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1.
J Sci Food Agric ; 102(3): 1002-1011, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-34312873

RESUMO

BACKGROUND: Astaxanthin (ASTA) is a kind of food-derived active ingredient (FDAI) with antioxidant and antidiabetic functions. It is nontoxic but its poor solubility and low bioavailability hinder its application in the food industry. In this study, a novel carrier, polyethylene glycol-grafted chitosan (PEG-g-CS) was applied to enhance the bioavailability of astaxanthin. It encapsulated astaxanthin completely by solvent evaporation to manufacture astaxanthin using poly (ethylene glycol)-graft-chitosan nanoparticles (ASTA-PEG-g-CS) nanoparticles to improve absorption. RESULTS: The ASTA-PEG-g-CS nanoparticles were spherical, with a particle size below 200 nm and a ζ potential of about -26 mV. Polyethylene glycol-grafted chitosan can encapsulate astaxanthin well, and the encapsulated astaxanthin was released rapidly - in 15 min in an in vitro release study. In a rat single-pass intestinal perfusion study, a low concentration of ASTA-PEG-g-CS nanoparticle (0.2 µg mL-1 ) was better absorbed in the intestine. In particular, the jejunum could absorb most astaxanthin without a change in the concentration. An in vivo release study also demonstrated that ASTA-PEG-g-CS nanoparticles enhanced oral bioavailability significantly. CONCLUSION: This novel carrier, PEG-g-CS, provided a simple way to encapsulate food, which improved the bioavailability of hydrophobic ingredients. © 2021 Society of Chemical Industry.


Assuntos
Intestinos/metabolismo , Administração Oral , Animais , Disponibilidade Biológica , Quitosana/química , Portadores de Fármacos/química , Composição de Medicamentos , Interações Hidrofóbicas e Hidrofílicas , Absorção Intestinal , Masculino , Nanopartículas/química , Tamanho da Partícula , Polietilenoglicóis/química , Ratos , Ratos Sprague-Dawley , Xantofilas/administração & dosagem , Xantofilas/química , Xantofilas/farmacocinética
2.
Res Vet Sci ; 138: 69-78, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34111716

RESUMO

Astaxanthin (AST) is a red pigment of carotenoid and is considered a high-quality keto-carotenoid pigment with food, livestock, cosmetic, therapeutic and nutraceutical proposes. Astaxanthin exists naturally in fish, crustacean, algae, and birds that naturally exists, principally as fatty acid esters. Many investigations have exhibited the beneficial impacts of astaxanthin when utilized as a pharmaceutical agent in animal nutrition. Astaxanthin has a variety of considerable biological actions, such as being antihypertensive, an antioxidant, anti-obesity properties, and anti-carcinogenic. Astaxanthin has recently acquired popularity as a powerful immunomodulator to maintain the health status and well-being of both animals and humans. The use of astaxanthin is broadly utilized in medical sciences and the nutrition pf aquatic species; however, it presently has limited applications in broader animal nutrition. Understanding astaxanthin's structure, source, and mode of action in the body provides a conceptual base for its clinical application and could enhance the screening of compounds associated with the treatment of many diseases. This review article aims to clarify the important aspects of astaxanthin such as its synthesis, bioavailability, and therapeutics actions, with special interest in practical applications. Awareness of this benefits and production is expected to aid the livestock industry to develop nutritional strategies that ensure the protection of animal health.


Assuntos
Criação de Animais Domésticos , Fatores Imunológicos , Gado , Animais , Disponibilidade Biológica , Fatores Imunológicos/síntese química , Fatores Imunológicos/farmacocinética , Fatores Imunológicos/uso terapêutico , Xantofilas/síntese química , Xantofilas/farmacocinética , Xantofilas/uso terapêutico
3.
Pharmacol Res ; 166: 105479, 2021 04.
Artigo em Inglês | MEDLINE | ID: mdl-33549728

RESUMO

Astaxanthin is a natural C40 carotenoid with numerous reported biological functions, most of them associated with its antioxidant and anti-inflammatory activity, standing out from other antioxidants as it has shown the highest oxygen radical absorbance capacity (ORAC), 100-500 times higher than ⍺-tocopherol and a 10 times higher free radical inhibitory activity than related antioxidants (α-tocopherol, α-carotene, ß -carotene, lutein and lycopene). In vitro and in vivo studies have associated astaxanthin's unique molecular features with several health benefits, including neuroprotective, cardioprotective and antitumoral properties, suggesting its therapeutic potential for the prevention or co-treatment of dementia, Alzheimer, Parkinson, cardiovascular diseases and cancer. Benefits on skin and eye health promotion have also been reported, highlighting its potential for the prevention of skin photo-aging and the treatment of eye diseases like glaucoma, cataracts and uveitis. In this review, we summarize and discuss the currently available evidence on astaxanthin benefits, with a particular focus on human clinical trials, including a brief description of the potential mechanisms of action responsible for its biological activities.


