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1.
J Endocrinol Invest ; 44(12): 2741-2748, 2021 Dec.
Article de Anglais | MEDLINE | ID: mdl-34173961

RÉSUMÉ

INTRODUCTION: Obstructive sleep apnoea (OSA) is an underdiagnosed condition frequently associated with glycaemic control impairment in patients with type 2 diabetes. AIM: To assess the relationship between glycometabolic parameters and OSA in obese non-diabetic subjects. METHODS: Ninety consecutive subjects (mean age 44.9 ± 12 years, mean BMI 42.1 ± 9 kg/m2) underwent polysomnography and a 2-h oral glucose tolerance test (OGTT). RESULTS: OSA was identified in 75% of subjects, with a higher prevalence of males compared to the group of subjects without OSA (62% vs 32%, p = 0.02). Patients with OSA had comparable BMI (42.8 kg/m2 vs 39.4 kg/m2), a higher average HbA1c (5.8% vs 5.4%, p < 0.001), plasma glucose at 120 min during OGTT (2 h-PG; 123 mg/dl vs 97 mg/dl, p = 0.009) and diastolic blood pressure (81.1 mmHg vs 76.2 mmHg, p = 0.046) than obese subjects without OSA. HbA1c and 2 h-PG were found to be correlated with the apnoea-hypopnoea index (AHI; r = 0.35 and r = 0.42, respectively) and with percent of sleep time with oxyhaemoglobin saturation < 90% (ST90; r = 0.44 and r = 0.39, respectively). Further, in a linear regression model, ST90 and AHI were found to be the main determinants of 2 h-PG (ß = 0.81, p < 0.01 and ß = 0.75, p = 0.02, respectively) after controlling for age, sex, waist circumference, physical activity, and C-reactive protein. Similarly, ST90 and AHI persisted as independent determinants of HbA1c (ß = 0.01, p = 0.01 and ß = 0.01, p = 0.01, respectively). CONCLUSION: Beyond the traditional clinical parameters, the presence of a normal-high value of 2 h-PG and HbA1c should raise suspicion of the presence of OSA in obese subjects.


Sujet(s)
Glycémie/métabolisme , Hémoglobine glyquée/analyse , Hyperglycémie , Obésité , Syndrome d'apnées obstructives du sommeil , Adulte , Indice de masse corporelle , Femelle , Hyperglycémie provoquée/méthodes , Humains , Hyperglycémie/diagnostic , Hyperglycémie/épidémiologie , Hyperglycémie/étiologie , Mâle , Obésité/diagnostic , Obésité/épidémiologie , Obésité/métabolisme , Obésité/physiopathologie , Polysomnographie/méthodes , Période post-prandiale , Prévalence , Facteurs de risque , Indice de gravité de la maladie , Syndrome d'apnées obstructives du sommeil/sang , Syndrome d'apnées obstructives du sommeil/diagnostic , Syndrome d'apnées obstructives du sommeil/épidémiologie , Syndrome d'apnées obstructives du sommeil/physiopathologie
2.
Helminthologia ; 56(1): 30-41, 2019 Mar.
Article de Anglais | MEDLINE | ID: mdl-31662670

