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1.
Phytochemistry ; 171: 112231, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31901473

RESUMO

Daphne giraldii Nitsche., a member of the genus Daphne (Thymelaeaceae), is a deciduous shrub with mild toxicity. Its rhizome bark, generally called 'Zushima' in Chinese, has many medicinal folkloric uses and good therapeutic effects. Previous studies investigating the chemical constituents and pharmacological activities of D. giraldii have focused on several major classes of compounds, such as coumarins, lignans and flavonoids, especially the interesting enantiomeric flavans. Extracts and pure compounds of D. giraldii were found to possess anti-inflammatory, anti-nociceptive, cytotoxicity, antimalarial, immunomodulating, sedative and hypnotic effects. They have also been reported to influence the cardiovascular functions and blood activities. This comprehensive review will describe the advances in the phytochemistry, pharmacology, medicinal uses and clinical applications of D. giraldii and its formulations covering the literature published from 1970 to 2018. Almost half of the reviewed studies were originally published in non-English languages (mainly in Chinese). Collectively, the aim of this article is to open new avenues for further in-depth pharmacological studies on D. giraldii.


Assuntos
Compostos Fitoquímicos/farmacologia , Thymelaeaceae/química , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Anti-Inflamatórios não Esteroides/farmacologia , Fármacos Antiobesidade/química , Fármacos Antiobesidade/isolamento & purificação , Fármacos Antiobesidade/farmacologia , Antimaláricos/química , Antimaláricos/isolamento & purificação , Antimaláricos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Humanos , Hipnóticos e Sedativos/química , Hipnóticos e Sedativos/isolamento & purificação , Hipnóticos e Sedativos/farmacologia , Fatores Imunológicos/química , Fatores Imunológicos/isolamento & purificação , Fatores Imunológicos/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação
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.
Nutrients ; 11(9)2019 Sep 10.
Artigo em Inglês | MEDLINE | ID: mdl-31509935

RESUMO

The alteration of white adipose tissue (WAT) "browning", a change of white into beige fat, has been considered as a new therapeutic strategy to treat obesity. In this study, we investigated the browning effect of black raspberry (Rubus coreanus Miquel) using in vitro and in vivo models. Black raspberry water extract (BRWE) treatment inhibited lipid accumulation in human mesenchymal stem cells (hMSCs) and zebrafish. To evaluate the thermogenic activity, BRWE was orally administered for 2 weeks, and then, the mice were placed in a 4 °C environment. As a result, BRWE treatment increased rectal temperature and inguinal WAT (iWAT) thermogenesis by inducing the expression of beige fat specific markers such as PR domain zinc-finger protein 16 (PRDM16), uncoupling protein 1 (UCP1), peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC1α), and t-box protein 1 (TBX1) in cold-exposed mice. Furthermore, ellagic acid (EA), a constituent of BRWE, markedly promoted beige specific markers: UCP1, PGC1α, TBX1, and nuclear respiratory factor 1 in beige differentiation media (DM)-induced 3T3-L1 adipocytes. Our findings indicate that BRWE can promote beige differentiation/activation, and EA is the active compound responsible for such effect. Thus, we suggest the nature-derived agents BRWE and EA as potential agents for obesity treatment.


Assuntos
Adipócitos Bege/efeitos dos fármacos , Adipócitos Brancos/efeitos dos fármacos , Adipogenia/efeitos dos fármacos , Tecido Adiposo Bege/efeitos dos fármacos , Tecido Adiposo Branco/efeitos dos fármacos , Fármacos Antiobesidade/farmacologia , Extratos Vegetais/farmacologia , Termogênese/efeitos dos fármacos , Células 3T3-L1 , Adipócitos Bege/metabolismo , Adipócitos Brancos/metabolismo , Tecido Adiposo Bege/metabolismo , Tecido Adiposo Branco/metabolismo , Animais , Fármacos Antiobesidade/isolamento & purificação , Temperatura Baixa , Regulação da Expressão Gênica , Humanos , Masculino , Células-Tronco Mesenquimais/efeitos dos fármacos , Células-Tronco Mesenquimais/metabolismo , Camundongos , Camundongos Endogâmicos C57BL , Extratos Vegetais/isolamento & purificação , Rubus/química , Transdução de Sinais , Peixe-Zebra
4.
Nutrients ; 11(9)2019 Sep 11.
Artigo em Inglês | MEDLINE | ID: mdl-31514294

