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1.
J Sci Food Agric ; 104(14): 9035-9045, 2024 Nov.
Article de Anglais | MEDLINE | ID: mdl-38989963

RÉSUMÉ

BACKGROUND: Extrusion cooking of cereal-legume flour mixture is an innovative strategy to introduce nutrient-enriched ready-to-eat snacks to the market. However, this thermal process triggers the formation of compounds that could impact safety aspects of these products. Maillard reaction markers and the end products known as melanoidins were evaluated to assess the toxicological and bioactive profiles of extruded snacks from corn-plus-common-bean-flour combinations. Different molecular weight fractions were isolated and purified to analyze their antioxidant activity and to investigate the role of melanoidins. RESULTS: The snack formulated with an 84:16 ratio of corn:common bean flours exhibited an enhanced toxicological profile. It displayed the lowest levels of acrylamide and furanic compounds, along with reduced blockage of lysine residues in the protein. Extrusion increased the antioxidant activity of uncooked flours (30 to 64%) and total phenolic compounds (26 to 50%), and decreased the available lysine (-72.7 to -79.5%). During the fractionation process, it was established that compounds within the range of 3-10 kDa made the greatest contribution to antioxidant activity. The fraction greater than 10 kDa, which included melanoidins, displayed 7 to 33% lower antioxidant activity. The purification of the fraction greater than 10 kDa revealed that pure melanoidins represented approximately one-third of the antioxidant activity in that fraction. Non-covalent adducts linked to the melanoidin core therefore had a relevant role in the antioxidant action of formulated snacks. CONCLUSION: This investigation illustrates the importance of considering both potential risks and associated benefits of compounds formed during the Maillard reaction while developing new extruded snacks. © 2024 The Author(s). Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.


Sujet(s)
Antioxydants , Farine , Réaction de Maillard , Polymères , Casse-croute , Zea mays , Antioxydants/composition chimique , Antioxydants/analyse , Zea mays/composition chimique , Farine/analyse , Polymères/composition chimique , Cuisine (activité) , Fabaceae/composition chimique , Phénols/composition chimique , Phénols/analyse , Acrylamide/composition chimique
2.
Plants (Basel) ; 12(21)2023 Nov 06.
Article de Anglais | MEDLINE | ID: mdl-37960136

RÉSUMÉ

Medicines for chronic inflammation can cause gastric ulcers and hepatic and renal issues. An alternative treatment for chronic inflammation is that of natural bioactive compounds, which present low side effects. Extracts of Jatropha cordata (Ortega) Müll. Arg. have been evaluated for their cytotoxicity and anti-inflammatory activity; however, testing pure compounds would be of greater interest. Campesteryl palmitate, n-heptyl ferulate, palmitic acid, and a mixture of sterols, i.e., brassicasterol, campesterol, ß-sitosterol, and stigmasterol, were obtained from an ethyl acetate extract from J. cordata (Ortega) Müll. Arg. bark using column chromatography. The toxicity and in vitro anti-inflammatory activities were evaluated using RAW 264.7 murine macrophage cells. None of the products assessed exhibited toxicity. The sterol mixture exhibited greater anti-inflammatory activity than the positive control, and nitric oxide (NO) inhibition percentages were 37.97% and 41.68% at 22.5 µg/mL and 30 µg/mL, respectively. In addition, n-heptyl ferulate decreased NO by 30.61% at 30 µg/mL, while campesteryl palmitate did not show anti-inflammatory activity greater than the positive control. The mixture and n-heptyl ferulate showed NO inhibition; hence, we may conclude that these compounds have anti-inflammatory potential. Additionally, further research and clinical trials are needed to fully explore the therapeutic potential of these bioactive compounds and their efficacy in treating chronic inflammation.

3.
Diagnostics (Basel) ; 13(16)2023 Aug 10.
Article de Anglais | MEDLINE | ID: mdl-37627903

RÉSUMÉ

Continuous ultrasound is recognized for its thermal effect and use in the tissue repair process. However, there is controversy about its dosage and efficacy. This study used infrared thermography, a non-invasive technique, to measure the short-term thermal effect of 3 MHz continuous ultrasound vs. a placebo, referencing the intensity applied. It was a single-blind, randomized clinical trial of 60 healthy volunteers (19-24 years old) divided into three equal groups. Group 1:1 W/cm2 for 5 min; Group 2: 0.5 W/cm2 for 10 min; and Group 3: the placebo for 5 min. The temperature was recorded through five thermographic images per patient: pre- and post-application, 5, 10, and 15 min later. After statistical analysis, a more significant decrease in temperature (p<0.05 ) was observed in the placebo group compared with the remaining groups after the application of continuous ultrasound. Group 1 was the one that generated the highest significant thermal effect (p<0.001), with an increase of 3.05 °C at 15 min, compared with the other two groups. It is concluded that to generate a thermal effect in the muscle, intensities of ≥1 W/cm2 are required, since the dosage maintained a temperature increase for more than 5 min.

