farmacologiaRESUMO
Nine cembranoid diterpenes 1-9, including four new compounds, crassumols D-G (1-4), were isolated from the methanol extract of the Vietnamese soft coral Lobophytum crassum. Spectroscopic methods were used to elucidate the structures of these compounds. Compound 5 exhibited a potent inhibitory effect on tumor necrosis factor-alpha (TNFα)-induced nuclear factor-kappa B (NF-κB) transcriptional activation in HepG2 cells and significantly inhibited the mRNA expression of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) in a dose-dependent manner.
Assuntos
Antozoários/química , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Diterpenos/química , Diterpenos/farmacologia , Fator de Necrose Tumoral alfa/imunologia , Animais , Anti-Inflamatórios/isolamento & purificação , Ciclo-Oxigenase 2/genética , Diterpenos/isolamento & purificação , Células Hep G2 , Humanos , NF-kappa B/genética , Óxido Nítrico Sintase Tipo II/genética , RNA Mensageiro/genética , Ativação Transcricional/efeitos dos fármacosRESUMO
Talaromyces sp. DC2 is an endophytic fungus that was isolated from the stem of Catharanthus roseus (L.) G. Don in Hanoi, Vietnam and is capable of producing vinca alkaloids. This study utilizes the PacBio Sequel technology to completely sequence the whole genome of Talaromyces sp. DC2The genome study revealed that DC2 contains a total of 34.58 Mb spanned by 156 contigs, with a GC content of 46.5%. The identification and prediction of functional protein-coding genes, tRNA, and rRNA were comprehensively predicted and highly annotated using various BLAST databases, including non-redundant (Nr) protein sequence, Gene Ontology (GO), Kyoto Encyclopedia of Genes and Genomes (KEGG), Clusters of Orthologous Groups (COG), and Carbohydrate-Active Enzymes (CAZy) databases. The genome of DC2 has a total of 149, 227, 65, 153, 53, and 6 genes responsible for cellulose, hemicellulose, lignin, pectin, chitin, starch, and inulin degradation, respectively. The Antibiotics and Secondary Metabolites Analysis Shell (AntiSMASH) analyses revealed that strain DC2 possesses 20 biosynthetic gene clusters responsible for producing secondary metabolites. The strain DC2 has also been found to harbor the DDC gene encoding aromatic L-amino acid decarboxylase enzyme. Conclusively, this study has provided a comprehensive understanding of the processes involved in secondary metabolites and the ability of the Talaromyces sp. DC2 strain to degrade plant cell walls.
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Anti-inflammatory and peroxisome proliferator-activated receptors (PPARs) transactivational effects of nine compounds (1 - 9) from the roots of Sophora flavescens were evaluated using NF-κB-luciferase, reverse transcriptase polymerase chain reaction, peroxisome proliferator response element (PPRE)-luciferase, and GAL-4-PPAR chimera assays. Compounds 4 and 8 significantly inhibited TNFα-induced NF-κB transcriptional activity in HepG2 cells in a dose-dependent manner, with IC50 values of 4.0 and 4.4 µM, respectively. Furthermore, the transcriptional inhibitory function of these compounds was confirmed by a decrease in cyclooxgenase 2 and inducible nitric oxide synthase gene expression levels in HepG2 cells. Compounds 1, 3, 5, 6, 8, and 9 significantly activated the transcription of PPARs in a dose-dependent manner, with EC50 values ranging from 1.1 to 13.0 µM. Compounds 1, 3, 5, 6, 8, and 9 exhibited dose-dependent PPARα transactivational activity, with EC50 values in a range of 0.9 - 16.0 µM. Compounds 1, 3, 8, and 9 also significantly upregulated PPARγ activity in a dose-dependent manner, with EC50 values of 10.5, 6.6, 15.7, and 1.6 µM, whereas compounds 1, 8, and 9 demonstrated transactivational PPARß(δ) effects with EC50 values of 11.4, 10.3, and 1.5 µM, respectively. These results provide a scientific rationale for the use of the roots of S. flavescens and warrant further studies to develop new agents for the prevention and treatment of inflammatory and metabolic diseases.
