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1.
Molecules ; 27(1)2022 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-35011491

RESUMO

Mangifera indica can generate up to 60% of polluting by-products, including peels. However, it has been shown that flavonoids and mangiferin are mainly responsible for the antioxidant, anti-inflammatory, and antibacterial activities closely related to the wound-healing process. The chemical composition of MEMI (methanolic extract of M. indica) was analyzed by HPLC-DAD, as well as concentrations of total phenol (TPC) and flavonoids (TFC) and antioxidant activity (SA50). Wound-healing efficacy was determined by measurements of wound contraction, histological analysis, and tensiometric method; moreover, anti-inflammatory, antibacterial, and acute dermal toxicity (OECD 402) were also evaluated. Phenol, resorcinol, conjugated resorcinol, and mangiferin were detected. TPC, TFC, and SA50 were 136 mg GAE/g, 101.66 mg QE/g, and 36.33 µg/mL, respectively. Tensile strength and wound contraction closure did not show significant differences between MEMI and dexpanthenol groups. Histological analysis (after 14 days) shows a similar architecture between MEMI treatment and normal skin. MEMI exhibits a reduction in edema. Staphylococcus epidermidis had an MIC of 2 mg/mL, while Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli reached 4 mg/mL. The MEMI showed no signs of toxicity. Therefore, this study demonstrates multiple targets that flavonoids and mangiferin of MEMI may present during the healing process.


Assuntos
Mangifera/química , Extratos Vegetais , Cicatrização/efeitos dos fármacos , Ferimentos e Lesões , Animais , Modelos Animais de Doenças , Flavonoides/química , Flavonoides/farmacologia , Masculino , Camundongos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ferimentos e Lesões/tratamento farmacológico , Ferimentos e Lesões/metabolismo , Ferimentos e Lesões/microbiologia , Xantonas/química , Xantonas/farmacologia
2.
Mediators Inflamm ; 2020: 5062506, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32377161

RESUMO

Cyrtocarpa procera is a plant used in traditional Mexican medicine to treat different gastrointestinal problems. Here, we investigated the effects of a C. procera methanolic extract in DSS-induced colitis mice. Ulcerative colitis (UC) was induced by administering 4% DSS in drinking water to female BALB/c mice. Compared to untreated mice with UC, the treatment group receiving the C. procera extract presented less severe UC symptoms of diarrhea, bleeding, and weight loss. Additionally, colon shortening was significantly reduced, and at the microscopic level, only minor damage was observed. Levels of proinflammatory cytokines such as TNF-α, IL-1ß, and IFNγ in serum as well as the MPO activity in the colon were significantly reduced in the C. procera methanolic extract-treated group. Moreover, the extract of C. procera reduced oxidative stress during UC, preventing the deterioration of the activity of antioxidant enzymes such as SOD, CAT, and GPx. Additionally, the extract decreased lipid peroxidation damage and its final products, such as malondialdehyde (MDA). In agreement with this, in vitro assays with the C. procera extract displayed good antioxidant capacity, probably due to the presence of polyphenolic compounds, in particular the flavonoids that were identified, such as chrysin, naringenin, kaempferol, and catechin, which have been reported to have anti-inflammatory and antioxidant activities. Therefore, the improvement of UC by the C. procera methanolic extract may be related to the action mechanisms of these compounds.


Assuntos
Anacardiaceae , Anti-Inflamatórios/uso terapêutico , Antioxidantes/uso terapêutico , Colite Ulcerativa/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Anacardiaceae/química , Animais , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/patologia , Colo/patologia , Citocinas/análise , Sulfato de Dextrana , Feminino , Camundongos , Camundongos Endogâmicos BALB C , Peroxidase/metabolismo , Casca de Planta/química , Índice de Gravidade de Doença
3.
S Afr J Bot ; 135: 240-251, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32963416

RESUMO

Metabolic syndrome comprises a cluster of metabolic disorders related to the development of cardiovascular disease and type 2 diabetes mellitus. In latter years, plant secondary metabolites have become of special interest because of their potential role in preventing and managing metabolic syndrome. Sesquiterpene lactones constitute a large and diverse group of biologically active compounds widely distributed in several medicinal plants used for the treatment of metabolic disorders. The structural diversity and the broad spectrum of biological activities of these compounds drew significant interests in the pharmacological applications. This review describes selected sesquiterpene lactones that have been experimentally validated for their biological activities related to risk factors of metabolic syndrome, together with their mechanisms of action. The potential beneficial effects of sesquiterpene lactones discussed in this review demonstrate that these substances represent remarkable compounds with a diversity of molecular structure and high biological activity, providing new insights into the possible role in metabolic syndrome management.

