Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 12 de 12
Filtrar
Mais filtros










Base de dados
Intervalo de ano de publicação
1.
Int J Mol Sci ; 22(14)2021 Jul 16.
Artigo em Inglês | MEDLINE | ID: mdl-34299238

RESUMO

This study focused on the biological evaluation and chemical characterization of Geranium pyrenaicum Burm. f. Different solvent extracts (hexane, ethyl acetate, methanol, and water extracts) were prepared. The phytochemical profile, antioxidant, and enzyme inhibitory activity were investigated. Cytotoxicity was assessed using VERO, FaDu, HeLa and RKO cells. The antiviral activity was carried out against HSV-1 (Herpes simplex virus 1) propagated in VERO cell line. The aqueous extract, possessing high phenolic content (170.50 mg gallic acid equivalent/g extract), showed the highest reducing capacity (613.27 and 364.10 mg Trolox equivalent/g extract, for cupric reducing antioxidant capacity and ferric reducing antioxidant power, respectively), radical scavenging potential (469.82 mg Trolox equivalent/g extract, against 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)), metal chelating ability (52.39 mg ethylenediaminetetraacetic acid equivalent/g extract) and total antioxidant capacity (3.15 mmol Trolox equivalent/g extract). Liquid chromatography-electrospray ionization-quadrupole time-of-flight-mass spectrometry (LC-ESI-QTOF-MS/MS) alloved to tentatively identify a total of 56 compounds in the extracts, including ellagitannins, gallic acid and galloyl derivatives amongst others. The ethyl acetate extracts substantially depressed cholinesterase enzymes (4.49 and 12.26 mg galantamine equivalent/g extract against AChE and BChE, respectively) and α-amylase enzyme (1.04 mmol acarbose equivalent/g extract). On the other hand, the methanolic extract inhibited tyrosinase (121.42 mg kojic acid equivalent/g extract) and α-glucosidase (2.39 mmol acarbose equivalent/g extract) activities. The highest selectivity towards all cancer cell lines (SI 4.5-10.8) was observed with aqueous extract with the FaDu cells being the most sensitive (CC50 40.22 µg/mL). It can be concluded that the presence of certain bioactive antiviral molecules may be related to the high anti HSV-1 activity of the methanolic extract. This work has generated vital scientific data on this medicinal plant, which is a prospective candidate for the creation of innovative phyto-pharmaceuticals.


Assuntos
Geranium/metabolismo , Extratos Vegetais/química , Animais , Antioxidantes , Antivirais , Linhagem Celular , Cromatografia Líquida de Alta Pressão/métodos , Flavonoides/análise , Humanos , Fenóis/análise , Compostos Fitoquímicos/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Estudos Prospectivos , Espectrometria de Massas por Ionização por Electrospray/métodos , Espectrometria de Massas em Tandem/métodos
2.
Food Chem Toxicol ; 153: 112268, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34015423

RESUMO

The Tanacetum genus is a big treasure with the presence of biologically-active compounds and members of this genus are widely used for the treatment of several diseases in traditional medicine system. Considering this fact, we aimed to analyze the extracts from Tanacetum vulgare L. in case of chemical profiles and biological effects. Chemical characterization was performed by using UHPLC-HRMS technique and showed the presence of several phytochemical groups (107 compounds were identified, including phenolic acids, flavonoids, terpenoids and fatty acids. Biological abilities were examined by using antioxidant (DPPH, ABTS, FRAP, CUPRAC, metal chelating and phosphomolybdenum assays) and enzyme inhibition (tyrosinase, amylase, glucosidase and cholinesterase) properties. Pharmaco-toxicological investigations were also performed with the aim to identify limits of biocompatibility, anti-oxidant and neuromodulatory effects, in hypothalamic HypoE22 cells. A bioinformatic analysis was also carried to unravel the putative protein-targets for the observed biological effects. Generally, the tested hexane and hydroalcoholic extracts displayed stronger activities in antioxidant and enzyme inhibitory assays, when compared with water. In addition, multivariate analysis was performed to understand the differences in both solvents and plant parts and we clearly observed the separation of these parameters. The extracts (10 µg/mL) also stimulated DAT and inhibited TNFα and BDNF gene expression, in HypoE22 cells. In parallel, the extracts were also able to stimulate norepinephrine release from this cell line. By contrast, in the concentration range 50-100 µg/mL, the extracts reduced the HypoE22 viability, thus demonstrating cytotoxicity at concentrations 5-10 fold higher compared to those effective as neuromodulatory. Our observations manifested that T. vulgare has several beneficial effects and it can be used as a potential natural raw material for designing further health-promoting applications in nutraceutical, cosmeceutical, and pharmaceutical areas.


