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1.
Food Chem ; 448: 139140, 2024 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-38574720

RESUMO

Theabrownins (TBs) are heterogeneous mixtures of water-soluble brown tea pigments, and important constituents to evaluate the quality of dark tea. TBs have numerous hydroxyl and carboxyl groups and are formed by the oxidative polymerization of tea polyphenols. Many biological activities attributed to TBs, including antioxidant, anti-obesity, and lipid-regulating, have been demonstrated. This review summarizes the research progress made on the formation mechanism and physicochemical properties of TBs. It also discusses their protective effects against various diseases and associated potential molecular mechanisms. Additionally, it examines the signaling pathways mediating the bioactivities of TBs and highlights the difficulties and challenges of TBs research as well as their research prospects and applications.


Assuntos
Antioxidantes , Humanos , Antioxidantes/química , Animais , Camellia sinensis/química , Chá/química , Polifenóis/química , Polifenóis/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Catequina/química , Fármacos Antiobesidade/química , Fármacos Antiobesidade/farmacologia
2.
Phytomedicine ; 128: 155528, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38555774

RESUMO

BACKGROUND: Obesity and hyperlipidemia can induce a variety of diseases, and have become major health problems worldwide. How to effectively prevent and control obesity has become one of the hot-spots of contemporary research. Mulberry leaf is the dried leaf of Morus alba L., which is approved by the Ministry of Health as a "homology of medicine and food", rich in diverse active constituents and with a variety of health effects including anti-obesity and anti-hyperlipidemia activities. PURPOSE: The review attempts to summarize and provide the molecular basis, mechanism, safety and products for further exploration and application of mulberry leaf on the treatment on the control of weight gain and obesity. METHODS: This review is conducted by using ScienceDirect, PubMed, CNKI and Web of Science databases following Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA). RESULTS: Based on the research progress of domestic and foreign scholars, the effective phytochemicals, molecular mechanisms and product applications of mulberry leaf in the prevention and treatment of obesity and related metabolic diseases were summarized. CONCLUSION: Mulberry leaf has excellent medicinal and health care value in obesity treatment. However, its pharmacodynamic substance basis and molecular mechanisms need to be further studied.


Assuntos
Fármacos Antiobesidade , Morus , Obesidade , Compostos Fitoquímicos , Folhas de Planta , Morus/química , Folhas de Planta/química , Obesidade/tratamento farmacológico , Humanos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , Fármacos Antiobesidade/farmacologia , Fármacos Antiobesidade/química , Animais , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Fitoterapia
3.
J Microbiol Biotechnol ; 34(3): 634-643, 2024 Mar 28.
Artigo em Inglês | MEDLINE | ID: mdl-38111312

RESUMO

Juglans mandshurica Maxim. walnut (JMW) is well-known for the treatment of dermatosis, cancer, gastritis, diarrhea, and leukorrhea in Korea. However, the molecular mechanism underlying its anti-obesity activity remains unknown. In the current study, we aimed to determine whether JMW can influence adipogenesis in 3T3-L1 preadipocytes and high-fat diet rats and determine the antioxidant activity. The 20% ethanol extract of JMW (JMWE) had a total polyphenol content of 133.33 ± 2.60 mg GAE/g. Considering the antioxidant capacity, the ABTS and DPPH values of 200 µg/ml of JMWE were 95.69 ± 0.94 and 79.38 ± 1.55%, respectively. To assess the anti-obesity activity of JMWE, we analyzed the cell viability, fat accumulation, and adipogenesis-related factors, including CCAAT-enhancer-binding protein alpha (C/EBPα), sterol regulatory element-binding protein-1c (SREBP1c), peroxisome proliferator-activated receptor-gamma (PPARγ), fatty acid synthase (FAS), and acetyl-CoA carboxylase (ACC). We found that total lipid accumulation and triglyceride levels were reduced, and the fat accumulation rate decreased in a dose-dependent manner. Furthermore, JMWE suppressed adipogenesis-related factors C/EBPα, PPARγ, and SREBP1c, as well as FAS and ACC, both related to lipogenesis. Moreover, animal experiments revealed that JMWE could be employed to prevent and treat obesity-related diseases. Hence, JMWE could be developed as a healthy functional food and further explored as an anti-obesity drug.


Assuntos
Fármacos Antiobesidade , Juglans , Camundongos , Ratos , Animais , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Juglans/metabolismo , Células 3T3-L1 , Dieta Hiperlipídica/efeitos adversos , PPAR gama/metabolismo , Adipócitos , Obesidade/tratamento farmacológico , Obesidade/metabolismo , Adipogenia , Fármacos Antiobesidade/química , Proteína alfa Estimuladora de Ligação a CCAAT/metabolismo , Proteína alfa Estimuladora de Ligação a CCAAT/farmacologia , Proteína alfa Estimuladora de Ligação a CCAAT/uso terapêutico , Acetil-CoA Carboxilase/metabolismo , Extratos Vegetais/metabolismo
4.
BMC Complement Med Ther ; 23(1): 3, 2023 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-36604684

