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1.
J Food Sci ; 84(11): 3075-3082, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31599971

RESUMO

The hypocholesterolemic effect of amaranth was studied in male Wistar rats fed a high-fat diet that was supplemented with amaranth flour, AF, or isolated protein, AI. Likewise, an in vitro test was carried out, in which the capacity of the AI, AF, the digested isolate, DAI, and the digested amaranth flour, DAF, to displace the cholesterol of the model micelles was evaluated. The in vivo results showed an increase in the excretion of cholesterol through feces (77% for AF7; 23% and 108% for AI30 and AF30, respect control) and a decrease in the content of hepatic cholesterol (98% for AF7; 96% and 53% for AI30 and AF30 respect control); whereas in vitro it was shown that both AF and DAF have greater power to displace cholesterol than the AI and DAI (IC50 0.1, 0.71, 0.2, and 2.1 for AF, DAF, AI, and DAI, respectively). These evidences show that the proteins and fibers of amaranth have an effect on cholesterol metabolism. PRACTICAL APPLICATION: Nowadays, consumers give great importance to the effect that food has on health. The results shown in this work evidence the potential hypocholesterolemic activity presented by amaranth, this is of great importance due to the increase in the incidence of dyslipidemia in the world population and the importance of amaranth as a nonextensive crop of excellent agronomic, nutritional, and bioactive properties suitable for preparation of functional foods.


Assuntos
Amaranthus/química , Anticolesterolemiantes/administração & dosagem , Dieta Hiperlipídica , Animais , Anticolesterolemiantes/análise , Colesterol/análise , Colesterol/metabolismo , Colesterol na Dieta , Fezes/química , Fígado/química , Masculino , Ratos , Ratos Wistar
2.
Anal Bioanal Chem ; 411(25): 6655-6665, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31410535

RESUMO

For the analysis of pigment-rich red yeast rice products, a fast quantitative high-performance thin-layer chromatography (HPTLC) method was newly developed and validated. The active ingredient lovastatin, present in lactone (LL) and hydroxy acid forms (LH), as well as the mycotoxin citrinin were analyzed in 19 red yeast rice products, including powders, dietary supplements, and Chinese proprietary medicines (Xuezhikang and Zhibituo). The HPTLC method including sample preparation allows a high throughput of matrix-rich samples (10 min per analysis) and is highly cost-efficient (running costs of 0.5 Euro per analysis). For a fast protocol, application volumes up to 10 µL were selected although higher application volumes will lower still the LODs, which were 30 mg/kg for LL and LH as well as 4 mg/kg for citrinin. Thanks to the minimalistic sample preparation, the overall mean recovery rate was good (109.9% ± 5.9%; repeated measurements of the three analytes per fresh sample preparation at three spike levels). Repeated calibrations (five per analyte) in the red yeast rice matrix showed highly satisfying determination coefficients (≥ 0.9991; mean 0.9996). For three analytes at three concentration levels, the obtained mean intermediate precisions in red yeast rice matrix analyzed over the whole procedure including sample preparation were highly satisfying (≤ 2.6%). Citrinin was not detectable in the samples down to the given LOD of 4.0 mg/kg for the 10-µL sample volume applied. The mean content of lovastatin in 15 RYR powders was 8.7 g/kg, with a rang of 1.5-26.2 g/kg. The content of lovastatin in Zhibituo tablets and Xuezhikang capsules was determined to be 2.7 and 11.1 g/kg, respectively. The two commercially available RYR dietary supplement samples showed the highest lovastatin contents of 40.7 and 41.4 g/kg. By these figures of merit, the HPTLC method was proven to be suited for the control of such matrix-rich, fermented food. Graphical abstract.


Assuntos
Anticolesterolemiantes/análise , Produtos Biológicos/análise , Citrinina/análise , Medicamentos de Ervas Chinesas/análise , Lovastatina/análise , Cromatografia Líquida de Alta Pressão/métodos , Cromatografia em Camada Delgada/métodos , Hidroxiácidos/análise , Lactonas/análise , Limite de Detecção
3.
Prostate ; 79(12): 1412-1419, 2019 09.
Artigo em Inglês | MEDLINE | ID: mdl-31231865

RESUMO

BACKGROUND: Statins have anticancer effects on prostate cancer both in vitro and in vivo. It is unclear whether this is due to systemic cholesterol-lowering or direct local growth inhibition in the prostate. It is also unclear whether statins can access the prostate; lipophilic statins could, in theory, pass lipid-enriched cell membranes by passive diffusion. However, statin concentrations in the human prostate have not been measured before. METHODS: The study population was based on a randomized clinical trial where 158 men with prostate cancer were randomized to use 80 mg atorvastatin (ATV) or placebo daily for a median of 27 days before radical prostatectomy. ATV and atorvastatin lactone (ATV-Lactone) concentrations in the plasma and in the prostate were measured with mass spectrometry in men randomized to the ATV arm. Linear trends between intraprostatic concentration and plasma concentration, body mass index, age, and duration of intervention were examined. The relative tissue concentrations of ATV and ATV-Lactone were calculated in prostatic tissue and plasma to evaluate drug homeostasis. Subgroup analyses were stratified by tumor and population characteristics. RESULTS: The analysis involved a total of 55 men. When limited to men whose tissue concentrations of ATV was measurable (n = 28, 50%), median ATV concentration was 212% higher in the tissue (median concentration 17.6 ng/g) compared to the plasma (median concentration 3.6 ng/mL). Also, ATV-L concentration was 590% higher in the tissue as compared to the plasma concentration. No statistically significant linear trends between the plasma and tissue concentrations were observed. When comparing the relative concentration of atorvastatin lactone over ATV, the concentrations were in balance in the plasma, In the prostate, however, the relative concentration of atorvastatin lactone was 57% lower compared to ATV (P = .009 for the difference between prostate tissue and plasma). No effect modification by tumor or population characteristics was observed. CONCLUSIONS: Measurable ATV concentrations in the prostate support ATV's ability to access the prostate from the circulation. ATV may accumulate in the prostate as intraprostatic concentrations are elevated compared to the plasma concentration.