Assuntos
Anti-Inflamatórios/uso terapêutico , Antioxidantes/uso terapêutico , Animais , Anti-Inflamatórios/farmacocinética , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacocinética , Antioxidantes/farmacologia , Doenças Cardiovasculares/tratamento farmacológico , Ensaios Clínicos como Assunto , Desenvolvimento de Medicamentos , Descoberta de Drogas , Humanos , Neoplasias/tratamento farmacológico , Doenças Neurodegenerativas/tratamento farmacológico , Xantofilas/farmacocinética , Xantofilas/farmacologia , Xantofilas/uso terapêutico
4.
Mol Nutr Food Res ; 65(2): e2000405, 2021 01.
Artigo em Inglês | MEDLINE | ID: mdl-33215789

RESUMO

SCOPE: Fucoxanthin is converted to fucoxanthinol and amarouciaxanthin A in the mouse body. However, further metabolism such as cleavage products (i.e., apocarotenoids) remains unclear. The fucoxanthin-derived apocarotenoid in vivo is investigated and the anti-inflammatory effect of apocarotenoids with fucoxanthin partial structure such as allenic bond and epoxide residue against activated macrophages and adipocytes in vitro is evaluated. METHODS AND RESULTS: LC-MS analysis indicates the presence of paracentrone, a C31 -allenic-apocarotenoid, in white adipose tissue of diabetic/obese KK-Ay and normal C57BL/6J mice fed 0.2% fucoxanthin diet for 1 week. In lipopolysaccharide-activated RAW264.7 macrophages, paracentrone as well as C26 - and C28 -allenic-apocarotenoids suppresses the overexpression of inflammatory factors. Further, apo-10'-fucoxanthinal, a fucoxanthin-derived apocarotenoid which retained epoxide residue, exhibits a most potent anti-inflammatory activity through regulating mitogen-activated protein kinases and nuclear factor-κB inflammatory signal pathways. In contrast, ß-apo-8'-carotenal without allenic bond and epoxide residue lacks suppressed inflammation. In 3T3-L1 adipocytes, paracentrone, and apo-10'-fucoxanthinal downregulate the mRNA expression of proinflammatory mediators and chemokines induced by co-culture with RAW264.7 cells. CONCLUSION: Dietary fucoxanthin accumulates as paracentrone as well as fucoxanthinol and amarouciaxanthin A in the mouse body. Allenic bond and epoxide residue of fucoxanthin-derived apocarotenoids have pivotal roles for anti-inflammatory action against activated macrophages and adipocytes.


Assuntos
Adipócitos/efeitos dos fármacos , Carotenoides/análise , Carotenoides/farmacologia , Macrófagos/efeitos dos fármacos , Xantofilas/farmacocinética , Células 3T3-L1 , Tecido Adiposo Branco/efeitos dos fármacos , Tecido Adiposo Branco/metabolismo , Animais , Anti-Inflamatórios não Esteroides/farmacologia , Carotenoides/metabolismo , Mediadores da Inflamação/metabolismo , Lipopolissacarídeos/farmacologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Obesos , Células RAW 264.7 , Xantofilas/metabolismo
5.
Mar Drugs ; 18(6)2020 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-32492769

RESUMO

Siphonaxanthin has been known to possess inhibitory effects against obesity, inflammation, and angiogenesis. However, little information on its in vivo bioavailability and biotransformation is available. To assess the bioavailability and metabolism of siphonaxanthin, its absorption and accumulation were evaluated using intestinal Caco-2 cells and Institute of Cancer Research (ICR) mice. Siphonaxanthin was absorbed and exhibited non-uniform accumulation and distribution patterns in tissues of ICR mice. Notably, in addition to siphonaxanthin, three main compounds were detected following dietary administration of siphonaxanthin. Because the compounds showed changes on mass spectra compared with that of siphonaxanthin, they were presumed to be metabolites of siphonaxanthin in ICR mice. Siphonaxanthin mainly accumulated in stomach and small intestine, while putative metabolites of siphonaxanthin mainly accumulated in liver and adipose tissues. Furthermore, siphonaxanthin and its putative metabolites selectively accumulated in white adipose tissue (WAT), especially mesenteric WAT. These results provide useful evidence regarding the in vivo bioactivity of siphonaxanthin. In particular, the results regarding the specific accumulation of siphonaxanthin and its metabolites in WAT have important implications for understanding their anti-obesity effects and regulatory roles in lipid metabolism.


