RESUMEN
Galium species are used worldwide for their antioxidant, antibacterial, antifungal, and antiparasitic properties. Although this plant has demonstrated its antitumor properties on various types of cancer, its biological activity on cutaneous melanoma has not been established so far. Therefore, the present study was designed to investigate the phytochemical profile of two extracts of G. verum L. herba (ethanolic and ethyl acetate) as well as the biological profile (antioxidant, antimicrobial, and antitumor effects) on human skin cancer. The extracts showed similar FT-IR phenolic profiles (high chlorogenic acid, isoquercitrin, quercitrin, and rutin), with high antioxidant capacity (EC50 of ethyl acetate phase (0.074 ± 0.01 mg/mL) > ethanol phase (0.136 ± 0.03 mg/mL)). Both extracts showed antimicrobial activity, especially against Gram-positive Streptococcus pyogenes and Staphylococcus aureus bacilli strains, the ethyl acetate phase being more active. Regarding the in vitro antitumor test, the results revealed a dose-dependent cytotoxic effect against A375 melanoma cell lines, more pronounced in the case of the ethyl acetate phase. In addition, the ethyl acetate phase stimulated the proliferation of human keratinocytes (HaCaT), while this effect was not evident in the case of the ethanolic phase at 24 h post-stimulation. Consequently, G. verum l. could be considered a promising phytocompound for the antitumor approach of cutaneous melanoma.
Asunto(s)
Antiinfecciosos , Galium , Melanoma , Rubiaceae , Neoplasias Cutáneas , Humanos , Etanol , Antioxidantes/farmacología , Antioxidantes/química , Galium/química , Rumanía , Espectroscopía Infrarroja por Transformada de Fourier , Extractos Vegetales/farmacología , Extractos Vegetales/química , Suplementos Dietéticos , Fitoquímicos/farmacología , Fitoquímicos/química , Antiinfecciosos/farmacología , Antiinfecciosos/químicaRESUMEN
Plants are commonly used in folk medicine. Research indicates that the mechanisms of biological activity of plant extracts may be essential in the treatment of various diseases. In this respect, we decided to test the ethanolic extracts of Bidens tripartita herb (BTH), Galium verum herb (GVH), and Rumicis hydrolapathum root (RHR) on angiogenic, anti-inflammatory, and antioxidant properties and their total polyphenols content. In vitro studies using endothelial cells were used to see tested extracts' angiogenic/angiostatic and anti-inflammatory properties. The DPPH assay and FRAP analysis were used to detect antioxidant properties of extracts. The Folin-Ciocalteu analysis was used to determine the content of total polyphenols. The results of gas chromatography-mass spectrometry analysis was also presented. In vitro study demonstrated that BTH, GVH, and RHR ethanolic extracts significantly increased cell invasiveness, compared with the control group. Increased endothelial proangiogenic invasiveness was accompanied by reduced metalloproteinase inhibitor 1 (TIMP-1) and raised in metalloproteinase 9 (MMP-9). Only BTH and GVH significantly reduced cell proliferation, while BTH and RHR facilitated migration. Additionally, tested extracts reduced the production of proangiogenic platelet-derived growth factor (PDGF) and hepatocyte growth factor (HGF). The most potent anti-inflammatory capacity showed BTH and GVH, reducing proinflammatory interleukin 8 (CXCL8) and interleukin 6 (Il-6), compared to RHR extract that has slightly less inhibited CXCL8 production without affecting IL-6 production. Moreover, we confirmed the antioxidant properties of all examined extracts. The highest activity was characterized by RHR, which has been correlated with the high content of polyphenols. In conclusion, the modifying influence of examined extracts can be promising in disorders with pathogenesis related to angiogenesis, inflammation and free radicals formation. BTH is the best choice among the three tested extracts with its antiangiogenic and anti-inflammatory properties.
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Galium , Rumex , Antioxidantes/farmacología , Antioxidantes/química , Galium/química , Células Endoteliales , Interleucina-6 , Polifenoles/farmacología , Extractos Vegetales/química , Antiinflamatorios/farmacología , Antiinflamatorios/química , EtanolRESUMEN
The aim of the present study was to examine three different Galium species from the native population of Estonia, Galium verum, Galium aparine, and Galium mollugo, to characterise their non-volatile and volatile phytochemical composition and antioxidant activity. The main groups of bioactive compounds in the plants were quantified by colorimetric tests, showing high concentrations of polyphenols (up to 27.2 ± 1.5 mg GAE/g), flavonoids (up to 7.3 ± 0.5 mg QE/g) and iridoids (up to 40.8 ± 2.9 mg AE/g). The species were compared using HPLC-DAD-MS/MS, revealing some key differences in the phytochemical makeup of the extracts. The most abundant compound in the extracts of Galium verum blossoms and herb was found to be asperuloside, in Galium aparine herb, asperulosidic acid, and in Galium mollugo herb, chlorogenic acid. Additionally, the composition of volatile compounds was analysed by SPME-GC-MS. The degree of variability between the samples was high, but three volatiles, hexanal, anethole, and ß-caryophyllene, were quantified (≥1%) in all analysed samples. The antioxidative activity of all extracts was evaluated using the ORACFL method, demonstrating that the Galium species from Estonia all exhibit strong antioxidant capacity (up to 9.3 ± 1.2 mg TE/g). Out of the extracts studied, Galium verum blossoms contained the highest amounts of bioactives and had the strongest antioxidant capacity.
