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1.
Lipids Health Dis ; 19(1): 24, 2020 Feb 08.
Artículo en Inglés | MEDLINE | ID: mdl-32035489

RESUMEN

BACKGROUND: The LDL-C lowering effect of ezetimibe has been attributed primarily to increased catabolism of LDL-C via up-regulation of LDL receptor (LDLR) and decreased cholesterol absorption. Recently, ezetimibe has been demonstrated to have reverse cholesterol transport (RCT) promoting effects in mice, hamsters and humans. However, the underlying mechanisms are still not clear. The aim of this study is to investigate whether ezetimibe improves RCT-related protein expression in LDLR-/- hamsters. METHODS: A high-fat diet was used to induce a human-like hyperlipidemia in LDLR-/- hamsters. Lipid profiles were assayed by commercially available kits, and the effects of ezetimibe on lipid metabolism-related protein expression were carried out via western blot. RESULTS: Our data demonstrated that ezetimibe administration significantly reduced plasma total cholesterol (~ 51.6% reduction, P < 0.01) and triglyceride (from ~ 884.1 mg/dL to ~ 277.3 mg/dL) levels in LDLR-/- hamsters fed a high-fat diet. Ezetimibe administration (25 mg/kg/d) significantly promoted the protein expression of cholesterol 7 alpha-hydroxylase A1 (CYP7A1), LXRß and peroxisome proliferator-activated receptor (PPAR) γ; and down-regulated the protein expression of PPARα and PPARß. However, it showed no significant effect on sterol regulatory element-binding protein (SREBP)-1c, SREBP-2, proprotein convertase subtilisin/kexin type 9 (PCSK9), Niemann-Pick C1-like 1 (NPC1L1), and ATP-biding cassette (ABC) G5/G8. CONCLUSION: Ezetimibe may accelerate the transformation from cholesterol to bile acid via promoting CYP7A1 and thereby enhance RCT. As a compensatory mechanism of TG lowering, ezetimibe promoted the protein expression of PPARγ and decreased PPARα and ß. These results are helpful in explaining the lipid-lowering effects of ezetimibe and the potential compensatory mechanisms.


Asunto(s)
Colesterol 7-alfa-Hidroxilasa/metabolismo , Ezetimiba/farmacología , Receptores Activados del Proliferador del Peroxisoma/metabolismo , Receptores de LDL/metabolismo , Animales , Transporte Biológico/efectos de los fármacos , Western Blotting , Colesterol/metabolismo , Cricetinae , Dieta Alta en Grasa , Metabolismo de los Lípidos/efectos de los fármacos , Receptores de LDL/deficiencia , Receptores de LDL/genética
2.
Biomed Chromatogr ; 34(8): e4845, 2020 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-32267542

RESUMEN

An ultra-high performance liquid chromatography tandem mass spectrometry method was developed for determination of homocysteine (HCY) in human plasma. The HCY was derivatized with 2-chloro-1-methylquinolinium tetrafluoroborate and isolated using solid-phase extraction. Derivatization, isolation and detection procedures were optimized. Satisfactory linearity was obtained with determination coefficients (r2 ) >0.999. The intra- and inter-day precisions were in the interval of 1.2-5.1% and accuracy was within ±7%. Mean recoveries were close to 100%. The limit of detection and the limit of quantification were 0.46 and 1.38 µmol/L, respectively. The method was then applied to investigate the relationship between plasma HCY and whole blood 5-methyltetrahydrofolate levels in healthy volunteers. The results revealed that the plasma level of HCY was significantly negatively correlated to whole blood 5-methyltetrahydrofolate in volunteers.