4.
J Am Coll Nutr ; 38(2): 162-170, 2019 02.
Artigo em Inglês | MEDLINE | ID: mdl-30211662

RESUMO

OBJECTIVE: Colon cancer occupies the third place in incidence worldwide; eating habits, in particular, consumption of hypercaloric diets, are relevant in its etiopathogenesis. On the other hand, foods can also modulate carcinogenesis: for example, proteins, which when hydrolyzed release peptides with biological activities, and legumes, especially, chickpea, represent a good source of hydrolysates. The objective of this work was to verify the inhibitory effect of chickpea hydrolyzed protein on azoxymethane (AOM)-induced carcinogenesis in mice fed a hypercaloric diet. METHODS: We hydrolyzed chickpea protein by pepsin, pancreatin, and a combined pepsin-pancreatin system, to test its anticarcinogenic and hypercaloric activity in mice that had consumed a hypercaloric diet or a normal diet but were injected with azoxymethane (AOM). RESULTS: A concentrate (70% proteins) was obtained from chickpea seeds (18.5% proteins), and extensive hydrolysates were obtained at 15 minutes, in all tested enzyme systems. The greatest activity was evidenced in the hydrolysates obtained with pepsin-pancreatin at 90 minutes. Animals that consumed the hypercaloric diet had a higher concentration of cholesterol and a higher atherogenic index, which were significantly reduced with the administration of chickpea protein hydrolysates with a dose-response effect (10, 20, or 30 mg/kg), whereas no effect was observed in animals that consumed the normal diet. In animals given AOM, aberrant crypts were observed, at a higher rate in animals that consumed the hypercaloric diet; with the consumption of hydrolysates by the animals that consumed either diet, the number of aberrant crypts was reduced with the 3 doses tested, and the effect was better in those animals fed the hypercaloric diet. The best effect in all tests was with 30 mg/kg body weight. CONCLUSION: The consumption of chickpea protein hydrolysates might confer a protective effect against colon carcinogenesis.


Assuntos
Carcinogênese/efeitos dos fármacos , Cicer/química , Substâncias Protetoras/farmacologia , Hidrolisados de Proteína/farmacologia , Sementes/química , Animais , Azoximetano , Carcinogênese/induzido quimicamente , Colo/efeitos dos fármacos , Neoplasias do Colo/etiologia , Dieta/efeitos adversos , Dieta/métodos , Modelos Animais de Doenças , Ingestão de Energia , Masculino , Camundongos
5.
J Food Sci Technol ; 56(7): 3225-3238, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31274890

RESUMO

ABSTRACT: Peltogyne mexicana heartwood might be a novel purple pigment source. The results of the present study demonstrate that the purple pigment is an important source of phenolic compounds (698.22 ± 2.99 mg GAE/g) and flavonoids (48.01 ± 0.51 mg EPE/g). UV-Vis spectrum and color parameters (L* a* b*) showed that purple pigment has different shades of purple-red (H° value 19.32 ± 0.02 in methanol and 22.85 ± 0.01 in ethanol) depending on the solvent and the pH. Also, the purple pigment did not exhibit acute oral toxicity at a single dose (2000 mg/kg body weight). No mutagenicity was observed in the Ames test with three Salmonella typhimurium strains. The purple pigment exhibited considerable coloring properties with a wider range of citric acid-dependent color hues in gelatin (H° from 280.3 to 319.9 and from 68.0 to 88.1), and higher color intensity than commercial anthocyanin. Minor variations in the hue were found in yogurt, for purple pigment with H° values from 317.5 to 315.0, and commercial anthocyanin from 82.6 to 88.7 and 276.9 to 295.5. However, purple pigment required lower concentrations to achieve superior effects. For gelatin and yogurt samples, similar variations in the color parameters L*, a*, b*, and pigment degradation were observed for purple pigment and commercial anthocyanin in the stability assay.

6.
J Cell Biochem ; 119(7): 5944-5959, 2018 07.
Artigo em Inglês | MEDLINE | ID: mdl-29600587

RESUMO

Ca2+ -activated Cl- channels (CaCCs) are anionic channels that regulate many important physiological functions associated with chloride and calcium flux in some somatic cells. The molecular identity of CaCCs was revealed to be TMEM16A and TMEM16B (also known as Anoctamin or ANO1 and ANO2, respectively) in all eukaryotes. A recent study suggests the presence of TMEM16A in human sperm and a relationship with the rhZP-induced acrosome reaction. However, to the best of our knowledge, little is known about the role of TMEM16A in other spermatic processes such as capacitation or motility. In this study, we evaluated the effects of two TMEM16A antagonists on capacitation, acrosome reaction, and motility in guinea pig sperm; these antagonists were T16Ainh-A01, belonging to a second generation of potent antagonists of TMEM16A, and niflumic acid (NFA), a well-known antagonist of TMEM16A (CaCCs). First of all, we confirmed that the absence of Cl- in the capacitation medium changes motility parameters, capacitation, and the progesterone-induced acrosome reaction. Using a specific antibody, TMEM16A was found as a protein band of ∼120 kDa, which localization was in the apical crest of the acrosome and the middle piece of the flagellum. Inhibition of TMEM16A by T16Ainh-A01 affected sperm physiology by reducing capacitation, blocking the progesterone-induced acrosome reaction under optimal capacitation conditions, inhibiting progressive motility, and the acquisition of hyperactivated motility, diminishing [Ca2+ ]i, and increasing [Cl- ]i. These changes in sperm kinematic parameters provide new evidence of the important role played by TMEM16A in the production of sperm capable of fertilizing oocytes.


