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1.
Einstein (Sao Paulo) ; 18: eAO4876, 2020.
Artigo em Inglês, Português | MEDLINE | ID: mdl-31576909

RESUMO

OBJECTIVE: To investigate the effects of sericin extracted from silkworm Bombyx mori cocoon on morphophysiological parameters in mice with obesity induced by high-fat diet. METHODS: Male C57Bl6 mice aged 9 weeks were allocated to one of two groups - Control and Obese, and fed a standard or high-fat diet for 10 weeks, respectively. Mice were then further subdivided into four groups with seven mice each, as follows: Control, Control-Sericin, Obese, and Obese-Sericin. The standard or high fat diet was given for 4 more weeks; sericin (1,000mg/kg body weight) was given orally to mice in the Control-Sericin and Obese-Sericin Groups during this period. Weight gain, food intake, fecal weight, fecal lipid content, gut motility and glucose tolerance were monitored. At the end of experimental period, plasma was collected for biochemical analysis. Samples of white adipose tissue, liver and jejunum were collected and processed for light microscopy analysis; liver fragments were used for lipid content determination. RESULTS: Obese mice experienced significantly greater weight gain and fat accumulation and had higher total cholesterol and glucose levels compared to controls. Retroperitoneal and periepididymal adipocyte hypertrophy, development of hepatic steatosis, increased cholesterol and triglyceride levels and morphometric changes in the jejunal wall were observed. CONCLUSION: Physiological changes induced by obesity were not fully reverted by sericin; however, sericin treatment restored jejunal morphometry and increased lipid excretion in feces in obese mice, suggesting potential anti-obesity effects.


Assuntos
Fármacos Antiobesidade/uso terapêutico , Dieta Hiperlipídica , Obesidade/tratamento farmacológico , Sericinas/uso terapêutico , Tecido Adiposo/patologia , Animais , Fármacos Antiobesidade/farmacologia , Peso Corporal/efeitos dos fármacos , Colesterol/análise , Dieta Hiperlipídica/efeitos adversos , Ingestão de Alimentos/efeitos dos fármacos , Fígado Gorduroso/patologia , Trânsito Gastrointestinal/efeitos dos fármacos , Teste de Tolerância a Glucose , Fígado/metabolismo , Masculino , Camundongos Endogâmicos C57BL , Camundongos Obesos , Obesidade/etiologia , Obesidade/fisiopatologia , Reprodutibilidade dos Testes , Sericinas/farmacologia , Fatores de Tempo , Resultado do Tratamento , Triglicerídeos/análise , Ganho de Peso/efeitos dos fármacos
2.
Chem Biodivers ; 16(10): e1900347, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31532890

RESUMO

Catechins in green tea are well-known to be effective in reducing the risk of obesity. The purpose of this study was to elucidate the effects of catechins present in green tea on adipocyte differentiation and mature adipocyte metabolism. Treatment of 3T3-L1 mouse adipocyte during differentiation adipocytes with (-)-epigallocatechin (EGC) and gallic acid (GA) resulted in dose-dependent inhibition of adipogenesis. Specifically, EGC increased adiponectin and uncoupling protein 1 (UCP1) transcription in mature adipocytes. Transcription levels of adipose triglyceride lipase (ATGL) and hormone-sensitive lipase (HSL) were not significantly impacted by either of the compounds. These results suggest that the EGC is the most effective catechin having anti-obesity activity. Finally, EGC is an attractive candidate component for remodeling obesity.


Assuntos
Tecido Adiposo Marrom/efeitos dos fármacos , Fármacos Antiobesidade/farmacologia , Catequina/análogos & derivados , Células 3T3-L1 , Tecido Adiposo Marrom/metabolismo , Animais , Fármacos Antiobesidade/química , Fármacos Antiobesidade/isolamento & purificação , Catequina/química , Catequina/isolamento & purificação , Catequina/farmacologia , Diferenciação Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Relação Dose-Resposta a Droga , Camundongos , Estrutura Molecular , Relação Estrutura-Atividade , Chá/química
3.
Eur J Med Chem ; 181: 111565, 2019 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-31387062

RESUMO

The human Carbonic anhydrases (hCA) VA and VB play a key role in ureagenesis, gluconeogenesis, lipogenesis and in the metabolism regulation, thus representing highly popular drug targets. Albeit several hCA inhibitors have been designed and are currently in clinical use, serious drug interactions have been reported due to their poor selectivity. In this perspective, the drug repurposing approach could be a useful tool in order to investigate the drug promiscuity/polypharmacology profile. In this study, virtual screening techniques and in vitro assays were combined to identify novel selective hCA VA inhibitors from among around 94000 compounds. The docking analysis highlighted 12 promising best hits, biologically characterized in terms of their hCA VA inhibitory activity. Interestingly, among them, the anticancer agents fludarabine and lenvatinib and the antiepileptic rufinamide were able to selectively inhibit the enzyme activity in the micromolar range, while a pyrido-indole derivative, the homovanillic acid sulfate and the desacetyl metabolite of the antibacterial cephapirin in the nanomolar range.