Asunto(s)
Cromatografía Líquida de Alta Presión/métodos , Homocisteína/sangre , Espectrometría de Masas en Tándem/métodos , Tetrahidrofolatos/sangre , Adulto , Estabilidad de Medicamentos , Femenino , Humanos , Límite de Detección , Modelos Lineales , Masculino , Reproducibilidad de los Resultados , Adulto Joven
3.
Chem Biodivers ; 17(2): e1900640, 2020 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-31805214

RESUMEN

The extract of the strain Aspergillus flavipes DL-11 exerted antibacterial activities against six Gram-positive bacteria. During the following bioassay-guided separation, ten diphenyl ethers (1-10), two benzophenones (11-12), together with two xanthones (13-14) were isolated. Among them, 4'-chloroasterric acid (1) was a new chlorinated diphenyl ether. Their structures were elucidated by extensive spectroscopic data analysis, including IR, HR-ESI-MS, NMR experiments, and by comparison with the literature data. All compounds showed moderate to strong antibacterial effects on different Gram-positive bacteria with MIC values that ranged from 3.13 to 50 µg/mL, but none of the compounds exhibited activity against Gram-negative bacteria Vibrio parahaemolyticus ATCC17802 (MIC>100 µg/mL). In particular, the MICs of some compounds are at the level of positive control.


Asunto(s)
Antibacterianos/química , Aspergillus/química , Benzofenonas/química , Éteres Fenílicos/química , Xantonas/química , Antibacterianos/aislamiento & purificación , Antibacterianos/farmacología , Aspergillus/metabolismo , Benzofenonas/aislamiento & purificación , Benzofenonas/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Conformación Molecular , Éteres Fenílicos/aislamiento & purificación , Éteres Fenílicos/farmacología , Xantonas/aislamiento & purificación , Xantonas/farmacología
4.
J Org Chem ; 84(3): 1299-1309, 2019 02 01.
Artículo en Inglés | MEDLINE | ID: mdl-30589544

RESUMEN

Enzyme-activated fluorogenic probes, which invoke enzymatic catalysis to trigger the generation of fluorescence, provide a versatile platform for monitoring biological processes. The development of fluorogenic probes that can readily penetrate the cell envelopes of bacteria are essential to examine intracellular targets of live bacterial cells. Herein, we present the design, synthesis, properties, and biological applications of two series of fluorogenic probes based on cyanine 5 for identification of bacterial nitroreductase (NTR). The selected fluorogenic probe 3 generates a rapid 10-fold fluorescence response after being catalytically reduced by NTR to the intermediate para-aminobenzyl substituted which then underwent a rearrangement elimination reaction. Moreover, probe 3 is cell permeable for both Gram-positive and Gram-negative bacterial cell envelopes and is selective for NTR over other biological analytes, thus minimizing the background signal and enabling the real-time intracellular imaging of NTR in live bacterial cells.


Asunto(s)
Bacterias/química , Colorantes Fluorescentes/síntesis química , Nitrorreductasas/química , Fluorescencia , Colorantes Fluorescentes/química , Humanos , Nitrorreductasas/metabolismo
5.
Zhongguo Zhong Yao Za Zhi ; 44(4): 774-780, 2019 Feb.
Artículo en Zh | MEDLINE | ID: mdl-30989891

RESUMEN

In this experiment,the antioxidant capacity of raspberry extract and the protective effect on liver injury induced by ConA in mice were investigated. Balb/C male mice were randomly divided into six groups: normal group,model group,bicyclol control group( 200 mg·kg~(-1)),low-dose raspberry extract group( 200 mg·kg~(-1)),middle-dose raspberry extract group( 400 mg·kg~(-1)),and highdose raspberry extract group( 800 mg·kg~(-1)). Each group was intragastrically administered with drugs according to the body weight once a day. Seven days later,all of the groups except for the normal group were treated with ConA( 20 mg·kg~(-1)) through tail vein injection to establish the acute liver injury model. The mice were put to death 8 hours later. The organ indexes were calculated. These rum levels of ALT,AST and LDH and the activities of SOD,CAT,GSH and MDA in liver tissue were detected. HE staining was used to observe the pathological changes of liver tissue in mice. Western blot was used to detect the expressions of Bax,Bcl-2,Nrf2 and Keap-1. The antioxidant capacity of raspberry extract was measured by CAA assay. The results showed that,raspberry extract had a strong antioxidant capacity. Simultaneously,compared with the model group,raspberry extract can significantly improve the pathological conditions of liver,and significantly reduce ALT,AST and LDH activities in serum of liver injury mice( P<0. 01). The activities of SOD,CAT in liver homogenate supernatant were significantly increased in the high-dose group,the content of GSH increased,while the content of MDA was sharply declined in the high-dose group( P<0. 01). Meanwhile,raspberry extract down-regulated the expressions of Bax and Keap-1 and up-regulated the expressions of Bcl-2 and Nrf2. CAA showed that the compound raspberry extract had a strong antioxidant capacity. Therefore,raspberry extract has an obvious protective effect on acute liver injury induced by ConA in mice.


Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas , Rubus , Animales , Antioxidantes , Hígado , Masculino , Ratones , Ratones Endogámicos BALB C , Sustancias Protectoras
6.
J Environ Sci (China) ; 67: 127-135, 2018 May.
Artículo en Inglés | MEDLINE | ID: mdl-29778144

RESUMEN

The effects of tourmaline on nitrogen removal performance and biofilm structures were comparatively investigated in two identical laboratory-scale sequencing batch biofilm reactors (SBBRs) (denoted SBBR1 and SBBR2) at different nitrogen loading rates (NLRs) varying from (0.24±0.01) to (1.26±0.02) g N/(L·day). SBBR1 was operated in parallel with SBBR2, but SBBR1 was filled with polyurethane foam loaded tourmaline (TPU) carriers and another (SBBR2) filled with polyurethane foam (PU) carriers. Results obtained from this study showed that the excellent and stable performance of SBBR1 was obtained. Ammonia nitrogen removal and total nitrogen removal were higher in SBBR1 than that in SBBR2 with increase of NLR. At an NLR of (0.24±0.01) g N/(L·day), the majority of the spherical and elliptical bacteria were surrounded by the extracellular polymeric substance (EPS) and bacillus or filamentous bacteria in two SBBRs biofilms. When NLR increased to (1.26±0.02) g N/(L·day), the clusters were more obvious in the SBBR1 biofilm than that in the SBBR2 biofilm. Bacteria in SBBR1 were inclined to synthesis more EPS, and the formed EPS could protect the bacteria from free ammonia (FA) under extreme condition NLR (1.26±0.02) g N/(L·day). The results of polymerase chain reaction-denaturing gradient gel electrophoresis analysis showed that the microbial community similarity in SBBR2 decreased more obviously than that in SBBR1 with the increase of NLR, which the microbial community in SBBR1 was relatively stable.


Asunto(s)
Biopelículas/efectos de los fármacos , Nitrógeno/metabolismo , Silicatos/metabolismo , Eliminación de Residuos Líquidos/métodos , Contaminantes del Agua/metabolismo , Biopelículas/crecimiento & desarrollo , Nitrógeno/análisis , Contaminantes del Agua/análisis
7.
Zhongguo Zhong Yao Za Zhi ; 43(4): 755-759, 2018 Feb.
Artículo en Zh | MEDLINE | ID: mdl-29600651

RESUMEN

Trace chemical constituents from the ethyl acetate extract of Red Yeast Rice were investigated. Four phenolic compounds were isolated by various column chromatographies, and their structures were identified on the basis of spectroscopic analysis including UV, MS, IR and NMR. The four compounds were identified as 2-methyl-5-(2'R-methyl-4'-hydroxy-butyl)-cinnamic acid(1), 5-(2'-hydroxy-6'-methyl phenyl)-3-methylfuran-2-carboxylic acid(2), daidzein(3), and genistein(4). Compound 1 was new and 2 was firstly discovered from the genus Monascus, while 3-4 were obtained from Red Yeast Rice for the first time.


Asunto(s)
Productos Biológicos/química , Monascus , Fenoles/química , Espectroscopía de Resonancia Magnética
8.
J Asian Nat Prod Res ; 19(10): 993-999, 2017 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-28671852

RESUMEN

In our research on novel secondary metabolites from micro-organisms, two new (1-2) and four known dihydroisocoumarins (3-6) were derived from soil fungus Hypoxylon sp. Their structures were determined with extensive NMR data analysis and ECD calculation comparing with those of experimental CD spectra. Interestingly, compounds 1 and 2 possessed the same planar structure and very similar NMR data, suggesting 1 and 2 were a pair of epimers at either C-3 or at C-4, confirmed by the totally opposite cotton effect around 250 nm in the CD spectra of 1 and 2. Moreover, for the first time, we revealed that the CD absorption peak at 250 nm was dominated by C-3 orientation, rather than the orientation of C-3 substituents, by intensive ECD investigations.