RÉSUMÉ

Plant parasitic nematodes (PPN) are important pests of numerous agricultural crops especially vegetables, able to cause remarkable yield losses correlated to soil nematode population densities at sowing or transplant. The concern on environmental risks, stemming from the use of chemical pesticides acting as nematicides, compels to their replacement with more sustainable pest control strategies. To verify the effect of aqueous extracts of the agro-industry waste coffee silverskin (CS) and brewers' spent grain (BSG) on the widespread root-knot nematode Meloidogyne incognita, and on the physiology of tomato plants, a pot experiment was carried out in a glasshouse at 25 ± 2 °C. The possible phytotoxicity of CS and BSG extracts was assessed on garden cress seeds. Tomato plants (landrace of Apulia Region) were transplanted in an artificial nematode infested soil with an initial population density of 3.17 eggs and juveniles/mL soil. CS and BSG were applied at rates of 50 and 100 % (1L/pot). Untreated and Fenamiphos EC 240 (nematicide) (0.01 µL a.i./mL soil) treated plants were used as controls. Reactive oxygen species (ROS) and chlorophyll content of tomato plants were estimated during the experiment. CS extract, at both doses, significantly reduced nematode population in comparison to the untreated control, although it was less effective than Fenamiphos. BSG extract did not reduce final nematode population compared to the control. Ten days after the first treatment, CS 100 %, BSG 50 % and BSG 100% elicited the highest ROS values, which considerably affected the growth of tomato plants in comparison to the untreated plants. The control of these pests is meeting with difficulties because of the current national and international regulations in force, which are limiting the use of synthetic nematicides. Therefore, CS extracts could assume economic relevance, as alternative products to be used in sustainable strategies for nematode management.

3.
Front Microbiol ; 10: 1550, 2019.
Article de Anglais | MEDLINE | ID: mdl-31333636

RÉSUMÉ

An increasing consumer demand for pomegranate has been globally observed, mainly thanks to the scientific evidence related to its functional and health-promoting features. Pomegranate fruits from twenty accessions identified in Southeastern Italy were characterized according to morphological and chemical features. Juices extracted from pomegranate fruits were fermented with selected Lactobacillus plantarum PU1 and the antioxidant activity investigated. Whey was added to juices to promote the microbial growth. Fermentation led to the increase of the radical scavenging activity (up to 40%) and significant inhibition of the linoleic acid peroxidation. The three fermented juices showing the highest antioxidant activity, and the corresponding unfermented controls, were further characterized. In detail, the cytotoxicity and the protective role toward artificially induced oxidative stress were determined on murine fibroblasts Balb 3T3 through the determination of the viability and the intracellular ROS (reactive oxygen species) scavenging activity (RSA). RSA reached values of ca. 70% in fermented juices, being ca. 40% higher than the unfermented and control samples. Phenols compounds of the pomegranate juices obtained from accessions "Bitonto Piscina," "Sanrà nero," and "Wonderful (reference cultivar) were analyzed through ultrahigh pressure liquid chromatography coupled with mass spectrometry, showing that a marked increase (up to 60%) of the ellagitannins derivatives occurred during fermentation. Sensory analysis showed suitability of the fermented juices to be used as beverage and food ingredient.

4.
J Dairy Sci ; 101(7): 5751-5757, 2018 Jul.
Article de Anglais | MEDLINE | ID: mdl-29605328

RÉSUMÉ

Ricotta forte is a traditional whey cheese, obtained through natural fermentation of fresh ricotta, that is getting increasing attention by food traders. In view of possible initiatives for its valorization, the chemical and sensory characteristics were investigated. Samples were obtained from 14 different manufacturer, and were subjected to chemical, biochemical, volatile organic compound, and sensory analyses. All samples presented low pH with high moisture (62-66%) and fat content (57-60% on dry matter). From a biochemical point of view, the electrophoretic patterns evidenced that ß-lactoglobulin was the main protein present at all sample ages. Only intermediate levels of proteolysis (20.69% ripening index) took place during aging, whereas the main biochemical event in this dairy product was lipolysis (2.10 mEq/g of acid degree value). Accordingly, free fatty acids dominated the volatile organic compound profile and strongly influenced the sensory characteristics with flavor described as rancid, pungent, acrid, and smelly feet: all associated with short-chain fatty acids such as acetic, propionic, butyric, and caproic. Finally, the sample age did not influence chemical composition, whereas it had significant effect on lipolysis and flavor intensity.


