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1.
Biomed Pharmacother ; 133: 111060, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33378969

RESUMO

The present study aims to reveal the compositions of Zhenshu TiaoZhi formula (FTZ) comprehensively, and investigate whether FTZ ameliorate glucolipid metabolism disorders in diabetic rats with the involvement of glucocorticoids in peripheral insulin-sensitive tissues. The fingerprint was established based on 11 batches of FTZ samples and chemical compostions of FTZ were identified by ultra performance liquid chromatography-time of flight/mass spectrometry (UPLC-TOF/MS). High-fat diet (HFD) and streptozotocin (STZ) induced diabetic rats were orally administrated with 3 and 6 g/kg body weight of FTZ for 8 weeks. Indices of glucolipid metabolism, including fasting blood glucose (FBG), fasting insulin, insulin resistance index (IRI) and blood lipids were evaluated after treatment of FTZ. The levels of HPA axis hormones were examined. Reverse transcription-polymerase chain reaction (RT-PCR) was adopted to investigate the relative mRNA expressions of 11ß-hydroxysteroid dehydrogenase 1 (11ß-HSD1) and glucolipid metabolic indicators. A reference fingerprint was established and 93 compounds of FTZ were tentatively identified. In vivo, FTZ treatment exerted antidiabetic and antidyslipidemic effects while decreased the level of corticotropin releasing hormone (CRH). 11ß-HSD1 mRNA showed similar trajectory in both liver, adipose and skeletal muscle tissues, which was up-regulated in diabetic group and ameliorated in FTZ groups. Furthermore, the expressions of glucose-6-phosphatase (G6Pase), phosphoenolpyruvate carboxykinase (PEPCK) and adipose triglyceride lipase (ATGL) were down-regulated in liver and skeletal muscle. These results elucidated the compositions of FTZ comprehensively and indicated its effect on ameliorating glucolipid metabolism of diabetic rats involved hypothalamus-pituitary-adrenal (HPA) axis homeostasis. Down-regulating 11ß-HSD1 in insulin-sensitive tissues might be a potential mechanism of FTZ in treating type 2 diabetes mellitus (T2DM).


Assuntos
Glicemia/efeitos dos fármacos , Diabetes Mellitus Experimental/tratamento farmacológico , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Hipoglicemiantes/análise , Hipoglicemiantes/farmacologia , Hipolipemiantes/farmacologia , Lipídeos/sangue , 11-beta-Hidroxiesteroide Desidrogenase Tipo 1/genética , 11-beta-Hidroxiesteroide Desidrogenase Tipo 1/metabolismo , Hormônio Adrenocorticotrópico/sangue , Animais , Biomarcadores/sangue , Glicemia/metabolismo , Cromatografia Líquida de Alta Pressão , Corticosterona/sangue , Hormônio Liberador da Corticotropina/sangue , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/induzido quimicamente , Hipolipemiantes/isolamento & purificação , Resistência à Insulina , Masculino , Espectrometria de Massas , Ratos Sprague-Dawley , Estreptozocina
2.
J Ethnopharmacol ; 265: 113188, 2021 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-32783985

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Stevia rebaudiana Bertoni is a perennial herb that belongs to the Asteraceae family. It is a natural sweetener plant known as "Sweet Leaf", "Sweet Herbs" and "Honey Leaf", which is estimated to be 300 times more sweetening than sugar cane. Stevia has been used as a traditional treatment for diabetes in many countries for hundreds of years. Several animal studies referred to the antihyperglycemic activity of stevia. However, the combined use of stevia with saxagliptin has not been studied so far, so this study has been done. The aim of the present study was to evaluate the antihyperglycemic effect of stevia alone and in combination with saxagliptin. MATERIALS AND METHODS: Diabetes was induced in rats by i.p. injection of streptozotocin and nicotinamide. Animals were divided into five groups, each contains eight rats. Group I: included negative controland group II: included diabetic control that received saline. Group III: included diabetic rats that received 400 mg/kg/day stevia aqueous extract. Group IV: included diabetic rats that received saxagliptin 10 mg/kg/day. Group V: included diabetic rats that received stevia 400 mg/kg + saxagliptin 10 mg/kg. Food and water intake were measured daily while body weight was measured weekly. After 3 weeks animals were sacrificed and blood and tissue samples were collected. Fasting blood glucose (FBG), serum insulin, serum dipeptidylepeptidase-4 (DPP-4), TC, TGs, LDL, HDL, GSH and MDA were measured in treated and control rats by colorimetric and ELISA methods. RESULTS: Both stevia and saxagliptin significantly reduced food, water intake, body weight and FBG. Stevia with saxagliptin produced more significant decrease in FBG. While serum insulin increased significantly in stevia, saxagliptin treated groups and their combination. Serum DPP-4 decreased significantly in all treated groups, concerning lipid profile, stevia and saxagliptin notably lowered TC, TGs, and LDL and increased HDL. Both stevia and saxagliptin remarkably decreased MDA and increased GSH compared to diabetic rats. In addition, stevia significantly improved the antidiabetic effects of saxagliptin. CONCLUSION: Stevia has an antihyperglycemic effect and could enhance the antidiabetic activity of saxagliptin. DPP-4 attenuation, antihyperlipidemic and antioxidant activity as well as improvement of insulin sensitivity may be involved in the antidiabetic action of stevia.