Assuntos
Antineoplásicos/análise , Atorvastatina/análise , Próstata/química , Neoplasias da Próstata/química , Administração Oral , Idoso , Anticolesterolemiantes/administração & dosagem , Anticolesterolemiantes/análise , Anticolesterolemiantes/sangue , Antineoplásicos/administração & dosagem , Antineoplásicos/sangue , Atorvastatina/administração & dosagem , Atorvastatina/sangue , Humanos , Lactonas/administração & dosagem , Lactonas/análise , Lactonas/sangue , Masculino , Pessoa de Meia-Idade , Prostatectomia , Neoplasias da Próstata/tratamento farmacológico , Neoplasias da Próstata/cirurgia
4.
Anal Bioanal Chem ; 411(6): 1219-1228, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30617392

RESUMO

A fully automated method for the determination of lovastatin in dietary supplements containing red yeast rice has been developed. It uses a sequential injection analysis system combined with solid-phase extraction applying highly selective molecularly imprinted polymer sorbent. A miniaturized column for on-line extraction was prepared by packing 4.5 mg of the sorbent in a 5.0 × 2.5-mm-i.d. cartridge, which was used in the flow manifold. Sequential injection analysis manifold enabled all steps of lovastatin extraction and continuous spectrophotometric detection at 240 nm. A limit of detection of 60 µg g-1, a limit of quantitation of 200 µg g-1, and a linear calibration range of 200-2000 µg g-1 were achieved. Intra-day and inter-day precision values (RSD) were ≤ 6.7% and ≤ 4.9%, respectively, and method recovery values of spiked red yeast rice extracts at 200, 1000, and 2000 µg g-1 concentration levels were 82.9, 95.2, and 87.7%. Our method was used for determination of lovastatin lactone in four dietary supplements containing red yeast rice as a natural source of lovastatin, also known as monacolin K. The extracted samples were subsequently analyzed by the reference UHPLC-MS/MS method. Statistical comparison of results (F test, t test, α = 0.05) obtained by both methods did not reveal significant difference. A substantial advantage of the new automated approach is high sample throughput thanks to the analysis time of 7.5 min, miniaturization via down-scaling the extraction column, and smaller sample and solvent consumption, as well as reduced generation of waste. Graphical abstract ᅟ.


Assuntos
Anticolesterolemiantes/análise , Produtos Biológicos/análise , Suplementos Nutricionais/análise , Lovastatina/análise , Impressão Molecular/métodos , Extração em Fase Sólida/métodos , Cromatografia Líquida de Alta Pressão/instrumentação , Cromatografia Líquida de Alta Pressão/métodos , Desenho de Equipamento , Análise de Injeção de Fluxo/instrumentação , Análise de Injeção de Fluxo/métodos , Limite de Detecção , Impressão Molecular/instrumentação , Polímeros/química , Extração em Fase Sólida/instrumentação , Espectrofotometria Ultravioleta/instrumentação , Espectrofotometria Ultravioleta/métodos , Espectrometria de Massas em Tandem/instrumentação , Espectrometria de Massas em Tandem/métodos
5.
Crit Rev Food Sci Nutr ; 59(12): 1949-1975, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-29388805

RESUMO

This review reported an updated survey on the molecular functional properties of bioactive peptides derived from different Latin American ancient grains such as Maize, common Bean, Amaranth, Quinoa and Chia seeds. Seed storage proteins ecrypt in their sequences diverse peptides associated with a wide range of beneficial effects on the human health and the most studied are antihypertensive, anti-cholesterolemic, antioxidant, anti-inflammatory, anticancer, antimicrobial and immunomodulatory properties. Additionally, in the last decades molecular properties have been also used for their characterization to understand their activities and it makes them highly attractive to be incorporated into food formulations and to complement or replace some conventional cereal grains. Due to the nutraceutical effects, today, these seeds are one of the main gastronomic trends of consumption worldwide due to their nutritional benefits and are part of the shopping lists of many people, among them vegetarians, vegans, celiacs or lovers of raw food. These seeds are a legacy of pre-Columbian civilizations reason why in our time they are considered as "Superfoods of the Gods", "The pre-hispanic superfoods of the future" and "The new golden seeds of the XXI century".


Assuntos
Produtos Agrícolas , Suplementos Nutricionais/análise , Grão Comestível/química , Peptídeos/química , Proteínas de Armazenamento de Sementes/análise , Amaranthus/química , Anti-Infecciosos/análise , Anti-Inflamatórios/análise , Anticolesterolemiantes/análise , Anti-Hipertensivos/análise , Antineoplásicos/análise , Antioxidantes/análise , Chenopodium quinoa/química , Humanos , Imunomodulação , América Latina , Sementes/química , Zea mays/química
6.
Food Funct ; 9(10): 5209-5219, 2018 Oct 17.
Artigo em Inglês | MEDLINE | ID: mdl-30206618

