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1.
Food Chem ; 369: 130875, 2022 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-34438342

RESUMO

Cardoon seeds collected in Greece at four different maturity stages (samples S1 to S4) were analysed in terms of chemical composition and in vitro bioactivities. The content of phenolic compounds (six compounds in total) increased with increasing maturity, and 3,5-O-dicaffeyolquinic (14.8-33.8 mg/g extract) acid was the compound detected in higher abundance. Mature seeds (sample S4) also revealed the highest content in lipids (23 g/100 g extract) and tocopherols (29.62 mg/100 g dw) and demonstrated the highest cytotoxic (GI50 of 97-216 µg/mL) and anti-inflammatory (IC50 = 148 µg/mL) activities, and capacity to inhibit the formation of thiobarbituric acid reactive substances (TBARS) (IC50 = 5 µg/mL). Cardoon seed hydroethanolic extracts also revealed high antibacterial and antifungal potential, particularly samples S3 and S1, respectively. This study proved the multifaceted potential associated with valorisation of cardoon seeds, while their biological and chemical composition can be influenced by the maturity stage.


Assuntos
Cynara , Anti-Inflamatórios , Fenóis/análise , Extratos Vegetais/farmacologia , Sementes/química
2.
Antioxidants (Basel) ; 10(10)2021 Oct 02.
Artigo em Inglês | MEDLINE | ID: mdl-34679706

RESUMO

The impact of two extraction solvents on the phenolic composition, antioxidant, and enzymes inhibitory and antimicrobial activities of two parts (leaves and stem bark) of P. kotschyi was studied. Two different LC-DAD-MSn approaches were used to identify and quantify the bioactive compounds in the different extracts. A total of thirty-two compounds were quantified, being the procyanidin the most abundant in stem bark while catechin and flavonoids are most abundant in leaves. Overall, the stem bark extraction using methanol showed higher amounts of total phenolic (131.83 ± 1.81 mg GAE/g) and flavanol (14.14 ± 0.11 mg CE/g) while the leaves extraction using water exhibited stronger levels of total flavonoid (44.95 ± 0.38 mg RE/g) and phenolic acid (63.58 ± 2.00 mg CAE/g). As regards the antioxidant assays, methanol stem bark extracts were characterized by the highest antioxidant activities (DPPH: 1.94 ± 0.01 mmol TE/g, ABTS: 3.31 ± 0.01 mmol TE/g, FRAP: 2.86 ± 0.02 mmol TE/g, CUPRAC: 5.09 ± 0.08 mmol TE/g, phosphomolybdenum: 5.16 ± 0.23 mmol TE/g and metal chelating: 17.12 ± 0.46 mg EDTAE/g). In addition, the methanolic extracts of stem bark had highest impact on acetylcholinesterase (2.54 mg GALAE/g), butyrylcholinesterase (5.48 mg GALAE/g). In contrast, the methanolic extracts of leaves was potent against tyrosinase (77.39 ± 0.21 mg KAE/g) and α-glucosidase (0.97 ± 0.01 mmol ACAE/g), while a higher anti-α-amylase (0.97 ± 0.01 mmol ACAE/g) was observed for water extracts of the same part. All of the tested extracts showed inhibitory effects on elastase, except methanolic leaves extracts. Additionally, the extracts exhibited appreciable antifungal toward A. ochraceus, A. fumigatus, P. ochrochloron, T. viride, and P. funiculosum and promising antibacterial activity against M. flavus, S. aureus, L. monocytogenes, E. coli, P. aeruginosa, E. cloacae, and S. typhimurium. Taken together, the outcomes demonstrated P. kotschyi as a novel source of bioactive molecules of interest with an evident therapeutic value.