Assuntos
Adamantano/análogos & derivados , Diabetes Mellitus Experimental/tratamento farmacológico , Dipeptídeos/farmacologia , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Stevia/química , Adamantano/administração & dosagem , Adamantano/farmacologia , Animais , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Glicemia/efeitos dos fármacos , Diabetes Mellitus Experimental/fisiopatologia , Dipeptídeos/administração & dosagem , Interações Ervas-Drogas , Hipoglicemiantes/administração & dosagem , Hipoglicemiantes/isolamento & purificação , Hipolipemiantes/isolamento & purificação , Hipolipemiantes/farmacologia , Resistência à Insulina , Masculino , Niacinamida , Extratos Vegetais/administração & dosagem , Ratos , Ratos Wistar , Estreptozocina
3.
J Ethnopharmacol ; 265: 113210, 2021 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-32795501

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: One of the commonly prescribed 'anti-diabetic' polyherbal mixtures by European herbalists is made of Rubus fruticosus and Vaccinium myrtillus leaves, Potentilla erecta roots, Geum urbanum aerial parts and Phaseolus vulgaris pods. AIM OF THE STUDY: This study aimed to evaluate the phytochemical composition, antioxidant capacity, potential toxicity, hypoglycemic, hypolipidemic, nephroprotective and hepatoprotective activities of this polyherbal mixture decoction. MATERIALS AND METHODS: The phytochemical composition was evaluated using HPLC-UV. The antioxidant activity was assessed using the DPPH test. Potential toxicity was evaluated using the acute and sub-chronic oral toxicity method. Diabetes was induced in Wistar female rats with a single intraperitoneal injection of alloxan monohydrate (150 mg/kg). The animals whose blood glucose was >20 mmol/L for 14 consecutive days were considered diabetic. For the next 14 days, D-10 and D-20 groups were treated with the polyherbal mixture (10 and 20 g of dry plant material/kg, respectively). I and M were control groups treated with insulin glargine (13 IU/kg) and metformin (150 mg/kg), respectively. Healthy control (HC) and diabetic control (DC) groups were treated with water. The blood glucose level was measured on days 14, 21 and 28. Lipid profile analysis was done on day 28. Pancreas, kidney and liver histopathology was evaluated using the H&E and Masson's trichrome staining. The liver tissue was additionally tested for PAS-positive cells. RESULTS: The HPLC-UV analysis revealed the presence of quinic, gallic and caftaric acid, arbutin, rutin, trifolin, astragalin, hyperoside, isoquercetin and quercitrin. The antioxidant activity of the extract was higher than the reference's one (p < 0.01). Treatment with the polyherbal mixture (10 and 20 g/kg) has shown no toxic effects. No major decline in blood sugar was recorded in I and M groups compared to the DC one (22.86 ±â€¯2.58, 28.5 ±â€¯0.42 and 27.82 ±â€¯0.9 mmol/L, respectively). The polyherbal mixture lowered the blood glucose level to the normal value (8.64 ±â€¯4.09, 5.26 ±â€¯1.3 and 6.76 ±â€¯1.54 mmol/L in D-10, D-20 and HC groups, respectively). Furthermore, it decreased the levels of total cholesterol, triglycerides, VLDL, LDL, atherogenic and cardiovascular risk indices (p < 0.001) compared to the DC group. In addition, the extract restored histopathological changes of the pancreas, kidneys and liver to the healthy animal level. CONCLUSION: Treatment with the polyherbal mixture extract was more effective than the standard drugs (insulin and metformin) in the amelioration of hyperglycemia, hyperlipidemia, and histopathological changes of the pancreas, kidney and liver tissue.


Assuntos
Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Tipo 1/tratamento farmacológico , Hipolipemiantes/farmacologia , Extratos Vegetais/farmacologia , Animais , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Glicemia/efeitos dos fármacos , Diabetes Mellitus Experimental/fisiopatologia , Diabetes Mellitus Tipo 1/fisiopatologia , Feminino , Hiperglicemia/tratamento farmacológico , Hiperlipidemias/tratamento farmacológico , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Hipolipemiantes/isolamento & purificação , Insulina/farmacologia , Rim/efeitos dos fármacos , Rim/patologia , Fígado/efeitos dos fármacos , Fígado/patologia , Metformina/farmacologia , Pâncreas/efeitos dos fármacos , Pâncreas/patologia , Plantas Medicinais/química , Ratos , Ratos Wistar
4.
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
5.
Nutr Metab Cardiovasc Dis ; 30(9): 1590-1599, 2020 08 28.
Artigo em Inglês | MEDLINE | ID: mdl-32605883

RESUMO

BACKGROUND AND AIMS: Hypercholesterolemia and oxidative stress are two of the most important risk factors for atherosclerosis. The aim of the present work was to evaluate mandarin (Citrus reticulata) peel oil (MPO) in cholesterol metabolism and lipid synthesis, and its antioxidant capacity. METHODS AND RESULTS: Incubation of hepatic HepG2 cells with MPO (15-60 µL/L) reduced cholesterogenesis and saponifiable lipid synthesis, demonstrated by [14C]acetate radioactivity assays. These effects were associated with a decrease in a post-squalene reaction of the mevalonate pathway. Molecular docking analyses were carried out using three different scoring functions to examine the cholesterol-lowering property of all the components of MPO against lanosterol synthase. Docking simulations proposed that minor components of MPO monoterpenes, like alpha-farnesene and neryl acetate, as well the major component, limonene and its metabolites, could be partly responsible for the inhibitory effects observed in culture assays. MPO also decreased RAW 264.7 foam cell lipid storage and its CD36 expression, and prevented low-density lipoprotein (LDL) lipid peroxidation. CONCLUSION: These results may imply a potential role of MPO in preventing atherosclerosis by a mechanism involving inhibition of lipid synthesis and storage and the decrease of LDL lipid peroxidation.