Assuntos
Xantofilas/metabolismo , Xantofilas/farmacocinética , Tecido Adiposo , Tecido Adiposo Branco , Animais , Disponibilidade Biológica , Células CACO-2 , Humanos , Metabolismo dos Lipídeos , Fígado/metabolismo , Camundongos , Distribuição Tecidual , Xantofilas/química
6.
Molecules ; 24(5)2019 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-30866561

RESUMO

Fucoxanthin has interesting anticancer activity, but is insoluble in water, hindering its use as a drug. Microencapsulation is used as a technique for improving drug delivery. This study aimed to formulate fucoxanthin-loaded microspheres (F-LM) for anticancer treatment of H1299 cancer cell lines and optimize particle size (PS) and encapsulation efficiency (EE). Using response surface methodology (RSM), a face centered central composite design (FCCCD) was designed with three factors: Polyvinylalcohol (PVA), poly(d,l-lactic-co-glycolic acid) (PLGA), and fucoxanthin concentration. F-LM was produced using a modified double-emulsion solvent evaporation method. The F-LM were characterized for release profile, release kinetics, and degradation pattern. Optimal F-LM PS and EE of 9.18 µm and 33.09%, respectively, with good surface morphology, were achieved from a 0.5% (w/v) PVA, 6.0% (w/v) PLGA, 200 µg/mL fucoxanthin formulation at a homogenization speed of 20,500 rpm. PVA concentration was the most significant factor (p < 0.05) affecting PS. Meanwhile, EE was significantly affected by interaction between the three factors: PVA, PLGA, and fucoxanthin. In vitro release curve showed fucoxanthin had a high burst release (38.3%) at the first hour, followed by a sustained release stage reaching (79.1%) within 2 months. Release kinetics followed a diffusion pattern predominantly controlled by the Higuchi model. Biodegradability studies based on surface morphology changes on the surface of the F-LM, show that morphology changed within the first hour, and F-LM completely degraded within 2 months. RSM under FCCCD design improved the difference between the lowest and highest responses, with good correlation between observed and predicted values for PS and EE of F-LM.


Assuntos
Antineoplásicos/química , Composição de Medicamentos/métodos , Xantofilas/química , Antineoplásicos/farmacocinética , Linhagem Celular Tumoral , Humanos , Microesferas , Tamanho da Partícula , Solubilidade , Xantofilas/farmacocinética
7.
Food Funct ; 10(3): 1386-1397, 2019 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-30747932

RESUMO

In this research, astaxanthin-rich nanopowder was prepared by nanoencapsulation and freeze-drying techniques with enhanced bioavailability and antioxidant activities. The nanopowder showed a maximum solubility of 230 mg mL-1 with an astaxanthin content as high as 2.9%. Compared with free astaxanthin, the astaxanthin-loaded nanopowder exhibited a more efficient antioxidant effect: an oral dose of 0.9 mg per kg BW significantly reduced the malondialdehyde and protein carbonyl contents, and increased the glutathione content as well as the superoxide dismutase activities in alcohol-induced acute hepatic injured mice, and maintained these oxidative stress indicators at a normal level for a longer period when treated with nanoencapsulated-astaxanthin than free astaxanthin. Simulated gastrointestinal tract studies demonstrated that the nanopowder with pH and DNase I-dependent dissociation properties delivered astaxanthin efficiently to the small intestine. Astaxanthin-rich nanopowder with a dose as high as 2.4 mg per kg BW (equivalent to astaxanthin) showed no chronic toxicity to mice in terms of hematology and pathological histology, indicating its impressive biocompatibility for biomedical applications. Pharmacokinetics and relative bioavailability (207%) of the nanopowder further proved that DNA/chitosan nanocarriers significantly improved the delivery efficiency of astaxanthin. With enhanced bioavailability and antioxidant activities, this novel type of astaxanthin-loaded nanopowder is expected to find broad application in the food and drug industry.