RESUMO

BACKGROUND: The use of conventional medical therapies has proven to have many setbacks and safety concerns that need further improvement. However, herbal medicine has been used for over 2000 years, and many studies have proven the use of herbs to be effective and safe. This article discussed the efficacy of different herbal products used in the management of obesity. To evaluate the efficacy of seven herbal-based weight loss products currently available on the Palestinian market, using in vitro assays to screen for antioxidants, anti-amylase, and anti-lipase effects for each product. METHOD: Pancreatic lipase and salivary amylase inhibitory activities, as well as antioxidant analysis, were tested in vitro on a variety of herbal products. Then the IC50 was measured for each test. RESULTS: The anti-lipase assay results, IC50 values in (µg/mL) of each of the seven products (Product A, product B, product C, product D, product E, product F, and product G) were 114.78, 532.1, 60.18, 53.33, 244.9, 38.9, and 48.97, respectively. The IC50 value for orlistat (Reference) was 12.3 µg/ml. On the other hand, the IC50 value for alpha amylase inhibition of the seven products (Product A, product B, product C, product D, product E, product F, and product F) were 345.93, 13,803.84 (Inactive), 73.79, 130.91, 165.95, 28.18, and 33.11 µg/ml respectively, while acarbose (Reference) was 23.38 µg/ml. The antioxidant activity (IC50 values) for the seven products (Product A, product B, product C, product D, product E, product F, and product F) were 1258.92, 707.94, 79.43, 186.20, 164.81, 17.53, and 10.47 µg/ml respectively. While the IC50 value for Trolox was 2.70 µg/ml. CONCLUSION: It can be concluded that the seven products showed varied anti-lipase, anti-amylase, and antioxidant effects. However, products F and G showed superiority in all categories.


Assuntos
Fármacos Antiobesidade , Extratos Vegetais , Plantas Medicinais , alfa-Amilases/química , Antioxidantes/química , Antioxidantes/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Oriente Médio , Fármacos Antiobesidade/química , Fármacos Antiobesidade/farmacologia
5.
Food Funct ; 13(5): 2925-2937, 2022 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-35191457

RESUMO

Obesity has been reported to be associated with gut microbiome dysbiosis. seabuckthorn fruits have traditionally been used in Tibetan foods and medicines for thousands of years. Seabuckthorn polysaccharide (SP) is one of the main functional components in seabuckthorn fruits. However, the effects of SP on a high-fat diet (HFD)-induced obesity have not yet been elucidated. The purpose of this study is to explore the amelioration effect of SP on obesity induced by HFD and to reveal its mechanism of gut microbiota and its metabolites. Results showed that 12-week SP (0.1%, w/w) dietary supplementation could significantly reduce body weight gain, serum lipid level and liver triglycerides level in obese mice. Notably, the SP treatment elevated p-AMPKα and PPARα proteins expression stimulated the phosphorylation of ACC1 and inhibited the protein expression of FAS, PPARγ, and CD36 in the mice liver. Further, SP also reorganized the gut microbiome by up-regulating the proportion of Muribaculaceae_unclassified, Bifidobacterium, Rikenellaceae_RC9_gut_group, Alistipes, and Bacteroides, and down-regulating the abundance of Lactobacillus, Firmicutes_unclassified, Dubosiella Bilophila, and Streptococcus in HFD-induced obese mice. Moreover, the production of microbial metabolites short-chain fatty acids (SCFAs) in feces has also increased. In addition, correlation analysis results showed that obesity-ameliorating effects of SP were highly associated with levels of SCFAs in feces. Therefore, the regulation of SP on liver lipid metabolism may be due to the variation of the gut microbiome and raised production of SCFAs. These results indicate that SP could play the part of a potential nutraceutical for ameliorating obesity through regulation of the gut-liver axis.


Assuntos
Fármacos Antiobesidade/farmacologia , Suplementos Nutricionais , Hippophae , Polissacarídeos/farmacologia , Animais , Fármacos Antiobesidade/administração & dosagem , Fármacos Antiobesidade/química , Dieta Hiperlipídica , Modelos Animais de Doenças , Microbioma Gastrointestinal/efeitos dos fármacos , Metabolismo dos Lipídeos/efeitos dos fármacos , Fígado/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Obesidade/prevenção & controle , Polissacarídeos/administração & dosagem , Polissacarídeos/química , Aumento de Peso/efeitos dos fármacos
6.
Food Funct ; 13(5): 2832-2845, 2022 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-35179169

RESUMO

Obesity continues to be a global public health challenge. Litchi chinensis seed is rich in bioactive ingredients with pharmacological effects, such as hypoglycemic activity and anti-oxidation. This study aimed to assess the potential anti-obesity effects of L. chinensis seed and the changes of gut microbiota and mycobiota compositions in obese zebrafish induced by a high-fat diet. The anti-obesity effects were supplemented and validated in high-fat diet-induced obese mice. In this study, various chemical components of L. chinensis seed water and ethanol extracts were detected using UHPLC-QE-MS, and both extracts showed strong in vitro antioxidant activities. Network pharmacology analysis showed the potential of the extracts to improve obesity. Litchi chinensis seed powder, water and ethanol extracts decreased the weight of obese zebrafish, improved lipid accumulation and lipid metabolism, regulated appetite, and inhibited cell apoptosis and inflammation of the liver and intestine. They showed similar effects in obese mice, and also reduced the weight of fat tissues, regulated insulin resistance and glucose metabolism, and improved the intestinal barrier. Additionally, L. chinensis seed modulated the compositions of gut microbiota and mycobiota in zebrafish, with the regulation of the proportion of bacteria that produce short-chain fatty acids or affect intestine health, including Cetobacterium, Trichococcus, Aeromonas, Staphylococcus, and Micrococcaceae, and the proportion of fungi that produce mycotoxins or have special metabolic capacities, including Penicillium, Candida, Rhodotorula, and Trichoderma. Spearman's correlation analysis revealed the potential link between zebrafish obesity parameters, gut bacteria and fungi. Overall, these findings indicated that L. chinensis seed effectively improved obesity.