RESUMO

Prunus persica (L.) Batsch is a deciduous fruit tree cultivated worldwide. The flower of P. persica (PPF), commonly called the peach blossom, is currently consumed as a tea for weight loss in East Asia; however, its anti-obesity effects have yet to be demonstrated in vitro or in vivo. Since PPF is rich in phytochemicals with anti-obesity properties, we aimed to investigate the effects of PPF on obesity and its underlying mechanism using a diet-induced obesity model. Male C57BL/6 mice were fed either normal diet, high-fat diet (HFD), or HFD containing 0.2% or 0.6% PPF water extract for 8 weeks. PPF significantly reduced body weight, abdominal fat mass, serum glucose, alanine transaminase and aspartate aminotransferase levels, and liver and spleen weights compared to the HFD control group. Real-time quantitative polymerase chain reaction analysis revealed that PPF suppressed lipogenic gene expression, including stearoyl-CoA desaturase-1 and -2 and fatty acid synthase, and up-regulated the fatty acid ß-oxidation gene, carnitine palmitoyltransferase-1, in the liver. Our results suggest that PPF exerts anti-obesity effects in obese mice and these beneficial effects might be mediated through improved hepatic lipid metabolism by reducing lipogenesis and increasing fatty acid oxidation.


Assuntos
Fármacos Antiobesidade/farmacologia , Ácidos Graxos/metabolismo , Flores/química , Lipogênese/efeitos dos fármacos , Fígado/efeitos dos fármacos , Obesidade/prevenção & controle , Extratos Vegetais/farmacologia , Prunus persica/química , Perda de Peso/efeitos dos fármacos , Animais , Fármacos Antiobesidade/isolamento & purificação , Biomarcadores/sangue , Dieta Hiperlipídica , Modelos Animais de Doenças , Ingestão de Alimentos , Regulação da Expressão Gênica , Lipogênese/genética , Fígado/enzimologia , Masculino , Camundongos Endogâmicos C57BL , Obesidade/sangue , Obesidade/genética , Obesidade/fisiopatologia , Tamanho do Órgão , Oxirredução , Extratos Vegetais/isolamento & purificação
5.
Mar Drugs ; 17(9)2019 Sep 13.
Artigo em Inglês | MEDLINE | ID: mdl-31540318

RESUMO

This study investigated the anti-obesity effect of a polysaccharide-rich red algae Gelidium amansii hot-water extract (GHE) in high-fat (HF) diet-induced obese hamsters. GHE contained 68.54% water-soluble indigestible carbohydrate polymers. Hamsters were fed with a HF diet for 5 weeks to induce obesity, and then randomly divided into: HF group, HF with 3% guar gum diet group, HF with 3% GHE diet group, and HF with orlistat (200 mg/kg diet) group for 9 weeks. The increased weights of body, liver, and adipose in the HF group were significantly reversed by GHE supplementation. Lower plasma leptin, tumor necrosis factor-α, and interleukin-6 levels were observed in the GHE+HF group compared to the HF group. GHE also increased the lipolysis rate and decreased the lipoprotein lipase activity in adipose tissues. GHE induced an increase in the phosphorylation of AMP-activated protein kinase (AMPK) and the protein expressions of peroxisome proliferator-activated receptor alpha (PPARα) and uncoupling protein (UCP)-2 in the livers. The decreased triglyceride and total cholesterol in the plasma and liver were also observed in obese hamsters fed a diet with GHE. These results suggest that GHE exerts a down-regulation effect on hepatic lipid metabolism through AMPK phosphorylation and up-regulation of PPARα and UCP-2 in HF-induced obese hamsters.


