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1.
Nutrients ; 16(6)2024 Mar 14.
Artigo em Inglês | MEDLINE | ID: mdl-38542742

RESUMO

Nutraceuticals represent an emerging and dynamic scientific field due to their important potential in integrated healthcare through nutritional and medicinal approaches that interact and complement each other mutually. In an attempt to find new sources for such preparations, the present research focuses on the species Craterellus cornucopioides (L.) Pers. (Cantharellaceae), also known as the black trumpet. This wild mushroom species is renowned for its culinary excellence and unique taste and is used especially in a dehydrated state. However, beyond its gastronomic value, recent scientific investigations have revealed its potential as a source of bioactive compounds with pharmaceutical and therapeutic significance. Our study aimed, therefore, to review the current data regarding the morphology, chemical profile, and medicinal potential of the black trumpet mushroom, highlighting its unique attributes. By conducting a comprehensive literature analysis, this paper contributes to the broader understanding of this remarkable fungal species as a potential functional food and its promising applications in the field of therapeutics.


Assuntos
Agaricales , Basidiomycota , Basidiomycota/química , Agaricales/química , Suplementos Nutricionais
2.
Antibiotics (Basel) ; 12(11)2023 Nov 20.
Artigo em Inglês | MEDLINE | ID: mdl-37998846

RESUMO

This study aimed to investigate the polyphenolic composition and antioxidant and antimicrobial potential of six Romanian Stachys species: S. officinalis, S. germanica, S. byzantina, S. sylvatica, S. palustris, and S. recta. The LC-MS/MS method was used to analyze the polyphenolic profile, while the phenolic contents were spectrophotometrically determined. The antioxidant activity was evaluated using the following methods: DPPH, FRAP, nitrite-induced autooxidation of hemoglobin, inhibition of cytochrome c-catalyzed lipid peroxidation, and electron paramagnetic resonance spectroscopy. The in vitro antimicrobial properties were assessed using agar-well diffusion, broth microdilution, and antibiofilm assays. Fifteen polyphenols were identified using LC-MS and chlorogenic acid was the major component in all the samples (1131.8-6761.4 µg/g). S. germanica, S. palustris, and S. byzantina extracts each displayed an intense antiradical action in relation to high contents of TPC (6.40 mg GAE/mL), flavonoids (3.90 mg RE/mL), and caffeic acid derivatives (0.89 mg CAE/mL). In vitro antimicrobial and antibiofilm properties were exhibited towards Candida albicans, Gram-positive and Gram-negative strains, with the most intense efficacy recorded for S. germanica and S. byzantina when tested against S. aureus. These results highlighted Stachys extracts as rich sources of bioactive compounds with promising antioxidant and antimicrobial efficacies and important perspectives for developing phytopharmaceuticals.

3.
Plants (Basel) ; 12(16)2023 Aug 14.
Artigo em Inglês | MEDLINE | ID: mdl-37631149

RESUMO

The Agastache genus is part of the Lamiaceae family and is native to North America, while one species, Agastache rugosa (A. rugosa), is native to East Asia. A review on the phytochemistry and bioactivity of Agastache genus was last performed in 2014. Since then, a lot of progress has been made on the characterization of the phytochemical and pharmacological profiles of Agastache species. Thus, the purpose of this paper is to present a summary of the findings on the phytochemistry and biological effects of several Agastache species, including both extracts and essential oil characterization. We performed a comprehensive search using PubMed and Scopus databases, following PRISMA criteria regarding the study selection process. The available data is focused mainly on the description of the chemical composition and bioactivity of A. rugosa, with fewer reports referring to Agastache mexicana (A. mexicana) and Agastache foeniculum (A. foeniculum). Agastache species are characterized by the dominance of flavonoids and phenolic acids, as well as volatile compounds, particularly phenylpropanoids and monoterpenes. Moreover, a series of pharmacological effects, including antioxidant, cytotoxic, antimicrobial, anti-atherosclerotic, and cardioprotective properties, have been reported for species from the Agastache genus.