Assuntos
Anoctamina-1/antagonistas & inibidores , Pirimidinas/farmacologia , Capacitação Espermática/efeitos dos fármacos , Motilidade dos Espermatozoides/efeitos dos fármacos , Tiazóis/farmacologia , Reação Acrossômica/efeitos dos fármacos , Animais , Anti-Inflamatórios não Esteroides/farmacologia , Cálcio/metabolismo , Canais de Cloreto/antagonistas & inibidores , Cloretos/metabolismo , Cobaias , Masculino , Ácido Niflúmico/farmacologia
7.
Nutr Cancer ; 68(5): 856-64, 2016 07.
Artigo em Inglês | MEDLINE | ID: mdl-27282923

RESUMO

In recent years, the consumption of vegetal-source proteins has been studied to determine their preventing effect on the development of several chronic diseases. The initial purpose of this report was to determine the effect of a hypercholesterolemic diet (HCD) given to mice, alone or with azoxymethane (AOM), on various obesity biochemical biomarkers, as well as on the induction of colon aberrant crypts (aberrant crypt foci; ACF). At the end of the 5-week assay, animals fed the HCD showed alterations in the level of total cholesterol, high- and low-density lipoproteins, and in the Atherogenic Index; besides, a significant elevation was observed in the number of ACF. Our second aim was to examine the effect of a Faba Protein Hydrolyzate (FPH) on mice fed the HCD. We first obtained protein hydrolyzates from the seeds of Vicia faba, determined the in vitro antioxidant potential with two tests, and, subsequently, evaluated the effect on obesity biomarkers and on the number of ACF. In the first case, we found that, generally, the best protective effect was obtained with the low dose of FPH (10 mg/kg) administered to animals fed the HCD, and injected AOM. With respect to the number of ACF, we observed that this dose was more effective, inhibiting such lesions to almost the level determined for the normocholesterolemic diet (NCD). Therefore, our results demonstrated the relevance of a HCD to develop anomalies in obesity biomarkers in mouse, as well as to increase the number of precarcinogenic lesions. Our results also showed a protective response with the administration of FPH, particularly with a specific dose, suggesting the need for extending research on the matter by widening the spectra of doses, in order to clearly define its potential to counteract the damage induced by the HCD, as well as to confirm if antioxidation in mice was involved in such an effect.


Assuntos
Anticarcinógenos/farmacologia , Hidrolisados de Proteína/farmacologia , Vicia faba/química , Focos de Criptas Aberrantes/tratamento farmacológico , Focos de Criptas Aberrantes/etiologia , Animais , Anticarcinógenos/análise , Antioxidantes/análise , Antioxidantes/farmacologia , Azoximetano/administração & dosagem , Azoximetano/efeitos adversos , Colesterol na Dieta/administração & dosagem , Colesterol na Dieta/efeitos adversos , Neoplasias Colorretais/tratamento farmacológico , Neoplasias Colorretais/etiologia , Dieta , Modelos Animais de Doenças , Masculino , Camundongos , Camundongos Endogâmicos ICR , Extratos Vegetais/análise , Extratos Vegetais/farmacologia , Hidrolisados de Proteína/análise
8.
Bioorg Med Chem ; 22(21): 5871-82, 2014 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-25311563

RESUMO

In the search for new potential hypolipidemic agents, the present study focused on the synthesis of 2-acyl phenols (6a-c and 7a-c) and their saturated side-chain alkyl phenols (4a-c and 5a-c), and on the evaluation of their hypolipidemic activity using a murine Tyloxapol-induced hyperlipidemic protocol. The whole series of compounds 4-7 greatly and significantly reduced elevated serum levels of total cholesterol, LDL-cholesterol, and triglycerides, with series 6 and 7 showing the greatest potency ever found in our laboratory. At the minimum dose (25mg/kg/day), the latter compounds lowered cholesterol by 68-81%, LDL by 72-86%, and triglycerides by 59-80%. This represents a comparable performance than that shown by simvastatin. Experimental evidence and docking studies suggest that the activity of these derivatives is associated with the inhibition of HMG-CoA reductase.


Assuntos
Anisóis/química , Anisóis/farmacologia , Inibidores de Hidroximetilglutaril-CoA Redutases/síntese química , Inibidores de Hidroximetilglutaril-CoA Redutases/farmacologia , Fenóis/química , Fenóis/farmacologia , Derivados de Alilbenzenos , Animais , Sítios de Ligação , Domínio Catalítico , Colesterol/sangue , LDL-Colesterol/sangue , Cristalografia por Raios X , Ativação Enzimática/efeitos dos fármacos , Humanos , Hidroximetilglutaril-CoA Redutases/química , Hidroximetilglutaril-CoA Redutases/metabolismo , Inibidores de Hidroximetilglutaril-CoA Redutases/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos ICR , Conformação Molecular , Simulação de Acoplamento Molecular , Ligação Proteica , Triglicerídeos/sangue , Aumento de Peso/efeitos dos fármacos
9.
Plant Foods Hum Nutr ; 69(1): 18-24, 2014 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-24249159