Assuntos
Antioxidantes/farmacologia , Antioxidantes/toxicidade , Nanopartículas/química , Água/química , Animais , Antioxidantes/química , Antioxidantes/farmacocinética , Disponibilidade Biológica , Masculino , Camundongos , Estresse Oxidativo , Distribuição Aleatória , Testes de Toxicidade Crônica , Xantofilas/química , Xantofilas/farmacocinética , Xantofilas/farmacologia , Xantofilas/toxicidade
8.
Nutrients ; 12(1)2019 Dec 27.
Artigo em Inglês | MEDLINE | ID: mdl-31892138

RESUMO

Sea buckthorn oil, derived from the fruits of the shrub, also termed seaberry or sandthorn, is without doubt a strikingly rich source of carotenoids, in particular zeaxanthin and ß-carotene. In the present study, sea buckthorn oil and an oil-in-water emulsion were subjected to a simulated gastro-intestinal in vitro digestion, with the main focus on xanthophyll bioaccessibility. Zeaxanthin mono- and di-esters were the predominant carotenoids in sea buckthorn oil, with zeaxanthin dipalmitate as the major compound (38.0%). A typical fatty acid profile was found, with palmitic (49.4%), palmitoleic (28.0%), and oleic (11.7%) acids as the dominant fatty acids. Taking into account the high amount of carotenoid esters present in sea buckthorn oil, the use of cholesterol esterase was included in the in vitro digestion protocol. Total carotenoid bioaccessibility was higher for the oil-in-water emulsion (22.5%) compared to sea buckthorn oil (18.0%) and even higher upon the addition of cholesterol esterase (28.0% and 21.2%, respectively). In the case of sea buckthorn oil, of all the free carotenoids, zeaxanthin had the highest bioaccessibility (61.5%), followed by lutein (48.9%), making sea buckthorn oil a potential attractive source of bioaccessible xanthophylls.


Assuntos
Hippophae/química , Óleos de Plantas/química , Xantofilas/farmacocinética , Disponibilidade Biológica , Digestão , Emulsões/química , Ácidos Graxos/análise , Frutas/química , Suco Gástrico/enzimologia , Humanos , Intestino Delgado/enzimologia , Luteína/farmacocinética , Esterol Esterase/metabolismo , Xantofilas/análise , Zeaxantinas/farmacocinética , beta Caroteno/farmacocinética
9.
Pharm Dev Technol ; 23(7): 674-681, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-27645209

RESUMO

Astaxanthin oleoresin (AO) has a number of beneficial physiological functions. However, its sensitivity to light, heat, oxygen and gastric fluids has limited its application. In this paper, we describe the preparation of AO enteric microcapsules by coacervation to improve its stability and enteric solubility, and evaluate their efficacy by measuring the drug loading, encapsulation efficiency, optical microscopic appearance, stability, in vitro release and bioavailability. The results obtained showed that the AO enteric microcapsules possessed a high encapsulation efficiency (85.9%), a satisfactory in vitro release profile, and the ability of the microencapsulated AO to resist the effects of light, heat and oxygen was improved by 2.2-fold, 3.1-fold and 2.4-fold, respectively, during storage. In addition, the bioavailability of AO microcapsules was approximately 1.29-fold higher than AO, which is important for pharmaceutical applications and as a functional food.


Assuntos
Alginatos/química , Antioxidantes/administração & dosagem , Portadores de Fármacos/química , Gelatina/química , Extratos Vegetais/administração & dosagem , Animais , Antioxidantes/química , Antioxidantes/farmacocinética , Cápsulas/química , Composição de Medicamentos/métodos , Estabilidade de Medicamentos , Emulsificantes/química , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Masculino , Extratos Vegetais/química , Extratos Vegetais/farmacocinética , Ratos Sprague-Dawley , Xantofilas/administração & dosagem , Xantofilas/química , Xantofilas/farmacocinética
10.
J Sci Food Agric ; 98(8): 3182-3189, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29230828

RESUMO

BACKGROUND: We synthesized astaxanthin succinate diester (ASD), a novel astaxanthin (AST) derivate, with succinic anhydride and free AST. ASD was purified and characterized using silica gel column chromatography and spectrometry, respectively. RESULTS: The ASD final synthesis rate was 82.63%. A stability test revealed a high AST and ASD retention rate at pH 5.0-7.0. ASD showed better stability than did AST under acidic conditions. Both sample ions showed lower retention rates under Fe2+ and Fe3+ states. The ASD metabolic curve showed serum and liver area under the curve from 0 h to time t (AUC0-t ) values of 45.05 ± 4.58 and 120.38 ± 23.66 µg h-1  mL-1 , respectively. The long-term accumulation was significantly higher in the ASD group than in the AST group, which showed higher accumulation in the heart, muscle and spleen than in other tissues in vivo. CONCLUSION: The thermal stability and bioavailability of ASD were higher than that of the non-esterified free AST and common free AST, respectively. Additionally, AST accumulation in different tissues of the ASD group was multifold higher than that of free AST. These results prove that ASD may serve as a better source of AST for human nutrition than does free AST. © 2017 Society of Chemical Industry.