Assuntos
Fármacos Antiobesidade/administração & dosagem , Suplementos Nutricionais , Obesidade/dietoterapia , Extratos Vegetais/administração & dosagem , Rodófitas/química , Adenilato Quinase/metabolismo , Animais , Fármacos Antiobesidade/química , Fármacos Antiobesidade/isolamento & purificação , Dieta Hiperlipídica/efeitos adversos , Modelos Animais de Doenças , Regulação para Baixo/efeitos dos fármacos , Humanos , Metabolismo dos Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Mesocricetus , Obesidade/etiologia , Orlistate/administração & dosagem , Fosforilação/efeitos dos fármacos , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Transdução de Sinais/efeitos dos fármacos , Proteína Desacopladora 2/metabolismo , Regulação para Cima/efeitos dos fármacos , Água/química
6.
Nutrients ; 11(9)2019 Aug 22.
Artigo em Inglês | MEDLINE | ID: mdl-31443565

RESUMO

Obesity is a global health threat. Herein, we evaluated the underlying mechanism of anti-obese features of bitter orange (Citrus aurantium Linné, CA). Eight-week-administration of CA in high fat diet-induced obese C57BL/6 mice resulted in a significant decrease of body weight, adipose tissue weight and serum cholesterol. In further in vitro studies, we observed decreased lipid droplets in CA-treated 3T3-L1 adipocytes. Suppressed peroxisome proliferator-activated receptor gamma (PPARγ) and CCAAT/enhancer binding protein alpha indicated CA-inhibited adipogenesis. Moreover, CA-treated primary cultured brown adipocytes displayed increased differentiation associated with elevation of thermogenic factors including uncoupling protein 1 and PPARγ coactivator 1 alpha as well. The effects of CA in both adipocytes were abolished in AMP-activated protein kinase alpha (AMPKα)-suppressed environments, suggesting the anti-adipogenic and pro-thermogenic actions of CA were dependent on AMPKα pathway. In conclusion, our results suggest CA as a potential anti-obese agent which regulates adipogenesis and thermogenesis via AMPKα.


Assuntos
Proteínas Quinases Ativadas por AMP/metabolismo , Adipogenia/efeitos dos fármacos , Tecido Adiposo/efeitos dos fármacos , Fármacos Antiobesidade/farmacologia , Citrus , Dieta Hiperlipídica , Obesidade/tratamento farmacológico , Extratos Vegetais/farmacologia , Termogênese/efeitos dos fármacos , Células 3T3-L1 , Adipócitos Marrons/efeitos dos fármacos , Adipócitos Marrons/enzimologia , Adipócitos Brancos/efeitos dos fármacos , Adipócitos Brancos/enzimologia , Tecido Adiposo/enzimologia , Tecido Adiposo/fisiopatologia , Animais , Fármacos Antiobesidade/isolamento & purificação , Citrus/química , Modelos Animais de Doenças , Ativação Enzimática , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Obesidade/enzimologia , Obesidade/fisiopatologia , Extratos Vegetais/isolamento & purificação , Transdução de Sinais
7.
Nutrients ; 11(7)2019 Jul 02.
Artigo em Inglês | MEDLINE | ID: mdl-31269728

RESUMO

Annona muricata Linn, commonly known as graviola, is one of the most popular plants used in Brazil for weight loss. The aim of this study is to evaluate the therapeutic effects of three different doses (50 mg/kg, 100 mg/kg, and 150 mg/kg) of aqueous graviola leaf extract (AGE) supplemented by oral gavage, on obese C57BL/6 mice. Food intake, body weight, an oral glucose tolerance test (OGTT), an insulin sensitivity test, quantification of adipose tissue cytokines, weight of fat pads, and serum biochemical and histological analyses of the liver, pancreas, and epididymal adipose tissue were measured. AGE had an anti-inflammatory effect by increasing IL-10 at doses of 50 and 100 mg/kg. Regarding the cholesterol profile, there was a significant decrease in LDL-cholesterol levels in the AGE 150 group, and VLDL-cholesterol and triglycerides in the AGE 100 and 150 groups. There was an increase in HDL cholesterol in the AGE 150 group. The extract was able to reduce the adipocyte area of the epididymal adipose tissue in the AGE 100 and 150 groups. According to the histological analysis of the liver and pancreas, no significant difference was found among the groups. There were no significant effects of AGE on OGTT and serum fasting glucose concentration. However, the extract was effective in improving glucose tolerance in the AGE 150 group.