4.
Plants (Basel) ; 12(3)2023 Jan 26.
Article de Anglais | MEDLINE | ID: mdl-36771644

RÉSUMÉ

The inflammatory process, although beneficial, can produce tissue damage and systemic damage when uncontrolled. Effective therapeutic alternatives with little or no side effects are of great therapeutic interest. This study aimed to determine the phytochemical composition of bark extracts from J. cordata, an endemic plant from México, and evaluate their in vitro anti-inflammatory activity. Hexane, ethyl acetate, and methanol extracts were characterized by qualitative phytochemical tests, and their bioactive groups were identified by 1H NMR and gas chromatography coupled to mass spectrometry (GC-MS). The extract's anti-inflammatory activity was evaluated as nitric oxide (NO) production and their cytotoxicity by an MTS cell proliferation assay in lipopolysaccharide (LPS)-activated RAW 264.7 cells at concentrations of 1-100 µg/mL. The hexane extract contained fatty acids, fatty esters, phytosterols, alkanes, vitamin E, and terpenoids; the ethyl acetate extract showed fatty acids, fatty esters, aromatic aldehyde, phytosterols, vitamin E, and terpenoids, while the methanolic extract showed fatty esters, fatty acid, aromatics aldehydes, and alcohol. The ethyl acetate extract showed the highest inhibition of NO production, followed by the methanolic extract and the hexane extract, without affecting the viability of RAW 264.7 macrophage cells. The results suggest that J. cordata extracts are a potential source of bioactive compounds with anti-inflammatory potential.

5.
Artrosc. (B. Aires) ; 30(3): 131-134, 2023.
Article de Espagnol | BINACIS, LILACS | ID: biblio-1519434

RÉSUMÉ

El tratamiento de las luxaciones acromioclaviculares busca reducir y controlar la inestabilidad vertical, horizontal y rotacional. El uso de los sistemas de tenosuspensión con botones ofrece buenos resultados. A pesar de ello, se presentan molestias y dolor en la región supraclavicular, los que son motivo de consulta postquirúrgica y necesidad de revisión para retiro.Presentamos el caso de un paciente de sexo masculino, de treinta y nueve años, quien luego de una caída desde su bicicleta sufre una luxación acromioclavicular tipo V, la que fue tratada mediante sistema de tenosuspensión coracoclavicular y cerclaje acromioclavicular asistida por artroscopía, con buenos resultados. Nivel de Evidencia: IV


Treatment of acromioclavicular dislocations seeks to reduce and control vertical, horizontal, and rotational instability. The use of tenosuspension systems with buttons offers good results. Despite this, there is discomfort and pain in the supraclavicular region, which are the reason for post-surgical consultation and the need for revision for removal.We present a case of a thirty-nine-year-old male patient who suffered a type V acromioclavicular dislocation after falling from a bicycle, which was treated with a coracoclavicular tenosuspension system and arthroscopically assisted acromioclavicular cerclage with good results. Level of Evidence: IV


Sujet(s)
Adulte , Arthroscopie/méthodes , Articulation glénohumérale , Articulation acromioclaviculaire
6.
Article de Espagnol | LILACS, BINACIS | ID: biblio-1523944

RÉSUMÉ

El pinzamiento subcoracoideo es un cuadro poco frecuente y, por lo tanto, su diagnóstico plantea un reto al cirujano ortopédico. Se manifiesta con un dolor sordo en la región subcoracoidea y dolor a la palpación en el proceso coracoideo, como resultado del pinzamiento del músculo subescapular entre el proceso coracoideo y el troquín del húmero. El objetivo de esta nota técnica es describir una alternativa diagnóstica y la inyección guiada por ecografía para atletas lanzadores con pinzamiento subcoracoideo. Nivel de Evidencia: IV


Subcoracoid impingement is a rare condition, therefore, its diagnosis poses a challenge to the orthopedic surgeon. It manifests with dull pain in the subcoracoid region and pain on palpation in the coracoid process as a result of impingement of the subscapularis muscle between the coracoid process and the lesser tubercle of the humerus. The objective of this technical note is to describe an alternative diagnosis and ultrasound-guided injection for throwing athletes with subcoracoid impingement. Level of Evidence: IV


Sujet(s)
Adolescent , Traumatismes sportifs , Articulation glénohumérale , Syndrome de conflit sous-acromial , Apophyse coracoïde
7.
Nat Prod Res ; 35(4): 593-599, 2021 Feb.
Article de Anglais | MEDLINE | ID: mdl-30931622

