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1.
Food Chem ; 335: 127645, 2021 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-32738537

RESUMO

The dried Ganoderma lucidum (GL) has been widely used for its pharmacological properties and bioactive ganoderic acids (GAs). Herein, extraction procedures combining ultra-sonication and heating were optimized using response surface methodology based on four variables (antioxidant activity, anti-diabetic activity, total GAs content, and total polysaccharide content) and principal component analysis. The extraction of freeze-dried GL at temperatures between 64.2 and 70 °C for 1.2 h maximized the antioxidant activity and GA content, whereas the polysaccharide content and anti-diabetic activity were maximized by extraction between 66.8 and 70 °C for more than 2.8 h. Heat-dried GL extracted at 50 °C for 3 h provided the greatest anti-inflammatory activity against HaCaT cells by suppressing the response to inflammation related cytokines at mRNA levels. These results suggest that extraction conditions might be a limiting factor for target-oriented investigations, and optimized extraction methods may improve the potential effect and quality of harvested GL products.


Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Antioxidantes/isolamento & purificação , Fracionamento Químico/métodos , Hipoglicemiantes/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Reishi/química , Triterpenos/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Linhagem Celular , Fracionamento Químico/instrumentação , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Polissacarídeos/farmacologia , Triterpenos/química , Triterpenos/farmacologia
2.
Chem Biol Interact ; 330: 109167, 2020 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-32603660

RESUMO

Recently, it has been shown that drimane-type sesquiterpenoids isolated from Zygogynum pancheri, a species native to New Caledonia, possessed significant α-amylase inhibitory activities. To further explore their antidiabetic potential, we investigated the effect of 1ß-O-(E-cinnamoyl)-6α-hydroxy-9epi-polygodial (D) and 1ß-E-O-p-methoxycinnamoyl-bemadienolide (L), two of the most active compounds of the series, on diabetic model rats. Compounds D and L (2 mg kg/day) were daily and orally administrated for 30 days to streptozotocin (STZ) (150 mg/kg) induced male diabetic Wistar rats. Animals were allocated into five groups of six rats. Comparatively to diabetic rats, treatments with D and L compounds were able to significantly (P < 0.05) decrease Fasting Blood Glucose (FBG) (70.15%, 71.02%), serum total cholesterol (46.27% and 39.38%), triglycerides (56.60% and 58.15%), creatinine (37.31% and 36.49%) and uric acid levels (67.76% and 69.68%), respectively. Compounds D and L also restored the altered plasma enzyme (aspartate aminotransferase, AST (47.83% and 43.20%), alanine aminotransferase, ALT (49.76% and 48.35%, alkaline phosphatase, ALP (72.78% and 73.21%)) and lactate dehydrogenase, LDH (47.95% and 53.93%) levels to near normal, respectively. Administration of Glymepiride, significantly (p < 0.05) reduced FBG (73.94%) in STZ induced diabetic rats. Additionally, the compounds D and L exhibited inhibitory effects in vivo on lipase activity of diabetic rats (54.83% and 52.25%), respectively. The outcomes of this study suggested that these two drimanes could be considered as efficient hypoglycemic, hypolipidemic and antiobesity agents for diabetes management and its complications.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Fitoterapia/métodos , Extratos Vegetais/farmacologia , Sesquiterpenos Policíclicos/isolamento & purificação , Animais , Fármacos Antiobesidade/isolamento & purificação , Fármacos Antiobesidade/farmacologia , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Hipolipemiantes/isolamento & purificação , Hipolipemiantes/farmacologia , Masculino , Nova Caledônia , Extratos Vegetais/química , Sesquiterpenos Policíclicos/farmacologia , Ratos , Ratos Wistar , Sesquiterpenos/isolamento & purificação , Sesquiterpenos/farmacologia , Winteraceae/química
3.
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
4.
Curr Pharm Biotechnol ; 21(11): 1059-1069, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32065099

RESUMO

BACKGROUND: The folkloric profile of Delonix regia demonstrates that it can be used in the management of diabetes. OBJECTIVE: The present study was conducted to evaluate the safety profile of the aerial part extracts of Delonix regia and their antidiabetic potential along with improvement in oxidative stress. MATERIALS AND METHODS: Phytochemical screening, total phenolic, and flavonoid contents along with in-vitro antioxidant and alpha-amylase inhibitory activities were determined. HPLC analysis, acute toxicity, glucose tolerance, in-vivo antidiabetic effect along with the influence on biochemical, oxidative stress parameters, and comet assay of the active extract were performed and assessed. RESULTS: Total phenolic (831.6±0.002 mg/g GAE) and flavonoid (361.4±0.002 mg/g QE) contents were found to be higher in the methanolic extract. Inhibitory concentration IC50 indicated better results for the methanolic extract in DPPH (47.6µg/mL) and alpha-amylase inhibitory (14.61µg/mL) assays. HPLC analysis of the methanolic extract confirmed the presence of quercetin, gallic acid, caffeic acid, cinnamic acid, ferulic acid, and p-coumaric acid. Acute oral toxicity exhibited no mortality and morbidity during the 24h period. The methanolic extract showed better tolerance to glucose. Streptozotocin- nicotinamide (55-110 mg/kg) induced hyperglycemia declined along with improvement in hematological, biochemical parameters and oxidative stress markers (SOD, CAT, H202) in a dose-dependent manner. The maximum effect was recorded at 500mg/kg dose. Comet assay was performed for genotoxic studies and it was observed that the methanolic extract of Delonix regia showed the maximum genoprotective effect at 100µg/mL. CONCLUSION: The findings suggest that the methanolic aerial part extract of Delonix regia exhibited hypoglycemic, antioxidant, and hypolipidemic activities. The antidiabetic effect was comparable to glibenclamide suggesting its therapeutic use as a natural anti-diabetic remedy.


