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1.
Molecules ; 26(20)2021 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-34684810

RESUMO

This study investigated the in vitro inhibitory potential of different solvent extracts of leaves of Barbeya oleoides on key enzymes related to type 2 diabetes mellitus (α-glucosidase and α-amylase) in combination with an aggregation assay (using 0.01% Triton X-100 detergent) to assess the specificity of action. The methanol extract was the most active in inhibiting α-glucosidase and α-amylase, with IC50 values of 6.67 ± 0.30 and 25.62 ± 4.12 µg/mL, respectively. However, these activities were significantly attenuated in the presence of 0.01% Triton X-100. The chemical analysis of the methanol extract was conducted utilizing a dereplication approach combing LC-ESI-MS/MS and database searching. The chemical analysis detected 27 major peaks in the negative ion mode, and 24 phenolic compounds, predominantly tannins and flavonol glycosides derivatives, were tentatively identified. Our data indicate that the enzyme inhibitory activity was probably due to aggregation-based inhibition, perhaps linked to polyphenols.


Assuntos
Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Rosales/química , Metabolismo dos Carboidratos/efeitos dos fármacos , Diabetes Mellitus Tipo 2/tratamento farmacológico , Avaliação Pré-Clínica de Medicamentos , Inibidores Enzimáticos/isolamento & purificação , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Técnicas In Vitro , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Plantas Medicinais/química , Polifenóis/química , Polifenóis/isolamento & purificação , Polifenóis/farmacologia , Espectrometria de Massas por Ionização por Electrospray , Espectrometria de Massas em Tandem , alfa-Amilases/antagonistas & inibidores
2.
Molecules ; 26(19)2021 Sep 24.
Artigo em Inglês | MEDLINE | ID: mdl-34641343

RESUMO

(-)-Epigallocatechin gallate (EGCG), the chief dietary constituent in green tea (Camellia sinensis), is relatively unstable under oxidative conditions. This study evaluated the use of non-thermal dielectric barrier discharge (DBD) plasma to improve the anti-digestive enzyme capacities of EGCG oxidation products. Pure EGCG was dissolved in an aqueous solution and irradiated with DBD plasma for 20, 40, and 60 min. The reactant, irradiated for 60 min, exhibited improved inhibitory properties against α-glucosidase and α-amylase compared with the parent EGCG. The chemical structures of these oxidation products 1-3 from the EGCG, irradiated with the plasma for 60 min, were characterized using spectroscopic methods. Among the oxidation products, EGCG quinone dimer A (1) showed the most potent inhibitory effects toward α-glucosidase and α-amylase with IC50 values of 15.9 ± 0.3 and 18.7 ± 0.3 µM, respectively. These values were significantly higher than that of the positive control, acarbose. Compound 1, which was the most active, was the most abundant in the plasma-irradiated reactant for 60 min according to quantitative high-performance liquid chromatography analysis. These results suggest that the increased biological capacity of EGCG can be attributed to the structural changes to EGCG in H2O, induced by cold plasma irradiation.


Assuntos
Camellia sinensis/química , Catequina/análogos & derivados , Inibidores de Glicosídeo Hidrolases/química , Gases em Plasma/efeitos adversos , alfa-Amilases/antagonistas & inibidores , Animais , Catequina/química , Catequina/farmacologia , Inibidores de Glicosídeo Hidrolases/farmacologia , Estrutura Molecular , Oxirredução , Pâncreas/enzimologia , Folhas de Planta/química , Saccharomyces cerevisiae/enzimologia , Proteínas de Saccharomyces cerevisiae/antagonistas & inibidores , Suínos , Água/química , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo
3.
Molecules ; 26(17)2021 Aug 27.
Artigo em Inglês | MEDLINE | ID: mdl-34500647

RESUMO

Diabetes mellitus is a major health problem globally. The management of carbohydrate digestion provides an alternative treatment. Flavonoids constitute the largest group of polyphenolic compounds, produced by plants widely consumed as food and/or used for therapeutic purposes. As such, isoxazoles have attracted the attention of medicinal chemists by dint of their considerable bioactivity. Thus, the main goal of this work was to discover new hybrid molecules with properties of both flavonoids and isoxazoles in order to control carbohydrate digestion. Moreover, the trifluoromethyl group is a key entity in drug development, due to its strong lipophilicity and metabolic stability. Therefore, the present work describes the condensation of a previously synthesized trifluoromethylated flavonol with different aryl nitrile oxides, affording 13 hybrid molecules indicated as trifluoromethylated flavonoid-based isoxazoles. The structures of the obtained compounds were deduced from by 1H NMR, 13C NMR, and HRMS analysis. The 15 newly synthesized compounds inhibited the activity of α-amylase with an efficacy ranging from 64.5 ± 0.7% to 94.7 ± 1.2% at a concentration of 50 µM, and with IC50 values of 12.6 ± 0.2 µM-27.6 ± 1.1 µM. The most effective compounds in terms of efficacy and potency were 3b, 3h, 3j, and 3m. Among the new trifluoromethylated flavonoid-based isoxazoles, the compound 3b was the most effective inhibitor of α-amylase activity (PI = 94.7 ± 1.2% at 50 µM), with a potency (IC50 = 12.6 ± 0.2 µM) similar to that of the positive control acarbose (IC50 = 12.4 ± 0.1 µM). The study of the structure-activity relationship based on the molecular docking analysis showed a low binding energy, a correct mode of interaction in the active pocket of the target enzyme, and an ability to interact with the key residues of glycosidic cleavage (GLU-230 and ASP-206), explaining the inhibitory effects of α-amylase established by several derivatives.


