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1.
Int J Mol Sci ; 22(22)2021 Nov 12.
Article in English | MEDLINE | ID: mdl-34830148

ABSTRACT

Phytosterols constitute a class of natural products that are an important component of diet and have vast applications in foods, cosmetics, and herbal medicines. With many and diverse isolated structures in nature, they exhibit a broad range of biological and pharmacological activities. Among over 200 types of phytosterols, stigmasterol and ß-sitosterol were ubiquitous in many plant species, exhibiting important aspects of activities related to neurodegenerative diseases. Hence, this mini-review presented an overview of the reported studies on selected phytosterols related to neurodegenerative diseases. It covered the major phytosterols based on biosynthetic considerations, including other phytosterols with significant in vitro and in vivo biological activities.


Subject(s)
Brain/metabolism , Neurodegenerative Diseases/prevention & control , Phytosterols/therapeutic use , Phytotherapy/methods , Plants, Medicinal/chemistry , Brain/pathology , Humans , Molecular Structure , Neurodegenerative Diseases/metabolism , Neuroprotective Agents/chemistry , Neuroprotective Agents/pharmacokinetics , Neuroprotective Agents/therapeutic use , Phytosterols/chemistry , Phytosterols/pharmacokinetics , Sitosterols/chemistry , Sitosterols/pharmacokinetics , Sitosterols/therapeutic use , Stigmasterol/chemistry , Stigmasterol/pharmacokinetics , Stigmasterol/therapeutic use
2.
Phytomedicine ; 69: 153201, 2020 Apr.
Article in English | MEDLINE | ID: mdl-32276177

ABSTRACT

BACKGROUND: Marine algae are rich in some unique biologically active secondary metabolites having diverse pharmacological benefits. Of these, sterols comprise a group of functional lipid compounds that have attracted much attention to natural product scientists. PURPOSE: This review was aimed to update information on the health effects of algae-derived phytosterols and their molecular interactions in various aspects of human health and diseases and to address some future perspectives that may open up a new dimension of pharmacological potentials of algal sterols. METHODS: A literature-based search was carried out to retrieve published research information on the potential health effects of algal phytosterols with their pharmacological mechanisms from accessible online databases, such as Pubmed, Google Scholar, Web of Science, and Scopus, using the key search terms of 'marine algae sterol' and 'health potentials such as antioxidant or anti-inflammatory or anti-Alzheimer's or anti-obesity or cholesterol homeostasis or hepatoprotective, antiproliferative, etc.' RESULTS: Phytosterols of marine algae, particularly fucosterol, have been investigated for a plethora of health benefits, including anti-diabetes, anti-obesity, anti-Alzheimer's, antiaging, anticancer, and hepatoprotection, among many others, which are attributed to their antioxidant, anti-inflammatory, immunomodulatory and cholesterol-lowering properties, indicating their potentiality as therapeutic leads. These sterols interact with enzymes and various other proteins that are actively participating in different cellular pathways, including antioxidant defense system, apoptosis and cell survival, metabolism, and homeostasis. CONCLUSION: In this review, we briefly overview the chemistry, pharmacokinetics, and distribution of algal sterols, and provide critical insights into their potential health effects and the underlying pharmacological mechanisms, beyond the well-known cholesterol-lowering paradigm.


Subject(s)
Phytosterols/chemistry , Phytosterols/pharmacology , Seaweed/chemistry , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/pharmacology , Antioxidants/chemistry , Antioxidants/pharmacology , Aquatic Organisms , Cholesterol/metabolism , Humans , Phaeophyceae/chemistry , Phytosterols/analysis , Phytosterols/pharmacokinetics , Rhodophyta/chemistry , Stigmasterol/analogs & derivatives , Stigmasterol/pharmacology , Tissue Distribution
3.
Xenobiotica ; 50(6): 677-684, 2020 Jun.
Article in English | MEDLINE | ID: mdl-30729838

ABSTRACT

1. The aim of this study was to develop a selective, rapid, accurate and sensitive ultrahigh performance liquid chromatography tandem mass spectrometry (UHPLC-MS/MS) method for pharmacokinetic (PK) studies of phytoecdysones and triterpenoid saponins after oral administration of five monomers, crude, wine-processed and salt-processed Radix Achyranthis bidentatae (RAB).2. A Thermo Hypersil GOLD C18 column (100 mm × 2.1 mm, 1.9 µm) coupled with a mobile phase of (A) acetonitrile and (B) water (both containing 0.3% acetic acid) was used for sample separation. The mass analysis was performed in a triple quadruple mass spectrometer using selected reaction monitoring (SRM) with negative scan mode.3. The results showed that this method exhibited desirable sensitivity, precision, stability and repeatability. The extraction recoveries of the compounds ranged from 94.2 to 99.8% and the matrix effects ranged from 93.3 to 100.5%. Comparing the Cmax and AUC of five analytes in those groups showed this tendency: salt-processed RAB > wine-processed RAB > crude RAB > monomer group. The results confirmed the feasibility of TCM theory to enhance the efficacy of processed RAB.