3.
Biology (Basel) ; 10(10)2021 Sep 23.
Artigo em Inglês | MEDLINE | ID: mdl-34681050

RESUMO

Aloesin is an aromatic chromone with increasing applications in the cosmetic and health food industries. To optimize its extraction from the Aloe vera leaf rind, the independent variables time (10-210 min), temperature (25-95 °C) and organic solvent composition (0-100%, w/w) were combined in a central composite design coupled with response surface methodology. The solvents consisted of binary mixtures of water with ethanol, propylene glycol, or glycerol. The aloesin levels quantified in each extract were used as response for optimization. The theoretical models were fitted to the experimental data, statistically validated, and used to obtain the optimal extraction conditions. Then, a dose-response analysis of the solid/liquid ratio (S/L) was performed under the optimal conditions determined for each alcohol-water system and revealed that a linear improvement in extraction efficiency can be achieved by increasing the S/L ratio by up to 40 g/L. This analysis also allowed to experimentally validate the predictive models. Furthermore, the aloesin-rich extracts revealed antioxidant activity through thiobarbituric acid reactive substances (TBARS) formation inhibition, antimicrobial effects against bacterial and fungal strains, and no toxicity for PLP2 cells. Overall, this study provided optimal extraction conditions for the recovery of aloesin from Aloe vera rind through an eco-friendly extraction process and highlighted its bioactive potential.

4.
Pharmaceuticals (Basel) ; 14(9)2021 Sep 20.
Artigo em Inglês | MEDLINE | ID: mdl-34577641

RESUMO

Chicory (Cichorium intybus L.) is an important industrial crop cultivated mainly to extract the dietary fiber inulin. However, chicory also contains bioactive compounds such as sesquiterpene lactones and certain polyphenols, which are currently discarded as waste. Plants are an important source of active pharmaceutical ingredients, including novel antimicrobials that are urgently needed due to the global spread of drug-resistant bacteria and fungi. Here, we tested different extracts of chicory for a range of bioactivities, including antimicrobial, antifungal and cytotoxicity assays. Antibacterial and antifungal activities were generally more potent in ethyl acetate extracts compared to water extracts, whereas supercritical fluid extracts showed the broadest range of bioactivities in our assays. Remarkably, the chicory supercritical fluid extract and a purified fraction thereof inhibited both methicillin-resistant Staphylococcus aureus (MRSA) and ampicillin-resistant Pseudomonas aeruginosa IBRS P001. Chicory extracts also showed higher antibiofilm activity against the yeast Candida albicans than standard sesquiterpene lactone compounds. The cytotoxicity of the extracts was generally low. Our results may thus lead to the development of novel antibacterial and antifungal preparations that are both effective and safe for human use.

5.
Artigo em Inglês | MEDLINE | ID: mdl-34501651

RESUMO

Flowers of the genus Impatiens are classified as edible; however, their inclusion in the human diet is not yet a common practice. Its attractive colours have stirred great interest by the food industry. In this sense, rose (BP) and orange (BO) I. balsamina flowers were nutritionally studied, followed by an in-depth chemical study profile. The non-anthocyanin and anthocyanin profiles of extracts of both flower varieties were also determined by high-performance liquid chromatography coupled to a diode array and mass spectrometry detector (HPLC-DAD-ESI/MS). The results demonstrated that both varieties presented significant amounts of phenolic compounds, having identified nine non-anthocyanin compounds and 14 anthocyanin compounds. BP extract stood out in its bioactive properties (antioxidant and antimicrobial potential) and was selected for incorporation in "bombocas" filling. Its performance as a colouring ingredient was compared with the control formulations (white filling) and with E163 (anthocyanins) colorant. The incorporation of the natural ingredient did not cause changes in the chemical and nutritional composition of the product; and although the colour conferred was lighter than presented by the formulation with E163 (suggesting a more natural aspect), the higher antioxidant activity could meet the expectations of the current high-demand consumer.


Assuntos
Antocianinas , Corantes de Alimentos/análise , Impatiens , Extratos Vegetais/análise , Antocianinas/análise , Antioxidantes , Cromatografia Líquida de Alta Pressão , Flores
6.
Antibiotics (Basel) ; 10(7)2021 Jul 02.
Artigo em Inglês | MEDLINE | ID: mdl-34356726