Assuntos
Fármacos Antiobesidade/farmacologia , Inibidores da Anidrase Carbônica/farmacologia , Reposicionamento de Medicamentos , Obesidade/tratamento farmacológico , Fármacos Antiobesidade/química , Anidrase Carbônica I/antagonistas & inibidores , Anidrase Carbônica I/metabolismo , Anidrase Carbônica II/antagonistas & inibidores , Anidrase Carbônica II/metabolismo , Inibidores da Anidrase Carbônica/química , Projeto Auxiliado por Computador , Descoberta de Drogas , Humanos , Simulação de Acoplamento Molecular , Obesidade/metabolismo
4.
Chem Commun (Camb) ; 55(61): 8919-8922, 2019 Aug 07.
Artigo em Inglês | MEDLINE | ID: mdl-31270526

RESUMO

Cancer development is often associated with lipid metabolic reprogramming, including aberrant lipid accumulation. We create novel paradigms endowed with dual functions of anticancer activity and inhibition of lipid accumulation by conjugating the natural product quercetin and synthetic alkylphospholipid drugs, and harnessing the biomedical effects of both. These conjugates offer fresh perspectives in the search for anticancer candidates.


Assuntos
Fármacos Antiobesidade/farmacologia , Antineoplásicos/farmacologia , Éteres Fosfolipídicos/farmacologia , Fosforilcolina/análogos & derivados , Quercetina/análogos & derivados , Quercetina/farmacologia , Fármacos Antiobesidade/síntese química , Antineoplásicos/síntese química , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos , Gotículas Lipídicas/metabolismo , Receptores X do Fígado/metabolismo , PPAR gama/metabolismo , Éteres Fosfolipídicos/síntese química , Fosforilcolina/síntese química , Fosforilcolina/farmacologia , Poli(ADP-Ribose) Polimerases/metabolismo , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Quercetina/síntese química , Transdução de Sinais/efeitos dos fármacos
5.
BMC Complement Altern Med ; 19(1): 100, 2019 May 08.
Artigo em Inglês | MEDLINE | ID: mdl-31068163

RESUMO

BACKGROUND: Obesity is a risk factor for many diseases including diabetes, cancer, arthritis, and cardiovascular diseases. Angiogenesis nourishes adipose tissues and contributes to obesity; it can be prevented by suppressing the expression of associated signaling molecules. Natural products have garnered attention owing to their safety and efficacy in treating several diseases, including obesity. METHODS: Crude Microcystins were extracted from the blooming Microcystis aeruginosa under stress conditions, by ultrasonication following by solvent extraction. The microcystin extract was evaluated for its potential of inhibiting angiogenesis and adipogenesis. The antiangiogenic activity of the microcystins extract was investigated using human umbilical vein endothelial cells (HUVECs), and its anti-obesity activity was determined in vitro by quantification of the accumulated lipids in mouse 3 T3-L1 cells via Oil Red O staining method. RESULTS: The microcystin extract suppressed HUVECs proliferation and tubes formation in Matrigel in a dose-dependent manner. RT-PCR analysis revealed the downregulation of the mRNA expression of angiogenesis-related signaling molecules, such as PI3K, ß-catenin, vascular endothelial growth factor receptor-2 (VEGFR-2), vascular endothelial-cadherin, Akt1, and NF-κB. Additionally, it inhibited the differentiation of premature 3 T3 cells and lipid accumulation in a dose-dependent manner. It suppressed adipogenesis and lipogenesis by reducing the expression level of peroxisome proliferator-activated receptor γ, CCAAT/enhancer binding protein α, and sterol regulatory element-binding protein. CONCLUSIONS: Crude microcystin exerts anti-angiogenic and anti-obesity effects due to the inhibitory effects on the genes expression of associated signaling molecules and transcriptional factors.


Assuntos
Adipogenia/efeitos dos fármacos , Inibidores da Angiogênese/farmacologia , Fármacos Antiobesidade/farmacologia , Microcistinas/farmacologia , Microcystis/química , Células 3T3-L1 , Adipócitos/efeitos dos fármacos , Adipócitos/metabolismo , Animais , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Células Endoteliais da Veia Umbilical Humana , Humanos , Lipogênese/efeitos dos fármacos , Lipogênese/genética , Camundongos , Neovascularização Patológica/metabolismo
6.
Mar Drugs ; 17(5)2019 May 27.
Artigo em Inglês | MEDLINE | ID: mdl-31137922

RESUMO

Fucoxanthin (FX), a marine carotenoid found in macroalgae and microalgae, exhibits several beneficial effects to health. The anti-obesity activity of FX is well documented, but FX has not been mass-produced or applied extensively or commercially because of limited availability of raw materials and complex extraction techniques. In this study, we investigated the anti-obesity effect of standardized FX powder (Phaeodactylum extract (PE)) developed from microalga Phaeodactylum tricornutum as a commercial functional food. The effects of PE on adipogenesis inhibition in 3T3-L1 adipocytes and anti-obesity in high-fat diet (HFD)-fed C57BL/6J mice were evaluated. PE and FX dose-dependently decreased intracellular lipid contents in adipocytes without cytotoxicity. In HFD-fed obese mice, PE supplementation for six weeks decreased body weight, organ weight, and adipocyte size. In the serum parameter analysis, the PE-treated groups showed attenuation of lipid metabolism dysfunction and liver damage induced by HFD. In the liver, uncoupling protein-1 (UCP1) upregulation and peroxisome proliferator activated receptor γ (PPARγ) downregulation were detected in the PE-treated groups. Additionally, micro computed tomography revealed lower fat accumulation in PE-treated groups compared to that in the HFD group. These results indicate that PE exerts anti-obesity effects by inhibiting adipocytic lipogenesis, inducing fat mass reduction and decreasing intracellular lipid content, adipocyte size, and adipose weight.


