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1.
Article in English | WPRIM | ID: wpr-922766

ABSTRACT

Crassostrea sikamea (C.sikamea) is an important edible and medicinal seafood in China. In the present study, a compound named flazin was separated and identified from the ethyl acetate extract of C.sikamea (EAECs) for the first time. In addition, the 3-(4, 5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetra zolium (MTS) assay revealed that EAECs and flazin inhibited the transformation of splenic lymphocytes in vitro. Moreover, flazin (20 μg·mL


Subject(s)
Animals , Carbolines , Crassostrea , Furans , Lymphocytes , Rats , Rats, Sprague-Dawley , Spleen
2.
Journal of Experimental Hematology ; (6): 1780-1784, 2021.
Article in Chinese | WPRIM | ID: wpr-922334

ABSTRACT

OBJECTIVE@#To investigate the effect of RITA on TP53 mutant human mantle cell lymphoma (MCL) cell line Mino and its possible mechanism.@*METHODS@#Mino cells were cultured in RPMI-1640 and treated with RITA at a concentration of 0-16 μmol/L for 24,48,72 hours. Cell viability was assessed by CCK-8 assay. The cells were treated by RITA (0-8 μmol/L) for 48 h, the cell apoptosis induced by RITA was detected by annexin V/PI flow cytometry. Western blot was performed to evaluate the expression of protein BCL-2, Caspase-3, Cleaved Caspase-3, PARP, MDM2, and P53 in Mino cells.@*RESULTS@#After treatment with 0.5, 1, 2, 4, 8, and 16 μmol/L RITA for 48 h, the proliferation inhibition rate of Mino cells was (1.2±5.6)%, (14.9±4.9)%, (41.7±5.0)%, (61.8±2.4)%, (70.2±2.8)%, and (70.8±2.4)%, respectively. RITA could inhibit the proliferation of Mino cells significantly, and statistical analysis showed that the inhibition rate was increased with the increasing of RITA concentration (r=0.767). After the cells were treated by 4 μmol/L RITA for 24, 48, and 72 h, the proliferation inhibition rate was (25.2±3.8)%, (61.8±2.4)%, and (87.0±0.7)%, respectively. Satistical analysis showed that the inhibition rate was also increased with the increasing of treatment time (r=0.978). The apoptosis rate of Mino cells treated by 0, 2, 4, and 8 μmol/L RITA for 48 h was (5.4±0.4)%, (15.3±0.6)%, (38.7±1.7)%, and (50.8±1.1)%, respectively, and it showed dose-dependent manner (r=0.961). Western blot showed that with the increasing of RITA concentration, the BCL-2 protein expression was decreased in a dose-dependent manner (r=0.932), moreover, PARP cleavage and Caspase-3 activation were found, while the protein expression of MDM2 and P53 showed no change.@*CONCLUSION@#RITA can inhibit the proliferation and induce the apoptosis of Mino cells significantly. The mechanism may be dependent on the Caspase pathway, but independent on the P53 pathway.


Subject(s)
Apoptosis , Cell Line, Tumor , Cell Survival , Furans , Humans , Lymphoma, Mantle-Cell , Mutation , Tumor Suppressor Protein p53
3.
Article in English | WPRIM | ID: wpr-922183

ABSTRACT

BACKGROUND@#In recent years, heated tobacco products (HTPs), which are widely used in Japan, have been sold by various brands using additives such as flavors. It has been reported that the components of mainstream smoke are different from those of conventional cigarettes. In this study, we established an analytical method for furans and pyridines in the mainstream smoke, which are characteristic of HTPs and particularly harmful among the generated components, and investigated the amount of component to which the smokers are exposed.@*METHODS@#We established a simple analytical method for simultaneous analysis of gaseous and particulate compounds in the mainstream smoke of HTPs (IQOS, glo, ploom S) in Japan by combining a sorbent cartridge and glass fiber filter (Cambridge filter pad (CFP)). Both the sorbent cartridge and CFP were extracted using 2-propanol and analyzed via GC-MS/MS to determine the concentration of furans and pyridines generated from each HTP.@*RESULTS@#The results showed that the levels of target furans such as furfural, 2-furanmethanol, 2(5H)-furanone, and 5-methylfurfural tended to be higher in the mainstream smoke of glo than in standard cigarettes (3R4F). Pyridine, which is generated at a high level in 3R4F as a combustion component, and 4-ethenylpyridine (EP), which is a known marker of environmental tobacco smoke, were detected. Among these components, 2-furanmethanol and pyridine are classified as Group 2B (possibly carcinogenic to humans) by the International Agency for Research on Cancer (IARC). Therefore, it is possible that they will contribute to the health effects caused by use of HTPs.@*CONCLUSIONS@#Using the new collection and analytical method for furans and pyridines in the mainstream smoke of HTPs, the level of each compound to which smokers are exposed could be clarified. By comprehensively combining information on the amount of ingredients and toxicity, it will be possible to perform a more detailed calculation of the health risks of using HTPs. In addition, the components detected in this study may be the causative substances of indoor pollution through exhaled smoke and sidestream smoke; therefore, environmental research on the chemicals generated from HTPs would be warranted in future studies.