Sujet(s)
Fromage/normes , Manipulation des aliments/méthodes , Goût , Lactosérum/métabolisme , Animaux , Fromage/analyse , Produits laitiers , Protéines de lactosérum
5.
Food Chem ; 233: 385-390, 2017 Oct 15.
Article de Anglais | MEDLINE | ID: mdl-28530589

RÉSUMÉ

Lactose intolerance is the decreased ability to digest lactose, and the population involved is rapidly increasing all over the world. Different procedures have been reported in the literature to quantify lactose in dairy products, but the official method of analysis is based on enzymatic assay. In this paper, the effectiveness of two enzymatic kits in detecting residual lactose in lactose-free milk was investigated, and a comparison with two alternative chromatographic methods was done. The investigation used several samples of UHT milk containing different levels of lactose, and the results highlighted the inadequacy of the enzymatic assays and of the HPLC-RI method to analyse lactose-free milk. An LC-MS/MS method using the formate adduct was developed, and it allowed quantitation of lactose and lactulose in all samples at a high level of precision and repeatability.


Sujet(s)
Lait/composition chimique , Animaux , Chromatographie en phase liquide à haute performance , Dosages enzymatiques , Lactose , Spectrométrie de masse en tandem
6.
J Dairy Sci ; 99(8): 6080-6085, 2016 Aug.
Article de Anglais | MEDLINE | ID: mdl-27179855

RÉSUMÉ

Canestrato di Moliterno is an Italian Protected Geographical Indication hard cheese, made in winter and spring from a mixture of ewe and goat milks, that has been poorly investigated. The present study was aimed at characterizing the cheese made in the warm season. Two series of samples, ripened in traditional rooms called fondaco as indicated in the official protocol of production, were taken from the main certified producers. The cheeses were analyzed for gross composition; proteolysis and lipolysis; volatile fraction; and organoleptic features. Gross composition was not completely homogeneous among the samples, but primary proteolysis and lipolysis were quite uniform. We observed variations in secondary proteolysis, likely caused by fluctuations in environmental conditions in the fondaco. The sensory profiles of the samples were homogeneous: the cheese was soluble, greasy, and adhesive, with a sheepfold and buttery odor. The main taste attributes were fermented, pungent, and bitter. Overall, the results of this study provide an initial contribution to the characterization of Canestrato di Moliterno, and could be used to improve marketing strategies.


Sujet(s)
Fromage/analyse , Capra , Saisons , Sensation , Ovis , Animaux , Femelle , Manipulation des aliments/méthodes , Italie , Lipolyse , Lait/composition chimique , Protéolyse , Goût
7.
J Dairy Sci ; 98(3): 1402-10, 2015 Mar.
Article de Anglais | MEDLINE | ID: mdl-25547300

RÉSUMÉ

Innovation in the small ruminant dairy sector faces structural challenges because dairies are often involved in breeding and produce cheeses that appeal essentially to local markets using traditional technologies and facilities. An investigation was carried out to produce Fior di latte, a traditional, soft pasta filata cheese, from sheep and goat milks at the farm level. Fior di latte is an Italian high-moisture, round mozzarella currently produced from cow and water buffalo milks; it is very popular in Europe. Cheesemaking trials were performed and the most appropriate technology proved to be a combination of direct acidification and lactic fermentation, with some modifications to the milk coagulation phase. The gross composition of the experimental cheeses was similar to that of bovine Fior di latte, and the overall hygienic quality was satisfactory even though the milk had not been pasteurized. The new cheeses were similar in appearance to the bovine type, but some specific features were detected. Besides the typical "goaty" and "sheepy" flavors, some novel and distinctive descriptors of odor, flavor, and texture were noted. Our experiment showed that good quality Fior di latte cheese that complies with microbiological requirements of the European legislation can be obtained from sheep and goat milks by appropriately modifying the cheesemaking technology.