Assuntos
Antioxidantes/farmacologia , Aterosclerose/prevenção & controle , Colesterol/metabolismo , Citrus , Dislipidemias/tratamento farmacológico , Células Espumosas/efeitos dos fármacos , Frutas , Hepatócitos/efeitos dos fármacos , Hipolipemiantes/farmacologia , Lipoproteínas LDL/metabolismo , Óleos Vegetais/farmacologia , Animais , Antioxidantes/isolamento & purificação , Aterosclerose/etiologia , Aterosclerose/metabolismo , Antígenos CD36/metabolismo , Citrus/química , Dislipidemias/complicações , Dislipidemias/metabolismo , Células Espumosas/metabolismo , Frutas/química , Células Hep G2 , Hepatócitos/metabolismo , Humanos , Hipolipemiantes/isolamento & purificação , Transferases Intramoleculares/antagonistas & inibidores , Transferases Intramoleculares/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Camundongos , Simulação de Acoplamento Molecular , Óleos Vegetais/isolamento & purificação , Células RAW 264.7
6.
Biomed Pharmacother ; 124: 109843, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31978768

RESUMO

Kaffir lime leaves and the rhizomes of galangal and lemongrass are the main ingredients in several Thai foods with desirable medicinal effects. Based on their beneficial activities, this study aimed to indicate the chemical properties and in vivo efficacy of a combination of the herbs at a 1:2:1 ratio in a water extract form. Its volatile constituents were analyzed by gas chromatography coupled with mass spectrometer, which mainly consists of eucalyptol, citronellal, and citral. Clinicohistopathological and electron microscopic studies demonstrated that the extract corrected blood cholesterol, LDL, HDL, and triglyceride levels similarly as simvastatin treatment in association with its antioxidative properties, as indicated by the levels of superoxide dismutase and malondialdehyde in serum and the increment of nuclear factor erythroid 2-related factor 2 levels in hepatocytes. Hepatitis was significantly less severe in rats fed the extract for 14 days than in simvastatin-treated rats. Regarding its immunomodulatory properties, the extract also accelerated hepatic resolution from steatohepatitis during hypercholesterolemia as indicated by the upregulation of vimentin, cytokeratin, and CD206+. Interestingly, liver mitochondria were also preserved in hypercholesterolemic rats treated with the extract in relation to their architecture and the expression of haloacid dehalogenase-like hydrolase domain-containing protein 3 as well as metabolic and energy regulators. Therefore, the study concluded that the water extract of kaffir lime leaves and the rhizomes of galangal and lemongrass has beneficial effects on blood cholesterol, the severity of steatohepatitis, and the maintenance of mitochondrial architecture via its antioxidative and immunomodulatory activities.


Assuntos
Hepatócitos/efeitos dos fármacos , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Extratos Vegetais/farmacologia , Alpinia/química , Animais , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Citrus/química , Cymbopogon/química , Hepatócitos/metabolismo , Hipercolesterolemia/tratamento farmacológico , Hipolipemiantes/isolamento & purificação , Hipolipemiantes/farmacologia , Lipídeos/sangue , Masculino , Mitocôndrias Hepáticas/efeitos dos fármacos , Mitocôndrias Hepáticas/metabolismo , Hepatopatia Gordurosa não Alcoólica/fisiopatologia , Ratos , Ratos Sprague-Dawley , Sinvastatina/farmacologia
7.
Nutrients ; 12(1)2020 Jan 20.
Artigo em Inglês | MEDLINE | ID: mdl-31968607

RESUMO

This study aimed to investigate the beneficial effects of seabuckthorn freeze-dried powder on high-fat diet-induced obesity and related lipid metabolism disorders, and further explored if this improvement is associated with gut microbiota. Results showed that seabuckthorn freeze-dried powder administration decreased body weight, Lee's index, adipose tissue weight, liver weight, and serum lipid levels. Moreover, treatment with seabuckthorn freeze-dried powder effectively reduced fat accumulation by modulating the relative expression of genes involved in lipid metabolism through down-regulation of encoding lipogenic and store genes, including SREBP-1c, PPAR-γ, ACC, and SCD1, and up-regulation of regulating genes of fatty acid oxidation, including HSL, CPT-1, and ACOX. Especially, seabuckthorn freeze-dried powder regulated the composition of gut microbiota, such as increasing the ratio of Firmicutes/Bacteroidetes, decreasing relative abundance of harmful bacteria (Desulfovibrio), and increasing relative abundance of beneficial bacteria (Akkermansia and Bacteroides). The changes of beneficial bacteria had a positive correlation with genes encoding lipolysis and a negative correlation with genes encoding lipid lipogenesis and store. The harmful bacteria were just the opposite. Besides, changes in gut microbiota had an obvious effect in the secretion of main metabolites-short-chain fatty acids (SCFAs), especially propionic acid. Thus, our results indicated that the seabuckthorn freeze-dried powder could ameliorate high-fat diet-induced obesity and obesity-associated lipid metabolism disorders by changing the composition and structure of gut microbiota.