Subject(s)
Furans/analysis , Gas Chromatography-Mass Spectrometry , Humans , Japan , Pyridines/analysis , Smoke/analysis , Tandem Mass Spectrometry , Tobacco Products
4.
Chinese Journal of Biotechnology ; (12): 473-485, 2021.
Article in Chinese | WPRIM | ID: wpr-878576

ABSTRACT

Lignocellulose is the most abundant renewable organic carbon resource on earth. However, due to its complex structure, it must undergo a series of pretreatment processes before it can be efficiently utilized by microorganisms. The pretreatment process inevitably generates typical inhibitors such as furan aldehydes that seriously hinder the growth of microorganisms and the subsequent fermentation process. It is an important research field for bio-refining to recognize and clarify the furan aldehydes metabolic pathway of microorganisms and further develop microbial strains with strong tolerance and transformation ability towards these inhibitors. This article reviews the sources of furan aldehyde inhibitors, the inhibition mechanism of furan aldehydes on microorganisms, the furan aldehydes degradation pathways in microorganisms, and particularly focuses on the research progress of using biotechnological strategies to degrade furan aldehyde inhibitors. The main technical methods include traditional adaptive evolution engineering and metabolic engineering, and the emerging microbial co-cultivation systems as well as functional materials assisted microorganisms to remove furan aldehydes.


Subject(s)
Aldehydes , Fermentation , Furans , Lignin/metabolism
5.
Article in Chinese | WPRIM | ID: wpr-880776

ABSTRACT

OBJECTIVE@#To investigate the protective effect of arctiin with anti-inflammatory bioactivity against triptolide-induced nephrotoxicity in rats and explore the underlying mechanism.@*METHODS@#Forty SD rats were divided into 4 groups for gastric lavage of normal saline, arctiin (500 mg/kg), triptolide (500 μg/kg), or both arctiin (500 mg/kg) and triptolide (500 μg/kg). Blood samples were collected for analysis of biochemical renal parameters, and the renal tissues were harvested for determining the kidney index and for pathological evaluation with HE staining. In the @*RESULTS@#In SD rats, arctiin significantly antagonized triptolide-induced elevation of BUN, Scr and kidney index (@*CONCLUSIONS@#Arctiin can protect the kidney from triptolide-induced damages in rats possibly through the anti-inflammatory pathway.


Subject(s)
Animals , Anti-Inflammatory Agents , Diterpenes/toxicity , Epoxy Compounds/toxicity , Furans , Glucosides , Kidney/drug effects , Phenanthrenes/toxicity , Rats , Rats, Sprague-Dawley
6.
Article in English | WPRIM | ID: wpr-812427

ABSTRACT

The present study was designed to improve storage stability and oral bioavailability of Ganneng dropping pills (GNDP) by transforming lignans of Herpetospermum caudigerum (HL) composed of herpetrione (HPE) and herpetin (HPN) into nanosuspension (HL-NS), the main active ingredient of GNDP, HL-NS was prepared by high pressure homogenization and lyophilized to transform into solid nanoparticles (HL nanoparticles), and then the formulated HL nanoparticles were perfused into matrix to obtain NS-GNDP by melting method. For a period of 3 months, the content uniformity, storage stability and pharmacokinetics test in vivo of NS-GNDP were evaluated and compared with regular GNDP at room temperature. The results demonstrated that uniformity of dosage units of NS-GNDP was acceptable according to the criteria of Chinese Pharmacopoeia 2015J. Physical stability of NS-GNDP was investigated systemically using photon correlation spectroscopy (PCS), zeta potential measurement, and scanning electron microscopy (SEM). There was a slight increase in particles and PI of HL-NS re-dispersed from NS-GNDP after storage for 3 months, compared with new formulated NS-GNDP, which indicated a good redispersibility of the NS-GNDP containing HL-NS after storage. Besides, chemical stability of NS-GNDP was studied and the results revealed that HPE and HPN degradation was less when compared with that of GNDP, providing more than 99% of drug residue after storage for 3 months. In the dissolution test in vitro, NS-GNDP remarkably exhibited an increased dissolution velocity compared with GNDP and no distinct dissolution difference existed within 3 months. The pharmacokinetic study showed that HPE and HPN in NS-GNDP exhibited a significant increase in AUC, C and decrease in T when compared with regular GNDP. These results indicated that NS-GNDP possessed superiority with improved storage stability and increased dissolution rate and oral bioavailability.