Subject(s)
Ecdysone/pharmacokinetics , Phytosterols/pharmacokinetics , Saponins/pharmacokinetics , Chromatography, High Pressure Liquid , Chromatography, Liquid , Drugs, Chinese Herbal/pharmacokinetics , Spectrometry, Mass, Electrospray Ionization , Tandem Mass Spectrometry , Triterpenes
4.
J Bioenerg Biomembr ; 51(2): 131-136, 2019 04.
Article in English | MEDLINE | ID: mdl-30739226

ABSTRACT

Phytosterol metabolism is unknown in the hypercholesterolemia of genetic origin. We investigated the metabolism of phytosterols in a cholesterol-free, phytosterol-containing standard diet in hypercholesterolemic mice knockouts for low density lipoprotein receptor (LDLR) and apolipoprotein E (apoE) mice compared to wild-type mice (controls). Phytosterols were measured in mice tissues by GCMS. ApoE-KO mice absorbed less phytosterols than LDLR-KO and the latter absorbed less phytosterols than control mice, because the intestinal campesterol content was low in both KO mice, and sitosterol was low in the intestine in apoE-KO mice as compared to LDLR-KO mice. Although the diet contained nine times more sitosterol than campesterol, the concentration of sitosterol was lower than that of campesterol in plasma in LDLR-KO, and in the liver in controls and in LDLR-KO, but only in apoE-KO. On the other hand, in the intestine sitosterol was higher than campesterol in controls, and in LDLR-KO but with a tendency only in apoE-KO. Because of the high dietary supply of sitosterol, sitosterol was better taken up by the intestine than campesterol, but the amount of sitosterol was lower than that of campesterol in the liver, while in the whole body the amounts of these phytosterols do not differ from each other. Therefore, via intestinal lymph less sitosterol than campesterol was transferred to the body. However, as compared to controls, in apoE-KO mice, but not in LDLR-KO mice, the increase in campesterol and sitosterol in plasma and in the whole body indicating that apoE-KO mice have a marked defect in the elimination of both phytosterols from the body.


Subject(s)
Animal Feed , Cholesterol/analogs & derivatives , Liver/metabolism , Phytosterols , Receptors, LDL/deficiency , Sitosterols , Animals , Cholesterol/pharmacokinetics , Cholesterol/pharmacology , Liver/pathology , Mice , Mice, Knockout, ApoE , Phytosterols/pharmacokinetics , Phytosterols/pharmacology , Receptors, LDL/metabolism , Sitosterols/pharmacokinetics , Sitosterols/pharmacology , Species Specificity
5.
Drug Dev Res ; 79(7): 339-351, 2018 11.
Article in English | MEDLINE | ID: mdl-30284738

ABSTRACT

Preclinical Research & Development Withanolide A (WA), a steroidal lactone is a major bioactive constituent of Withania somnifera (L.) with remarkable neuropharmacological activity. In this study, we investigated the permeability, plasma protein binding (PPB), blood partitioning, intravenous (i.v.), and oral pharmacokinetics as well as i.v. tissue distribution (TD) of pure WA in a rat model. The PPB, RBCs partitioning, and permeability of WA were determined by Ultra Performance Liquid Chromatography (UPLC) method. However, the pharmacokinetics and TD of WA were evaluated by validated and sensitive liquid chromatography coupled mass spectrometry (LC-ESI-MS/MS) method. The PPB and permeability of WA were determined by equilibrium dialysis and parallel artificial membrane permeability assay method, respectively. The results demonstrated that WA has high PPB and passive permeability. Furthermore, WA was found to have fast equilibration between RBCs and plasma. Following i.v. (2 mg/kg) and per-oral (25 mg/kg) administration of WA, the max concentration (Cmax ) in plasma was found as 85.53 ± 6.54 and 48.04 ±5.78 ng/mL, respectively. The TD study results indicated that WA has a rapid and wide TD. The maximum concentration in various tissues was found in following order: Clung > Cliver > Ckidney ≈ Cspleen > Cheart > Cbrain . The preclinical in vitro, as well as pharmacokinetics and TD results, are anticipated to support the future preclinical and clinical application of WA.


Subject(s)
Blood Proteins/pharmacokinetics , Neuroprotective Agents/pharmacokinetics , Phytosterols/pharmacokinetics , Withania , Withanolides/pharmacokinetics , Animals , Blood Proteins/analysis , Lactones/analysis , Lactones/blood , Lactones/pharmacokinetics , Male , Neuroprotective Agents/analysis , Neuroprotective Agents/blood , Permeability/drug effects , Phytosterols/analysis , Phytosterols/blood , Protein Binding/physiology , Rats , Rats, Sprague-Dawley , Tandem Mass Spectrometry/methods , Tissue Distribution/drug effects , Tissue Distribution/physiology , Withanolides/analysis , Withanolides/blood
6.
Br J Nutr ; 119(6): 599-609, 2018 03.
Article in English | MEDLINE | ID: mdl-29397797