RESUMO

The hypocholesterolemic effect and the modification of serum biomarkers of a dietary plant sterol (PS) intake, cholesterol precursors and cytokines after the consumption of milk-based fruit beverages with a milk fat globule membrane were evaluated by a randomized, double-blind, crossover, multiple dose bioavailability study. Postmenopausal women (n = 38) consumed daily 250 mL of a beverage with or without 2 g of PS added during 6 weeks in each of the study periods. With the intake of the PS-added beverage, significant decreases (mg dL-1) in serum total cholesterol (pre-treatment: 220.0 ± 27.8 vs. post-treatment: 212.9 ± 25.8; p < 0.05) and LDL-cholesterol (129.4 ± 28.5 vs. 121.7 ± 24.4; p < 0.05) were detected. The cholesterol precursor lathosterol (11.2%), markers of the dietary PS intake (campesterol 43.1% and ß-sitosterol 32.5%), and anti-inflammatory IL-10 cytokine (22.5%) increased significantly, with a concomitant significant reduction in pro-inflammatory IL-1ß (6.7%). No variations in HDL-cholesterol, other sterols (desmosterol and stigmasterol) or cytokines (IL-6, IL-8, IL-12p70 and TNF-α) were detected. These results indicated that this kind of PS-enriched milk-based fruit beverage is suitable during the period of clinical intervention, and its consumption may be an adequate way to improve PS functionality since a significant reduction in cholesterol levels has been observed. Therefore, the intake of this beverage could contribute to reduce the risk of cardiovascular disease also obtaining a beneficial effect on the serum inflammatory status in postmenopausal women.


Assuntos
Anticolesterolemiantes/metabolismo , Bebidas/análise , Citocinas/metabolismo , Glicolipídeos/metabolismo , Glicoproteínas/metabolismo , Hipercolesterolemia/dietoterapia , Lipídeos/sangue , Fitosteróis/metabolismo , Anticolesterolemiantes/análise , HDL-Colesterol/sangue , LDL-Colesterol/sangue , Citocinas/genética , Método Duplo-Cego , Feminino , Humanos , Hipercolesterolemia/sangue , Pessoa de Meia-Idade , Pós-Menopausa/metabolismo
7.
Pak J Pharm Sci ; 31(4(Supplementary)): 1577-1582, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30058551

RESUMO

A precise, sensitive and quick High Performance Liquid Chromatographic (HPLC) method for the determination of rosuvastatin calcium in bulk and tablet dosage forms has been validated. The chromatographic scheme involved: Sil-20A auto sampler, LC-20A pump, SPD-20A UV/visible detector with separation attained by C18 column at 40ºC temperature through a mobile phase of acetonitrile and buffer (50:50) at a flow rate of 1.0ml/min. The method is precise (%RSD for intra-day and inter-day extended between 1.06-1.54% and 0.103-1.78%) and linear (r2=0.9997). Limit of detection and quantification (LOD & LOQ) of the adopted method were 0.78 and 1.56µg/ml. The proposed HPLC method was established to be sensitive, precise and swift that can be proficiently adopted in quality control/quality assurance laboratories for predictable investigation of the bulk and oral solid dosage forms of rosuvastatin calcium.


Assuntos
Anticolesterolemiantes/análise , Anticolesterolemiantes/química , Rosuvastatina Cálcica/análise , Rosuvastatina Cálcica/química , Tecnologia Farmacêutica/normas , Cromatografia Líquida de Alta Pressão/métodos , Cromatografia Líquida de Alta Pressão/normas , Formas de Dosagem , Comprimidos , Tecnologia Farmacêutica/métodos
8.
J Ethnopharmacol ; 224: 290-296, 2018 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-29772355

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Morus nigra L. is a plant native to Asia, and well adapted to the Brazilian climate. It is popularly known as "amoreira preta", and is part of the National List of Plants of Interest to the Brazilian Unified Health System. It is used in folk medicine mainly to soften the effects of menopause, as anti-inflammatory, antidiabetic and antihypertensive. However, information on safe doses and use is still precarious. AIM OF THE STUDY: To identify the chemical composition of the ethanolic extract of Morus nigra L. leaves (EEMN), as well as perform a toxicological study in male and female rats. MATERIALS AND METHODS: The chemical composition of the extract was performed by HPLC/DAD. In the acute study, the dose administered was 2000 mg/kg, and signs of toxicity and mortality was observed. In the sub-acute study, the extract was administered at doses of 500, 750 and 1000 mg/kg for 28 days. Behavioral changes, object recognition test, renal and hepatic tissue assessments, biochemical and hematological parameters were determined. The extract was administered orally to male and female rats in both studies. RESULTS: Quercetin and caffeic acid showed as major compounds in the extract. In the acute treatment, the extract was classified as safe (category 5), according to the protocol. In the subacute study, there was a decrease in AST in males (750 and 1000 mg/kg) and females (1000 mg/kg), reduction of total cholesterol in females (750 and 1000 mg/kg), and increase in renal and hepatic change the LPO levels. CONCLUSION: The present investigation showed that EEMN did not present significant toxic effects when administered orally. Moreover, presented a potentially protective action of organs and possesses hypocholesterolemic activity, thus, it is shown as a promising natural source to be used in pharmacology.


Assuntos
Anticolesterolemiantes/toxicidade , Morus , Extratos Vegetais/toxicidade , Administração Oral , Animais , Anticolesterolemiantes/análise , Catalase/metabolismo , Colesterol/sangue , Feminino , Rim/efeitos dos fármacos , Rim/metabolismo , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Reconhecimento Visual de Modelos/efeitos dos fármacos , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/toxicidade , Extratos Vegetais/análise , Folhas de Planta/química , Ratos Wistar , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo , Testes de Toxicidade Aguda , Testes de Toxicidade Subaguda
9.
Plant Foods Hum Nutr ; 73(2): 101-107, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29679358

RESUMO

In previous studies, it has not been reported that protein isolated from chia interferes favorably with antibacterial activity, and reduces cholesterol synthesis. The objective of this study was to determine whether commonly used commercial microbial proteases can be utilized to generate chia protein-based antibacterial and hypocholesterolemic hydrolysates/peptides, considering the effects of protein extraction method. Alcalase, Flavourzyme and sequential Alcalase-Flavourzyme were used to produce hydrolysates from chia protein (CF), protein-rich fraction (PRF) and chia protein concentrates (CPC1 and CPC2). These hydrolysates were evaluated for their antimicrobial activity against Gram-positive (G+) and Gram-negative (G-) microorganisms. The protein hydrolysates were purified by ultrafiltration through a membrane with 3 kDa nominal molecular weight, for evaluation of hypocholesterolemic activity. An inhibition zone was observed when the hydrolysate was tested against S. aureus, and minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) values were obtained. Peptides from chia protein with molecular mass lower than 3 kDa reduced up to 80.7% of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase) enzymatic reaction velocity. It was also observed that, independent of the method used to obtain chia proteins, the fractions showed relevant bioactivity. Moreover, the intensity of the bioactivity varied with the method for obtaining the protein and with the enzyme used in the hydrolysis process. This is the first report to demonstrate that chia peptides are able to inhibit cholesterol homeostasis.