Assuntos
Adipogenia/efeitos dos fármacos , Fármacos Antiobesidade/farmacologia , Produtos Biológicos/farmacologia , Estramenópilas/química , Xantofilas/farmacologia , Adipócitos/efeitos dos fármacos , Animais , Fármacos Antiobesidade/isolamento & purificação , Dieta Hiperlipídica , Alimento Funcional/análise , Camundongos Endogâmicos C57BL , Microalgas/química
7.
Phytother Res ; 33(7): 1851-1864, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31119811

RESUMO

We investigated the effects of the prenylated flavonoid-standardized extract (PFE) from the seeds of Psoralea corylifolia L. on countering obesity, which increases energy expenditure and stimulates thermogenesis in subcutaneous white adipose tissue (sWAT) and brown adipose tissue (BAT). For 12 weeks, C57BL/6 mice were fed a controlled high-fat diet (HFD) or HFDs with 0.2% or 0.5% w/w PFE. In vitro, the differentiation of 3 T3-L1 cells was used to elicit thermogenesis in the presence of PFE. PFE obviously reduced body weight and fat mass in a dose-dependent manner, increased energy expenditure, improved insulin sensitivity, and prevented hepatic steatosis by increasing lipid oxidation and secretion in HFD-fed mice. Moreover, PFE induced clear browning in sWAT, significantly increased phosphorylation of AMPKα1/2 and p38, increased BAT activity and the differentiation of 3 T3-L1 by increasing the expression of uncoupling protein 1 and other thermogenic genes. Our study showed that PFE prevented obesity by increasing browning and activating thermogenic genes in sWAT and BAT, improving glucose homeostasis, and protecting hepatic steatosis.


Assuntos
Fármacos Antiobesidade/farmacologia , Flavonoides/farmacologia , Obesidade/tratamento farmacológico , Extratos Vegetais/farmacologia , Psoralea , Tecido Adiposo Marrom/efeitos dos fármacos , Tecido Adiposo Branco/efeitos dos fármacos , Animais , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Obesidade/genética , Obesidade/metabolismo , Prenilação , Sementes , Termogênese/efeitos dos fármacos
8.
Microb Pathog ; 132: 222-229, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31059755

RESUMO

The emerging incidence of antibiotic resistance trait among the bacteria populating poultry presents a devastating public health issue. On the other hand, at present, diabetes and obesity are the most serious public health issues and are increasing subsequently at alarming rate. In view of this, the present in vitro context was aimed to investigate the antibacterial activities of Momordica charantia (M. charantia) fruits extracts against poultry associated Bacillus spp. and to assess further its phytoconstituents, alpha-(α)-glucosidase activities, and anti-obesity properties. The anti-pathogenic attributes of M. charantia fruit extracts were carried out using disc diffusion assay and results showed the pronounced antibacterial trait of ethanolic extract with maximum zone of inhibition of 28.3 ±â€¯1.2 mm against Bacillus licheniformis. The qualitative phytochemical analyses of fruit extracts illustrated the presence of diverse phytoconstituents. The α-glucosidase inhibition assay for the extracts was performed according to the α-glucosidase activity kit. The results depicted the lowest α-glucosidase activity (57.13 ±â€¯2.3 to 18.14 ±â€¯1.3 U/L) in the presence of ethanolic extract at varied concentrations. The anti-obesity potentialities of fruit extracts were demonstrated in terms of porcine pancreatic lipase (PPL type II) activity using p-nitro-phenyl butyrate (p-NPB) as a substrate. The ethanolic extract of M. charantia fruits was observed to exhibit maximum inhibition of pancreatic lipase ranging from 20.12 ±â€¯2.3 to 68.34 ±â€¯1.3% in a dose dependent manner with an IC50 value of 607.6 ±â€¯1.3 µg/mL. FTIR and GC-MS results indicated the presence of distinct compounds in the ethanol extract and major bioactive constituents were found to be Dimethyl sulfone (35.24%), 9-octadecanamide (20.52%), Pentadecanoic acid (6.64%), Lanost-9 (11)-en-18-oic acid, 23-(acetylxyl)-3-(4-bromobenzoyl) oxyl-20-hydroxyl-gamma-lactone (2.6%), and 2,2-sulfonyldiethanol (2.46%). In conclusion, M. charantia fruits could be of great concern in pharmaceutical industries due to its adequate biological properties and may also help in the management of poultry associated bacterial pathogens.