Asunto(s)
Antioxidantes , Galium , Antioxidantes/farmacología , Galium/química , Estonia , Espectrometría de Masas en Tándem , Flavonoides , Extractos Vegetales/farmacología , Fitoquímicos/farmacologíaRESUMEN
Extracts from aerial parts of G. aparine (cleavers) constitute a herbal remedy with monography in British Herbal Pharmacopeia. On the European market, there are several drugs and food supplements consisting of Galium extracts. In folk medicine, cleavers was used topically in Europe, Asia, and the Americas to treat skin diseases. In several remedies, cleavers is also listed as an immunomodulatory active herb influencing the defense response of the human body. The aim of this study was to investigate the immunostimulatory activity and antioxidant potential in vitro of a raw infusion of cleavers and bioactive fractions. The functional activity of lymphocytes in the reaction of the lymphocyte blast transformation (RLBT) method was used for immunomodulatory activity assays and direct scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), and hydrogen peroxide (H2O2) was chosen for the examination of antioxidant activity. It was shown that both the raw extract and fractions show significant immunostimulatory and scavenging activities. The obtained data partially justify the traditional use of cleavers as topical remedy for skin infections and for wounds.
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Galium/química , Linfocitos/inmunología , Fitoquímicos/farmacología , Extractos Vegetales/farmacología , Hojas de la Planta/química , Antioxidantes , Humanos , Linfocitos/efectos de los fármacosRESUMEN
The chemical composition of the volatile fraction from Galium verum L. (leaves and flowers) and Cruciata laevipes Opiz (whole plant), Rubiaceae, was investigated. Samples from these two plant species were collected at full bloom in Val di Susa (Western Alps, Turin, Italy), distilled in a Clevenger-type apparatus, and analyzed by GC/FID and GC/MS. A total of more than 70 compounds were identified, making up 92%-98% of the total oil. Chemical investigation of their essential oils indicated a quite different composition between G. verum and C. laevipes, both in terms of the major constituents and the dominant chemical classes of the specialized metabolites. The most abundant compounds identified in the essential oils from G. verum were 2-methylbenzaldheyde (26.27%, corresponding to 11.59 µg/g of fresh plant material) in the leaves and germacrene D (27.70%; 61.63 µg/g) in the flowers. C. laevipes essential oils were instead characterized by two sesquiterpenes, namely ß-caryophyllene (19.90%; 15.68 µg/g) and trans-muurola-4(15),5-diene (7.60%; 5.99 µg/g); two phenylpropanoids, benzyl alcohol (8.30%; 6.71 µg/g), and phenylacetaldehyde (7.74%; 6.26 µg/g); and the green-leaf alcohol cis-3-hexen-1-ol (9.69%; 7.84 µg/g). The ecological significance of the presence of such compounds is discussed.
Asunto(s)
Flores/química , Galium/química , Hojas de la Planta/química , Rubiaceae/química , Compuestos Orgánicos Volátiles/aislamiento & purificación , Acetaldehído/análogos & derivados , Acetaldehído/química , Acetaldehído/aislamiento & purificación , Altitud , Benzaldehídos/química , Benzaldehídos/aislamiento & purificación , Alcohol Bencilo/química , Alcohol Bencilo/aislamiento & purificación , Cromatografía de Gases y Espectrometría de Masas , Hexanoles/química , Hexanoles/aislamiento & purificación , Humanos , Italia , Extracción Líquido-Líquido/métodos , Aceites de Plantas/química , Sesquiterpenos Policíclicos/química , Sesquiterpenos Policíclicos/aislamiento & purificación , Sesquiterpenos de Germacrano/química , Sesquiterpenos de Germacrano/aislamiento & purificación , Compuestos Orgánicos Volátiles/química , Compuestos Orgánicos Volátiles/clasificaciónRESUMEN
The aim of our study was to determine a chemical composition of methanol extract of Galium verum as well as to assess its effects on functional recovery and redox status of isolated rat heart after ischemia. Rats were divided into control and G. verum group, which included animals treated with 500 mg/kg of methanol extract of G. verum for 28 days. Parameters of heart function and oxidative stress markers were estimated. Cell morphology was evaluated by hematoxylin and eosin (HE) staining. Our results demonstrated for the first time that G. verum extract preserved cardiac contractility, systolic, and diastolic function as wells as structural damage of the heart after ischemia. Furthermore, G. verum extract modulated the activity of antioxidant enzymes and alleviated the production of pro-oxidants.