Assuntos
Antibacterianos/farmacologia , Anticolesterolemiantes/farmacologia , Peptídeos/farmacologia , Hidrolisados de Proteína/farmacologia , Salvia/química , Staphylococcus aureus/efeitos dos fármacos , Antibacterianos/análise , Antibacterianos/isolamento & purificação , Anticolesterolemiantes/análise , Anticolesterolemiantes/isolamento & purificação , Colesterol , Endopeptidases/metabolismo , Hidrólise , Peso Molecular , Peptídeo Hidrolases/metabolismo , Peptídeos/análise , Peptídeos/isolamento & purificação , Hidrolisados de Proteína/análise , Hidrolisados de Proteína/isolamento & purificação , Subtilisinas/metabolismo
10.
Food Funct ; 9(4): 2121-2135, 2018 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-29644368

RESUMO

The present investigation was aimed to study the effect of detoxification on the nutrients and antinutrients of wild apricot kernel followed by its hypocholesterolemic effect in male Wistar albino rats. The results revealed a non-significant (p > 0.05) effect of detoxification on the proximate composition except total carbohydrates and protein content. However, detoxification led to a significant (p < 0.05) decrease in l-ascorbic acid (76.82%), ß-carotene (25.90%), dietary fiber constituents (10.51-28.92%), minerals (4.76-31.08%) and antinutritional factors (23.92-77.05%) (phenolics, tannins, trypsin inhibitor activity, saponins, phytic acid, alkaloids, flavonoids, oxalates) along with the complete removal (100%) of bitter and potentially toxic hydrocyanic acid (HCN). The quality parameters of kernel oil indicated no adverse effects of detoxification on free fatty acids, lipase activity, acid value and peroxide value, which remained well below the maximum permissible limit. Blood lipid profile demonstrated that the detoxified apricot kernel group exhibited significantly (p < 0.05) increased levels of HDL-cholesterol (48.79%) and triglycerides (15.09%), and decreased levels of total blood cholesterol (6.99%), LDL-C (22.95%) and VLDL-C (7.90%) compared to that of the raw (untreated) kernel group. Overall, it can be concluded that wild apricot kernel flour could be detoxified efficiently by employing a simple, safe, domestic and cost-effective method, which further has the potential for formulating protein supplements and value-added food products.


Assuntos
Anticolesterolemiantes/análise , Antimetabólitos/análise , Contaminação de Alimentos/prevenção & controle , Manipulação de Alimentos , Alimentos Especializados/análise , Prunus armeniaca/química , Sementes/química , Animais , Anticolesterolemiantes/efeitos adversos , Anticolesterolemiantes/economia , Anticolesterolemiantes/uso terapêutico , Antimetabólitos/efeitos adversos , Contaminação de Alimentos/economia , Ingredientes de Alimentos/efeitos adversos , Ingredientes de Alimentos/análise , Ingredientes de Alimentos/economia , Indústria de Processamento de Alimentos/economia , Alimentos Especializados/efeitos adversos , Alimentos Especializados/economia , Humanos , Cianeto de Hidrogênio/efeitos adversos , Cianeto de Hidrogênio/análise , Hipercolesterolemia/sangue , Hipercolesterolemia/prevenção & controle , Resíduos Industriais/efeitos adversos , Resíduos Industriais/análise , Resíduos Industriais/economia , Masculino , Valor Nutritivo , Tamanho da Partícula , Prunus armeniaca/efeitos adversos , Prunus armeniaca/crescimento & desenvolvimento , Distribuição Aleatória , Ratos Wistar , Reprodutibilidade dos Testes , Sementes/efeitos adversos , Sementes/crescimento & desenvolvimento , Meio Selvagem , beta Caroteno/análise , beta Caroteno/uso terapêutico
11.
Farm. comunitarios (Internet) ; 10(1): 33-40, mar. 2018. tab, graf
Artigo em Espanhol | IBECS | ID: ibc-171291

RESUMO

Introducción: Las dislipemias son alteraciones de las lipoproteínas que transportan el colesterol y los triglicéridos, siendo consideradas factor de riesgo de enfermedades cardiovasculares. La eficacia de la utilización de productos vegetales cono el ajo (Allium sativum) para prevenir y tratar dislipemias es discutida. Hay pocos estudios publicados sobre el efecto de estos productos en el ámbito de la farmacia comunitaria. Objetivos: Estudiar la variación de los valores de colesterol total en pacientes tratados con un complemento alimenticio a base de ajo en cápsulas. Relacionar dichos valores con factores demográficos y con la toma o no de medicamentos hipocolesterolemiantes de prescripción médica (MHPM). Comprobar si los resultados obtenidos concuerdan con los encontrados en la bibliografía. Material y métodos: Estudio experimental y controlado realizado en una farmacia comunitaria. Los pacientes que aceptaron participar se dividieron aleatoriamente en dos grupos, grupo intervención (GI) que tomaba complemento alimenticio de ajo y grupo control (GC) que no lo tomaba. Resultados: 59 sujetos, 29 pertenecientes al GC y 30 al GI. Mayor descenso del colesterol total en los que no tomaban MHPM, pero no puede atribuirse al efecto del complemento alimenticio administrado ya que el descenso se produce en los dos grupos. No se encontraron diferencias significativas entre los grupos. En los que ya tomaban MHP, el efecto del complemento alimenticio fue prácticamente inapreciable. Conclusiones: En las condiciones del estudio realizado, el efecto del complemento alimenticio de ajo no parece ser lo suficientemente efectivo como para reducir los niveles de colesterol de forma significativa (AU)