RESUMO

The objective of this study was to evaluate the effect of reduced-calorie avocado paste on lipid serum profile, insulin sensitivity, and hepatic steatosis in rats fed a hypercholesterolemic-high fructose diet. Thirty five male Wistar rats were randomly separated in five groups: Control group (ground commercial diet); hypercholesterolemic diet plus 60% fructose solution (HHF group); hypercholesterolemic diet plus 60% fructose solution supplemented with avocado pulp (HHF+A group); hypercholesterolemic diet plus 60% fructose solution supplemented with reduced-calorie avocado paste (HHF+P group); and hypercholesterolemic diet plus 60% fructose solution supplemented with a reduced-calorie avocado paste plus fiber (HHF+FP group). The A, P, and FP were supplemented at 2 g/kg/d. The study was carried out for seven weeks. Rats belonging to the HHF group exhibited significantly (P ≤ 0.05) higher total cholesterol, triglycerides, and insulin levels in serum as well as lower insulin sensitivity than the control group. Supplementation with reduced-calorie avocado paste showed a significant (P ≤ 0.05) decrease in total cholesterol (43.1%), low-density lipoprotein (45.4%), and triglycerides (32.8%) in plasma as well as elevated insulin sensitivity compared to the HHF group. Additionally, the liver enzymes alanine aminotransferase and aspartate aminotransferase decreased significantly in the HHF-P group (39.8 and 35.1%, respectively). These results are likely due to biocompounds present in the reduced-calorie avocado paste, such as polyphenols, carotenoids, chlorophylls, and dietary fibre, which are capable of reducing oxidative stress. Therefore, reduced-calorie avocado paste attenuates the effects of a hypercholesterolemic-high fructose diet in rats.


Assuntos
Colesterol na Dieta/metabolismo , Fígado Gorduroso/metabolismo , Frutose/metabolismo , Resistência à Insulina , Insulina/sangue , Lipídeos/sangue , Persea/química , Alanina Transaminase/sangue , Animais , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Aspartato Aminotransferases/sangue , Colesterol na Dieta/administração & dosagem , Colesterol na Dieta/efeitos adversos , Dieta/efeitos adversos , Carboidratos da Dieta/administração & dosagem , Carboidratos da Dieta/efeitos adversos , Carboidratos da Dieta/metabolismo , Suplementos Nutricionais , Fígado Gorduroso/etiologia , Fígado Gorduroso/prevenção & controle , Frutose/administração & dosagem , Frutose/efeitos adversos , Frutas/química , Fígado/efeitos dos fármacos , Fígado/enzimologia , Fígado/metabolismo , Masculino , Estresse Oxidativo , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos , Ratos Wistar
10.
J Sci Food Agric ; 92(11): 2349-57, 2012 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-22430394

RESUMO

BACKGROUND: The effect of functional foods alone or in combination (cocoa + soy + oats + fish oil) on hepatic damage in rats affected with metabolic syndrome was investigated. RESULTS: Rats that were given cocoa showed a decrease in the levels of triglycerides (TGs) and glucose (63 and 32% respectively) as well as a decrease in blood pressure (15%). Animals fed with soy showed a reduction of 21% in total cholesterol, 15% in blood pressure and 44% in TGs, while feeding oats reduced the concentration of TGs by 53% (P < 0.5). Fish oil caused a reduction in TGs (56%) and glucose (26%). The effect on blood pressure was statistically significant for the groups supplemented with cocoa, soy, cocoa + oats and the total mix. The main finding was a reduction in liver steatosis in animals supplemented with cocoa + oats (from 30 to 4.7% steatosis). Cocoa or fish oil alone did not protect the liver from damage, while cocoa + fish oil did. CONCLUSION: The most relevant effects were that the cocoa + oats mix decreased steatosis by a very large percentage, as did the cocoa + fish oil mix and the mix of all four functional foods.


Assuntos
Avena/química , Cacau , Suplementos Nutricionais , Óleos de Peixe/uso terapêutico , Alimento Funcional , Síndrome Metabólica/dietoterapia , Alimentos de Soja , Animais , Antioxidantes/análise , Cacau/química , Fígado Gorduroso/etiologia , Fígado Gorduroso/prevenção & controle , Óleos de Peixe/análise , Alimento Funcional/análise , Hipercolesterolemia/etiologia , Hipercolesterolemia/prevenção & controle , Hiperglicemia/etiologia , Hiperglicemia/prevenção & controle , Hipertensão/etiologia , Hipertensão/prevenção & controle , Hipertrigliceridemia/etiologia , Hipertrigliceridemia/prevenção & controle , Fígado/patologia , Masculino , Síndrome Metabólica/sangue , Síndrome Metabólica/patologia , Síndrome Metabólica/fisiopatologia , Hepatopatia Gordurosa não Alcoólica , Distribuição Aleatória , Ratos , Ratos Wistar , Sementes/química , Alimentos de Soja/análise
11.
Plant Foods Hum Nutr ; 67(4): 365-70, 2012 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-23135897

RESUMO

The purpose of this study was to evaluate the hypolipidemic effect of a methanolic extract from Opuntia joconostle seeds fed to mice in a hypercholesterolemic diet. Acute toxicity of the methanolic extract was investigated by an established method. Phenolic composition and antioxidant activity were determined by high-performance liquid chromatography and DPPH, respectively. The total phenolic content of Opuntia joconostle seeds was 47.85 ± 1.29 mg gallic acid equivalents/g dry weight. The main phenolic compounds were identified as quercetin, rutin, and cafeic acid. Percent inhibition of DPPH⁺ was 49.76 ± 0.49 %. The oral LD50 for the methanolic extract from the Opuntia joconostle seeds was >5,000 mg/kg BW. Mice fed a hypercholesterolemic diet for six days exhibited significantly (P ≤ 0.001) higher plasma lipid levels than mice fed a normal diet. Remarkably, supplementation with methanolic extract from Opuntia joconostle at doses of 1, 2, and 5 g/kg body weight significantly (P ≤ 0.001) prevented the increase in total cholesterol, low-density lipoprotein cholesterol, triglycerides level, and atherogenic index. Similar concentrations of the HDL cholesterol were observed in both treated and control groups. A significant dose-dependent reduction in lipid levels was noted for treated groups compared to the hypercholesterolemic group. We attribute this result to the seeds' phenolic composition. This methanolic extract has potential to be included in short-term hypercholesterolemia treatment regimens as it exhibits hypolipidemic activity with no apparent toxic manifestations.