Assuntos
Antioxidantes/síntese química , Antioxidantes/farmacocinética , Ésteres/química , Ácido Succínico/química , Animais , Antioxidantes/química , Disponibilidade Biológica , Ésteres/farmacocinética , Masculino , Camundongos , Camundongos Endogâmicos ICR , Ácido Succínico/farmacocinética , Distribuição Tecidual , Xantofilas/síntese química , Xantofilas/química , Xantofilas/farmacocinética
11.
Food Chem ; 197(Pt A): 325-32, 2016 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-26616956

RESUMO

Plum and cabbage are rich in carotenoids and polyphenols. However, their bioactivity depends on their release and intestinal uptake. Four varieties of Brassicaceae (Duchy, Scots Kale, Kale, Kalorama) and Prunus (Cherry Plum, Plum 620, Ersinger, Italian Plum) were studied; bioaccessibility following in vitro digestion, cellular uptake (Caco-2 vs. co-culture cell model: Caco-2:HT-29-MTX (90:10%) and colonic fermentation were determined for carotenoids/polyphenols; the influence of certain kitchen preparations was likewise studied. Carotenoids were non-significantly influenced by the latter, while for polyphenols, boiling and steaming significantly reduced total phenolics (p<0.05). Carotenoid bioaccessibility did not differ significantly between Prunus vs. Brassicaceae varieties, but xanthophyll was higher than carotene bioaccessibility (p<0.01). Polyphenol bioaccessibility was low (<10%), possibly compromised by the cream containing test meal. Total carotenoid cellular uptake varied between varieties (0.3-4.1%), being higher for carotenes (4.1%) than for xanthophylls (1.6%, p<0.01), and were higher for the co-culture cell model compared to Caco-2 cells (p<0.01). Total carotenoid recovery in the colonic fraction varied from 4% to 25%. Lower bioaccessibility of carotenes thus appeared to be somewhat counterbalanced by higher cellular uptake. The potential positive role of the mucus layer for cellular uptake and the fate of the colonic digesta deserve further attention in the future.


Assuntos
Brassica/química , Carotenoides/farmacocinética , Polifenóis/farmacocinética , Prunus domestica/química , Disponibilidade Biológica , Células CACO-2 , Técnicas de Cocultura , Células HT29 , Humanos , Mucosa Intestinal/metabolismo , Intestinos/citologia , Intestinos/efeitos dos fármacos , Xantofilas/farmacocinética , alfa-Amilases/metabolismo
12.
Mar Drugs ; 12(1): 128-52, 2014 Jan 07.
Artigo em Inglês | MEDLINE | ID: mdl-24402174

RESUMO

There is currently much interest in biological active compounds derived from natural resources, especially compounds that can efficiently act on molecular targets, which are involved in various diseases. Astaxanthin (3,3'-dihydroxy-ß, ß'-carotene-4,4'-dione) is a xanthophyll carotenoid, contained in Haematococcus pluvialis, Chlorella zofingiensis, Chlorococcum, and Phaffia rhodozyma. It accumulates up to 3.8% on the dry weight basis in H. pluvialis. Our recent published data on astaxanthin extraction, analysis, stability studies, and its biological activities results were added to this review paper. Based on our results and current literature, astaxanthin showed potential biological activity in in vitro and in vivo models. These studies emphasize the influence of astaxanthin and its beneficial effects on the metabolism in animals and humans. Bioavailability of astaxanthin in animals was enhanced after feeding Haematococcus biomass as a source of astaxanthin. Astaxanthin, used as a nutritional supplement, antioxidant and anticancer agent, prevents diabetes, cardiovascular diseases, and neurodegenerative disorders, and also stimulates immunization. Astaxanthin products are used for commercial applications in the dosage forms as tablets, capsules, syrups, oils, soft gels, creams, biomass and granulated powders. Astaxanthin patent applications are available in food, feed and nutraceutical applications. The current review provides up-to-date information on astaxanthin sources, extraction, analysis, stability, biological activities, health benefits and special attention paid to its commercial applications.