Asunto(s)
Medicamentos Herbarios Chinos/aislamiento & purificación , Isocumarinas/aislamiento & purificación , Xylariales/química , Medicamentos Herbarios Chinos/química , Isocumarinas/química , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Microbiología del Suelo , Estereoisomerismo
9.
Saudi Pharm J ; 25(4): 464-468, 2017 May.
Artículo en Inglés | MEDLINE | ID: mdl-28579876

RESUMEN

In this study, our purpose is to discover the correlation between polysaccharides sulfated structure and anti-tumor activity. Sulfated polysaccharide from Sargassum fusiforme were synthesized with the chlorosulfonic acid pyridine method. The inhibitory effect of Sargassum fusiforme polysaccharides and the application of MTT assay before and after chemical modification on the proliferation of hepatocellular carcinoma HepG-2 cells in vitro were studied. Sulfated polysaccharide from sargassum fusiforme DS is 0.803. The modified polysaccharide has certain inhibitory effect on HepG-2 cells, and its inhibition on the cells growth has improved compared with the original SFPs. The sulfated polysaccharide from Sargassum fusiforme has the ability to enhance anti-tumor activities.

10.
Saudi Pharm J ; 25(4): 633-637, 2017 May.
Artículo en Inglés | MEDLINE | ID: mdl-28579903

RESUMEN

As research was conducted on the early apoptosis of human breast cancer cell MCF-7 caused by lycorine hydrochloride and the expression of the related apoptosis proteins. The early-period apoptosis rate of human breast cancer cell MCF-7 was tested with the AnnexinV/PI double staining and flow cytometry. The Western Blotting method was also used to detect the protein expression conditions of Fas, FasL, Caspase-8 and Bid. The results showed that the higher the dose, the higher the rate of apoptosis and that the rate of apoptosis was dependent on the dose; the relative protein activity of Fas, FasL, Caspase-8 and bid gradually rose with the increase of lycorine dosage and the activities revealed certain dose-independence. Results showed that lycorine hydrochloride could induce the apoptosis of human breast cancer cell MCF-7 through the death receptor pathway.

11.
Biomed Chromatogr ; 30(12): 1975-1983, 2016 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-27239783

RESUMEN

Evodia rutaecarpa (E. rutaecarpa) has been used to treat aches, vomiting and dysentery in traditional Chinese medicine. However, as a mildly toxic herb its toxic components have not been elucidated. An attempt was made to illuminate the hepatotoxic constituents of E. rutaecarpa. The 50% ethanol extracts of E. rutaecarpa from 19 different sources were used to establish UPLC fingerprints and administered to mice at a dose of 35 g/kg (crude medicine weight/mouse weight) once daily for 14 days. Serum levels of alanine transaminase, aspartate aminotransferase and liver coefficient were used as indices of liver injury. Additionally, the characteristic peaks of 19 fingerprints were identified. Spectrum-effect relationships between fingerprints and hepatotoxic indicators were analyzed using bivariate correlation analysis (BCA). The UPLC fingerprints were established and a total of 28 main compounds were identified. Because of the inherent variations in chemical compositions, the liver injury levels were different among the E. rutaecarpa samples from 19 sites of production. BCA results indicated that compounds dihydrorutaecarpine, 6-acetoxy-5-epilimonin, goshuyuamide I, 1-methyl-2-[(Z)-5-undecenyl]-4(1H)-quinolone, 1-methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone, evocarpine and 1-methyl-2-[(6Z,9Z)-6,9-pentadecadienyl]-4(1H)-quinolone were tentatively determined as the primary hepatotoxic components. The present study provides a valuable method for the discovery of hepatotoxic constituents by combination of fingerprints and hepatotoxicity index.