Assuntos
Anticolesterolemiantes/uso terapêutico , Hipercolesterolemia/tratamento farmacológico , Opuntia/química , Fenóis/uso terapêutico , Fitoterapia , Sementes/química , Animais , Anticolesterolemiantes/química , Anticolesterolemiantes/isolamento & purificação , Antioxidantes/metabolismo , Colesterol na Dieta/efeitos adversos , HDL-Colesterol/sangue , HDL-Colesterol/efeitos dos fármacos , LDL-Colesterol/sangue , LDL-Colesterol/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/uso terapêutico , Hipercolesterolemia/sangue , Hipercolesterolemia/etiologia , Masculino , Metanol , Camundongos , Modelos Animais , Fenóis/química , Fenóis/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/uso terapêutico , Triglicerídeos/sangue
12.
Plant Foods Hum Nutr ; 67(1): 10-6, 2012 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-22383066

RESUMO

Avocado seed contains elevated levels of phenolic compounds and exhibits antioxidant properties. We investigated the effect of Avocado Seed Flour (ASF) on the lipid levels in mice on a hyperlipidemic diet. The concentration of phenols was determined by high-performance liquid chromatography, antioxidant activity was evaluated using the Trolox equivalent antioxidant capacity method, and dietary fiber was measured using the Association of Official Analytical Chemists (AOAC) method. The LD50 of ASF was determined using Lorke's method and hypolipidemic activity was evaluated in a hypercholesterolemic model in mice. Protocatechuic acid was the main phenolic compound found in ASF, followed by kaempferide and vanillic acid. The total phenolic content in the methanolic extract of ASF was 292.00 ± 9.81 mg gallic acid equivalents/g seed dry weight and the antioxidant activity resulted in 173.3 µmol Trolox equivalents/g DW. In addition, a high content of dietary fiber was found (34.8%). The oral LD50 for ASF was 1767 mg/kg body weight, and treatment with ASF significantly reduced the levels of total cholesterol, LDL-C, and prediction of the atherogenic index. Therefore, the antioxidant activity of phenolic compounds and dietary fiber in ASF may be responsible for the hypocholesterolemic activity of ASF in a hyperlipidemic model of mice.


Assuntos
Hipercolesterolemia/tratamento farmacológico , Hipolipemiantes/farmacologia , Persea/química , Fenóis/farmacologia , Sementes/química , Animais , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Fibras na Dieta/metabolismo , Fibras na Dieta/farmacologia , Modelos Animais de Doenças , Farinha , Hidroxibenzoatos/química , Hidroxibenzoatos/isolamento & purificação , Hidroxibenzoatos/farmacologia , Hipercolesterolemia/sangue , Hipolipemiantes/química , Hipolipemiantes/isolamento & purificação , Dose Letal Mediana , Masculino , Camundongos , Oxirredução , Fenóis/química , Fenóis/isolamento & purificação
13.
J Biomed Biotechnol ; 2011: 968984, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-22174560

RESUMO

Obesity, type II diabetes, and hyperlipidaemia, which frequently coexist and are strongly associated with oxidative stress, increase the risk of cardiovascular disease. An increase in carbohydrate intake, especially of fructose, and a high-fat diet are both factors that contribute to the development of these metabolic disorders. In recent studies carried out in diabetic rats, authors reported that Ibervillea sonorae had hypoglycaemic activity; saponins and monoglycerides present in the plant could be responsible for the effects observed. In the present study, we determined the effects of an aqueous I. sonorae extract on a murine model of obesity and hyperglycaemia, induced by a high-calorie diet, and the relationship of these effects with hepatic oxidation. A high-fat diet over a period of 8 weeks induced weight gain in the mice and increased triglycerides and blood glucose levels. Simultaneous treatment with I. sonorae aqueous extracts, at doses of 100, 200, and 400 mg/kg, decreased triglycerides and glycaemia levels, prevented an increase in body weight in a dose-dependent manner, and decreased hepatic lipid oxidation at a dose of 200 mg/kg. These data suggest that the aqueous extract from I. sonorae root prevents obesity, dyslipidaemia, and hyperglycaemia induced by a hypercaloric diet; however, high doses may induce toxicity.