Assuntos
Fármacos Antiobesidade/farmacologia , Antioxidantes/farmacologia , Litchi , Extratos Vegetais/farmacologia , Animais , Fármacos Antiobesidade/química , Antioxidantes/química , Dieta Hiperlipídica , Modelos Animais de Doenças , Microbioma Gastrointestinal/efeitos dos fármacos , Metabolismo dos Lipídeos/efeitos dos fármacos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Obesidade/prevenção & controle , Extratos Vegetais/química , Sementes , Peixe-Zebra
7.
Food Funct ; 13(5): 2846-2856, 2022 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-35179170

RESUMO

Obesity is a serious global health issue, and the societal interventions during the COVID-19 pandemic may have perturbed energy homeostasis, which affects the condition of obesity. Tea is a traditional beverage in Asia and has been shown to provide many beneficial health effects. Oolong tea is semifermented, with its chemical composition comprising features of green (unfermented) and black (fermented) tea. Although green tea has anti-obesity properties, studies on the anti-obesity ability of oolong tea are still scarce. In this study, we analyzed the chemical composition of oolong tea extract (OTE) and investigated the effects of OTE on high-fat diet-induced obese rats. OTE contained more (-)-epigallocatechin-3-gallate, (-)-epigallocatechin, and (-)-gallocatechin-3-gallate than theaflavins and theasinensins. Rats fed with a high-fat diet (HFD) and treated with 0.5% OTE exhibited significantly reduced body weight and visceral fat weight compared with the HFD-only group. OTE also decreased adipocyte size, lipogenesis-related protein sterol regulatory element-binding protein 1 (SREBP1) and fatty acid synthase (FASN) protein expression and increased thermogenesis-related protein peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC1α) and uncoupling protein 1 (UCP1) protein expression in epididymal adipose tissue compared with the HFD group. Moreover, the OTE groups had a significantly higher abundance of Candidatus arthromitus and Hydrogenoanaerobacterium and a lower abundance of Ruminococcus1, Oscillibacter, and Odoribacter compared with the HFD group. All these results show that OTE can alleviate weight gain by regulating lipid metabolism and modulating the distribution of the gut microbiota to decrease lipid accumulation in adipose tissue.


Assuntos
Fármacos Antiobesidade/farmacologia , Extratos Vegetais/farmacologia , Chá , Tecido Adiposo/metabolismo , Animais , Fármacos Antiobesidade/química , Dieta Hiperlipídica , Modelos Animais de Doenças , Microbioma Gastrointestinal/efeitos dos fármacos , Metabolismo dos Lipídeos/efeitos dos fármacos , Masculino , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley
8.
Molecules ; 27(3)2022 Jan 28.
Artigo em Inglês | MEDLINE | ID: mdl-35164174

RESUMO

Since the potential of (3:1) mixtures of Atractylodes macrocephala and Amomum villosum extracts has been proposed in the management of obesity, the purpose of present study was to investigate the effects of AME:AVE (3:1) mixture on weight loss, obesity-related biochemical parameters, adipogenesis and lipogenesis related proteins in 3T3-L1 cells and HFD-induced obesity in a mouse model. Treatment with AME:AVE (3:1) mixture inhibited lipid accumulation. Furthermore, the treatment with 75 and 150 mg/kg of AME:AVE (3:1) significantly decreased the body weight gain, white adipose tissue (WAT) weight, and plasma glucose level in HFD-induced obese mice. Moreover, treatment with 75 and 150 mg/kg AME:AVE (3:1) also significantly lowered the size of adipocytes in adipose tissue and reduced the lipid accumulation in liver. AME:AVE (3:1) treatment significantly decreased the expression of proteins related to adipogenesis and lipogenesis in 3T3-L1 adipocytes and WAT of HFD-induced obese mice. These results suggest that the AME:AVE herbal mixture (3:1) has anti-obesity effects, which may be elicited by regulating the expression of adipogenesis and lipogenesis-related proteins in adipocytes and WAT in HFD-induced obesity in mice.


Assuntos
Adipócitos/efeitos dos fármacos , Amomum , Fármacos Antiobesidade/uso terapêutico , Atractylodes , Obesidade/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Células 3T3-L1 , Amomum/química , Animais , Fármacos Antiobesidade/química , Fármacos Antiobesidade/farmacologia , Atractylodes/química , Dieta Hiperlipídica/efeitos adversos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Obesidade/etiologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia
9.
Molecules ; 28(1)2022 Dec 21.
Artigo em Inglês | MEDLINE | ID: mdl-36615228