Subject(s)
Animals , Benzofurans , Chemistry , Biological Availability , Cucurbitaceae , Chemistry , Drug Carriers , Chemistry , Drug Compounding , Drug Stability , Freeze Drying , Furans , Chemistry , Humans , Lignans , Chemistry , Pharmacokinetics , Male , Nanoparticles , Chemistry , Particle Size , Plant Extracts , Chemistry , Rats , Rats, Sprague-Dawley , Solubility
7.
Article in English | WPRIM | ID: wpr-773637

ABSTRACT

The present study was designed to improve storage stability and oral bioavailability of Ganneng dropping pills (GNDP) by transforming lignans of Herpetospermum caudigerum (HL) composed of herpetrione (HPE) and herpetin (HPN) into nanosuspension (HL-NS), the main active ingredient of GNDP, HL-NS was prepared by high pressure homogenization and lyophilized to transform into solid nanoparticles (HL nanoparticles), and then the formulated HL nanoparticles were perfused into matrix to obtain NS-GNDP by melting method. For a period of 3 months, the content uniformity, storage stability and pharmacokinetics test in vivo of NS-GNDP were evaluated and compared with regular GNDP at room temperature. The results demonstrated that uniformity of dosage units of NS-GNDP was acceptable according to the criteria of Chinese Pharmacopoeia 2015J. Physical stability of NS-GNDP was investigated systemically using photon correlation spectroscopy (PCS), zeta potential measurement, and scanning electron microscopy (SEM). There was a slight increase in particles and PI of HL-NS re-dispersed from NS-GNDP after storage for 3 months, compared with new formulated NS-GNDP, which indicated a good redispersibility of the NS-GNDP containing HL-NS after storage. Besides, chemical stability of NS-GNDP was studied and the results revealed that HPE and HPN degradation was less when compared with that of GNDP, providing more than 99% of drug residue after storage for 3 months. In the dissolution test in vitro, NS-GNDP remarkably exhibited an increased dissolution velocity compared with GNDP and no distinct dissolution difference existed within 3 months. The pharmacokinetic study showed that HPE and HPN in NS-GNDP exhibited a significant increase in AUC, C and decrease in T when compared with regular GNDP. These results indicated that NS-GNDP possessed superiority with improved storage stability and increased dissolution rate and oral bioavailability.


Subject(s)
Animals , Benzofurans , Chemistry , Biological Availability , Cucurbitaceae , Chemistry , Drug Carriers , Chemistry , Drug Compounding , Drug Stability , Freeze Drying , Furans , Chemistry , Humans , Lignans , Chemistry , Pharmacokinetics , Male , Nanoparticles , Chemistry , Particle Size , Plant Extracts , Chemistry , Rats , Rats, Sprague-Dawley , Solubility
8.
Clinics ; 73(supl.1): e482s, 2018. graf
Article in English | LILACS | ID: biblio-952842

ABSTRACT

This review will discuss the contributions of marine natural molecules, a source only recently found to have pharmaceutical prospects, to the development of anticancer drugs. Of the seven clinically utilized compounds with a marine origin, four are used for the treatment of cancer. The development of these drugs has afforded valuable knowledge and crucial insights to meet the most common challenges in this endeavor, such as toxicity and supply. In this context, the development of these compounds will be discussed herein to illustrate, with successful examples provided by cytarabine, trabectedin, eribulin and brentuximab vedotin, the steps involved in this process as well as the scientific advances and technological innovation potential associated with developing a new drug from marine resources.


Subject(s)
Biotechnology/methods , Aquatic Organisms/chemistry , Drug Development/methods , Neoplasms/drug therapy , Antineoplastic Agents/therapeutic use , Oceans and Seas , Immunoconjugates/therapeutic use , Immunoconjugates/pharmacology , Immunoconjugates/chemistry , Cytarabine/chemistry , Drug Discovery , Trabectedin/chemistry , Furans/chemistry , Brentuximab Vedotin , Ketones/chemistry , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemistry
9.
Braz. j. microbiol ; 48(4): 791-800, Oct.-Dec. 2017. graf
Article in English | LILACS | ID: biblio-889166

ABSTRACT

ABSTRACT Lignocellulose-derived inhibitors have negative effects on the ethanol fermentation capacity of Saccharomyces cerevisiae. In this study, the effects of eight typical inhibitors, including weak acids, furans, and phenols, on glucose and xylose co-fermentation of the recombinant xylose-fermenting flocculating industrial S. cerevisiae strain NAPX37 were evaluated by batch fermentation. Inhibition on glucose fermentation, not that on xylose fermentation, correlated with delayed cell growth. The weak acids and the phenols showed additive effects. The effect of inhibitors on glucose fermentation was as follows (from strongest to weakest): vanillin > phenol > syringaldehyde > 5-HMF > furfural > levulinic acid > acetic acid > formic acid. The effect of inhibitors on xylose fermentation was as follows (from strongest to weakest): phenol > vanillin > syringaldehyde > furfural > 5-HMF > formic acid > levulinic acid > acetic acid. The NAPX37 strain showed substantial tolerance to typical inhibitors and showed good fermentation characteristics, when a medium with inhibitor cocktail or rape straw hydrolysate was used. This research provides important clues for inhibitors tolerance of recombinant industrial xylose-fermenting S. cerevisiae.


