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The increasing prevalence and complications related to liver diseases (caused by infection, toxic agents, or metabolic syndrome), together with insufficient existence of treatments, make evident the need for better therapeutic alternatives. Therefore, the aim of this study was to determine the effect of 4-hydroxychalcone (4-HC) as preventive and curative treatment in acute and chronic liver injury, respectively. Liver damage was induced with carbon tetrachloride (C[Cl.sub.4]) in Wistar rats. Rats were divided into two groups: (1) acute liver injury and (2) chronic liver injury. In turn, each group was divided into four subgroups: (i) control (water); (ii) dimethyl sulfoxide 10%; (iii) C[Cl.sub.4]; and (iv) 4-HC. The pre-treatment with 4-HC decreased transaminases, IL-6 serum levels, and hepatic malondialdehyde, increased IL-10 serum levels and hepatic glutathione, and decreased liver damage (necrosis, steatosis, and inflammatory infiltrate). In contrast, treatment with 4-HC after the induction of chronic liver injury decreased IL-6 serum levels and liver damage (steatosis, inflammatory infiltrate, ballooning cells, steatofibrosis, and fibrosis degree). Thus, the 4-HC treatment is proposed as a preventive treatment against acute liver injury; moreover, these results suggested the potential of 4-HC as a curative treatment against chronic liver injury, but other scheme treatments must be evaluated in future. Key words: 4-hydroxychalcone, fibrosis, steatosis, acute liver injury, chronic liver injury, preventive treatment, curative treatment L'augmentation de la prevalence des maladies hepatiques et des complications qui y sont liees (causees par l'infection, les agents toxiques ou le syndrome metabolique), de meme que de traitements existants insuffisants, mettent en evidence le besoin de meilleurs choix d'options therapeutiques. Par consequent, cette etude avait pour but d'etablir l'effet de la 4hydroxychalcone (4-HC) en tant que traitement preventif et curatif de l'insuffisance hepatique aigue et chronique, respectivement. Nous avons obtenu des dommages hepatiques a l'aide de tetrachlorure de carbone (CCl4]) chez des rats Wistar. Nous avons reparti les rats dans deux groupes : (1) insuffisance hepatique aigue et (2) insuffisance hepatique chronique. Ensuite, nous avons reparti les rats de chacun des groupes dans quatre sous-groupes : (i) temoin (eau); (ii) dimethylsulfoxyde a 10 %; (iii) CCl4; et (iv) 4-HC. L'administration prealable de 4-HC a entraine un abaissement des transaminases, des taux seriques d'IL-6 et de malondialdehyde hepatique, ainsi qu'une hausse des taux seriques d'IL-10 et de glutathion hepatique, avec une attenuation des lesions hepatiques (necrose, steatose et infiltrats inflammatoires). Par ailleurs, l'administration de 4-HC apres la production d'une insuffisance hepatique chronique a entraine un abaissement des taux seriques d'IL-6 et une attenuation des dommages hepatiques (steatose, infiltrats inflammatoires, gonflement cellulaire, steatofibrose et degre de fibrose). Par consequent, nous proposons l'administration de 4-HC comme traitement preventif contre l'insuffisance hepatique aigue. En outre, ces resultats laissent entrevoir le potentiel de l'administration de 4-HC comme traitement curatif contre l'insuffisance hepatique chronique. Cependant, d'autres schemas therapeutiques devront etre evalues dans le futur. [Traduit par la Redaction] Mots-cles : 4-hydroxychalcone, fibrose, steatose, insuffisance hepatique aigue, insuffisance hepatique chronique, Traitement preventif, traitement curatif, Introduction The liver is affected by different infection diseases (mainly hepatitis B and C), toxic agents (alcohol abuse and drugs), and metabolic syndromes (e.g., non-alcoholic steatohepatitis, NASH) (Crespo Yanguas et [...]