RÉSUMÉ

Pithecellobium dulce is distributed in America and Asia where is widely used in traditional medicine. This study describes the bioguided fractionation of the methanol extract (ME) obtained from the P. dulce fruit that showed in vitro activity against Hymenolepis nana; Artemia salina assay was used to determine toxicity; and the purified compound was computationally analysed to obtain its absorption-distribution-metabolism-excretion-and-toxicity properties (ADMET). The ME and its fractions were more active than praziquantel (PZQ), and the purified compound was characterized as N-malonyl-(+)-tryptophan (NMT). Parasites treated with NMT showed shorter paralysis and death times (5 and 7 min) than those treated with PZQ (15 and 30 min), both used at 20 mg/mL. Toxicity and ADMET prediction results supported the slight-hazardousness and efficacy of the assayed fractions/compound. This is the first report of the antiparasitary activity of both the P. dulce ME and NMT, showing their potential to treat human H. nana infections.


Sujet(s)
Fabaceae/composition chimique , Fruit/composition chimique , Hymenolepis nana/physiologie , Tryptophane/isolement et purification , Tryptophane/pharmacologie , Animaux , Artemia/effets des médicaments et des substances chimiques , Fractionnement chimique , Humains , Hymenolepis nana/effets des médicaments et des substances chimiques , Extraits de plantes/pharmacologie
8.
Bioorg Chem ; 105: 104359, 2020 12.
Article de Anglais | MEDLINE | ID: mdl-33096310

RÉSUMÉ

The stereoselective synthesis and anti- Hymenolepis nana activity of six Linezolid-type compounds, obtained by chemical modification of l-Alanine, are reported in this work. The synthetic strategy was to prepare diasteromeric N,N-dibenzylamino oxazolidinones 1 and 2, and coupling with 4-(4-bromophenyl)morpholine (3) to obtain N,N-dibenzylamino Linezolid analogues 4 and 5. A hydrogenolysis reaction over 4 and 5 resulted in amino-free Linezolid analogues 6 and 7, which were acetylated to reach diasteromeric Linezolid analogues 8 and 9. The six Linezolid analogues 4-9 show in vitro antiparasitic activity against Hymenolepis nana cestode, but not against several bacterial strains. Interestingly, compounds 6, 7 and 9 exhibit high potency, having shorter paralysis and death times after exposure (6-10 and 18-21 min, respectively), shorter than those found with antihelmintic compound Praziquantel (20 and 30 min) at 20 mg/mL. In addition, a cytocompatibility assay of 6-9 with human cells (ARPE-19 cells) demonstrate a non-cytotoxic effect at 0.4 mM. These results show the pharmacological potential of the newly reported Linezolid-type analogues as antiparasitic agents against Hymenolepis nana.


Sujet(s)
Antibactériens/pharmacologie , Antiparasitaires/pharmacologie , Hymenolepis nana/effets des médicaments et des substances chimiques , Linézolide/pharmacologie , Staphylococcus aureus/effets des médicaments et des substances chimiques , Animaux , Antibactériens/synthèse chimique , Antibactériens/composition chimique , Antiparasitaires/synthèse chimique , Antiparasitaires/composition chimique , Lignée cellulaire , Prolifération cellulaire/effets des médicaments et des substances chimiques , Relation dose-effet des médicaments , Humains , Linézolide/synthèse chimique , Linézolide/composition chimique , Tests de sensibilité microbienne , Simulation de docking moléculaire , Structure moléculaire , Tests de sensibilité parasitaire , Relation structure-activité
9.
Bioorg Chem ; 95: 103483, 2020 01.
Article de Anglais | MEDLINE | ID: mdl-31838285

RÉSUMÉ

Worldwide studies towards development of new drugs with a lower rate in emergence of bacterial resistance have been conducted. The molecular docking analysis gives a possibility to predict the activity of new compounds before to perform their synthesis. In this work, the molecular docking analysis of 64 Linezolid dipeptide-type analogues was performed to predict their activity. The most negative scores correspond to six Fmoc-protected analogues (9as, 9bs, 9bu, 10as, 10ax and 10ay) where Fmoc group interacts in PTC for Linezolid. Twenty-six different Fmoc-protected Linezolid dipeptide-type analogues 9(as-bz) and 10(as-bz) were synthesized and tested in antimicrobial experiments. Compounds 9as, 9ay, 9ax, 10as, 10ay and 9bu show significant activity against group A Streptococcus clinical isolated. Analogue 10ay also display high activity against ATCC 25923 Staphylococcus aureus strain and MRSA-3, MRSA-4 and MRSA-5 clinical isolates, with MIC values lower than Linezolid. The highest activity against multidrug-resistant clinical isolates of Mycobacterium tuberculosis was exhibited by 9bu. Finally, a cytotoxicity assay with ARPE-19 human cells revealed a non-cytotoxic effect of 9bu and 10ay at 50 and 25 µM, respectively.