Asunto(s)
Cromatografía Liquida/métodos , Evodia/química , Hígado/efectos de los fármacos , Espectrometría de Masas/métodos , Extractos Vegetales/análisis , Extractos Vegetales/toxicidad , Alanina Transaminasa/sangre , Animales , Aspartato Aminotransferasas/sangre , Femenino , Masculino , Ratones , Análisis de Componente Principal
12.
Pharm Biol ; 54(7): 1219-22, 2016 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-26155822

RESUMEN

CONTEXT: Patrinia villosa (Thunb.) Juss (Valerianaceae) is an important ancient herbal medicine widely used for inflammation, wound healing, and abdominal pain. But little is known of the phytochemical constituents of this herbal plant. OBJECTIVE: The objective of this study is to isolate and identify the bioactive components from P. villosa. MATERIALS AND METHODS: A 70% EtOH extract of P. villosa was subjected to normal-phase silica, ODS silica gel column chromatography, and semi-preparative HPLC chromatography after partitioned successively with light petroleum, dichloromethane and n-BuOH. Chemical structures of the compounds were elucidated by spectroscopic methods including UV, 1D-NMR, 2D-NMR, HR-ESI-MS, and CD spectra. The cytotoxic activity of the new component was determined with the SMMC-7721 cell line using the MTT method after incubation for 48 h. RESULTS: A new flavonoid named patriniaflavanone A (1) along with four known compounds was isolated from P. villosa. The four known compounds were identified as luteolin 7-O-glucuronide-6″-methyl ester (2), p-hydroxyphenylacetic acid methyl ester (3), trans-caffeic acid (4), and trans-caffeic acid methylate (5) by comparison of their spectral data with the reported data. The IC50 value of patriniaflavanone A (1) on SMMC-7721 was 61.27 µM. DISCUSSION AND CONCLUSION: This is the first report on the isolation and identification of patriniaflavanone A (1), and compounds 2-5 were isolated for the first time from the title plant. Patriniaflavanone A (1) exhibited moderate cytotoxic activity.


Asunto(s)
Antineoplásicos Fitogénicos/aislamiento & purificación , Flavonoides/aislamiento & purificación , Patrinia/química , Antineoplásicos Fitogénicos/farmacología , Carcinoma Hepatocelular/tratamiento farmacológico , Carcinoma Hepatocelular/patología , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Cromatografía Líquida de Alta Presión , Dicroismo Circular , Flavonoides/farmacología , Humanos , Neoplasias Hepáticas/tratamiento farmacológico , Neoplasias Hepáticas/patología , Espectroscopía de Resonancia Magnética , Estructura Molecular , Fitoterapia , Hojas de la Planta , Plantas Medicinales , Espectrometría de Masa por Ionización de Electrospray , Espectrofotometría Ultravioleta
13.
Zhong Yao Cai ; 39(4): 867-71, 2016 Apr.
Artículo en Zh | MEDLINE | ID: mdl-30132597

RESUMEN

Objective: To investigate the mechanism of human liver cancer HepG-2 cells apoptosis induced by total saponins of Ornithogalum caudatum( OCA-TS). Methods: The anti-proliferative effects of OCA-TS on HepG-2 cells was detected by MTT assay; the inverted microscope was used to observe cell morphology; transmission electron microscope( TEM) was used to observe the cellular ultrastructure changes; flow cytometry method was used to detect the apoptosis rate, mitochondrial membrane potential, and protein expression level of Cyt-C; Caspase-3 activity was measured by ELISA. Results: OCA-TS can inhibit the proliferation of HepG-2 cells and the IC50 was 79. 80 ± 0. 18 µg / m L. After treated by OCA-TS, cells became round, and the refractivity of cells receded, the number of suspension cells increased. By TEM method, the cells presented typical apoptosis characteristics. With the increasing of concentration of OCA-TS, cell apoptosis rate, the protein expression level of Cyt-C and the activity of Caspase-3 were increased markedly( P < 0. 05 or P < 0. 01). Conclusion: OCA-TS can effectively inhibit the proliferation of human liver cancer HepG-2 cells by inducing apoptosis of HepG-2 cells through mitochondrial pathway.