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.Key words: high sucrose, metabolic syndrome, NAFLD, NASH, rat model.La consommation elevee de boissons sucrees est associee a l'obesite et a la resistance a l'insuline. Ces pathologies sont directement liees a la presentation d'une surcharge en graisse du foie non alcoolique (ou NAFLD pour << nonalcoholic fatty liver disease >>), etat considere comme faisant partie du syndrome metabolique (SM). Comme la prevalence de ces etats est en croissance a l'echelle mondiale, des modeles experimentaux animaux ont ete mis au point en vue d'en mieux comprendre la physiopathologie; malgre tout, peu d'etudes ont porte sur son evolution en association avec le SM et l'ingestion de boissons sucrees. Par consequent, cette etude avait pour but de comprendre les caracteristiques physiopathologiques de la NAFLD en lien avec la concentration de saccharose et la duree de l'ingestion chez le rat. Nous avons reparti des rats Wistar dans 2 groupes avec un acces libre a l'eau du robinet ou a de l'eau contenant du saccharose a 30%, et nous les avons euthanasies apres 12,16 ou 20 semaines; les rats de 2 autres groupes avaient acces a du saccharose a 40 ou a 50% et etaient euthanasies apres 20 semaines. Nous avons mesure des parametres biochimiques et des taux de cytokines seriques, ainsi que procede a une evaluation de l'histologie. L'ingestion de saccharose a 30% engendrait une steatose hepatique a 16 semaines (grade 2) et a 20 semaines (grade 3). Entre-temps, sur 20 semaines, le saccharose a 40% entrainait une steatohepatite non alcoolique (ou NASH pour << nonalcoholic steatohepatitis >>) de grade 5, et le saccharose a 50% entrainait une NASH de grade 6 avec de la fibrose. Cette etude montrait que le grade de la NAFLD augmentait en fonction de la duree de l'induction et de la teneur en saccharose de la boisson ingeree. [Traduit par la Redaction]Mots-cles : teneur elevee en saccharose, syndrome metabolique, NAFLD, NASH, modele chez le rat., IntroductionThe development of obesity and diabetes mellitus has been associated with high consumption of sugary drinks (ENSANUT-MC 2017; Pandit et al. 2012; WHO 2016). Indeed, there is a direct relationship [...]

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. [ABSTRACT FROM AUTHOR]

Abstract: The fruit of Vitex mollis Kunth contains water‐soluble melanin (SM), whose properties have been poorly described. This study determined physicochemical characteristics, the inhibition of carbohydrate digestive enzymes (amylase and α‐glucosidase), and antioxidant activity (ABTS, DPPH, ORAC, and β‐carotene bleaching) of SM (partially purified, aqueous extraction), water‐insoluble melanin (IM) (pure, alkali‐acid extraction), and organic (i.e., methanol, ethanol, and methanol : water 8:2 vol/vol) and aqueous extracts of V. mollis fruit. SM and IM were characterized by UV and IR spectroscopy, and their spectra showed signals characteristic of melanins. They also showed similar antioxidant (1,321–2,664 μmol TE/g), and α‐glucosidase inhibitory (IC50 1.48–0.022 mg/mL) activities, values that were better than those of the organic extracts (ABTS < 746 µmol TE/g and IC50 > 4.87 mg/mL, respectively). In addition, SMs showed higher extraction yields than IMs. Therefore, SM shares nutraceutical properties with IM and can be obtained by simple and environmentally friendly methods. Practical applications: Melanins show biological activities (e.g., antioxidant, immunostimulatory, UV‐, and radiation‐protective) and their consumption has been associated with health benefits. However, studies of plant melanins are scarce because their extraction involves harsh pH conditions and the yields are usually low. The results showed that melanin was the main pigment in Vitex mollis fruit and water‐soluble. Moreover, the extraction method was simple, ecological, and produced high yields. Both water‐soluble and water‐insoluble melanins showed similar biological activities (antioxidant and α glucosidase inhibition). Species of Vitex are commonly employed as food and in folk medicine (e.g., premenstrual and gynecological disorders, gastrointestinal problems and inflammation, bacterial infections). Soluble melanins of V. mollis could be used as food supplement or in pharmaceutical preparations. [ABSTRACT FROM AUTHOR]