Assuntos
Antioxidantes/uso terapêutico , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Fabaceae/química , Hipoglicemiantes/uso terapêutico , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/uso terapêutico , Animais , Antioxidantes/administração & dosagem , Antioxidantes/toxicidade , Dano ao DNA , Relação Dose-Resposta a Droga , Hiperglicemia/tratamento farmacológico , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/toxicidade , Medicina Tradicional , Componentes Aéreos da Planta/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Ratos Wistar
5.
Carbohydr Res ; 489: 107927, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-32062396

RESUMO

Diabetes mellitus is the most common metabolic disorder characterized by chronic hyperglycemia. There has been a surge of research studies aiming to use natural products in the management of diabetes. The objective of this study was to isolate and characterize the structure and anti-diabetic mechanisms of the main ingredient from Rosa canina. The oligosaccharide was isolated from Rosa canina fruits and characterized by a combination of FTIR, NMR and Mass spectrometry. Wistar rats were divided into negative control, diabetic (type 2), isolated oligosaccharide (IO)-treated diabetic and positive diabetic controls. Oral glucose tolerance, gluconeogenesis and α-glucosidase inhibitory tests as well as immunohistochemistry and quantitative real time-PCR were performed to elucidate the molecular anti-diabetic mechanisms of IO. Structural analyses confirmed the oligosaccharide structure of isolated fraction. Gluconeogenesis and α-glucosidase activity were inhibited by IO in diabetic rats. The oral glucose tolerance test was improved significantly in the group treated with the IO (P < 0.05). Pancreatic ß-cells and tissue pathological examination showed a significant improvement after the treatment period. In addition, the expression of Ngn3, Nkx6.1 and insulin increased in oligosaccharide-treated compared to untreated diabetic rats. Owing to the verified anti-diabetic effects and regenerative potential, isolated oligosaccharide could be considered as the promising drug in the management of diabetes.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Oligossacarídeos/uso terapêutico , Extratos Vegetais/uso terapêutico , Rosa/química , Animais , Configuração de Carboidratos , Diabetes Mellitus Experimental/induzido quimicamente , Frutas/química , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Masculino , Oligossacarídeos/química , Oligossacarídeos/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Ratos , Ratos Wistar , Estreptozocina
6.
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
7.
Chemosphere ; 247: 125852, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-31927183

RESUMO

An adsorbent was developed from the residues of Moringa oleifera Lam. seed husks functionalized with iron nanoparticles for subsequent application to the removal of metformin from contaminated water. The material, MOM-Fe3O4, was characterized using TEM, SEM imaging, and EDX analysis, which revealed that iron nanoparticles were retained in the pores. The application of MOM-Fe3O4 to waste water resulted in a 93.9% reduction in the metformin content, demonstrating the efficacy of the material. Kinetic and equilibrium data were fitted to the pseudo-first-order and Langmuir models, respectively. The thermodynamic parameters indicated an exothermic and reversible process. A high adsorption capacity, 65.01 mg g-1 at 298 K, demonstrated the potential of using the new material as a low-cost adsorbent for the removal of pharmaceuticals such as metformin.


Assuntos
Metformina/isolamento & purificação , Nanopartículas/química , Poluentes Químicos da Água/isolamento & purificação , Purificação da Água/métodos , Adsorção , Hipoglicemiantes/isolamento & purificação , Ferro/química , Cinética , Moringa oleifera/química , Termodinâmica , Purificação da Água/economia
8.
Carbohydr Polym ; 232: 115766, 2020 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-31952583

RESUMO

Type 2 diabetes mellitus plagues many people in China and the world, and its nephritis complication is the leading cause of death for patients. Paecilomyces hepiali contained various functional components, especially polysaccharides, which possesses well pharmacological activities. In this study, polysaccharide purified from Paecilomyces hepiali fermented mycelium entitled PHEA was obtained, and its structure was systemically characterized using fourier transform infrared spectroscopy (FT-IR) and nuclear magnetic resonance (NMR). In C57BL/KsJ (BKS).Cg-Dock7m +/+ Leprdb/JNju mice (db/db mice), via detecting the alternations on biochemical criterions, pathological indicators and protein expressions related to nuclear factor-E2-related factor 2 (Nrf2) and nuclear factor-κB (NF-κB) signaling in serum and/or tissues including muscle, liver and kidney after 8-week PHEA administration, the hypoglycemic, hypolipidemic, and anti-diabetic nephropathic activities of PHEA were confirmed. The purified P. Hepiali polysaccharide with the anti-diabetic and -nephritic properties was first reported in this study via regulating Nrf2-meadited NF-κB signaling in db/db mice.