Asunto(s)
Antioxidantes/farmacología , Cardiotónicos/farmacología , Galium/química , Contracción Miocárdica , Daño por Reperfusión Miocárdica/tratamiento farmacológico , Extractos Vegetales/farmacología , Animales , Masculino , Daño por Reperfusión Miocárdica/etiología , Daño por Reperfusión Miocárdica/patología , Oxidación-Reducción , Estrés Oxidativo/efectos de los fármacos , Ratas , Ratas WistarRESUMEN
Galium verum L. (G. verum, lady's bedstraw) is a perennial herbaceous plant, belonging to the Rubiaceae family. It has been widely used throughout history due to multiple therapeutic properties. However, the effects of this plant species on functional recovery of the heart after ischemia have still not been fully clarified. Therefore, the aim of our study was to examine the effects of methanol extract of G. verum on myocardial ischemia/reperfusion (I/R) injury in spontaneously hypertensive rats (SHR), with a special emphasis on the role of oxidative stress. Rats involved in the research were divided randomly into two groups: control (spontaneously hypertensive rats (SHR)) and G. verum group, including SHR rats treated with the G. verum extract (500 mg/kg body weight per os) for 4 weeks. At the end of the treatment, in vivo cardiac function was assessed by echocardiography. Rats were sacrificed and blood samples were taken for spectrophotometric determination of systemic redox state. Hearts from all rats were isolated and retrogradely perfused according to the Langendorff technique. After a stabilization period, hearts were subjected to 20-minute ischemia, followed by 30-minute reperfusion. Levels of prooxidants were spectrophotometrically measured in coronary venous effluent, while antioxidant enzymes activity was assessed in heart tissue. Cell morphology was evaluated by hematoxylin and eosin (HE) staining. 4-week treatment with G. verum extract alleviated left ventricular hypertrophy and considerably improved in vivo cardiac function. Furthermore, G. verum extract preserved cardiac contractility, systolic function, and coronary vasodilatory response after ischemia. Moreover, it alleviated I/R-induced structural damage of the heart. Additionally, G. verum extract led to a drop in the generation of most of the measured prooxidants, thus mitigating cardiac oxidative damage. Promising potential of G. verum in the present study may be a basis for further researches which would fully clarify the mechanisms through which this plant species triggers cardioprotection.
Asunto(s)
Galium/química , Hipertensión/tratamiento farmacológico , Daño por Reperfusión Miocárdica/tratamiento farmacológico , Animales , Modelos Animales de Enfermedad , Masculino , RatasRESUMEN
Background: Galium is a plant rich in iridoid glycosides, flavonoids, anthraquinones, and small amounts of essential oils and vitamin C. Recent works showed the antibacterial, antifungal, antiparasitic, and antioxidant activity of this plant genus. Methods: For the determination of the multicomponent phenolic pattern, liquid phase microextraction procedures were applied, combined with HPLC-PDA instrument configuration in five Galium species aerial parts (G. verum, G. album, G. rivale, G. pseudoaristatum, and G. purpureum). Dispersive Liquidâ»Liquid MicroExtraction (DLLME) with NaCl and NAtural Deep Eutectic Solvent (NADES) medium and Ultrasound-Assisted (UA)-DLLME with ß-cyclodextrin medium were optimized. Results: The optimal DLLME conditions were found to be: 10 mg of the sample, 10% NaCl, 15% NADES or 1% ß-cyclodextrin as extraction solvent-400 µL of ethyl acetate as dispersive solvent-300 µL of ethanol, vortex time-30 s, extraction time-1 min, centrifugation at 12000× g for 5 min. Conclusions: These results were compared with microwave-assisted extraction procedures. G. purpureum and G. verum extracts showed the highest total phenolic and flavonoid content, respectively. The most potent extract in terms of antioxidant capacity was obtained from G. purpureum, whereas the extract obtained from G. album exhibited the strongest inhibitory effect against tyrosinase.
