Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 1.358
Filtrar
1.
Food Chem ; 334: 127565, 2021 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-32717686

RESUMO

The chemical composition, antioxidant activity (AA), cytotoxic activity, antihemolytic effects, and enzyme inhibition (EI) of lyophilized jabuticaba (Myrciaria jaboticaba) seed extract (LJE) was studied. The main compounds found were castalagin, vescalagin, procyanidin A2, and ellagic acid. LJE was more toxic to cancer cells than to normal cells, meaning relative toxicological safety. This cytotoxic effect can be attributed to the pro-oxidant effect observed in the reactive oxygen species (ROS) generation assay. LJE inhibited α-amylase, α-glucosidase, and ACE-I activities and protected human erythrocytes from hemolysis. LJE was incorporated into yogurts at different concentrations and the total phenolic content, AA, and EI increased in a dose-dependent manner. LJE-containing yogurt presented 86% sensory acceptance. The yogurt was administered to Wistar rats bearing cancer and it modulated the gut bacterial microbiota, having a prebiotic effect. LJE is a potential functional ingredient for food companies looking for TPC, AA, and prebiotic effect in vivo.


Assuntos
Neoplasias do Colo/tratamento farmacológico , Microbioma Gastrointestinal/efeitos dos fármacos , Myrtaceae/química , Polifenóis/farmacologia , Iogurte , 1,2-Dimetilidrazina/toxicidade , Inibidores da Enzima Conversora de Angiotensina/química , Inibidores da Enzima Conversora de Angiotensina/farmacologia , Animais , Antioxidantes/química , Antioxidantes/farmacologia , Catequina/análise , Catequina/farmacologia , Neoplasias do Colo/induzido quimicamente , Neoplasias do Colo/microbiologia , Humanos , Taninos Hidrolisáveis/análise , Taninos Hidrolisáveis/farmacologia , Masculino , Fenóis/análise , Extratos Vegetais/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polifenóis/análise , Proantocianidinas/análise , Proantocianidinas/farmacologia , Ratos Wistar , Sementes/química , alfa-Amilases/antagonistas & inibidores
2.
Food Chem ; 335: 127505, 2021 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-32739823

RESUMO

Dysregulation of glucose homeostasis result in hyperglycemia and pigmented rice, unique combination of high quality starch and phenolics has the potential in regulating it. In this study, pigmented rice was characterized in terms of nutraceutical starch (NS) and phenolic content. Further the effect of rice phenolics on carbolytic enzyme inhibition, glucose uptake, hepatic glucose homeostasis and anti-glycation ability was analyzed in vitro. The most relevant effect on enzyme inhibition (α-amylase: IC50-42.34 µg/mL; α-glucosidase: IC50:63.89 µg/mL), basal uptake of glucose (>39.5%) and anti-glycation ability (92%) was found in red rice (RR), than black rice (BR). The role of RR phenolics in regulating glucose homeostasis was deciphered using hepatic cell line system, which found up-regulation of glucose transporter 2 (GLUT2) and glycogen synthase 2 (GYS2); while expression of gluconeogenic genes were found down regulated. To our knowledge this study is the first report validating the role of starch-phenolic quality towards anti-hyperglycemic effect of RR.


Assuntos
Glucose/metabolismo , Homeostase , Hiperglicemia/metabolismo , Fígado/metabolismo , Oryza/química , Proantocianidinas/análise , Amido/análise , Transporte Biológico/efeitos dos fármacos , Suplementos Nutricionais/análise , Inibidores de Glicosídeo Hidrolases/farmacologia , Homeostase/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fenol/análise , Fenol/farmacologia , alfa-Amilases/antagonistas & inibidores
3.
J Food Sci ; 85(7): 2177-2185, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-32672871

RESUMO

Phenolic profiles, antioxidant, antiproliferative, and hypoglycemic activities of the whole Ehretia macrophylla Wall. (EMW) fruit were investigated in the present study. Catechin (CE), o-methoxy benzoic acid (o-MBA), and rosmarinic acid (RA) were the predominant phenolics in free extract, while CE, vanillic acid (VA), and o-MBA were for bound extract. These extracts exhibited potential antioxidant capacity measured by peroxyl radical scavenging capacity (PSC), oxygen radical absorbance capacity (ORAC), and cellular antioxidant activity (CAA) assays. This fruit also possessed dose-dependently antiproliferative activity, and this may be due to the synergistic and additive effects of individual phenolics. Furthermore, EMW fruit showed favorable hypoglycemic activity via inhibition of activities of α-glucosidase and α-amylase, enhancement of glucose consumption, glycogen accumulation, and glycogen synthase 2 (GYS2) activity, and downregulation of activities of glucose-6-phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK). Therefore, EMW fruit has the potential as an ingredient of functional foods to improve human health and shows promising applications with additional health and economical benefits. PRACTICAL APPLICATION: EMW fruit is a plant-based food rich in natural phenolic compounds, which suggesting its potential bioactivities for humans such as antioxidant, antiproliferative, and hypoglycemic activities. Our findings would provide a logical strategy to promote the comprehensive utilization of phenolics in EMW fruit with both health and economical benefits.