Assuntos
Annona , Fármacos Antiobesidade/farmacologia , Dieta Hiperlipídica , Transtornos do Metabolismo de Glucose/tratamento farmacológico , Obesidade/tratamento farmacológico , Extratos Vegetais/farmacologia , Adiposidade/efeitos dos fármacos , Animais , Annona/química , Fármacos Antiobesidade/isolamento & purificação , Fármacos Antiobesidade/toxicidade , Biomarcadores/sangue , Glicemia/efeitos dos fármacos , Glicemia/metabolismo , Modelos Animais de Doenças , Feminino , Transtornos do Metabolismo de Glucose/sangue , Transtornos do Metabolismo de Glucose/fisiopatologia , Mediadores da Inflamação/sangue , Resistência à Insulina , Lipídeos/sangue , Masculino , Camundongos Endogâmicos C57BL , Obesidade/sangue , Obesidade/fisiopatologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Folhas de Planta , Ratos Wistar , Ganho de Peso/efeitos dos fármacos
8.
Nutrients ; 11(7)2019 Jul 03.
Artigo em Inglês | MEDLINE | ID: mdl-31277301

RESUMO

The edible seaweed Gelidium elegans (GEE) is known to inhibit adipocyte differentiation. However, there has been no report on its effects in humans. In this study, we investigated whether GEE reduces body weight or fat mass in obese or overweight individuals. A total of 78 participants were randomly assigned to the test (GEE extract 1000 mg/day) and placebo groups at a 1:1 ratio, and treated for 12 weeks. At six or 12 weeks after randomization, they were evaluated for anthropometric parameters, biomarkers, and body composition. Changes in body weight and fat mass between the two groups was significantly different, as determined using ANCOVA adjusted for baseline, calorie intake, and physical activity. Body weight and fat mass were significantly decreased by GEE after 12 weeks but increased in the placebo group. Moreover, although not significant, triglyceride levels tended to decrease after GEE intake. There was no significant difference in other laboratory biomarkers between the two groups. Taken together, these results suggested that GEE significantly reduced body weight, especially fat mass, in overweight or obese individuals.


Assuntos
Adiposidade/efeitos dos fármacos , Fármacos Antiobesidade/uso terapêutico , Suplementos Nutricionais , Obesidade/tratamento farmacológico , Alga Marinha/química , Perda de Peso/efeitos dos fármacos , Adulto , Fármacos Antiobesidade/efeitos adversos , Fármacos Antiobesidade/isolamento & purificação , Biomarcadores/sangue , Suplementos Nutricionais/efeitos adversos , Método Duplo-Cego , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Obesidade/sangue , Obesidade/fisiopatologia , Fatores de Tempo , Resultado do Tratamento , Adulto Jovem
9.
Nutrients ; 11(5)2019 May 27.
Artigo em Inglês | MEDLINE | ID: mdl-31137884

RESUMO

: Aronia melanocarpa are a rich source of anthocyanins that have received considerable interest for their relations to human health. In this study, the anti-adipogenic effect of cyanidin-3-O-galactoside-enriched Aronia melanocarpa extract (AM-Ex) and its underlying mechanisms were investigated in an in vivo system. Five-week-old male C57BL/6N mice were randomly divided into five groups for 8-week feeding with a control diet (CD), a high-fat diet (HFD), or a HFD with 50 (AM-Ex 50), 100 (AM-Ex 100), or 200 AM-Ex (AM-Ex 200) mg/kg body weight/day. HFD-fed mice showed a significant increase in body weight compared to the CD group, and AM-Ex dose-dependently inhibited this weight gain. AM-Ex significantly reduced the food intake and the weight of white fat tissue, including epididymal fat, retroperitoneal fat, mesenteric fat, and inguinal fat. Treatment with AM-Ex (50 to 200 mg/kg) reduced serum levels of leptin, insulin, triglyceride, total cholesterol, and low density lipoprotein (LDL)-cholesterol. Real-time reverse transcription-polymerase chain reaction (RT-PCR) analysis revealed that AM-Ex suppressed adipogenesis by decreasing CCAAT/enhancer binding protein , peroxisome proliferator-activated receptor , sterol regulatory element-binding protein-1c, peroxisome proliferator-activated receptor gamma coactivator-1, acetyl-CoA carboxylase 1, ATP-citrate lyase, fatty acid synthase, and adipocyte protein 2 messenger RNA (mRNA) expressions. These results suggest that AM-Ex is potentially beneficial for the suppression of HFD-induced obesity by modulating multiple pathways associated with adipogenesis and food intake.