Assuntos
Fármacos Antiobesidade/farmacologia , Dislipidemias/prevenção & controle , Microbioma Gastrointestinal/efeitos dos fármacos , Hippophae , Hipolipemiantes/farmacologia , Lipídeos/sangue , Obesidade/prevenção & controle , Extratos Vegetais/farmacologia , Ganho de Peso/efeitos dos fármacos , Adiposidade/efeitos dos fármacos , Animais , Fármacos Antiobesidade/isolamento & purificação , Biomarcadores/sangue , Modelos Animais de Doenças , Dislipidemias/sangue , Dislipidemias/genética , Dislipidemias/microbiologia , Liofilização , Regulação da Expressão Gênica , Hippophae/química , Hipolipemiantes/isolamento & purificação , Masculino , Camundongos Endogâmicos C57BL , Obesidade/sangue , Obesidade/genética , Obesidade/microbiologia , Extratos Vegetais/isolamento & purificação , Pós
8.
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
9.
Cardiovasc Toxicol ; 20(1): 82-99, 2020 02.
Artigo em Inglês | MEDLINE | ID: mdl-31183600

RESUMO

This study investigated whether the whole-plant aqueous extract of Crataegus aronia (C. aronia) could protect against or alleviate high-fat diet (HFD)-induced aortic vascular inflammation in rats by inhibiting the NLRP-3 inflammasome pathway and examined some mechanisms of action with respect to its antioxidant and hypolipidemic effects. Adult male Wistar rats were divided into five groups (n = 6/each): standard diet (10% fat) fed to control rats, control + C. aronia (200 mg/kg), HFD (40% fat), HFD + C. aronia, and HFD post-treated with C. aronia. The HFD was fed for 8 weeks and C. aronia was administered orally for 4 weeks. In addition, isolated macrophages from control rats were pre-incubated with two doses of C. aronia (25 and 50 µg/mL) with or without lipopolysaccharide (LPS) stimulation. Only in HFD-fed rats, co- and post-C. aronia therapy lowered circulatory levels of LDL-C and ox-LDL-c and aortic protein levels of LOX-1 and CD36. C. aronia also inhibited the nuclear accumulation of NF-κB and lowered protein levels of NLRP-3, caspase-1, and mature IL-1ß. In vitro, in the absence of ox-LDL-c, C. aronia led to reduced nuclear levels of NF-κB, ROS generation, and protein NLRP-3 levels, in both LPS-stimulated and unstimulated macrophages, in a dose-dependent manner. However, protein levels of LOX-1 were not affected by C. aronia in unstimulated cells. In conclusion, C. aronia inhibits the NLRP-3 inflammasome pathway, induced by HFD feeding in the aorta of rats, mainly by its hypolipidemic effect and in vitro, in LPS-stimulated macrophages, by its antioxidant effect.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Aorta/efeitos dos fármacos , Aortite/prevenção & controle , Aterosclerose/prevenção & controle , Hipolipemiantes/farmacologia , Inflamassomos/antagonistas & inibidores , Proteína 3 que Contém Domínio de Pirina da Família NLR/antagonistas & inibidores , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Antioxidantes/isolamento & purificação , Aorta/imunologia , Aorta/metabolismo , Aorta/patologia , Aortite/etiologia , Aortite/imunologia , Aortite/metabolismo , Aterosclerose/etiologia , Aterosclerose/imunologia , Aterosclerose/metabolismo , Células Cultivadas , Crataegus , Dieta Hiperlipídica , Modelos Animais de Doenças , Hipolipemiantes/isolamento & purificação , Inflamassomos/imunologia , Inflamassomos/metabolismo , Mediadores da Inflamação/metabolismo , Macrófagos Peritoneais/efeitos dos fármacos , Macrófagos Peritoneais/imunologia , Macrófagos Peritoneais/metabolismo , Masculino , Proteína 3 que Contém Domínio de Pirina da Família NLR/imunologia , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/isolamento & purificação , Ratos Wistar , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais/efeitos dos fármacos
10.
Mar Drugs ; 17(10)2019 Sep 29.
Artigo em Inglês | MEDLINE | ID: mdl-31569458