Echeveria species (Crassulaceae) are used in traditional medicine and some of their biological activities are demonstrated (e.g. antimicrobial, anti-inflammatory, anticancer). However, their chemical composition has been scarcely studied. The methanol extracts (ME) of three Echeveria species (E. craigiana, E. kimnachii and E. subrigida) from Mexico were analyzed for the sterol (GC-MS) and phenolic (HPLC-DAD-ESI-MSn ) composition. Eleven sterols were identified, E. kimnachii showed the highest total content (7.87 mg/g ME), and the main constituents were γ-sitosterol in E. craigiana (33.9%) and E. subrigida (54.4%), and lupenone in E. kimnachii (28.9%). The phenolic analysis showed differences among the Echeveria species, which contained flavonoids derivatives and tannins as the main components. The main flavonoids in E. craigiana were hexoside derivatives of quercetin and isorhamnetin, both with a 3-hydroxy-3-methylglutaroyl substituent; in E. subrigida hexosides of isorhamnetin, quercetin and kaempferol; and E. kimnachii showed the greatest diversity including proanthocyanidins and less common flavonoid derivatives of kaempferol O,O-disubstituted by acyl derivatives. The characteristic phytochemicals of each studied Echeveria species could be responsible of its specific biological activities and useful as chemotaxonomic markers. The kaempferol derivatives in E. kimnachii are rare in nature and they will be isolated and characterized. [ABSTRACT FROM AUTHOR]

Introduction. Pithecellobium dulce is a legume native to tropical America that produces edible arils which can be white or red. The plant is also grown in Asia and, to date, predominantly fruits produced in Asia have been the subject of scientific studies. We studied white and red arils produced in America. Materials and methods. White aril and red aril fruits were evaluated in an array of reagent-based assays to determine nutritional and nutraceutical properties. Results and discussion. White arils and red arils showed similar physicochemical characteristics, with high content of vitamin C (79.7–82.6 mg·100 g–1 fresh weight) and dietary fiber (5.83–6.12% fw). The anthocyanin content of red arils (29.5 mg·100 g–1 fw, as cyanidin-3-glucoside equivalents) was similar to that of strawberry. Total phenolics (517 mg·100 g–1 fw, as gallic acid equivalents) and antioxidant activities (ABTS, 224 mg; DPPH, 223 mg, as vitamin C equivalents) of red arils were 1.3 times higher than those in white arils. The methanolic extract of red arils showed a higher α-glucosidase inhibition (IC50 2.9 mg·mL–1) than acarbose (IC50 4.9 mg·mL–1). The methanolic extract [(50, 100 and 500) μg per tube] of red and white arils showed positive-strong antimutagenic activities (inhibition in the range 25–70%) in the assay (Salmonella typhimurium YG1024 strain, 1-nitropyrene as mutagen, 200 ng per tube). We are reporting for the first time remarkably high characteristics (i.e., antioxidant, inhibition of α-amylase and α-glucosidase and content of dietary fiber) of P. dulce fruits, mainly of the red ones; properties which combined permit us to suggest that consumption of these fruits could have beneficial health effects in people with diabetes. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

This study reports the in silico design of 30 6 H -1,2-oxazin-6-ones against DHFR and PTC antimicrobial targets. Docking compounds 1, 3, 4, 6, and 8 with both enzymes was favorable, outperforming Trimethoprim with DHFR. Therefore, 12 6 H -1,2-oxazin-6-ones, including the most promising compounds, were synthesized through an aminolysis reaction of β-cyanoketones with hydroxylamine hydrochloride, obtaining moderate to high yields (55-88%). Subsequently, antibacterial studies were conducted against five bacteria: four Gram-positive MRSA (ATCC 43300 and three clinical isolates) and one Gram-negative ( E. coli ATCC 25922). Compounds 1, 2, 3, 4, 6, and 8 inhibited bacterial growth with MIC values ranging from 3.125 to 200 μg mL -1 . Compound 1 showed better activity against Gram-positive bacteria than Linezolid. Toxicity assays indicated no adverse effects of the active oxazinones in silico and in vitro . This study demonstrated the antibacterial potential of the selected 6 H -1,2-oxazin-6-ones against resistant human pathogenic bacteria., Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (This journal is © The Royal Society of Chemistry.)