4.
Pharmaceuticals (Basel) ; 16(3)2023 Feb 26.
Artigo em Inglês | MEDLINE | ID: mdl-36986458

RESUMO

The present research investigated the in vivo anti-inflammatory and cardioprotective activities, as well as the antioxidant potential of Taraxacum officinale tincture (TOT), in relation to the polyphenolic composition. Chromatographic and spectrophotometric techniques were used to determine the polyphenolic profile of TOT and the antioxidant activity was preliminarily assessed in vitro by DPPH• and FRAP spectrophotometric methods. The in vivo anti-inflammatory and cardioprotective activities were studied in rat turpentine-induced inflammation and in rat isoprenaline-induced myocardial infarction (MI) models. The main polyphenolic compound identified in TOT was cichoric acid. The oxidative stress determinations showed the capacity of the dandelion tincture not only to decrease the total oxidative stress (TOS), the oxidative stress index (OSI), and the total antioxidant capacity (TAC), but also the malondialdehide (MDA), thiols (SH), and nitrites/nitrates (NOx) levels both in inflammation and MI models. In addition, aspartate aminotransferase (AST), alanine aminotransferase (ALT), creatin kinase-MB (CK-MB), and nuclear factor kappa B (NF-κB) parameters were decreased by the administration of the tincture. The results show that T. officinale could be considered a valuable source of natural compounds with important benefits in pathologies linked to oxidative stress.

5.
Molecules ; 28(4)2023 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-36838592

RESUMO

The aim of the present study was to correlate the antioxidant, antimicrobial, and cytotoxic activities of hydroalcoholic extracts obtained from the aerial parts of three Dracocephalum moldavica L. cultivars with their polyphenolic compositions. The polyphenols were identified and quantified using spectrophotometrical methods and LC-MS analysis. Their antioxidant capacities were assessed using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) methods. Their in vitro antimicrobial efficacies were assessed using the agar well diffusion and broth microdilution methods. Their cytotoxicity was investigated on normal diploid foreskin fibroblasts (BJ) and on colorectal adenocarcinoma (DLD-1) cell lines. The results pointed out significant amounts of polyphenolic compounds in the compositions of the tested cultivars, with rosmarinic acid as the main compound (amounts ranging between 5.337 ± 0.0411 and 6.320 ± 0.0535 mg/mL). All three cultivars displayed significant antioxidant (IC50 ranging between 35.542 ± 0.043 and 40.901 ± 0.161 µg/mL for the DPPH assay, and for the FRAP assay 293.194 ± 0.213 and 330.165 ± 0.754 µmol Trolox equivalent/mg dry vegetal material) and antimicrobial potential (especially towards the Gram-positive bacteria), as well as a selective toxicity towards the tumoral line. A significant positive correlation was found between antioxidant activity and the total phenolic acids (r2 = 0.987) and polyphenols (r2 = 0.951). These findings bring further arguments for strongly considering D. moldavica cultivars as promising vegetal products, which warrants further investigation.


Assuntos
Anti-Infecciosos , Antineoplásicos , Antioxidantes/química , Extratos Vegetais/química , Polifenóis/farmacologia , Anti-Infecciosos/farmacologia
6.
Molecules ; 27(13)2022 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-35807229

RESUMO

Rosmarinus officinalis L. is a species that is widely known for its culinary and medicinal uses. The purpose of the present study consisted of the evaluation of the antiproliferative and antimicrobial effects of R. officinalis-loaded liposomes (L-R). Characterization of the liposomes was performed by establishing specific parameters. The load of the obtained liposomes was analyzed using an LC-MS method, and antiproliferative assays evaluated the cell viability on a liver adenocarcinoma cell line and on a human hepatic stellate cell line. Antimicrobial assays were performed by agar-well diffusion and by broth microdilution assays. The obtained liposomes showed high encapsulation efficiency, suitable particle size, and good stability. High amounts of caffeic (81.07 ± 0.76), chlorogenic (14.10 ± 0.12), carnosic (20.03 ± 0.16), rosmarinic (39.81 ± 0.35), and ellagic (880.02 ± 0.14) acids were found in their composition, together with other polyphenols. Viability and apoptosis assays showed an intense effect on the cancerous cell line and a totally different pattern on the normal cells, indicating a selective toxicity towards the cancerous ones and an anti-proliferative mechanism. Antimicrobial potential was noticed against all tested bacteria, with a better efficacy towards Gram-positive species. These results further confirm the biological activities of R. officinalis leaf extract, and proposes and characterizes novel delivery systems for their encapsulation, enhancing the biological activities of polyphenols, and overcoming their limitations.