Introduction: Dyslipidemia is an abnormal level of the lipoproteins that transport cholesterol and triglycerides, and it is considered a risk factor for cardiovascular diseases. The effectiveness of using plant-based products like garlic (Allium sativum) to prevent and treat dyslipidemia is under debate. Few studies have been published on the effect of these products in the context of the community pharmacy. Objectives: Study the variation of total cholesterol values in patients treated with a garlic-based dietary supplement in capsule form. Link these values to demographic factors and to the use or non-use of prescription cholesterol-lowering drugs. Determine whether the results are consistent with those found in the bibliography. Materials and Methods: Experimental, controlled study conducted in a community pharmacy. The patients who agreed to participate were divided randomly into two groups, the intervention group (IG), which took a garlic-based dietary supplement, and the control group (CG), which did not take it. Results: 59 subjects, 29 corresponding to the CG and 30 to the IG. Greater decrease in total cholesterol in the subjects who did not take the prescription cholesterol-lowering drugs, but this result cannot be attributed to the effect of the dietary supplement administered since a decrease occurred in both groups. No significant differences were detected between the groups. In the subjects who were already taking the prescription cholesterol-lowering drugs, the effect of the dietary supplement was practically negligible. Conclusions: Under the conditions of the study, administration of the garlic-based dietary supplement does not appear to be effective enough to reduce cholesterol levels significantly (AU)


Assuntos
Humanos , Hipercolesterolemia/dietoterapia , Alho , Extratos Vegetais/uso terapêutico , Anticolesterolemiantes/análise , Avaliação de Resultado de Intervenções Terapêuticas , Serviços Comunitários de Farmácia/estatística & dados numéricos , Fenômenos Fisiológicos da Nutrição do Lactente , Estudos de Casos e Controles
12.
Food Funct ; 9(2): 925-936, 2018 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-29313544

RESUMO

Kenaf is one of the important commercial fiber crops worldwide and defatted kenaf seed meal (DKSM) is a secondary by-product from the kenaf industry. Thus, efforts to turn this low-cost agricultural waste into value-added functional food ingredients will definitely bring advantageous impacts to the community health, environment and economy. The present study was aimed to investigate the cardioprotective properties of DKSM and its phenolics-saponins rich extract (PSRE) in diet-induced hypercholesterolemic rat model. Hypercholesterolemia was induced in Sprague-Dawley rats via atherogenic diet feeding and dietary interventions were conducted by incorporating DKSM (15% and 30%) and equivalent levels of PSRE (2.3% and 4.6%, respectively, equivalent to the total content of phenolics and saponins in DKSM groups) into the atherogenic diets. After 10 weeks of DKSM and PSRE supplementation, the hepatosomatic index, hepatosteatosis, serum lipid profile, Castelli risk indexes as well as hepatic and renal functions of hypercholesterolemic rats were significantly improved (p < 0.05). Besides, the levels of hepatic Hmgcr and serum Pcsk9 were lowered, along with transcriptional upregulations of hepatic Cyp7a1, Abca1, Lcat, ApoA2 and ApoE (p < 0.05). The gene expression of hepatic Ldlr was marginally enhanced by DKSM supplementation (p > 0.05), but superiorly upregulated by PSRE (p < 0.05). The combined results showed that hypercholesterolemia and the atherogenic risk in rats were effectively attenuated by DKSM and PSRE supplementation, possibly via modulations of multiple vital processes in hepatic cholesterol metabolism. Furthermore, phenolics and saponins may be the bioactives conferring DKSM and PSRE with their anti-hypercholesterolemic properties. In conclusion, DKSM and PSRE are prospective cardioprotective functional food ingredients for hypercholesterolemic individuals.


Assuntos
Anticolesterolemiantes/administração & dosagem , Hibiscus/química , Hipercolesterolemia/tratamento farmacológico , Hipercolesterolemia/genética , Fenóis/administração & dosagem , Saponinas/administração & dosagem , Animais , Anticolesterolemiantes/análise , Apolipoproteína A-II/genética , Apolipoproteína A-II/metabolismo , LDL-Colesterol/metabolismo , Dieta Aterogênica/efeitos adversos , Suplementos Nutricionais/análise , Humanos , Hipercolesterolemia/metabolismo , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Fenóis/análise , Pró-Proteína Convertase 9/genética , Pró-Proteína Convertase 9/metabolismo , Ratos , Ratos Sprague-Dawley , Saponinas/análise , Sementes/química
13.
Drug Test Anal ; 10(3): 609-617, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-28758363