Subject(s)
Saccharomyces cerevisiae/drug effects , Xylose/metabolism , Glucose/metabolism , Phenols/metabolism , Phenols/pharmacology , Saccharomyces cerevisiae/growth & development , Saccharomyces cerevisiae/genetics , Saccharomyces cerevisiae/metabolism , Acids/metabolism , Acids/pharmacology , Industrial Microbiology , Fermentation , Furans/metabolism , Furans/pharmacology
10.
An. acad. bras. ciênc ; 89(1,supl): 383-390, May. 2017. tab, graf
Article in English | LILACS | ID: biblio-886664

ABSTRACT

ABSTRACT A simple and sensitive method for simultaneous determination of furan and vinyl acetate (VA) in vapor phase of mainstream cigarette smoke with cold trap and gas chromatography-mass spectrometry (GC-MS) was developed. A Cambridge filter pad (CFP) was placed in front of the impingers of smoking machine to remove the particle phase from cigarette smoke. Furan and VA in vapor phase of mainstream cigarette smoke were collected in two impingers connected in series by filled with methanol at -78°C. The solutions were added with deuterium-labeled furan-d4 and VA-d6 as internal standards and analyzed by GC-MS. The results showed that the calibration curves for furan and VA were linear (r2 > 0.9995) over the studied concentration range. The intra- and inter-day precision values for furan and VA were <7.07% and <9.62%, respectively. The extraction recoveries of furan and VA were in the range of 94.5-97.7% and 92.3-94.9%, respectively. Moreover, the limits of detection for furan and VA were 0.028 µg mL-1 and 1.3 ng mL-1, respectively. The validated method has been successfully applied to determine the emissions of furan and VA in the vapor phase of mainstream cigarette smoke under International Organization for Standardization (ISO) and Canadian Intense (CI) smoking regimen.


Subject(s)
Smoke/analysis , Vinyl Compounds/analysis , Furans/analysis , Calibration , Reproducibility of Results , Gas Chromatography-Mass Spectrometry
11.
São Paulo; s.n; 2017. 133 p.
Thesis in Portuguese | LILACS | ID: biblio-875665

ABSTRACT

Introdução: Dioxinas, furanos e bifenilas policloradas são poluentes tóxicos para a saúde humana incluindo riscos de incidência de cânceres, efeitos de neurodesenvolvimento, lesões dérmicas, cloroacne. Estes compostos são poluentes orgânicos persistentes (POPs) que podem ser transportados de longas distâncias da fonte de emissão e se bioacumular em ecossistemas. A atmosfera poluída foi recentemente classificada como carcinogênica para os seres humanos pela Organização Mundial da Saúde, mostrando a importância de sua caracterização, principalmente para compostos tóxicos. Entretanto, técnica de coleta ativa tem custo elevado para POPs, e existem poucos estudos de calibração que validem a substituição. Objetivos: Avaliar a toxicidade equivalente da atmosfera por dioxinas, furanos e bifenilas cloradas, utilizando técnicas de coleta ativa e passiva, e verificar gradiente de concentração nos ambientes urbano, urbano/industrial e de background. Método: Amostras de ar foram coletadas, utilizando coletores ativos e passivos, durante dois períodos consecutivos de quatro meses: de setembro a dezembro de 2014 (período 1) e de maio a agosto de 2015 (período 2) em três cidades de São Paulo, SP, em ambientes urbano, urbano/industrial e de background. Todas as amostras foram extraídas com solução de tolueno:acetona (9:1) em Soxhlet por 24 h e padrões marcados (13C12-PCDD/Fs e 13C12-PCBs) foram adicionados em cada amostra antes do processo de extração. Os extratos foram purificados em coluna de sílica mista (40 por cento H2SO4 e 10 por cento AgNO3) seguida por coluna de alumina. O procedimento analítico foi realizado utilizando HRGC/HRMS (High Resolution Gas Chromatograph/High Resolution Mass Spectrometer) operando em ionização de impacto de elétrons com energia de 35 eV no modo SIM (Select Ion Monitoring) e resolução de 10.000. Resultados mostraram que: (1) existe variação sazonal para concentrações de PCDD/Fs no ar entre os períodos 1 e 2 (p=0,03), enquanto as concentrações de dl-PCBs não foram estatisticamente diferentes nestes períodos (p=0,52); (2) existe gradiente de concentração de PCDD/Fs e dl- PCBs que aumenta na seguinte ordem: background


Introduction: Dioxins, furans and polychlorinated biphenyls are toxic pollutants for human health including risks of cancer incidence, neurodevelopmental effects, dermal lesions, chloracne. These compounds are persistent organic pollutants (POPs) that can be transported to long distances from the emission source and they are bioaccumulated in ecosystems. Recently, the outdoor air pollution were classified as carcinogenic to humans by the World Health Organization, showing the importance of its characterization for toxic compounds. However, active air monitoring has a high cost for POPs, and there is a few calibration studies which support that substitution. Objective: To assess the equivalent toxicity of the atmosphere regarding the measurement of dioxins, furans and polychlorinated biphenyls, using active and passive air samplers, and to evatuate the contrasting concentrations at urban, urban/industrial and background sites. Method: Air samples were collected, using active and passive samplers, over two consecutive periods of four months: from September to December 2014 (period 1) and from May to August 2015 (period 2) at three cities in São Paulo, SP, covering urban, urban/industrial and background sites. All samples were extracted with toluene:acetone (9:1) in a Soxhlet apparatus for 24 hours and surrogate standards (13C12-PCDD/F and 13C12-PCBs) were spiked on each sample media prior to extraction procedure. The extracts were purified on an silica column (40 per cent H2SO4 and 10 per cent AgNO3) followed by an alumina column. The analytical procedure was carried out using HRGC/HRMS (High Resolution Gas Chromatograph/High Resolution Mass Spectrometer) operating in electron impact ionization with an energy of 35 eV in SIM (selected ion monitoring) mode and 10.000 resolution power. Results show that (1) there are seasonal variations for PCDD/F concentrations in air between period 1 and 2 (p=0.03), whereas dl-PCB levels were not statistically different (p=0.52) in those periods. (2) PCDD/F and dl-PCB air levels are in the following order: background