Assuntos
Adipogenia/efeitos dos fármacos , Tecido Adiposo Branco/efeitos dos fármacos , Antocianinas/farmacologia , Fármacos Antiobesidade/farmacologia , Dieta Hiperlipídica , Galactosídeos/farmacologia , Obesidade/tratamento farmacológico , Photinia , Extratos Vegetais/farmacologia , Ganho de Peso/efeitos dos fármacos , Adipogenia/genética , Tecido Adiposo Branco/metabolismo , Tecido Adiposo Branco/fisiopatologia , Animais , Antocianinas/isolamento & purificação , Fármacos Antiobesidade/isolamento & purificação , Modelos Animais de Doenças , Galactosídeos/isolamento & purificação , Regulação da Expressão Gênica , Camundongos Endogâmicos C57BL , Obesidade/genética , Obesidade/metabolismo , Obesidade/fisiopatologia , Photinia/química , Extratos Vegetais/isolamento & purificação , Transdução de Sinais
10.
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
11.
Nutrients ; 11(5)2019 May 24.
Artigo em Inglês | MEDLINE | ID: mdl-31137609

RESUMO

Obesity is one of major health challenges in the industrial world. Although rice hull has been reported to show various bioactivities, no studies have evaluated its anti-obesity effect. We hope to demonstrate the anti-obesity effect of rice hull extract (RHE) and the underlying mechanism in high-fat diet (HFD)-induced obese mice and 3T3-L1 preadipocytes. Serum lipid profiles were determined by enzymatic methods. Histological analysis of liver and epididymis fat tissues was carried out with hematoxylin and eosin stain. The mRNA expression of adipogenic markers was analyzed with qRT-PCR and western blotting. Oral administration of RHE reduced body weight gain and fat accumulation in HFD-fed mice. RHE also reduced lipid accumulation by inhibiting the mRNA expression of adipogenic-related genes in HFD-fed obese mice and differentiated preadipocytes. The downregulation of adipogenesis by RHE was mediated through the phosphorylation of AMP-activated protein kinase (AMPK) and acetyl-CoA carboxylase (ACC). In addition, RHE induced the phosphorylation of c-Jun N-terminal kinases (JNK) and extracellular-signal-regulated kinases (ERK) in liver and epididymis adipose tissues of HFD-fed obese mice. Taken together, these findings indicate that RHE could inhibit the differentiation of adipose cell and prevent HFD-induced obesity, suggesting its potential in the prevention of obesity and metabolic syndrome and related-disorders.


Assuntos
Adipócitos/efeitos dos fármacos , Adipogenia/efeitos dos fármacos , Adiposidade/efeitos dos fármacos , Fármacos Antiobesidade/farmacologia , Dieta Hiperlipídica , Obesidade/prevenção & controle , Oryza , Extratos Vegetais/farmacologia , Sementes , Células 3T3-L1 , Proteínas Quinases Ativadas por AMP/metabolismo , Adipócitos/metabolismo , Adipócitos/patologia , Adipogenia/genética , Animais , Fármacos Antiobesidade/isolamento & purificação , Modelos Animais de Doenças , Lipídeos/sangue , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Obesidade/sangue , Obesidade/patologia , Obesidade/fisiopatologia , Oryza/química , Fosforilação , Extratos Vegetais/isolamento & purificação , Sementes/química , Transdução de Sinais , Ganho de Peso/efeitos dos fármacos
12.
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
13.
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
14.
J Ethnopharmacol ; 236: 173-182, 2019 May 23.
Artigo em Inglês | MEDLINE | ID: mdl-30851371