Sujet(s)
Antibactériens/pharmacologie , Dipeptides/pharmacologie , Conception de médicament , Linézolide/pharmacologie , Mycobacterium tuberculosis/effets des médicaments et des substances chimiques , Staphylococcus aureus/effets des médicaments et des substances chimiques , Antibactériens/synthèse chimique , Antibactériens/composition chimique , Lignée cellulaire , Prolifération cellulaire/effets des médicaments et des substances chimiques , Survie cellulaire/effets des médicaments et des substances chimiques , Dipeptides/synthèse chimique , Dipeptides/composition chimique , Relation dose-effet des médicaments , Humains , Linézolide/synthèse chimique , Linézolide/composition chimique , Tests de sensibilité microbienne , Simulation de docking moléculaire , Structure moléculaire , Relation structure-activité
10.
Bioorg Chem ; 94: 103491, 2020 01.
Article de Anglais | MEDLINE | ID: mdl-31818480

RÉSUMÉ

Imine functionality is found in many compounds with important biological activity. Thus, the development of novel synthetic approaches for imines is important. In this work, it is propose an easy, eco-friendly and straightforward synthesis pathway of aryl imines under microwave irradiation catalyzed by Alumina-sulfuric acid. In addition, the in vitro enzymatic inhibition, antioxidant activity and molecular docking studies were performed. The aryl imines were isolated with yields in the range of 37-94%. All aryl imines synthesized were evaluated for in vitro inhibitory potential against α-glucosidase and α-amylase enzymes and the results exhibited that the most of the compounds displayed inhibitory activity against both enzymes. The (E)-1-(4-nitrophenyl)-N-(pyridin-2-yl)methanimine (3d) was 1.15-fold more active than acarbose against α-amylase whilst the (E)-1-phenyl-N-(pyridin-2-yl)methanimine (3c) displayed similar activity that acarbose against α-glucosidase. The molecular docking studies in α-glucosidase and α-amylase reveal that aryl imines mainly establish an H-bond with the R2-subtituent and hydrophobic interactions with the R1-subtituent. The docking analysis reveals these synthetic aryl imines 3d-i interact in same active site than acarbose drug in both enzymes.


Sujet(s)
Inhibiteurs des glycoside hydrolases/pharmacologie , Imines/pharmacologie , Simulation de docking moléculaire , alpha-Amylases/antagonistes et inhibiteurs , alpha-Glucosidase/métabolisme , Animaux , Relation dose-effet des médicaments , Inhibiteurs des glycoside hydrolases/synthèse chimique , Inhibiteurs des glycoside hydrolases/composition chimique , Humains , Imines/synthèse chimique , Imines/composition chimique , Structure moléculaire , Relation structure-activité , Suidae , alpha-Amylases/métabolisme
11.
Int J Food Sci Nutr ; 71(3): 388-393, 2020 May.
Article de Anglais | MEDLINE | ID: mdl-31530040

RÉSUMÉ

Mexico ranks 2nd in adult obesity and 4th in milk intake worldwide. Low levels of IGF-1 have been related to obesity and can be reverted by milk intake. The rs6214 polymorphism has been associated with an increase in the expression of IGF-1. Therefore, the aim of the study was to evaluate the association between both, rs6214 polymorphism and milk intake, and obesity. We analysed 99 adult volunteers, with and without a history of milk intake, for the presence of this polymorphism through qPCR and body composition by electro-bioimpedance. Univariate logistic regression analyses showed that TT genotype is inversely associated with obesity and body fat mass. Besides, milk intake is also related to low obesity, body fat mass and visceral fat, and high percentage of lean mass. Multivariate logistic regression analyses confirm the univariate relationships, showing a clear inverted association between TT genotype, milk intake and obesity.


Sujet(s)
Régime alimentaire , Facteur de croissance IGF-I/génétique , Lait , Obésité/génétique , Polymorphisme de nucléotide simple , Adulte , Animaux , Composition corporelle/génétique , Femelle , Génotype , Humains , Modèles logistiques , Mâle , Mexique , Adulte d'âge moyen , Jeune adulte
12.
J Food Biochem ; 43(12): e13077, 2019 12.
Article de Anglais | MEDLINE | ID: mdl-31608463