Assuntos
Fármacos Antiobesidade/farmacologia , Frutose/química , Hiperglicemia/tratamento farmacológico , Obesidade/tratamento farmacológico , Extratos Vegetais/farmacologia , Ração Animal , Animais , Peso Corporal , Linfócitos T CD8-Positivos/imunologia , Relação Dose-Resposta a Droga , Hiperglicemia/metabolismo , Fígado/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos ICR , Oxigênio/química , Raízes de Plantas , Triglicerídeos/química , Água/química
14.
Biomed Pharmacother ; 137: 111345, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-33556873

RESUMO

The aim of this work was to evaluate the gastroprotective activity of a Mexican propolis on indomethacin-induced gastric ulcers in a mouse model. The following contents of the ethanolic extract of propolis of Chihuahua (EEPCh) were determined: antioxidant activity (SA50), total phenolic content (TPC), total flavonoid content (TFC), and chemical composition by HPLC-DAD and HPLC-MS, as well as acute toxicity by OECD Guideline 423. Gastric lesions were induced by intragastric indomethacin treatment in male ICR mice. As the positive control, omeprazole was administered, and three doses of EEPCh were evaluated (50, 150 and 300 mg/kg). Gastric mucosal injury, histological changes and mucosal content were evaluated by means of H&E and PAS staining. For homogenized gastric tissues, the following were evaluated: TBARS, MPO, and PGE2 levels; SOD and GPx antioxidant enzymatic activity; and the concentrations of the proinflammatory cytokines, TNF-α, IL-1ß and IL-6. EEPCh had a significant SA50 of 41.55 µg/mL. The TPC of EEPCh was 860 mg GAE/g, and its TFC was 49.58 mg QE/g. Different phenolic compounds were identified in the extract and were not toxic. The EEPCh doses decreased mucosal damage and histological injuries, maintained the mucosal content and reduced the TBARS, MPO and concentrations of proinflammatory cytokines in gastric ulcer tissues. The 150 and 300 mg/kg doses increased the SOD activity and maintained the PGE2 content. Only the 300 mg/kg dose increased the GPx activity. The results of this study suggest that EEPCh displays gastroprotective effects by means of its antioxidant activity and anti-inflammatory effects and promotes ulcer protection through the maintenance of mucosal content and PGE2 levels.


Assuntos
Antiulcerosos/química , Antiulcerosos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Própole/química , Própole/farmacologia , Úlcera Gástrica/prevenção & controle , Animais , Antiulcerosos/uso terapêutico , Antioxidantes/análise , Citocinas/metabolismo , Dinoprostona/metabolismo , Modelos Animais de Doenças , Feminino , Flavonoides/análise , Flavonoides/química , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/lesões , Mucosa Gástrica/patologia , Glutationa Peroxidase/efeitos dos fármacos , Glutationa Peroxidase/metabolismo , Indometacina/toxicidade , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Malondialdeído/metabolismo , Camundongos Endogâmicos ICR , Omeprazol/farmacologia , Fenóis/análise , Fenóis/química , Extratos Vegetais/uso terapêutico , Própole/uso terapêutico , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/patologia , Superóxido Dismutase/efeitos dos fármacos , Superóxido Dismutase/metabolismo
15.
Nutrients ; 13(9)2021 Sep 11.
Artigo em Inglês | MEDLINE | ID: mdl-34579045

RESUMO

Gastric ulcer disease induced by the consumption of NSAIDs is a major public health problem. The therapy used for its treatment causes adverse effects in the patient. Propolis is a natural product that has been used for the treatments of different diseases around the world. Nevertheless, there is little information about the activity of propolis in gastric ulcers caused by treatment with NSAIDs. Therefore, this review evaluates and compares the gastroprotective potential of propolis and its function against NSAID-induced gastric ulcers, for which a systematic search was carried out in the PubMed and ScienceDirect databases. The main criteria were articles that report the gastroprotective activity of propolis against the damage produced by NSAIDs in the gastric mucosa. Gastroprotection was related to the antioxidant, antisecretory, and cytoprotective effects, as well as the phenolic compounds present in the chemical composition of propolis. However, most of the studies used different doses of NSAIDs and propolis and evaluated different parameters. Propolis has proven to be a good alternative for the treatment of gastric ulcer disease. However, future studies should be carried out to identify the compounds responsible for these effects and to determine their potential use in people.


Assuntos
Antiulcerosos/farmacologia , Antioxidantes/farmacologia , Apiterapia , Própole/farmacologia , Úlcera Gástrica/tratamento farmacológico , Animais , Anti-Inflamatórios não Esteroides/efeitos adversos , Mucosa Gástrica/efeitos dos fármacos , Humanos , Úlcera Gástrica/induzido quimicamente , Resultado do Tratamento
16.
Bioorg Med Chem ; 18(12): 4238-48, 2010 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-20576575

RESUMO

A series of alpha-asarone-based analogues was designed by conducting docking experiments with published crystal structures of human HMG-CoA reductase. Indeed, synthesis and evaluation of this series showed a highly hypocholesterolemic in vivo activity in a murine model, as predicted by previous docking studies. In agreement with this model, the polar groups attached to the benzene ring could play a key role in the enzyme binding and probably also in its biological activity, mimicking the HMG-moiety of the natural substrate. The hypolipidemic action mechanism of these compounds was investigated by developing a simple, efficient, and novel model for determining HMG-CoA reductase inhibition. The partial purification of the enzyme from Schizosaccharomyces pombe allowed for testing of alpha-asarone- and fibrate-based analogues, resulting in positive and significant inhibitory activity.