RESUMO

The goal of this research is to investigate the antimicrobial activity of nineteen previously synthesized 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole derivatives. The compounds were tested against a panel of three Gram-positive and three Gram-negative bacteria, three resistant strains, and six fungi. Minimal inhibitory, bactericidal, and fungicidal concentrations were determined by a microdilution method. All of the compounds showed antibacterial activity that was more potent than both reference drugs, ampicillin and streptomycin, against all bacteria tested. Similarly, they were also more active against resistant bacterial strains. The antifungal activity of the compounds was up to 80-fold higher than ketoconazole and from 3 to 40 times higher than bifonazole, both of which were used as reference drugs. The most active compounds (2, 3, 6, 7, and 19) were tested for their inhibition of P. aeruginosa biofilm formation. Among them, compound 3 showed significantly higher antibiofilm activity and appeared to be equipotent with ampicillin. The prediction of the probable mechanism by docking on antibacterial targets revealed that E. coli MurB is the most suitable enzyme, while docking studies on antifungal targets indicated a probable involvement of CYP51 in the mechanism of antifungal activity. Finally, the toxicity testing in human cells confirmed their low toxicity both in cancerous cell line MCF7 and non-cancerous cell line HK-2.

7.
Artigo em Inglês | MEDLINE | ID: mdl-34335850

RESUMO

Artemisia absinthium L. (Asteraceae) is traditionally used for gastrointestinal ailments and disorders linked to numerous risk factors including microbial infections. We aimed to provide contemporary evidence for its ethnopharmacological use and determine its antimicrobial capacity and mode of action, cytotoxicity, and phenolic constituents. Ethnopharmacological survey was conducted using semistructured interviews. Antimicrobial and antibiofilm capacities were determined by microdilution/crystal violet assay, respectively. Modes of action tested include estimation of exopolysaccharide production (congo red binding assay) and interference with membrane integrity (crystal violet uptake and nucleotide leakage assay). Cytotoxicity was determined using crystal violet assay. Polyphenolic profiling was done by advanced liquid chromatography/mass spectrometry (UHPLC-LTQ OrbiTrap MS). Artemisia absinthium in Serbia is traditionally used for gastrointestinal disorders, among others. Further study revealed high antifungal capacity of herb ethanolic extract towards range of Candida species (MIC 0.5-1 mg/mL) along with promising antibacterial activities (MIC 0.25-4 mg/mL). Interference with membrane integrity could be observed as a possible antimicrobial mechanism. Antibiofilm potential can be considered as high (towards C. krusei) to limited (towards P. aeruginosa) and moderate based on reduction in exopolysaccharide content. In concentrations up to 400 µg/mL, no cytotoxicity was observed towards HaCaT and HGF-1 cell lines. Polyphenolic analysis revealed twenty-one different constituents. A. absinthium usage as a gastrointestinal ailment remedy has been confirmed in vitro by its antimicrobial capacity towards microorganisms whose presence is linked to the diseases and associated complications and noncytotoxic nature of the natural product. The observed activities could be attributed to the present phenolic compounds.

8.
Molecules ; 26(14)2021 Jul 16.
Artigo em Inglês | MEDLINE | ID: mdl-34299579

RESUMO

Herein we report the synthesis of some new 1H-1,2,4-triazole functionalized chromenols (3a-3n) via tandem reactions of 1-(alkyl/aryl)-2-(1H-1,2,4-triazole-1-yl) with salicylic aldehydes and the evaluation of their antifungal activity. In silico prediction of biological activity with computer program PASS indicate that the compounds have a high novelty compared to the known antifungal agents. We did not find any close analog among the over 580,000 pharmaceutical agents in the Cortellis Drug Discovery Intelligence database at the similarity cutoff of 70%. The evaluation of antifungal activity in vitro revealed that the highest activity was exhibited by compound 3k, followed by 3n. Their MIC values for different fungi were 22.1-184.2 and 71.3-199.8 µM, respectively. Twelve from fourteen tested compounds were more active than the reference drugs ketoconazole and bifonazole. The most sensitive fungus appeared to be Trichoderma viride, while Aspergillus fumigatus was the most resistant one. It was found that the presence of the 2-(tert-butyl)-2H-chromen-2-ol substituent on the 4th position of the triazole ring is very beneficial for antifungal activity. Molecular docking studies on C. albicans sterol 14α-demethylase (CYP51) and DNA topoisomerase IV were used to predict the mechanism of antifungal activities. According to the docking results, the inhibition of CYP51 is a putative mechanism of antifungal activity of the novel chromenol derivatives. We also showed that most active compounds have a low cytotoxicity, which allows us to consider them promising antifungal agents for the subsequent testing activity in in vivo assays.


Assuntos
Antifúngicos , Cromonas , Hypocreales/crescimento & desenvolvimento , Fungos Mitospóricos/crescimento & desenvolvimento , Simulação de Acoplamento Molecular , Antifúngicos/síntese química , Antifúngicos/química , Antifúngicos/farmacologia , Cromonas/síntese química , Cromonas/química , Cromonas/farmacologia , Avaliação Pré-Clínica de Medicamentos
9.
Molecules ; 26(13)2021 Jul 02.
Artigo em Inglês | MEDLINE | ID: mdl-34279400

RESUMO

BACKGROUND: Infectious diseases still affect large populations causing significant morbidity and mortality. Bacterial and fungal infections for centuries were the main factors of death and disability of millions of humans. Despite the progress in the control of infectious diseases, the appearance of resistance of microbes to existing drugs creates the need for the development of new effective antimicrobial agents. In an attempt to improve the antibacterial activity of previously synthesized compounds modifications to their structures were performed. METHODS: Nineteen thiazolidinone derivatives with 6-Cl, 4-OMe, 6-CN, 6-adamantan, 4-Me, 6-adamantan substituents at benzothiazole ring were synthesized and evaluated against panel of four bacterial strains S. aureus, L. monocytogenes, E. coli and S. typhimirium and three resistant strains MRSA, E. coli and P. aeruginosa in order to improve activity of previously evaluated 6-OCF3-benzothiazole-based thiazolidinones. The evaluation of minimum inhibitory and minimum bactericidal concentration was determined by microdilution method. As reference compounds ampicillin and streptomycin were used. RESULTS: All compounds showed antibacterial activity with MIC in range of 0.12-0.75 mg/mL and MBC at 0.25->1.00 mg/mL The most active compound among all tested appeared to be compound 18, with MIC at 0.10 mg/mL and MBC at 0.12 mg/mL against P. aeruginosa. as well as against resistant strain P. aeruginosa with MIC at 0.06 mg/mL and MBC at 0.12 mg/mL almost equipotent with streptomycin and better than ampicillin. Docking studies predicted that the inhibition of LD-carboxypeptidase is probably the possible mechanism of antibacterial activity of tested compounds. CONCLUSION: The best improvement of antibacterial activity after modifications was achieved by replacement of 6-OCF3 substituent in benzothiazole moiety by 6-Cl against S. aureus, MRSA and resistant strain of E. coli by 2.5 folds, while against L. monocytogenes and S. typhimirium from 4 to 5 folds.


Assuntos
Anti-Infecciosos/síntese química , Inibidores de Proteases/síntese química , Tiazolidinas/síntese química , Anti-Infecciosos/farmacologia , Proteínas de Bactérias/antagonistas & inibidores , Proteínas de Bactérias/química , Proteínas de Bactérias/metabolismo , Carboxipeptidases/antagonistas & inibidores , Carboxipeptidases/química , Carboxipeptidases/metabolismo , Listeria monocytogenes/efeitos dos fármacos , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Simulação de Acoplamento Molecular , Inibidores de Proteases/farmacologia , Salmonella typhimurium/efeitos dos fármacos , Tiazolidinas/farmacologia
10.
Plants (Basel) ; 10(6)2021 Jun 10.
Artigo em Inglês | MEDLINE | ID: mdl-34200649

RESUMO

Given the importance of colour in the general acceptance or rejection of a product, the use of colorants is a widespread practice, particularly in the food industry. At the same time, with the increasing consumers' awareness of the health effects that some artificial colorants can exert, there is a growing tendency to prioritize foodstuffs containing natural additives. In this work, Morus nigra L. and Rubus fruticosus L. fruit juices were characterized in terms of anthocyanins, organic acids, free sugars, and tocopherols, as also regarding their bioactive properties. Given their richness in anthocyanins, this study also aimed to prepare different solid colouring formulations by the spray-drying technique, using as stabilizers maltodextrin and arabic gum. Six free sugars and two organic acids were detected in the fruit juices, as well as the four tocopherol isoforms. Two cyanidin derivatives were found in M. nigra (cyanidin-3-O-glucoside and cyanidin-O-rhamnoside) and other four in R. fruticosus (cyanidin-O-hexoside, cyanidin-3-O-glucoside, cyanidin-O-pentoside, and cyanidin-3-O-dioxaloilglucoside). The developed colouring formulations revealed a good stability over time, in terms of anthocyanin concentration and colour parameters, and revealed to be safe for consumption, either concerning their low microbial load and lack of cytotoxicity. Thus, they represent a promising natural alternative to the massively used artificial colorants.

11.
Chem Biodivers ; 18(8): e2100299, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34086421

RESUMO

The article reports the chemical composition, antioxidant, six key enzymes inhibitory and antimicrobial activities of two solvent extracts (water and methanol) of leaves and stem bark of Uapaca togoensis. For chemical composition, methanol extract of stem bark exhibited significant higher total phenolic (129.86 mg GAE/g) and flavanol (10.44 mg CE/g) contents. Methanol extract of leaves and water extract of stem bark showed high flavonoids (20.94 mg RE/g) and phenolic acid (90.40 mg CAE/g) content, respectively. In addition, HPLC-ESI-TOF-MS analysis revealed that U. togoensis was rich in procyanidins. The methanol and water extracts of stem bark had overall superior antioxidant activity; however, only methanol extract of stem bark showed higher inhibition of cholinesterase (AChE: 2.57 mg GALAE/g; BChE: 4.69 mg GALAE/g), tyrosinase (69.53 mg KAE/g) and elastase (2.73 mmol CE/g). Potent metal chelating ability was showed by water extract of leaves (18.94 mg EDTAE/g), higher inhibition of amylase was detected for water extracts of leaves (0.94 mmol ACAE/g) and stem bark (0.92 mmol ACAE/g). The tested extracts have shown wide-spectrum antibacterial properties and these effects have shown to be more effective against Aspergillus ochraceus, Penicillium funiculosum, Trichoderma viride, Bacillus cereus, Escherichia coli and Pseudomonas aeruginosa. The results revealed that the antioxidant, enzyme inhibitory and antimicrobial activities depended on the extraction solvents and the parts of plant. Bioinformatics analysis on the 17 major compounds showed modulation of pathway associated with cancer. In brief, U. togoensis might be valuable as potential source of natural agents for therapeutic application.


Assuntos
Biflavonoides/química , Catequina/química , Biologia Computacional/métodos , Inibidores Enzimáticos/química , Magnoliopsida/química , Extratos Vegetais/química , Proantocianidinas/química , Amilases/antagonistas & inibidores , Amilases/metabolismo , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Antioxidantes/química , Biflavonoides/isolamento & purificação , Biflavonoides/metabolismo , Biflavonoides/farmacologia , Catequina/isolamento & purificação , Catequina/metabolismo , Catequina/farmacologia , Cromatografia Líquida de Alta Pressão , Análise por Conglomerados , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/metabolismo , Inibidores Enzimáticos/farmacologia , Fungos/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Magnoliopsida/metabolismo , Testes de Sensibilidade Microbiana , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Casca de Planta/química , Casca de Planta/metabolismo , Folhas de Planta/química , Folhas de Planta/metabolismo , Proantocianidinas/isolamento & purificação , Proantocianidinas/metabolismo , Proantocianidinas/farmacologia , Espectrometria de Massas por Ionização por Electrospray
12.
J Pharm Biomed Anal ; 203: 114184, 2021 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-34107441

RESUMO

The methanolic and water extracts of Carapa procera leaves and stem barks were screened for their phytochemical content using a multi-technique approach. The extracts were also assessed for their in vitro antioxidant capacity along with their anti-diabetic (α-amylase, α-glucosidase), anti-tyrosinase, anti-elastase and anti-cholinesterase (AChE, BChE) activities. Furthermore, antibacterial and antifungal effects were determined against several bacterial and fungal strains. Data Integration Analysis for Biomarker discovery using Latent components (DIABLO) integrative analysis was conducted on collected data to determine the influence of extraction solvents and plant parts on phytochemical content, antioxidant properties and enzyme inhibitory properties of C. procera samples. Additionally, the major identified compounds were screened as modulators of multiple pathways involved in human diseases via Gene Ontology (GO) enrichment analysis. Results showed that methanolic stem bark extract exhibited the most potent ABTS scavenging, Cu2+ and Fe3+ reducing power, total antioxidant capacity and Fe2+ chelating power and displayed the highest total flavanol content. Methanolic extracts of leaves and stem barks were abounded with phenolics and had the greatest anti-AChE, anti-BChE, anti-tyrosinase and anti-elastase activities. A significant antifungal activity was observed, with the lowest minimum inhibitory concentration and minimum fungicidal values of 0.07 and 0.15 mg/mL, respectively. DIABLO integrative analysis suggested that the phytochemical content and biological activities varied significantly within the plant parts and were influenced by types of solvent used. GO enrichment analysis on the main bioactive compounds showed modulation of multiple pathways associated with cancer. Obtained results demonstrated that stem bark and leaves of C. procera can be considered as promising sources of bioactive molecules with high pharmacological values.


Assuntos
Meliaceae , Extratos Vegetais , Antioxidantes/farmacologia , Cromatografia Líquida , Porcelana Dentária , Humanos , Ligas Metalo-Cerâmicas , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Espectrometria de Massas em Tandem , Titânio
13.
Food Funct ; 12(15): 6780-6792, 2021 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-34109332

RESUMO

Lentinus crinitus (L.) Fr. (Basidiomycota: Polyporales) is a wild mushroom with several biotechnological applications; however, there are few studies on its chemical composition and antimicrobial activity. Therefore, this study aims to evaluate the chemical composition, cytotoxicity, and antimicrobial activity of L. crinitus basidiocarp. For that, its nutritional value (AOAC procedures) and its composition in some hydrophilic and lipophilic compounds (chromatographic techniques) were assessed. Moreover, the potential hepatotoxic effects were evaluated using a primary cell culture obtained from porcine liver, and its growth inhibitory capacity was also evaluated against four human tumour cell lines (spectrophotometric assays). The antimicrobial activity was evaluated by microdilution against eight bacteria and fungi. The basidiocarp has a high content of carbohydrates and, therefore, a relatively high energetic value. It is also rich in soluble sugars, ß-tocopherol, phenolic acids, mainly p-hydroxybenzoic acid, and organic acids, mainly malic acid. L. crinitus did not show cytotoxicity in non-tumour cells, but it did not inhibit the growth of human tumour cell lines either. The basidiocarp has a wide antimicrobial activity, inhibiting the growth of different species of bacteria and fungi. It showed minimum bactericidal and fungicidal concentration values similar to or lower than those verified by commercial antibiotics or food additives used as preservatives. The antimicrobial activity was more evident against Listeria monocytogenes, Salmonella enterica, and Penicillium ochrochloron, followed by Aspergillus ochraceus and Trichoderma viride, when compared to the controls. The results obtained in this study showed that L. crinitus basidiocarp has great potential to be used by the industry without toxicity risks.

14.
Foods ; 10(3)2021 Mar 22.
Artigo em Inglês | MEDLINE | ID: mdl-33810113

RESUMO

In the present work, sage (Salvia officinalis L.) and basil (Ocimum basilicum L.) were exploited for their preservative purposes, as viable alternatives to artificial ones. The ultrasound-assisted extraction (UAE) of bioactive compounds was pre-optimized using factorial screening analysis, prior to applying response surface methodology (RSM). The obtained extracts were characterized in terms of phenolic compounds by high-performance liquid chromatography coupled to photodiode array detector and mass spectrometer HPLC-DAD-ESI/MS and bioactivities, namely the antioxidant, antimicrobial and cytotoxic potential. In addition, the most promising extracts were incorporated into yogurts, that were further screened for nutritional and physico-chemical properties and microbial load, over a shelf life of 14 days. According to the obtained results, the solvent percentage is the most relevant factor for obtaining rosmarinic acid-rich extract, followed by the extraction time and ultrasonic power. For the antioxidant and antimicrobial activity, sage showed the best result for both analysis and none of the two plant extracts were hepatotoxic. Finally, both extracts did not show changes in the physicochemical and nutritional characteristics of the yogurts and did not interfere with the growth of lactic acid bacteria, an important microorganism during yogurt fermentation. These results highlight the high potential of sage and basil as natural preservatives.

15.
Foods ; 10(4)2021 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-33806049

RESUMO

Fruit bio-residues can be interesting for the recovery of bioactive molecules, such as phenolic compounds, tocopherols, vitamins, among others. These compounds can be targeted at the food industry and used for the development of functional foods or as food additives. In some cases, fruit epicarps are converted into by-products with non-commercial value, and generally, these fruit parts have a higher content in bioactive compounds than the fruit pulp. From this perspective, S. odorifera, a Brazilian fruit, has an inedible epicarp that could be explored to obtain biological compounds. Therefore, the aims of this study were to evaluate the chemical composition and the antioxidant, anti-proliferative, anti-inflammatory, and antimicrobial bioactivities of this by-product. S. odorifera epicarp showed a total of four organic acids, four phenolic compounds, highlighting the high concentration of anthocyanins (24 ± 1 mg/g dry weight (dw)) and high content of tocopherols (366 ± 2 mg/100 g dw). The hydroethanolic extract showed considerable antioxidant activity (EC50 values of 48.2 ± 0.5 and 27 ± 1 µg/mL for TBARS and OxHLIA assays, respectively), as also antibacterial and antifungal activities (minimal inhibitory concentrations (MICs) ≤ 2.2 mg/mL). The results obtained in this study suggest that Sicana odorifera epicarp represents a reliable option for the development of novel natural-based colorants with functional/bioactive proprieties.

16.
Molecules ; 26(5)2021 Mar 03.
Artigo em Inglês | MEDLINE | ID: mdl-33802535

RESUMO

The attractive colour characteristics of the flowers of the species Impatiens walleriana have been arousing great interest in the food industry, which is looking for potential natural sources of colouring ingredients. In this sense, the present work focused on the chemical and bioactive characterization of pink and orange flowers of I. walleriana. The phenolic compounds were determined by HPLC-DAD-ESI/MS; in addition, different bioactivities (antioxidant, antimicrobial, anti-inflammatory and cytotoxicity) were also analysed. Both samples studied showed significant amounts of phenolic compounds, especially phenolic acids, flavonoids, and anthocyanins, which justifies the excellent performance in the different bioactivities studied. The orange variety, despite having a greater variety of phenolic compounds, showed a total amount of compounds lower than the pink variety. Overall, the flowers of I. walleriana emerge as a promising resource to be explored by the food industry.


Assuntos
Antocianinas/análise , Flavonoides/análise , Flores/química , Hidroxibenzoatos/análise , Impatiens/química , Extratos Vegetais/farmacologia , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Proliferação de Células , Flores/metabolismo , Impatiens/metabolismo , Células Tumorais Cultivadas
17.
Pharmaceuticals (Basel) ; 14(5)2021 Apr 28.
Artigo em Inglês | MEDLINE | ID: mdl-33925239

RESUMO

Two Balkan Peninsula endemics, Nepeta rtanjensis and N. argolica subsp. argolica, both characterized by specialized metabolite profiles predominated by iridoids and phenolics, are differentiated according to the stereochemistry of major iridoid aglycone nepetalactone (NL). For the first time, the present study provides a comparative analysis of antimicrobial and immunomodulating activities of the two Nepeta species and their major iridoids isolated from natural sources-cis,trans-NL, trans,cis-NL, and 1,5,9-epideoxyloganic acid (1,5,9-eDLA), as well as of phenolic acid rosmarinic acid (RA). Methanol extracts and pure iridoids displayed excellent antimicrobial activity against eight strains of bacteria and seven strains of fungi. They were especially potent against food-borne pathogens such as L. monocytogenes, E. coli, S. aureus, Penicillium sp., and Aspergillus sp. Targeted iridoids were efficient agents in preventing biofilm formation of resistant P. aeruginosa strain, and they displayed additive antimicrobial interaction. Iridoids are, to a great extent, responsible for the prominent antimicrobial activities of the two Nepeta species, although are probably minor contributors to the moderate immunomodulatory effects. The analyzed iridoids and RA, individually or in mixtures, have the potential to be used in the pharmaceutical industry as potent antimicrobials, and in the food industry to increase the shelf life and safety of food products.

18.
Antibiotics (Basel) ; 10(3)2021 Mar 17.
Artigo em Inglês | MEDLINE | ID: mdl-33802949

RESUMO

In this study, we report the design, synthesis, computational and experimental evaluation of the antimicrobial activity, as well as docking studies of new 5-methylthiazole based thiazolidinones. All compounds demonstrated antibacterial efficacy, some of which (1, 4, 10 and 13) exhibited good activity against E. coli and B. cereus. The evaluation of antibacterial activity against three resistant strains, MRSA, P. aeruginosa and E. coli, revealed that compound 12 showed the best activity, higher than reference drugs ampicillin and streptomycin, which were inactive or exhibited only bacteriostatic activity against MRSA, respectively. Ten out of fifteen compounds demonstrated higher potency than reference drugs against a resistant strain of E. coli, which appeared to be the most sensitive species to our compounds. Compounds 8, 13 and 14 applied in a concentration equal to MIC reduced P. aeruginosa biofilm formation by more than 50%. All compounds displayed antifungal activity, with compound 10 being the most active. The majority of compounds showed better activity than ketoconazole against almost all fungal strains. In order to elucidate the mechanism of antibacterial and antifungal activities, molecular docking studies on E. coli Mur B and C. albicans CYP51 and dihydrofolate reductase were performed. Docking analysis of E. coli MurB indicated a probable involvement of MurB inhibition in the antibacterial mechanism of tested compounds while docking to 14α-lanosterol demethylase (CYP51) and tetrahydrofolate reductase of Candida albicans suggested that probable involvement of inhibition of CYP51 reductase in the antifungal activity of the compounds. Potential toxicity toward human cells is also reported.

19.
Food Chem ; 351: 129263, 2021 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-33631614

RESUMO

Nowadays, the use of carob (Ceratonia siliqua L.) is reduced to its seeds. In fact, the food additive E410, locust bean gum, is obtained from its endosperm. However, the available information regarding the bioactive potential of carob seeds is limited and, often, with poorly established terminologies, not allowing the reader to know if the studied samples included seedless or seeded samples. So, the present study intended to carry out a chemical characterization of carob seeds focused on their bioactive compounds and test their bioactive properties. Carob seeds proved to be a source of tocopherols and organic acids, including phenolic compounds. Its antioxidant potential was demonstrated in vitro, as well as its antimicrobial capacity. This work proves that carob seeds have other functions in addition to those associated with E410. Thus, another potential can be given to the locust bean seed, namely the function of food preservative.


Assuntos
Fracionamento Químico/métodos , Fabaceae/química , Sementes/química , Antioxidantes/análise , Antioxidantes/isolamento & purificação , Fenóis/análise , Fenóis/isolamento & purificação
20.
Pharmaceuticals (Basel) ; 14(1)2021 Jan 12.
Artigo em Inglês | MEDLINE | ID: mdl-33445425

RESUMO

Anthriscus cerefolium (L.) Hoffm. is a plant traditionally used around the globe since antiquity. Although widely used in many traditional medicines in different cultures, from the scientific point of view it is poorly investigated. Glioblastoma, a tumor type with poor prognosis, is the most common and lethal brain tumor in adults. Current therapeutic strategies for glioblastoma include surgery, radiation and chemotherapy. On the other hand, it has been revealed that patients with cancers are highly susceptible to microbial infections due to the invasive nature of cancer treatment approaches. This study was designed to investigate the chemical profile of herba Anthriscii cerefoli methanolic extract by applying UHPLC-LTQ OrbiTrap MS4 analysis and to analyze its anti-glioblastoma and antimicrobial activities. This study revealed that methanolic extract of herba Anthrisc cerefolii contained phenolic acids and flavonoids, with 32 compounds being identified. Anti-glioblastoma activity was investigated in vitro using A172 glioblastoma cell line. The cytotoxic effects of the extract on A172 cells were compared to the same effect on primary human gingival fibroblast (HGF-1) cells. Decreased rate of proliferation and changes in cell morphology were detected upon treatment of A172 cells with the extract. The antimicrobial activity of extract was tested against Staphylococcus aureus and Candida species. The extract was active against the tested bacterium and yeasts, inhibiting free floating cells and microbial biofilms. This study is the first one to provide a detailed description of the chemical profile of A. cerefolium extract dealing with scientific insights into its anti-glioblastoma and antimicrobial activities.

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