RÉSUMÉ

The water-soluble melanins (SM) of Randia echinocarpa fruit possess interesting biological activities and have been scarcely characterized. In this study, SM were obtained at boiling (SMBT) and room (SMRT) temperatures and characterized by UV-Vis, IR, thermogravimetric analysis, and GC-MS of the hydrolysis products of the SM; besides, the solid-state 13 C NMR, elemental analysis, and acute and sub-acute toxicity of the SMBT were determined. SMBT and SMRT contain organic acids and carbohydrates and their spectroscopic signals and thermograms were similar, but the SMBT yield was higher. The SMBT were characterized by their elemental composition (C 48.260 ± 0.011%, N 3.693 ± 0.009% and H 6.093 ± 0.076%) consistent with the presence of aromatic rings and eumelanins, degradation temperature at 300°C, 13 C NMR signals supporting melanin-bonding with carbohydrates and organic acids, and innocuity in Balb/C mice (acute assay, LD50  > 5 g/kg b.w.; sub-acute assay, no lethality at 500 mg/kg b.w. for 30 days). PRACTICAL APPLICATIONS: The consumption of melanins has been associated with health benefits because of their biological activities (e.g., antioxidant, immunostimulatory, UV- and radiation-protective). Randia echinocarpa is employed in Mexican traditional medicine against chronic degenerative diseases (e.g., cancer and diabetes) and ailments of organs (e.g., kidney and lung) and systems (e.g., circulatory and gastrointestinal). The R. echinocarpa fruit contains water-soluble melanins (SM) that inhibit carbohydrate-digestive enzymes and show high antioxidant activity; thus, SM could be useful for the prevention and treatment of diabetes. This study showed that the SM structure contains melanin-bonding organic acids and carbohydrates, which could be associated with the SM solubility and higher yield, and that SMBT were innocuous in the acute and sub-acute assays in mice. Thus, the R. echinocarpa SMBT could be used as safe potential ingredients to develop functional products.


Sujet(s)
Fruit/composition chimique , Mélanines/analyse , Extraits de plantes/analyse , Animaux , Souris , Souris de lignée BALB C , Rubiaceae , Solubilité , Tests de toxicité
13.
Eur J Pharmacol ; 863: 172699, 2019 Nov 15.
Article de Anglais | MEDLINE | ID: mdl-31563650

RÉSUMÉ

Nonalcoholic fatty liver disease (NAFLD) is the most common liver disease in the world. Despite the impact of this pathology in the population, nowadays there is no specific treatment for this disease, focusing its treatment on risks factors. However, it is imperative the existence of a specific treatment, due to this, the aim of this study was to determine the therapeutic effect of treatment with metformin, 4-hydroxychalcone or co-treatment on male Wistar rats with NAFLD. Wistar rats were divided into two groups with free access to either tap water or 50% sucrose (NAFLD) during 25 weeks. After 20 weeks of induction each were divided into four groups that received daily p.o. administration of: i) saline solution (1 ml); ii) metformin (200 mg/kg/day); iii) 4-hydroxychalcone (80 mg/kg/day) and i.v.) co-treatment (metformin plus 4-hydroxychalcone at the doses mentioned above), for 5 weeks. In healthy rats: metformin and co-treatment modified food and total caloric intake and induced diarrhea; but none of the treatments changed the other parameters evaluated. Meanwhile in rats with NAFLD: i) metformin inhibited hepatic total cholesterol and TGF-ß, increased diarrhea frequency, and slightly decreased liver steatosis, and fibrosis; ii) 4-hydroxychalcone decreased IL-6, TNF-α and TGF-ß, increased IL-10, and markedly decreased liver steatosis and fibrosis; and iii) co-treatment markedly decreased food intake, total caloric intake, and body weight, increased diarrhea; increased IL-10, showing and intermediate effect on decrease TNF-α, TGF-ß, liver steatosis and fibrosis. Our results showed that 4-hydroxychalcone treatment was the most effective among the treatments tested against NAFLD.


Sujet(s)
Chalcones/pharmacologie , Metformine/pharmacologie , Stéatose hépatique non alcoolique/traitement médicamenteux , Animaux , Chalcones/usage thérapeutique , Collagène/biosynthèse , Cytokines/sang , Diarrhée/complications , Interactions médicamenteuses , Consommation alimentaire/effets des médicaments et des substances chimiques , Foie/effets des médicaments et des substances chimiques , Foie/métabolisme , Foie/anatomopathologie , Mâle , Metformine/usage thérapeutique , Stéatose hépatique non alcoolique/sang , Stéatose hépatique non alcoolique/complications , Stéatose hépatique non alcoolique/anatomopathologie , Nutriments/métabolisme , Rats , Rat Wistar
14.
Can J Physiol Pharmacol ; 97(1): 23-36, 2019 Jan.
Article de Anglais | MEDLINE | ID: mdl-30388378