Assuntos
Anti-Inflamatórios/farmacologia , Flavonoides/farmacologia , Receptores Ativados por Proliferador de Peroxissomo/agonistas , Raízes de Plantas/química , Sophora/química , Ativação Transcricional/efeitos dos fármacos , Ciclo-Oxigenase 2/metabolismo , Células Hep G2 , Humanos , NF-kappa B/antagonistas & inibidores , NF-kappa B/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Receptores Ativados por Proliferador de Peroxissomo/classificação , Extratos Vegetais/farmacologia , Fator de Necrose Tumoral alfa/metabolismoRESUMO
In this study, strain DM10 was isolated from mangrove roots and characterized as a halotolerant plant growth-promoting bacterium. Strain DM10 exhibited the ability to solubilize phosphate, produce siderophore, show 1-aminocyclopropane-1-carboxylic acid deaminase activity, and hydrolyze starch. The rice plants subjected to a treatment of NaCl (200 mM) and inoculated with strain DM10 showed an improvement in the shoot length, root length, and dried weight, when compared to those exposed solely to saline treatment. The comprehensive genome sequencing of strain DM10 revealed a genome spanning of 4,171,745 bp, harboring 3626 protein coding sequences. Within its genome, strain DM10 possesses genes responsible for both salt-in and salt-out strategies, indicative of a robust genetic adaptation aimed at fostering salt tolerance. Additionally, the genome encodes genes involved in phosphate solubilization, such as the synthesis of gluconic acid, high-affinity phosphate transport systems, and alkaline phosphatase. In the genome of DM10, we identified the acdS gene, responsible for encoding 1-aminocyclopropane-1-carboxylate deaminase, as well as the amy1A gene, which encodes α-amylase. Furthermore, the genome of DM10 contains sequences associated with the iron (3+)-hydroxamate and iron uptake clusters, responsible for siderophore production. Such data provide a deep understanding of the mechanism employed by strain DM10 to combat osmotic and salinity stress, facilitate plant growth, and elucidate its molecular-level behaviors.
RESUMO
Phytochemical study on the roots of Asarum sieboldii resulted in the isolation of one new compound, (1R,2S,5R,6R)-5'-O-methylpluviatilol (1) and 12 known compounds (2-13). Their structures were determined by extensive spectroscopic methods, including 1D and 2D NMR, and MS spectra. The absolute configuration of compound 1 was established using CD spectrum. Compounds 4, 5, and 12/13 significantly inhibited TNFα-induced NF-κB transcriptional activity in HepG2 cells in a dose-dependent manner, with IC(50) values ranging from 6.4 to 9.4 µM. Furthermore, the transcriptional inhibitory function of these compounds was confirmed based on decreases in COX-2 and iNOS gene expression in HepG2 cells. Compounds 1-3, 6,7, 10, and 11 significantly activated the transcriptional activity of PPARs in a dose-dependent manner, with EC(50) values ranging from 1.7 to 20.9 µM. Compounds 7, 10, and 11 exhibited significant dose-dependent PPARα transactivational activity, with EC(50) values of 19.5, 15.7, and 4.0 µM, respectively. Compounds 1, 6, 7, 10, and 11 activated PPARγ transcriptional activity, with EC(50) values ranging from 3.6 to 22.6 µM, whereas compounds 10 and 11 significantly increased PPARß(δ) transactivational activity, with EC(50) values of 22.6 and 4.9 µM, respectively. These results provide a scientific support for the use of the roots of A. sieboldii and warrant further studies to develop new agents for the prevention and treatment of the inflammatory and metabolic diseases.