Assuntos
Animais , Anti-Inflamatórios , Antineoplásicos , Antioxidantes , Disponibilidade Biológica , Produtos Biológicos/química , Biotecnologia , Fármacos Cardiovasculares , Estabilidade de Medicamentos , Humanos , Hipoglicemiantes , Fatores Imunológicos , Biologia Marinha , Xantofilas/efeitos adversos , Xantofilas/biossíntese , Xantofilas/química , Xantofilas/isolamento & purificação , Xantofilas/farmacocinética , Xantofilas/farmacologia
13.
PLoS One ; 8(11): e79280, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24260184

RESUMO

BACKGROUND: Cardiac troponin is the biochemical gold standard to diagnose acute myocardial infarction. Interestingly however, elevated cardiac troponin concentrations are also frequently observed during and after endurance-type exercise. Oxidative stress associated with prolonged exercise has been proposed to contribute to cardiac troponin release. Therefore, the aim of this study was to assess the effect of 4 week astaxanthin supplementation (a potent cartenoid antioxidant) on antioxidant capacity and exercise-induced cardiac troponin release in cyclists. METHODS: Thirty-two well-trained male cyclists (age 25±5, weight 73±7 kg, maximum O2 uptake 60±5 mL·kg(-1)·min(-1), Wmax 5.4±0.5 W·kg(-1); mean ± SD) were repeatedly subjected to a laboratory based standardized exercise protocol before and after 4 weeks of astaxanthin (20 mg/day), or placebo supplementation in a double-blind randomized manner. Blood samples were obtained at baseline, at 60 min of cycling and immediately post-exercise (≈ 120 min). RESULTS: The pre-supplementation cycling trial induced a significant rise of median cardiac troponin T concentrations from 3.2 (IQR 3.0-4.2) to 4.7 ng/L (IQR 3.7-6.7), immediately post-exercise (p<0.001). Four weeks of astaxanthin supplementation significantly increased mean basal plasma astaxanthin concentrations from non-detectable values to 175±86 µg·kg(-1). However, daily astaxanthin supplementation had no effect on exercise-induced cardiac troponin T release (p = 0.24), as measured by the incremental area under the curve. Furthermore, the elevation in basal plasma astaxanthin concentrations was not reflected in changes in antioxidant capacity markers (trolox equivalent antioxidant capacity, uric acid, and malondialdehyde). Markers of inflammation (high-sensitivity C-reactive protein) and exercise-induced skeletal muscle damage (creatine kinase) were equally unaffected by astaxanthin supplementation. CONCLUSION: Despite substantial increases in plasma astaxanthin concentrations, astaxanthin supplementation did not improve antioxidant capacity in well-trained cyclists. Accordingly, exercise-induced cardiac troponin T concentrations were not affected by astaxanthin supplementation. TRIAL REGISTRATION: ClinicalTrials.gov NCT01241877.


Assuntos
Antioxidantes/administração & dosagem , Ciclismo/fisiologia , Suplementos Nutricionais , Troponina T/sangue , Adolescente , Adulto , Antioxidantes/farmacocinética , Método Duplo-Cego , Humanos , Masculino , Xantofilas/administração & dosagem , Xantofilas/farmacocinética
14.
J Agric Food Chem ; 61(16): 3842-51, 2013 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-23473626

RESUMO

Astaxanthin mono- (AXME) and diesters (AXDE) were characterized and examined for anticancer potency with total carotenoids (TC) and astaxanthin (AX) against UV-7,12-dimethylbenz(a)anthracene (DMBA)-induced skin cancer model in rat. At 200 µg/kg bw, AXDE and AXME reduced UV-DMBA-induced tumor incidences up to 96 and 88%, respectively, when compared to AX (66%) and TC (85%). UV-DMBA has been known to generate high levels of free radicals and tyrosinase enzyme, leading to characteristic symptoms of skin pigmentation and tumor initiation. Intriguingly, ~7-fold increase in tyrosinase and 10-fold decrease in antioxidant levels were normalized by AXDE and AXME as opposed to only ~1.4-2.2-fold by AX and TC, respectively. This result together with the appearance of 72 and 58 ng/mL of retinol in the serum of respective AXE-treated (AXDE + AXME) and AX-treated animals suggested that better anticancer potency of AXEs could be due to increased bioavailability.


Assuntos
Antioxidantes/farmacologia , Clorófitas/química , Ésteres/farmacologia , Monofenol Mono-Oxigenase/antagonistas & inibidores , Neoplasias Cutâneas/prevenção & controle , 9,10-Dimetil-1,2-benzantraceno , Animais , Antioxidantes/análise , Disponibilidade Biológica , Carcinógenos , Ratos , Ratos Wistar , Neoplasias Cutâneas/induzido quimicamente , Neoplasias Cutâneas/patologia , Vitamina A/sangue , Xantofilas/sangue , Xantofilas/farmacocinética , Xantofilas/farmacologia
15.
Nutrition ; 29(1): 338-44, 2013 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-23237656