Assuntos
Anisóis/química , Hidroximetilglutaril-CoA Redutases/química , Inibidores de Hidroximetilglutaril-CoA Redutases/síntese química , Schizosaccharomyces/efeitos dos fármacos , Derivados de Alilbenzenos , Animais , Anisóis/síntese química , Anisóis/uso terapêutico , Sítios de Ligação , Simulação por Computador , Diabetes Mellitus Experimental/tratamento farmacológico , Modelos Animais de Doenças , Desenho de Fármacos , Humanos , Hidroximetilglutaril-CoA Redutases/metabolismo , Inibidores de Hidroximetilglutaril-CoA Redutases/química , Inibidores de Hidroximetilglutaril-CoA Redutases/uso terapêutico , Masculino , Camundongos , Camundongos Endogâmicos ICR
17.
J Med Food ; 22(6): 567-577, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31021307

RESUMO

In the production of chocolate, only cocoa seeds are used, generating by-products that are generally discarded, increasing the risk of environmental contamination. Given fiber, carbohydrates, proteins, and flavonoid content the use of cacao pod husks can generate nutraceutical products for human consumption. In contrast, obesity represents a major public health problem worldwide. Cacao derivatives are able to modulate overweight and lipid disorders. The objective of present work was to prepare and characterize products using cacao by-products and analyze their effects on altered cardiometabolic risk markers in an obesity model induced by high fat diet and fructose ingestion in rats. The effects of a pellet and extracts made with outer pod husk and kernel husk for 5 weeks were analyzed in an obesity rat model. The treatments significantly decreased body weight by 39%, systolic blood pressure by 27%, triglycerides by 55%, total cholesterol by 24%, low-density lipoprotein cholesterol by 37%, and the triglycerides/high-density lipoprotein ratio by 54%. Cacao by-products improved the metabolic function of obese animals, without causing secondary effects.


Assuntos
Cacau/química , Doenças Cardiovasculares/prevenção & controle , Obesidade/prevenção & controle , Extratos Vegetais/administração & dosagem , Animais , Pressão Sanguínea/efeitos dos fármacos , Peso Corporal/efeitos dos fármacos , Doenças Cardiovasculares/metabolismo , Doenças Cardiovasculares/fisiopatologia , LDL-Colesterol/metabolismo , Dieta Hiperlipídica/efeitos adversos , Modelos Animais de Doenças , Humanos , Masculino , Obesidade/metabolismo , Extratos Vegetais/química , Ratos , Ratos Wistar , Triglicerídeos/metabolismo , Resíduos/análise
18.
J Ethnopharmacol ; 240: 111875, 2019 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-31034952

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Buddleja cordata Humb. Bonpl. & Kunth, known by the population as Tepozán blanco, is a shrub plant used in traditional herbal medicine in Mexico for the treatment of tumors, cancer, sores, skin burns, rheumatic pains and diseases related to inflammatory processes such as arthritis; authors adjudicate this etno-medicinal effect to the presence of secondary metabolites in the plant such as verbascoside, however due to its low concentration in recent years biotechnological tools are applied as cell culture to biosynthesize these pharmacological active metabolites in greater quantities. AIM OF THE STUDY: Evaluate the possible toxic effect after a daily administration of MeOH extracts from wild plant leaves (Bc-Wp), and cell culture (Bc-Cc) of B. cordata for 28 days, and after their anti-edematous and antioxidant activities in vivo, as well their effect on the cytokines profile during experimental arthritis induced by complete Freund's adjuvant. MATERIALS AND METHODS: Both extracts were evaluated in CD1 male mice first in a toxicity test of repeated dose administrations (1 g/kg) for 28 days, after which pharmacological activity of both extracts was measure during experimental induced arthritis where three doses were tested, at the end of the study edema formation, body weight gain and antioxidant activity were measure in edema and ganglionic tissues. Finally, dose that exerted the best protective effect (250 mg/kg) was evaluated to quantify its effect over ganglionic tissue concentration of lymphocytes T CD4+, and cytokines (IL-1ß, TNF-α and IL-10), as well histological analysis in arthritic mice. RESULTS: Both extracts (Bc-Wp and Bc-Cc) did not exert lethality, however body weight gain and food in-take were lower than in healthy mice administered with vehicles, also extract-treated animals showed a decrease in serum lipid concentration and only Bc-Wp extract treated animals decrease serum alkaline phosphatase after 28 daily administration compared to healthy un-treated mice. During experimental arthritis best inhibition effect over edema development was observed in those animals administered with both extracts at dose of 250 mg/kg (Bc-Wp and Bc-Cc) on day 28, compared to CFA un-treated mice. Also both extracts reduce oxidative damage over lipids and proteins at the same dose, in both ganglionic and edema tissue, as well antioxidant enzymatic response was reduced in both tissues compared to arthritic un-treated group. In ganglionic tissue of arthritic mice, CD4+ lymphocytes concentration was reduced by Bc-Wp and Bc-Cc treatment (250 mg/kg) respectively, as well IL-1ß, and TNF-α levels. Only arthritic animals treated with Bc-Cc extract at 250 mg/kg generated a significant increase of IL-10 doubling the levels compared to CFA un-treated group. Histological analysis of popliteal ganglion showed that both extracts decrease the incidence of lytic lesions, lipid inclusions and leukocyte infiltration. CONCLUSION: Methanolic extracts of wild Buddleja cordata and its cell cultures did not generated lethality after a daily administration for 28 days at 1 g/kg, but it was observed that both showed a lipid-lowering effect. Also at dose of 250 mg/kg both extracts exerted anti-edematous, protection against the oxidation of lipid and proteins, regulation on antioxidant enzymatic response, down-regulation on lymphocytes CD4+ producers of IL-1ß and TNF-α, an increase in IL-10 levels, which caused a decrease in leukocyte infiltration in ganglionic tissue during experimental arthritis.