Subject(s)
Air Pollution , Data Collection/methods , Dioxins/toxicity , Furans/toxicity , Polychlorinated Biphenyls , Gas Exhaust , Industrial Zones , Organic Chemicals/toxicity , Urban Area
12.
Article in English | WPRIM | ID: wpr-812437

ABSTRACT

The present study aimed at developing a natural compound with anti-allergic effect and stability under latex glove manufacturing conditions and investigating whether its anti-allergic effect is maintained after its addition into the latex. The effects of nine natural compounds on growth of the RBL-2H3 cells and mouse primary spleen lymphocytes were determined using MTT assay. The compounds included glycyrrhizin, osthole, tetrandrine, tea polyphenol, catechin, arctigenin, oleanolic acid, baicalin and oxymatrine. An ELISA assay was used for the in vitro anti-type I/IV allergy screening; in this process β-hexosaminidase, histamine, and IL-4 released from RBL-2H3 cell lines and IFN-γ and IL-2 released from mouse primary spleen lymphocytes were taken as screening indices. The physical stability of eight natural compounds and the dissolubility of arctigenin, selected based on the in vitro pharnacodynamaic screening and the stability evaluation, were detected by HPLC. The in vivo pharmacodynamic confirmation of arctigenin and final latex product was evaluated with a passive cutaneous anaphylaxis (PCA) model and an allergen-specific skin response model. Nine natural compounds showed minor growth inhibition on RBL-2H3 cells and mouse primary spleen lymphocytes. Baicalin and arctigenin had the best anti-type I and IV allergic effects among the natural compounds based on the in vitro pharmacodynamic screening. Arctigenin and catechin had the best physical stability under different manufacturing conditions. Arctigenin was the selected for further evaluation and proven to have anti-type I and IV allergic effects in vivo in a dose-dependent manner. The final product of the arctigenin-containing latex glove had anti-type I and IV allergic effects in vivo which were mainly attributed to arctigenin as proved from the dissolubility results. Arctigenin showed anti-type I and IV allergic effects in vitro and in vivo, with a good stability under latex glove manufacturing conditions, and a persistent anti-allergic effect after being added into the latex to prevent latex allergy.


Subject(s)
Animals , Anti-Allergic Agents , Pharmacology , Biological Products , Pharmacology , Cell Line , Cell Survival , Furans , Chemistry , Pharmacokinetics , Pharmacology , Hypersensitivity , Hypersensitivity, Delayed , Hypersensitivity, Immediate , Latex , Latex Hypersensitivity , Lignans , Chemistry , Pharmacokinetics , Pharmacology , Lymphocytes , Mice , Mice, Inbred BALB C
13.
Acta Pharmaceutica Sinica ; (12): 100-104, 2016.
Article in English | WPRIM | ID: wpr-320010

ABSTRACT

A new caffeate compound, (E)-erythro-syringylglyceryl caffeate (1), was isolated from the roots and rhizomes of Nardostachys chinensis Batal., together with nine known phenolic compounds, including (+)-licarin A (2), naringenin 4', 7-dimethyl ether (3), pinoresinol-4-O-β-D-glucoside (4), caraphenol A (5), Z-miyabenol C (6), protocatechuic acid (7), caffeic acid (8), gallic acid (9) and vanillic acid (10). Their chemical structures were elucidated on the basis of spectroscopic data and physicochemical properties. Furthermore, this is the first report of compounds 2, 5 and 6 from Nardostachys genus.


Subject(s)
Caffeic Acids , Chemistry , Flavanones , Chemistry , Furans , Chemistry , Glucosides , Chemistry , Hydroxybenzoates , Chemistry , Lignans , Chemistry , Nardostachys , Chemistry , Plant Roots , Chemistry , Rhizome , Chemistry , Vanillic Acid , Chemistry
14.
Article in Chinese | WPRIM | ID: wpr-256583