Asunto(s)
Apoptosis/efectos de los fármacos , Ornithogalum , Carcinoma Hepatocelular , Caspasa 3 , Línea Celular Tumoral , Proliferación Celular , Citocromos c , Citometría de Flujo , Humanos , Neoplasias Hepáticas , Potencial de la Membrana Mitocondrial , Saponinas
14.
Am J Med Genet A ; 167A(10): 2357-65, 2015 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-26079994

RESUMEN

Hereditary nonsyndromic hearing loss is extremely heterogeneous. Mutations in the transmembrane channel-like gene1 (TMC1) are known to cause autosomal dominant and recessive forms of nonsyndromic hearing loss linked to the loci of DFNA36 and DFNB7/11, respectively. We characterized a six-generation Chinese family (5315) with progressive, postlingual autosomal dominant nonsyndromic hearing loss (ADNSHL). By combining targeted capture of 82 known deafness genes, next-generation sequencing and bioinformatic analysis, we identified TMC1 c.1714G>A (p. D572N) as the disease-causing mutation. This mutation co-segregated with hearing loss in other family members and was not detected in 308 normal controls. In order to determine the prevalence of TMC1 c.1714G>A in Chinese ADNSHL families, we used DNA samples from 67 ADNSHL families with sloping audiogram and identified two families carry this mutation. To determine whether it arose from a common ancestor, we analyzed nine STR markers. Our results indicated that TMC1 c.1714G>A (p.D572N) account for about 4.4% (3/68) of ADNSHL in the Chinese population.


Asunto(s)
Biología Computacional/métodos , Pérdida Auditiva Sensorineural/genética , Proteínas de la Membrana/genética , Mutación , Adulto , Pueblo Asiatico , Audiometría , Secuencia de Bases , Estudios de Casos y Controles , Niño , Análisis Mutacional de ADN , Femenino , Expresión Génica , Genes Dominantes , Sitios Genéticos , Marcadores Genéticos , Pérdida Auditiva Sensorineural/etnología , Pérdida Auditiva Sensorineural/patología , Heterocigoto , Secuenciación de Nucleótidos de Alto Rendimiento , Humanos , Masculino , Datos de Secuencia Molecular , Linaje
15.
Biomed Chromatogr ; 29(7): 1016-26, 2015 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-25404485

RESUMEN

Compared with chemical drugs, it is a huge challenge to identify active ingredients of multicomponent traditional Chinese medicine (TCM). For most TCMs, metabolism investigation of absorbed constituents is a feasible way to clarify the active material basis. Although Andrographis paniculata (AP) has been extensively researched by domestic and foreign scholars, its metabolism has seldom been fully addressed to date. In this paper, high-performance liquid chromatography/quadrupole time-of-flight mass spectrometry was applied to analysis and characterization of AP metabolism in rat urine and feces samples after oral administration of ethanol extract. The differences in metabolites and metabolic pathways between the two biological samples were further compared. The chemical structures of 20 components were tentatively identified from drug-treated biological samples, including six prototype components and 14 metabolites, which underwent such main metabolic pathways as hydrolyzation, hydrogenation, dehydroxylation, deoxygenation, methylation, glucuronidation, sulfonation and sulfation. Two co-existing components were found in urine and feces samples, suggesting that some ingredients' metabolic processes were not unique. This study provides a comprehensive report on the metabolism of AP in rats, which will be helpful for understanding its mechanism.


Asunto(s)
Andrographis/química , Cromatografía Líquida de Alta Presión/métodos , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/metabolismo , Espectrometría de Masas/métodos , Administración Oral , Animales , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/análisis , Heces/química , Masculino , Ratas , Ratas Wistar
16.
J Asian Nat Prod Res ; 17(5): 468-74, 2015 May.
Artículo en Inglés | MEDLINE | ID: mdl-26031203

RESUMEN

Chemical examination of the fermentation broth of a sponge-associated fungus Trichoderma harzinum HMS-15-3 led to the isolation of four pairs of new C13 lipid enantiomers namely harzianumols A-H (1a-4b). Their structures were elucidated on the basis of extensive spectroscopic (IR, MS, 1D, and 2D NMR) data analysis, including the modified Mosher's method for the assignment of their absolute configurations. The new compounds were evaluated for antihyperlipidemic effects in HepG2 cells.