Assuntos
Antioxidantes/química , Boraginaceae/química , Hipoglicemiantes/química , Fenóis/química , Extratos Vegetais/química , Antioxidantes/farmacologia , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Frutas/química , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Humanos , Hipoglicemiantes/farmacologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/química , alfa-Glucosidases/química
4.
Food Chem ; 333: 127418, 2020 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-32653680

RESUMO

Fermented camel milk possesses a weak (liquid-like) gel structure. We aimed to 1) investigate the characteristics, bioactivities and rheological properties of the exopolysaccharide (EPS) produced by Lactococcus garvieae-C47 (exopolysaccharide-C47 product), a potential probiotic bacterium, on milk extracted from camels and 2) examine the rheological properties of the fermented camel milk produced by L. garvieae-C47. Exopolysaccharide-C47 product (molecular weight: 7.3 × 106 Da) was composed of the following monosaccharides: glucose (82.51%), arabinose (5.32%) and xylose (12.17%). The antioxidant, antitumor and α-amylase inhibitory activities of exopolysaccharide-C47 product reached up to 67.52, 59.35 and 91.0%, respectively. The apparent viscosity of exopolysaccharide-C47 product decreased with the increase in shear rate and declined by increasing the temperature up to 50 °C. The rheological properties of exopolysaccharide-C47 product are influenced by the salt type and pH value. The exopolysaccharide product produced by L. garvieae C47 possesses valuable health benefits and has the ability to improve the weak structure of fermented camel milk.


Assuntos
Fermentação , Lactococcus/metabolismo , Leite/microbiologia , Polissacarídeos Bacterianos/química , Polissacarídeos Bacterianos/farmacologia , Probióticos/metabolismo , Reologia , Animais , Antineoplásicos/química , Antineoplásicos/metabolismo , Antineoplásicos/farmacologia , Antioxidantes/química , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Camelus , Inibidores Enzimáticos/química , Inibidores Enzimáticos/metabolismo , Inibidores Enzimáticos/farmacologia , Humanos , Peso Molecular , Polissacarídeos Bacterianos/biossíntese , Viscosidade , alfa-Amilases/antagonistas & inibidores
5.
Food Chem ; 328: 126930, 2020 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-32485581

RESUMO

The objective of this study was to quantify the phenolic compounds and to evaluate and compare the biological activities of the ethyl acetate (EtOAc), methanolic (MeOH) and aqueous extracts from the Micromeria nervosa aerial parts, based on their antioxidant activity and enzymatic inhibition. Total phenolic and flavonoid contents were calculated and individual compo3unds were detected using LC-ESI-MS/MS. The antioxidant activity was determined using six different assays while enzymatic activity was determined by α-amylase and tyrosinase enzyme inhibition. The main phenolic constituents detected in the extracts were rosmarinic acid. In the antioxidant assays the aqueous extract was shown to be more efficient than the others. The EtOAc and MeOH extracts presented higher inhibitory activity with respect to α-amylase and tyrosinase. Regardless of the solvent, the results suggest M. nervosa aerial extracts present a biological potential due to their antioxidant activity and enzymatic inhibition.


Assuntos
Antioxidantes/química , Inibidores Enzimáticos/análise , Lamiaceae/química , Fenóis/análise , Extratos Vegetais/química , Espectrometria de Massas em Tandem , Cromatografia Líquida de Alta Pressão , Cinamatos/análise , Depsídeos/análise , Flavonoides/análise , Lamiaceae/metabolismo , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Componentes Aéreos da Planta/química , Componentes Aéreos da Planta/metabolismo , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo
6.
Food Chem ; 331: 127240, 2020 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-32585546

RESUMO

The present study focused on the phytochemical profiling along with evaluation of in vitro antioxidant, α-glucosidase and α-amylase inhibitory activities of various crudes and fractions obtained from Lepisanthes fruticosa (Roxb) Leenh fruit. Ethanolic seed crude extract exhibited the strongest radical scavenging, ß-carotene bleaching activity, α-glucosidase inhibition and the highest total phenolic content (TPC). Column chromatography afforded various fractions with fraction M4 being the most potent due to the strongest radical scavenging, ß-carotene bleaching, α-glucosidase inhibition and greatest amount of TPC. Liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis of ethanolic seed crude extract and fraction M4 showed the presence of various phytochemicals with antioxidant and antidiabetic properties, which include mostly flavonoids and tannins. The results may suggest that the ethanolic crude seed extract and its fraction could be an excellent source of bioactive phytochemicals with antioxidant and antidiabetic potential.