Assuntos
Anti-Infecciosos , Rosmarinus , Anti-Infecciosos/farmacologia , Humanos , Lipossomos , Extratos Vegetais/farmacologia , Polifenóis/farmacologia
7.
Plants (Basel) ; 11(10)2022 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-35631802

RESUMO

The aim of the present study was to investigate the polyphenolic profile and the anti-inflammatory and anti-nociceptive activities of four traditionally used medicinal plants from Burkina Faso: Parkia biglobosa, Detarium microcarpum, Vitellaria paradoxa and Sclerocarya birrea. The analysis of the main phenolic compounds was performed by the HPLC-UV-MS method. The anti-inflammatory effect of the aqueous bark extracts was investigated by the λ-carrageenan-induced rat paw edema test. The anti-nociceptive activity was evaluated by the Randall−Selitto test under inflammatory conditions. Seven phenolic acids (gallic, protocatechuic, gentisic, vanillic, p-coumaric, ferulic, and syringic acids), and three flavonoids (catechin, epicatechin, and quercitrin) were identified in the plant samples. High contents of gallic acid were determined in the D. microcarpum, P. biglobosa and S. birrea extracts (190−300 mg/100 g), and V. paradoxa extract was the richest in epicatechin (173.86 mg/100 g). The λ-carrageenan-induced inflammation was significantly reduced (p < 0.001) by the P. biglobosa and D. microcarpum extracts (400 mg/kg p.o.). Under the inflammatory conditions, a significant anti-nociceptive activity (p < 0.001) was obtained after 2−3 h from the induction of inflammation. The effects of the tested extracts could be related to the presence of polyphenols and could be useful in the management of certain inflammatory diseases.

8.
Antioxidants (Basel) ; 11(2)2022 Jan 24.
Artigo em Inglês | MEDLINE | ID: mdl-35204101

RESUMO

In this study, the biological activities of four extracts from Vitis vinifera by-products: two pomace extracts, white (WPE) and red (RPE), a canes extract (CE), and their combination (CoE), were evaluated, to be included in freeze-drying mouthwashes formulations. The cytocompatibility and anticancerous potential of the four extracts were tested on three cancerous cell lines, as well as the cytoprotective activity against nicotine-induced cytotoxicity and the antioxidant potential determined on a human gingival fibroblasts (HGF) cell line. Additionally, the anti-inflammatory activity and the antimicrobial activity against several microorganisms from the oral microbiome were tested. Freeze-dried mouthwashes with CoE were prepared and characterized, both as lyophilizates and after reconstitution. The four tested extracts showed the highest cytotoxicity on MDA-kb2 cell line. The antioxidant potential was demonstrated for WPE, RPE, CE, and CoE, both in non-stimulated and H2O2 stimulated conditions. The four extracts reduced the levels of proinflammatory cytokines (IL-6, IL-8, and IL-1ß) in a dose-dependent manner, confirming their anti-inflammatory activity. The antimicrobial activity of tested extracts was shown against pathogenic bacteria from the oral microbiome. Mouthwashes of CoE with poloxamer-407, xylitol, and different ratios of mannitol were prepared by freeze-drying leading to porous formulations with interesting mechanical properties and reconstitution times.