RESUMO

OBJECTIVE: The bioaccessibility of bioactives from pistachios has not been previously evaluated. In the present study we quantified the release of polyphenols, xanthophylls (lutein), and tocopherols from pistachios (raw pistachios, roasted salted pistachios, and muffins made with raw pistachios) during simulated human digestion. METHODS: A dynamic gastric model of digestion that provides a realistic and predictive simulation of the physical and chemical processing and accurately mimics the residence time and the luminal environment within the human stomach was used for the digestion studies. RESULTS: More than 90% of the polyphenols were released in the gastric compartment, with virtually total release in the duodenal phase. No significant differences were observed between raw shelled and roasted salted pistachio. The presence of a food matrix (muffin) decreased the bioaccessibility of protocatechuic acid (78%) and luteolin (36%). Almost 100% bioaccessibility of lutein and tocopherols was found after duodenal digestion, with no difference among the three samples. CONCLUSION: The rapid release of the assayed bioactives in the stomach maximizes the potential for absorption in the duodenum and contributes to the beneficial relation between pistachio consumption and health-related outcomes.


Assuntos
Digestão/fisiologia , Pistacia , Polifenóis/farmacocinética , Tocoferóis/farmacocinética , Xantofilas/farmacocinética , Disponibilidade Biológica , Carotenoides/química , Carotenoides/farmacocinética , Manipulação de Alimentos , Mucosa Gástrica/metabolismo , Humanos , Absorção Intestinal/fisiologia , Luteína/química , Luteína/farmacocinética , Modelos Biológicos , Pistacia/química , Polifenóis/química , Tocoferóis/química , Xantofilas/química
16.
Mar Drugs ; 10(3): 604-616, 2012 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-22611357

RESUMO

The World Health Organization (WHO) estimates that 2.3 billion people will be overweight and 700 million obese in 2015. The reasons for this disastrous trend are attributed to the global tendency toward the reduced magnitude of exercise and physical activity and the increased dietary intake of fats, sugars and calories with reduced amount of vitamins and minerals. To prevent life-style-related diseases, like Metabolic Syndrome (MS), researchers' attention is increasingly focusing on some of the so called "functional foods" which may be useful for their prevention and treatment. One of these functional ingredients is fucoxanthin (FX), a characteristic carotenoid present in edible brown seaweeds, such as Undaria pinnatifida (Wakame), Hijikia fusiformis (Hijiki), Laminaria japonica (Ma-Kombu) and Sargassum fulvellum. The increasing popularity of this molecule is certainly due to its anti-obesity effect, primarily detected by murine studies. These works revealed FX mediated induction of uncoupling protein-1 (UCP-1) in abdominal white adipose tissue (WAT) mitochondria, leading to the oxidation of fatty acids and heat production in WAT. Beyond this important role, in recent studies FX has shown a great antioxidant activity, anti-cancer, anti-diabetic and anti-photoaging properties. The aim of this review is to highlight the main effects of FX on human health.


Assuntos
Fármacos Antiobesidade/farmacologia , Phaeophyceae/química , Alga Marinha/química , Xantofilas/farmacologia , Animais , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Fármacos Cardiovasculares/farmacologia , Humanos , Hipoglicemiantes/farmacologia , Camundongos , Envelhecimento da Pele/efeitos dos fármacos , Xantofilas/biossíntese , Xantofilas/isolamento & purificação , Xantofilas/farmacocinética , Xantofilas/toxicidade
17.
Anticancer Res ; 32(2): 507-17, 2012 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-22287739

RESUMO

BACKGROUND: The molecular basis of interaction of selected carotenoids and xanthophylls with ascorbic acid on cancer cells was studied to determine their anticancer effects. MATERIALS AND METHODS: Drug accumulation was measured in a human ABCB1 gene-transfected mouse lymphoma cell line and in a human lung cancer cell line by flow cytometry; furthermore, their anticancer effects were determined in mice in vivo. RESULTS: Several carotenoids inhibited the multidrug resistance of cancer cells. Ascorbic acid improved the effect of certain xanthophylls, but the effect of capsanthin was not modified. Capsanthin had weak (12%) but capsorubin (85%) had a remarkable antiproliferative effect on A549 lung cancer cells. Capsorubin reduced immediate-early tumor antigen expression, while capsanthin was not effective. Capsorubin accumulates selectively in the nuclei of cancer cells. CONCLUSION: The Authors suggest a special complex formation between membrane-bound capsorubin and ascorbic acid, which can be exploited in experimental chemotherapy.