Assuntos
Fármacos Antiobesidade/farmacologia , Diabetes Mellitus/tratamento farmacológico , Flavonoides/farmacologia , Hipoglicemiantes/farmacologia , Isoxazóis/farmacologia , alfa-Amilases/antagonistas & inibidores , Fármacos Antiobesidade/química , Diabetes Mellitus/metabolismo , Flavonoides/química , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Humanos , Hipoglicemiantes/química , Isoxazóis/química , Simulação de Acoplamento Molecular , Relação Estrutura-Atividade , alfa-Glucosidases/metabolismo
4.
Biomed Res Int ; 2021: 1585692, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34485509

RESUMO

In traditional medicine, various parts of the plant Juglans regia L. are used to treat several pathological conditions including diabetes and infectious and periodontal diseases. This includes the bark of Juglans regia. The present study is aimed at evaluating for the first time the mineral composition, investigating the antidiabetic and antibacterial properties of Moroccan J. regia bark, and finally determining the correlations between the chemical composition of the tested extracts and their biological activities. The mineral composition was determined using inductively coupled plasma atomic emission spectroscopy. Then, nine extracts were prepared by different methods and modalities of extractions and investigated for their antidiabetic activities, via tests of inhibition of alpha-amylase, alpha-glucosidase, and beta-galactosidase enzymes, and for their antibacterial activities against six strains involved in infectious diseases and periodontology. Finally, the correlation between the chemical compositions of the different extracts prepared and their antidiabetic and antibacterial potencies was determined by Principal Component Analysis (PCA). J. regia is an important source of mineral elements, mainly Fe (19849.8), K (3487.8), Mg (2631.03), and P (691.02) mg/kg plant material. All the extracts of J. regia possess antidiabetic activity, and in particular, the macerated acetone extract gave the highest inhibitory activity against alpha-amylase (IC50 value of 5445.33 ± 82.58 µg/mL), alpha-glucosidase (IC50 value of 323.7 ± 1.71 µg/mL), and beta-galactosidase (IC50 value of 811.2 ± 8.32 µg/mL). For the results of antibacterial activity, the macerated acetone extract at the concentration of 80 mg/mL was found to be the most active by inducing inhibition diameters of 12, 17, 18, 11, 14.5, and 16 mm against Escherichia coli, Proteus mirabilis, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis, and Listeria innocua, respectively. PCA allowed us to deduce that the extracts richer in polyphenols, in particular, the two acetone and ethanol macerates, have a better antidiabetic activity against alpha-glucosidase as well as a better antibacterial activity. The results of the present study revealed that the aqueous and organic macerate extracts showed a better antidiabetic activity and justified the use of J. regia bark as an antibacterial and antiseptic agent in traditional Moroccan medicine in the treatment of dental affections.


Assuntos
Juglans/química , Minerais/análise , Casca de Planta/química , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidores , alfa-Glucosidases/química , beta-Galactosidase/antagonistas & inibidores , Antibacterianos/farmacologia , Hipoglicemiantes/farmacologia , Técnicas In Vitro , alfa-Glucosidases/metabolismo
5.
Molecules ; 26(17)2021 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-34500753

RESUMO

Oxidative stress is one of the significant precursors of various metabolic diseases such as diabetes, Parkinson's disease, cardiovascular diseases, cancer, etc. Various scientific reports have indicated that secondary plant metabolites play an important role in preventing oxidative stress and its harmful effects. In this respect, this study was planned to investigate the phenolic profile and antioxidant and antidiabetic potentials of the aqueous extracts from Turkish Cistus species by employing in vitro methods. In vitro digestion simulation procedure was applied to all extracts to estimate the bioavailability of their phenolic contents. Total phenolic, flavonoid, phenolic acid and proanthocyanidin contents were determined for all phases of digestion. In addition, changes in the quantity of the assigned marker flavonoids (tiliroside, hyperoside and quercitrin) were monitored by High-Performance Thin Layer Chromatography (HPTLC) analysis. The antioxidant activity potentials of the extracts were studied by various methods to reveal their detailed activity profiles. On the other hand, in vitro α-amylase and α-glucosidase enzymes and advanced-glycation end product (AGE) inhibitory activities of the extracts were determined to evaluate the antidiabetic potentials of extracts. The results showed that aqueous extracts obtained from the aerial parts of Turkish Cistus species have rich phenolic contents and potential antioxidant and antidiabetic activities; however, their bioactivity profiles and marker flavonoid concentrations might significantly be affected by human digestion. The results exhibited that total phenolic contents, antioxidant activities and diabetes-related enzyme inhibitions of the bioavailable samples were lower than non-digested samples in all extracts.