Assuntos
Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Frutas/química , Momordica charantia/química , Extratos Vegetais/farmacologia , Animais , Fármacos Antiobesidade/farmacologia , Bacillus/efeitos dos fármacos , Lipase/metabolismo , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Aves Domésticas , Doenças das Aves Domésticas/tratamento farmacológico , Doenças das Aves Domésticas/microbiologia , Suínos , alfa-Glucosidases/metabolismo
9.
Mar Drugs ; 17(5)2019 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-31083362

RESUMO

Obesity is a complex disease resulting in several metabolic co-morbidities and is increasing at epidemic rates. The marine environment is an interesting resource of novel compounds and in particular cyanobacteria are well known for their capacity to produce novel secondary metabolites. In this work, we explored the potential of cyanobacteria for the production of compounds with relevant activities towards metabolic diseases using a blend of target-based, phenotypic and zebrafish assays as whole small animal models. A total of 46 cyanobacterial strains were grown and biomass fractionated, yielding in total 263 fractions. Bioactivities related to metabolic function were tested in different in vitro and in vivo models. Studying adipogenic and thermogenic gene expression in brown adipocytes, lipid metabolism and glucose uptake in hepatocytes, as well as lipid metabolism in zebrafish larvae, we identified 66 (25%) active fractions. This together with metabolite profiling and the evaluation of toxicity allowed the identification of 18 (7%) fractions with promising bioactivity towards different aspects of metabolic disease. Among those, we identified several known compounds, such as eryloside T, leptosin F, pheophorbide A, phaeophytin A, chlorophyll A, present as minor peaks. Those compounds were previously not described to have bioactivities in metabolic regulation, and both known or unknown compounds could be responsible for such effects. In summary, we find that cyanobacteria hold a huge repertoire of molecules with specific bioactivities towards metabolic diseases, which needs to be explored in the future.


Assuntos
Fármacos Antiobesidade/farmacologia , Cianobactérias/química , Obesidade/tratamento farmacológico , Adipócitos Marrons/efeitos dos fármacos , Adipócitos Marrons/fisiologia , Animais , Fármacos Antiobesidade/química , Fármacos Antiobesidade/toxicidade , Cianobactérias/crescimento & desenvolvimento , Cianobactérias/metabolismo , Expressão Gênica/efeitos dos fármacos , Glucose/metabolismo , Células Hep G2 , Humanos , Metabolismo dos Lipídeos/efeitos dos fármacos , Obesidade/metabolismo , PPAR gama/metabolismo , Testes de Toxicidade , Proteína Desacopladora 1/metabolismo , Peixe-Zebra
10.
J Oleo Sci ; 68(5): 471-479, 2019 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-30971641

RESUMO

Blueberry leaf is currently a popular dietary supplement. Effects of dietary blueberry leaf and its active components on body fat accumulation were examined. C57BL/6J mice were fed high-fat, high-sucrose diet with or without 3% blueberry leaf extract (BLEx) or 3% concentrated-polyphenolic BLEx (CP BLEx) for 8 weeks. Compared to mice fed a high-fat, high-sucrose diet without blueberry leaf, BLEx and CP BLEx significantly reduced body weight and adipose tissue weight gain. Adipocytes were also smaller and and liver lipid accumulatioin was significantly inhibited in mice fed either BLEx or CP BLEx. These effects tended to be more pronounced in mice fed CP BLEx compared to in mice fed BLEx. Together, results suggest that blueberry leaf inhibits body fat accumulation typically observed in mice fed a high-fat, high-sucrose diet, and that inhibition is attributable to polyphenolic components in leaf extracts.


Assuntos
Tecido Adiposo/metabolismo , Fármacos Antiobesidade/farmacologia , Mirtilos Azuis (Planta)/química , Dieta Hiperlipídica/efeitos adversos , Carboidratos da Dieta/efeitos adversos , Obesidade/metabolismo , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Sacarose/efeitos adversos , Animais , Fármacos Antiobesidade/administração & dosagem , Peso Corporal/efeitos dos fármacos , Ácido Clorogênico/administração & dosagem , Ácido Clorogênico/farmacologia , Metabolismo dos Lipídeos/efeitos dos fármacos , Fígado/metabolismo , Masculino , Camundongos Endogâmicos C57BL , Obesidade/prevenção & controle , Extratos Vegetais/administração & dosagem , Folhas de Planta/química , Polifenóis/administração & dosagem , Proantocianidinas/administração & dosagem , Proantocianidinas/farmacologia
11.
Int J Mol Sci ; 20(7)2019 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-30939798

RESUMO

Brown adipose tissue (BAT), an organ that burns energy through uncoupling thermogenesis, is a promising therapeutic target for obesity. However, there are still no safe anti-obesity drugs that target BAT in the market. In the current study, we performed large scale screening of 636 compounds which were approved by Food and Drug Administration (FDA) to find drugs that could significantly increase uncoupling protein 1 (UCP1) mRNA expression by real-time PCR. Among those UCP1 activators, most of them were antibiotics or carcinogenic compounds. We paid particular attention to fluvastatin sodium (FS), because as an inhibitor of the cellular hydroxymethyl glutaryl coenzyme A (HMG-CoA) reductase, FS has already been approved for treatment of hypercholesteremia. We found that in the cellular levels, FS treatment significantly increased UCP1 expression and BAT activity in human brown adipocytes. Consistently, the expression of oxidative phosphorylation-related genes was significantly increased upon FS treatment without differences in adipogenic gene expression. Furthermore, FS treatment resisted to high-fat diet (HFD)-induced body weight gain by activating BAT in the mice model. In addition, administration of FS significantly increased energy expenditure, improved glucose homeostasis and ameliorated hepatic steatosis. Furthermore, we reveal that FS induced browning in subcutaneous white adipose tissue (sWAT) known to have a beneficial effect on energy metabolism. Taken together, our results clearly demonstrate that as an effective BAT activator, FS may have great potential for treatment of obesity and related metabolic disorders.