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Cynometra cauliflora Linn. belongs to the Fabaceae family and is known locally in Malaysia as nam-nam. Traditionally, a decoction of the C. cauliflora leaves is used for treating hyperlipidemia and diabetes. AIM OF THE STUDY: This study aims to investigate the anti-obesity and lipid lowering effects of ethanolic extract of C. cauliflora leaves and its major compound (vitexin) in C57BL/6 obese mice induced by high-fat diet (HFD), as well as to further identify the molecular mechanism underlying this action. METHODS AND MATERIAL: Male C57BL/6 mice were fed with HFD (60% fat) for 16 weeks to become obese. The treatment started during the last 8 weeks of HFD feeding and the obese mice were treated with C. cauliflora leaf extract at 200 and 400 mg/kg/day, orlistat (10 mg/kg) and vitexin (10 mg/kg). RESULTS: The oral administration of C. cauliflora (400 and 200 mg/kg) and vitexin significantly reduced body weight, adipose tissue and liver weight and lipid accumulation in the liver compared to control HFD group. Both doses of C. cauliflora also significantly (P ≤ 0.05) decreased serum triglyceride, LDL, lipase, IL-6, peptide YY, resistin levels, hyperglycemia, hyperinsulinemia, and hyperleptinemia compared to the control HFD group. Moreover, C. cauliflora significantly up-regulated the expression of adiponectin, Glut4, Mtor, IRS-1 and InsR genes, and significantly decreased the expression of Lepr in white adipose tissue. Furthermore, C. cauliflora significantly up-regulated the expression of hypothalamus Glut4, Mtor and NF-kB genes. GC-MS analysis of C. cauliflora leaves detected the presence of phytol, vitamin E and ß-sitosterol. Besides, the phytochemical evaluation of C. cauliflora leaves showed the presence of flavonoid, saponin and phenolic compounds. CONCLUSION: This study shows interesting outcomes of C. cauliflora against HFD-induced obesity and associated metabolic abnormalities. Therefore, the C. cauliflora extract could be a potentially effective agent for obesity management and its related metabolic disorders such as insulin resistance and hyperlipidemia.


Assuntos
Fármacos Antiobesidade/uso terapêutico , Dieta Hiperlipídica/efeitos adversos , Fabaceae/química , Metabolismo dos Lipídeos/efeitos dos fármacos , Obesidade/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Administração Oral , Animais , Fármacos Antiobesidade/isolamento & purificação , HDL-Colesterol/sangue , LDL-Colesterol/sangue , Citocinas/sangue , Fígado/efeitos dos fármacos , Fígado/enzimologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Obesidade/sangue , Obesidade/metabolismo , Extratos Vegetais/isolamento & purificação , Triglicerídeos/sangue
16.
Artigo em Inglês | MEDLINE | ID: mdl-30706829

RESUMO

BACKGROUND AND OBJECTIVE: Lipase inhibitors have gained great interest because they could help in the therapy of many diseases, however, unfortunately, only a few drugs are currently available on the market. Therefore, the aim of this work was to evaluate for the first time the lipase inhibition effect of Thapsia garganica extracts from seeds, leaves and roots. METHODS: Polyphenols and flavonoids contents were determined using spectrophotometric method. Inhibitory activity of ethyl acetate extracts from seeds, leaves and roots of T. garganica against Candida rugosa lipase was determined. To uncover the active constituents responsible for this anti-lipase activity, further investigations were performed by employing theoretical docking simulations, using AutoDock Vina program to discuss the nature of interactions and the inhibition mechanism by major bioactive compounds synthesized by this plant. RESULTS: Seeds, leaves and roots extracts of T. garganica showed appreciable contents of polyphenols and flavonoids which is most in seeds extract with 2.90±0.02mg GAE/gdw and 1.53±0.05mg QE/gdw, respectively. Hence, their inhibitory activities against Candida rugosa lipase were determined as IC50 of 1.19mg/ml, 1.96mg/ml and 1.87mg/ml, respectively. Docking simulations have shown that nortribolid and tribolid are best inhibitors for both lipases (Candida rugosa and human pancreatic lipases). CONCLUSION: Testing the anti-lipase activity of the ethyl acetate extracts of T. garganica revealed a potent lipase inhibition activity, which suggests the use of these molecules as anti-obesity drugs.