ABSTRACT

<p><b>OBJECTIVE</b>To observe the effect of RITA, a small molecule that targets p53, combined with temozolomide (TMZ) on proliferation, colony formation and apoptosis of human glioblastoma U87 cells and explore the underlying mechanism.</p><p><b>METHODS</b>Cultured U87 cells were treated with RITA (1, 5, 10, 20 µmol/L), TMZ, or RITA+TMZ (half dose) for 24, 48 or 72 h. MTS assay were used to detect the cell proliferation, and the cell proliferation rate and inhibitory rate were calculated. The effect of combined treatments was evaluated by the q value. The expressions of p53, p21 and other apoptosis-associated genes were detected by qRT-PCR and Western blotting; cell apoptosis was assayed using flow cytometry with Annexin V/PI double staining; colony formation of the cells was detected with crystal violet staining.</p><p><b>RESULTS</b>MTS assay showed that RITA at the 4 doses more potently inhibited U87 cell viability than TMZ at 72 h (P=0.000) with inhibitory rates of 25.94%-41.38% and 3.84%-8.20%, respectively. RITA combined with TMZ caused a more significant inhibition of U87 cells (29.21%-52.11%) than RITA (P<0.01) and TMZ (P=0.000) alone. At the doses above 5 µmol/L, the combined treatments with RITA+TMZ for 48 h resulted in q values exceeding 1.2 and showed an obvious synergistic effect of the drugs. Both RITA and TMZ, especially the latter, significantly increased the expressions of p53, p21, puma, and other apoptosis-associated genes to accelerate apoptosis and inhibit the growth and colony formation of U87 cells, and the effect was more obvious with a combined treatment.</p><p><b>CONCLUSION</b>RITA inhibits the growth of human glioblastoma cells and enhance their sensitivity to TMZ by up-regulating p53 expression, and when combined, RITA and TMZ show a synergistic effect to cause a stronger cell inhibition.</p>


Subject(s)
Apoptosis , Cell Line, Tumor , Cell Proliferation , Cell Survival , Dacarbazine , Pharmacology , Furans , Pharmacology , Glioblastoma , Drug Therapy , Humans
15.
Article in English | WPRIM | ID: wpr-258842

ABSTRACT

We assessed the effects of furan and lycopene on the histopathological and biochemical changes on lungs, body and lung weights, and food consumption of rats. Furan and diabetes caused histopathological changes, increment in malondialdehyde levels, and decrease in antioxidant enzyme activities. Lycopene showed a protective effect against these damages, except for glutathione-S-transferase and glutathione peroxidase activities. Consequently, furan and diabetes resulted in lung toxicity. Our findings demonstrate that furan treatment resulted in more alterations in histology and biochemical parameters in diabetic rats and lycopene showed protective effects against these alterations.


Subject(s)
Animals , Antioxidants , Pharmacology , Carotenoids , Pharmacology , Diabetes Mellitus, Experimental , Pathology , Furans , Toxicity , Lung , Pathology , Male , Rats, Wistar
16.
Article in Chinese | WPRIM | ID: wpr-286889

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effect of arctiin on advanced oxidation protein product (AOPP)-induced epithelial-to-mesenchymal transition (EMT) in tubular cells and explore the mechanisms underlying this effect.</p><p><b>METHODS</b>Human proximal tubular cells (HK-2 cells) were treated with bovine serum albumin (BSA) or AOPPs in the presence or absence of arctiin. The expressions of E-cadherin, vimentin, and GRP78 at the protein and mRNA levels in the cells were examined using Western blotting and quantitative real-time PCR. The level of reactive oxygen species (ROS) was measured by flow cytometry with DCFH-DA as the fluorescent probe.</p><p><b>RESULTS</b>Compared with BSA-treated cells, the cells treated with AOPPs showed decreased expression of epithelial cell marker E-cadherin and overexpression of mesenchymal marker vimentin and endoplasmic reticulum stress marker GRP78 with an increased ROS level. These changes induced by AOPPs were partly inhibited by arctiin.</p><p><b>CONCLUSION</b>Arctiin can ameliorate AOPP-induced EMT in tubular cells by inhibiting endoplasmic reticulum stress, and oxidative stress response may participate in this process.</p>


Subject(s)
Advanced Oxidation Protein Products , Cadherins , Metabolism , Cell Line , Endoplasmic Reticulum Stress , Epithelial Cells , Cell Biology , Epithelial-Mesenchymal Transition , Furans , Pharmacology , Glucosides , Pharmacology , Heat-Shock Proteins , Metabolism , Humans , Kidney Tubules , Cell Biology , Oxidative Stress , Reactive Oxygen Species , Metabolism , Vimentin , Metabolism
17.
Bol. latinoam. Caribe plantas med. aromát ; 14(3): 171-178, mayo 2015. ilus, tab
Article in English | LILACS | ID: biblio-907482

ABSTRACT

Compounds such as triclosan, diclofenac and trimetropin posses antibacterial activity, including mycobacterial; their structures are based on two aromatic rings joined by a methylene or a heteroatom. Since a similar structural system is found in natural diarylfuran- based lignans, we studied plants known with this type of lignans, as potential active against Mycobacterium tuberculosis. Fractions of the active extracts were tested for anti-TB activity and their chemical constituents analyzed by NMR spectroscopy. Several extracts and chromatographical fractions exhibited > 90 percent inhibition of M. tuberculosis at 128 ug/mL. Methylpluviatilol, a pure compound isolated from Virola sebifera, was active at this concentration.. These findings suggest that plant species of the families here studied may yield novel lead compounds for the development of antimycobacterial agents.


Compuestos tales como triclosan, diclofenac y trimetoprim poseen actividad antibacterial, incluyendo la antimicobacterial; sus estructuras están basadas en dos anillos aromáticos unidos por un metileno o un heteroátomo. Debido a que en la naturaleza se encuentra un sistema estructural similar del tipo diarilfurano en los lignanos, así como otros subtipos, nosotros estudiamos plantas contra Mycobacterium tuberculosis, de las que se sabe contienen lignanos Las fracciones cromatográficas de los extractos activos fueron ensayadas para actividad anti.Tb y sus constituyentes químicos se analizaron por espectroscopía de RMN. Varios extractos y fracciones cromatográficas exhibieron una inhibición superior al 90 por ciento a 128 ug/mL; el compuesto metilpluviatilol, aislado de mostró una inhibición del 99 por ciento a esa concentración. Esos hechos sugieren que las especies de plantas de las familias aquí estudiadas podrían suministrar nuevos compuestos líderes para el desarrollo de agentes antimicobacteriales.


Subject(s)
Anti-Bacterial Agents/pharmacology , Furans/pharmacology , Lignans/pharmacology , Mycobacterium tuberculosis , Biological Assay , Magnetic Resonance Spectroscopy
18.
Dental press j. orthod. (Impr.) ; 20(2): 29-34, Mar-Apr/2015. tab, graf
Article in English | LILACS | ID: lil-745854

ABSTRACT

OBJECTIVE: The purpose of this study was to assess the influence of magnification and superimposition of structures on CBCT-generated lateral cephalometric radiographs (LCR) using different segments of the cranium. METHODS: CBCT scans of 10 patients were selected. Four LCR were generated using Dolphin Imaging(r) software: full-face, right side, left side and center of the head. A total of 40 images were imported into Radiocef Studio 2(r), and the angles of the most common cephalometric analyses were traced by the same observer twice and within a 10-day interval. Statistical analyses included intraexaminer agreement and comparison between methods by means of intraclass correlation coefficient (ICC) and Bland-Altman agreement tests. RESULTS: Intraexaminer agreement of the angles assessed by ICC was excellent (> 0.90) for 83% of measurements, good (between 0.75 and 0.90) for 15%, and moderate (between 0.50 and 0.75) for 2% of measurements. The comparison between methods by ICC was excellent for 68% of measurements, good for 26%, and moderate for 6%. Variables presenting wider confidence intervals (> 6o) in the Bland-Altman tests, in intraexaminer assessment, were: mandibular incisor angle, maxillary incisor angle, and occlusal plane angle. And in comparison methods the variables with wider confidence interval were: mandibular incisor, maxillary incisor, GoGn, occlusal plane angle, Frankfort horizontal plane (FHP), and CoA. CONCLUSION: Superimposition of structures seemed to influence the results more than magnification, and neither one of them significantly influenced the measurements. Considerable individual variability may occur, especially for mandibular and maxillary incisors, FHP and occlusal plane. .


OBJETIVO: o objetivo do presente estudo foi avaliar a influência da sobreposição estrutural e da magnificação nas radiografias cefalométricas laterais (RCL) geradas por meio de tomografias computadorizadas de feixe cônico (TCFC), usando diferentes segmentos do crânio. MÉTODOS: foram selecionadas 10 tomografias de pacientes. Quatro RCL foram geradas usando Dolphin Imaging, sendo face total, lado direito, lado esquerdo e o centro da cabeça. Um total de 40 imagens foi importado para o Radiocef Studio, e os ângulos das análises cefalométricas mais comuns foram medidos pelo mesmo observador, duas vezes, em um intervalo de 10 dias. As análises estatísticas incluíram concordância intraexaminador e comparação entre os métodos por meio do coeficiente de correlação intraclasse (ICC) e testes de concordância de Bland-Altman. RESULTADOS: a concordância intraexaminador dos ângulos avaliados pelo ICC foi excelente (> 0,90) para 83% das medições, boa (entre 0,75 e 0,90) para 15%, e moderada (entre 0,50 e 0,75) para 2% das medições. A comparação entre os métodos por ICC foi excelente para 68% das medições, boa para 26% e moderada para 6%. As variáveis que apresentaram intervalos de confiança mais amplos (> 6°) nos testes de Bland-Altman, na avaliação intraexaminador, foram: incisivo superior, incisivo inferior e plano oclusal, enquanto nos métodos de comparação, as variáveis com intervalos de confiança mais amplos foram: incisivo inferior, incisivo superior, GoGn, ângulo do plano oclusal, plano horizontal de Frankfort e CoA. CONCLUSÃO: a sobreposição estrutural pareceu influenciar os resultados mais do que a magnificação, mas os métodos não influenciaram significativamente as medições. Considerável variabilidade individual pode ocorrer especialmente para os incisivos superiores e inferiores, plano horizontal de Frankfort e plano oclusal. .