ABSTRACT

The aim of the study was to investigate how the dietary sterol composition, including cholesterol, phytosterol:cholesterol ratio and phytosterols, affect the absorption, biliary excretion, retention, tissue storage and distribution of cholesterol and individual phytosterols in Atlantic salmon (Salmo salar L.). A feeding trial was conducted at two different temperatures (6 and 12°C), using nine different diets with varying contents of phytosterols, cholesterol and phytosterol:cholesterol ratio. Cholesterol retention values were clearly dependent on dietary cholesterol, and showed that fish fed cholesterol levels <1000 mg/kg feed produced considerable quantities of cholesterol de novo. Despite this production, cholesterol content increased with increasing dietary cholesterol in liver, plasma, bile, muscle, adipose tissue and whole fish at 12°C, and in plasma, bile and whole fish at 6°C. The tissue sterol composition generally depended on the dietary cholesterol content and on the dietary phytosterol:cholesterol ratio, but not on the dietary phytosterol content in itself. Campesterol and brassicasterol appeared to be the phytosterols with the highest intestinal absorption in Atlantic salmon. There was a high biliary excretion of campesterol, but not of brassicasterol, which accumulated in tissues and particularly in adipose tissue, with 2-fold-higher retention at 12°C compared with 6°C. Campesterol had the second highest retention of the phytosterols in the fish, but with no difference between the two temperatures. Other phytosterols had very low retention. Although brassicasterol retention decreased with increasing dietary phytosterols, campesterol retention decreased with increasing dietary cholesterol, indicating differences in the uptake mechanisms for these two sterols.


Subject(s)
Diet/veterinary , Salmo salar , Sterols/analysis , Animals , Cholestadienols/administration & dosage , Cholestadienols/pharmacokinetics , Cholesterol/administration & dosage , Cholesterol/analogs & derivatives , Cholesterol/pharmacokinetics , Intestinal Absorption , Liver/metabolism , Phytosterols/administration & dosage , Phytosterols/pharmacokinetics
7.
Clin Nutr ; 37(1): 262-269, 2018 02.
Article in English | MEDLINE | ID: mdl-28063717

ABSTRACT

BACKGROUND: Phytosterols in vegetable oil (VO)-based lipid emulsions (LE) likely contribute to parenteral nutrition-associated cholestasis (PNAC) in preterm infants. No characterization of plasma phytosterol half-lives has been done in very low birth weight (VLBW) preterm infants receiving parenteral nutrition (PN) with LE. METHODS: In a prospective cohort study, 45 VLBW preterm infants who received PN underwent serial blood sample measurements of sitosterol (SITO), campesterol (CAMP), and stigmasterol (STIGM). Plasma phytosterol half-lives were calculated from the phytosterol concentrations-decay curves by using a single-compartment model. RESULTS: After the stop of the intravenous LE, study infants had significantly lower plasma total CAMP, STIGM and SITO concentrations. The decay of plasma phytosterol concentrations was monoexponential. Half-life of plasma total CAMP, STIGM and SITO was 13.5 ± 6.9, 10.3 ± 4.5 and 10.3 ± 4.0 days, respectively. Plasma phytosterol half-lives did not correlate with gestational age, birth weight, cumulative phytosterol intakes and plasma conjugated bilirubin. CONCLUSION: VLBW preterm infants on PN with LE had rather long plasma phytosterol half-lives similar to hypercholesterolemic adults and phytosterolemic homozygotes patients. We speculate that the accumulation of phytosterols could contribute to their vulnerability to PNAC. CLINICAL TRIAL REGISTRY: The Ethics Committee of Marche-Italy (DG/469); www.clinicaltrials.gov (identification number NCT02758834).


Subject(s)
Fat Emulsions, Intravenous , Infant, Very Low Birth Weight , Parenteral Nutrition, Total/methods , Phytosterols , Plant Oils , Birth Weight , Cohort Studies , Fat Emulsions, Intravenous/administration & dosage , Fat Emulsions, Intravenous/pharmacokinetics , Fat Emulsions, Intravenous/therapeutic use , Female , Gestational Age , Humans , Infant, Newborn , Infant, Very Low Birth Weight/blood , Infant, Very Low Birth Weight/metabolism , Male , Phytosterols/blood , Phytosterols/metabolism , Phytosterols/pharmacokinetics , Plant Oils/administration & dosage , Plant Oils/pharmacokinetics , Plant Oils/therapeutic use , Prospective Studies
8.
Biomed Pharmacother ; 88: 786-794, 2017 Apr.
Article in English | MEDLINE | ID: mdl-28157655

ABSTRACT

Phytosterols are naturally occurring compounds in plants, structurally similar to cholesterol. The human diet is quite abundant in sitosterol and campesterol. Phytosterols are known to have various bioactive properties including reducing intestinal cholesterol absorption which alleviates blood LDL-cholesterol and cardiovascular problems. It is indicated that phytosterol rich diets may reduce cancer risk by 20%. Phytosterols may also affect host systems, enabling antitumor responses by improving immune response recognition of cancer, affecting the hormone dependent endocrine tumor growth, and by sterol biosynthesis modulation. Moreover, phytosterols have also exhibited properties that directly inhibit tumor growth, including reduced cell cycle progression, apoptosis induction, and tumor metastasis inhibition. The objective of this review is to summarize the current knowledge on occurrences, chemistry, pharmacokinetics and potential anticancer properties of phytosterols in vitro and in vivo. In conclusion, anticancer effects of phytosterols have strongly been suggested and support their dietary inclusion to prevent and treat cancers.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Neoplasms/drug therapy , Neoplasms/prevention & control , Phytosterols/pharmacology , Animals , Antineoplastic Agents, Phytogenic/pharmacokinetics , Diet , Humans , Neoplasms/epidemiology , Phytosterols/chemistry , Phytosterols/pharmacokinetics
9.
J Diet Suppl ; 14(4): 433-445, 2017 Jul 04.
Article in English | MEDLINE | ID: mdl-28121472