Assuntos
Ácido Ascórbico/farmacologia , Neoplasias/tratamento farmacológico , Neoplasias/metabolismo , Xantofilas/farmacologia , Transportador 1 de Cassete de Ligação de ATP , Transportadores de Cassetes de Ligação de ATP/biossíntese , Transportadores de Cassetes de Ligação de ATP/genética , Transportadores de Cassetes de Ligação de ATP/metabolismo , Animais , Ácido Ascórbico/farmacocinética , Linhagem Celular Tumoral , Resistência a Múltiplos Medicamentos , Resistencia a Medicamentos Antineoplásicos , Sinergismo Farmacológico , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Neoplasias Pulmonares/genética , Neoplasias Pulmonares/metabolismo , Linfoma de Células T/tratamento farmacológico , Linfoma de Células T/genética , Linfoma de Células T/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos CBA , Neoplasias Pancreáticas/tratamento farmacológico , Neoplasias Pancreáticas/metabolismo , Transfecção , Xantofilas/farmacocinética , Ensaios Antitumorais Modelo de Xenoenxerto
18.
Mar Drugs ; 9(10): 1806-1828, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-22072997

RESUMO

The marine carotenoid fucoxanthin can be found in marine brown seaweeds, the macroalgae, and diatoms, the microalgae, and has remarkable biological properties. Numerous studies have shown that fucoxanthin has considerable potential and promising applications in human health. In this article, we review the current available scientific literature regarding the metabolism, safety, and bioactivities of fucoxanthin, including its antioxidant, anti-inflammatory, anticancer, anti-obese, antidiabetic, antiangiogenic and antimalarial activities, and its protective effects on the liver, blood vessels of the brain, bones, skin, and eyes. Although some studies have shown the bioavailability of fucoxanthin in brown seaweeds to be low in humans, many studies have suggested that a dietary combination of fucoxanthin and edible oil or lipid could increase the absorption rate of fucoxanthin, and thus it might be a promising marine drug.


Assuntos
Diatomáceas/química , Alga Marinha/química , Xantofilas/uso terapêutico , Anti-Inflamatórios/farmacocinética , Anti-Inflamatórios/uso terapêutico , Fármacos Antiobesidade/farmacocinética , Fármacos Antiobesidade/uso terapêutico , Antineoplásicos/farmacocinética , Antineoplásicos/uso terapêutico , Antioxidantes/farmacocinética , Antioxidantes/uso terapêutico , Disponibilidade Biológica , Fármacos Dermatológicos/farmacocinética , Fármacos Dermatológicos/uso terapêutico , Humanos , Hipoglicemiantes/farmacocinética , Hipoglicemiantes/uso terapêutico , Fígado/efeitos dos fármacos , Xantofilas/química , Xantofilas/farmacocinética
19.
Adv Food Nutr Res ; 64: 111-28, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-22054942

RESUMO

The importance of marine algae as sources of functional ingredients has been well recognized due to their valuable health beneficial effects. Therefore, isolation and investigation of novel bioactive ingredients with biological activities from marine algae have attracted great attention. Among functional ingredients identified from marine algae, fucoxanthin has received particular interest. Fucoxanthin has been attributed with extraordinary potential for protecting the organism against a wide range of diseases and has considerable potential and promising applications in human health. Fucoxanthin has been reported to exhibit various beneficial biological activities such as antioxidant, anticancer, anti-inflammatory, antiobesity, and neuroprotective activities. In this chapter, the currently available scientific literatures regarding the most significant activities of fucoxanthin are summarized.


Assuntos
Phaeophyceae/química , Xantofilas/farmacologia , Xantofilas/farmacocinética , Disponibilidade Biológica , Humanos , Estrutura Molecular , Xantofilas/química
20.
Mar Drugs ; 9(6): 1024-1037, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-21747746

RESUMO

Dietary carotenoids, especially xanthophylls, have attracted significant attention because of their characteristic biological activities, including anti-allergic, anti-cancer, and anti-obese actions. Although no less than forty carotenoids are ingested under usual dietary habits, only six carotenoids and their metabolites have been found in human tissues, suggesting selectivity in the intestinal absorption of carotenoids. Recently, facilitated diffusion in addition to simple diffusion has been reported to mediate the intestinal absorption of carotenoids in mammals. The selective absorption of carotenoids may be caused by uptake to the intestinal epithelia by the facilitated diffusion and an unknown excretion to intestinal lumen. It is well known that ß-carotene can be metabolized to vitamin A after intestinal absorption of carotenoids, but little is known about the metabolic transformation of non provitamin A xanthophylls. The enzymatic oxidation of the secondary hydroxyl group leading to keto-carotenoids would occur as a common pathway of xanthophyll metabolism in mammals. This paper reviews the absorption and metabolism of xanthophylls by introducing recent advances in this field.


Assuntos
Xantofilas/metabolismo , Xantofilas/farmacocinética , Animais , Dieta , Difusão Facilitada , Humanos , Absorção Intestinal , Mucosa Intestinal/metabolismo
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