Asunto(s)
Lípidos/aislamiento & purificación , Trichoderma/química , Animales , Lípidos/química , Lípidos/farmacología , Biología Marina , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Poríferos/microbiología
17.
Molecules ; 20(3): 4290-306, 2015 Mar 06.
Artículo en Inglés | MEDLINE | ID: mdl-25756649

RESUMEN

Sauromatum giganteum (Engl.) Cusimano & Hett Tuber are used in Chinese folklore medicine for treatment of neoplasms. However, the claim has not been scientifically validated. The aim of the study is to screen the antitumor bioactive fraction of Sauromatum giganteum (Engl.) Cusimano & Hett Tuber and sensitive tumor cell lines using a cytotoxicity assay in vitro and tumor transplantation method in vivo, to support its use in folk medicine. The petroleum ether fraction, chloroform fraction, ethyl acetate fraction, n-butanol fraction and water fraction were successively extracted by turn by the maceration under reflux assay. Screening of antitumor bioactive fraction and sensitive cell lines were measured by MTT assay and the serum pharmacology method, and in vivo the antitumor activities of the active fraction was evaluated by using S180 or H22 tumor-bearing mice model and Kunming mice. The active constituents of ethyl acetate fraction of Sauromatum giganteum (Engl.) Cusimano & Hett were characterized by UPLC-TOF-MS. Compared with control groups, mice serum containing ethyl acetate fraction had a inhibition effect on SMMC-7721 cell, SGC-7901 cell, MCF-7 cell, HeLa cell, A549 cell, HT-29, and MDA-MB-231, respectively, but mice serum containing other four fractions had no different with that of control group. The inhibition capabilities of mice serum containing ethyl acetate fraction on the seven cell lines in descending order is SGC-7901 > SMMC-7721 > MCF-7 > HT-29 > A549 > HeLa > MDA-MB-231. In vivo the inhibition rate of 106, 318, 954 mg/kg·d ethyl acetate fraction dry extract to sarcoma S180 is 15.22%, 26.15% and 40.24%, respectively, and life prolonging rate to hepatoma H22 is 33.61%, 40.16% and 55.74%. A total of 14 compounds were identified in the ethyl acetate fraction of Sauromatum giganteum (Engl.) Cusimano & Hett. The results of the experimental studies proved the antitumor activity of Sauromatum giganteum (Engl.) Cusimano & Hett and supported the traditional use of this plant. These data indicate the potential for the use of ethyl acetate fraction of Sauromatum giganteum (Engl.) Cusimano & Hett Tuber in tumor therapy, anti-tumor activity on cancer cell line in descending order is SGC-7901 > SMMC-7721 > MCF-7 > HT-29 > A549 > HeLa > MDA-MB-231.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Araceae/química , Proliferación Celular/efectos de los fármacos , Neoplasias/tratamiento farmacológico , Extractos Vegetales/farmacología , Tubérculos de la Planta/química , Espectrometría de Masa por Láser de Matriz Asistida de Ionización Desorción/métodos , Animales , Cromatografía Liquida , Femenino , Humanos , Masculino , Ratones , Neoplasias/metabolismo , Neoplasias/patología , Células Tumorales Cultivadas , Ensayos Antitumor por Modelo de Xenoinjerto
18.
Water Sci Technol ; 72(3): 472-7, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-26204080

RESUMEN

Rhodospirillum rubrum has the potential for biomass resource recycling combined with sewage purification. However, low biomass production and yield restricts the potential for sewage purification. This research investigated the improvement of biomass production, yield and organics reduction by Mg²âº in R. rubrum wastewater treatment. Results showed that with optimal dosage (120 mg/L), biomass production reached 4,000 mg/L, which was 1.5 times of that of the control group. Biomass yield was improved by 43.3%. Chemical oxygen demand (COD) removal reached over 90%. Hydraulic retention time was shortened by 25%. Mechanism analysis indicated that Mg²âº enhanced the isocitrate dehydrogenase and Ca²âº/Mg²âº-ATPase activities, bacteriochlorophyll content on respiration and photophosphorylation. These effects then enhanced ATP production, which led to more biomass accumulation and COD removal. With 120 mg/L Mg²âº dosage, the isocitrate dehydrogenase and Ca²âº/Mg²âº-ATPase activities, bacteriochlorophyll content, ATP production were improved, respectively, by 33.3%, 50%, 67%, 41.3% compared to those of the control group.