RESUMO

Fungal marine microorganisms are a valuable source of bioactive natural products. Fungal secondary metabolites mainly comprise alkaloids, terpenoids, peptides, polyketides, steroids, and lactones. Proteins and peptides from marine fungi show minimal human toxicity and less adverse effects comparable to synthetic drugs. This review summarizes the chemistry and the biological activities of peptides that were isolated and structurally elucidated from marine fungi. Relevant fungal genera including Acremonium, Ascotricha, Aspergillus, Asteromyces, Ceratodictyon, Clonostachys, Emericella, Exserohilum, Microsporum, Metarrhizium, Penicillium, Scytalidium, Simplicillium, Stachylidium, Talaromyces, Trichoderma, as well as Zygosporium were extensively reviewed. About 131 peptides were reported from these 17 genera and their structures were unambiguously determined using 1D and 2D NMR (one and two dimensional nuclear magnetic resonance) techniques in addition to HRMS (high resolution mass spectrometry). Marfey and Mosher reactions were used to confirm the identity of these compounds. About 53% of the isolated peptides exhibited cytotoxic, antimicrobial, and antiviral activity, meanwhile, few of them showed antidiabetic, lipid lowering, and anti-inflammatory activity. However 47% of the isolated peptides showed no activity with respect to the examined biological activity and thus required further in depth biological assessment. In conclusion, when searching for bioactive natural products, it is worth exploring more peptides of fungal origin and assessing their biological activities.


Assuntos
Organismos Aquáticos/química , Produtos Biológicos/farmacologia , Fungos/química , Peptídeos/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Antivirais/química , Antivirais/isolamento & purificação , Antivirais/farmacologia , Produtos Biológicos/química , Produtos Biológicos/isolamento & purificação , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Hipolipemiantes/química , Hipolipemiantes/isolamento & purificação , Hipolipemiantes/farmacologia , Peptídeos/química , Peptídeos/isolamento & purificação
11.
Nutrients ; 11(9)2019 Aug 22.
Artigo em Inglês | MEDLINE | ID: mdl-31443489

RESUMO

Blood lipids are an important biomarker of cardiovascular health and disease. Among the lipid biomarkers that have been widely used to monitor and predict cardiovascular diseases (CVD), elevated LDL and low HDL cholesterol (C), as well as elevated triglyceride-rich lipoproteins, deserve special attention in their predictive abilities, and thus have been the targets of several therapeutic and dietary approaches to improving lipid profiles. Among natural foods and nutraceuticals, dietary berries are a rich source of nutrients, fiber, and various types of phytochemicals. Berries as whole fruits, juices, and purified extracts have been shown to lower total and LDL-C, and increase HDL-C in clinical studies in participants with elevated blood lipids, type 2 diabetes or metabolic syndrome. This short review aimed to further discuss the mechanisms and magnitude of the lipid-lowering effects of dietary berries, with emphasis on reported clinical studies. Based on the emerging evidence, colorful berry fruits may thus be included in a healthy diet for the prevention and management of CVD.


Assuntos
Doenças Cardiovasculares/prevenção & controle , Diabetes Mellitus Tipo 2/dietoterapia , Dieta Saudável , Suplementos Nutricionais , Sucos de Frutas e Vegetais , Frutas/química , Hiperlipidemias/dietoterapia , Hipolipemiantes/administração & dosagem , Lipídeos/sangue , Lipoproteínas/sangue , Síndrome Metabólica/dietoterapia , Compostos Fitoquímicos/administração & dosagem , Animais , Biomarcadores/sangue , Doenças Cardiovasculares/sangue , Doenças Cardiovasculares/diagnóstico , Doenças Cardiovasculares/epidemiologia , Diabetes Mellitus Tipo 2/sangue , Diabetes Mellitus Tipo 2/diagnóstico , Diabetes Mellitus Tipo 2/epidemiologia , Humanos , Hiperlipidemias/sangue , Hiperlipidemias/diagnóstico , Hiperlipidemias/epidemiologia , Hipolipemiantes/isolamento & purificação , Síndrome Metabólica/sangue , Síndrome Metabólica/diagnóstico , Síndrome Metabólica/epidemiologia , Compostos Fitoquímicos/isolamento & purificação
12.
Artigo em Inglês | MEDLINE | ID: mdl-31233943

RESUMO

In the present study, a simple and efficient method based on orthogonal experimental design and macroporous resin chromatography was established for the first time for enrichment of polymethoxyflavones (PMFs) from the peels of Citrus reticulata 'Chachi' (CRC). The optimum conditions of extraction and enrichment process were as follows: use of a liquid to solid ratio of 1 to 14, two-hour extraction time repeated twice with 70% ethanol; use of HPD-450 macroporous resin, wash solvent of purified water and 25% aqueous ethanol, and 70% aqueous ethanol as desorption solvent. The purity of PMFs in the resulting extract reached 62.26%. Our data indicate that the PMFs purified could potently alleviate high-fat diet-induced hyperlipidaemia. The PMFs were nontoxic as determined by acute toxicity test. The method established was suitable for large-scale separation of PMFs from CRC peels and the PMFs might be developed as an anti-hyperlipidaemia agent or dietary supplement.