Subject(s)
DNA Repair , Deoxyguanosine/analogs & derivatives , Escherichia coli Proteins/genetics , Escherichia coli/genetics , Gene Expression Regulation, Bacterial , Mutagenesis/radiation effects , Sugar Acids/metabolism , Biological Assay , DNA Breaks, Double-Stranded , DNA Polymerase beta/genetics , DNA Polymerase beta/metabolism , Deoxyguanosine/chemistry , Deoxyguanosine/metabolism , Escherichia coli Proteins/metabolism , Escherichia coli/metabolism , Escherichia coli/radiation effects , Flap Endonucleases/genetics , Flap Endonucleases/metabolism , Furans/chemistry , Furans/metabolism , Gamma Rays , Mutation , Plasmids , Sugar Acids/chemistry
19.
Rev. paul. pediatr ; 33(1): 34-41, Jan-Mar/2015. tab, graf
Article in English | LILACS | ID: lil-744698

ABSTRACT

OBJECTIVE: Identifying at what age infants enrolled in public day care centers are introduced to soft drinks and industrialized juice, as well as comparing the nutritional composition of these goods with natural fruit juice. METHODS: A cross-sectional study with the mothers of 636 children (aged 0 to 36 months) from nurseries of day care centers, who were asked questions about the age of feeding introduction. This study evaluated the proximate composition of soft drinks and artificial juice, comparing them with those of natural fruit juice regarding energy, sugar, fiber, vitamin C, and sodium values. The chemical composition of fruit juice was obtained by consulting the Table of Food Composition and, for industrialized drinks, the average nutritional information on the labels of the five most consumed product brands. RESULTS: The artificial drinks were consumed before the first year of life by more than half of the children studied, however, approximately 10% consumed them before the age of 6 months. With regard to the comparison among the drinks, artificial fruit juice beverages and soft drinks proved to contain from nine to 13 times higher amounts of sodium, and 15 times less vitamin C than natural juices. CONCLUSIONS: The introduction of soft drinks and industrialized juice in the diet of infants was inopportune and premature.. When compared to natural fruit juice, these have inferior nutritional composition, which suggests the urgent need for measures based on strategies for food and nutrition education in order to promote awareness and the maintenance of healthy eating habits. .


OBJETIVO: Identificar a idade de introdução do refrigerante e de sucos industrializados na dieta de lactentes matriculados em berçários de creches públicas e comparar as composições nutricionais dessas bebidas com as do suco de fruta natural. MÉTODOS: Estudo transversal com 636 crianças (de zero a 36 meses) de berçários de creches, cujas mães foram entrevistadas sobre idade de introdução dos alimentos. Avaliaram-se as composições centesimais do refrigerante e sucos industrializados, comparando-as com as do suco de laranja natural para valor energético, açúcar, fibra, vitamina C e sódio. A composição centesimal do suco de laranja foi obtida por meio de consulta à Tabela de Composição de Alimentos e, para as bebidas industrializadas, utilizaram-se as médias das informações nutricionais contidas nos rótulos de cinco marcas mais consumidas dos produtos. RESULTADOS: O refrigerante e suco industrializado foram consumidos antes do primeiro ano de vida por mais da metade das crianças estudadas, sendo que cerca de 10% o consumiram antes dos seis meses. Quando comparadas à composição do suco de laranja natural, bebidas forneceram quantidades de 9 a 13 vezes superiores de sódio e 15 vezes inferiores de vitamina C. CONCLUSÕES: A introdução de refrigerantes e sucos industrializados na dieta dos lactentes foi inoportuna e precoce. Comparados ao suco de fruta natural, tais bebidas possuem composição nutricional inferior, sugerindo a necessidade de medidas fundamentadas em estratégias de educação alimentar e nutricional como forma de promover a formação e manutenção de hábitos alimentares saudáveis. .


Subject(s)
Anti-Bacterial Agents/pharmacology , Bacteria/drug effects , Drug Resistance, Multiple, Bacterial/drug effects , Fluoroquinolones/pharmacology , Furans/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/chemical synthesis , Dose-Response Relationship, Drug , Fluoroquinolones/chemistry , Furans/chemistry , Microbial Sensitivity Tests , Models, Molecular , Molecular Structure , Structure-Activity Relationship
20.
Article in English | WPRIM | ID: wpr-812516

ABSTRACT

This paper reports a pharmacophylogenetic study of a medicinal plant family, Ranunculaceae, investigating the correlations between their phylogeny, chemical constituents, and pharmaceutical properties. Phytochemical, ethnopharmacological, and pharmacological data were integrated in the context of the systematics and molecular phylogeny of the Ranunculaceae. The chemical components of this family included several representative metabolic groups: benzylisoquinoline alkaloids, ranunculin, triterpenoid saponin, and diterpene alkaloids, among others. Ranunculin and magnoflorine were found to coexist in some genera. The pharmacophylogenetic analysis, integrated with therapeutic information, agreed with the taxonomy proposed previously, in which the family Ranunculaceae was divided into five sub-families: Ranunculoideae, Thalictroideae, Coptidoideae, Hydrastidoideae, and Glaucidioideae. It was plausible to organize the sub-family Ranunculoideae into ten tribes. The chemical constituents and therapeutic efficacy of each taxonomic group were reviewed, revealing the underlying connections between phylogeny, chemical diversity, and clinical use, which should facilitate the conservation and sustainable utilization of the pharmaceutical resources derived from the Ranunculaceae.


Subject(s)
Alkaloids , Therapeutic Uses , Aporphines , Therapeutic Uses , Biodiversity , Furans , Humans , Methylglycosides , Phylogeny , Phytotherapy , Plant Extracts , Chemistry , Therapeutic Uses , Plants, Medicinal , Chemistry , Ranunculaceae , Chemistry , Saponins , Therapeutic Uses , Terpenes , Therapeutic Uses
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