RÉSUMÉ

The high intake of sweetened drinks is associated with obesity and insulin resistance. These pathologies are directly related to the development of nonalcoholic fatty liver disease (NAFLD), considered a condition of metabolic syndrome (MS). Due to their increasing worldwide prevalence, experimental animal models have been developed to gain a better understanding of its physiopathology; notwithstanding, few studies have evaluated its progression in association with MS and ingestion of sweetened drinks. Therefore, the aim of this study was to understand the pathophysiologic characteristics of NAFLD related to sucrose concentration and time of ingestion in rats. Wistar rats were divided into 2 groups with free access to either tap water or 30% sucrose, and euthanized at 12, 16, or 20 weeks; and 2 additional groups were given free access to either 40% or 50% sucrose and were euthanized at 20 weeks. Biochemical parameters and levels of serum cytokines were measured, and histology was performed. Ingestion of 30% sucrose induced liver steatosis until 16 weeks (grade 2) and 20 weeks (grade 3). Meanwhile, during 20 weeks, 40% sucrose induced grade 5 of nonalcoholic steatohepatitis (NASH) and 50% sucrose induced grade 6 of NASH and fibrosis. This study demonstrated that increasing time of induction and concentration of sucrose ingestion resulted in a higher grade of NAFLD.


Sujet(s)
Saccharose alimentaire/administration et posologie , Saccharose alimentaire/effets indésirables , Stéatose hépatique non alcoolique/étiologie , Stéatose hépatique non alcoolique/anatomopathologie , Animaux , Poids/physiologie , Cytokines/sang , Mâle , Stéatose hépatique non alcoolique/sang , Obésité/sang , Obésité/étiologie , Obésité/anatomopathologie , Rats , Rat Wistar , Facteurs temps
15.
Plant Foods Hum Nutr ; 73(4): 308-313, 2018 Dec.
Article de Anglais | MEDLINE | ID: mdl-30238426

RÉSUMÉ

Red arils of Pithecellobium dulce fruit, commonly known as guamuchil, show high antioxidant (AOx) and α-glucosidase inhibitory (IαG) activities, which have been mainly associated with the content of unknown anthocyanins. In this study, the AOx (i.e., DPPH and ABTS as Trolox equivalents, µmol TE/g) and IαG (as half-maximal inhibitory concentration, IC50, mg/mL) activities of the anthocyanin-rich fraction (ARF) obtained from red arils were contrasted with those of the methanol extract (ME), and the main ARF anthocyanins were characterized by HPLC-DAD-ESI-MS, GC-MS and 1H-NMR. The AOx and IαG values of the ARF (DPPH = 597.8; ABTS = 884.01; IαG = 0.06) were better than those of the ME (DPPH = 41.5; ABTS = 142.3; IαG = 17.5); remarkably, the ARF IαG value was about 42 times lower than that of acarbose. The main anthocyanins in ARF were pelargonidin 3-O-glucoside and cyanidin 3-O-glucoside. Thus, the consumption of red P. dulce arils could provide health benefits for prevention/treatment of chronic degenerative diseases such as diabetes.


Sujet(s)
Anthocyanes/analyse , Anthocyanes/pharmacologie , Antioxydants/pharmacologie , Fabaceae/composition chimique , Inhibiteurs des glycoside hydrolases/pharmacologie , Anthocyanes/composition chimique , Antioxydants/composition chimique , Chromatographie en phase liquide à haute performance , Fruit/composition chimique , Chromatographie gazeuse-spectrométrie de masse , Glucosides/analyse , Glucosides/pharmacologie , Inhibiteurs des glycoside hydrolases/composition chimique , Spectroscopie par résonance magnétique , Spectrométrie de masse ESI
16.
Braz. J. Pharm. Sci. (Online) ; 54(3): e17343, 2018. tab, graf
Article de Anglais | LILACS | ID: biblio-974391

RÉSUMÉ

The hymenolepiosis by Hymenolepis nana is a major public health problem in developing countries, and the commercial drugs against this parasitosis are not enough effective. The combination of antiparasitic and antioxidant agents has improved the treatment of some parasitoses. Thus, the development of new cestocidal and antioxidant agents to treat the hymenolepiosis cases is important. In the present study, four hydroxy- and four dihydroxy-chalcones were synthesized using the catalyst boron trifluoride diethyl etherate (BF3•OEt2). The antioxidant activity and antiparasitic against H. nana of chalcones were tested, as well as the toxicity by the brine shrimp lethality bioassay and the method of Lorke. The antioxidant activity was measured by three radical scavenging assays: 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing antioxidant power (FRAP). The hydroxyl substitution pattern (number and position), mainly in ring B, was responsible for the chalcone antiparasitic activity. At least one meta or para hydroxyl group in ring B was essential for activity of the synthetic chalcones against H. nana; The time taken for the parasite to die by the 3b and 3e chalcones (20 mg/mL) treatment was up to six times lower than the control drug Praziquantel. On the other hand, chalcones with catechol structure in ring B (3g and 3h) showed the highest antioxidant values. The toxicity evaluations suggests that synthetic hydroxychalcones with cestocidal (3b and 3e) and antioxidant (3g and 3h) activities are safe compounds and potential in vivo agents to treat this parasitosis