Assuntos
Cromatografia/métodos , Citrus/química , Flavonas/isolamento & purificação , Hipolipemiantes/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Animais , Feminino , Flavonas/administração & dosagem , Flavonas/química , Frutas/química , Humanos , Hiperlipidemias/tratamento farmacológico , Hipolipemiantes/administração & dosagem , Hipolipemiantes/química , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química
13.
Biomed Pharmacother ; 115: 108907, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31071507

RESUMO

Plantaginis semen, the dried mature seed of Plantago asiatica L. or Plantago deprdssa Willd., has a prominent effect on the treatment of obesity, type 2 diabetes and lipid disorders, however, its clinical application is limited due to inadequate in-depth mechanism exploration and incomplete discussion of action targets of its in vivo. Therefore, an untargeted metabolomics approach was firstly applied to study the serum metabolic differences in mice. Metabolomics analysis was performed using ultra performance liquid chromatography quadrupole time of flight mass spectrometry (UPLC-QTOF-MS) together with multivariate statistical data analysis. The results showed that Plantaginis semen can mainly improve blood lipids, some degree in blood glucose and insulin levels in high-fat mice, in addition, the phenotype of liver and fat stained sections demonstrated remarkable results. A total of 22 metabolites involved in arachidonic acid, glycerophospholipid, glycosphingolipid, linoleate, Omega-3 fatty acid, phosphatidylinositol phosphate and tyrosine metabolisms were identified. In further, it was found that the possible mechanisms of Plantaginis semen on hyperlipidemic mice lied in the biosynthesis of thyroxine, biological effects of enzymes of phospholipase A2 activity, glucosylceramide synthase and inositol essential enzyme 1α, genes expressions of fatty acid metabolism and inflammation. Serum metabolomics revealed that Plantaginis semen could cure the organism disease via regulating multiple metabolic pathways which will be helpful for understanding the mechanism of this herb and providing references for better applications of it in clinic, even researches on other TCMs.


Assuntos
Medicamentos de Ervas Chinesas/uso terapêutico , Hiperlipidemias/tratamento farmacológico , Hipolipemiantes/uso terapêutico , Metabolismo dos Lipídeos/efeitos dos fármacos , Plantago/química , Sementes/química , Tecido Adiposo/efeitos dos fármacos , Tecido Adiposo/metabolismo , Tecido Adiposo/patologia , Animais , Cromatografia Líquida de Alta Pressão , Dieta Hiperlipídica , Modelos Animais de Doenças , Medicamentos de Ervas Chinesas/isolamento & purificação , Hiperlipidemias/sangue , Hiperlipidemias/metabolismo , Hipolipemiantes/isolamento & purificação , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Masculino , Espectrometria de Massas , Metabolômica , Camundongos Endogâmicos C57BL
14.
J Agric Food Chem ; 67(18): 5278-5288, 2019 May 08.
Artigo em Inglês | MEDLINE | ID: mdl-30964673

RESUMO

Diabetes and its complications are one of the most concerned metabolic diseases worldwide and threaten human health severely. Hypoglycemic and hypolipidemic effects of glucomannan extracted from konjac on high-fat diet and streptozocin-induced type 2 diabetic rats were evaluated in this study. Administration of konjac glucomannan significantly decreased the levels of fasting blood glucose, serum insulin, glucagon-like peptide 1, and glycated serum protein. The concentrations of serum lipids, including total cholesterol, triacylglycerols, low-density lipoprotein cholesterol, and non-esterified fatty acid, were notably reduced by konjac glucomannan treatment. In addition, antioxidant capacity, pancreatic injury, and adipose cell hypertrophy were ameliorated by konjac glucomannan administration in type 2 diabetic rats. Besides, ultra performance liquid chromatography-quadrupole time-of-flight mass spectrometry-based lipidomics analysis was used to explore the improvement of lipid metabolic by konjac glucomannan treatment. The disturbance of glycerolipid (diacylglycerol, monoacylglycerol, and triacylglycerol), fatty acyl (acylcarnitine and hydroxyl fatty acid), sphingolipid (ceramide and sphingomyelin), and glycerophospholipid (phosphatidylcholine) metabolism were attenuated by the glucomannan treatment. This study provided new insights for investigating the anti-diabetic effects of konjac glucomannan and suggests that konjac glucomannan may be a promising nutraceutical for treating type 2 diabetes.


Assuntos
Amorphophallus/química , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/administração & dosagem , Hipolipemiantes/administração & dosagem , Mananas/administração & dosagem , Animais , Glicemia/metabolismo , Diabetes Mellitus Tipo 2/sangue , Diabetes Mellitus Tipo 2/etiologia , Diabetes Mellitus Tipo 2/genética , Dieta Hiperlipídica/efeitos adversos , Ácidos Graxos não Esterificados/sangue , Peptídeo 1 Semelhante ao Glucagon/sangue , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Hipolipemiantes/química , Hipolipemiantes/isolamento & purificação , Insulina/sangue , Masculino , Mananas/química , Mananas/isolamento & purificação , Ratos , Ratos Wistar
15.
Br J Clin Pharmacol ; 85(7): 1607-1611, 2019 07.
Artigo em Inglês | MEDLINE | ID: mdl-30875097

RESUMO

It has been claimed that Nigella sativa seeds (NSS), also known as black cumin, have antidiabetic and lipid-lowering properties. Our pilot study investigated the effects of powdered NSS on insulin secretion and lipid profile in healthy male volunteers. We conducted a double-blind, randomized, placebo-controlled 4-week trial in 30 subjects, receiving NSS powder (1 g/day) or placebo orally (15 subjects/group). Insulin secretion as determined by the hyperglycaemic clamp technique, insulin sensitivity as well as cholesterol and triglycerides serum concentrations, were measured before and after treatment. NSS powder administration was clinically well tolerated. It did not modify fasting glycaemia and insulinaemia, and was ineffective on glucose-induced insulin secretion and insulin sensitivity. No significant changes on serum lipids were observed after treatment in any treatment groups, nor between the two treatment groups. However, in the treated group only, there was a significant correlation between total cholesterol change after treatment and its baseline level (r = -0.71, P = 0.006, n = 13), and between low-density lipoprotein (LDL) cholesterol change after treatment and its baseline level (r = -0.74, P = 0.004, n = 13). No such correlations were found for high-density lipoprotein (HDL) cholesterol, and for triglycerides. These results do not confirm any NSS effect on glucose regulation; however, they suggest that NSS powder may be of interest in lowering lipid concentrations in hyperlipidaemic subjects.