Assuntos
Diabetes Mellitus Tipo 2/tratamento farmacológico , Nefropatias Diabéticas/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Micélio/química , Polissacarídeos/uso terapêutico , Animais , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Tipo 2/metabolismo , Nefropatias Diabéticas/metabolismo , Modelos Animais de Doenças , Fermentação , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Transgênicos , Micélio/metabolismo , NF-kappa B/antagonistas & inibidores , NF-kappa B/metabolismo , Tamanho da Partícula , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Transdução de Sinais/efeitos dos fármacos , Propriedades de Superfície
9.
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
10.
Nat Prod Res ; 34(1): 3-9, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31282220

RESUMO

Okra, Abelmoschus esculentus L. (Moench), also known as Lady's Fingers, gombo, or bamje, is an annual plant belonging to the Malvaceae family. Traditional olistic medicine since centuries directly associates this plant and its parts to a beneficial health hypoglycemic effect. Since the abscisic acid (ABA) has been associated to an interesting hypoglycemic effect, this triggered us to verify and quantify the presence of the abscisic acid in the okra phytocomplex. In particular, ABA, a plant derived hormone, has been proven by recent studies to be effective on mammals. To determine and quantify the ABA content, different parts of the Okra plant extracts have been evaluated, and HPLC-DAD analysis has been used allowing us to report for the first time the presence of this isoprenoid compound. Bioaccessibility has been also investigated using a simulated gastro intestinal (GI) digestion protocol with the aim of explore the possibility of okra extract as nutraceutical.


Assuntos
Abelmoschus/química , Ácido Abscísico/análise , Diabetes Mellitus/tratamento farmacológico , Extratos Vegetais/química , Cromatografia Líquida de Alta Pressão , Suplementos Nutricionais , Hipoglicemiantes/análise , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Malvaceae
11.
Nat Prod Res ; 34(4): 575-579, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30317870

RESUMO

The whole plant, Tricholepis chaetolepis, powder was investigated using proximate and fluorescence analysis along with determining the extractive values. Total phenolics, flavonoids and total protein contents of n-hexane, chloroform and methanolic extracts of the whole plant were also determined. The anti-diabetic activity of all the three extracts of the plant was determined by in vitro alpha-amylase inhibition assay. The anti-oxidant potential was evaluated using Phosophomolybdenum and DPPH methods. The anti-inflammatory potential of all extracts were determined by carrageenan-induced rat paw oedema model. The evaluation of the plant extracts exhibited the anti-diabetic, anti-oxidant, and anti-inflammatory activities in dose dependent fashion. The research concludes that Tricholepis chaetolepis extracts contain phenol, flavonoids, and tannins that show observable anti-oxidant and anti-diabetic potential. It is also concluded that the methanol extract of the plant showed the maximum effect against inflammation induced by carrageenan in rat paw oedema as compared with n-hexane and chloroform extracts.


Assuntos
Anti-Inflamatórios/isolamento & purificação , Antioxidantes/isolamento & purificação , Asteraceae/química , Hipoglicemiantes/isolamento & purificação , Extratos Vegetais/química , Animais , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Edema/tratamento farmacológico , Flavonoides/análise , Hipoglicemiantes/farmacologia , Inflamação/tratamento farmacológico , Metanol , Fenóis/análise , Extratos Vegetais/farmacologia , Proteínas de Plantas/análise , Ratos , Solventes , Taninos/farmacologia , Taninos/uso terapêutico
12.
J Ethnopharmacol ; 248: 112308, 2020 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-31622745

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Dendrobium officinale polysaccharide (DOP) is the main active ingredient of Dendrobium officinale Kimura & Migo, which is a precious traditional Chinese medicine and often used in treatment of hepatitis, diabetes, obesity and rheumatoid arthritis. AIM OF THE STUDY: DOP exhibits significant hypoglycemic activity, while its mechanism remains unclear. The present study aims to investigate the hypoglycemic mechanisms of DOP based on the glucagon-mediated signaling pathways and the liver glycogen structure, which catalyze hepatic glucose metabolism, and provide new knowledge about the antidiabetic mechanism of DOP and further evidence for its clinical use for diabetes. MATERIALS AND METHODS: DOP were obtained from the dry stems of Dendrobium officinale by water extraction and alcohol precipitation method. T2DM mice model was established by high-fat diet combined with streptozotocin. Liver histopathological changes were observed by H&E and PAS straining. Pancreatic histology was studied by H&E staining and immunofluorescence analysis. The levels of glucagon and insulin were detected by Elisa Kit and the hepatic glycogen content was detected by GOPOD. The expressions of the hepatic glycogen-related metabolism enzymes, hepatic gluconeogenesis enzymes, and the related protein in cAMP-PKA and Akt/FoxO1 signaling pathways were detected by western blots. Liver glycogen was extracted from the liver tissues by sucrose density gradient centrifugation, and size exclusion chromatography (SEC) was used to analyze the structure of liver glycogen. RESULTS: DOP could significantly affect the glucagon-mediated signaling pathways, cAMP-PKA and Akt/FoxO1, to further promote hepatic glycogen synthesis, inhibit hepatic glycogen degradation and hepatic gluconeogenesis. Moreover, DOP could reverse the instability of the liver glycogen structure and thus probably suppressed glycogen degradation. Thus, DOP finally would ameliorate hepatic glucose metabolism via glucagon-mediated signaling pathways and modifying liver-glycogen structure in diabetic mice. CONCLUSIONS: The hypoglycemic mechanism of DOP might be associated with the regulation of glucagon-mediated hepatic glycogen metabolism and gluconeogenesis, and of liver glycogen structure, contributing to improved hepatic glucose metabolism in diabetic mice.