Sujet(s)
Maladies parasitaires/traitement médicamenteux , Hymenolepis nana/immunologie , Chalcones/administration et posologie , Antioxydants/effets indésirables , Antiparasitaires/effets indésirables
17.
Pharm Biol ; 55(1): 1473-1482, 2017 Dec.
Article de Anglais | MEDLINE | ID: mdl-28347185

RÉSUMÉ

CONTEXT: Helicteres vegae Cristóbal (Sterculiaceae) (Hv) and Heliopsis sinaloensis B.L. Turner (Asteraceae) (Hs) are endangered and poorly studied plant species; related plants have been used against chronic-degenerative and infectious diseases. Therefore, Hv and Hs could be sources of bioactive compounds against these illnesses. OBJECTIVE: To determine the chemical composition and biological activities (antioxidant, antimutagenic and antimicrobial) of Hv and Hs leaves (L) and stems (S). MATERIALS AND METHODS: Methanol extracts (ME) of each plant/tissue were evaluated for their phytochemicals; phenolics (HPLC-DAD-ESI-MS); antioxidant activity (AA) (0.125-4 mg/mL) (DPPH, ABTS, ORAC and ß-carotene discoloration); antimutagenicity (0.5 and 1 mg/plate) (Ames assay, tester strain Salmonella enterica serovar Typhimurium YG1024, 1-nitropyrene as mutagen); activity against human pathogens (1 mg/mL); and toxicity (0.01-2 mg/mL) (Artemia salina assay). RESULTS: All ME showed flavonoids and triterpenes/steroids. The ME-SHv had the highest content of total phenolics (TP) (2245.82 ± 21.45 mg GAE/100 g d.w.) and condensed tannins (603.71 ± 1.115 mg CE/100 g d.w.). The compounds identified were flavonoids (kaempferol 7-O-coumaroylhexoside, and two kaempferol 7-O-rhamnosylhexosides) and phenolics [rosmarinic acid, and 3'-O-(8″-Z-caffeoyl) rosmarinic acid]. The ME-LHs showed the highest content of flavonoids (357.88 mg RE/g d.w.) and phenolic acids (238.58 mg CAE/g d.w.) by HPLC. The ME-SHv showed the highest AA. All ME were strong antimutagens (63.3-85.7%). Only the Hs extracts were toxic (ME-LHs, LC50 = 94.9 ± 1.7 µg/mL; ME-SHs, LC50 = 89.03 ± 4.42 µg/mL). DISCUSSION AND CONCLUSIONS: Both Hv and Hs are potential sources of preventive and therapeutic agents against chronic-degenerative diseases.


Sujet(s)
Anti-infectieux/pharmacologie , Antimutagènes/pharmacologie , Antioxydants/pharmacologie , Asteraceae/composition chimique , Malvaceae/composition chimique , Extraits de plantes/pharmacologie , Animaux , Anti-infectieux/composition chimique , Anti-infectieux/isolement et purification , Anti-infectieux/toxicité , Antimutagènes/composition chimique , Antimutagènes/isolement et purification , Antimutagènes/toxicité , Antioxydants/composition chimique , Antioxydants/isolement et purification , Antioxydants/toxicité , Artemia/effets des médicaments et des substances chimiques , Bactéries/effets des médicaments et des substances chimiques , Bactéries/croissance et développement , Benzothiazoles/composition chimique , Dérivés du biphényle/composition chimique , Chromatographie en phase liquide à haute performance , Giardia lamblia/effets des médicaments et des substances chimiques , Giardia lamblia/croissance et développement , Méthanol/composition chimique , Tests de sensibilité microbienne , Tests de mutagénicité , Capacité d'absorption des radicaux oxygénés , Tests de sensibilité parasitaire , Phytothérapie , Picrates/composition chimique , Extraits de plantes/composition chimique , Extraits de plantes/isolement et purification , Extraits de plantes/toxicité , Feuilles de plante/composition chimique , Tiges de plante/composition chimique , Plantes médicinales , Salmonella typhimurium/effets des médicaments et des substances chimiques , Salmonella typhimurium/génétique , Solvants/composition chimique , Spectrométrie de masse ESI , Acides sulfoniques/composition chimique , Bêtacarotène/composition chimique
18.
Biomed Res Int ; 2015: 905204, 2015.
Article de Anglais | MEDLINE | ID: mdl-26090457