Assuntos
Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Tanacetum/química , Animais , Antioxidantes/análise , Antioxidantes/química , Antioxidantes/toxicidade , Artemia/efeitos dos fármacos , Linhagem Celular , Inibidores Enzimáticos/análise , Inibidores Enzimáticos/química , Inibidores Enzimáticos/toxicidade , Etanol/química , Flores/química , Hexanos/química , Análise Multivariada , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/química , Compostos Fitoquímicos/toxicidade , Componentes Aéreos da Planta/química , Extratos Vegetais/análise , Extratos Vegetais/química , Extratos Vegetais/toxicidade , Caules de Planta/química , Mapas de Interação de Proteínas , Ratos , Solventes/química , Água/química
3.
Foods ; 9(6)2020 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-32492817

RESUMO

Fibigia clypeata (L.) Medik. is a poorly studied plant species belonging to the Brassicaceae family, and usually used as cress in the salads. The current investigation aimed at assessing the antioxidant potential and inhibitory activity of ethyl acetate, methanol, and aqueous extracts of F. clypeata against key enzymes targeted in the management of type II diabetes (α-amylase and α-glucosidase), Alzheimer's disease (acetylcholinesterase and butyrylcholinesterase), and skin hyperpigmentation (tyrosinase). Cytotoxicity of the extracts was also determined using normal VERO and cancer FaDu and SCC-25 cell lines. Besides, LC-MS was employed to investigate the detailed phytochemical profiles of the extracts. The methanol extract showed potent enzyme inhibitory activity (4.87 mg galantamine equivalent/g, 3.52 mg galantamine equivalent/g, 126.80 mg kojic acid equivalent/g, and 24.68 mg acarbose equivalent/g, for acetylcholinesterase, butyrylcholinesterase, tyrosinase, and α-glucosidase, respectively) and antioxidant potential (96.52, 109.10, 154.02, and 104.85 mg trolox equivalent/g, for DPPH, ABTS, CUPRAC, and FRAP assays, respectively). Interestingly, caffeic acid-O-hexoside derivative, caffeyl alcohol O-glucopyranoside, and ferulic acid derivative were identified in all extracts. F. clypeata extracts showed no cytotoxicity towards VERO cell line and a weak cytotoxic potential against FaDu and SCC-25 cell lines. Interesting scientific evidence gathered from the present study support further investigation on F. clypeata in the view of designing and developing a novel therapeutic agent for the management of Alzheimer's disease, type II diabetes, skin hyperpigmentation problems, as well as cancer.