Assuntos
Antioxidantes/química , Inibidores Enzimáticos/análise , Fenóis/análise , Extratos Vegetais/química , Sapindaceae/química , Cromatografia Líquida de Alta Pressão , Inibidores Enzimáticos/química , Flavonoides/análise , Flavonoides/química , Frutas/química , Frutas/metabolismo , Fenóis/química , Sapindaceae/metabolismo , Espectrometria de Massas em Tandem , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , alfa-Glucosidases/química , alfa-Glucosidases/metabolismo
7.
Diabetes Metab Syndr ; 14(4): 689-694, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32442919

RESUMO

BACKGROUND: The inhibition of α-amylase and α-glucosidase activities is one of the major practical strategies for the control of postprandial hyperglycemia. Salvia officinalis L. is known by its various bioactive compounds and its effective therapeutic properties towards illnesses including diabetes. OBJECTIVE: The present study aimed to evaluate the in vitro inhibitory effect of S. officinalis on key digestive enzymes linked to type 2 diabetes and to identify its hemolytic effect. METHODS: Hydro-methanol decoction extract and fractions of ethyl acetate and n-butanol were investigated for their in vitro α-amylase and α-glucosidase inhibitory activities, compared to acarbose as a standard. Furthermore, they were evaluated for their hemolytic effect. RESULTS: Phytochemical composition demonstrated the richness of S. officinalis in secondary metabolites. Extract and fractions inhibited the activity of both enzymes. They showed weak hemolytic activity. Quantitative estimation of total phenolic and flavonoids revealed that ethyl acetate fraction contained the highest amount of these compounds (450.51 ± 0.6 µg GAE/mg DE and 352.01 ± 0.78 µg CE/mg of DE, respectively). It showed the best antidiabetic activity tested both by α-amylase and α-glucosidase assays (IC50 = 46.52 ± 2.68 and 104.58 ± 0.06 µg/mL, respectively). Moreover, this fraction showed the least hemolytic effect (11.58 ± 0.1%). CONCLUSIONS: S. officinalis extract and fractions are promising sources of α-amylase and α-glucosidase inhibitors.


Assuntos
Inibidores de Glicosídeo Hidrolases/análise , Hipoglicemiantes/análise , Salvia officinalis/química , alfa-Amilases/antagonistas & inibidores , Flavonoides/análise , Hemólise/efeitos dos fármacos , Fenóis/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia
8.
Food Chem ; 326: 126962, 2020 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-32413753

RESUMO

A concise method of natural blue pigment from Vaccinium bracteatum thunb. leaves (VBTL) was proposed firstly in this research. The potential properties of new pigment source needed to be assessed for further application. During the shelf life and thermal-accelerated storage, the blue pigment was prone to stable in the mildly acidic system, which was observed retention of 35.85% for storage of 12 weeks in pH 4.0. The 65% of blue pigment retained after the in vitro simulated digestion. The blue pigment exhibited inhibition effect on the pancreatic α-amylase (IC50 = 2.915 mg/mL). The analysis of inhibition kinetics indicated the blue pigment was an uncompetitive inhibitor. Through fluorescence quenching and circular dichroism study, the blue pigment inhibited α-amylase activity via the structural unfolding of α-amylase molecule and changing the secondary structure. These findings provided the new evidence of the digestion resistibility of VBTL pigment and the functional food - "Wu mi".