RÉSUMÉ

Background and Objectives. A new two-step hysteroscopic myomectomy carried out in the office setting and without anesthesia was feasible for the excision of submucous myomas. The objective of this study was to assess whether removal of submucous myomas from the uterine cavity after hysteroscopic laser enucleation is necessary. Methods. Between June 2009 and April 2013, all outpatients with symptomatic myomatosis (bleeding, pelvic pain, and infertility) assessed ultrasonographically were eligible to participate in a prospective study. All patients underwent office hysteroscopic enucleation of submucous myomas. Enucleated myomas were left in the uterine cavity. Neither anesthesia nor antibiotic prophylaxis was used. Results. Sixty-one women (mean age: 47.3 years) were included. Regardless of hysteroscopic localization and grading, all myomas were enucleated. The mean (standard deviation, SD) diameter of the myoma as measured by the ultrasound scan was 22.6 (8.5) mm. In 29 cases (47.5%), the diameter of the resected myoma was >20 mm and in 10 cases (16.4%) >30 mm. After a mean follow-up of 68.2 (16.5) days, none of the patients showed a residual myoma inside the uterine cavity. Conclusions. The present results indicate that leaving laser-enucleated submucous myoma in the uterine cavity is a feasible and safe therapeutic option.


Sujet(s)
Hystéroscopie , Myome/chirurgie , Myomectomie de l'utérus , Tumeurs de l'utérus/chirurgie , Adulte , Brésil , Femelle , Humains , Lasers , Adulte d'âge moyen , Myome/anatomopathologie , Tumeurs de l'utérus/anatomopathologie
19.
Int J Mol Sci ; 15(4): 5277-91, 2014 Mar 26.
Article de Anglais | MEDLINE | ID: mdl-24675696

RÉSUMÉ

Staphylococcus aureus is one of the most common causes of nosocomial infections. The purpose of this study was the synthesis and in vitro evaluation of antimicrobial activity of 10 new 3-oxazolidin-2-one analogues on 12 methicillin resistant S. aureus (MRSA) clinical isolates. S. aureus confirmation was achieved via catalase and coagulase test. Molecular characterization of MRSA was performed by amplification of the mecA gene. Antimicrobial susceptibility was evaluated via the Kirby-Bauer disc diffusion susceptibility test protocol, using commonly applied antibiotics and the oxazolidinone analogues. Only (R)-5-((S)-1-dibenzylaminoethyl)-1,3-oxazolidin-2-one (7a) exhibited antibacterial activity at 6.6 µg. These results, allow us to infer that molecules such as 7a can be potentially used to treat infections caused by MRSA strains.


Sujet(s)
Antibactériens/pharmacologie , Staphylococcus aureus résistant à la méticilline/effets des médicaments et des substances chimiques , Oxazolidinones/pharmacologie , Infections à staphylocoques/traitement médicamenteux , Animaux , Antibactériens/effets indésirables , Antibactériens/synthèse chimique , Artemia/effets des médicaments et des substances chimiques , Protéines bactériennes/génétique , Tests d'agents antimicrobiens par diffusion à partir de disques , Multirésistance bactérienne aux médicaments , Oxazolidinones/effets indésirables , Oxazolidinones/synthèse chimique , Protéines de liaison aux pénicillines , Inhibiteurs de la synthèse protéique/effets indésirables , Inhibiteurs de la synthèse protéique/synthèse chimique , Inhibiteurs de la synthèse protéique/pharmacologie , Résistance aux bêta-lactamines/génétique
20.
ScientificWorldJournal ; 2014: 725981, 2014.
Article de Anglais | MEDLINE | ID: mdl-24511299

RÉSUMÉ

A regioselective synthesis has been developed for the preparation of a series of N,N'-disubstituted 4,4'-carbonylbis(carbamoylbenzoic) acids and N,N'-disubstituted bis(carbamoyl) terephthalic acids by treatment of 3,3',4,4'-benzophenonetetracarboxylic dianhydride (1) and 1,2,4,5-benzenetetracarboxylic dianhydride (2) with arylalkyl primary amines (A-N). The carbamoylcarboxylic acid derivatives were synthesized with good yield and high purity. The specific reaction conditions were established to obtain carbamoyl and carboxylic acid functionalities over the thermodynamically most favored imide group. Products derived from both anhydrides 1 and 2 were isolated as pure regioisomeric compounds under innovative experimental conditions. The chemo- and regioselectivity of products derived from dianhydrides were determined by NMR spectroscopy and confirmed by density functional theory (DFT). All products were characterized by NMR, FTIR, and MS.


Sujet(s)
Anhydrides/composition chimique , Acides carboxyliques/composition chimique , Acides carboxyliques/synthèse chimique , Techniques de chimie synthétique , Modèles moléculaires , Conformation moléculaire
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