Assuntos
Lipase/antagonistas & inibidores , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Thapsia/química , Fármacos Antiobesidade/química , Fármacos Antiobesidade/isolamento & purificação , Fármacos Antiobesidade/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Bioensaio , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Humanos , Técnicas In Vitro , Lipase/química , Lipase/metabolismo , Modelos Moleculares , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Folhas de Planta/química , Raízes de Plantas/química , Polifenóis/química , Polifenóis/isolamento & purificação , Polifenóis/farmacologia , Sementes/química
17.
J Agric Food Chem ; 67(4): 1092-1103, 2019 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-30621393

RESUMO

In this study, the antiobesity effects of n-butanol extract of lotus seeds (LBE) were evaluated in cultured 3T3-L1 preadipocytes and in high-fat diet (HFD)-fed mice. LBE decreased lipid contents in mature 3T3-L1 cells without obvious cytotoxicity. Meanwhile, LBE supplementation also led to weight loss and improved plasma lipid profiles in HFD-fed mice. Furthermore, LBE could activate AMP-activated protein kinase (AMPK) accompanied by down-regulation of lipogenesis related genes (PPARγ, aP2, LPL, C/EBPα, FAS, SREBP-1c) and up-regulation of lipolysis genes (adiponectin and PPARα) in vitro and in vivo. Collectively, our data demonstrated LBE possesses antiadipogenic and antilipogenic activities which are, at least partially, mediated by the activation of AMPK signaling pathways.


Assuntos
Proteínas Quinases Ativadas por AMP/metabolismo , Adipócitos/efeitos dos fármacos , Fármacos Antiobesidade/administração & dosagem , Lotus/química , Obesidade/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Células 3T3-L1 , Proteínas Quinases Ativadas por AMP/genética , Adipócitos/enzimologia , Adipócitos/metabolismo , Adipogenia/efeitos dos fármacos , Animais , Fármacos Antiobesidade/isolamento & purificação , Proteína alfa Estimuladora de Ligação a CCAAT/genética , Proteína alfa Estimuladora de Ligação a CCAAT/metabolismo , Dieta Hiperlipídica/efeitos adversos , Humanos , Metabolismo dos Lipídeos/efeitos dos fármacos , Lipogênese/efeitos dos fármacos , Masculino , Camundongos , Camundongos Endogâmicos ICR , Obesidade/genética , Obesidade/metabolismo , Obesidade/fisiopatologia , PPAR gama/genética , PPAR gama/metabolismo , Extratos Vegetais/isolamento & purificação , Sementes/química , Proteína de Ligação a Elemento Regulador de Esterol 1/genética , Proteína de Ligação a Elemento Regulador de Esterol 1/metabolismo
18.
Biomed Pharmacother ; 111: 503-516, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30597304

RESUMO

Obesity and overweight have increased at an alarming rate in the world during the last three decades. Obesity is a crucial factor in the development of metabolic abnormalities, including glucose intolerance, insulin resistance, metabolic syndrome, low-grade inflammation and oxidative stress. A similar scinario occurs during the aging process where alterations of the energetic metabolism homeostasis and a chronic systematic low-grade inflammation have been observed. Oxidative stress and poor physical performance can increase the risk of metabolic disease. Despite the diverse studies on the pathophysiological effects of obesity, its impact related to gender and through life, particularly during aging, hasn't received a reasonable attention. The purpose of this review is to outline the pathophysiological mechanisms and metabolic alterations associated with obesity, with an emphasis on the monosodium glutamate (MSG)-induced obese model. MSG-induced obesity associated inflammation and declined adiponectin were more obvious in male mice, while glucose tolerance, insulin sensitivity and the redox balance were altered with increased age of both male and female mice. These findings indicate that the metabolic alterations in MSG-induced obesity are associated with the gender as well as aging. Therefore, the MSG obesity model is of a resonable value to underlie the relationship between gender, aging and metabolic alterations in obesity. In addition, we reviewed the medicinal plants and their active constituents which have been used to treat MSG-induced obesity. Given the significat value of this model, studies are needed to scrutinize the benificial effects and underlying mechanisms of medicinal plants with proven anti-obesity activity.