RESUMO

We developed and validated a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method to detect and quantitate 14 anti-diabetic, 2 anti-obesity, and 3 cholesterol-lowering drugs in botanical dietary supplements marketed for blood sugar management. Many botanical dietary supplements which carry label statements related to blood sugar management are available over the Internet. Potential adulteration of such dietary supplements with anti-diabetic and other prescription drugs, some of which have been removed from the market due to adverse events, is of concern. No significant matrix effects were observed and mean recoveries of all 19 analytes from a single product matrix were 88 to 113% at spiking concentrations from 500 to 2000 µg/g. Mean recoveries of metformin, phenformin, and sibutramine from matrices prepared from multiple product composites ranged from 93 to 115% at a spiking concentration of 100 µg/g. The relative standard deviations (RSD) (%) of intra-day analyses ranged from 0.2 to 13 for all recovery studies. Eighty dietary supplements obtained in the USA and carrying label statements related to blood sugar management were analyzed using this method and none were found to be adulterated with the above 19 drugs. Two products obtained outside of the USA and known to be adulterated were also analyzed by this method and found to contain phenformin, glibenclamide, and sibutramine. This method provided satisfactory selectivity, linearity, accuracy, precision, and sensitivity for rapid determination of 19 drugs and has broad applicability for the analysis of dietary supplements for possible adulteration with these compounds.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Suplementos Nutricionais/análise , Hipoglicemiantes/análise , Extratos Vegetais/análise , Espectrometria de Massas em Tandem/métodos , Fármacos Antiobesidade/análise , Anticolesterolemiantes/análise , Contaminação de Medicamentos , Limite de Detecção
14.
Nutr. clín. diet. hosp ; 38(1): 128-134, 2018. tab, graf
Artigo em Português | IBECS | ID: ibc-175414

RESUMO

Introdução: O colesterol é essencial para a vida. Em excesso no sangue, deposita-se nas paredes das artérias promovendo seu estreitamento ou obstrução. Objetivos: O objetivo foi verificar o possível efeito hipocolesterolêmico da semente de linhaça. Materiais e Métodos: Utilizaram-se 30 ratos Wistar fêmeas divididos em três grupos: Controle, Hipercolesterolêmico, e Linhaça. Os parâmetros avaliados foram: ingestão hídrica; ingestão de ração; peso corporal; gordura peritoneal e níveis de colesterol; Resultados e Discussão: O grupo controle apresentou maior ingestão hídrica (57,46 ± 0,13mL) e ração (30,68 ± 1,96g) quando comparados ao hipercolesterolêmico e linhaça; Para peso corporal total, somente o controle não sofreu alteração; Em relação ao acúmulo de gordura peritoneal, o grupo hipercolesterolêmico se sobressaiu (17,06 ± 3,99g) em comparação ao linhaça e ao controle; para os níveis de colesterol sérico, o grupo controle obteve (1,14 ± 0,14g), sendo observado portanto no grupo linhaça (1,66 ± 0,16g), uma maior aproximação para o resultado do grupo controle do que do hipercolesterolêmico (2,20 ± 6,32g), resultado que nos leva a reconhecer que a linhaça surtiu efeito benéfico sobre o colesterol. Conclusão: Os resultados obtidos demonstram benefícios na utilização da semente para redução dos níveis de gordura peritoneal, peso total e colesterol


Introduction: Cholesterol is essential for life, when in excess in blood, is deposited on the artery walls promoting its narrowing or obstruction. Objectives: The objective was to verify the possible hypocholesterolemic effect of linseed. Methods: We used 30 female Wistar rats divided into three groups: control, hypercholesterolemic, and linseed. The evaluated parameters were: water intake, feed intake, body weight, peritoneal fat, and cholesterol levels; Results and Discussion: The results were: the control group had a higher fluid intake (57.46 ± 0.13ml) and feed (30.68 ± 1.96g) when compared to hypercholesterolemic and linseed; for total body weight, only the control group did not change; in relation to the accumulation of peritoneal fat, the hypercholesterolemic group stood out (17.06 ± 3.99g) compared to linseed and control; for serum cholesterol levels, the control group obtained (1.14 ± 0.14g), thus being observed in linseed group (1.66 ± 0.16g), closer to the result of the control group than the hypercholesterolemic (2.20 ± 6.32g), a result that leads us to recognize that linseed has had a beneficial effect on cholesterol.Conclusion: The results obtained demonstrate benefits in the use of the seed to reduce levels of peritoneal fat, total weight and cholesterol


No disponible


Assuntos
Animais , Ratos , Linho , Sementes , Anticolesterolemiantes/análise , Hipercolesterolemia/dietoterapia , Sobrepeso/dietoterapia , Modelos Animais de Doenças , Estudos de Casos e Controles , Ingestão de Líquidos , Leptina , Arginina/farmacocinética , Glutamina/farmacocinética , Histidina/farmacocinética
15.
J Oleo Sci ; 66(6): 551-556, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28566641

RESUMO

Rice bran oil (RBO) is healthy gift generously given by nature to mankind. RBO is obtained from rice husk, a byproduct of rice milling industry and is gaining lot of importance as cooking oil due to presence of important micronutrient, gamma oryzanol. Its high smoke point is beneficial for its use for frying and deep frying of food stuff. It is popular because of balanced fatty acid profile (most ideal ratio of saturated, monounsaturated and polyunsaturated fatty acids), antioxidant capacity, and cholesterollowering abilities. Rice bran wax which is secondary by-product obtained as tank settling from RBO is used as a substitute for carnauba wax in cosmetics, confectionery, shoe creams etc. It can be also used as a source for fatty acid and fatty alcohol. The article is intended to highlight for the importance of RBO and its applications.


Assuntos
Óleos Industriais , Óleos Vegetais/química , Anticolesterolemiantes/análise , Antioxidantes/análise , Cosméticos , Ácidos Graxos/análise , Álcoois Graxos , Fenilpropionatos , Óleo de Farelo de Arroz , Ceras
16.
Acta Pharm ; 66(4): 479-490, 2016 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-27749253

RESUMO

Two methods were developed for separation and quantitation of amlodipine (AML) and atorvastatin (ATV) in the presence of their acidic degradation products. The first method was a simple isocratic RP-HPLC method while the second was capillary electrophoresis (CE). Degradation products were obtained by acidic hydrolysis of the two drugs and their structures were elucidated for the first time by IR and MS spectra. Degradation products did not interfere with the determination of either drug and the assays were therefore stability-indicating. The linearity of the proposed methods was established over the ranges 1-50 µg mL-1 for AML and ATV in the HPLC method and in the range of 3-50 and 4-50 µg mL-1 for AML and ATV, respectively, in the CE method. The proposed methods were validated according to ICH guidelines. The methods were successfully applied to estimation of AML and ATV in combined tablets.