Assuntos
Anti-Inflamatórios/farmacologia , Asarum/química , Furanos/farmacologia , PPAR alfa/agonistas , Fenóis/farmacologia , Raízes de Plantas/química , Ativação Transcricional/efeitos dos fármacos , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Ciclo-Oxigenase 2/genética , Ciclo-Oxigenase 2/metabolismo , Relação Dose-Resposta a Droga , Furanos/química , Furanos/isolamento & purificação , Células Hep G2 , Humanos , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Inflamação/patologia , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , NF-kappa B/genética , NF-kappa B/metabolismo , Óxido Nítrico Sintase Tipo II/genética , Óxido Nítrico Sintase Tipo II/metabolismo , PPAR alfa/genética , Fenóis/química , Fenóis/isolamento & purificação , República da Coreia , Transcrição Gênica/efeitos dos fármacos , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/metabolismoRESUMO
In the screening search for NF-κB inhibitory and PPAR transactivational agents from medicinal plants, a methanol extract of the whole plant of Tacca plantaginea and its aqueous fraction showed the significant activities. Bioassay-guided fractionation combined with repeated chromatographic separation of the aqueous fraction of the methanol extract of T. plantaginea resulted in the isolation of two new diarylheptanoid glycosides, plantagineosides A (1) and B (2), an unusual new cyclic diarylheptanoid glycoside, plantagineoside C (3), and three known compounds (4-6). Their structures were determined by extensive spectroscopic and chemical methods. Compounds 3-6 significantly inhibited TNFα-induced NF-κB transcriptional activity in HepG2 cells in a dose-dependent manner, with IC(50) values ranging from 0.9 to 9.4 µM. Compounds 1-6 significantly activated the transcriptional activity of PPARs in a dose-dependent manner, with EC(50) values ranging from 0.30 to 10.4 µM. In addition, the transactivational effects of compounds 1-6 were evaluated on three individual PPAR subtypes, including PPARα, γ, and ß(δ). Compounds 1-6 significantly enhanced the transcriptional activity of PPARß(δ), with EC(50) values in a range of 11.0-30.1 µM. These data provide the rationale for using T. plantaginea and its components for the prevention and treatment of inflammatory and metabolic diseases.
Assuntos
Diarileptanoides/química , Dioscoreaceae/química , Glicosídeos/química , NF-kappa B/metabolismo , Receptores Ativados por Proliferador de Peroxissomo/metabolismo , Transcrição Gênica/efeitos dos fármacos , Antimetabólitos/química , Antimetabólitos/farmacologia , Diarileptanoides/farmacologia , Ativação Enzimática/efeitos dos fármacos , Glicosídeos/farmacologia , Células Hep G2 , Humanos , Espectroscopia de Ressonância Magnética , Metanol/química , Estrutura MolecularRESUMO
A novel withanolide glucoside, plantagiolide I (1), a new withanolide glucoside, plantagiolide J (2), and six known compounds (3-8) were isolated from the whole plant of Tacca plantaginea. Their structures were determined by spectroscopic and chemical methods. Compound 3 significantly inhibited tumor necrosis factor alpha (TNFα)-induced nuclear factor-kappaB (NF-κB) transcriptional activity in HepG2 cells in a dose-dependent manner, with IC(50) values of 9.0 µM. Compounds 1-8 enhanced the transcriptional activity of peroxisome proliferator-activated receptors (PPARs) in a dose-dependent manner, with EC(50) values ranging from 1.6 to 49.7 µM. In addition, the transactivational effects of compounds 1-8 on three individual PPAR subtypes, including PPARα, ß(δ), and γ were evaluated. Compounds 1-8 significantly activated the transcriptional activity of PPARß(δ), with EC(50) values in a ranging from 4.1 to 29.6 µM. These results provide scientific support for the use of T. plantaginea and its components for the prevention and treatment of inflammatory and metabolic diseases.
Assuntos
Dioscoreaceae/química , Glucosídeos/farmacologia , NF-kappa B/antagonistas & inibidores , Receptores Ativados por Proliferador de Peroxissomo/metabolismo , Extratos Vegetais/farmacologia , Ativação Transcricional/efeitos dos fármacos , Vitanolídeos/farmacologia , Relação Dose-Resposta a Droga , Glucosídeos/química , Glucosídeos/isolamento & purificação , Células Hep G2 , Humanos , Conformação Molecular , NF-kappa B/metabolismo , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Relação Estrutura-Atividade , Células Tumorais Cultivadas , Vitanolídeos/química , Vitanolídeos/isolamento & purificaçãoRESUMO
In this paper, a novel bimetallic Fe-Cu metal-organic framework combined with 1,3,5-benzenetricarboxylic acid (Fe-Cu-BTC) are synthesized using hydrothermal reaction. The bimetallic Fe-Cu-BTC with high BET (1504 cm3 g-1) and high Langmuir surface area (1831 cm3 g-1) is composited by gold nanoparticles to improve the conductivity and to develop their synergistic effect. A novel bisphenol A (BPA) sensor was prepared by dropcasting Fe-Cu-BTC on glassy carbon electrodes (GCE) followed by AuNPs electrodeposition. The Fe-Cu-BTC framework were characterized by X-ray photoelectron spectroscopy (XPS), X-ray diffraction (XRD), scanning electron microscopy (SEM), transmission electron microscopy studies (TEM), FT-IR, BET measurements and EDX spectra. Cyclic voltammetry (CV) and differential pulse voltammetry (DPV) were carried out for surveying the electrochemical properties of the sensors and for the quantification of BPA. Two linear ranges of BPA concentrations 0.1-1.0 µM and 1.0-18 µM with 18 nM limit of detection were obtained. The developed sensor was used to measure the concentration of BPA in samples extracted from rain coat with the recovery ranging from 85.70 to 103.23%.