Assuntos
Tecido Adiposo Marrom/efeitos dos fármacos , Fármacos Antiobesidade/uso terapêutico , Fluvastatina/uso terapêutico , Obesidade/tratamento farmacológico , Tecido Adiposo Marrom/metabolismo , Animais , Fármacos Antiobesidade/farmacologia , Células Cultivadas , Metabolismo Energético , Fluvastatina/farmacologia , Humanos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Proteína Desacopladora 1/genética , Proteína Desacopladora 1/metabolismo
12.
Mar Drugs ; 17(4)2019 Mar 29.
Artigo em Inglês | MEDLINE | ID: mdl-30934943

RESUMO

Obesity is associated with several health complications and can lead to the development of metabolic syndrome. Some of its deleterious consequences are related to insulin resistance, which adversely affects blood glucose regulation. At present, there is a growing concern regarding healthy food consumption, owing to awareness about obesity. Seaweeds are well-known for their nutritional benefits. The brown alga Ishige okamurae (IO) has been studied as a dietary supplement and exhibits various biological activities in vitro and in vivo. The bioactive compounds isolated from IO extract are known to possess anti-obesity and anti-diabetic properties, elicited via the regulation of lipid metabolism and glucose homeostasis. This review focuses on IO extract and its bioactive compounds that exhibit therapeutic effects through several cellular mechanisms in obesity and diabetes. The information discussed in the present review may provide evidence to develop nutraceuticals from IO.


Assuntos
Fármacos Antiobesidade/farmacologia , Hipoglicemiantes/farmacologia , Obesidade/tratamento farmacológico , Feófitas/química , Animais , Glicemia/metabolismo , Suplementos Nutricionais , Humanos , Metabolismo dos Lipídeos/efeitos dos fármacos , Obesidade/sangue
13.
Nutrients ; 11(4)2019 Apr 16.
Artigo em Inglês | MEDLINE | ID: mdl-30995824

RESUMO

Supplementation with inulin-propionate ester (IPE), which delivers propionate to the colon, suppresses ad libitum energy intake and stimulates the release of satiety hormones acutely in humans, and prevents weight gain. In order to determine whether IPE remains effective when incorporated into food products (FP), IPE needs to be added to a widely accepted food system. A bread roll and fruit smoothie were produced. Twenty-one healthy overweight and obese humans participated. Participants attended an acclimatisation visit and a control visit where they consumed un-supplemented food products (FP). Participants then consumed supplemented-FP, containing 10 g/d inulin or IPE for six days followed by a post-supplementation visit in a randomised crossover design. On study visits, supplemented-FP were consumed for the seventh time and ad libitum energy intake was assessed 420 min later. Blood samples were collected to assess hormones and metabolites. Resting energy expenditure (REE) was measured using indirect calorimetry. Taste and appearance ratings were similar between FP. Ad libitum energy intake was significantly different between treatments, due to a decreased intake following IPE-FP. These observations were not related to changes in blood hormones and metabolites. There was an increase in REE following IPE-FP. However, this effect was lost after correcting for changes in fat free mass. Our results suggest that IPE suppresses appetite and may alter REE following its incorporation into palatable food products.


Assuntos
Apetite/efeitos dos fármacos , Metabolismo Basal/efeitos dos fármacos , Suplementos Nutricionais , Manipulação de Alimentos , Inulina/farmacologia , Obesidade , Propionatos/farmacologia , Fármacos Antiobesidade/farmacologia , Fármacos Antiobesidade/uso terapêutico , Calorimetria Indireta , Colo , Estudos Cross-Over , Método Duplo-Cego , Ingestão de Energia/efeitos dos fármacos , Feminino , Hormônios/sangue , Humanos , Inulina/uso terapêutico , Masculino , Pessoa de Meia-Idade , Obesidade/dietoterapia , Obesidade/metabolismo , Obesidade/fisiopatologia , Sobrepeso , Propionatos/uso terapêutico , Descanso , Resposta de Saciedade/efeitos dos fármacos , Paladar
14.
In Vivo ; 33(3): 707-715, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31028187

RESUMO

BACKGROUND/AIM: The rapid increase in the number of people who are overweight or obese, which increases the risk of diseases and health problems, is becoming an important issue. Herein, we investigated whether olive leaf extract (OLE) has potent anti-obesity effects in high-fat induced mouse models. MATERIALS AND METHODS: C57BL/6 mice were randomized into normal control, high-fat diet (HFD), HFD with OLE, and HFD with garcinia groups and administered experimental diets for 12 weeks. Body weight and food intake were measured once per week and obesity-related biomarkers were evaluated in the serum and adipose tissue. RESULTS: OLE significantly suppressed weight gain, food efficiency ratio, visceral fat accumulation, and serum lipid composition in HFD-induced mice. Furthermore, the expression of adipogenesis- and thermogenesis-related molecules was decreased in the OLE-treated group. CONCLUSION: OLE prevents obesity development by regulating the expression of molecules involved in adipogenesis and thermogenesis.


Assuntos
Fármacos Antiobesidade/farmacologia , Olea/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Adipogenia/efeitos dos fármacos , Tecido Adiposo/efeitos dos fármacos , Tecido Adiposo/metabolismo , Animais , Fármacos Antiobesidade/química , Biomarcadores , Peso Corporal/efeitos dos fármacos , Dieta Hiperlipídica/efeitos adversos , Modelos Animais de Doenças , Metabolismo dos Lipídeos , Masculino , Camundongos , Obesidade/tratamento farmacológico , Obesidade/etiologia , Obesidade/metabolismo , Extratos Vegetais/química , Termogênese/efeitos dos fármacos
15.
Life Sci ; 228: 316-322, 2019 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-31022407

RESUMO

Body adiposity is an important risk factor for the development of chronic non-transmissible diseases. Studies on the process of adipogenesis have been extensively performed in vivo and in vitro models to describe the molecular and cellular bases of adipose tissue development and the effect of natural products in this process. The açai seed extract (ASE) has been evidenced as a potential regulator of body mass. In our work high-fat diet-fed mice treated with ASE (300 mg/Kg/d) (HFD-ASE) showed a lower adipose index (-32.63%, p < 0.001) than the high-fat diet-fed mice group (HFD) and the adipocytes from the HFD group were considerably enlarged (p < 0.001) compared to those in the control group (CG) and HFD-ASE group (+175% and +123%, respectively). We also evaluated the effects of ASE on the modulation of adipogenesis in 3T3-L1 cells. ASE exposure (25 and 100 µg/mL) led to a decrease of 26.6 (p < 0.05) in proliferation and also inhibited pre-adipocyte differentiation through the decreasing expression (p < 0.05) of transcription factors and adipogenic proteins such as PPARÉ£, SREBP-1, and FAS. These results show that the ASE reduce adipogenesis and suppress lipid accumulation in the in vivo model and in 3T3-L1 adipocytes and reinforce ASE as a potential strategy to modulate adipogenesis.


Assuntos
Adipócitos/efeitos dos fármacos , Adipogenia/efeitos dos fármacos , Fármacos Antiobesidade/farmacologia , Dieta Hiperlipídica/efeitos adversos , Euterpe/química , Extratos Vegetais/farmacologia , Células 3T3-L1 , Adipócitos/metabolismo , Adiposidade/efeitos dos fármacos , Animais , Fármacos Antiobesidade/química , Metabolismo dos Lipídeos/efeitos dos fármacos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Obesidade/metabolismo , Obesidade/prevenção & controle , Extratos Vegetais/química , Sementes/química
16.
Nutrients ; 11(4)2019 Apr 03.
Artigo em Inglês | MEDLINE | ID: mdl-30987244

RESUMO

The main purpose of this study was to investigate the hepatotoxic potential and effects on the gut microbiome of decaffeinated green tea extract (dGTE) in lean B6C3F1 mice. Gavaging dGTE over a range of 1X-10X mouse equivalent doses (MED) for up to two weeks did not elicit significant histomorphological, physiological, biochemical or molecular alterations in mouse livers. At the same time, administration of dGTE at MED comparable to those consumed by humans resulted in significant modulation of gut microflora, with increases in Akkermansia sp. being most pronounced. Results of this study demonstrate that administration of relevant-to-human-consumption MED of dGTE to non-fasting mice does not lead to hepatotoxicity. Furthermore, dGTE administered to lean mice, caused changes in gut microflora comparable to those observed in obese mice. This study provides further insight into the previously reported weight management properties of dGTE; however, future studies are needed to fully evaluate and understand this effect.


Assuntos
Fármacos Antiobesidade/farmacologia , Bactérias/efeitos dos fármacos , Microbioma Gastrointestinal/efeitos dos fármacos , Extratos Vegetais/farmacologia , Chá/química , Animais , Fármacos Antiobesidade/isolamento & purificação , Fármacos Antiobesidade/toxicidade , Bactérias/crescimento & desenvolvimento , Doença Hepática Induzida por Substâncias e Drogas/etiologia , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/patologia , Relação Dose-Resposta a Droga , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Masculino , Camundongos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Medição de Risco , Magreza
17.
Molecules ; 24(5)2019 Mar 11.
Artigo em Inglês | MEDLINE | ID: mdl-30862039