Assuntos
Anlodipino/análise , Anticolesterolemiantes/análise , Anti-Hipertensivos/análise , Atorvastatina/análise , Bloqueadores dos Canais de Cálcio/análise , Química Farmacêutica/métodos , Inibidores de Hidroximetilglutaril-CoA Redutases/análise , Anlodipino/análogos & derivados , Anlodipino/química , Anticolesterolemiantes/química , Anti-Hipertensivos/química , Atorvastatina/análogos & derivados , Atorvastatina/química , Bloqueadores dos Canais de Cálcio/química , Calibragem , Cromatografia Líquida de Alta Pressão , Cromatografia de Fase Reversa , Combinação de Medicamentos , Estabilidade de Medicamentos , Eletroforese Capilar , Ácidos Heptanoicos/química , Ácido Clorídrico/química , Hidrólise/efeitos dos fármacos , Inibidores de Hidroximetilglutaril-CoA Redutases/química , Limite de Detecção , Estrutura Molecular , Pirróis/química , Reprodutibilidade dos Testes , Comprimidos
17.
Rev. fitoter ; 16(1): 5-14, jun. 2016. ilus, tab, graf
Artigo em Espanhol | IBECS | ID: ibc-155715

RESUMO

Es ampliamente conocido que los niveles altos de colesterol están relacionados con el riesgo cardiovascular. La levadura de arroz rojo o levadura roja de arroz es un producto obtenido a partir de una levadura (Monascus purpureus Went.), que crece sobre este cereal. Entre sus componentes destaca la monacolina K, también conocida como lovastatina, sustancia relacionada con la disminución del colesterol mediante la inhibición de la HMG-CoA reductasa. El policosanol, mezcla de alcoholes alifáticos, obtenido de la caña de azúcar (Saccharum officinarum L.), además de modular dicha enzima, aumenta la actividad de los receptores LDL y tiene un efecto antioxidante y antiagregante. Mediante este trabajo se aportan los resultados de 65 pacientes en los cuales se ha observado una disminución media, estadísticamente significativa, de los niveles de colesterol (22% del colesterol total y 29% del LDL) y una disminución del 22% de los triglicéridos, tras tomar durante 2 meses un producto compuesto por: levadura roja de arroz con un contenido diario de 10 mg monacolina K y 14 mg de policosanol extraído de la caña de azúcar. La combinación de la monacolina K y el policosanol se plantean como una opción en pacientes con riesgo cardiovascular bajo o moderado (AU)


É amplamente conhecido que os níveis elevados de colesterol estão associados a um risco acrescido de doença cardiovascular. O arroz vermelho fermentado (ou levedura de arroz vermelho) é um produto obtido a partir de uma levedura (Monascus purpureus Went.), que cresce no arroz. Entre os seus componentes destaca-se a monacolina K, também conhecida como lovastatina, substância relacionada com a redução do colesterol através da inibição da HMG-CoA redutase. O policosanol, que consiste numa mistura de álcoois alifáticos de cadeia longa obtida a partir da cana-de-açúcar (Saccharum officinarum L.), além de modular a mesma enzima (HMG-CoA redutase), aumenta a actividade de receptores de LDL e tem efeitos antioxidantes e antiagregantes plaquetários. Este trabalho reporta os resultados de 65 participantes nos quais se observou uma diminuição média estatisticamente significativa do valor de colesterol (22% do colesterol total e 29% do LDL), assim como uma diminuição de 22% do valor dos triglicéridos, após a toma, durante dois meses, de um produto composto por arroz vermelho fermentado e policosanol, correspondendo a uma toma diária de 10 mg de monacolina K e 14 mg de policosanol. Assim, a associação de monacolina K, e policosanol apresenta-se como uma opção para doentes com risco cardiovascular baixo ou moderado (AU)


It is widely known that high cholesterol levels are associated with cardiovascular risk. Red yeast rice or red rice yeast is a product obtained from a yeast (Monascus purpureus Went.), which grows on rice. Among its constituents, it stand out monacolin K, also known as lovastatin, compound related to the cholesterol lowering effect through the inhibition of the HMG-CoA reductase. Polycosanol is a mixture of long chain aliphatic alcohols obtained from sugar cane (Saccharum officinarum L.). In addition of modulating that enzyme, it increases the activity of LDL receptors and has antioxidant and antiplatelet effect. In the present work, results in 65 patients treated for 2 mounts with a product combining red yeast rice (providing 10 mg/day of monacolin K) and policosanol from sugar cane (14 mg/day). An average decrease, statistically significant, of blood cholesterol (22% of total cholesterol and 29% of LDL) and triglycerides (22% ) has been observed. The combination of monacolin K and polycosanol is considered an option for patients with low or moderate cardiovascular risk (AU)


Assuntos
Oryza , Anticolesterolemiantes/análise , Anticolesterolemiantes/uso terapêutico , Colesterol/uso terapêutico , Hiperlipidemias/terapia , Monascus , Saccharum , Fitoterapia/métodos , Hiperlipidemias/prevenção & controle , Doenças Cardiovasculares/prevenção & controle , Triglicerídeos/uso terapêutico , Doenças Cardiovasculares/classificação , Fitoterapia , Extratos Vegetais/uso terapêutico , Estudos Prospectivos
18.
Cell Physiol Biochem ; 38(5): 1815-30, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27160211