Assuntos
Dendrobium , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Glucagon/metabolismo , Glucose/metabolismo , Glicogênio/metabolismo , Hipoglicemiantes/farmacologia , Fígado/efeitos dos fármacos , Extratos Vegetais/farmacologia , Polissacarídeos/farmacologia , Transdução de Sinais/efeitos dos fármacos , Animais , Dendrobium/química , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Tipo 2/induzido quimicamente , Diabetes Mellitus Tipo 2/metabolismo , Dieta Hiperlipídica , Glicogênio/química , Hipoglicemiantes/isolamento & purificação , Fígado/metabolismo , Masculino , Camundongos Endogâmicos C57BL , Estrutura Molecular , Extratos Vegetais/isolamento & purificação , Polissacarídeos/isolamento & purificação , Estreptozocina
13.
J Ethnopharmacol ; 248: 112326, 2020 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-31639486

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Mulberry (Morus alba L.) leaves have been widely applied to controlling blood glucose as a efficacious traditional Chinese medicine or salutary medical supplement. The extracts of mulberry leaf suppress inflammatory mediators and oxidative stress, protect the pancreatic ß-cells and modulate glucose metabolism in diabetic rats. Our previous studies and others have shown that mulberry leaf extract has excellent therapeutic effects on type 2 diabetes mellitus (T2DM), however, the underlying mechanism remains to be studied. AIM OF THE STUDY: Skeletal muscle insulin resistance (IR) plays an important role in the pathogenesis of T2DM. The aim of this study was to investigate the effects and mechanisms of Mulberry leaf flavonoids (MLF) in L6 skeletal muscle cells and db/db mice. MATERIALS AND METHODS: L6 skeletal muscle cells were cultured and treated with/without MLF for in vitro studies. For in vivo studies, the db/db mice with/without MLF therapy were used. Coomassie brilliant blue staining and α-SMA immunofluorescence staining were used to identify the differentiated L6 cells. Glucose level and ATP level of L6 myotubes were performed by optical density detection and cell viability was performed by MTT method. Mitochondrial membrane potential of L6 myotubes was detected by JC-1 fluorescent staining. ROS level of L6 myotubes was detected by DCFH-DA fluorescent staining. The body weight, food intake, and blood glucose of the mice were measured in different treatment days. Oral glucose tolerance test (OGTT), starch glucose tolerance test (STT) and insulin tolerance test (ITT) were performed in mice. Glycated hemoglobin, glycated serum protein, insulin, liver and muscle glycogen, total cholesterol (TC), triglyceride (TG), high-density lipoprotein cholesterol (HDL-c) and low-density lipoprotein cholesterol (LDL-c) of the mice were detected by corresponding kit. The pathologic change of pancreas and skeletal muscle of mice were performed by H & E staining. Immunohistochemistry staining was used to detect the GLUT4 and p-AMPK expressions in skeletal muscle in mice. GLUT4, CPT-1, NRF1, COXIV, PGC-1α, and p-AMPK expression levels in L6 cells and mice were detected by western bolt assay. RESULTS: MLF and metformin significantly ameliorated muscle glucose uptake and mitochondrial function in L6 muscle cells. MLF also increased the phosphorylation of AMPK and the expression of PGC-1α, and up-regulated the protein levels of m-GLUT4 and T-GLUT4. These effects were reversed by the AMPK inhibitor compound C. In db/db mice, MLF improve diabetes symptoms and insulin resistance. Moreover, MLF elevated the levels of p-AMPK and PGC-1α, raised m-GLUT4 and T-GLUT4 protein expression, and ameliorated mitochondrial function in skeletal muscle of db/db mice. CONCLUSIONS: MLF significantly improved skeletal muscle insulin resistance and mitochondrial function in db/db mice and L6 myocytes through AMPK-PGC-1α signaling pathway, and our findings support the therapeutic effects of MLF on type 2 diabetes.