RESUMO

Menopause is associated with changes in body composition (a decline in lean body mass and an increase in total fat mass), leading to an increased risk of metabolic syndrome, nonalcoholic fatty liver disease, and heart disease. A healthy diet to control body weight is an effective strategy for preventing and treating menopause-related metabolic syndromes. In the present study, we investigated the effect of long-term feeding of edible oils (soybean oil (SO), tea seed oil (TO), and lard oil (LO)) on female ovariectomized (OVX) mice. SO, TO, and LO comprise mainly polyunsaturated fatty acids (PUFA), monounsaturated fatty acids (MUFA), and saturated fatty acids (SFA), respectively. However, there have been quite limited studies to investigate the effects of different fatty acids (PUFA, MUFA, and SFA) on physiological adaption and metabolic homeostasis in a menopausal population. In this study, 7-week-old female Institute of Cancer Research (ICR) mice underwent either bilateral laparotomy (sham group, n = 8) or bilateral oophorectomy (OVX groups, n = 24). The OVX mice given a high-fat diet (HFD) were randomly divided into three groups: OVX+SO, OVX+TO, and OVX+LO. An HFD rich in SO, TO, or LO was given to the OVX mice for 12 weeks. Our findings revealed that the body weight and relative tissues of UFP (uterus fatty peripheral) and total fat (TF) were significantly decreased in the OVX+TO group compared with those in the OVX+SO and OVX+LO groups. However, no significant difference in body weight or in the relative tissues of UFP and TF was noted among the OVX+SO and OVX+LO groups. Furthermore, mice given an HFD rich in TO exhibited significantly decreased accumulation of liver lipid droplets and adipocyte sizes of UFP and brown adipose tissue (BAT) compared with those given an HFD rich in SO or LO. Moreover, replacing SO or LO with TO significantly increased oral glucose tolerance. Additionally, TO improved endurance performance and exhibited antifatigue activity by lowering ammonia, blood urea nitrogen, and creatine kinase levels. Thus, tea seed oil (TO) rich in MUFA could prevent obesity, reduce physical fatigue, and improve exercise performance compared with either SO (PUFA)- or LO(SFA)-rich diets in this HFD-induced obese OVX mice model.


Assuntos
Fármacos Antiobesidade/farmacologia , Fadiga/metabolismo , Atividade Motora/efeitos dos fármacos , Obesidade/metabolismo , Óleos Vegetais/farmacologia , Sementes/química , Chá/química , Animais , Fármacos Antiobesidade/química , Peso Corporal/efeitos dos fármacos , Dieta Hiperlipídica , Modelos Animais de Doenças , Fadiga/tratamento farmacológico , Ácidos Graxos Monoinsaturados/metabolismo , Ácidos Graxos Insaturados/metabolismo , Glicogênio/metabolismo , Fígado/efeitos dos fármacos , Fígado/metabolismo , Camundongos , Obesidade/tratamento farmacológico , Obesidade/etiologia , Tamanho do Órgão/efeitos dos fármacos , Óleos Vegetais/química
18.
J Sci Food Agric ; 99(9): 4482-4492, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30868582

RESUMO

BACKGROUND: This study aimed to investigate the profiles of bioactive components in roasted Lycium chinense leaves (LCLs) and its in vitro anti-obesity activity after digestion processes. RESULTS: Chlorogenic acid, kaempferol-3-sophoroside-7-glucoside, kaempferol-3-sophoroside, and kaempferol-3-glucoside were discovered as bioactive components in various ratios of ethanol (EtOH) extract in LCLs by using ultra-performance liquid chromatography-electrospray ionization-mass spectrophotometry (UPLC-ESI-MS). The roasting process followed by a 30% EtOH extraction tended to decrease the content of chlorogenic acid and kaempferol-3-glucoside, and enhanced the content of kaempferol-3-sophoroside-7-glucoside. It effectively inhibited pancreatic lipase activity by 62.50 ± 4.81%, which was approximately 1.71 percentage points higher than that of the dried-nonroasted LCL extract (60.79 ± 3.75%). Its bioaccessible fraction obtained from in vitro digestion significantly and dose dependently reduced intracellular lipid accumulation by adipocyte 3T3-L1 compared with a 30% EtOH extraction. At a concentration of 200 µg mL-1 , it inhibited lipid accumulation up to 29.55% in 3T3-L1 cells, which indicated that human digestive enzymes converted kaempferol-3-sophoroside-7-glucoside to kaempferol metabolites that have anti-obesity effects. CONCLUSION: This study suggests that the profiling of bioactive components by processing methods and a bioaccessible fraction could be crucial to improve the bioactivity of LCLs, and potentially be a natural anti-obesity ingredient after oral intake. © 2019 Society of Chemical Industry.


Assuntos
Fármacos Antiobesidade/química , Fármacos Antiobesidade/farmacologia , Lycium/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Células 3T3-L1 , Adipócitos/efeitos dos fármacos , Adipócitos/metabolismo , Animais , Fármacos Antiobesidade/isolamento & purificação , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Lipase/antagonistas & inibidores , Lipase/química , Camundongos , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química
19.
Carbohydr Polym ; 214: 303-310, 2019 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-30926001

RESUMO

We aimed to investigate the anti-obesity effects of chondroitin sulfate (CS) oligosaccharides obtained from cartilage of the skate Raja pulchra and to compare them with those of CSs of other molecular weights (MWts) (skate CS polysaccharides) and origins (shark CS, bovine CS). CSs suppressed pancreatic lipase activity as well as proliferation and lipid accumulation in mature adipocytes. Higher MWt CS had a greater lipase inhibitory activity than lower MWt CS. CSs of different origin show differing potencies for lipase inhibition and effects on adipocytes. Also, dietary intake of skate CS oligosaccharides could ameliorate obesity in high-fat diet mice model: it prevented gaining in body weight, liver weight and adipose tissue weight, maintained lower food consumption, inhibited intestinal absorption of triglyceride, and adjusted the serum endotoxin level. In conclusion, skate CS oligosaccharides have an anti-obesity activity, and the MWt and origin of the CSs may affect this activity.