Assuntos
Antioxidantes/farmacologia , Cistus/química , Diabetes Mellitus/tratamento farmacológico , Hipoglicemiantes/farmacologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Antioxidantes/química , Antioxidantes/metabolismo , Compostos de Bifenilo/antagonistas & inibidores , Cistus/metabolismo , Diabetes Mellitus/metabolismo , Relação Dose-Resposta a Droga , Produtos Finais de Glicação Avançada/antagonistas & inibidores , Produtos Finais de Glicação Avançada/metabolismo , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/metabolismo , Estrutura Molecular , Estresse Oxidativo/efeitos dos fármacos , Fenóis/química , Fenóis/metabolismo , Picratos/antagonistas & inibidores , Extratos Vegetais/química , Extratos Vegetais/metabolismo , Relação Estrutura-Atividade , Turquia , Água/química , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo
6.
Theor Appl Genet ; 134(10): 3427-3441, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34245321

RESUMO

KEY MESSAGE: Wheat cultivars largely differ in the content and composition of ATI proteins, but heritability was quite low for six out of eight ATIs. The genetic architecture of ATI proteins is built up of few major and numerous small effect QTL. Amylase trypsin inhibitors (ATIs) are important allergens in baker's asthma and suspected triggers of non-celiac wheat sensitivity (NCWS) inducing intestinal and extra-intestinal inflammation. As studies on the expression and genetic architecture of ATI proteins in wheat are lacking, we evaluated 149 European old and modern bread wheat cultivars grown at three different field locations for their content of eight ATI proteins. Large differences in the content and composition of ATIs in the different cultivars were identified ranging from 3.76 pmol for ATI CM2 to 80.4 pmol for ATI 0.19, with up to 2.5-fold variation in CM-type and up to sixfold variation in mono/dimeric ATIs. Generally, heritability estimates were low except for ATI 0.28 and ATI CM2. ATI protein content showed a low correlation with quality traits commonly analyzed in wheat breeding. Similarly, no trends were found regarding ATI content in wheat cultivars originating from numerous countries and decades of breeding history. Genome-wide association mapping revealed a complex genetic architecture built of many small, few medium and two major quantitative trait loci (QTL). The major QTL were located on chromosomes 3B for ATI 0.19-like and 6B for ATI 0.28, explaining 70.6 and 68.7% of the genotypic variance, respectively. Within close physical proximity to the medium and major QTL, we identified eight potential candidate genes on the wheat reference genome encoding structurally related lipid transfer proteins. Consequently, selection and breeding of wheat cultivars with low ATI protein amounts appear difficult requiring other strategies to reduce ATI content in wheat products.


Assuntos
Cromossomos de Plantas/genética , Fenótipo , Proteínas de Plantas/metabolismo , Locos de Características Quantitativas , Triticum/metabolismo , Inibidores da Tripsina/metabolismo , alfa-Amilases/antagonistas & inibidores , Regulação da Expressão Gênica de Plantas , Estudo de Associação Genômica Ampla , Melhoramento Vegetal , Proteínas de Plantas/genética
7.
Molecules ; 26(14)2021 Jul 09.
Artigo em Inglês | MEDLINE | ID: mdl-34299456

RESUMO

The inhibition of certain digestive enzymes by target food matrices represents a new approach in the treatment of socially significant diseases. Proving the ability of fruits to inhibit such enzymes can support the inclusion of specific varieties in the daily diets of patients with diabetes, obesity, Alzheimer's disease, etc., providing them with much more than just valuable micro- and macromolecules. The current study aimed atidentifying and comparing the GC-MS metabolic profiles of eight peach varieties ("Filina", "Ufo 4, "Gergana", "Laskava", "July Lady", "Flat Queen", "Evmolpiya", and "Morsiani 90") grown in Bulgaria (local and introduced) and to evaluate the inhibitory potential of their extracts towards α-glucosidase, α-amylase, lipase, and acetylcholinesterase. In order to confirm samples' differences or similarities, principal component analysis (PCA) and hierarchical cluster analysis (HCA) were also applied to the identified metabolites. The results provide important insights into the metabolomic profiles of the eight peach varieties and represent a first attempt to characterize the peels of the peach varieties with respect to α-glucosidase-, α-amylase-, lipase-, and acetylcholinesterase-inhibitory activities. All of the studied peach extracts displayed inhibitory activity towards α-glucosidase (IC50: 125-757 mg/mL) and acetylcholinesterase (IC50: 60-739 mg/mL), but none of them affected α-amylase activity. Five of the eight varieties showed inhibitory activity towards porcine pancreatic lipase (IC50: 24-167 mg/mL). The obtained results validate the usefulness of peaches and nectarines as valuable sources of natural agents beneficial for human health, although further detailed investigation should be performed in order to thoroughly identify the enzyme inhibitors responsible for each activity.