4.
Molecules ; 25(10)2020 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-32455936

RESUMO

Anacamptis pyramidalis (L.) Rich. forms part of the Orchidaceae family that is highlyvalued for its horticultural as well as therapeutic benefits. The present study set out to investigatethe inhibitory activity of A. pyramidalis tubers against key biological targets for the management oftype 2 diabetes, Alzheimer disease, and skin hyperpigmentation. In addition, the antioxidantpotential of the extracts was also assessed using multiple methods. The detailed phytochemicalprofiles of the extracts were determined using high-performance liquid chromatography. Based onqualitative phytochemical fingerprint, a network pharmacology analysis was conducted as well.Parishin was identified from the water extract only, whereas gastrodin and caffeic acid derivativeswere present in the methanol extract. The methanol extract exhibited high inhibitory activityagainst tyrosinase (69.69 mg kojic acid equivalent/g extract), α-amylase (15.76 mg acarboseequivalent/g extract), and α-glucosidase (20.07 mg acarbose equivalent/g extract). Similarly, themethanol extract showed highest antioxidant potential (22.12, 44.23, 45.56, and 29.38 mg Troloxequivalent/g extract, for 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), CUPric Reducing Antioxidant Capacity (CUPRAC),and Ferric Reducing Antioxidant Power (FRAP) assays, respectively). Finally, the results ofnetwork pharmacology analysis, besides corroborating traditional uses of plant extracts in themanagement of cold and flu, confirmed a direct involvement of identified phytochemicals in theobserved enzyme inhibitory effects, especially against tyrosinase, α-amylase, and α-glucosidase.Furthermore, based on the results of both colorimetric assays and network pharmacology analysis related to the activity of A. pyramidalis extracts and identified phytocompounds on enzymesinvolved in type 2 diabetes, a docking study was conducted in order to investigate the putativeinteractions of oxo-dihydroxy octadecenoic acid trihydroxy octadecenoic acid against aldosereductase, peroxisome proliferator-activated receptor (PPAR)-α, dipeptidyl peptidase (DPP)-IV,and α-glucosidase. Docking analysis suggested the inhibitory activity of these compounds againstthe aforementioned enzymes, with a better inhibitory profile shown by oxo-dihydroxyoctadecenoic acid. Overall, the present findings supported the rationale for the use of A.pyramidalis as source of bioactive metabolites and highlight, today more than ever, for the strongnecessity of linkage strategy between wild resource valorization and conservation policy.


Assuntos
Antioxidantes/farmacologia , Inibidores de Glicosídeo Hidrolases/farmacologia , Orchidaceae/química , Compostos Fitoquímicos/química , Doença de Alzheimer/tratamento farmacológico , Antioxidantes/química , Simulação por Computador , Diabetes Mellitus Tipo 2/tratamento farmacológico , Inibidores de Glicosídeo Hidrolases/química , Horticultura/métodos , Humanos , Hiperpigmentação/tratamento farmacológico , Metanol/química , Simulação de Acoplamento Molecular , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Dermatopatias/tratamento farmacológico , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/química , alfa-Glucosidases/química , alfa-Glucosidases/efeitos dos fármacos
5.
J Sci Food Agric ; 100(5): 1998-2006, 2020 Mar 30.
Artigo em Inglês | MEDLINE | ID: mdl-31849067

RESUMO

BACKGROUND: In this investigation, the chemical and biological profiles of three Turkish Crataegus species (Crataegus orientalis, Crataegus szovitsii and Crataegus tanacetifolia) were studied in order to provide the first comprehensive characterization and their health-promoting potential. In this respect, polyphenolic profiles were evaluated using ultrahigh-performance liquid chromatography-quadrupole time-of-flight mass spectrometry. The in vitro antioxidant activities of the Crataegus samples were evaluated by using free-radical scavenging, phosphomolybdenum, ferrous-ion chelating, and reducing power assays. The inhibitory activities against α-glucosidase, amylase, cholinesterases (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)), and tyrosinase were also established. RESULTS: The untargeted metabolomic approach highlighted the effect of both extraction types and species on the phenolic profiles of different Crateagus tissues (i.e. leaves and twigs). The methanolic extracts showed the maximum radical scavenging and reducing activity in all test systems, whereas for ferrous-ion chelating assays the decocted and infused extracts showed the highest activity. Only the methanolic extracts were effective against AChE and BChE. The extract tested showed remarkable inhibitory effects against tyrosinase and α-glucosidase, whereas all the extracts exhibited modest inhibition against α-amylase. Overall, the twig extracts of the three species studied showed superior antioxidant and enzyme inhibitory activities. CONCLUSION: On the basis of these results, the three Crataegus species can be classified as potent bioresources for high-value phytochemicals, which warrant further investigations for developing novel nutraceuticals. © 2019 Society of Chemical Industry.