Assuntos
Inibidores Enzimáticos/química , Pigmentos Biológicos/química , Extratos Vegetais/química , Vaccinium myrtillus/química , alfa-Amilases/antagonistas & inibidores , Folhas de Planta/química , alfa-Amilases/química
9.
Food Chem ; 324: 126847, 2020 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-32344340

RESUMO

This study aimed to investigate the inhibitory effect of chestnut inner skin extract (CISE) on the activity of postprandial blood sugar-related enzymes. In total, 12 flavonoids were identified by HPLC-TOF-MS. CISE showed strong and weak inhibition on α-amylase and α-glucosidase, with the IC50 of 27.2 and 2.3 µg/mL, respectively. The inhibition modes of CISE against α-amylase and α-glucosidase were mixed-type and non-competitive type, respectively. Epicatechin gallate noncompetitively inhibited α-amylase, α-glucosidase and dipeptidyl peptidase IV (DPP-IV). Analysis by ultraviolet-visible spectroscopy, fluorescence spectroscopy and circular dichroism suggested that flavonoids altered the hydrophobicity and microenvironment of these enzymes. CISE decreased the starch bioavailability by reducing the enzymatic hydrolysis rate and increasing the fraction of undigested starch. The extract reduced the rapidly digestible starch and increased the resistant starch after incorporation into A-, B- or C- crystallinity starch. Thus, the chestnut inner skin is a useful resource for regulating postprandial blood sugar level.


Assuntos
Inibidores da Dipeptidil Peptidase IV/farmacologia , Fagaceae/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Extratos Vegetais/farmacologia , Disponibilidade Biológica , Catequina/análogos & derivados , Catequina/farmacologia , Dipeptidil Peptidase 4/química , Dipeptidil Peptidase 4/metabolismo , Inibidores da Dipeptidil Peptidase IV/química , Flavonoides/análise , Inibidores de Glicosídeo Hidrolases/química , Nozes/química , Extratos Vegetais/química , Amido/farmacocinética , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/química , alfa-Glucosidases/química
10.
BMC Complement Med Ther ; 20(1): 129, 2020 Apr 28.
Artigo em Inglês | MEDLINE | ID: mdl-32345272

RESUMO

BACKGROUND: Evolvulus alsinoides (Linn.) Linn. (Convolvulaceae) is a therapeutic herb alleviating brain patterns associated with three categories of regulatory principles of the body, mind, and behaviour. In the current research, enzyme inhibition and cytotoxic potentials of E. alsinoides (L.) L. leaf extract has been studied validating its potential application. METHODS: The plant phenolics in the leaf extracts obtained via cold-maceration with solvents viz.: n-hexane, chloroform, ethyl acetate, methanol, and water were quantitatively analyzed. The antioxidant potency was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and Ferric Reducing Ability of Plasma (FRAP) assays at five concentrations (100-500 µg). The enzyme inhibition potential was performed with α-amylase, α-glucosidase, and acetylcholinesterase at seven concentrations (25-500 µg). The experiments were done in triplicates and statistically validated using Minitab-17 and SPSS 22. RESULTS: Water extract contain 45.08 ± 0.02 mg GAE/g, 49.30 ± 0.07 mg GAE/g, 211.21 ± 0.02 mg QE/g tannins, phenolics, flavonoids respectively. Its antioxidant activity was supported by IC50 52.43 ± 0.2 µg/mL (DPPH assay) and 41.58 ± 0.03 (FRAP assay). Methanolic extract inhibits α-amylase with IC50 1.33 ± 0.05 µg/mL. Water extract inhibits α-glucosidase and acetylcholinesterase with IC50 3.58 ± 0.02 µg/mL and 4.46 ± 0.03 µg/mL. Cytotoxicity studies with SH-SY5Y cell-line substantiate the inhibition potential of water extract with IC50 103.0035 µg/mL. DISCUSSION AND CONCLUSIONS: The extracts with potent antioxidant and enzyme-inhibiting activity were determined. The findings of the research are the first report about the inhibition effects of Evolvulus alsinoides (Linn.) Linn extracts against α-amylase, α-glucosidase and acetylcholinesterase. The extracts shall be examined in future studies to evaluate its pharmaceutical potential.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Inibidores da Colinesterase/farmacologia , Diabetes Mellitus/tratamento farmacológico , Inibidores de Glicosídeo Hidrolases/farmacologia , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidores , Acetilcolinesterase , Doença de Alzheimer/enzimologia , Linhagem Celular Tumoral , Convolvulaceae/química , Diabetes Mellitus/enzimologia , Humanos , Índia , Medicina Ayurvédica , Extratos Vegetais/química , Folhas de Planta/química , alfa-Glucosidases
11.
Arch Biochem Biophys ; 687: 108369, 2020 07 15.
Artigo em Inglês | MEDLINE | ID: mdl-32335047