Assuntos
Secreção de Insulina/efeitos dos fármacos , Lipídeos/sangue , Nigella sativa/química , Extratos Vegetais/farmacologia , Adulto , Método Duplo-Cego , Glucose/metabolismo , Humanos , Hipolipemiantes/efeitos adversos , Hipolipemiantes/isolamento & purificação , Hipolipemiantes/farmacologia , Masculino , Projetos Piloto , Extratos Vegetais/efeitos adversos , Sementes , Adulto Jovem
16.
Pak J Pharm Sci ; 32(1(Special)): 383-389, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30852474

RESUMO

.This study aimed to investigate the hypolipidemic and antioxidant activities of volatile oils from Michelia martini Levl. The antioxidant property of volatile oils from Michelia martini in vitro was investigated by establishment of various systems. High fat diet induced rats were used to assess the hypolipidemic and antioxidant activities of Michelia martini volatile oils in vivo. The level of total cholesterol, triglycerides, high density lipoprotein cholesterol, low density lipoprotein cholesterol, alanine transaminase, aspartate aminotransferase, alkaline phosphatase and gamma-glutamyl transpeptidase in serum, and the activities of catalase, malondialdehyde, super oxide dismutase and glutathione in liver of rats were assayed by standard procedures. Our results showed that Michelia martini exhibits strong hypolipidemic and antioxidant activities both in vitro and vivo. Our data were also supplemented with histopathological studies on liver tissues and aorta sections of rats.


Assuntos
Antioxidantes/farmacologia , Hipolipemiantes/farmacologia , Magnoliaceae/química , Óleos Voláteis/farmacologia , Óleos Vegetais/farmacologia , Anfotericina B/toxicidade , Animais , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/química , Células CHO , Cricetulus , Dieta Hiperlipídica/efeitos adversos , Relação Dose-Resposta a Droga , Hiperlipidemias/sangue , Hiperlipidemias/prevenção & controle , Hipolipemiantes/isolamento & purificação , Lipídeos/sangue , Masculino , Óleos Voláteis/isolamento & purificação , Picratos/química , Folhas de Planta/química , Óleos Vegetais/isolamento & purificação , Ratos Sprague-Dawley
17.
Molecules ; 24(4)2019 Feb 17.
Artigo em Inglês | MEDLINE | ID: mdl-30781592

RESUMO

Artemisia integrifolia L (Compositae) is a medicinal and edible plant. To investigate its antihyperlipidemic effect, a crude lipophilic extract and the composing compounds were isolated and fractioned from the petroleum ether extract of aerial parts of A. integrifolia using column chromatography on silica gel. The anti-hyperlipidemia effect was studied in a rat model of acute hyperlipidemia, which was induced by triton WR-1339. A new compound, integrinol (4), together with nine known compounds, namely chamazulene (1), acetylenes (E)-2 (2), acetylenes (E)-3 (3), eugenol (5), palmitic acid (6), oleic acid (7), linoleic acid (8), linolenic acid (9) and 12,13-epoxylinolenic acid were isolated from the crude lipophilic extract of A. integrifolia. The LD50 value of the crude extract was more than 4g/kg. In Triton WR-1339-induced acute hyperlipidemia model, the crude lipophilic extract (200 mg/kg) significantly reduced total cholesterol (TC) by 70% (p ≤ 0.01) and triglycerides (TGs) by 94% (p ≤ 0.001). The fractioned compounds, such as chamazulene (1), acetylene-2 (2), and linolenic acid (9), used at 4 mg/kg dose, also significantly decreased the concentrations of TC (32%, 33% and 64%, respectively) and TGs (48%, 33% and 93%, respectively). These compounds (i.e., chamazulene, acetylenes (E)-2, and linolenic acid) were considered to be responsible for the bioactive antihyperlipidemic effect. In conclusion, the crude lipid extract of Artemisia integrifolia L could be used as a potential treatment to avert hyperlipidemia. Further studies to confirm these results in other models of hyperlipidemia (e.g., diet-induced obesity) are warranted.


Assuntos
Artemisia/química , Interações Hidrofóbicas e Hidrofílicas , Hipolipemiantes/química , Hipolipemiantes/farmacologia , Fracionamento Químico , Hipolipemiantes/isolamento & purificação , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Compostos Fitoquímicos/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia
18.
J Nat Prod ; 82(2): 412-416, 2019 02 22.
Artigo em Inglês | MEDLINE | ID: mdl-30724086

RESUMO

Euphorhelipanes A (1) and B (2), two Euphorbia diterpenoids with a new 4-(5,5-dimethylheptan-2-yl)-2,7-dimethylbicyclo[4.3.0]nonane skeleton, were isolated from a 95% ethanol extract of the whole plants of Euphorbia helioscopia. Their structures were elucidated by spectroscopic data analysis, quantum chemical calculations, and single-crystal X-ray diffraction data. Compounds 1 and 2 represent the first examples of Euphorbia diterpenoids with a 5/6 fused carbon ring system, and their plausible biosynthetic pathways originating from jatrophanes are proposed. Compounds 1 and 2 showed a triglyceride-lowering effect in oleic-acid-stimulated HuH7 cells at concentrations of 1-50 µM.