Assuntos
Crataegus/química , Inibidores Enzimáticos/química , Extratos Vegetais/química , Antioxidantes/metabolismo , Butirilcolinesterase/química , Crataegus/metabolismo , Inibidores Enzimáticos/metabolismo , Metabolômica , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/química , Fenóis/química , Fenóis/metabolismo , Extratos Vegetais/metabolismo , Turquia , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/química , alfa-Glucosidases/química
6.
Food Chem Toxicol ; 135: 111052, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31837349

RESUMO

Ethnobotanical evidences report the use of Rhododendron luteum Sweet (Ericaceae) in traditional medicinal systems. However, R. luteum has been associated to the occurrence of 'mad honey' poisoning. In the present study, the ethyl acetate, methanol, and water extracts of R. luteum were investigated for their in vitro antioxidant, enzyme inhibition, and cytotoxic properties. The cytotoxicity of R. luteum extracts on A549 lung cancer cell line was evaluated using MTT cell viability assay. Besides, HPLC-ESI-MSn approach was employed to elucidate the secondary metabolite profiles of R. luteum in order to establish any structure-activity relationship. Methanol and water extracts of R. luteum possessed highest radical scavenging and reducing properties while the ethyl acetate extract showed highest metal chelating properties. In terms of enzyme inhibition, the methanol and ethyl acetate extracts of R. luteum, possessing epigallocatechin, were active inhibitors of cholinesterase enzymes, α-glucosidase, and tyrosinase. Water extract caused growth inhibition of A549 cells with 207.2 µg/ml IC50 value. Though R. luteum has received little scientific attention due to the occurrence of grayanotoxins in the plant, however, data presented in this work shows promising biological activity of R. luteum and highlighted its role as a potential source of antioxidant and key enzyme inhibitors.


Assuntos
Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Extratos Vegetais/farmacologia , Rhododendron/química , Células A549 , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Humanos
7.
Molecules ; 24(14)2019 Jul 16.
Artigo em Inglês | MEDLINE | ID: mdl-31315236

RESUMO

Ethyl acetate (EA), methanol (MeOH), and aqueous extracts of aerial parts of Anthemis tinctoria var. pallida (ATP) and A. cretica subsp. tenuiloba (ACT) were investigated for their phenol and flavonoid content, antioxidant, and key enzyme inhibitory potentials. All extracts displayed antiradical effects, with MeOH and aqueous extracts being a superior source of antioxidants. On the other hand, EA and MeOH extracts were potent against AChE and BChE. Enzyme inhibitory effects against tyrosinase and α-glucosidase were observed, as well. We also studied Anthemis extracts in an ex vivo experimental neurotoxicity paradigm. We assayed extract influence on oxidative stress and neurotransmission biomarkers, including lactate dehydrogenase (LDH) and serotonin (5-HT), in isolated rat cortex challenged with K+ 60 mM Krebs-Ringer buffer (excitotoxicity stimulus). An untargeted proteomic analysis was finally performed in order to explore the putative mechanism in the brain. The pharmacological study highlighted the capability of ACT water extract to blunt K+ 60 mM increase in LDH level and 5-HT turnover, and restore physiological activity of specific proteins involved in neuron morphology and neurotransmission, including NEFMs, VAMP-2, and PKCγ, thus further supporting the neuroprotective role of ACT water extract.


Assuntos
Anthemis/química , Flavonoides/química , Fármacos Neuroprotetores/química , Fenóis/química , Acetilcolinesterase/metabolismo , Antioxidantes/química , Antioxidantes/farmacologia , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Flavonoides/farmacologia , Proteínas Ligadas por GPI/metabolismo , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Monofenol Mono-Oxigenase/antagonistas & inibidores , Fármacos Neuroprotetores/farmacologia , Fenóis/farmacologia , Componentes Aéreos da Planta/química , Extratos Vegetais/química , alfa-Glucosidases/metabolismo
8.
J Pharm Biomed Anal ; 173: 75-85, 2019 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-31121457

RESUMO

The phytochemical composition of different extracts obtained from stinking chamomile (Anthemis cotula L.) was investigated. Ethanol was used as solvent and accelerated solvent extraction (ASE), microwave assisted extraction (MAE), maceration, soxhlet extraction (SE), and ultrasound assisted extraction (UAE) were applied on plant material. Comparison of the phytochemical contents, antioxidant, and enzyme inhibitory properties were performed. The most abundant sesquiterpene in the extracts was anthecotuloide, while the most present phenolics were caffeoyl quinic acid, quercetin, and kaempferol derivatives. UAE extract was the most efficient in the extraction of sesquiterpenoids and polyphenols. Considering the assays on antioxidant activity and enzyme inhibition, ASE extract showed highest phenolic content (62.92 mg gallic acid equivalent/g extract). Likewise, this extract showed highest radical scavenging (103.44 mg trolox equivalent [TE]/g extract and 155.70 mg TE/g extract, for DPPH and ABTS assays respectively) and reducing power potential (435.32 and 317.89 mg TE/g extract, for CUPRAC and FRAP assays, respectively). The different extracts showed similar results in the enzyme inhibition assays suggesting that the extraction methods used have no effect on observed enzyme activities. Novelty of our findings are the inhibitory action of the ethanol extract of A. cotula aerial parts on key enzymes associated with Alzheimer's disease (acetyl cholinesterase, butyryl cholinesterase), type 2 diabetes (α-amylase, α-glucosidase), and skin hyperpigmentation disorders (tyrosinase). Data collected from the present work further appraises the multiple potential biological properties of stinking chamomile suggesting the need for further investigation on its constituents.


Assuntos
Anthemis/química , Fracionamento Químico/métodos , Extratos Vegetais/isolamento & purificação , Cromatografia Líquida de Alta Pressão/métodos , Inibidores Enzimáticos/análise , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/farmacologia , Sequestradores de Radicais Livres/análise , Sequestradores de Radicais Livres/isolamento & purificação , Sequestradores de Radicais Livres/farmacologia , Lactonas/análise , Lactonas/isolamento & purificação , Micro-Ondas , Componentes Aéreos da Planta/química , Extratos Vegetais/análise , Extratos Vegetais/farmacologia , Polifenóis/análise , Polifenóis/isolamento & purificação , Sesquiterpenos/análise , Sesquiterpenos/isolamento & purificação , Solventes/química , Ondas Ultrassônicas
9.
Food Chem Toxicol ; 127: 237-250, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30914354

RESUMO

In the present study, the biological properties, including, the enzyme inhibitory and antioxidant activities, as well as, the phytochemical profile of the ethyl acetate, methanol, and water extracts of Rubus sanctus Schreb. and Rubus ibericus Juz. leaves were determined using in vitro bioassays. Wide range of phytochemicals, including, hydroxybenzoic acids, hydroxycinnamic acids, acylquinic acids, ellagitannins, flavonoids, and triterpenoid saponins were determined using UHPLC-ESI/HRMS technique. The ethyl acetate and methanol extracts of the studied Rubus species effectively inhibited acetyl and butyryl cholinesterase. On the other hand, R. sanctus water extract showed low inhibition against α-amylase and prominent inhibitory action against α-glucosidase. Data collected from this study reported the radical scavenging and reducing potential of the studied Rubus species. Investigation of the protective effects of the different extracts of R. sanctus and R. ibericus in experimental model of ulcerative colitis was performed. The extracts were also tested on spontaneous migration of human colon cancer cells (HCT116) in wound healing experimental paradigm. Only R. sanctus methanol extract inhibited spontaneous HCT116 migration in the wound healing test. Our results suggested that R. sanctus and R. ibericus may be potential candidates as sources of biologically-active compounds for the development of nutraceuticals, pharmaceuticals, and/or cosmetics.