ABSTRACT

Creatine monohydrate represents one of the largest sports supplement markets. Enhancing creatine (CRE) stability in aqueous solutions, such as with microencapsulation, represents innovation potential. Ten physically active male volunteers were randomly assigned in a double-blind design to either placebo (PLA) (3-g maltodextrin; n = 5) or microencapsulated CRE (3-g creatine monohydrate; n = 5) conditions. Experimental conditions involved ingestion of the samples in a 70-mL ready-to-drink format. CRE was delivered in a novel microencapsulation matrix material consisting entirely of hydrolyzed milk protein. Three hours after ingestion, plasma creatine concentrations were unchanged during PLA, and averaged ∼45 µM. During CRE, plasma creatine concentration peaked after 30 min at 101.6 ± 14.9 µM (p < 0.05), representing a 2.3-fold increase over PLA. Thereafter, plasma creatine concentration gradually trended downwards but remained significantly elevated (∼50% above resting levels) 3 hr after ingestion. These results demonstrate that the microencapsulated form of creatine monohydrate reported herein remains bioavailable when delivered in aqueous conditions, and has potential utility in ready-to-drink formulations for creatine supplementation.


Subject(s)
Creatine/pharmacokinetics , Diosgenin/pharmacokinetics , Phytosterols/pharmacokinetics , Adult , Biological Availability , Creatine/administration & dosage , Creatine/blood , Diosgenin/administration & dosage , Double-Blind Method , Drug Compounding , Drug Stability , Eating , Healthy Volunteers , Humans , Male , Milk Proteins , Phytosterols/administration & dosage , Protein Hydrolysates , Random Allocation , Solutions
10.
Clín. investig. arterioscler. (Ed. impr.) ; 28(6): 283-294, nov.-dic. 2016. ilus, tab
Article in Spanish | IBECS | ID: ibc-158499

ABSTRACT

En este trabajo se describe qué son los esteroles vegetales, la estructura química de los mismos para entender su mecanismo de acción hipocolesterolemiante, así como sus indicaciones y sus contraindicaciones en la práctica clínica


This paper describes what are plant sterols, the chemical structure to understand their mechanism of cholesterol-lowering action, and indications and contraindications in clinical practice


Subject(s)
Humans , Phytosterols/pharmacokinetics , Anticholesteremic Agents/pharmacokinetics , Cardiovascular Diseases/prevention & control , Hypercholesterolemia/drug therapy , Risk Factors , Practice Patterns, Physicians'
11.
J Sep Sci ; 39(21): 4060-4070, 2016 Nov.
Article in English | MEDLINE | ID: mdl-27591043

ABSTRACT

A liquid chromatography with atmospheric pressure chemical ionization tandem mass spectrometry method was developed and validated to investigate the pharmacokinetic properties of ß-sitosterol, campesterol, and stigmasterol in rat plasma. Cholesterol-d6 was used as an internal standard. To avoid interference of the three phytosterols in rat plasma and minimize matrix effects, a small volume (10 µL) of 4% bovine serum albumin was used as a surrogate matrix for making calibrators and quality control samples. Rat plasma (10 µL) samples were extracted by liquid-liquid extraction with methyl tert-butyl ether and separated on a Kinetex C18 column. The detection was performed on a triple quadrupole tandem mass spectrometer in selected reaction monitoring mode using positive atmospheric pressure chemical ionization. This assay was linear over concentration ranges of 250-5000 ng/mL (ß-sitosterol), 250-5000 ng/mL (campesterol), and 50-2000 ng/mL (stigmasterol). Additionally, a second set of quality controls made in rat plasma was also evaluated against calibration curves made using the surrogate matrix. All the validation data, including the specificity, precision, accuracy, recovery, matrix effect, stability, and incurred sample reanalysis conformed to the acceptance requirements. Our method was successfully applied to study the pharmacokinetics of three phytosterols in rats.


Subject(s)
Cholesterol/analogs & derivatives , Phytosterols/blood , Sitosterols/blood , Stigmasterol/blood , Zea mays/chemistry , Animals , Cholesterol/blood , Cholesterol/pharmacokinetics , Chromatography, High Pressure Liquid , Phytosterols/pharmacokinetics , Rats , Reproducibility of Results , Sitosterols/pharmacokinetics , Stigmasterol/pharmacokinetics , Tandem Mass Spectrometry
12.
Nutr. hosp ; 33(3): 685-691, mayo-jun. 2016. tab, graf
Article in Spanish | IBECS | ID: ibc-154489