Assuntos
Anti-Inflamatórios/uso terapêutico , Artrite Experimental/tratamento farmacológico , Buddleja , Edema/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Animais , Anti-Inflamatórios/farmacologia , Células Cultivadas , Linfócitos/efeitos dos fármacos , Masculino , Metanol/química , Camundongos , Fitoterapia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Solventes/química
19.
Bol. latinoam. Caribe plantas med. aromát ; 23(2): 273-290, mar. 2024. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1552583

RESUMO

The aim of the present study was to assess the impacts of roasting and the type of extraction solvent (ethanol or water) on the hypolipidemic act ivity of xoconostle fruit peel extracts in a tyloxapol - induced model of hyperlipidemia. Water and ethanol extracts from raw and roasted Opuntia joconostle peels were obtained to quantify the phytochemicals contained within and assess their hypolipidemic ac tivity in rats (n=5) against tyloxapol - induced dyslipidemia (400 mg/kg). The raw ethanol and water extracts, as well as the roasted water extract (200 mg/kg), showed hypolipidemic activity in the tyloxapol - treated group ( p <0.05). In contrast, the roasted s ample extracted with ethanol did not show this effect. The concentrations of phenolic compounds (39.80 mg GAE/g) and flavonoids (16.42 ± 0.14 mg QE/g) were higher in the ethanolic extracts than in the aqueous extracts. Conversely, the concentration of beta lains (115.51 ± 1.66 mg/100 g) was higher in the water extracts than in the ethanol extracts. It was concluded that the roasting process modified the concentration of some phytochemicals and their antioxidant capacity in vitro , producing a hypolipidemic ef fect in tyloxapol - induced hyperlipidemic rats


El objetivo del presente estudio fue evaluar el impacto del tostado y del tipo de disolvente de e xtracción (etanol o agua) sobre la actividad hipolipidémica de los extractos de cáscara de frutos de xoconostle en un modelo de hiperlipidemia inducido por el tyloxapol. Se obtuvieron extractos acuosos y etanólicos de cáscara cruda y asada de Opuntia jocon ostle para cuantificar los fitoquímicos que contienen y evaluar su actividad hipolipidémica en ratas (n=5) contra la dislipidemia inducida por el tyloxapol (400 mg/kg). Los extractos acuosos y etanólicos crudos, así como el extracto acuoso tostado (200 mg/ kg), mostraron actividad hipolipidémica en el grupo tratado con tiloxapol ( p <0,05). En cambio, la muestra asada y extraída con etanol no mostró este efecto. Las concentraciones de compuestos fenólicos (39,80 mg GAE/g) y flavonoides (16,42 ± 0,14 mg QE/g) f ueron mayores en los extractos etanólicos que en los acuosos. Por el contrario, la concentración de betalaínas (115,51 ± 1,66 mg/100 g) fue mayor en los extractos acuosos que en los etanólicos. Se concluyó que el proceso de asado modificó la concentración de algunos fitoquímicos y su capacidad antioxidante in vitro , produciendo un efecto hipolipidémico en ratas hiperlipidémicas inducidas por el tyloxapol.


Assuntos
Extratos Vegetais/biossíntese , Opuntia/metabolismo , Opuntia/química , Hipolipemiantes/metabolismo
20.
Environ Toxicol Chem ; 27(3): 612-6, 2008 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-17973560

RESUMO

Heavy metals, such as Fe, Zn, and Cd, are major pollutants in aquatic ecosystems. These toxicants usually are present in these ecosystems in the form of mixtures, and their effect on exposed organisms is the result of interactions occurring between the metals as well as with other pollutants and environmental factors. The present study evaluated the uptake of Cd, Fe, and Zn individually and as a mixture and their effect on adenosine triphosphate (ATP) content in Limnodrillus hoffmeisteri, an important aquatic organism given its resistance to large amounts of these xenobiotics. Test organisms were exposed for 96 h to sediment treated with each of these metals individually and as a mixture. The metal concentrations used were equivalent to the zero lethal concentration of these pollutants as determined in a previous study. At the end of the exposure period, metal concentration in medium and organism as well as ATP content in the latter were quantified. Metal uptake was measured by determining the bioconcentration factor at 96 h. All three metals elicited an important decrease in ATP content when acting singly and as part of a mixture. When present as a mixture, their uptake and effect on L. hoffmeisteri are modified. Therefore, a joint-action toxicity approach should be used for toxicity evaluations involving these pollutants.


Assuntos
Trifosfato de Adenosina/metabolismo , Cádmio/metabolismo , Ferro/metabolismo , Oligoquetos/efeitos dos fármacos , Oligoquetos/metabolismo , Zinco/metabolismo , Animais , Cádmio/toxicidade , Monitoramento Ambiental , Ferro/toxicidade , Poluentes Químicos da Água/metabolismo , Poluentes Químicos da Água/toxicidade , Zinco/toxicidade
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