Assuntos
Proteínas Quinases Ativadas por AMP/metabolismo , Glicemia/efeitos dos fármacos , Diabetes Mellitus Tipo 2/tratamento farmacológico , Flavonoides/farmacologia , Hipoglicemiantes/farmacologia , Resistência à Insulina , Mitocôndrias Musculares/efeitos dos fármacos , Morus , Músculo Esquelético/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Biomarcadores/sangue , Glicemia/metabolismo , Linhagem Celular , Diabetes Mellitus Tipo 2/sangue , Diabetes Mellitus Tipo 2/enzimologia , Modelos Animais de Doenças , Ativação Enzimática , Flavonoides/isolamento & purificação , Transportador de Glucose Tipo 4/metabolismo , Hipoglicemiantes/isolamento & purificação , Lipídeos/sangue , Masculino , Camundongos , Mitocôndrias Musculares/enzimologia , Morus/química , Músculo Esquelético/enzimologia , Coativador 1-alfa do Receptor gama Ativado por Proliferador de Peroxissomo/metabolismo , Fosforilação , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química
14.
J Ethnopharmacol ; 248: 112331, 2020 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-31655149

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Undesired effects of synthetic antidiabetic agents have made researchers to seek for safer and healthier resources. With this aspect, herbal materials have attracted substantial research interest and are being extensively investigated. Considering that herb-drug interactions can be a double-edged sword presenting both risks and benefits, investigation of such interactions is greatly in demand. AIM OF THE STUDY: to investigate possible beneficial effects of hydroalcoholic extract of SecurigeraSecuridaca seed (HESS) on antioxidant capacity, fibroblast growth factor 21 (FGF21) and insulin resistance in Streptozotocin (STZ)-induced diabetic rats, alone and in combination with glibenclamide. MATERIALS AND METHODS: Forty male Wistar rats were randomly divided in to eight equal groups including healthy and diabetic controls and six treated groups with a various doses of HESS alone and in combination with glibenclamide, for 35 consecutive days. Serum samples were taken and analyzed for biochemical profile, HOMA indexes, FGF21, oxidative/nitrosative stress and inflammatory biomarkers as compared with the controls. Moreover, total phenolic and flavonoid contents of herbal extract were assessed. RESULTS: The herbal extract was found to be rich in flavonoid and phenolic components. Both of glibenclamide and the HESS decreased glucose and insulin resistance, as well as increased body weight and insulin sensitivity. Moreover, the extract could mitigate oxidative/nitrosative stress and inflammation dose-dependently, however, the standard drug was less effective than HESS. Induction of diabetes increased FGF21 levels and both of the treatments could reduce its contents, however, glibenclamide was more effective than HESS. CONCLUSIONS: The results clearly show that there is no contradiction between HESS and glibenclamide. Moreover, the herbal extract could augment antioxidant and anti-inflammatory properties of the standard drug.


Assuntos
Antioxidantes/farmacologia , Diabetes Mellitus Experimental/tratamento farmacológico , Fabaceae , Fatores de Crescimento de Fibroblastos/sangue , Glibureto/farmacologia , Hipoglicemiantes/farmacologia , Resistência à Insulina , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Sementes , Animais , Antioxidantes/isolamento & purificação , Biomarcadores/sangue , Glicemia/efeitos dos fármacos , Glicemia/metabolismo , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/induzido quimicamente , Quimioterapia Combinada , Fabaceae/química , Hipoglicemiantes/isolamento & purificação , Insulina/sangue , Masculino , Extratos Vegetais/isolamento & purificação , Ratos Wistar , Sementes/química , Estreptozocina
15.
J Ethnopharmacol ; 248: 112356, 2020 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-31669668

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Tinospora sinensis Lour. (Merr.) belongs to the family Menispermaceae and its stem extract have been used traditionally in broad aspects of therapeutic remedies including debility, dyspepsia, fever, jaundice, ulcer, bronchitis, urinary disease, skin disease, liver disease and diabetes. AIM OF THE STUDY: The aim of the study was to evaluate the protective effects of methanol extract of stem of Tinospora sinensis (METS) on streptozotocin induced pancreatic islet cell injuries of diabetic rats and its correlation to its phytochemical profiles. MATERIALS AND METHODS: A high-performance liquid chromatography technique (HPLC) was used to identify and quantify the major phytochemicals present in the METS. Diabetic rats were administered with METS at a dose of (100, 200 and 400 mg/kg respectively orally) and standard drug Metformin (300 mg/kg) was given orally to group serving positive control. Effect of the METS on glucose homeostasis, oxidative stress, antioxidant status, histopathology of pancreas and also on intracellular reactive oxygen species (ROS), mitochondrial membrane potential, apoptosis, cell cycle of pancreatic islet cells were studied in diabetic rats. RESULTS: The major phytochemicals identified and quantified by HPLC in the extract were berberine, caffeic acid, myricetin and ferulic acid. This result showed that methanol extract exhibited good antioxidant effect. The methanol extract of the plant prevented the diabetogenic effect of STZ and significantly lowered the fasting blood glucose level, glycated haemoglobin and increased insulin and C-peptide level in treated rats. METS reduced apoptosis of STZ treated islet cells by significantly decreasing pro-inflammatory cytokines (TNFα, IL6), intracellular ROS generation, lipid peroxidation, nitric oxide (NO) production and increasing mitochondrial membrane potential and sub-G0 peak area, enzymatic and nonenzymatic antioxidants. CONCLUSION: The results revealed that the methanol extract of the stem of the plant possesses protective effects against diabetes and associated complications.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Apoptose/efeitos dos fármacos , Diabetes Mellitus Experimental/prevenção & controle , Hipoglicemiantes/farmacologia , Ilhotas Pancreáticas/efeitos dos fármacos , Extratos Vegetais/farmacologia , Tinospora , Animais , Anti-Inflamatórios/isolamento & purificação , Antioxidantes/isolamento & purificação , Glicemia/efeitos dos fármacos , Glicemia/metabolismo , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Experimental/patologia , Hemoglobina A Glicada/metabolismo , Hipoglicemiantes/isolamento & purificação , Mediadores da Inflamação/metabolismo , Ilhotas Pancreáticas/metabolismo , Ilhotas Pancreáticas/patologia , Peroxidação de Lipídeos/efeitos dos fármacos , Lipídeos/sangue , Masculino , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Mitocôndrias/patologia , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/isolamento & purificação , Ratos Wistar , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais , Estreptozocina , Tinospora/química
16.
J Ethnopharmacol ; 247: 112273, 2020 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-31586692