Assuntos
Extratos Vegetais/farmacologia , Prunus persica/metabolismo , Acetilcolinesterase/metabolismo , Amilases/metabolismo , Antioxidantes/farmacologia , Bulgária , Inibidores da Colinesterase/farmacologia , Inibidores Enzimáticos/farmacologia , Frutas/química , Frutas/metabolismo , Cromatografia Gasosa-Espectrometria de Massas/métodos , Inibidores de Glicosídeo Hidrolases/farmacologia , Lipase/antagonistas & inibidores , Lipase/metabolismo , Metaboloma , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Prunus persica/química , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo
8.
Molecules ; 26(14)2021 Jul 06.
Artigo em Inglês | MEDLINE | ID: mdl-34299396

RESUMO

In this study, two previously undescribed diterpenoids, (5R,10S,16R)-11,16,19-trihydroxy-12-O-ß-d-glucopyranosyl-(1→2)-ß-d-glucopyranosyl-17(15→16),18(4→3)-diabeo-3,8,11,13-abietatetraene-7-one (1) and (5R,10S,16R)-11,16-dihydroxy-12-O-ß-d-glucopyranosyl-(1→2)-ß-d-glucopyranosyl-17(15→16),18(4→3)-diabeo-4-carboxy-3,8,11,13-abietatetraene-7-one (2), and one known compound, the C13-nor-isoprenoid glycoside byzantionoside B (3), were isolated from the leaves of Clerodendrum infortunatum L. (Lamiaceae). Structures were established based on spectroscopic and spectrometric data and by comparison with literature data. The three terpenoids, along with five phenylpropanoids: 6'-O-caffeoyl-12-glucopyranosyloxyjasmonic acid (4), jionoside C (5), jionoside D (6), brachynoside (7), and incanoside C (8), previously isolated from the same source, were tested for their in vitro antidiabetic (α-amylase and α-glucosidase), anticancer (Hs578T and MDA-MB-231), and anticholinesterase activities. In an in vitro test against carbohydrate digestion enzymes, compound 6 showed the most potent effect against mammalian α-amylase (IC50 3.4 ± 0.2 µM) compared to the reference standard acarbose (IC50 5.9 ± 0.1 µM). As yeast α-glucosidase inhibitors, compounds 1, 2, 5, and 6 displayed moderate inhibitory activities, ranging from 24.6 to 96.0 µM, compared to acarbose (IC50 665 ± 42 µM). All of the tested compounds demonstrated negligible anticholinesterase effects. In an anticancer test, compounds 3 and 5 exhibited moderate antiproliferative properties with IC50 of 94.7 ± 1.3 and 85.3 ± 2.4 µM, respectively, against Hs578T cell, while the rest of the compounds did not show significant activity (IC50 > 100 µM).


Assuntos
Abietanos/química , Antineoplásicos/farmacologia , Inibidores da Colinesterase/farmacologia , Clerodendrum/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Glicosídeos/farmacologia , Folhas de Planta/química , Humanos , Neoplasias/tratamento farmacológico , Células Tumorais Cultivadas , alfa-Amilases/antagonistas & inibidores
9.
Molecules ; 26(14)2021 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-34299476

RESUMO

In this study, the health-promoting benefits of different fruits grown in Madeira Island, namely lemon (Citrus limon var. eureka), tangerine (Citrus reticulata var. setubalense), pitanga (Eugenia uniflora var. red), tomato (Solanum lycopersicum var. gordal) and uva-da-serra, an endemic blueberry (Vaccinium padifolium Sm.), were investigated. The phenolic composition (total phenolics and total flavonoids content) and antioxidant capacity (assessed through ABTS and DPPH assays) were measured revealing a high phenolic potential for all fruits, except tomato, while uva-da-serra is particularly rich in flavonoids. In relation to the antioxidant capacity, the highest values were obtained for pitanga and uva-da-serra extracts. The bioactive potential was also assessed through the ability of the extracts to inhibit digestive enzymes linked to diabetes (α-amylase, α- and ß-glucosidases) and hypertension (angiotensin-converting enzyme, ACE). The results obtained point to a very high bioactive potential with the selected samples exhibiting very important ACE anti-enzymatic capacities. A statistical analysis of the obtained data reveals a very strong correlation between ABTS and TPC, and a strong contribution of the fruit polyphenols for enzyme inhibition, and thus, presenting high antihypertensive and antidiabetic capacities. Overall, the results obtained clearly show a high bioactive potential of the selected fruits that should be further studied, in terms of specific phenolic composition. Moreover, these results strongly support the valorisation of pitanga seeds usually discarded as a waste, and uva-da-serra, an endemic and wild bush, as potential bioresources of bioactive compounds with impact in human diet.


Assuntos
Antioxidantes/farmacologia , Inibidores da Colinesterase/farmacologia , Flavonoides/farmacologia , Frutas/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidores , Humanos
10.
Molecules ; 26(9)2021 May 04.
Artigo em Inglês | MEDLINE | ID: mdl-34064448

RESUMO

The 2-amino-5-(3/4-fluorostyryl)acetophenones were prepared and reacted with benzaldehyde derivatives to afford the corresponding 5-styryl-2-aminochalcone hybrids. The trans geometry of the styryl and α,ß-unsaturated carbonyl arms, and the presence of NH…O intramolecular hydrogen bond were validated using 1H-NMR and X-ray data. The 2-amino-5-styrylacetophenones and their 5-styryl-2-aminochalcone derivatives were screened in vitro for their capability to inhibit α-glucosidase and/or α-amylase activities. Their antioxidant properties were evaluated in vitro through the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide (NO) free radical scavenging assays. Kinetic studies of the most active derivatives from each series against α-glucosidase and/or α-amylase activities have been performed supported by molecular docking studies to determine plausible protein-ligand interactions on a molecular level. The key aspects of the pharmacokinetics of these compounds, i.e., absorption, distribution, metabolism, and excretion have also been simulated at theoretical level. The most active compounds from each series, namely, 2a and 3e, were evaluated for cytotoxicity against the normal monkey kidney cells (Vero cells) and the adenocarcinomic human epithelial (A549) cell line to establish their safety profile at least in vitro.


Assuntos
Antioxidantes/farmacologia , Carboidratos/química , Chalconas/síntese química , Chalconas/farmacologia , Simulação por Computador , Inibidores Enzimáticos/farmacologia , Receptores de Droga/química , Células A549 , Animais , Morte Celular/efeitos dos fármacos , Chalconas/química , Chalconas/farmacocinética , Chlorocebus aethiops , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Humanos , Cinética , Conformação Molecular , Simulação de Acoplamento Molecular , Termodinâmica , Células Vero , alfa-Amilases/antagonistas & inibidores , alfa-Glucosidases/metabolismo
11.
Food Chem ; 361: 130144, 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34082387

RESUMO

Effect of high-intensity ultrasound (HIU) compared with thermal treatments on baobab fruit pulp (BFP) quality and bioactive properties were investigated. HIU treatments, particularly at intensities of 687.5 W/cm2 for 5 min, and 344 W/cm2 for 15 min significantly (p < 0.05) increased the cloudiness index, ascorbic acid (AA) retention, total phenolic and flavonoid contents, and antioxidant capacity besides a more potent α-amylase and α-glucosidase inhibition relative to thermally treated samples. Moreover, the physicochemical parameters, colour index, and browning index were maintained with HIU besides lower 5-hydroxymethylfurfural values than thermal processing. HPLC analysis revealed that the content of most phenolic compounds was the highest in HIU treatments besides a 235-256% increase in procyanidin C1 compared with control samples. The AA retention following HIU treatments was 87.62-102.86% compared to 30.47-61.90% in thermally treated samples. Our analyses portrayed ultrasound as a feasible alternative to conventional thermal processing of BFP.


Assuntos
Adansonia/química , Inibidores Enzimáticos/farmacologia , Frutas/química , Ultrassom/métodos , alfa-Amilases/antagonistas & inibidores , Antioxidantes/análise , Antioxidantes/química , Ácido Ascórbico/análise , Biflavonoides/análise , Catequina/análise , Inibidores Enzimáticos/análise , Inibidores Enzimáticos/química , Flavonoides/análise , Inibidores de Glicosídeo Hidrolases/análise , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Fenóis/análise , Proantocianidinas/análise , alfa-Glucosidases/metabolismo
12.
Molecules ; 26(11)2021 May 24.
Artigo em Inglês | MEDLINE | ID: mdl-34073905

RESUMO

Medicinal plants offer imperative sources of innovative chemical substances with important potential therapeutic effects. Among them, the members of the genus Inula have been widely used in traditional medicine for the treatment of several diseases. The present study investigated the antioxidant (DPPH, ABTS and FRAP assays) and the in vitro anti-hyperglycemic potential of aerial parts of Inula viscosa (L.) Aiton (I. viscosa) extracts through the inhibition of digestive enzymes (α-amylase and α-glucosidase), responsible of the digestion of poly and oligosaccharides. The polyphenolic profile of the Inula viscosa (L.) Aiton EtOAc extract was also investigated using HPLC-DAD/ESI-MS analysis, whereas the volatile composition was elucidated by GC-MS. The chemical analysis resulted in the detection of twenty-one polyphenolic compounds, whereas the volatile profile highlighted the occurrence of forty-eight different compounds. Inula viscosa (L.) Aiton presented values as high as 87.2 ± 0.50 mg GAE/g and 78.6 ± 0.55mg CE/g, for gallic acid and catechin, respectively. The EtOAc extract exhibited the higher antioxidant activity compared to methanol and chloroform extracts in different tests with (IC50 = 0.6 ± 0.03 µg/mL; IC50 = 8.6 ± 0.08 µg/mL; 634.8 mg ± 1.45 AAE/g extract) in DPPH, ABTS and FRAP tests. Moreover, Inula viscosa (L.) Aiton leaves did show an important inhibitory effect against α-amylase and α-glucosidase. On the basis of the results achieved, such a species represents a promising traditional medicine, thanks to its remarkable content of functional bioactive compounds, thus opening new prospects for research and innovative phytopharmaceuticals developments.


Assuntos
Antioxidantes/química , Inula/química , Compostos Fitoquímicos/química , Folhas de Planta/química , alfa-Amilases/antagonistas & inibidores , alfa-Glucosidases/efeitos dos fármacos
13.
Int J Biol Macromol ; 184: 289-296, 2021 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-34119546

RESUMO

Inhibiting the activity of the intestinal enzyme α-amylase that catalyzes the degradation of starch into glucose can control blood glucose and provide an essential way for the treatment of Type-II diabetes mellitus (T2DM). Here, we compared the structural information of chondroitin sulfate (CS) from different origins and the effects on activity of α-amylase and blood glucose have been investigated. The inhibitory effects of shark and porcine CSs against α-amylase activity is obvious with IC50 values of 11.97 and 14.42 mg/ml, respectively, but the bovine CS almost no effect. From the data of fluorescence spectroscopic analyses, CSs from shark and pig quench Try fluorescence intensity of the enzyme, whereas bovine CS induces an increase. In vivo, oral administration of shark and porcine CSs efficiently suppresses postprandial blood glucose levels in normal and diabetic mice. Our study found that CSs from different sources showed different biological functions even if both molecular weight and disaccharide subunit composition are almost the same, and demonstrated that the CSs from shark and pig as α-amylase inhibitors could be regarded as a novel functional food ingredient in T2DM management.


Assuntos
Sulfatos de Condroitina/administração & dosagem , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/administração & dosagem , alfa-Amilases/antagonistas & inibidores , Administração Oral , Animais , Glicemia/efeitos dos fármacos , Bovinos , Sulfatos de Condroitina/química , Sulfatos de Condroitina/farmacologia , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/enzimologia , Diabetes Mellitus Tipo 2/sangue , Diabetes Mellitus Tipo 2/induzido quimicamente , Diabetes Mellitus Tipo 2/enzimologia , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Concentração Inibidora 50 , Masculino , Camundongos , Tubarões , Especificidade da Espécie , Estreptozocina , Suínos , Resultado do Tratamento
14.
Int J Biol Macromol ; 184: 380-392, 2021 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-34126149

RESUMO

Russula virescens is an edible wild mushroom that is widely distributed in south of China. This research aimed to analyze the structure characterization and evaluate the hypoglycemic, anticancer and immunological activities of two water soluble polysaccharides RVP-1 and RVP-2 from R. virescens. The results showed RVP-1 and RVP-2 were non-triple helix structured hetero-polysaccharides with different weight-average molecular weight 14,883 and 13,301 Da, respectively. Both RVP-1 and RVP-2 were composed of galactose, glucose, mannose and fructose, and the sugar residues were mainly linked by 1,6→, 1,2→, 1→ and 1,3,6→ glycosidic bonds. Moreover, the antidiabetic, anticancer and immune activities of RVP-1 and RVP-2 were explored in vitro methods. The two polysaccharides have potential for inhibiting α-glucosidase and α-amylase activities, suppressing HepG-2, A549 and MCF-7 cancer cells proliferation, and activating macrophage RAW 264.7 cells to secret immune cytokines for mediating cellular immune response. These findings provided a scientific basis for further utilization of polysaccharide from R. virescens.


Assuntos
Antineoplásicos/química , Antioxidantes/química , Basidiomycota/química , Citocinas/metabolismo , Polissacarídeos Fúngicos/química , Hipoglicemiantes/química , Células A549 , Animais , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Sequência de Carboidratos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Polissacarídeos Fúngicos/farmacologia , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Células Hep G2 , Humanos , Hipoglicemiantes/farmacologia , Células MCF-7 , Camundongos , Peso Molecular , Células RAW 264.7 , alfa-Amilases/antagonistas & inibidores
15.
Food Chem ; 359: 129889, 2021 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-33934030

RESUMO

The objective was to analyze the phenolic composition, antioxidant capacity, and physical characteristics of 10 blackcurrant cultivars, their juices, and the enzymatic inhibition of dipeptidyl peptidase-IV, α-amylase, α-glucosidase, nitric oxide synthase, and cyclooxygenase-2. Fruit masses ranged from 0.47 to 1.22 g and diameters from 7.42 to 14.42 mm. For the juices, pH ranged from 2.80 to 2.96, soluble solids from 11.33% to 17.5%, total acidity from 3.17 to 4.26 g/100 mL, and viscosity from 1.28 to 273.83 mPa·s. Total anthocyanins (TA) ranged from 1.81 to 5.48 mg eq cyanidin 3-O-glucoside/100 g, total polyphenols (TP) from 7.67 to 39.70 mg eq gallic acid/100 g, total condensed tannins from 3.24 to 7.76 g eq catechin/100 g, and antioxidant capacity from 219.24 to 499.26 µmol eq Trolox/100 g. Juices of the cultivars Coronet and Consort contained the highest levels of TA, TP, and antioxidants. Whistler cultivar contained high concentrations of major anthocyanins. Juices from all cultivars favorably inhibited the activities of enzymes used as surrogate biochemical markers for T2 diabetes and inflammation.