Asunto(s)
Bioensayo/métodos , Galium/química , Microextracción en Fase Líquida/métodos , Microondas , Fenoles/aislamiento & purificación , Flavonoides/análisisRESUMEN
The present article discusses the results of an immunomodulatory activity of Galii veri herba, Galium verum herb (Galium verum L., Rubiaceae) fluid water extract and the effect of the polysaccharide and phenolic complexes of the letter on the immunomodulatory activity. The same extract was fractionated into a polysaccharide complex (PSC) and a polyphenolic complex (PPC). In the obtained substances, the contents of hydroxycinnamic derivates, flavonoids and polyphenols were determined spectrophotometrically; polysaccharides were quantified gravimetrically; the immunomodulatory activity of the substances was determined in the reaction of lymphocyte blast transformation. It has been established that the fluid extract of Galium verum herb contains 6.3% polysaccharides, 4.2% hydroxycinnamic derivates expressed as chlorogenic acid, 0.4% flavonoids expressed as rutin, 3.7% polyphenols expressed as gallic acid. PPC contains 4.48% hydroxycinnamic derivates expressed as chlorogenic acid, 0.43% flavonoids expressed as rutin, and 3.95% polyphenols expressed as gallic acid. The lowest immunomodulatory activity was found for PPC. A significantly higher activity was determined for PSC. The highest immunomodulatory activity was established for the fluid extract at a dilution of 1/20, its activity being by 59.4% higher compared with the lymphocyte spontaneous transformation and by 18.5% higher than that of the reference substance PHA. The obtained results enable an assumption of a synergistic effect of PPC and PSC of Galium verum herb fluid extract on the potency of its immunomodulatory activity. Key words: Galium verum L. ⢠immunomodulatory activity ⢠lymphocyte blast transformation ⢠fluid water extract ⢠polysaccharide complex ⢠polyphenols complex.
Asunto(s)
Flavonoides/farmacología , Galium/química , Factores Inmunológicos/farmacología , Fenoles/farmacología , Extractos Vegetales/farmacología , Antioxidantes , Células Cultivadas , Humanos , Linfocitos/efectos de los fármacosRESUMEN
Galium verum is a well-known medicinal plant which is used in various pathologies. G. verum extracts are characterized here using chromatography, where among the rich pool of phenolic acids of flavonoids two known anti-stress modulators, chlorogenic acid and rutin are identified in high quantities. Additionally, the extracts are characterized using a series of in vitro assays (EPR, DPPH, TPC and TEAC). Considering the chemical findings, the potential beneficial effects of the G. verum extract are explored here in a living organism exposed to stress induced oxidative damages. Thus, the biochemical-modulatory and antioxidant roles of two doses of G. verum extract are examined in animals exposed to acute restraint and dark stress (S). The animals were divided in groups [control, S, SG1 (exposed to 25 mg G. verum extract), SG2 (50 mg extract)]. Increased levels of lipid peroxidation (TBARS from 4.43 to 8.06 nmol/mL), corticosterone from 0.43 to 1.96 µg/dL and epinephrine from 44.43 to 126.7 µg/mL, as well as decreased antioxidant enzymes activities (SOD/CAT) were observed in the S group. The G. verum extract afforded a near-normal equilibrium within the biochemical parameters of animals exposed to RS, by reducing oxidative damage (TBARS at a 3.73 nmol/mL; CS at 0.90 µg/dL; EP at 63.72 µg/mL) and by restoring the antioxidant balance.
Asunto(s)
Antioxidantes/farmacología , Oscuridad/efectos adversos , Galium/química , Extractos Vegetales/farmacología , Especies Reactivas de Oxígeno/farmacología , Restricción Física/psicología , Estrés Psicológico/metabolismo , Alanina Transaminasa/metabolismo , Animales , Aspartato Aminotransferasas/metabolismo , Colesterol/metabolismo , Corticosterona/sangre , Relación Dosis-Respuesta a Droga , Epinefrina/sangre , Femenino , Peroxidación de Lípido/efectos de los fármacos , Estrés Oxidativo/efectos de los fármacos , Polifenoles/farmacología , Ratas , Ratas Wistar , Estrés Psicológico/sangre , Estrés Psicológico/enzimología , Estrés Psicológico/etiologíaRESUMEN
PURPOSE: In this study we developed and tested an iron oxide nanoparticle conjugated with DTPA and Trastuzumab, which can efficiently be radiolabeled with 99m-Tc and Ga-68, generating a nanoradiopharmaceutical agent to be used for SPECT and PET imaging. METHODS: The production of iron oxide nanoparticle conjugated with DTPA and Trastuzumab was made using phosphorylethanolamine (PEA) surface modification. Both radiolabeling process was made by the direct radiolabeling of the nanoparticles. The in vivo assay was done in female Balb/c nude mice xenografted with breast cancer. Also a planar imaging using the radiolabeled nanoparticle was performed. RESULTS: No thrombus and immune response leading to unwanted interaction and incorporation of nanoparticles by endothelium and organs, except filtration by the kidneys, was observed. In fact, more than 80% of 99mTc-DTPA-TZMB@Fe3O4 nanoparticles seems to be cleared by the renal pathway but the implanted tumor whose seems to increase the expression of HER2 receptors enhancing the uptake by all other organs. CONCLUSION: However, even in this unfavorable situation the tumor bioconcentrated much larger amounts of the nano-agent than normal tissues giving clear enough contrast for breast cancer imaging for diagnostics purpose by both SPECT and PET technique. Graphical Abstract á .