ABSTRACT

Introducción: la hipercolesterolemia es uno de los principales factores de riesgo en la enfermedad cardiovascular. Los esteroles vegetales se han postulado como agentes reguladores y beneficiosos para el control de esta. Objetivo: analizar el efecto de los esteroles vegetales añadidos en una leche en la reducción del colesterol plasmático en adultos jóvenes. Métodos: ensayo clínico, controlado, aleatorizado, doble ciego y cruzado. Los esteroles (2,24 g diarios) fueron administrados en dos tomas de 350 ml de una leche comercial desnatada, durante dos periodos de 3 semanas, separados por una ‘fase de lavado’ de 2 semanas, en el grupo experimental. Al grupo control se le administró la misma cantidad de leche desnatada, sin esteroles. Tanto al inicio como al final de cada periodo de intervención se extrajeron muestras sanguíneas. Se analizaron la composición corporal, hábitos de salud y los siguientes marcadores sanguíneos: perfil lipídico, hematológico, inflamación, etc. Resultados: se incluyeron 54 personas en el estudio con una edad media de 38,8 ± 7,3 años. La diferencia porcentual entre los marcadores basales y finales para el colesterol total, colesterol-LDL, colesterol-HDL, triglicéridos y colesterol no-HDL fueron del 9,73%, 12,5%, 1,9%, 3,15% y 13,2%, respectivamente. Se obtuvieron diferencias estadísticamente significativas entre el grupo experimental y el grupo control, para todos los marcadores analizados excepto para los triglicéridos. Conclusión: los esteroles vegetales suministrados en un alimento de consumo habitual, como la leche, pueden ser una estrategia terapéutica no farmacológica para el control de la hipercolesterolemia de alto interés sanitario (AU)


Introduction: Hypercholesterolemia is one of the most relevant risk factors in cardiovascular disease, and plant sterols have been postulated as beneficial regulator agents for the control of the disease. Objective: Analyze the effect of added plant sterols in milk in reducing plasma cholesterol in young adults. Methods: A randomized, clinical controlled trial, double-blind crossover study. Sterols (2.24 g per day) were administrated in two doses of 350 ml of commercial skimmed milk, during two phases of three weeks respectively separated by a washout period of 2 weeks, in the experimental group. The same amount of skimmed milk was administrated to the control group, but with no sterols. At the beginning and end of each phase blood draws were performed. Anthropometric data and health habits were analyzed and the following blood laboratory markers: lipid profile, hematology, inflammation, etc. were collected. Results: Fifty four people were included in the study with an average age of 38.8 ± 7.3 years. Differences between baseline and final scores percentage were 9.73 %, 12.5 %, 1.9 %, 3.15 % y 13.2 % for total cholesterol, LDL-cholesterol, HDL-cholesterol, triglycerides and No HDL-cholesterol, respectively. Statistically significant differences were found between the experimental group and the control group for all biomarkers analyzed except for triglycerides. Conclusion: Plant sterols supplied in commonly consumed food, such as milk, may be a non- pharmacological therapeutic strategy of hypercholesterolemia with high health interest (AU)


Subject(s)
Humans , Male , Female , Hypercholesterolemia/drug therapy , Phytosterols/pharmacokinetics , Risk Factors , Cardiovascular Diseases/prevention & control , Lipoproteins, LDL , Dietary Supplements , Biomarkers/analysis
13.
Biochem Biophys Res Commun ; 476(2): 82-9, 2016 07 22.
Article in English | MEDLINE | ID: mdl-27179780

ABSTRACT

UNLABELLED: The effect of oryzanol (well known hypolipidemic component in rice bran oil) and its chemical constituents- ferulic acid (FA) and phytosterols on hypolipidemia were investigated. METHODS AND RESULTS: Docking (in silico) studies showed that FA had a better binding ability with lipase while sterols bound well with HMG-CoA reductase. Further in vivo studies of feeding high fat (30%) to rats increased body weights, serum TC, TG, non-HDL-C and reduced HDL-C were observed, compared to normal diet fed group (ND). ORZ treated groups alleviated the lipid profile. Furthermore, increased organ weights, higher intestinal lipase activity, and liver lipid peroxidation was observed in the high-fat group (HF). These effects were ameliorated in oryzanol concentrate fed groups (ORZ). Higher fecal fat was found in ORZ groups, analysis of fecal matter by mass spectroscopy revealed the presence of FA. In vitro, a bile acid binding study supported the strong affinity of sterol towards bile acids. In conclusion, oryzanol in the intestine is cleaved into FA and sterol by intestinal lipase enzymes both lipase and HMG-CoA reductase activities were inhibited, respectively. These hydrolysates eliminated the bile acids, thus lowering lipid profiles.


Subject(s)
Coumaric Acids/pharmacology , Hydroxymethylglutaryl CoA Reductases/metabolism , Hydroxymethylglutaryl-CoA Reductase Inhibitors/pharmacology , Hypolipidemic Agents/pharmacology , Lipase/metabolism , Phenylpropionates/pharmacology , Phytosterols/pharmacology , Animals , Bile Acids and Salts/metabolism , Body Weight/drug effects , Coumaric Acids/chemistry , Drinking/drug effects , Eating/drug effects , Humans , Hydroxymethylglutaryl-CoA Reductase Inhibitors/chemistry , Hydroxymethylglutaryl-CoA Reductase Inhibitors/pharmacokinetics , Hypolipidemic Agents/chemistry , Hypolipidemic Agents/pharmacokinetics , Lipase/antagonists & inhibitors , Male , Oryza/chemistry , Phenylpropionates/chemistry , Phenylpropionates/pharmacokinetics , Phytosterols/chemistry , Phytosterols/pharmacokinetics , Protein Binding , Rats, Wistar
14.
Mol Nutr Food Res ; 60(4): 749-59, 2016 Apr.
Article in English | MEDLINE | ID: mdl-26773424