Assuntos
Antocianinas/análise , Antioxidantes/análise , Extratos Vegetais/farmacologia , Polifenóis/análise , Proantocianidinas/análise , Ribes/química , Antocianinas/farmacologia , Inibidores de Ciclo-Oxigenase 2/análise , Inibidores da Dipeptidil Peptidase IV/análise , Frutas/química , Sucos de Frutas e Vegetais/análise , Inibidores de Glicosídeo Hidrolases/análise , Óxido Nítrico Sintase/antagonistas & inibidores , Fenóis/análise , Extratos Vegetais/química , Polifenóis/farmacologia , Proantocianidinas/farmacologia , alfa-Amilases/antagonistas & inibidores
16.
Food Chem ; 359: 129934, 2021 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-33940476

RESUMO

This study aimed to evaluate inhibitory activity of anthocyanins from purple sweet potato and blueberries against α-amylase and α-glucosidase, as well as investigate the inhibition mechanism of diacylated anthocyanins (Diacylated AF-PSP). Diacylated AF-PSP better inhibited α-amylase (IC50 = 0.078 mg mL-1) and α-glucosidase (IC50 = 1.56 mg mL-1) than other anthocyanin fractions, which was a mixed-type inhibitor. Fluorescence analysis indicated that Diacylated AF-PSP bound to the enzymes mainly through hydrogen bonds and influenced the microenvironments of proteins. Additionally, surface hydrophobicity and circular dichroism spectra results confirmed conformational changes in the enzymes induced by Diacylated AF-PSP. Molecular docking further demonstrated the interaction of Diacylated AF-PSP with enzyme active site, which might be stabilized by its acyl groups. Finally, 160 mg kg-1 Diacylated AF-PSP significantly decreased (p < 0.01) blood glucose level peak by 20.52% after starch administration in SD rats. This study provided theoretical evidences for utilization of diacylated anthocyanins in hyperglycemia-management functional foods.


Assuntos
Antocianinas/farmacologia , Inibidores Enzimáticos/farmacologia , Ipomoea batatas/química , alfa-Amilases/antagonistas & inibidores , alfa-Glucosidases/efeitos dos fármacos , Animais , Masculino , Simulação de Acoplamento Molecular , Ratos , Ratos Sprague-Dawley , Amido/metabolismo
17.
J Biosci Bioeng ; 132(1): 9-17, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-33934979

RESUMO

Rice is a source of bioactive compounds related to human health and has been used for both consumption and traditional medicine. The authors investigated the synergistic and additive effect of rice extract (RE) combined with five aromatic compounds against three enzymes: α-glucosidase, α-amylase and tyrosinase. RE was purified by thin-layer chromatography (TLC) and preparative TLC (PTLC) with different solvent systems. RE had higher α-glucosidase and α-amylase inhibitory activity than the five aromatic compounds, while the five aromatic compounds had higher tyrosinase inhibitory activity than RE. The combination of RE/acarbose produced synergic inhibition of α-glucosidase and α-amylase, whereas RE showed additive inhibition of both enzymes when combined with aromatic compounds. The five aromatic compounds showed additive inhibition of tyrosinase when combined with RE. The combination of 2-methoxy-4-vinylphenol/vanillin/guaiacol produced synergistic inhibition of α-amylase while showing antagonism of α-glucosidase and tyrosinase. Interestingly, the RE produced additive inhibition of α-glucosidase, α-amylase and tyrosinase when combined with the 2-methoxy-4-vinylphenol/vanillin/guaiacol combination. RE had rich bioactive compounds related to α-glucosidase, α-amylase and tyrosinase inhibitory activity. Volatile compounds, including 2-methoxy-4-vinylphenol, vanillin and guaiacol, enhanced the inhibitory activity of RE against α-glucosidase, α-amylase and tyrosinase activities.


Assuntos
Inibidores de Glicosídeo Hidrolases/farmacologia , Hidrocarbonetos Aromáticos/farmacologia , Monofenol Mono-Oxigenase/antagonistas & inibidores , Oryza/química , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidores , alfa-Glucosidases/metabolismo , Interações Medicamentosas , Humanos
18.
Biomed Res Int ; 2021: 6652777, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33987444