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Anticuerpos Monoclonales/química , Neoplasias de la Mama/diagnóstico por imagen , Galium/química , Isótopos/química , Nanopartículas de Magnetita/química , Pentetato de Tecnecio Tc 99m/química , Tecnecio/química , Animales , Transporte Biológico , Medios de Contraste/química , Endotelio/metabolismo , Femenino , Humanos , Marcaje Isotópico , Cinética , Ratones Endogámicos BALB C , Ratones Desnudos , Microscopía Electrónica de Transmisión/métodos , Tamaño de la Partícula , Tomografía de Emisión de Positrones , Cintigrafía , Propiedades de Superficie , Distribución Tisular , Tomografía Computarizada de Emisión de Fotón ÚnicoRESUMEN
The present article discusses the results of the research into the phytochemical profile and immunomodulatory activity of Galii veri herba (Galium verum L., Rubiaceae) ethanolic extracts. The extracts under study were obtained from the plant material by means of maceration technique with 20% aqueous ethanol solution (fluid extract I), 60% aqueous ethanol solution (fluid extract II) and 96% ethanol (fluid extract III) on heating. In the substances obtained, the content of hydroxycinnamic derivatives, flavonoids and polyphenols were determined spectrophotometrically; polysaccharides were quantified gravimetrically; the immunomodulatory activity of the substances under study was determined in the reaction of lymphocyte blast transformation (RLBT). It was established that fluid extract I contained 2.4% polysaccharides, 3.1% hydroxycinnamic derivatives, 0.24% flavonoids, and 2.9% polyphenols; the fluid extract II contained 4.13% hydroxycinnamic derivatives, 0.16% flavonoids, and 3.84% polyphenols; fluid extract III contained 2.7% hydroxycinnamic derivatives, 0.18% flavonoids and 2.7% polyphenols. All the extracts under study possessed a marked stimulant effect on the transformation activity of the immunocompetent blood cells. The highest immunomodulatory activity was established for 96% ethanol extract: the percentage of lymphocytes proliferating in RLBT under the influence of this extract increased by 6.77- 8.04 times in comparison with their spontaneous transformation and by 1.14-1.36 times in comparison with phytohemagglutinin. The results obtained give grounds for further research in the mechanisms of the immunomodulatory activity of the extracts of G. verum herb. Key words: ethanolic extracts Galium verum L. immunomodulatory activity lymphocyte blast transformation.
Asunto(s)
Galium/química , Factores Inmunológicos/farmacología , Extractos Vegetales/farmacología , Células Cultivadas , Etanol , Flavonoides/farmacología , Humanos , Linfocitos/efectos de los fármacos , Polifenoles/farmacologíaRESUMEN
Intercropping affects heavy-metal uptake in plants. In this study, three cadmium (Cd)-accumulator species (Stellaria media, Malachium aquaticum, and Galium aparine) were intercropped together in Cd-contaminated soil to study the effects of intercropping on co-remediation. Mutual intercropping significantly increased the biomasses of S. media, M. aquaticum, and G. aparine compared with their respective monocultures. The photosynthetic pigment contents of three species were not significantly affected by mutual intercropping. Mutual intercropping did not increase the Cd contents in roots and shoots of G. aparine, but it increased the Cd contents in roots of S. media and M. aquaticum. It also decreased the Cd contents in shoots of S. media and M. aquaticum. Only G. aparine intercropped with M. aquaticum and three-species intercropping increased Cd-accumulation levels in whole plants of each species. Only S. media intercropped with M. aquaticum and three-species intercropping increased the Cd accumulation at the whole plant level in every plant in a single pot, with S. media intercropped with M. aquaticum showing the greatest increase. Therefore, S. media intercropped with M. aquaticum and three-species intercropping may improve the efficiency of phytoremediation of Cd-contaminated soil, with S. media intercropped with M. aquaticum representing the best combination.