RESUMO
Chemical investigation of a peanut-associated fungal strain Aspergillus niger IMBC-NMTP01 resulted in isolation and identification of 14 secondary metabolites, including two new, epi-aspergillusol (1) and aspernigin (3), and 12 known compounds: pyrophen (2), 2-(hydroxyimino)-3-(4-hydroxyphenyl)propanoic acid (4), aspergillusol A (5), rubrofusarin B (6), nigerasperone A (7), fonsecin (8), TMC-256C1 (9), pyranonigrin A (10), orlandin (11), nigerasperone C (12), asperpyrone A (13), and 5-(hydroxymethyl)-2-furancarboxylic acid (14). Compounds 9, 12-14 showed cytotoxicity toward all six human cancer cell lines, including HepG2, KB, HL-60, MCF-7, SK-Mel2, and LNCaP, with IC50 values ranging from 8.4 to 84.5 µM, compounds 3-5 were cytotoxic against five cancer cell lines except HepG2, whereas 1 exhibited cytotoxicity toward HepG2, KB, and MCF-7 cells. All of the compounds, except 2 and 13, inhibited NO overproduction in LPS-induced RAW264.7 cells. In addition, all of the compounds displayed antimicrobial effects against Enterococcus faecalis, whereas 13 compounds, except 10, significantly inhibited the growth of the yeast Candida albicans.
Assuntos
Anti-Infecciosos , Aspergillus niger , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Arachis , Linhagem Celular Tumoral , Humanos , Células MCF-7 , Estrutura MolecularRESUMO
Penicillium is a rich source of bioactive compounds. Among all Penicillium species, Penicillium oxalicum has been reported to produce various types of secondary metabolites, including alkaloids, phenolics, and tetrahydroxanthone dimeric compounds, exhibiting many pharmacological effects, such as antiviral, antibacterial, and cytotoxic activities. Three secondary metabolites were isolated from a fermented culture of the sponge-associated fungal strain P. oxalicum CLC-MF05: oxaline (1), isorhodoptilometrin (2), and 5-hydroxy-7-(2'-hydroxypropyl)-2-methyl-chromone (3). Their chemical structures were identified by 1D and 2D NMR and high-resolution mass spectroscopic analyses and compared with previously reported data. All three compounds inhibited NO and PGE2 overproduction and iNOS and COX-2 overexpression in both LPS-stimulated BV2 and rat primary microglia. These metabolites also repressed mRNA expression of TNF-α, IL-1ß, IL-6, and IL-12. Further, mechanistic studies revealed that the inhibitory actions of compounds 1-3 were regulated by the inactivation of the NF-κB and MAPK signaling pathways. Furthermore, inactivation of the TLR4/MyD88 pathway contributed to the anti-neuroinflammatory activity of these compounds. These results suggest that compounds 1-3 represent potential anti-inflammatory candidates for the treatment of neurodegenerative diseases; however, further investigation is needed.
Assuntos
Anti-Inflamatórios/farmacologia , Microglia/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Penicillium , Poríferos , Animais , Anti-Inflamatórios/química , Organismos Aquáticos , Lipopolissacarídeos , Camundongos , NF-kappa B/metabolismo , Fármacos Neuroprotetores/química , Células RAW 264.7/efeitos dos fármacos , RatosRESUMO
A new iridoid, named methylscutelloside (1) together with 19 known compounds belonging to the iridoids (2-4), monoterpenoids (5), flavonoids (6-8), triterpenoids (9-14), and phenylethanoids (15-20) were isolated from the flowers of Buddleja officinalis. Their chemical structures were elucidated on the basis of physicochemical properties, and by spectroscopic methods including 1D, 2D NMR, and MS. All isolated compounds were tested in vitro for their effects on the proliferation of rat aortic vascular smooth muscle cells (VSMCs). Among them, iridoids were the main active components and showed significant inhibitory effects on PDGF-BB-induced proliferation in rat aortic VSMCs.