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Luohanguo (LHG), a traditional Chinese medicine, could clear heat, moisten the lung, soothe the throat, restore the voice, and lubricate intestine and open the bowels. LHG has been utilized for the treatment of sore throats and hyperglycemia in folk medicine as a homology of medicine and food. The hypoglycemic pharmacology of LHG has attracted considerable attention, and mogrosides have been considered to be active ingredients against diabetes mellitus. We have found that these mogrosides could be metabolized into their secondary glycosides containing 1-3 glucose residues in type 2 diabetes mellitus (T2DM) rats in previous studies. These metabolites may be the antidiabetic components of LHG in vivo. Thus far, no reports have been found on reducing blood glucose of mogrosides containing 1-3 glucose residues. AIMS OF THE STUDY: The aim of this study was to confirm that mogrosides containing 1-3 glucose residues were the active components of LHG for antidiabetic effects and to understand their potential mechanisms of action. MATERIALS AND METHODS: First, the special fraction of mogrosides containing 1-3 glucose residues was separated from a 50% ethanol extract of LHG, and the chemical components were identified by ultra-performance liquid chromatography (UPLC) and named low-polar Siraitia grosvenorii glycosides (L-SGgly). Second, the antidiabetic effects of L-SGgly were evaluated by HFD/STZ-induced (high-fat diet and streptozocin) obese T2DM rats by indexing fasting blood glucose (FBG), fasting insulin (FINS), and insulin resistance, and then compared with other fractions in the separation process. The changes in serum lipid levels were also detected. Finally, possible mechanisms of antidiabetic activity of L-SGgly were identified as increasing GLP-1 levels and activating liver AMPK in T2DM rats. RESULTS: The chemical analysis of L-SGgly showed that they contain 11-oxomogroside V, mogroside V, mogroside III, mogroside IIE, mogroside IIIA1, mogroside IIA1, and mogroside IA1, respectively. The total content of the mogrosides in L-SGgly was 54.4%, including 15.7% mogroside IIA1 and 12.6% mogroside IA1. L-SGgly showed excellent effects on obese T2DM rats compared with the other fractions of LHG extract, including significantly reducing the levels of FBG (p < 0.001) and modifying insulin resistance (p < 0.05). Meanwhile, they could significantly decrease the content of triglyceride (p < 0.01), total cholesterol (p < 0.01), low-density lipoprotein cholesterol (p < 0.01) and free fatty acid (p < 0.001) and increase the content of high-density lipoprotein cholesterol (p < 0.001) in serum of T2DM rats. Moreover, L-SGgly can significantly increase (p < 0.01) GLP-1 levels and decrease (p < 0.01) IL-6 levels in T2DM rat serum. AMPK-activating activity in T2DM rats was also upregulated by L-SGgly, but no statistical significance was shown. CONCLUSION: L-SGgly, fractions separated from LHG extract, were verified to have obvious anti-hyperglycemic and anti-hyperlipidemic effects on T2DM rats. Furthermore, L-SGgly regulated insulin secretion in T2DM rats by increasing GLP-1 levels. These findings provide an explanation for the antidiabetic role of LHG.


Assuntos
Cucurbitaceae/química , Diabetes Mellitus Tipo 2/tratamento farmacológico , Medicamentos de Ervas Chinesas/farmacologia , Glicosídeos/farmacologia , Hipoglicemiantes/farmacologia , Hipolipemiantes/farmacologia , Obesidade/tratamento farmacológico , Triterpenos/farmacologia , Administração Oral , Animais , Glicemia/análise , Glicemia/efeitos dos fármacos , Glicemia/metabolismo , Fracionamento Químico , Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2/sangue , Diabetes Mellitus Tipo 2/etiologia , Dieta Hiperlipídica/efeitos adversos , Medicamentos de Ervas Chinesas/análise , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/uso terapêutico , Peptídeo 1 Semelhante ao Glucagon/metabolismo , Glicosídeos/análise , Glicosídeos/isolamento & purificação , Glicosídeos/uso terapêutico , Humanos , Hipoglicemiantes/análise , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/uso terapêutico , Hipolipemiantes/análise , Hipolipemiantes/isolamento & purificação , Hipolipemiantes/uso terapêutico , Insulina/metabolismo , Metabolismo dos Lipídeos/efeitos dos fármacos , Masculino , Obesidade/sangue , Obesidade/etiologia , Ratos , Estreptozocina/toxicidade , Triterpenos/análise , Triterpenos/isolamento & purificação , Triterpenos/uso terapêutico
17.
J Ethnopharmacol ; 247: 112257, 2020 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-31589968