RESUMO

Background: The leaves of Hagenia abyssinica have been used in the management of diabetes mellitus in Ethiopian folk medicine. Thus, this study is aimed at investigating the in vitro α-amylase and α-glucosidase inhibitory and antioxidant activities of the crude extract and solvent fractions of H. abyssinica leaves. Methods: The in vitro α-amylase and α-glucosidase inhibitory and antioxidant activities of the plant extract were assessed using 3,5-dinitrosalicylic acid (DNSA), p-nitro-phenyl-a-D glucopyranoside (p-NPG), and 1,1-diphenyl-2-picrylhydrazyl (DPPH) assays, respectively. Each value of percent inhibition of α-amylase, α-glucosidase, and DPPH scavenging effect was presented as means ± SEM (n = 3). Results: The α-amylase inhibitory activity of the crude extract and solvent fractions was found to be concentration-dependent. The strongest activity was exhibited by the crude extract at the highest concentration with a percentage inhibition of 74.52% (IC50, 14.52 µg/ml) followed by water fraction 68.24% (IC50, 16.31 µg/ml), ethyl acetate fraction 61.57% (IC50, 18.73 µg/ml), and chloroform fraction 56.87% (IC50, 21.57 µg/ml) of H. abyssinica leaves. In the α-glucosidase inhibition assay, the maximum activity was exhibited by the aqueous fraction 62.54% (IC50, 11.67 µg/ml) followed by ethyl acetate fraction 54.97% (IC50, 15.89 µg/ml), crude extract 46.79% (IC50, >16.5 µg/ml), and chloroform fraction 36.44% (IC50, >16.5 µg/ml). In the antioxidant assay, the crude extract exhibited the highest antioxidant activity 86.36% (IC50, 10.25 µg/ml) followed by water fraction 78.59% (IC50, 13.86 µg/ml), ethyl acetate fraction 71.58% (IC50, 16.34 µg/ml), and chloroform fraction 63.65% (IC50, 18.83 µg/ml). Conclusion: This study has revealed that H. abyssinica leaves possess noticeable in vitro α-amylase and α-glucosidase inhibitory and antioxidant activities.


Assuntos
Antioxidantes/farmacologia , Inibidores de Glicosídeo Hidrolases/farmacologia , Extratos Vegetais , Rosaceae/química , alfa-Amilases/antagonistas & inibidores , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Solventes/química , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo
19.
J Chromatogr A ; 1647: 462153, 2021 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-33957349

RESUMO

Pittosporum angustifolium, known as gumbi gumbi, is a native Australian plant, which has traditionally been used as an Aboriginal medicine. This study investigates the effect of different solvents and extractive fermentation on the content and natural products composition of Pittosporum angustifolium extracts, and compares their antioxidant activity, in vitro α-amylase inhibition, and anti-inflammatory properties. Anti-inflammatory activity of the extracts was determined by measuring the inhibition of nitric oxide (NO) production. Extracts were characterised with FTIR-ATR spectroscopy, and screened for antioxidant activities and α-amylase inhibitory activity via High-performance thin-layer chromatography (HPTLC)-Effect-directed analysis (EDA) with direct bioautography. HPTLC combined with chemical derivatization and bioassays was used for EDA screening. The results show that lactic acid fermentation of gumbi gumbi leaves boosts the antioxidant activity in extracts by increasing the total phenolic content, but does not affect (increase or decrease) α-amylase inhibitory activity or nitrogen scavenging/anti-inflammatory activity. Analysis of the ATR-FTIR spectra from the band at RF = 0.85 that inhibits α-amylase, suggests that fatty acid esters are responsible for the enzyme inhibition; both saturated fatty acid esters in unfermented extracts and unsaturated fatty acid esters in fermented extracts. The ATR-FTIR spectra of the polyphenolics in fermented extracts (RF = 0.15-0.20) suggests the presence of soluble lignin fragments (i.e. lignins depolymerized into monomers and oligomers during the fermentation process).


Assuntos
Antioxidantes/análise , Extratos Vegetais/análise , Rosales/química , Antioxidantes/química , Antioxidantes/farmacologia , Bioensaio , Cromatografia Líquida de Alta Pressão , Cromatografia em Camada Delgada , Fermentação , Extratos Vegetais/química , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidores
20.
Food Chem ; 358: 129812, 2021 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-33940289

RESUMO

Prunus fruits are recognized to be rich sources of polyphenols with health promoting effect. In this work we evaluated the phenolic profile and bioactivity, namely antioxidant capacity, antiproliferative effect in HT29, and inhibition capacity of α-glucosidase (α-Gls), α-amylase (α-Amy) and human dipeptidyl peptidase III (hDPP III) activities, of traditional Prunus fruits grown in Serbia. Fifteen Prunus samples were investigated and compared: common European plum and three old plum subspecies ('vlaskaca', damson plum and white damson), purple-leaf cherry plum, red and white cherry plum, sweet cherry, sweet cherry-wild type, sour cherry, steppe cherry, mahaleb cherry, blackthorn, peach, and apricot. Principal Component Analysis highlighted steppe cherry and blackthorn as Prunus species with the highest bioactive potential. In silico analysis pointed out rutinoside derivatives of cyanidin and quercetin as the most potent inhibitors of α-Gls, α-Amy and hDPP III enzymes. Quercetin 3-O-rutinoside showed the highest binding energy to α-Gls (-10.6 kcal/mol).


Assuntos
Antioxidantes/análise , Frutas/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Polifenóis/análise , Prunus/química , Antocianinas/análise , Antocianinas/farmacologia , Antioxidantes/farmacologia , Proliferação de Células/efeitos dos fármacos , Simulação por Computador , Avaliação Pré-Clínica de Medicamentos/métodos , Glucosídeos/metabolismo , Glucosídeos/farmacologia , Inibidores de Glicosídeo Hidrolases/química , Células HT29 , Humanos , Simulação de Acoplamento Molecular , Fenóis/análise , Polifenóis/farmacologia , Quercetina/análogos & derivados , Quercetina/metabolismo , Quercetina/farmacologia , alfa-Amilases/antagonistas & inibidores
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