Asunto(s)
Reactores Biológicos , Magnesio , Rhodospirillum rubrum/efectos de los fármacos , Rhodospirillum rubrum/crecimiento & desarrollo , Aguas del Alcantarillado , Análisis de la Demanda Biológica de Oxígeno , Biomasa , Metabolismo Energético , Consumo de Oxígeno , Reciclaje , Rhodospirillum rubrum/metabolismo , Eliminación de Residuos Líquidos , Aguas Residuales
19.
Pharm Biol ; 53(10): 1481-7, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-25857322

RESUMEN

CONTEXT: Chrysin, a natural flavonoid, has been shown to possess multiple pharmacological activities including anti-atherosclerosis. OBJECTIVE: The effects of chrysin on foam cell formation and cholesterol flow in RAW264.7 macrophages were investigated in this work to explore the potential mechanism underlying its anti-atherogenic activity. MATERIALS AND METHODS: The inhibitive effect of chrysin on foam cell formation and cholesterol accumulation induced by oxidized low-density lipoprotein cholesterol (ox-LDL) was assessed by oil red O staining and intracellular total cholesterol and triglyceride quantification in RAW264.7 macrophages. The action of chrysin on cholesterol efflux and influx was tested by fluorescent assays. Real-time quantitative PCR was used to quantify the relative expression of cholesterol flow-associated genes and luciferase assay was applied to test the transcription activity of peroxisome proliferator-activated receptor gamma (PPARγ). RESULTS: Chrysin dose dependently inhibited the formation of foam cells and prevented the enhanced cholesterol accumulation by ox-LDL. Treatment with chrysin (10 µM) significantly enhanced cholesterol efflux and substantially inhibited cholesterol influx. Simultaneously, chrysin significantly increased the mRNA levels of PPARγ, liver X receptor alpha (LXRα), ATP-binding cassette, sub-family A1 (ABCA1), and sub-family G1 (ABCG1), decreased scavenger receptor A1 (SR-A1) and SR-A2, and increased the transcriptional activity of PPARγ. DISCUSSION AND CONCLUSION: Chrysin is a new inhibitor of foam cell formation that may stimulate cholesterol flow. Up-regulation of the classical PPARγ-LXRα-ABCA1/ABCG1 pathway and down-regulation of SR-A1 and SR-A2 may participate in its suppressive effect on intracellular cholesterol accumulation.


Asunto(s)
Colesterol/metabolismo , Flavonoides/farmacología , Células Espumosas/efectos de los fármacos , Macrófagos/efectos de los fármacos , Pandanaceae , Animales , Transporte Biológico/efectos de los fármacos , Transporte Biológico/fisiología , Línea Celular , Colesterol/agonistas , Relación Dosis-Respuesta a Droga , Flavonoides/aislamiento & purificación , Células Espumosas/metabolismo , Macrófagos/metabolismo , Ratones
20.
Adv Mater ; 36(21): e2312013, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38270245

RESUMEN

The recent discovery of room-temperature ferromagnetism in 2D van der Waals (vdW) materials, such as Fe3GaTe2 (FGaT), has garnered significant interest in offering a robust platform for 2D spintronic applications. Various fundamental operations essential for the realization of 2D spintronics devices are experimentally confirmed using these materials at room temperature, such as current-induced magnetization switching or tunneling magnetoresistance. Nevertheless, the potential applications of magnetic skyrmions in FGaT systems at room temperature remain unexplored. In this work, the current-induced generation of magnetic skyrmions in FGaT flakes employing high-resolution magnetic transmission soft X-ray microscopy is introduced, supported by a feasible mechanism based on thermal effects. Furthermore, direct observation of the current-induced magnetic skyrmion motion at room temperature in FGaT flakes is presented with ultra-low threshold current density. This work highlights the potential of FGaT as a foundation for room-temperature-operating 2D skyrmion device applications.

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