RESUMO

Ornamental plants often gain relevance not only for their decorative use, but also as a source of phytochemicals with interesting healing properties. Herein, spontaneous Centranthus ruber (L.) DC. and Tropaeolum majus L., mainly used as ornamental species but also traditionally consumed and used in popular medicine, were investigated. The aerial parts were extracted with methanol trough maceration, and resultant crude extracts were partitioned using solvents with increasing polarity. As previous studies mostly dealt with the phenolic content of these species, the phytochemical investigation mainly focused on nonpolar constituents, detected with GC-MS. The total phenolic and flavonoid content was also verified, and HPTLC analyses were performed. In order to explore the potential antiarthritic and anti-obesity properties, extracts and their fractions were evaluated for their anti-denaturation effects, with the use of the BSA assay, and for their ability to inhibit pancreatic lipase. The antioxidant properties and the inhibitory activity on the NO production were verified, as well. Almost all the extracts and fractions demonstrated good inhibitory effects on NO production. The n-hexane and dichloromethane fractions from T. majus, as well as the n-hexane fraction from C. ruber, were effective in protecting the protein from heat-induced denaturation (IC50 = 154.0 ± 1.9, 270.8 ± 2.3 and 450.1 ± 15.5 µg/mL, respectively). The dichloromethane fractions from both raw extracts were also effective in inhibiting pancreatic lipase, with IC50 values equal to 2.23 ± 0.02 mg/mL (for C. ruber sample), and 2.05 ± 0.02 mg/mL (T. majus). Obtained results support the traditional use of these species for their beneficial health properties and suggest that investigated plant species could be potential sources of novel antiarthritic and anti-obesity agents.


Assuntos
Fármacos Antiobesidade , Antioxidantes , Pancrelipase , Compostos Fitoquímicos , Extratos Vegetais , Tropaeolum , Valerianaceae , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Cloreto de Metileno , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Tropaeolum/química , Valerianaceae/química , Pancrelipase/antagonistas & inibidores , Pancrelipase/química , Desnaturação Proteica/efeitos dos fármacos , Fármacos Antiobesidade/química , Fármacos Antiobesidade/isolamento & purificação , Fármacos Antiobesidade/farmacologia
10.
J Ethnopharmacol ; 280: 114418, 2021 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-34271111

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The leaves of Cecropia pachystachya Trécul (Urticaceae), known as embaúba, are used as hypoglycemic and for weight reduction in Brazilian traditional medicine. AIM OF THE STUDY: This study investigated the effects of a pharmaceutical formulation (ECP20) containing C. pachystachya extract on some metabolic alterations caused by a hypercaloric diet in mice. MATERIAL AND METHODS: Mice were randomly fed with a standard or hypercaloric diet and orally treated with ECP20 or vehicle for 13 weeks. Subsequently, adiposity, glucose intolerance, and the presence of nonalcoholic fatty liver disease were assessed. Adipose tissue and liver were collected after euthanasia and frozen at -80 °C for histological and antioxidant analyzes. The effect of ECP20 on the differentiation of 3T3-L1 pre-adipocytes was also investigated. RESULTS: Animals treated with ECP20 showed less weight gain, reduced glycemia, glucose tolerance restored, and hepatoprotective effect. Also, ECP20 presented significant in vivo antioxidant activity. Treatment of 3T3-L1 preadipocytes with ECP20 did not inhibit cellular differencing. CONCLUSIONS: Therefore, ECP20 presented promising effects in the control of obesity and related disorders. Considering that glucose intolerance and hyperglycemia are strong evidence for the development of type 2 diabetes, the findings corroborated the traditional use of C. pachystachya to treat this disease. The chlorogenic acid and the flavonoids orientin and iso-orientin, present in the extract, might be involved in the activities found.


Assuntos
Fármacos Antiobesidade/farmacologia , Cecropia/química , Dieta/efeitos adversos , Ingestão de Energia/efeitos dos fármacos , Hepatopatias/prevenção & controle , Extratos Vegetais/farmacologia , Animais , Fármacos Antiobesidade/química , Glicemia/efeitos dos fármacos , Teste de Tolerância a Glucose , Masculino , Medicina Tradicional , Camundongos , Obesidade/induzido quimicamente , Obesidade/prevenção & controle , Fitoterapia , Extratos Vegetais/química , Plantas Medicinais
11.
Can J Vet Res ; 85(3): 177-185, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34248261

RESUMO

From 50 to 60% of companion animals in the United States are overweight or obese and this obesity rate is rising. As obesity is associated with a number of health problems, an agent that can help weight loss in pets and assist in clinically managing obesity through veterinary prescription foods and medication would be beneficial. Many studies have shown that celastrol, a phytochemical compound found in Celastrus orbiculatus extract (COE), has anti-obesity and anti-inflammatory effects, although these effects have not yet been determined in canine or canine-derived cells. The objective of this study was to investigate the effects of celastrol on the adipogenic differentiation and lipolysis of canine adipocytes. Primary preadipocytes were isolated from the gluteal region of a beagle dog and the primary adipocytes were differentiated into mature adipocytes by adipocyte differentiation media containing isobutylmethylxanthine, dexamethasone, and insulin. In a water-soluble tetrazolium (WST) assay, the cell viability of mature adipocytes was decreased after treatment with COE (0, 0.93, 2.32, and 4.64 nM celastrol) in a concentration-dependent manner, although preadipocytes were not affected. Oil Red O (ORO) staining revealed that COE inhibited the differentiation into mature adipocytes and lipid accumulation in adipocytes. In addition, treatment with COE significantly reduced triglyceride content and increased lipolytic activities by 1.5-fold in canine adipocytes. Overall, it was concluded that COE may enhance anti-obesity activity in canine adipocytes by inhibiting lipid accumulation and increasing lipolytic activity.