9.
Plants (Basel) ; 10(12)2021 Dec 18.
Artigo em Inglês | MEDLINE | ID: mdl-34961280

RESUMO

The present study aimed to compare two polyphenolic-enriched extracts obtained from the Thymus marschallianus Willd. (Lamiaceae) species, harvested from culture (TMCE in doses of 0.66 µg GAE/mL and 0.066 µg GAE/mL) and from spontaneous flora (TMSE in doses of 0.94 µg GAE/mL and 0.094 µg GAE/mL) by assessing their biological effects on human umbilical vein endothelial cells (HUVECs) exposed to normoglycemic (137 mmol/L glucose) and hyperglycemic conditions (200 mmol/L glucose). Extracts were obtained by solid phase extraction (SPE) and analyzed by chromatographical (HPLC-DAD) and spectrophotometrical methods. Their effects on hyperglycemia were evaluated by the quantification of oxidative stress and NF-ĸB, pNF-ĸB, HIF-1α, and γ-H2AX expressions. The HPLC-DAD analysis highlighted significant amounts of rosmarinic acid (ranging between 0.18 and 1.81 mg/g dry extract), luteolin (ranging between 2.04 and 17.71 mg/g dry extract), kaempferol (ranging between 1.85 and 7.39 mg/g dry extract), and apigenin (ranging between 4.97 and 65.67 mg/g dry extract). Exposure to hyperglycemia induced oxidative stress and the activation of NF-ĸ increased the expression of HIF-1α and produced DNA lesions. The polyphenolic-enriched extracts proved a significant reduction of oxidative stress and γ-H2AX formation and improved the expression of HIF-1α, suggesting their protective role on endothelial cells in hyperglycemia. The tested extracts reduced the total NF-ĸB expression and diminished its activation in hyperglycemic conditions. The obtained results bring evidence for the use of the polyphenolic-enriched extracts of T. marschallianus as adjuvants in hyperglycemia.

10.
Molecules ; 26(11)2021 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-34067400

RESUMO

Syringa vulgaris L. (common lilac) is one of the most popular ornamental species, but also a promising not comprehensively studied source of bioactive compounds with important therapeutic potential. Our study was designed to characterize the chemical composition and to assess the antioxidant and cytotoxic properties of ethanolic extracts obtained from S. vulgaris L. flowers, leaves, bark, and fruit. The chemical profile of the ethanolic extracts was investigated using chromatographic (HPLC-DAD-ESI+, GC-MS) and spectral (UV-Vis, FT-IR) methods, while the protective effect against free radicals was evaluated in vitro by different chemical assays (DPPH, FRAP, CUPRAC). The cytotoxic activity was tested on two tumoral cell lines, HeLa, B16F10, using the MTT assay. Significant amounts of free or glycosylated chemical components belonging to various therapeutically important structural classes, such as phenyl-propanoids (syringin, acteoside, echinacoside), flavonoids (quercetin, kaempferol derivatives) and secoiridoids (secologanoside, oleuropein, 10-hydroxy oleuropein, demethyloleuropein, syringalactone A, nuzhenide, lingstroside) were obtained for the flowers, leaves and bark extracts, respectively. Furthermore, MTT tests pointed out a significant cytotoxic potential expressed in a non-dose-dependent manner toward the tumoral lines. The performed methods underlined that S. vulgaris extracts, in particular belonging to flowers and leaves, represent valuable sources of compounds with antioxidant and antitumoral potential.


Assuntos
Antioxidantes/química , Flores/química , Estresse Oxidativo , Extratos Vegetais/química , Folhas de Planta/química , Syringa/química , Animais , Linhagem Celular Tumoral , Cromatografia Líquida de Alta Pressão , Flavonoides/análise , Cromatografia Gasosa-Espectrometria de Massas , Glucosídeos , Glicosídeos , Células HeLa , Humanos , Melanoma Experimental , Camundongos , Fenóis , Fenilpropionatos , Folhas de Planta/metabolismo , Quercetina/análise , Espectroscopia de Infravermelho com Transformada de Fourier
11.
Molecules ; 26(6)2021 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-33804618