ABSTRACT

SCOPE: The ability of different plant sterols/stanols (PS) mixtures, which differed in the degree of B-ring saturation and aliphatic side chain structure and saturation, to reduce cholesterol (CH) micellarization was explored. METHODS AND RESULTS: Experiments were performed using an in vitro digestion model, synthetic mixed micelles, and pure porcine pancreatic lipases. Sterols were measured by GC-FID. The ability of PS to reduce CH micellarization was dependent on the form of PS and on the type of delivery matrix (low-fat yogurt or olive oil). Long-chain PS esters delivered in the yogurt matrix, and medium chain PS esters delivered in olive oil provided the greatest reduction in CH micellarization. In yogurt, the ability to impair CH micellarization was inversely related (rho = -0.41, p < 0.0005) to PS melting point. In olive oil, the more hydrophobic PS mixtures, i.e. those rich in long-chain PS esters, had the lower ability to impair CH micellarization. CONCLUSIONS: Different forms of PS have a different ability to impair CH micellarization. This ability depends on the transfer efficiency of PS from the food matrix to the micelle, which in turn depends on the melting point and the hydrophobicity of PS and on the delivery food matrix.


Subject(s)
Cholesterol/chemistry , Food , Micelles , Phytosterols/chemistry , Animals , Digestion/physiology , Hydrolysis , Lipase/chemistry , Lipase/metabolism , Pancreas/enzymology , Phytosterols/pharmacokinetics , Swine , Yogurt
15.
Food Funct ; 7(1): 110-7, 2016 Jan.
Article in English | MEDLINE | ID: mdl-26447847

ABSTRACT

The bioaccessibility (BA) of total and individual plant sterols (PS) of four commercial PS-enriched fermented milk beverages (designated as A to D) was evaluated using in vitro gastrointestinal digestion including the formation of mixed micelles. The fat content of the samples ranged from 1.1 to 2.2% (w/w), and PS enrichment was between 1.5 and 2.9% (w/w). ß-Sitosterol, contained in all samples, was higher in samples A and B (around 80% of total PS). The campesterol content was C (22%) > A (7%) > B (5%). Sitostanol was the most abundant in sample D (85%). Stigmasterol was only present in sample C (33%). The greatest BA percentage for total PS corresponded to samples A and B (16-17%), followed by sample D (11%) and sample C (9%). The total BA was not related to the protein, lipid or PS content of the beverages, whereas samples with higher carbohydrates and fiber contents showed lower BA. The BA of the individual PS differed according to the sample considered, and was not related to the PS profile of the sample, thus indicating strong dependency upon the matrix (PS ingredient and other components). Although in vivo studies should be carried out to better assess the functionality of PS in functional foods such as enriched fermented milk beverages, our in vitro study is a useful preliminary contribution to evaluation of the efficacy of these products.


Subject(s)
Cultured Milk Products/chemistry , Food, Fortified/analysis , Phytosterols/administration & dosage , Phytosterols/pharmacokinetics , Biological Availability , Cholesterol/administration & dosage , Cholesterol/analogs & derivatives , Cholesterol/analysis , Dietary Carbohydrates/analysis , Dietary Fats/analysis , Dietary Fiber/analysis , Digestion , Functional Food , Gastrointestinal Tract/metabolism , Micelles , Models, Biological , Phytosterols/analysis , Sitosterols/administration & dosage , Sitosterols/analysis , Stigmasterol/administration & dosage , Stigmasterol/analysis
16.
Nutr. hosp ; 32(4): 1462-1467, oct. 2015.
Article in English | IBECS | ID: ibc-143637

ABSTRACT

The effect of diet on cardiovascular disease prevention has been widely studied for many years. Numerous studies have confirmed that diets rich in fruits and vegetables (Mediterranean diet) are beneficial to the cardiovascular system and various bioactive food components have preventive effect on chronic diseases such as cardiovascular disease. In this paper we review the effect of bioactive substances included in the group of flavonoids (catechins and proanthocyanidins, anthocyanins and isoflavones), stilbenes such as resveratrol, bioactive peptides, plant sterols and polyunsaturated fatty acids omega-3 on the cardiovascular system (AU)


El efecto de la dieta sobre la prevención de las enfermedades cardiovasculares ha sido ampliamente estudiado durante muchos años. Numerosos estudios han corroborado que las dietas ricas en frutas y hortalizas (dieta mediterránea) resultan cardiosaludables y que diversas sustancias bioactivas que componen los alimentos tienen un efecto preventivo en diversas enfermedades crónicas como son las enfermedades cardiovasculares. En esta revisión vamos a tratar ciertas sustancias bioactivas, como son algunas incluidas en el grupo de los flavonoides (catequinas y proantocianidinas, antocianinas e isoflavonas), estilbenos como el resveratrol, péptidos bioactivos, esteroles vegetales y ácidos grasos poliinsaturados omega-3 (AU)


Subject(s)
Humans , Cardiovascular Diseases/prevention & control , Protective Agents/pharmacokinetics , Nutrition Therapy/methods , Flavonoids/pharmacokinetics , Stilbenes/pharmacokinetics , Phytosterols/pharmacokinetics , Fatty Acids, Unsaturated/pharmacokinetics
17.
Rev. esp. cardiol. (Ed. impr.) ; 68(8): 665-671, ago. 2015. tab, ilus
Article in Spanish | IBECS | ID: ibc-138930