De 50 à 60 % des animaux de compagnie aux États-Unis sont en surpoids ou obèses et ce taux d'obésité est en augmentation. Comme l'obésité est associée à un certain nombre de problèmes de santé, un agent qui peut aider à la perte de poids chez les animaux de compagnie et à la gestion clinique de l'obésité au moyen d'aliments et de médicaments sur ordonnance vétérinaire serait bénéfique. De nombreuses études ont montré que le célastrol, un composé phytochimique présent dans l'extrait de Celastrus orbiculatus (COE), a des effets anti-obésité et anti-inflammatoires, bien que ces effets n'aient pas encore été déterminés dans les cellules canines ou dérivées de canins. L'objectif de cette étude était d'étudier les effets du célastrol sur la différenciation adipogène et la lipolyse des adipocytes canins. Des pré-adipocytes primaires ont été isolés de la région fessière d'un chien beagle et les adipocytes primaires ont été différenciés en adipocytes matures par des milieux de différenciation adipocytaires contenant de l'isobutylméthylxanthine, de la dexaméthasone et de l'insuline. Dans un essai au tétrazolium hydrosoluble (WST), la viabilité cellulaire des adipocytes matures a diminué après traitement avec du COE (0, 0,93, 2,32 et 4,64 nM de célastrol) d'une manière dépendante de la concentration, bien que les pré-adipocytes n'aient pas été affectés. La coloration Oil Red O (ORO) a révélé que le COE inhibait la différenciation en adipocytes matures et l'accumulation de lipides dans les adipocytes. De plus, le traitement avec le COE a considérablement réduit la teneur en triglycérides et augmenté les activités lipolytiques de 1,5 fois dans les adipocytes canins. Dans l'ensemble, il a été conclu que le COE peut améliorer l'activité anti-obésité dans les adipocytes canins en inhibant l'accumulation de lipides et en augmentant l'activité lipolytique.(Traduit par Docteur Serge Messier).


Assuntos
Adipócitos/efeitos dos fármacos , Fármacos Antiobesidade/farmacologia , Celastrus/química , Cães , Extratos Vegetais/farmacologia , Adipogenia , Animais , Fármacos Antiobesidade/química , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Extratos Vegetais/química
12.
Int J Biol Macromol ; 183: 2074-2087, 2021 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-34097961

RESUMO

Lycium barbarum polysaccharides (LBPs) are known for their beneficial effects on diabetes, NAFLD and related chronic metabolic diseases induced by high-fat diet (HFD). However, the relevant researches are mainly about the whole crude polysaccharides, the specific active ingredient of LBPs and its bioactivity have been rarely explored. Herein, a homogeneous polysaccharide (LBP-W) was isolated and purified from crude LBPs. Structure characterizations indicated that LBP-W contained a main chain consisting of a repeated unit of →6)-ß-Galp(1 â†’ residues with branches composed of α-Araf, ß-Galp and α-Rhap residues at position C-3. The objective of this study was to evaluate the anti-obesogenic effect of LBP-W and figure out the underlying mechanisms. In vivo efficacy trial illustrated that LBP-W supplements can alleviate HFD-induced mice obesity significantly. Gut microbiota analysis showed that LBP-W not only improved community diversity of intestinal flora, but also regulated their specific genera. Moreover, LBP-W can increase the content of short-chain fatty acids (SCFAs), a metabolite of the intestinal flora. In summary, all these results demonstrated that the homogeneous polysaccharide purified from L. barbarum could be used as a prebiotic agent to improve obesity by modulating the composition of intestinal flora and the metabolism of SCFAs.


Assuntos
Fármacos Antiobesidade/farmacologia , Bactérias/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Metabolismo Energético/efeitos dos fármacos , Microbioma Gastrointestinal/efeitos dos fármacos , Obesidade/tratamento farmacológico , Prebióticos , Animais , Fármacos Antiobesidade/química , Arabinose/química , Arabinose/farmacologia , Bactérias/crescimento & desenvolvimento , Bactérias/metabolismo , Biomarcadores/sangue , Glicemia/efeitos dos fármacos , Glicemia/metabolismo , Modelos Animais de Doenças , Medicamentos de Ervas Chinesas/química , Disbiose , Ácidos Graxos/sangue , Galactose/química , Galactose/farmacologia , Masculino , Camundongos Endogâmicos C57BL , Estrutura Molecular , Obesidade/sangue , Obesidade/microbiologia , Ramnose/química , Ramnose/farmacologia , Relação Estrutura-Atividade
13.
J Microbiol Biotechnol ; 31(7): 1011-1021, 2021 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-34099594

RESUMO

The root bark of Ulmus davidiana var. japonica (Japanese elm) is used in Korea and other East Asian countries as a traditional herbal remedy to treat a variety of inflammatory diseases and ailments such as edema, gastric cancer and mastitis. For this study, we investigated the lipid metabolism and anti-obesity efficacy of ethyl alcohol extract of Ulmus davidiana var. japonica root bark (UDE). First, HPLC was performed to quantify the level of (+)-catechin, the active ingredient of UDE. In the following experiments, cultured 3T3-L1 pre-adipocytes and high-fat diet (HFD)-fed murine model were studied for anti-obesity efficacy by testing the lipid metabolism effects of UDE and (+)-catechin. In the test using 3T3-L1 pre-adipocytes, treatment with UDE inhibited adipocyte differentiation and significantly reduced the production of adipogenic genes and transcription factors PPARγ, C/EBPα and SREBP-1c. HFD-fed, obese mice were administered with UDE (200 mg/kg per day) and (+)-catechin (30 mg/kg per day) by oral gavage for 4 weeks. Weight gain, epididymal and abdominal adipose tissue mass were significantly reduced, and a change in adipocyte size was observed in the UDE and (+)-catechin treatment groups compared to the untreated control group (***p < 0.001). Significantly lower total cholesterol and triglyceride levels were detected in UDE-treated HFD mice compared to the control, revealing the efficacy of UDE. In addition, it was found that lipid accumulation in hepatocytes was also significantly reduced after administration of UDE. These results suggest that UDE has significant anti-obesity and lipid metabolism effects through inhibition of adipocyte differentiation and adipogenesis.