Sujet(s)
Fromage/analyse , Manipulation des aliments/méthodes , Lait/composition chimique , Animaux , Buffles , Bovins , Fromage/microbiologie , Fromage/normes , Matières grasses alimentaires/analyse , Femelle , Fermentation , Manipulation des aliments/normes , Microbiologie alimentaire , Qualité alimentaire , Capra , Mâle , Lait/microbiologie , Protéines de lait/analyse , Odorisants , Ovis aries , Goût
8.
Food Chem ; 129(2): 319-328, 2011 Nov 15.
Article de Anglais | MEDLINE | ID: mdl-30634233

RÉSUMÉ

Spaghetti were produced in a pilot plant from semolina and semolina blended with increasing amounts of barley flour. According to size exclusion high-performance liquid chromatography (SE-HPLC), barley proteins interact with semolina proteins during pasta making, forming polymers of high molecular weight. Of these, the unextractable polymeric proteins (UPP) were at significantly higher concentrations than in spaghetti made from semolina. The decrease of both S-S bonds and -SH free groups in barley semolina spaghetti, with respect to that made of semolina, suggested that polymerisation among the different classes of proteins involves a new bonding arrangement. Due to ß-glucan hydrophilicity and competition with starch for water, the replacement of increasing amounts of semolina with barley flour was able to increase the optimal cooking time. The sensory properties of composite spaghetti were judged as better than the control because of the higher firmness and the lower bulkiness and stickiness of the former.

9.
J Dairy Sci ; 93(8): 3487-96, 2010 Aug.
Article de Anglais | MEDLINE | ID: mdl-20655416

RÉSUMÉ

This study was undertaken to evaluate the effect of lamb rennet paste containing probiotic strains on proteolysis, lipolysis, and glycolysis of ovine cheese manufactured with starter cultures. Cheeses included control cheese made with rennet paste, cheese made with rennet paste containing Lactobacillus acidophilus culture (LA-5), and cheese made with rennet paste containing a mix of Bifidobacterium lactis (BB-12) and Bifidobacterium longum (BB-46). Cheeses were sampled at 1, 7, 15, and 30 d of ripening. Starter cultures coupled with probiotics strains contained in rennet paste affected the acidification and coagulation phases leading to the lowest pH in curd and cheese containing probiotics during ripening. As consequence, maturing cheese profiles were different among cheese treatments. Cheeses produced using rennet paste containing probiotics displayed higher percentages of alpha(S1)-I-casein fraction than traditional cheese up to 15 d of ripening. This result could be an outcome of the greater hydrolysis of alpha-casein fraction, attributed to higher activity of the residual chymosin. Further evidence for this trend is available in chromatograms of water-soluble nitrogen fractions, which indicated a more complex profile in cheeses made using lamb paste containing probiotics versus traditional cheese. Differences can be observed for the peaks eluted in the highly hydrophobic zone being higher in cheeses containing probiotics. The proteolytic activity of probiotic bacteria led to increased accumulation of free amino acids. Their concentrations in cheese made with rennet paste containing Lb. acidophilus culture and cheese made with rennet paste containing a mix of B. lactis and B. longum were approximately 2.5 and 3.0 times higher, respectively, than in traditional cheese. Principal component analysis showed a more intense lipolysis in terms of both free fatty acids and conjugated linoleic acid content in probiotic cheeses; in particular, the lipolytic pattern of cheeses containing Lb. acidophilus is distinguished from the other cheeses on the basis of highest content of health-promoting molecules. The metabolic activity of the cheese microflora was also monitored by measuring acetic, lactic, and citric acids during cheese ripening. Cheese acceptability was expressed for color, smell, taste, and texture perceived during cheese consumption. Use of probiotics in trial cheeses did not adversely affect preference or acceptability; in fact, panelists scored probiotic cheeses higher in preference over traditional cheese, albeit not significantly.