ABSTRACT

Introducción y objetivos. El consumo de estanoles vegetales puede contribuir a un mejor control a largo plazo del colesterol. El objetivo es evaluar la eficacia del aporte de estanoles vegetales, a dosis de 2 g/día, en la reducción de las cifras de colesterol unido a lipoproteínas de baja densidad de los pacientes con hipercolesterolemia. Métodos. Se realizó un ensayo clínico aleatorizado, a doble ciego y controlado con placebo, en el que se incluyó a 182 sujetos adultos diagnosticados de hipercolesterolemia. Se administró yogur líquido con 2 g de estanoles vegetales a 91 sujetos del grupo intervención y yogur no suplementado a 91 del grupo control. La variable principal fue la variación del perfil lipídico a los 12 meses. Resultados. En comparación con el placebo, a los 12 meses se observó una disminución significativamente superior del colesterol unido a lipoproteínas de baja densidad en el grupo que tomó estanoles: 13,7 (intervalo de confianza del 95%, 3,2-24,1) mg/dl (p = 0,011). En este grupo fue significativamente superior la proporción de sujetos que redujeron en más del 10% sus cifras de colesterol unido a lipoproteínas de baja densidad (riesgo relativo = 1,7; intervalo confianza del 95%, 1,1-2,7). En el grupo tratado, el colesterol unido a lipoproteínas de baja densidad descendió, en promedio, un 11,0 ± 23,9%. Conclusiones. Los resultados confirman que la administración de estanoles vegetales en dosis de 2 g/día durante 1 año produce una reducción significativa (ligeramente superior al 10%) de las concentraciones de colesterol unido a lipoproteínas de baja densidad en sujetos con hipercolesterolemia (AU)


Introduction and objectives. Plant stanol consumption may improve long-term cholesterol control. The aim of the present study was to evaluate the effectiveness of 2 g/day of plant stanols in reducing low-density lipoprotein cholesterol levels in patients with hypercholesterolemia. Methods. This randomized, double-blind, and placebo-controlled study included 182 adults diagnosed with hypercholesterolemia. A yogurt drink containing 2 g of plant stanols was administered to 91 participants in the intervention group; 91 participants in the control group received unsupplemented yogurt. The primary end point was the change in the lipid profile at 12 months. Results. Low-density lipoprotein cholesterol levels at 12 months were significantly more reduced in the stanol intervention group than in the control group: 13.7 (95% confidence interval, 3.2-24.1) mg/dL (P = .011). A reduction of more than 10% in low-density lipoprotein cholesterol was achieved by a significantly higher proportion of participants in the intervention group (relative risk = 1.7; 95% confidence interval, 1.1-2.7). In this group, the mean (standard deviation) level of low-density lipoprotein cholesterol decreased by 11.0% (23.9%). Conclusions. Our results confirm that administration of plant stanols at a dosage of 2 g/day for 12 months significantly reduces (by slightly more than 10%) the concentrations of low-density lipoprotein cholesterol in individuals with hypercholesterolemia (AU)


Subject(s)
Female , Humans , Male , Middle Aged , Hypercholesterolemia/diagnosis , Hypercholesterolemia/therapy , Phytosterols/therapeutic use , Cardiovascular Diseases/prevention & control , Lipoproteins, LDL/metabolism , Lipid Metabolism , Phytosterols/pharmacokinetics , Phytosterols/standards , Primary Health Care/methods , Primary Health Care/trends , Cholesterol/metabolism , Cholesterol/therapeutic use , Sterol Esterase/therapeutic use , Double-Blind Method
18.
Nutr. hosp ; 32(2): 696-701, ago. 2015. tab
Article in English | IBECS | ID: ibc-140004

ABSTRACT

Introduction: the abuse of steroid hormones administered in chronic form may cause alterations in the lypidic profile, conveying na increase in the levels of LDL, and reduction in the levels of HDL. In average, 53.44% of the lypidic composition of the avocado core is composed of oleic acid (which is a phytosterol) and the study of the hypolipemiating effect of these substances has been performed aiming at the prevention and control of dislypidemias. Objective: to assess the potential hypolipemiant power of the avocado oil on the lypidogram of adult male Wistar rats submitted to prolonged androgenic hiperestimulation. Materials and methods: twenty eight Wistar rats were divided in 4 groups of 7 animals: the control group (CG); Avocado Oil Group (AOG) fed with a staple based on Avocado Oil; Induced Grupo (IG); and the Induced Grupo fed with a staple based on Avocado Oil (AOIG). The inducing was performed through surgery to subcutaneously implant sillicon pellets suffed with 1ml of testosterone propionate which were replaced at every 4 weeks. Results: VLDL (AOIG: 28.14±4.45; IG:36.83±5.56 mg/ml); Triglicerides (AOIG: 140.07±22.66; IG: 187.2±27 mg/ml); HDL (AOIG: 40, 67±1.2; GI: 35.09±0.8; AOG: 32.31±2.61 e CG: 32.36±4.93mg/ml) Testosterone (AOIG:1.42±0.46; GI: 2.14±0.88; AOG: 2.97±1.34 e CG:1.86±0.79ng/ml). Conclusion: avocado Oil exerted a direct regulating effect on the lypidic profile, acting efficiently on animals submmited to androgenic stimulation through a prolonged period (AU)


Introducción: el uso abusivo de hormonas esteroides administradas crónicamente puede ocasionar cambios en el perfil lipídico, lo que lleva a un aumento de LDL y niveles reducidos de HDL. El promedio (53,44%) de la composición de lípidos de la pulpa de aguacate está compuesto por ácido oleico (que es un fitosterol), y el estudio del efecto hipolipemiante de estas sustancias se ha celebrado para la prevención y el control de la dislipemia. Objetivo: evaluar el potencial de reducción de lípidos del aceite de aguacate en ratones Wistar machos adultos sometidos a hiperestimulación androgénica prolongada. Material y métodos: veintiocho ratas se dividieron en 4 grupos de 7 animales: Grupo Control (GC); Grupo de Aceite de Aguacate (GOA), alimentado a base de aceite de aguacate; Grupo Inducido (GI) y el grupo alimentado con base de aceite de aguacate inducida por la dieta (GIOA). La indución fue hecha mediante perdigones de silicona subcutáneos, implantados por cirugía, llenos de 1 ml de propionato de testosterona, que fueron cambiados cada 4 semanas. Resultados: VLDL (GIOA: 28,14 ± 4,45; GI: 36,83 ± 5,56 mg/ml); triglicéridos (GIOA: 140.07 ± 22.66, GI 187: 2 ± 27 mg/ml); HDL (GIOA: 40,67 ± 1,2; GI: 35,09 ± 0,8; GOA: 32,31 ± 2,61 eGC: 32,36 ± 4,93 mg/ml); testosterona (GIOA: 1,42 ± 0,46; GI: 2,14 ± 0,88; GOA: 2,97 ± 1,34 eGC: 1,86 ± 0,79 ng/ml). Conclusión: El aceite de aguacate ha tenido un efecto regulador directo sobre el perfil lipídico, actuando eficazmente en los animales sometidos a estimulación de andrógenos durante períodos prolongado (AU)


Subject(s)
Animals , Female , Male , Mice , Persea , Persea/radiation effects , Lipoproteins, HDL/analysis , Lipoproteins, HDL , Cholesterol, HDL/analysis , Lipoproteins, LDL/analysis , Oleic Acid/isolation & purification , Lipids/analysis , Models, Animal , Phytosterols/analysis , Phytosterols/pharmacokinetics , Rats, Wistar/physiology , Gonadal Steroid Hormones/analysis , Gonadal Steroid Hormones/metabolism , Gonadal Steroid Hormones/therapeutic use
19.
J AOAC Int ; 98(3): 679-684, 2015.
Article in English | MEDLINE | ID: mdl-26086252

ABSTRACT

Most clinical phytosterol studies are performed by adding purified supplements to smaller phytosterol amounts present in the natural diet. However, natural dietary phytosterols themselves may also have important effects on cholesterol metabolism. Epidemiological work using food frequency questionnaires to estimate dietary intake suggest that extremes of normal consumption may be associated with 3-14% changes in LDL cholesterol. Standardized food databases do not have enough phytosterol values to allow calculation of phytosterol intake for individuals outside of specialized studies. Natural diets contain phytosterol amounts ranging from less than 60 mg/2000 kcal to over 500 mg/2000 kcal. Physiological studies in which whole body cholesterol metabolism is investigated show large effects of natural dietary phytosterols on cholesterol absorption efficiency, cholesterol biosynthesis and cholesterol excretion which exceed the magnitude of changes in LDL cholesterol. The dual effects of natural phytosterols on both LDL-C and whole body cholesterol metabolism need to be considered in relating them to potential protection from coronary heart disease risk.


Subject(s)
Diet , Phytosterols/analysis , Animals , Anticholesteremic Agents/pharmacology , Food Analysis , Humans , Phytosterols/pharmacokinetics , Phytosterols/pharmacology
20.
Pediatr Res ; 78(2): 181-9, 2015 Aug.
Article in English | MEDLINE | ID: mdl-25897540

ABSTRACT

BACKGROUND: Phytosterols in soybean oil (SO) lipids likely contribute to parenteral nutrition-associated liver disease (PNALD) in infants. No characterization of phytosterol metabolism has been done in infants receiving SO lipids. METHODS: In a prospective cohort study, 45 neonates (36 SO lipid vs. 9 control) underwent serial blood sample measurements of sitosterol, campesterol, and stigmasterol. Mathematical modeling was used to determine pharmacokinetic parameters of phytosterol metabolism and phytosterol exposure. RESULTS: Compared to controls, SO lipid-exposed infants had significantly higher levels of sitosterol and campesterol (P < 0.01). During SO lipid infusion, sitosterol and campesterol reached half of steady-state plasma levels within 1.5 and 0.8 d, respectively. Steady-state level was highest for sitosterol (1.68 mg/dl), followed by campesterol (0.98 mg/dl), and lowest for stigmasterol (0.01 mg/dl). Infants born < 28 wk gestational age had higher sitosterol steady-state levels (P = 0.03) and higher area under the curve for sitosterol (P = 0.03) during the first 5 d of SO lipid (AUC5) than infants born ≥ 28 wk gestational age. CONCLUSION: Phytosterols in SO lipid accumulate rapidly in neonates. Very preterm infants receiving SO lipid have higher sitosterol exposure, and may have poorly developed mechanisms of eliminating phytosterols that may contribute to their vulnerability to PNALD.


Subject(s)
Parenteral Nutrition , Phytosterols/pharmacokinetics , Female , Half-Life , Humans , Infant, Newborn , Male , Prospective Studies
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