Assuntos
Fármacos Antiobesidade/farmacologia , Dieta Hiperlipídica/efeitos adversos , Metabolismo dos Lipídeos/efeitos dos fármacos , Obesidade/tratamento farmacológico , Ulmus/química , Células 3T3-L1 , Adipócitos/citologia , Adipócitos/efeitos dos fármacos , Adipócitos/metabolismo , Adipogenia/efeitos dos fármacos , Adipogenia/genética , Animais , Fármacos Antiobesidade/administração & dosagem , Fármacos Antiobesidade/química , Catequina/administração & dosagem , Catequina/farmacologia , Diferenciação Celular/efeitos dos fármacos , Hepatócitos/efeitos dos fármacos , Hepatócitos/metabolismo , Lipídeos/sangue , Camundongos , Obesidade/etiologia , Obesidade/metabolismo , Obesidade/patologia , Casca de Planta/química , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Aumento de Peso/efeitos dos fármacos
14.
Molecules ; 26(11)2021 May 28.
Artigo em Inglês | MEDLINE | ID: mdl-34071722

RESUMO

Obesity is a serious health complication in almost every corner of the world. Excessive weight gain results in the onset of several other health issues such as type II diabetes, cancer, respiratory diseases, musculoskeletal disorders (especially osteoarthritis), and cardiovascular diseases. As allopathic medications and derived pharmaceuticals are partially successful in overcoming this health complication, there is an incessant need to develop new alternative anti-obesity strategies with long term efficacy and less side effects. Plants harbor secondary metabolites such as phenolics, flavonoids, terpenoids and other specific compounds that have been shown to have effective anti-obesity properties. Nanoencapsulation of these secondary metabolites enhances the anti-obesity efficacy of these natural compounds due to their speculated property of target specificity and enhanced efficiency. These nanoencapsulated and naive secondary metabolites show anti-obesity properties mainly by inhibiting the lipid and carbohydrate metabolizing enzymes, suppression of adipogenesis and appetite, and enhancing energy metabolism. This review focuses on the plants and their secondary metabolites, along with their nanoencapsulation, that have anti-obesity effects, with their possible acting mechanisms, for better human health.


Assuntos
Produtos Biológicos/química , Química Verde , Nanomedicina/métodos , Obesidade/tratamento farmacológico , Obesidade/metabolismo , Adipócitos/citologia , Adipogenia , Animais , Fármacos Antiobesidade/química , Diferenciação Celular , Flavonoides/química , Humanos , Camundongos , Nanopartículas/química , Fenol/química , Extratos Vegetais/química , Poliésteres/química , Polietilenoglicóis/química , Polifenóis/química , Terpenos/química
15.
Biophys Chem ; 274: 106607, 2021 07.
Artigo em Inglês | MEDLINE | ID: mdl-33957576

RESUMO

Obesity is a global health problem characterized by excessive fat deposition in adipose tissues and can be managed by targeting pancreatic lipase (PL) activity. In the present study, we investigated the in vitro antioxidant and anti-obesity potentials of methanolic leaf extract of Justicia carnea(MEJC) using lipase inhibition kinetics model. In silico evaluations of MEJC bioactive compounds as potential drug-like agents and inhibitors of PL were also investigated using SwissADME prediction tool, semi-empirical quantum mechanics(SQM), molecular electrostatic potential(MEP) and molecular docking analysis. Gas chromatography-mass spectrometry(GC-MS) revealed presence of campesterol, stigmasterol, beta-amyrin etc. MEJC scavenged reactive species and inhibited PL activity via a mixed inhibition pattern (Ki = 107.69 µg/mL; Kii = 398.00 µg/mL) with IC50 > orlistat's IC50. Molecular docking of GC-MS identified compounds with porcine PL showed compounds 8,10,12 and 14 having high PL-binding affinity and similar binding pose with orlistat. Hydrophobic interactions and van der Waals forces were predominantly involved in the ligands' interactions with some key catalytic site amino acid residues (Ser-153,His-264). Compounds 10,12,13 and 14 indicated high drug-likeness, bioavailability, electronegativity, ELUMO-EHOMO energy gaps and MEP. Our findings show that MEJC is a rich natural source of antioxidant and anti-obesity agents which could be optimized for development of new anti-obesity drugs.


Assuntos
Fármacos Antiobesidade/farmacologia , Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Lipase/antagonistas & inibidores , Obesidade/tratamento farmacológico , Extratos Vegetais/farmacologia , Fármacos Antiobesidade/química , Fármacos Antiobesidade/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/antagonistas & inibidores , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Humanos , Justicia/química , Cinética , Lipase/metabolismo , Simulação de Acoplamento Molecular , Obesidade/metabolismo , Picratos/antagonistas & inibidores , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Teoria Quântica
16.
J Chromatogr A ; 1647: 462102, 2021 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-33964619

RESUMO

Despite the widespread use of artichoke-based food supplements for obesity control (FSOC), studies on evaluation of the quality/authenticity of these commercial products are scarce. To that aim, a new multi-analytical strategy, based on the use of gas chromatography coupled to mass spectrometry (GC-MS) and high performance liquid chromatography coupled to ultraviolet and mass spectrometry detection (HPLC-UV-MS), in combination with chemometrics, has been developed. Twenty-one artichoke FSOC and different bract and leaf extracts (used as reference samples) were analysed. Sugars, inositols, caffeoylquinic acids, dicaffeoylquinic acids, flavonoids and their glycosides were detected in reference samples and in most artichoke FSOC. Low concentrations of bioactives, and the presence of other compounds probably related to heat treatment during manufacturing (difructosyl anhydrides, 3-deoxyglucosone), or to the addition of caloric additives (maltose, maltotriose) or non-declared plants (e.g. pinitol, disaccharides, silybin derivatives) were also detected in some FSOC by either GC-MS or HPLC-UV-MS. Application of Principal Component Analysis to the combined GC-MS + HPLC-UV data matrix, proved that this multi-analytical strategy provides advantages over single analytical techniques for the detection of the wide variety of fraudulent practices affecting authenticity of artichoke FSOC and for assessment of their quality.


Assuntos
Fármacos Antiobesidade , Cynara scolymus , Suplementos Nutricionais , Fármacos Antiobesidade/análise , Fármacos Antiobesidade/química , Fármacos Antiobesidade/normas , Cromatografia Líquida de Alta Pressão/métodos , Suplementos Nutricionais/análise , Suplementos Nutricionais/normas , Cromatografia Gasosa-Espectrometria de Massas/métodos , Extratos Vegetais/química
17.
Int J Biol Macromol ; 182: 825-837, 2021 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-33864863

RESUMO

Artemisia sphaerocephala Krasch polysaccharide (ASKP) consists of two main fractions, 60P (molecular weight at 551 kDa) and 60S (molecular weight at 39 kDa). The anti-obesity effects of ASKP and its two fractions were investigated in high-fat-diet-fed mice and showed similar capability in efficiently preventing the development of obesity. The final body weight and body weight gain of obesity mice model were reduced by 12.44% and 35.33% by ASKP, 10.63% and 34.35% by 60P, and 7.82% and 20.04% by 60S. They also showed similar efficiency to ameliorate dyslipidemia, systematic inflammation, and gut dysbiosis. The colonic genes of barrier integrity were significantly upregulated and the genes of hepatic lipid metabolism and that of colonic inflammatory response were suppressed. They attenuated the gut dysbiosis in obese mice, such as the significant enrichment of beneficial genera (Bifidobacterium and Olsenella) and suppression of harmful ones (Mucispirillum and Helicobacter). Significant enrichment of carbohydrate metabolism associated with the promotion of short-chain fatty acid production and decrease of the metabolisms related to obesity and gut dysbiosis (valine, leucine, and isoleucine biosynthesis, and nitrogen metabolism) were also observed by the administration of ASKP, 60P, and 60S. Overall, these polysaccharides showed potential in acting as prebiotics in preventing high-fat-diet-induced obesity.


Assuntos
Fármacos Antiobesidade/uso terapêutico , Artemisia/química , Obesidade/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Polissacarídeos/uso terapêutico , Animais , Fármacos Antiobesidade/química , Fármacos Antiobesidade/farmacologia , Dieta Hiperlipídica/efeitos adversos , Microbioma Gastrointestinal , Isoleucina/biossíntese , Leucina/biossíntese , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Nitrogênio/metabolismo , Obesidade/etiologia , Obesidade/microbiologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polissacarídeos/química , Polissacarídeos/farmacologia , Valina/biossíntese
18.
PLoS One ; 16(4): e0250261, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33878116

RESUMO

Obesity is an enduring medical issue that has raised concerns around the world. Natural plant extracts have shown therapeutic potential in preventing oxidative stress and inflammation related to obesity complications. In this study, Senna alexandrina Mill. leaves were utilized to treat high-fat diet-related metabolic disorders and non-alcoholic fatty liver diseases. Plasma biochemical assays were conducted to determine the lipid profiles and oxidative stress parameters, and the gene expression of antioxidant enzymes and inflammatory mediators was measured. Histological stained livers of high-fat diet-fed rats were observed. S. alexandrina leaf powder supplementation prevented the increase in cholesterol and triglyceride levels in high-fat diet-fed rats. Moreover, S. alexandrina leaves also reduced lipid peroxidation and nitric oxide production in these rats. Prevention of oxidative stress by S. alexandrina leaf supplementation in high-fat diet-fed rats is regulated by enhancing the antioxidant enzyme activity, followed by the restoration of corresponding gene expressions, such as NRF-2, HO-1, SOD, and CAT. Histological staining provides further evidence that S. alexandrina leaf supplementation prevents inflammatory cell infiltration, lipid droplet deposition, and fibrosis in the liver of high-fat diet-fed rats. Furthermore, this investigation revealed that S. alexandrina leaf supplementation controlled non-alcoholic fatty liver disease by modulating the expression of fat metabolizing enzymes in high-fat diet-fed rats. Therefore, S. alexandrina leaf supplementation inhibits fatty liver inflammation and fibrosis, suggesting its usefulness in treating non-alcoholic steatohepatitis. Thus, this natural leaf extract has potential in treatment of obesity related liver dysfunction.