Assuntos
Diterpenos/isolamento & purificação , Euphorbia/química , Hipolipemiantes/isolamento & purificação , Triglicerídeos/sangue , Linhagem Celular Tumoral , Diterpenos/química , Diterpenos/farmacologia , Humanos , Hipolipemiantes/química , Hipolipemiantes/farmacologia , Ácido Oleico/farmacologia
19.
Artigo em Inglês | MEDLINE | ID: mdl-30727935

RESUMO

OBJECTIVE: Traditionally prepared infusions and decoctions are commonly used in the management of diabetes mellitus, in southern Nigeria; one of such is the aqueous extract of the sclerotia of Pleurotus tuberregium ("usu" milk). In this study, the effects of the extract on the body weights, tissue/ organ weights, fasting blood glucose, blood/plasma lipid profiles and atherogenic indices were investigated in normal and alloxan-induced diabetic rabbits. METHODS: Diabetes mellitus was induced by the injection of alloxan (120 mg/kg body weight) via the marginal ear vein. The extract was administered orally at 100, 200 and 300 mg/kg to normal and diabetic rabbits; while metformin was administered at 50 mg/kg. The crude extract was analyzed by gas chromatography, coupled to flame ionization detector. RESULTS: Thirty-one known flavonoids were detected, consisting mainly of isoquercetin (28.5%), luteolin (24.3%), quercetin (18.8%) and kaempferol (11.3%). Sitosterol (82.0%) and stigmasterol (12.5%) were the most abundant of the seven phytosterols detected. Compared to the diabetic control, the treatment significantly (p<0.05) lowered the weights of the kidney and liver, as well as the levels of blood glucose and triglyceride, plasma VLDL, LDL and non-HDL cholesterol, atherogenic index of plasma, cardiac risk ratio, atherogenic coefficient and Castelli's risk index II. It, however, significantly (p<0.05) increased plasma HDL cholesterol, without significantly affecting blood total cholesterol levels. CONCLUSION: This study showed that the extract was hypoglycemic, and improved lipid profile and atherogenic indices, thus highlighting its cardioprotective potential, thereby supporting its use in the management of diabetes mellitus.


Assuntos
Glicemia/efeitos dos fármacos , Diabetes Mellitus Experimental/tratamento farmacológico , Flavonoides/farmacologia , Hipoglicemiantes/farmacologia , Hipolipemiantes/farmacologia , Extratos Vegetais/farmacologia , Pleurotus , Sitosteroides/farmacologia , Aloxano , Animais , Biomarcadores/sangue , Glicemia/metabolismo , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/induzido quimicamente , Jejum/sangue , Flavonoides/isolamento & purificação , Hipoglicemiantes/isolamento & purificação , Hipolipemiantes/isolamento & purificação , Lipídeos/sangue , Extratos Vegetais/isolamento & purificação , Pleurotus/química , Coelhos , Sitosteroides/isolamento & purificação
20.
Food Res Int ; 116: 676-686, 2019 02.
Artigo em Inglês | MEDLINE | ID: mdl-30716995

RESUMO

Different oregano species have been traditionally used as infusions in folk medicine. Oregano medicinal properties, such as antioxidant and anti-inflammatory, have been partially attributed to its polyphenolic content. However, information regarding bioaccessibility of oregano polyphenols is limited. Cell-based antioxidant activity, and in vitro hypoglycemic, and hypolipidemic properties of polyphenolic extracts from three species of oregano species, namely, Hedeoma patens (HP), Lippia graveolens (LG) and Lippia palmeri (LP), subjected to simulated gastrointestinal digestion were evaluated. LC-TOF-MS analysis of HP, LG and LP allowed the identification of 9 flavonoids and 6 hydroxycinnamic acid derivatives with nutraceutical significance. Oregano polyphenolic extracts and digests from HP, LG, and LP exhibited cellular antioxidant capacity, hypoglycemic and hypolipidemic properties. Altogether, our results suggest that HP, LG and LP polyphenols exhibit potential for use as hypoglycemic, hypolipidemic, and antioxidant agents.


Assuntos
Antioxidantes/farmacologia , Digestão , Inibidores de Glicosídeo Hidrolases/farmacologia , Hipolipemiantes/farmacologia , Lipase/antagonistas & inibidores , Origanum/química , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Antioxidantes/isolamento & purificação , Células CACO-2 , Cromatografia Líquida de Alta Pressão , Ácido Gástrico/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Humanos , Hipolipemiantes/isolamento & purificação , Secreções Intestinais/química , Lipase/metabolismo , Oxirredução , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/isolamento & purificação , Polifenóis/isolamento & purificação , Espectrometria de Massas por Ionização por Electrospray
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