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Hydrolea zeylanica L. Vahl. (Hydroleaceae) is an aquatic medicinal plant used as leafy vegetable in some parts of India. In south Odisha and Hazaribag district of Jharkhand, India, decoction of leaves is used as household remedy for diabetes. To our knowledge, no prior studies have examined the antidiabetic activity of H. zeylanica to validate its ethnomedicinal claim. PURPOSE: With this aim in mind, we examined the bioactivity of hydroalcohol fraction of leaves of H. zeylanica (HAHZ) in streptozotocin-induced oxidative stress in diabetic rats. MATERIALS AND METHODS: In vitro antidiabetic and free radical scavenging activities of different fractions of H. zeylanica were performed. The most effective bioactive fraction e.g. HAHZ was considered for kinetic studies to understand the mode of inhibition of α-glucosidase and α-amylase. To understand the chemical composition, GC-MS/MS and LC-MS/MS analysis of HAHZ were performed. To find out the molecular mechanism of action of HAHZ, streptozotocin-induced oxidative stress and metabolic changes in diabetic rats were studied. RESULTS: HAHZ demonstrated significantly higher radical scavenging and antidiabetic activities. Kinetic analysis revealed that HAHZ inhibited α-glucosidase competitively, and α-amylase mixed competitively. To understand the chemical composition, GC-MS/MS and LC-MS/MS analysis of HAHZ identified 32 compounds and among which R-limonene (0.52%), perillartine (0.41%), N-formyl-L-lysine (1.49%), limonen-6-ol, pivalate (1.43%), lidocaine (1.70%) and gamolenic acid (2.80%) were reported to have antioxidant and antidiabetic activities. HAHZ-400 mg/kg showed significant (p < 0.001) improvement in serum markers (SGOT, SGPT, ALP, total bilirubin, total protein, triglycerides, total cholesterol, HDL-C, LDL-C) and oxidative markers (MDA, SOD, CAT, GSH) in serum, liver and pancreas at effective dose dependent manner. In histopathological observation, HAHZ-400 mg/kg showed marked improvement in restoring cellular architecture of liver and pancreas. CONCLUSION: In diabetic rats, the improvement in glycemic control mechanism was achieved upon stimulating insulin secretion by R-limonene, perillartine, N-formyl-L-lysine, limonen-6-ol, pivalate, lidocaine and gamolenic acid of HAHZ.


Assuntos
Organismos Aquáticos/química , Diabetes Mellitus Experimental/tratamento farmacológico , Depuradores de Radicais Livres/farmacologia , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Solanales/química , Animais , Glicemia/efeitos dos fármacos , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/induzido quimicamente , Etnofarmacologia , Feminino , Depuradores de Radicais Livres/isolamento & purificação , Depuradores de Radicais Livres/uso terapêutico , Humanos , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/uso terapêutico , Índia , Insulina/metabolismo , Masculino , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/uso terapêutico , Folhas de Planta/química , Ratos , Estreptozocina/toxicidade
18.
Biochem Pharmacol ; 174: 113785, 2020 04.
Artigo em Inglês | MEDLINE | ID: mdl-31887289

RESUMO

Regeneration of ß-cells by differentiation of pancreatic progenitor cells has the potential to fundamentally solve the problems of the loss of ß-cell function and mass during disease progression in both type 1 or 2 diabetes. Therefore, discovery of novel differentiation inducers to promote islet regeneration is of great significance. Pancreatic and duodenal homeobox1 (PDX-1) is a key transcription factor that promotes the development and maturation of pancreatic ß-cells. To screen potential novel small molecules for enhancing differentiation of PNAC-1 cells, a human pancreatic ductal cell lines into insulin-producing cells (IPCs), we developed a high-throughput screening method through fusing the PDX-1 promoter region with a luciferase reporter gene. We screened and identified that andrographolide named C1037 stimulates PDX-1 expression in both mRNA and protein level and significantly promotes PANC-1 cells differentiation into IPCs as compared with that of control cells. The therapeutic effect of C037 in Streptozotocin induced diabetic mouse model through differentiation of pancreatic ductal cells into insulin positive islets was also observed. Our study provides a novel method to screen compounds regulating the differentiation of pancreatic progenitor cells having the potential of enhancing islet regeneration for diabetes therapy.