Assuntos
Fármacos Antiobesidade/farmacologia , Fígado Gorduroso/dietoterapia , Obesidade/dietoterapia , Estresse Oxidativo/efeitos dos fármacos , Folhas de Planta/química , Senna/química , Animais , Fármacos Antiobesidade/química , Catalase/genética , Catalase/metabolismo , HDL-Colesterol/sangue , LDL-Colesterol/sangue , Dieta Hiperlipídica/efeitos adversos , Fígado Gorduroso/etiologia , Fígado Gorduroso/metabolismo , Fígado Gorduroso/patologia , Regulação da Expressão Gênica , Heme Oxigenase (Desciclizante)/genética , Heme Oxigenase (Desciclizante)/metabolismo , Gotículas Lipídicas/efeitos dos fármacos , Peroxidação de Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Masculino , Fator 2 Relacionado a NF-E2/genética , Fator 2 Relacionado a NF-E2/metabolismo , Obesidade/etiologia , Obesidade/metabolismo , Obesidade/patologia , Pós/administração & dosagem , Ratos , Ratos Wistar , Superóxido Dismutase/genética , Superóxido Dismutase/metabolismo , Triglicerídeos/sangue
19.
Curr Top Med Chem ; 21(10): 863-877, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33676390

RESUMO

Obesity has become a worldwide health problem. It triggers additional co-morbidities like cardiovascular diseases, cancer, depression, sleep disorders, gastrointestinal problems and many more. Excess accumulation of fat in obesity could be caused by many factors like sedentary lifestyle, consumption of high-fat diet, genetic predisposition, etc. Imbalanced energy metabolism i.e., greater energy consumption than utilisation, invariably underlies obesity. Considering the high prevalence and continuous, uncontrolled increase of this major public health issue, there is an urgent need to find appropriate therapeutic agents with minimal or no side effects. The high prevalence of obesity in recent years has led to a surge in the number of drugs available in the market that claim to control obesity. Although there is a long list of medicines and management strategies that are available, selecting the right therapeutic intervention and feasible management of obesity is a challenge. Several phytochemicals like hydroxycitric acid, flavonoids, tannins, anthocyanins, phytohaemagglutinin, thymoquinone and epigallocatechin gallate have been shown to possess promising anti-obesity properties. However, studies providing information on how various phytochemicals exert their anti-obesity effects are inadequate. This calls for more experimentation in this less explored area of research. Additionally, the complication of obesity arises when it is a result of multiple factors and associated with a number of co-morbidities. In order to handle such complexities, combinatorial therapeutic interventions become effective. In this review, we have described the medicinal chemistry of different highly effective phytochemicals which can be used in the effective treatment and management of obesity.


Assuntos
Fármacos Antiobesidade/química , Inibidores Enzimáticos/química , Obesidade/tratamento farmacológico , Compostos Fitoquímicos/química , Extratos Vegetais/química , Plantas/química , Adipocinas/química , Animais , Antocianinas/química , Fármacos Antiobesidade/farmacologia , Benzoquinonas/química , Catequina/análogos & derivados , Catequina/química , Citratos/química , Descoberta de Drogas , Quimioterapia Combinada , Metabolismo Energético/efeitos dos fármacos , Inibidores Enzimáticos/farmacologia , Flavonoides/química , Humanos , Lipídeos/química , Compostos Fitoquímicos/farmacologia , Fito-Hemaglutininas/química , Extratos Vegetais/farmacologia , Transdução de Sinais , Taninos/química
20.
Molecules ; 26(2)2021 Jan 09.
Artigo em Inglês | MEDLINE | ID: mdl-33435518

RESUMO

Obesity is one of the risk factors associated with cardiovascular diseases, hypertension, abnormal liver function, diabetes, and cancers. Orlistat is currently available to treat obesity, but it is associated with adverse side effects. Natural resources are widely used for obesity treatment. Hence, this study aimed to investigate the anti-obesity activity of Elateriospermum tapos (E. tapos) shell extract in obesity induced Sprague Dawley rats. The rats' obesity was induced by a high-fat (HF) diet made up of 50% standard rat pellet, 20% milk powder, 6% corn starch, and 24% ghee and a cafeteria (CAF) diet such as chicken rolls, salty biscuits, cakes, and cheese snacks. A hot aqueous method for the extraction of E. tapos shells was applied by using 500 mL of distilled water for about 24 h. Various dosages of E. tapos shell extract (10 mg/kg, 100 mg/kg, and 200 mg/kg) were used. At the end of the study, body weight, caloric intake, organ weight, lipid profile, lipoprotein lipase (LPL) activity, and histopathology analysis were carried out. E. tapos shell extract treated groups showed a reduction in body weight, positive lipid-lowering effect, decrements in triglyceride accumulation and LPL activity, and positive improvement in histopathology analysis. A dose of 200 mg/kg showed the most effective result compared to 10 mg/kg and 100 mg/kg doses.


Assuntos
Fármacos Antiobesidade/farmacologia , Euphorbiaceae/química , Obesidade/tratamento farmacológico , Extratos Vegetais/farmacologia , Administração Oral , Animais , Fármacos Antiobesidade/administração & dosagem , Fármacos Antiobesidade/química , Peso Corporal/efeitos dos fármacos , Dieta Hiperlipídica/efeitos adversos , Fígado/efeitos dos fármacos , Fígado/patologia , Masculino , Obesidade/induzido quimicamente , Obesidade/patologia , Tamanho do Órgão/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley
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