RESUMO

BACKGROUND/AIMS: To develop a suitable hepatocyte-like cell model that could be a substitute for primary hepatocytes with essential transporter expression and functions. Induced hepatocyte-like (iHep) cells directly reprogrammed from mice fibroblast cells were fully characterized. METHODS: Naïve iHep cells were transfected with nuclear hepatocyte factor 4 alpha (Hnf4α) and treated with selected small molecules. Sandwich cultured configuration was applied. The mRNA and protein expression of transporters were determined by Real Time PCR and confocal. The functional transporters were estimated by drug biliary excretion measurement. The inhibition of bile acid efflux transporters by cholestatic drugs were assessed. RESULTS: The expression and function of p-glycoprotein (P-gp), bile salt efflux pump (Bsep), multidrug resistance-associated protein 2 (Mrp2), Na+-dependent taurocholate cotransporting polypeptide (Ntcp), and organic anion transporter polypedtides (Oatps) in iHep cells were significantly improved after transfection of hepatocyte nuclear factor 4 alpha (Hnf4α) and treatment with selected inducers. In vitro intrinsic biliary clearances (CLb,int) of optimized iHep cells for rosuvastatin, methotrexate, d8-TCA (deuterium-labeled sodium taurocholate acid) and DPDPE ([D-Pen2,5] enkephalin hydrate) correlated well with that of sandwich-cultured primary mouse hepatocytes (SCMHs) (r2 = 0.984). Cholestatic drugs were evaluated and the results were compared well with primary mice hepatocytes. CONCLUSION: The optimized iHep cells expressed functional drug transporters and were comparable to primary mice hepatocytes. This study suggested direct reprogramming could provide a potential alternative to primary hepatocytes for drug candidate hepatobiliary disposition and hepatotoxicity screening.


Assuntos
Anticolesterolemiantes/metabolismo , Reprogramação Celular , Fator 4 Nuclear de Hepatócito/metabolismo , Proteínas de Membrana Transportadoras/metabolismo , Membro 1 da Subfamília B de Cassetes de Ligação de ATP/genética , Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo , Membro 11 da Subfamília B de Transportadores de Cassetes de Ligação de ATP , Transportadores de Cassetes de Ligação de ATP/genética , Transportadores de Cassetes de Ligação de ATP/metabolismo , Animais , Anticolesterolemiantes/análise , Anticolesterolemiantes/toxicidade , Ácidos e Sais Biliares/metabolismo , Técnicas de Cultura de Células , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , D-Penicilina (2,5)-Encefalina/análise , D-Penicilina (2,5)-Encefalina/metabolismo , D-Penicilina (2,5)-Encefalina/toxicidade , Fibroblastos/citologia , Fibroblastos/metabolismo , Expressão Gênica/efeitos dos fármacos , Fator 4 Nuclear de Hepatócito/genética , Hepatócitos/citologia , Hepatócitos/metabolismo , Proteínas de Membrana Transportadoras/genética , Metotrexato/análise , Metotrexato/metabolismo , Metotrexato/toxicidade , Camundongos , Camundongos Endogâmicos ICR , Proteínas Associadas à Resistência a Múltiplos Medicamentos/genética , Proteínas Associadas à Resistência a Múltiplos Medicamentos/metabolismo , Transportadores de Ânions Orgânicos/genética , Transportadores de Ânions Orgânicos/metabolismo , Transportadores de Ânions Orgânicos Dependentes de Sódio/genética , Transportadores de Ânions Orgânicos Dependentes de Sódio/metabolismo , Rosuvastatina Cálcica/análise , Rosuvastatina Cálcica/metabolismo , Rosuvastatina Cálcica/toxicidade , Bibliotecas de Moléculas Pequenas/química , Bibliotecas de Moléculas Pequenas/farmacologia , Simportadores/genética , Simportadores/metabolismo
19.
Plant Foods Hum Nutr ; 71(2): 183-9, 2016 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-27086310

RESUMO

The phenolic constituents of the aqueous-ethanolic extract of Tunisian Ficus carica (F. carica) fruit (FE) and its antihyperlipidemic and antioxidant activities in high-fat diet-induced hyperlipidemic rats (HFD) were evaluated. The obtained results demonstrated that the FE improved the lipid profile by decreasing the total cholesterol, triglyceride, low-density lipoprotein cholesterol and increasing high-density lipoprotein cholesterol levels. It also reduced the content of thiobarbituric acid-reactive substances and increased the antioxidant enzymes in liver, heart and kidney in HFD-fed rats. These antihyperlipidemic effects and in vivo antioxidative effects correlated with the in vitro phenolic content scavenging ability. Thus, the major phenolic compounds were identified using reversed-phase ultra-high-performance liquid chromatography (RP-UHPLC) coupled with two detection systems: diode-array detection (DAD) and quadrupole time-of-flight (QTOF) mass spectrometry (MS). Therefore, in the negative ionization mode, 28 phenolic compounds, including hydroxybenzoic acids, hydroxycinnamic acids, flavanoids and hydroxycoumarins were characterized. Dihydroxybenzoic acid di-pentoside, the flavonol quercetin 3-O-rutinoside and the flavone assigned as apigenin 8-C-glucoside were the main representative compounds in 'Tounsi' fruits. This work was complemented by the detection of seven other phenolic compounds in the positive ionization mode, including anthocyanins and furanocoumarins. Overall, these results have shown that the FE has a significant hypocholesterolemic effect and antioxidant activity in HFD-fed rats. This beneficial effect may be partly due to these phenolic constituents, especially vitexin, dihydroxybenzoic acid di-pentoside as well as rutin.


Assuntos
Anticolesterolemiantes/análise , Antioxidantes/análise , Ficus/química , Hiperlipidemias/prevenção & controle , Fenóis/análise , Animais , Cromatografia de Fase Reversa , Dieta Hiperlipídica/efeitos adversos , Modelos Animais de Doenças , Frutas/química , Humanos , Hiperlipidemias/induzido quimicamente , Peroxidação de Lipídeos , Masculino , Espectrometria de Massas , Ratos
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