RESUMO

A neutral tea polysaccharide (TPSN) was isolated from green tea. Gas chromatography analysis showed that TPSN was composed of d-glucose, l-arabinose and d-galactose residues at a molar ratio of 90.0: 9.1: 0.9. The weight-averaged molecular weight of TPSN was determined as about 2.0 × 105 g mol-1 using static light scattering analysis. The result of nuclear magnetic resonance (NMR) spectroscopy indicated that TPSN and water-soluble starch had similar structures. TPSN exhibited inhibitory activity towards α-amylase through the noncompetitive inhibition mechanism, but the tertiary structure of α-amylase related to enzymatic activity, analyzed using circular dichroism spectroscopy, was not affected by TPSN. Meanwhile, TPSN exhibited hydrolysis properties catalyzed by α-amylase. Molecular docking analysis revealed that the various behaviors of TPSN to α-amylase could be attributed to that the different chain segments of TPSN combined with different amino acid residues of α-amylase.


Assuntos
Inibidores Enzimáticos/química , Polissacarídeos/química , Chá/química , alfa-Amilases/antagonistas & inibidores , Animais , Camellia sinensis/química , Ensaios Enzimáticos , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/metabolismo , Hidrólise , Cinética , Simulação de Acoplamento Molecular , Peso Molecular , Polissacarídeos/isolamento & purificação , Polissacarídeos/metabolismo , Ligação Proteica , Suínos , alfa-Amilases/metabolismo
12.
Acta Biochim Pol ; 67(1): 41-47, 2020 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-32129972

RESUMO

The chemical composition of Succisa pratensis is not well known. The existing data indicate a substantial content of flavonoids, which include luteolin and apigenin 7-glucosides. The aim of this study was to elaborate the isolation protocol of these flavonoids from flowers and leaves of S. pratensis, to carry out their characterization, as well as evaluate the effect of S. pratensis extracts on activation of transcription factor NF-κB and α-amylase activity. The extraction protocol applied in this study allowed isolation and characterization of flavonoid fraction of S. pratensis. Their identity was confirmed by NMR spectra analysis, UV spectroscopy and electrospray ionization-tandem MS evaluation. Treatment of pancreatic α-amylase with S. pratensis extract inhibited this enzyme's activity to an extent comparable to that of isolated luteolin and apigenin 7-glucosides. Incubation of HepG2 cells for 24 h with S. pratensis extracts or isolated flavonoids resulted in moderate reduction in NF-κB transcription factor activation evaluated in terms of translocation of its active subunits from cytosol into nucleus and subsequently diminished expression of the COX-2 gene. Expression of NF-κB was also reduced. The most significantly diminished NF-κB activation and expression, as well as COX-2 expression, was found to result from treatment with isolated flavonoids and ethyl acetate extract of S. pratensis leaves. These results indicate that S. pratensis flavonoids may modulate the metabolic and signaling pathways whose deregulation is related to pathogenesis of liver cancer. Further studies are required to confirm these observations and assess the chemopreventive and/or therapeutic potential of the S. pratensis herb.


Assuntos
Apigenina/farmacologia , Glucosídeos/farmacologia , Neoplasias Hepáticas/metabolismo , Luteolina/farmacologia , NF-kappa B/metabolismo , Extratos Vegetais/farmacologia , alfa-Amilases/metabolismo , Inibidores de Ciclo-Oxigenase 2/farmacologia , Dipsacaceae/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Células Hep G2 , Humanos , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/etiologia , Extratos Vegetais/uso terapêutico , alfa-Amilases/antagonistas & inibidores
13.
J Food Sci ; 85(4): 1060-1069, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32147838

RESUMO

Inonotus obliquus is a traditional mushroom well known for its therapeutic value. In this study, various solvent fractions of I. obliquus were preliminarily screened for their antioxidant, α-amylase and α-glucosidase inhibition properties. To improve the drug delivery, the active fraction (ethyl acetate fraction) of I. obliquus was synthesized into fungisome (ethyl acetate phophotidyl choline complex, EAPC) and its physical parameters were assessed using Fourier transform infrared spectroscopy (FTIR), High performance liquid chromatography (HPLC), Scanning electron microscope (SEM), and ς potential analysis. Then normal human hepatic L02 cells was used to evaluate the cytotoxicity of EAPC. The results showed that EA fraction possesses significant free radical scavenging, α-amylase and α-glucosidase inhibition properties. FTIR, SEM, and HPLC analysis confirmed the fungisome formation. The particle size of EAPC was 102.80 ± 0.42 nm and the ς potential was -54.30 ± 0.61 mV. The percentage of drug entrapment efficiency was 97.13% and the drug release rates of EAPC in simulated gastric fluid and simulated intestinal fluid were 75.04 ± 0.29% and 93.03 ± 0.36%, respectively. EAPC was nontoxic to L02 cells, however it could selectively fight against the H2 O2 induced oxidative damage in L02 cells. This is the first study to provide scientific information to utilize the active fraction of I. obliquus as fungisome. PRACTICAL APPLICATIONS: Inonotus obliquus (IO) is a traditional medicinal fungus. The extracts of IO have obvious antioxidant and hypoglycemic activities. Ethyl acetate (EA) fraction of IO was encapsulated in liposomes to form EAPC. EAPC has a sustained-release effect. It has nontoxic to L02 cells and could protect L02 cells from oxidative damage caused by hydrogen peroxide. This study could provide new ideas for the treatment of diabetes.