Assuntos
Fármacos Antiobesidade/uso terapêutico , Sulfatos de Condroitina/uso terapêutico , Obesidade/tratamento farmacológico , Oligossacarídeos/uso terapêutico , Células 3T3-L1 , Adipócitos/efeitos dos fármacos , Animais , Fármacos Antiobesidade/química , Fármacos Antiobesidade/farmacologia , Bovinos , Proliferação de Células/efeitos dos fármacos , Sulfatos de Condroitina/química , Sulfatos de Condroitina/farmacologia , Endotoxinas/análise , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/uso terapêutico , Lipase/antagonistas & inibidores , Gotículas Lipídicas/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos , Oligossacarídeos/química , Oligossacarídeos/farmacologia , Tubarões , Raias , Suínos
20.
Mater Sci Eng C Mater Biol Appl ; 99: 12-24, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30889655

RESUMO

The association of numerous advantages of natural active compounds (from vegetal and herbs) and endogenous lipid in the same delivery system is a straightforward approach for the development of safe and better tolerated anti-obesity therapy. In the present study we envisage a novel concept for obesity therapy, devoted to the development of innovative lipid nanostructured formulas with improved gastric tolerability and enhanced specificity in adipose cells targeting. For this purpose, an anti-obesity herbal active from red pepper extract - Capsaicin (Cap) and an endogenous lipid regulator of appetite - oleoylethanolamide (OEA) or a structural analogue of OEA - Phenylalaninol oleamide (PAO), are simultaneously integrated within the same delivery system - nanostructured lipid carriers (NLC) prepared with linseed oil that has anti-inflammatory and hypotriglyceridemic properties. The NLC-OEA/PAO-Cap presented mean diameters under 200 nm, size that allow an efficient uptake of actives by enterocytes and lead to an extended biological action of all actives - Cap, OEA/PAO and linolenic acid. NLC revealed a polidispersity index ranging from 0.16 to 0.22, which represents a narrow dispersion around mean size and suggests an adequate unimodal behavior. The two types of NLC co-loaded with Cap and OEA/PAO were both negatively charged, with zeta potentials of -42.8 mV and -58.5 mV that offered a guarantee for an excellent stability of NLC in time. Despite to the competition between the accommodations of both actives into the lipid core of nanocarriers, the entrapment efficiency exceeds 92% for OEA/PAO and is ranged between 71 and 82% for Cap. In the presence of NLC-OEA/PAO-Cap, ABTS+⁎ inhibition proceeded in a Capsaicin concentration dependent manner and was dependent on the type of NLC formulation. A remarkable radical-scavenging activity against ABTS+⁎ was determined for Cap and OEA based-NLC. The in vitro release demonstrated that NLC played an important role on the delay of Cap dissolution; the NLC have ensured a slow release of Cap, eg only 21% Cap was released after 24 h of in vitro experiments. The in vivo pharmacological evaluation has revealed that the NLC-OEA/PAO-Cap treatment resulted in a body weight decrease and improves the lipid and glucose profile, as compared to the obese mice batch. Obesity mice treated with NLC-OEA exhibited a weight loss of ~15% and ~10% weight loss for NLC-POA, after 10-days treatment. Administration of NLC-OEA/PAO-Cap to the Albino Swiss mice led to significant decrease of glucose level (e.g. 117.4 mg/dL for NLC-OEA-Cap treated mice versus 213.9 mg/dL for obese mice batch) and exhibited a desired decrease effect of triglyceride (e.g. 71.1 mg/dL for NLC-OEA-Cap versus 129.5, for obese batch). Moreover, the cholesterol values have been lowered to almost half from the value determined for the control batches. Overall, study highlights that using appropriate lipid mediators in association with an herbal anti-obesity active, both formulated into lipid nanocarriers, could enhance the therapeutic response in the obesity treatment.


Assuntos
Fármacos Antiobesidade/uso terapêutico , Portadores de Fármacos/química , Lipídeos/química , Nanoestruturas/química , Obesidade/tratamento farmacológico , Animais , Fármacos Antiobesidade/administração & dosagem , Fármacos Antiobesidade/farmacologia , Antioxidantes/farmacologia , Peso Corporal/efeitos dos fármacos , Varredura Diferencial de Calorimetria , Capsaicina/farmacologia , Preparações de Ação Retardada/farmacologia , Modelos Animais de Doenças , Liberação Controlada de Fármacos , Endocanabinoides/farmacologia , Comportamento Alimentar , Cinética , Camundongos , Obesidade/sangue , Ácidos Oleicos/farmacologia , Tamanho da Partícula , Eletricidade Estática , Temperatura Ambiente
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