Assuntos
Compostos Fitoquímicos/análise , Rubus/química , Acetatos/química , Acetilcolinesterase/efeitos dos fármacos , Animais , Artemia/efeitos dos fármacos , Butirilcolinesterase/efeitos dos fármacos , Inibidores da Colinesterase/farmacologia , Cromatografia Líquida de Alta Pressão/métodos , Células HCT116 , Humanos , Masculino , Metanol/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Ratos Sprague-Dawley , Rubus/classificação , Especificidade da Espécie , Espectrometria de Massas por Ionização por Electrospray/métodos , Cicatrização/efeitos dos fármacos
10.
J Ethnopharmacol ; 235: 293-300, 2019 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-30763694

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Hypericum perforatum L. (Hypericaceae) has been used as a traditional therapeutic for skin wounds, burns, cuts and stomach ailments including stomach ache, ulcers for a long time in many societies. Although many studies about its antibacterial properties can be found, there is a lack of studies about its quorum sensing inhibition properties, which effects bacterial vulnerability directly, on Pseudomonas aeruginosa. AIM OF THE STUDY: Evaluation of anti-quorum sensing (anti-QS) and anti-biofilm activity of ethanol, methanol, acetone and ultra-sonicated extracts of Hypericum perforatum L. (HP) which is a well-known wound healer, against P. aeruginosa. MATERIALS AND METHODS: Aerial parts of HP were extracted with ethanol, methanol and acetone. In addition, separate extractions with ultrasonication were carried out with same solvents. Anti-QS activity tests with different doses of HP extracts were performed by employing biomonitor strains, of which the promoter of QS regulating and green fluorescent protein (GFP) genes were fusioned. For anti-biofilm activity, HP extracts were applied to wild type PAO1 strains and biofilm inhibition was quantified via crystal violet staining method. RESULTS: HP's ethanol, methanol and acetone extracts (250 µg/ml doses) inhibited LasIR signalling pathway up to 65.43%, 59.60%, 55.95% and same solvent extracts obtained with ultrasonication inhibited 71.33%, 64.47%, 57.35% respectively. Moreover, inhibition rates of RhlIR pathway were 28.80%, 50.83%, 45.84% for ethanol, methanol, acetone extracts (250 µg/ml doses) and 51.43%, 57.41%, 50.02% for ultrasonication extracts (250 µg/ml doses), compared to untreated controls. In the experiments, ethanol, methanol, acetone and ultra-sonicated extracts of HP did not inhibit biofilm formation. CONCLUSIONS: This study shows that HP plant is capable for blocking of las and rhl QS systems of P. aeruginosa. However, it was observed that ethanol, methanol and acetone extract of the plant samples did not show anti-biofilm activity against P. aeruginosa. This led us to thinking that biofilm formation was caused via another pathway such as IQS or PQS. Further studies with isolated active compounds of HP might give a better understanding of the effects on biofilm formation of P. aeruginosa.