Assuntos
Agaricales/química , Antioxidantes/farmacologia , Basidiomycota/química , Inibidores Enzimáticos/farmacologia , Peróxido de Hidrogênio/toxicidade , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidores , Antioxidantes/química , Antioxidantes/isolamento & purificação , Linhagem Celular , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Hepatócitos/efeitos dos fármacos , Hepatócitos/metabolismo , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , alfa-Amilases/química , alfa-Glucosidases/química
14.
Int J Mol Sci ; 21(4)2020 Feb 11.
Artigo em Inglês | MEDLINE | ID: mdl-32053943

RESUMO

The phenolic profiles, hypoglycemic activity, and molecular mechanism of the effect on type 2 diabetes mellitus (T2DM) of four highland barley varieties were investigated in the present study. The fundamental phenolics in highland barley were ferulic acid, naringin, and catechin, which mainly existed in bound form. These varieties showed favorable hypoglycemic activity via inhibition of α-glucosidase and α-amylase activities, enhancement of glucose consumption, glycogen accumulation and glycogen synthase 2 (GYS2) activity, and down-regulation of glucose-6-phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK) activities. Specifically, ZQ320 variety exhibited the strongest hypoglycemic activity compared to the other varieties. Highland barley phenolics could inhibit gluconeogenesis and motivate glycogen synthesis via down-regulating the gene expression of G6Pase, PEPCK, and glycogen synthase kinase 3ß (GSK3ß), while activating the expression of insulin receptor substrate-1 (IRS-1), phosphatidylinositol 3 kinase (PI3K), serine/threonine kinase (Akt), GYS2, and glucose transporter type 4 (GLUT4). Therefore, phenolics from highland barley could be served as suitable candidates for therapeutic agent in T2DM to improve human health.


Assuntos
Hordeum/química , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Fenóis/química , Fenóis/farmacologia , Diabetes Mellitus Tipo 2/tratamento farmacológico , Diabetes Mellitus Tipo 2/metabolismo , Gluconeogênese/efeitos dos fármacos , Glucose/metabolismo , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Células Hep G2 , Humanos , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo
15.
Sci Rep ; 10(1): 3530, 2020 02 26.
Artigo em Inglês | MEDLINE | ID: mdl-32103043

RESUMO

Butea monosperma is one of the extensively used plants in traditional system of medicines for many therapeutic purposes. In this study, the antioxidant activity, α-glucosidase and α-amylase inhibition properties of freeze drying assisted ultrasonicated leaf extracts (hydro-ethanolic) of B. monosperma have been investigated. The findings revealed that 60% ethanolic fraction exhibited high phenolic contents, total flavonoid contents, highest antioxidant activity, and promising α-glucosidase and α-amylase inhibitions. The UHPLC-QTOF-MS/MS analysis indicated the presence of notable metabolites of significant medicinal potential including apigenin, apigenin C-hexoside C-pentoside, apigenin C-hexoside C-hexoside, apigenin-6,8-di-C-pentoside and genistin etc., in B. monosperma leave extract. Docking studies were carried out to determine the possible role of each phytochemical present in leaf extract. Binding affinity data and interaction pattern of all the possible phytochemicals in leaf extract of B. monosperma revealed that they can inhibit α-amylase and α-glucosidase synergistically to prevent hyperglycemia.