Assuntos
Diferenciação Celular/efeitos dos fármacos , Diterpenos/farmacologia , Proteínas de Homeodomínio/metabolismo , Hipoglicemiantes/farmacologia , Secreção de Insulina/efeitos dos fármacos , Células Secretoras de Insulina/efeitos dos fármacos , Ductos Pancreáticos/efeitos dos fármacos , Transativadores/metabolismo , Andrographis/química , Animais , Técnicas de Cultura de Células , Diferenciação Celular/genética , Linhagem Celular , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Tipo 1/tratamento farmacológico , Diabetes Mellitus Tipo 1/metabolismo , Diterpenos/isolamento & purificação , Diterpenos/uso terapêutico , Expressão Gênica/efeitos dos fármacos , Teste de Tolerância a Glucose , Proteínas de Homeodomínio/genética , Humanos , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/uso terapêutico , Células Secretoras de Insulina/metabolismo , Masculino , Camundongos , Ductos Pancreáticos/metabolismo , Transativadores/genética
19.
Carbohydr Polym ; 228: 115381, 2020 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-31635744

RESUMO

Sargassum fusiforme polysaccharides, acidic water-soluble polysaccharides extract from Sargassum fusiforme, are mainly composed of alginic acid, fucoidan and laminaran. Alginic acid is carboxyl-containing polysaccharide formed by joining ß-D-mannuronic acid and α-L-guluronic acid through ß-(1→4)/α-(1→4) glycosidic bond. Fucoidan, a natural water-soluble sulfated heteropolysaccharide with fucose and sulfuric acid groups as the core structure, is mainly linked by L-fucose through α-(1→3) glycosidic bond and has the strongest biological activity. Laminaran is mainly composed of ß-D-glucose through ß-(1→3) glycosidic bond linkage. Sargassum fusiforme polysaccharides have a variety of pharmacological activities, including antioxidant, anti-tumor, promoting immunity, anti-aging, prompting bone growth, lowering blood glucose, anti-coagulation, anti-virus, anti-bacteria, anti-fatigue, promoting growth and development, and skin protection. These activities are closely related to the functions of fucoidan in Sargassum fusiforme polysaccharides, which fucoidan is able to strengthen immune system and antioxidation in human body. In this review, the composition, the isolation and purification, and the biological activities of Sargassum fusiforme polysaccharides are discussed and can bereference for further study.


Assuntos
Ácido Algínico , Glucanos , Polissacarídeos , Sargassum/metabolismo , Envelhecimento/efeitos dos fármacos , Ácido Algínico/química , Ácido Algínico/isolamento & purificação , Ácido Algínico/farmacologia , Animais , Bactérias/efeitos dos fármacos , Linhagem Celular , Carboidratos da Dieta/isolamento & purificação , Carboidratos da Dieta/farmacologia , Glucanos/química , Glucanos/isolamento & purificação , Glucanos/farmacologia , Humanos , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Camundongos , Neoplasias/tratamento farmacológico , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Polissacarídeos/farmacologia , Ratos , Vírus/efeitos dos fármacos
20.
J Sci Food Agric ; 100(2): 509-516, 2020 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-31487036

RESUMO

BACKGROUND: Emblica officinalis, known as amla in Ayurveda, has been used as a folk medicine to treat numerous pathological conditions, including diabetes. However, the novel extract of E. officinalis fruit extract (amla fruit extract, AFE, Saberry®) containing 100 g kg-1 ß-glucogallin along with hydrolyzable tannins has not yet been extensively studied for its antidiabetic potential. OBJECTIVE: The aim of this study was to investigate the antidiabetic and antioxidant activities of AFE and its stability during gastric stress as well as its thermostability. METHODS: The effect of AFE on the inhibition of pancreatic α-amylase and salivary α-amylase enzymes was studied using starch and yeast α-glucosidase enzyme using 4-nitrophenyl α-d-glucopyranoside as substrate. Further, 2,2-diphenyl-1-picrylhydrazyl radical scavenging and reactive oxygen species inhibition assay was performed against AFE. RESULTS: AFE potently inhibited the activities of α-amylase and α-glucosidase in a concentration-dependent manner with half maximal inhibitory concentration (IC50 ) values of 135.70 µg mL-1 and 106.70 µg mL-1 respectively. Furthermore, it also showed inhibition of α-glucosidase (IC50 562.9 µg mL-1 ) and dipeptidyl peptidase-4 (DPP-4; IC50 3770 µg mL-1 ) enzyme activities. AFE is a potent antioxidant showing a free radical scavenging activity (IC50 2.37 µg mL-1 ) and protecting against cellular reactive oxygen species (IC50 1.77 µg mL-1 ), and the effects elicited could be attributed to its phytoconstituents. CONCLUSION: AFE showed significant gastric acid resistance and was also found to be thermostable against wet heat. Excellent α-amylase, α-glucosidase, and DPP-4 inhibitory activities of AFE, as well as antioxidant activities, strongly recommend its use for the management of type 2 diabetes mellitus. © 2019 The Authors. Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.


Assuntos
Antioxidantes/química , Inibidores da Dipeptidil Peptidase IV/química , Frutas/química , Inibidores de Glicosídeo Hidrolases/química , Phyllanthus emblica/química , Extratos Vegetais/química , Antioxidantes/isolamento & purificação , Diabetes Mellitus Tipo 2/enzimologia , Dipeptidil Peptidase 4/química , Inibidores da Dipeptidil Peptidase IV/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Extratos Vegetais/isolamento & purificação , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/química , alfa-Glucosidases/química
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