RESUMO

Rosmarinus officinalis L. is a widely known species for its medicinal uses, that is also used as raw material for the food and cosmetic industry. The aim of the present study was to offer a novel perspective on the medicinal product originating from this species and to test its hepatoprotective activity. The tested sample consisted in a tincture obtained from the fresh young shoots. Compounds that are evaluated for this activity are polyphenols and terpenoids, that are identified and quantified by HPLC-UV-MS and GC-MS. Antioxidant activity was assessed in vitro, using the DPPH, FRAP and SO assays. Hepatoprotective activity was tested in rats with experimentally-induced hepatotoxicity. In the chemical composition of the tincture, phenolic diterpenes (carnosic acid, carnosol, rosmanol, rosmadial) and rosmarinic acid were found to be the majority compounds, alongside with 1,8-cineole, camphene, linalool, borneol and terpineol among monoterpenes. In vitro, the tested tincture proved significant antioxidant capacity. Results of the in vivo experiment showed that hepatoprotective activity is based on an antioxidant mechanism. In this way, the present study offers a novel perspective on the medicinal uses of the species, proving significant amounts of polyphenols and terpenes in the composition of the fresh young shoots tincture, that has proved hepatoprotective activity through an antioxidant mechanism.


Assuntos
Antioxidantes/farmacologia , Doença Hepática Induzida por Substâncias e Drogas , Estresse Oxidativo/efeitos dos fármacos , Brotos de Planta/química , Rosmarinus/química , Animais , Antioxidantes/química , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/patologia , Cinamatos/química , Cinamatos/farmacologia , Depsídeos/química , Depsídeos/farmacologia , Diterpenos/química , Diterpenos/farmacologia , Avaliação Pré-Clínica de Medicamentos , Monoterpenos/química , Monoterpenos/farmacologia , Ratos , Ácido Rosmarínico
12.
Front Pharmacol ; 11: 581470, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33071792

RESUMO

The effects of two lyophilized extracts obtained from the aerial parts of Thymus marschallianus Willd. and harvested from wild flora (TMW) and obtained from culture (TMC) were evaluated in Wistar rats with experimentally induced hyperglycemia. The hyperglycemia was induced by streptozotocin (STZ) administration and the obtained results were evaluated in comparison for TMW and TMC. The polyphenolic composition of extracts was evaluated by spectrophotometrical and LC-MS methods. In vitro antioxidant capacity assays (DPPH, FRAP, EPR) were performed in order to preliminary establish the ability of tested samples to protect against free radical induced damage. Afterwards, the effects of these extracts were assessed in vivo on rats with experimental-induced hyperglycemia. Oxidative stress biomarkers (e.g. malondialdehyde-MDA), phosphorylated transcription factor subunit of nuclear kappaB (NF-kB) p65, methyl CpG binding protein (MECP) 2 and histone deacetylase 1 (HDAC1) expressions in hippocampus and frontal lobe were assessed. Open Field Test (OFT) and Elevated Plus Maze (EPM) were conducted on tested animals. Malondialdehyde (MDA) levels and HDAC1and MeCP2 expressions increased significantly in hippocampus (p<0.05) and frontal lobe (p<0.001) of diabetes group compared to the control group in parallel with decreasing of GSH/GSSG ratio. TMW and TMC administration reduced blood glucose levels and diminished lipid peroxidation, HDAC1 expression and enhanced antioxidant capacity in frontal lobe. TMW improved central locomotion of rats, increased phospho-NFkB p65 and diminished MECP2 expressions in hippocampus. Both tested samples exerted a beneficial effect by increasing the antioxidant defense. Our findings indicate that the administration of these extracts might represent a good option in the treatment of diabetes and its complications.

13.
Antioxidants (Basel) ; 9(6)2020 Jun 08.
Artigo em Inglês | MEDLINE | ID: mdl-32521718

RESUMO

Oral health is considered an important factor of general health and it contributes to the quality of life. Despite the raising awareness of preventive measures, the prevalence of oral health conditions continues to increase. In this context, a growing interest in investigating natural resources like Vitis vinifera (V. vinifera) phenolic compounds (PhCs) as oral health promoters has emerged. This paper aims to review the evidence about the bioactivities of V. vinifera by-products in oral health. Up to date, a high number of studies have thoroughly reported the antimicrobial and antiplaque activity of V. vinifera extracts against S. mutans or in multi-species biofilms. Moreover, the bioactive compounds from V. vinifera by-products have been shown to modulate the periodontal inflammatory response and the underlying oxidative stress imbalance induced by the pathogenic bacteria. Considering these beneficial effects, the utility of V. vinifera by-products in the maintaining of oral health and the necessary steps towards the development of oral care products were emphasized. In conclusion, the high potential of V. vinifera by-products could be valorized in the development of oral hygiene products with multi-target actions in the prevention and progression of several oral conditions.

14.
Antioxidants (Basel) ; 9(5)2020 Apr 30.
Artigo em Inglês | MEDLINE | ID: mdl-32365793

RESUMO

Winery industry by-products have a great reuse potential in the pharmaceutical and cosmetic fields due to their bioactive compounds. This study investigates the phytochemical profile and the bioactivity of Vitis vinifera variety Feteasca neagra tendrils extract (TE) and leaves extract (LE), intended to be used in oral hygiene products recommended in periodontal disease. The evaluation of the phenolic content was performed by colorimetric analysis. Liquid chromatography coupled with mass spectrometry was used to determine the chemical profile of the two extracts obtained from V. vinifera. Moreover, the antioxidant activity of the extracts was determined by spectrophotometric methods, as well as on human gingival fibroblasts (HGF) cell line. The cytocompatibility and cytoprotective effect against nicotine-induced cytotoxicity were tested, as well as the anti-inflammatory and antimicrobial effects. The TE showed higher total polyphenolic content, rich in rutin, compared to the leaves extract that displayed important amounts of isoquercitrin. The antioxidant effect was confirmed by both non-cellular and cellular tests. The cytocompatibility of the extracts was confirmed at a wide range of concentrations. The cytoprotective effect was demonstrated in HGF exposed to cytotoxic doses of nicotine; 300 µg/mL of both tested extracts decreased nicotine toxicity by approximately 20%. When challenged with E. coli polysaccharides, in HGF cells co-exposed to TE and LE, a reduction in the release of proinflammatory cytokines (IL-8, IL-6 and IL-1ß) was observed. The extracts were both able to reduce the levels of reactive oxygen species and inflammatory cytokines, and had notable antimicrobial effects on pathogenic bacteria associated with periodontitis.

15.
Plants (Basel) ; 10(1)2020 Dec 30.
Artigo em Inglês | MEDLINE | ID: mdl-33396775

RESUMO

The present study analyzed the methanol extract and tincture obtained from the spontaneous Romanian Cichorium intybus species, in order to evaluate polyphenols content and some biological properties. Chromatographic and spectrophotometric methods were used for the analysis of polyphenols and the antioxidant capacity was assessed in vitro with DPPH● (2,2-diphenyl-picrylhydrazil) and FRAP (ferric-reducing antioxidant power) tests. The cardio-protective effects of Cichorii herba tincture on myocardial ischemia induced by isoprenaline and nephroprotection on renal failure induced by gentamicin were evaluated on rats. Also, aspartate aminotrasferase (AST), alanine aminotransferase (ALT), creatine kinase-MB (CK-MB) and creatinine clearance (CrCl) were measured. The antioxidant effect was evaluated by determining total oxidative stress (TOS), oxidative stress index (OSI, total antioxidant capacity (TAC), malondyaldehide (MDA), total thiols (SH) and total nitrites and nitrates (NOx). Cichoric acid was the main polyphenolic compound. The extracts had moderate in vitro antioxidant activity but the in vivo antioxidant and anti-inflammatory effects were significant and associated with myocardial and renal dysfunction improvement. The results were attributed to the content of polyphenols in the extracts, for which reason C. intybus may be considered an important raw material for pharmaceuticals formulations recommended in the prevention or treatment of heart or kidney diseases.

16.
Oxid Med Cell Longev ; 2019: 1607903, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31687075

RESUMO

Schiff bases (SBs) are chemical compounds displaying a significant pharmacological potential. They are able to modulate the activity of many enzymes involved in metabolism and are found among antibacterial, antifungal, anti-inflammatory, antioxidant, and antiproliferative drugs. A new thiazolyl-triazole SB was obtained and characterized by elemental and spectral analysis. The antibacterial and antifungal ability of the SB was evaluated against Gram-positive and Gram-negative bacteria and against three Candida strains. SB showed good antibacterial activity against L. monocytogenes and P. aeruginosa; it was two times more active than ciprofloxacin. Anti-Candida activity was twofold higher compared with that of fluconazole. The effect of the SB on cell viability was evaluated by colorimetric measurement on cell cultures exposed to various SB concentrations. The ability of the SB to modulate oxidative stress was assessed by measuring MDA, TNF-α, SOD1, COX2, and NOS2 levels in vitro, using human endothelial cell cultures exposed to a glucose-enriched medium. SB did not change the morphology of the cells. Experimental findings indicate that the newly synthetized Schiff base has antibacterial activity, especially on the Gram-negative P. aeruginosa, and antifungal activity. SB also showed antioxidant and anti-inflammatory activities.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Células Endoteliais da Veia Umbilical Humana/patologia , Estresse Oxidativo/efeitos dos fármacos , Bases de Schiff/farmacologia , Tiazóis/farmacologia , Antioxidantes/farmacologia , Bactérias/efeitos dos fármacos , Biomarcadores/metabolismo , Compostos de Bifenilo/química , Sobrevivência Celular/efeitos dos fármacos , Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos , Células Endoteliais da Veia Umbilical Humana/metabolismo , Humanos , Inflamação/patologia , Peroxidação de Lipídeos/efeitos dos fármacos , Malondialdeído/metabolismo , Testes de Sensibilidade Microbiana , Picratos/química , Bases de Schiff/química , Tiazóis/química , Fator de Necrose Tumoral alfa/metabolismo
17.
Biomolecules ; 9(10)2019 09 25.
Artigo em Inglês | MEDLINE | ID: mdl-31557922

RESUMO

The aim of the present study was to establish the best experimental conditions that lead to the extracts richest in polyphenolic compounds obtained from pomace and canes of Vitis vinifera. In this regard, a D-Optimal design of experiments (DoE) method was applied to investigate the extraction process parameters from each of three materials: red pomace (RP), white pomace (WP) and canes (C). The input variables were the extraction temperature and the ethanol ratio and as response, the total polyphenols content (TPC) was determined. A design space was generated for each of the plant materials and the most concentrated polyphenol extracts were obtained using 50% ethanol at a temperature of 80 °C. Further, the phenolic profiles of the concentrated extracts were detected by LC/MS/MS and the results showed that WP extract was richer in polyphenolic compounds, both flavonoid and phenolic acids, followed by the RP and C extracts. The antioxidant assays revealed that WP and RP extracts exhibited a higher antioxidant activity which correlated to the high content of polyphenols. These findings revealed that RP, WP and C, currently considered agricultural wastes from winery, may be valorized as an important source of natural antioxidants.


Assuntos
Antioxidantes/isolamento & purificação , Temperatura Alta , Polifenóis/isolamento & purificação , Vitis/química , Antioxidantes/química , Antioxidantes/farmacologia , Benzotiazóis/antagonistas & inibidores , Cromatografia Líquida de Alta Pressão , Hemoglobinas/química , Nitritos/química , Polifenóis/química , Polifenóis/farmacologia , Ácidos Sulfônicos/antagonistas & inibidores , Espectrometria de Massas em Tandem
18.
Molecules ; 24(17)2019 Aug 26.
Artigo em Inglês | MEDLINE | ID: mdl-31455036

RESUMO

Thymus marschallianus Willd. is a Lamiaceae species spread in a large variety of habitats worldwide. The aim of the present research was to analyse two different samples belonging to this species, one obtained from the spontaneous flora and one from culture. The total polyphenols, flavonoids, and phenolic acid contents were spectrophotometrically determined. Qualitative and quantitative analysis of polyphenols was performed by an HPLC-DAD-ESI (+)-MS method. For the antibacterial assay, the well-diffusion and the broth microdilution methods were used. Analysis of polyphenols revealed for both samples the presence of flavonoids like luteolin, quercetin, apigenin and their derivatives, but also of rosmarinic acid and methyl-rosmarinate. Differences regarding the amount of these compounds were emphasized. Significantly larger amounts of flavonoids were found for the sample harvested in the spontaneous flora, while for the rosmarinic acid, larger amounts were found for the cultured sample. Both samples displayed promising antibacterial activity, particularly towards Gram positive organisms. T. marschallianus represents, therefore, a rich source of polyphenolic compounds that prove its promising potential as a medicinal species.


Assuntos
Anti-Infecciosos/farmacologia , Compostos Fitoquímicos/farmacologia , Thymus (Planta)/química , Anti-Infecciosos/química , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Flavonoides/química , Flavonoides/farmacologia , Bactérias Gram-Positivas/efeitos dos fármacos , Hidroxibenzoatos/química , Hidroxibenzoatos/farmacologia , Compostos Fitoquímicos/química , Polifenóis/química , Polifenóis/farmacologia
19.
J Enzyme Inhib Med Chem ; 34(1): 898-908, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30938216

RESUMO

The rapid emergence of bacterial resistance to antibiotics currently available for treating infectious diseases requires effective antimicrobial agents with new structural profiles and mechanisms of action. Twenty-three thiazolin-4-one derivatives were evaluated for their antibacterial activity by determining the growth inhibition zone diameter, the minimum inhibitory concentration (MIC), and the minimum bactericidal concentration (MBC), against gram-positive and gram-negative bacteria. Compounds 3a-c, 3e-h, 6b-c and 9a-c expressed better MIC values than moxifloxacin, against Staphylococcus aureus. Compounds 3h and 9b displayed similar effect to indolmycin, a tryptophanyl-tRNA ligase inhibitor. Due to their structural analogy to indolmycin, all compounds were subjected to molecular docking on tryptophanyl-tRNA synthetase. Compounds 3a-e, 6a-e, 8 and 9a-e exhibited better binding affinities towards the target enzymes than indolmycin. The antioxidant potential of the compounds was evaluated by four spectrophotometric methods. Thiazolin-4-ones 3e, 6e and 9e presented better antiradical activity than ascorbic acid, trolox and BHT, used as references.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Tiazóis/farmacologia , Triptofano-tRNA Ligase/antagonistas & inibidores , Antibacterianos/síntese química , Antibacterianos/química , Antioxidantes/síntese química , Antioxidantes/química , Compostos de Bifenilo/antagonistas & inibidores , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Conformação Molecular , Simulação de Acoplamento Molecular , Picratos/antagonistas & inibidores , Relação Estrutura-Atividade , Tiazóis/síntese química , Tiazóis/química , Triptofano-tRNA Ligase/metabolismo
20.
Pak J Pharm Sci ; 31(5(Supplementary)): 2027-2032, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30393208

RESUMO

The Ranunculus species are poorly known as medicinal plants. They have potential toxicity given by the ranunculin and its enzymatic degradation compounds: protoanemonin and anemonin. This paper aims to evaluate the anemonin content of four species: R. bulbosus, R. ficaria, R. sardous and R. sceleratus. The evaluation was performed by TLC and HPLC. There were evaluated two types of extracts hydroalcoholic (HA) and glycerol-ethanol (GE). The most concentrated extract in anemonin was found to be the R. sardous aerial part HA extract: 2.66 mg/ml. The lowest anemonin content is in R. sceleratus: 0.13-0.19 mg/ml. In R. bulbosus aerial part the anemonin content is less than the used HPLC method detection limits (7.68 mg/ml). In all cases the GE extracts are less concentrated in anemonin, being more safely for human administration.


Assuntos
Furanos/análise , Extratos Vegetais/análise , Extratos Vegetais/genética , Ranunculus/genética , Cromatografia Líquida de Alta Pressão/métodos , Furanos/química , Humanos , Extratos Vegetais/química , Especificidade da Espécie
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