Assuntos
Butea/química , Inibidores de Glicosídeo Hidrolases/química , Hipoglicemiantes/química , Compostos Fitoquímicos/química , Extratos Vegetais/química , Folhas de Planta/química , Etanol/química , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/química , alfa-Glucosidases/química
16.
Sci Rep ; 10(1): 2109, 2020 02 07.
Artigo em Inglês | MEDLINE | ID: mdl-32034276

RESUMO

Diplocyclos palmatus (L.) C. Jeffrey is an important medicinal plant used in several reproductive medicines. It serves as a wide source of tetracyclic triterpens called cucurbitacins. Response surface methodology (RSM) with Box-Behnken design (BBD) was studied to optimize the production of cucurbitacins. RSM put forth the ideal conditions such as 1:30 SS ratio (g/mL), 80 rpm (mixing extraction speed), 150 µm mean particle size, 30 min extraction time and 50 °C using chloroform in continuous shaking extraction (CSE) and showed the highest cucurbitacin I (CUI) content (2.345 ± 0.1686 mg/g DW). Similarly, the highest yield of cucurbitacin B (CUB) (1.584 ± 0.15 mg/g DW) was recorded at ideal conditions (1:40 g/mL SS ratio and 60 min time and others similar to CUI). Among the tested extraction methods, the highest CUI, CUB, and CUI + B yield (1.437 ± 0.03, 0.782 ± 0.10, 2.17 ± 0.35 mg/g DW, respectively) as well as promising DPPH radical scavenging activity (25.06 ± 0.1 µgAAE/g DW) were recorded from the SBAE (steam bath assisted extraction). In addition, MAE and UAE revealed the highest inhibition of α-amylase (68.68%) and α-glucosidase (56.27%) enzymes, respectively. Fruit extracts showed potent anticancer activity against breast (MCF-7) and colon (HT-29) cancer cell lines (LC50 - 44.27 and 46.88 µg/mL, respectively). Our study proved that SS ratio, particle size and temperature were the most positively influencing variables and served to be the most efficient for the highest recovery of CUI and CUB. Based on the present study, the fruits of D. palmatus were revealed as a potent antioxidant, anti-diabetic and anticancer bio-resource that could be explored further to develop novel drug to manage diabetes, cancer and oxidative stress related disorders.


Assuntos
Cucurbitaceae/química , Cucurbitacinas/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Plantas Medicinais/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Cucurbitacinas/farmacologia , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/farmacologia , Células HT29/efeitos dos fármacos , Humanos , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Células MCF-7/efeitos dos fármacos , Extratos Vegetais/farmacologia , alfa-Amilases/antagonistas & inibidores
17.
J Chromatogr A ; 1620: 460970, 2020 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-32089291

RESUMO

This study focuses on the health benefits of several fresh herbs that are commonly used in the Mediterranean diet. Antioxidant activity, phytosterol content and α-amylase inhibitory activity of fresh basil, lavender, oregano, rosemary, sage, and thyme are analyzed and compared. High-performance thin-layer chromatography (HPTLC) combined with effect directed analysis was used to detect and quantify biological active compounds on chromatograms. The highest antioxidant activity was measured in the extract from oregano leaf, while the highest terpenoid content was in basil leaf extract. All extracts except lavender leaf and lavender flower extracts showed α-amylase inhibition. The same compound at hRF = 68 in basil, oregano, rosemary, sage, and thyme extracts was responsible for α-amylase inhibition. Combined with effect-directed assays and attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy, hyphenated HPTLC allowed a fast characterization of the active compound. ATR spectral analysis of this band tentatively identified oleanolic acid (or its derivative) to be responsible for the α-amylase inhibition.


Assuntos
Lamiaceae/química , Extratos Vegetais/química , alfa-Amilases/antagonistas & inibidores , Antioxidantes/farmacologia , Bioensaio , Cromatografia em Camada Delgada , Inibidores Enzimáticos/farmacologia , Fitosteróis/análise , Extratos Vegetais/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier , Terpenos/análise
18.
Microb Pathog ; 140: 103955, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31899325