Assuntos
Fármacos Antiobesidade/uso terapêutico , Obesidade/induzido quimicamente , Obesidade/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Plantas Medicinais , Glutamato de Sódio/toxicidade , Animais , Fármacos Antiobesidade/isolamento & purificação , Fármacos Antiobesidade/farmacologia , Modelos Animais de Doenças , Metabolismo Energético/efeitos dos fármacos , Metabolismo Energético/fisiologia , Aromatizantes/toxicidade , Humanos , Obesidade/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Estresse Oxidativo/fisiologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia
19.
Biomed Pharmacother ; 110: 224-238, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30481727

RESUMO

In the present scenario, obesity is a challenging health problem and its prevalence along with comorbidities are on the rise around the world. According to world health organization and organisation for economic co-operation and development epidemiology reports, overweight and obesity are the fifth foremost causes of deaths globally. The increasing rate of obesity is becoming a mammoth problem which enormously affects an individual's quality of life. The conventional therapy of obesity mainly involves synthetic moieties and surgical procedures, which has many harmful side effects and chances of recurrence with severity. Hence, the Present review is a metanalysis of all the available data on the use of the plants with their biological source, active phytochemical constituents and a probable mechanism of action as natural anti-obesity agents. The metanalysis of data during the period of 2000-2018 was performed with the help of scientific data search engine National Center for Biotechnology Information (NCBI/PubMed). This data reveals the need and scope of further research in the development of new natural phytoconstituents for the management of obesity.


Assuntos
Fármacos Antiobesidade/uso terapêutico , Gerenciamento Clínico , Obesidade/tratamento farmacológico , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/uso terapêutico , Fármacos Antiobesidade/isolamento & purificação , Produtos Biológicos/isolamento & purificação , Produtos Biológicos/uso terapêutico , Flavonoides/isolamento & purificação , Flavonoides/uso terapêutico , Previsões , Humanos , Obesidade/metabolismo , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/isolamento & purificação
20.
Molecules ; 23(10)2018 Oct 19.
Artigo em Inglês | MEDLINE | ID: mdl-30347741

RESUMO

Natural products generally contain complex and multiple bioactive compounds that are responsible for the effects on health through complicated synergistic and/or suppressive actions. As an important raw material of local ethnic minority tea, ethnomedicines and food supplements in southwestern areas of China, Docynia indica (Wall.) Decne (DID) mainly consists of phlorizin (PHZ), which is the main active component. In this study, the holistic activities and the interactions of components of PHZ, non-phlorizin (NP) in the DID extract (DIDE) were evaluated. A rapid and effective high-speed counter-current chromatography (HSCCC) was performed to knock out PHZ from DIDE and the purity of PHZ was 96.01% determined by HPLC, with a recovery rate of 96.76%. After 13 weeks of treatment course in a high-fat diet (HFD)-induced obese mice model, the results revealed that the DIDE and PHZ significantly decreased weight gain, blood lipid levels, hyperplasia of adipocytes and alleviated inflammation (p < 0.05). Both DIDE and PHZ improves insulin resistance (p < 0.001). Meanwhile, the intestinal barrier function was improved compared to HFD group, through the determination of serum lipopolysaccharides (LPS), glucagon-likepeptide-2 (GLP-2) and hematoxylin-eosin staining of jejunum. Interestingly, after NP treatment, the metabolic syndrome of the HFD-induced obesity appeared to have a similar improvement. All the experiments showed that there is a synergistic weakening phenomenon when PHZ and NP interact with each other in the mixed state. In conclusion, for the PHZ and NP showing a good effect on anti-obesity, anti-inflammation, and intestinal barrier function, DIDE could be a good source of functional food to prevent obesity.


Assuntos
Inflamação/tratamento farmacológico , Obesidade/tratamento farmacológico , Florizina/administração & dosagem , Extratos Vegetais/química , Rosaceae/química , Tecido Adiposo/efeitos dos fármacos , Animais , Fármacos Antiobesidade/administração & dosagem , Fármacos Antiobesidade/química , Fármacos Antiobesidade/isolamento & purificação , Dieta Hiperlipídica/efeitos adversos , Humanos , Inflamação/genética , Inflamação/patologia , Resistência à Insulina/genética , Fígado/efeitos dos fármacos , Camundongos , Camundongos Obesos , Obesidade/genética , Obesidade/patologia , Florizina/química , Florizina/isolamento & purificação
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