Sujet(s)
Fromage/analyse , Chymosine/métabolisme , Glycolyse , Lipolyse , Protéines de lait/métabolisme , Probiotiques/métabolisme , Animaux , Bifidobacterium/classification , Bifidobacterium/métabolisme , Fromage/microbiologie , Manipulation des aliments/méthodes , Microbiologie alimentaire , Lactobacillus acidophilus/métabolisme , Ovis
10.
Protein J ; 28(7-8): 333-40, 2009 Oct.
Article de Anglais | MEDLINE | ID: mdl-19771496

RÉSUMÉ

An interesting and quite complex protein pattern has been described at ovine milk proteins but the genetic control of the variation observed was assessed only in few cases. The aim of this work was to characterize the ovine alpha ( s2 )-casein (CSN1S2) B variant, first observed in the Italian Gentile di Puglia, a fine-wooled ovine breed, and to investigate its occurrence in two further breeds, the Sarda and Camosciata, which are the most widespread dairy breeds in Italy. The B variant differs from the most common form A with two amino acid exchanges: Asp(75) --> Tyr(75) and Ile(105) --> Val(105). The first substitution, resulting in a loss of a negative charge, is responsible for the higher isoelectric point of the B protein variant, which allows its detection by isoelectric focusing electrophoresis (IEF). The occurrence of CSN1S2*B in Sarda and Comisana was demonstrated. Since the Asp(75) --> Tyr(75) substitution modifies the protein electric charge, milk properties may result affected to some extent.


Sujet(s)
Allèles , Caséines/génétique , Polymorphisme génétique , Animaux , Focalisation isoélectrique , Protéines de lait/génétique , Mutation faux-sens , Ovis , Électricité statique
11.
J Dairy Sci ; 92(9): 4211-7, 2009 Sep.
Article de Anglais | MEDLINE | ID: mdl-19700682

RÉSUMÉ

The effect of some quality parameters of the milk (refrigeration time, pH, protein, and fat/protein ratio) on the extent of acidification in the production technology of table Mozzarella without starters was investigated. A screening phase carried out at the laboratory level demonstrated that variations of the milk characteristics require different levels of acidification to keep constant the quality of the cheese. The elaboration of the data collected throughout the successive experimentation on industrial scale allowed us to find a mathematical model to describe the relationships between the pH of the curd at stretching time and the milk characteristics, of which the protein concentration and the refrigeration time play the main roles.


Sujet(s)
Fromage/normes , Lait/composition chimique , Lait/normes , Analyse de variance , Animaux , Fromage/analyse , Manipulation des aliments , Concentration en ions d'hydrogène , Facteurs temps
12.
J Food Sci ; 74(4): C307-11, 2009.
Article de Anglais | MEDLINE | ID: mdl-19490316

RÉSUMÉ

Capillary electrophoresis was used to characterize glutenin proteins from ancient varieties of Southern Italy common wheat and to determine the technological properties of wheat flours based on a glutenin index. Three zones were identified in the electropherograms, indicated as A, B, and C according to electroelution order. The three zones corresponded to the low molecular weight glutenin subunits and to the y- and x-type high molecular weight subunits, respectively. The ratio B/C was correlated to the alveographic parameter P/L. These results indicated that flours resulting in a B/C ratio lower than 2 produced elastic doughs whereas flours resulting in a B/C ratio higher than 2 produced doughs more resistant to extension. This study showed that capillary electrophoresis is useful for determining the types and quantities of gluten proteins in the evaluation of wheat-flour technological properties of a limited number of noncommercial varieties as evidenced by the x-type content which seems to strongly influence the flour technological parameters.


Sujet(s)
Électrophorèse capillaire , Farine/analyse , Glutens/analyse , Triticum/composition chimique , Électrophorèse sur gel de polyacrylamide , Glutens/composition chimique , Masse moléculaire , Sous-unités de protéines/analyse , Sous-unités de protéines/composition chimique , Rhéologie
13.
J Dairy Sci ; 92(4): 1319-29, 2009 Apr.
Article de Anglais | MEDLINE | ID: mdl-19307613

RÉSUMÉ

The safeguard of river buffalo Mozzarella cheese, a Protected Designation of Origin dairy product, has prompted an analytical study to trace the milk and curd used as raw material in cheesemaking. This is to prevent the illegal use of milk or curd from different geographical areas outside of those indicated in the official production protocol. For this purpose, we studied primary proteolysis occurring in fresh and frozen milk and curd to identify a molecular marker that could indicate the raw material used. Whole casein from frozen river buffalo milk was separated using cation-exchange chromatography and sodium dodecyl sulfate-PAGE, and a protein component with an estimated molecular weight of 15.3 kDa was detected. This protein component was revealed in fresh river buffalo milk as a faint electrophoresis band, which drastically increased in intensity in refrigerated and frozen milk as well as in curd and was found to be associated with beta-CN through hydrophobic interaction. By using matrix-assisted laser desorption/ionization-time of flight peptide mass mapping, this component was identified as the C-terminal fragment f(69-209) of beta-CN (expected molecular weight of 15,748.8 Da). beta-Casein f(69-209), originating from the early hydrolysis of Lys(68)-Ser(69) by plasmin, has no counterpart in bovine milk. The increased rate of hydrolysis by plasmin toward the cleavage site Lys(68)-Ser(69) has to be ascribed to the elevated proline content of the peptide 61-73. The favored production of beta-CN f(69-209) has also drawn attention to the complementary proteose peptone beta-CN f(1-68) that is presumed to play a physiological role in inducing milk secretion similar to that of beta-CN f(1-29). The higher in vivo and in vitro production rate, compared with gamma(1)-CN formation, indicates that beta-CN f(69-209) and its complementary fragment are candidate molecular markers to evaluate milk and curd freshness. We suggested [corrected] indirect ELISA analysis based on the determination of remaining nonhydrolyzed beta-CN to perform a quantitative evaluation of proteolysis.


Sujet(s)
Buffles/physiologie , Caséines/analyse , Basse température , Lait/composition chimique , Animaux , Marqueurs biologiques/analyse , Bovins , Fromage/analyse , Chromatographie en phase liquide , Électrophorèse sur gel de polyacrylamide , Manipulation des aliments , Technologie alimentaire , Spectrométrie de masse MALDI
16.
Angle Orthod ; 71(3): 170-6, 2001 Jun.
Article de Anglais | MEDLINE | ID: mdl-11407768

RÉSUMÉ

We measured the skeletal effects of Herbst appliance treatment in a retrospective sample of 25 boys (aged 10.7-14.5 years) and 25 girls (aged 10.7-14.3 years). Selection criteria were (1) a pretreatment full Class II molar relationship (ANB angle: average, 6.7 degrees; range, 2.5-10.5 degrees) and (2) a posttreatment full Class I or overcorrected Class I molar relationship within 6-8 months. A first t-test was used to evaluate variations between pre- and posttreatment cephalometric measures. Then, compared with the appropriate age- and sex-matched European norm, every pre- and posttreatment value was transformed into a z-score on the distribution of the norm value and a second t-test was performed. The second t-test was to study variations between pre- and posttreatment z-scores in order to neutralize the effect of natural growth. Posttreatment, the mandible showed a remarkable forward repositioning without opening of the gonial angle, particularly in males. Only ANB and Xi-CF-PTV angles were significantly different when the effect of normal growth was excluded. In males, ramus height and mandibular basal length were significantly increased when total variation was considered (ie, not excluding the effect of normal growth). In females, only the mandibular ramus height was significantly increased. In conclusion, even short-term Herbst therapy can be efficacious, with the most frequent effect being mandibular forward repositioning followed by mandibular ramus elongation. The statistical procedure used counteracts the effect of growth and sex on the results. Moreover, z-scores are adimensional measures with which any kind of parameter may be compared and scaled to each other in the perspective of a more reliable mutivariated interpretation of cephalometric variables.


Sujet(s)
Céphalométrie/statistiques et données numériques , Mandibule/anatomie et histologie , Appareils orthodontiques fonctionnels , Adolescent , Analyse de variance , Études cas-témoins , Enfant , Femelle , Humains , Mâle , Malocclusion de classe II/thérapie , Mandibule/croissance et développement , Maxillaire/anatomie et histologie , Valeurs de référence , Études rétrospectives , Facteurs sexuels ,
18.
J Antibiot (Tokyo) ; 51(9): 872-9, 1998 Sep.
Article de Anglais | MEDLINE | ID: mdl-9820238

RÉSUMÉ

The structure of a product, isolated during the synthesis of the semisynthetic glycopeptide MDL 63,246, was elucidated on the basis of spectroscopic methods and proved to be a novel glycopeptide containing a 3-oxazolin-5-one ring between positions 36 and 38. Subjected to acid hydrolysis this compound gave the corresponding pseudo aglycone and aglycone derivatives which maintained the original oxazolinone structure. Tested for antibacterial activity, these compounds showed a moderate activity against Gram-positive and inactive against Gram-negative bacteria.


Sujet(s)
Antibactériens/composition chimique , Antibactériens/pharmacologie , Bactéries à Gram positif/effets des médicaments et des substances chimiques , Antibactériens/synthèse chimique , Bactéries à Gram négatif/effets des médicaments et des substances chimiques , Spectroscopie par résonance magnétique , Tests de sensibilité microbienne , Structure moléculaire , Téicoplanine/analogues et dérivés , Téicoplanine/composition chimique
19.
J Antibiot (Tokyo) ; 50(8): 665-70, 1997 Aug.
Article de Anglais | MEDLINE | ID: mdl-9315079

RÉSUMÉ

A novel product, isolated from a culture broth of Actinoplanes ianthinogenes fermented for producing purpuromycin, was purified and its structure established on the basis of physico-chemical data and chemical reactions. The new product resulted to be structurally related to griseorhodins, a group of hydroquinonic antibiotics obtained from Streptomyces californicus. This compound showed a weak activity against Gram-positive and resulted inactive against Gram-negative bacteria and Candida albicans.


Sujet(s)
Antibactériens/composition chimique , Antibactériens/isolement et purification , Naphtoquinones/composition chimique , Naphtoquinones/isolement et purification , Antibactériens/pharmacologie , Fermentation , Tests de sensibilité microbienne , Structure moléculaire , Naphtoquinones/pharmacologie , Spiranes/composition chimique , Spiranes/isolement et purification , Spiranes/pharmacologie , Relation structure-activité
20.
J Med Chem ; 40(6): 967-71, 1997 Mar 14.
Article de Anglais | MEDLINE | ID: mdl-9083486

RÉSUMÉ

Purpuromycin (1) is an antibiotic with a broad spectrum of antimicrobial activity, encompassing bacteria, fungi, and protozoa, particularly those involved in vaginal infections. With the aim of enhancing the solubility and reducing the serum binding, a chemical program of modifications was undertaken on the natural compound, and a new interesting series of derivatives at the naphthoquinone system was synthesized and evaluated as potential topical agents for vaginal infections. In particular three semisynthetic derivatives, 7'-amino (8a), 7'-methylamino (8b), 7'-ethylamino (8c), of 7'-demethoxypurpuromycin seemed to be the most promising. They were tested for in vitro activity against three of the most important vaginal pathogens and showed activity similar to that of purpuromycin against Candida isolates while they were significantly more active against Trichomonas vaginalis and Gardnerella vaginalis, which are cultured in media containing blood or serum. This is probably due to the fact that the activity of the derivatives is less antagonized by these supplements than that of purpuromycin.


Sujet(s)
Antibactériens/pharmacologie , Anti-infectieux locaux/pharmacologie , Candida/effets des médicaments et des substances chimiques , Gardnerella vaginalis/effets des médicaments et des substances chimiques , Naphtoquinones/pharmacologie , Trichomonas vaginalis/effets des médicaments et des substances chimiques , Vagin/microbiologie , Animaux , Antibactériens/synthèse chimique , Antibactériens/composition chimique , Anti-infectieux locaux/synthèse chimique , Anti-infectieux locaux/composition chimique , Femelle , Humains , Tests de sensibilité microbienne , Structure moléculaire , Naphtoquinones/synthèse chimique , Naphtoquinones/composition chimique
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