Assuntos
Antibacterianos/farmacologia , Hypericum/química , Extratos Vegetais/farmacologia , Pseudomonas aeruginosa/efeitos dos fármacos , Antibacterianos/administração & dosagem , Antibacterianos/isolamento & purificação , Biofilmes/efeitos dos fármacos , Relação Dose-Resposta a Droga , Medicina Tradicional/métodos , Testes de Sensibilidade Microbiana , Componentes Aéreos da Planta , Extratos Vegetais/administração & dosagem , Percepção de Quorum/efeitos dos fármacos
11.
J Biomol Struct Dyn ; 37(12): 3269-3281, 2019 08.
Artigo em Inglês | MEDLINE | ID: mdl-30058457

RESUMO

Tragopogon dubius and Tussilago farfara are consumed as vegetables and used in folk medicine to manage common diseases. Herein, the chemical compositions and biological activities of different leaf extracts (ethyl acetate, methanol, and water) of T. dubius and T. farfara were evaluated. The antibacterial, antifungal, and antioxidant abilities of the extracts were tested using different assays including free radical scavenging, reducing power, phosphomolybdenum, and metal chelating assays. Enzyme inhibitory potentials were evaluated against cholinesterases, tyrosinase, α-amylase and α-glucosidase. Complexes of bioactive compounds (chlorogenic and rosmarinic acid) were docked into the enzymatic cavity of α-glucosidase and subjected to molecular dynamic calculation, enzyme conformational stability, and flexibility analysis. T. dubius and T. farfara extracts showed remarkable antioxidant potentials. Ethyl acetate extracts of T. dubius and T. farfara were the most potent inhibitors of acetylcholinesterase and butyrylcholinesterase. T. dubius ethyl acetate extract and T. farfara methanolic extract showed noteworthy activity against α-glucosidase. High performance liquid chromatography analysis revealed the abundance of some phenolic compounds including chlorogenic and rosmarinic acids. Ethyl acetate extract of T. dubius showed notable antifungal activity against all strains. Docking studies showed best pose for chlorogenic acid was stabilized by a network of hydrogen bonds with residues Asp1157, Asp1279, whereas rosmarinic acid showed several hydrogen bonds with Asp1157, Asp1420, Asp1526, Lys1460 and Trp1369. This study further validates the use of T. dubius and T. farfara in traditional medicine, as well as act as a stimulus for further studies for future biomedicine development. Communicated by Ramaswamy H. Sarma.


Assuntos
Asteraceae/química , Tragopogon/química , Tussilago/química , Acetilcolinesterase/metabolismo , Antioxidantes/química , Butirilcolinesterase/metabolismo , Cinamatos/farmacologia , Depsídeos/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Flavonoides/sangue , Flavonoides/farmacologia , Simulação de Acoplamento Molecular/métodos , Monofenol Mono-Oxigenase/metabolismo , Fenóis/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo
12.
Comput Biol Chem ; 75: 111-119, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29772456

RESUMO

Salvia sclarea L. is traditionally used to manage common human ailments and is consumed as a food product. This study aimed to establish the phytochemical profile and antioxidant potential of ethyl acetate, methanol, and water extracts of Salvia sclarea. The inhibitory action of the extracts against α-amylase, α-glucosidase, acetylcholinesterase, butyrylcholinesterase, and tyrosinase was also investigated. Methanol extract showed the highest phenolic and flavonoid contents (81.78 mg GAE/g extract and 40.59 mg RE/g extract, respectively). Reversed phase high performance liquid chromatography with diode array detector analysis revealed that S. sclarea was rich in rosmarinic acid. The water extract exhibited the lowest inhibitory activity against α-amylase but the upmost activity against α-glucosidase (0.19 and 18.24 mmol ACAE/g extract, respectively). Experimental data showed that only the water extract (8.86 mg KAE/g extract) significantly inhibited tyrosinase. Docking studies showed that quercetin binds to tyrosinase by two hydrogen and a pi-pi bonds. Salvia sclarea showed interesting biological activity against key enzymes involved in the pathogenesis of common ailments.


Assuntos
Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Simulação de Acoplamento Molecular , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Salvia/química , Acetilcolinesterase , Antioxidantes/química , Antioxidantes/isolamento & purificação , Butirilcolinesterase , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Humanos , Ligantes , Monofenol Mono-Oxigenase , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Relação Estrutura-Atividade , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , alfa-Glucosidases
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...