Asunto(s)
Biodegradación Ambiental , Cadmio/análisis , Galium/metabolismo , Contaminantes del Suelo/análisis , Stellaria/metabolismo , Biomasa , Cadmio/metabolismo , Monitoreo del Ambiente , Galium/química , Metales Pesados , Raíces de Plantas/química , Plantas , Contaminantes del Suelo/metabolismo , Stellaria/químicaRESUMEN
OBJECTIVES: Combined positron emission tomography (PET) and magnetic resonance imaging (MRI) targeting the prostate-specific membrane antigen (PSMA) with a 68Ga-labelled PSMA-analog (68Ga-PSMA-11) is discussed as a promising diagnostic method for patients with suspicion or history of prostate cancer. One potential drawback of this method are severe photopenic (halo-) artifacts surrounding the bladder and the kidneys in the scatter-corrected PET images, which have been reported to occur frequently in clinical practice. The goal of this work was to investigate the occurrence and impact of these artifacts and, secondly, to evaluate variants of the standard scatter correction method with regard to halo-artifact suppression. METHODS: Experiments using a dedicated pelvis phantom were conducted to investigate whether the halo-artifact is modality-, tracer-, and/or concentration-dependent. Furthermore, 31 patients with history of prostate cancer were selected from an ongoing 68Ga-PSMA-11-PET/MRI study. For each patient, PET raw data were reconstructed employing six different variants of PET scatter correction: absolute scatter scaling, relative scatter scaling, and relative scatter scaling combined with prompt gamma correction, each of which was combined with a maximum scatter fraction (MaxSF) of MaxSF = 75% or MaxSF = 40%. Evaluation of the reconstructed images with regard to halo-artifact suppression was performed both quantitatively using statistical analysis and qualitatively by two independent readers. RESULTS: The phantom experiments did not reveal any modality-dependency (PET/MRI vs. PET/CT) or tracer-dependency (68Ga vs. 18F-FDG). Patient- and phantom-based data indicated that halo-artifacts derive from high organ-to-background activity ratios (OBR) between bladder/kidneys and surrounding soft tissue, with a positive correlation between OBR and halo size. Comparing different variants of scatter correction, reducing the maximum scatter fraction from the default value MaxSF = 75% to MaxSF = 40% was found to efficiently suppress halo-artifacts in both phantom and patient data. In 1 of 31 patients, reducing the maximum scatter fraction provided new PET-based information changing the patient's diagnosis. CONCLUSION: Halo-artifacts are particularly observed for 68Ga-PSMA-11-PET/MRI due to 1) the biodistribution of the PSMA-11-tracer resulting in large OBRs for bladder and kidneys and 2) inaccurate scatter correction methods currently used in clinical routine, which tend to overestimate the scatter contribution. If not compensated for, 68Ga-PSMA-11 uptake pathologies may be masked by halo-artifacts leading to false-negative diagnoses. Reducing the maximum scatter fraction was found to efficiently suppress halo-artifacts.
Asunto(s)
Artefactos , Galium/química , Imagen por Resonancia Magnética , Tomografía de Emisión de Positrones , Humanos , Masculino , Persona de Mediana EdadRESUMEN
OBJECTIVE: To investigate the effects of flavone from Galium verum L (FGVL) on hydrogen peroxide induced oxidative injury in human umbilical vein endothelial cells (HUVEC), and explore related mechanisms. METHODS: HUVEC were divided into five groups: control group (1640 complete medium), injured group (HUVEC treated with 100 µmol/L hydrogen peroxide for 4 h), FGVL group (HUVEC treated with 12.5 mg/L FGVL (group F1), 25.0 mg/L (group F2), 50.0 mg/L (group F3) for 24 h before hydrogen peroxide). The nitric oxide content was measured by nitric acid reductase method. The 6-keto-Prostacyclin-F1α (6-keto-PGF1α), thromboxane B2 (TXB2), interleukin(IL)-6 and IL-22 were determined by ELISA.mRNA expression of phosphatidylinositol 3-kinase (PI3K), protein kinase B (Akt) and endothelial nitric oxide synthase (eNOS) was detected by RT-PCR.Protein expression of p-Akt (ser(473)) and p-eNOS (ser(1177)) was determined by Western blot.Cell apoptosis was observed with fluorescence microscope after Hoechst33258 staining. RESULTS: (1) The contents of nitric oxide were significantly lower in the injured group than in the control group ((34.11±1.78) µmol/L vs. (74.81±2.93) µmol/L, P<0.05), which was significantly increased in group F2 ((41.86±2.32) µmol/L) and group F3 ((62.79±1.16) µmol/L) compared with injured group (both P<0.05). (2)The secretion level of 6-keto-PGF1α was significantly lower in the injured group ((44.84±3.87) ng/L) than in the control group ((82.38±3.98) ng/L, P<0.05), which was significantly increased in group F1 ((52.76±1.78) ng/L), FGVL 2 group which was(56.58±1.44) ng/L and FGVL 3 group which was(67.78±2.02) ng/L than that of injured group(all P<0.05). The secretion level of TXB2 was significantly higher in the injured group((43.37±3.96) ng/L) than in the control group ((25.56±1.75) ng/L, P<0.05), which was significantly reduced group F2 group ((32.41±1.68) ng/L) and group F3 ((28.23±2.15) ng/L) than that of injured group(both P<0.05). (3) The contents of IL-6 and IL-22 were significantly higher in the injured group ((539.74±11.63) ng/L) and ((23.70±3.05) ng/L, respectively) than in the control group ((288.67±19.52) ng/L) and ((23.70±3.05) ng/L, respectively, both P<0.05). The contents of IL-6 were significantly lower in group F1, F2 and F3 compared to that of injured group(all P<0.05). The contents of IL-22 were significantly lower in group F2 and F3 than that of injured group(both P<0.05). (4)The relative levels of PI3K mRNA and eNOS mRNA in injured group (0.68±0.09 and 0.22±0.03, respectively) were significantly lower compared to control group(0.81±0.12 and 0.63±0.11, respectively, both P<0.05), PI3K mRNA in group F2 (0.76±0.03) and group F3 (PI3K mRNA 0.83±0.06) as well as eNOS mRNA in group F1 (0.37±0.08), F2 (0.53±0.04) and F3 (0.56±0.09) than those of injured group(all P<0.05). The mRNA expression of Akt was similar among groups (P>0.05). (5) The relative levels of p-Akt (ser(473)) and p-eNOS (ser(1177)) in injured group (0.48±0.05 and 0.23±0.03, respectively) were significantly lower compared to control group (0.71±0.12 and 0.66±0.05, respectively, both P<0.05), which was up-regulated in group F1, F2 and F3 groups compared to injured group(all P<0.05). (6) The cell apoptosis rate in injured groups was significantly higher compared to control group which ((63.67±11.37)% vs. (4.67±1.15)%, P<0.05) which was significantly reduced in group F1((43.33±4.16)%), F2((18.33±4.93)%) and F3((15.67±2.08)%) compared to injured group(all P<0.05). CONCLUSION: The FGVL can reduce hydrogen peroxide induced oxidative injury in HUVEC by increasing the level of nitric oxide through PI3K/Akt/eNOS pathway.
Asunto(s)
Flavonas/farmacología , Galium/química , Células Endoteliales de la Vena Umbilical Humana/efectos de los fármacos , Estrés Oxidativo/efectos de los fármacos , Apoptosis , Células Cultivadas , Humanos , Peróxido de Hidrógeno/efectos adversos , Interleucina-6/metabolismo , Interleucinas/metabolismo , Óxido Nítrico/metabolismo , Óxido Nítrico Sintasa de Tipo III/metabolismo , Fosfatidilinositol 3-Quinasas/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Regulación hacia Arriba , Interleucina-22RESUMEN
In this paper, a liquid chromatography-atmospheric pressure chemical ionization-mass spectrometry in negative mode method was developed for the identification and quantitative determination of 13 individual phenolics (chlorogenic acid, caffeic acid, coumaric acid, ferulic acid, (+)-catechin, (-)-epicatechin, rutin, quercitrin, isoquercitrin, fisetin, isorhamnetin, hesperidin and chrysin) from ethanolic extracts [30, 50 and 70% (w/v)] of Calendula officinalis, Hypericum perforatum, Galium verum and Origanum vulgare and some commercial extracts of these medicinal herbs. Correlation coefficients (r(2)) from calibration curves for all the compounds were between 0.9971 and 0.9996. Limit of detection was in the range of 0.070-0.280 µg/mL and limit of quantification was from 0.233 to 0.932 µg/mL. The method was partially validated and the results obtained are: the intra- and interday relative standard deviation values were within 0.086 and 2.821% and recovery values vary from 95.84% (coumaric acid) to 103.20% (rutin).
Asunto(s)
Calendula/química , Cromatografía Líquida de Alta Presión/métodos , Galium/química , Hypericum/química , Espectrometría de Masas/métodos , Origanum/química , Fenoles/análisis , Límite de Detección , Extractos Vegetales/química , Plantas Medicinales/químicaRESUMEN
Galium verum, also known as Lady's Bedstraw, is an herbaceous plant native to Europe and Asia, and has been used in traditional medicine as an anticancer medicine applied in most cases as a decoction. The influence of a Galium verum decoction on the head and neck cancer cell lines HLaC78 and FADU was analyzed and proved to be toxic in high doses on both cell lines. Cytotoxicity appeared to be influenced by expression of p-glycoprotein (MDR-1) in the carcinoma cell lines. Mucosal keratinocytes, although void of MDR-1 expression, showed only low sensitivity against high Galium concentrations. Sublethal doses of Galium extract acted as strong inhibitors of motility, as shown by a spheroid-based invasion analysis on Matrigel-coated surfaces. Inhibition of invasion was significantly more pronounced in the invasive HLaC78 cell line. mRNA expression analysis of matrix metalloproteinases MMP-2 and MMP-9 and their inhibitors TIMP-1/-2 revealed significant TIMP-1 upregulation after an 8-h Galium exposition in FADU cells. Gelatinolytic activity, however, was not influenced by Galium extract in HLaC78, in the FADU cells MMP-2/-9 activity was slightly increased after incubation with Galium extract. In primary mucosal keratinocytes, Galium decoction protected DNA against benz[a]pyrene, one of the most DNA toxic agents in cigarette smoke. In conclusion Galium extract may be useful as a preventive and/or a concomitant therapeutic approach in head and neck cancer.
Asunto(s)
Antioxidantes/farmacología , Galium/química , Neoplasias de Cabeza y Cuello/patología , Queratinocitos/efectos de los fármacos , Extractos Vegetales/farmacología , Subfamilia B de Transportador de Casetes de Unión a ATP/genética , Subfamilia B de Transportador de Casetes de Unión a ATP/metabolismo , Animales , Línea Celular Tumoral , Movimiento Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Daño del ADN , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Neoplasias de Cabeza y Cuello/tratamiento farmacológico , Neoplasias de Cabeza y Cuello/genética , Neoplasias de Cabeza y Cuello/metabolismo , Humanos , Membrana Mucosa/citología , RatasRESUMEN
Galium verum, also known as Lady's Bedstraw, is a herbaceous perennial plant of the family Rubiaceae, native to Europe and Asia and used in traditional medicine as an anticancer medicine. It is used as a decoction in most traditional recipes, applied externally as well as internally. We produced a Galium verum decoction and applied it in vitro to chemosensitive (Hep-2 and HLaC79) and chemoresistant, P-glycoprotein-overexpressing (Hep2-Tax, HLaC79-Tax) laryngeal carcinoma cell lines. It could be demonstrated that Galium aqueous extract is cytotoxic for all cell lines. A detailed spheroid-based 3D invasion analysis of Hep2 and Hep2-Tax in semisolid collagen gels and on different extracellular matrix coatings was performed, which showed an inhibition of invasion by sublethal concentrations of Galium decoction and proved to be even more pronounced in the more aggressively invading chemoresistant Hep2-Tax cell line. Gelatinolytic activity of MMP-2 was downregulated in three of the four cell lines. Angiogenesis (endothelial tube formation) in contrast, was not affected by Galium aqueous extract. Gene expression array on HLaC79 and Hep2 cell lines treated with Galium decoction vs. untreated controls revealed no unique pathway activation patterns in these cells. Results are discussed with respect to the use of herbal drugs as a preventive and/or a concomitant therapeutic approach in head and neck cancer.
Asunto(s)
Carcinoma/tratamiento farmacológico , Neoplasias Laríngeas/tratamiento farmacológico , Extractos Vegetales/administración & dosificación , Apoptosis/efectos de los fármacos , Carcinoma/genética , Línea Celular Tumoral , Movimiento Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Galium/química , Regulación Neoplásica de la Expresión Génica/efectos de los fármacos , Humanos , Neoplasias Laríngeas/genética , Metaloproteinasa 2 de la Matriz/biosíntesis , Extractos Vegetales/químicaRESUMEN
Portulaca oleracea L. has been used as folk medicine in different countries to treat different ailments in humans. P. oleracea L. polysaccharide (POL-P), extracted from P. oleracea L., is found to have bioactivities such as hypoglycemic and hypolipidemic activities, antioxidant and antitumor activities. In our study, a water-soluble polysaccharide (POL-P3b) was successfully purified from Galium verum L. by DEAE cellulose and Sephadex G-200 column chromatography. To evaluate the anticancer efficacy and associated mechanisms of POL-P3b on cervical cancer in vitro and in vivo, we showed that treatment of HeLa cell with POL-P3b inhibited cell proliferation. In addition, POL-P3b significantly inhibited tumor growth in U14-bearing mice. Further analysis indicated that POL-P3b possesses the activity of inhibiting cervical cancer cell growth in vitro and in vivo at a concentration- and time-dependent manner, and the mechanisms were associated with Sub-G1 phase cell cycle arrest, triggering DNA damage and inducing apoptosis.
Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Carcinoma/tratamiento farmacológico , Extractos Vegetales/farmacología , Polisacáridos/farmacología , Portulaca/química , Neoplasias del Cuello Uterino/tratamiento farmacológico , Animales , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/uso terapéutico , Apoptosis/efectos de los fármacos , Ciclo Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Femenino , Galium/química , Células HeLa , Humanos , Ratones , Fitoterapia , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Polisacáridos/química , Polisacáridos/uso terapéutico , SolubilidadRESUMEN
We demonstrated a promising route to enhance the performance of inverted organic photovoltaic (OPV) devices by the incorporation of CuGaSe2 (CGS) quantum dots (QDs) into the ZnO buffer layer of P3HT:PCBM-based devices. The modification of QDs provides better band alignment between the organic/cathode interface, improves ZnO crystal quality, and increases photon absorption, leading to more effective carrier transport/collection. By employing this energy-harvesting scheme, short-circuit current density, open-circuit voltage, and fill factor of the OPV device after CGS QD modification are improved by 9.43%, 7.02% and 6.31%, respectively, giving rise to a 23.8% enhancement in the power conversion efficiency.