RESUMO

Eleusine coracana (Finger millet) has high nutritional value with numerous health benefits and is of low cost. Isolation of beta-glucan (ßG) from E. coracana (Ec-ßG) has gained increasing research attention. UV-vis spectroscopy used to measure the surface plasmon resonance at 361 nm to confirm the presence of polysaccharides (glucan molecules) in Ec-ßG. X-ray diffraction analysis of Ec-ßG displayed a crystalline nature and confirmed the presence of the ßG molecule. Further, the bioactive compounds of Ec-ßG were screened using gas chromatography-mass spectrometry. The antibacterial activity of Ec-ßG against both Gram-positive (Lysinibacillus fusiformis, Enterococcus faecalis) and Gram-negative (Proteus vulgaris, Shigella sonnei) bacteria were assessed through minimum inhibitory concentrations <70 µg/ml of Ec-ßG. In addition, the antibiofilm activity and bacterial viability of Ec-ßG at 100 µg/ml was confirmed by light and confocal laser scanning microscopy. Furthermore, Ec-ßG inhibits α-amylase and α-glucosidase at an IC50 -value of 1.23 and 1.42 µg/ml, respectively. Superoxide anion scavenging activity at IC50-1.4 µg/ml and DPPH radical scavenging activity at IC50-1.2 µg/ml showed that Ec-ßG had potential antioxidant property. The in vitro hemolysis assay for biocompatibility of Ec-ßG at 200 µg/ml showed 0.06 ± 0.09%. Therefore, Ec-ßG has the potential to act as a suggestive agent for antibacterial, antidiabetic, and antioxidant activity.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Biofilmes/efeitos dos fármacos , Eleusine/química , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , beta-Glucanas/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Enterococcus faecalis/efeitos dos fármacos , Enterococcus faecalis/fisiologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/farmacologia , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Shigella sonnei/efeitos dos fármacos , Shigella sonnei/fisiologia , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/química , beta-Glucanas/química , beta-Glucanas/isolamento & purificação
19.
Int J Biol Macromol ; 146: 508-517, 2020 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-31923490

RESUMO

Impacts of hot water extraction (HWE), pressurized water extraction (PWE), high-speed shearing homogenization extraction, microwave assisted extraction (MAE), ultrasound assisted extraction (UAE), ultrasound assisted enzymatic extraction, and ultrasound-microwave assisted extraction (UMAE) on physicochemical characteristics and bioactivities of polysaccharides from loquat (Eriobotrya japonica) leaves (LLPs) were investigated. Results showed that the degrees of esterification, contents of phenolics and uronic acids, constituent monosaccharides, apparent viscosities, and molecular weights of LLPs varied by different extraction methods. Bioactivities of LLPs were also significantly affected by different extraction methods. The high molecular weight and high degree of esterification of LLP-W and LLP-P extracted by HWE and PWE, respectively, might contribute to their strong binding capacities. The strong antioxidant activities and inhibitory effects on α-amylase and α-glucosidase were found in LLP-M and LLP-U extracted by MAE and UAE, respectively, which might be attributed to their contents of uronic acids, contents of total phenolics, and molecular weights. The low molecular weights and viscosities of LLP-U and LLP-UM extracted by UMAE might contribute to their strong prebiotic effects. These findings could provide scientific foundations for selecting appropriate extraction methods to obtain LLPs with desired bioactivities for applications in the pharmaceutical and functional food industries.


Assuntos
Fenômenos Químicos , Eriobotrya/química , Folhas de Planta/química , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Antioxidantes/farmacologia , Benzotiazóis/química , Compostos de Bifenilo/química , Colesterol/metabolismo , Esterificação , Inibidores de Glicosídeo Hidrolases/farmacologia , Peso Molecular , Monossacarídeos/análise , Óxido Nítrico/metabolismo , Picratos/química , Reologia , Espectroscopia de Infravermelho com Transformada de Fourier , Ácidos Sulfônicos/química , Viscosidade , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo
20.
Food Chem ; 313: 126099, 2020 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-31927321

RESUMO

Diabetes mellitus is a metabolic disorder characterized by hyperglycemia, which can be counteracted by inhibition of α-glucosidase and α-amylase, both involved in the carbohydrate metabolism. Fourteen C-glucosidic ellagitannins and three galloylated glucoses were studied as potential α-glucosidase and α-amylase inhibitors. Most of the compounds were found to be moderate inhibitors of α-amylase, but potent inhibitors of α-glucosidase, showing low-micromolar IC50 values, far lower than that of the antidiabetic drug acarbose. This selectivity can be an advantage for their possible application as functional food ingredients with anti-diabetic properties because strong α-amylase inhibition generally causes undesired side effects. The best inhibitors were selected for further studies. Intrinsic fluorescence measurements confirmed their high affinity towards α-glucosidase, highlighting a static quenching mechanism. Circular dichroism measurements and kinetics of inhibition indicated that the most active C-glucosidic ellagitannin roburin D (RobD) is a competitive inhibitor, whereas α-pentagalloylglucose (α-PGG) acts as a mixed-type inhibitor.


Assuntos
Taninos Hidrolisáveis/química , Hipoglicemiantes/química , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo , Dicroísmo Circular , Glucosídeos/química , Taninos Hidrolisáveis/metabolismo , Hipoglicemiantes/metabolismo , Concentração Inibidora 50 , Cinética , Espectrometria de Fluorescência , alfa-Amilases/antagonistas & inibidores , alfa-Glucosidases/química
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA