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1.
J Plast Surg Hand Surg ; 54(6): 337-343, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32876517

RESUMEN

Moist exposed burn ointment (MEBO) is an oil-based herbal paste, purported to be efficacious in managing burn wounds and more commonly used in Asia and the Middle East. A PRISMA-compliant systematic review was performed to analyse the evidence for the use of MEBO on burn wounds. Wound healing rate was the primary outcome of interest. PubMed-listed randomised controlled trials (RCTs) comparing the efficacy of MEBO with placebo, standard care or other therapies in the treatment of partial thickness burns in adults and children were eligible for inclusion (November 2019). Six RCTs were eligible. The majority of trials comparing wound healing between MEBO and SSD favoured MEBO (two of three). There may be improved healing in MEBO-treated wounds vs. those treated with povidone-iodine + bepanthenol cream. There was no difference between MEBO and Acquacel Ag, but Helix Aspersa had faster healing rates than MEBO. However, all evidence was from moderately to poorly reported trials with a high risk of bias, thereby limiting the strength of this evidence. In conclusion, the evidence for MEBO in English-language literature was poor and inconsistent with respect to wound healing rate and analgesis compared to 1% SSD, Acquacel Ag, Helix aspersa cream and povidone-iodine + bepanthenol cream. Blinded RCTs comparing MEBO to both placebo and other common topical treatments may further improve the confidence in concluding their analysis. There is some evidence that MEBO is as safe as its comparators as shown by the low complication rate.


Asunto(s)
Quemaduras/tratamiento farmacológico , Sitoesteroles/administración & dosificación , Cicatrización de Heridas/efectos de los fármacos , Administración Tópica , Analgesia , Humanos , Pomadas/administración & dosificación , Sitoesteroles/efectos adversos
2.
Drug Dev Res ; 80(7): 921-932, 2019 11.
Artículo en Inglés | MEDLINE | ID: mdl-31298752

RESUMEN

The physicochemical properties, stability, in vivo antihyperalgesic activity, and skin irritation potential of the carbomer hydrogels with the new chemical entity escin ß-sitosterol (ES) phytosome were characterized and compared with those containing escin. Physicochemical characterization of the hydrogels (performed 48 hr after preparation) included organoleptic examination, pH measurement, light microscopy, differential scanning calorimetry analysis and rheological tests. The obtained results showed that increasing concentration of the active substances within 1-5% affected the appearance (color and transparency) of the hydrogels, their pH, consistency, and rheological behavior. Unlike acidic escin, which was dissolved in the liquid phase of the pseudoplastic hydrogels E1-E5 and reduced their maximal apparent viscosity (ηmax ), minimal apparent viscosity (ηmin ), and hysteresis area (H) in comparison to the plain carbomer hydrogel, amphiphilic ES-enhanced ηmax , ηmin , and thixotropy of the hydrogels ES1-ES5, which is favorable for prolonged retention at skin surface. Evaluation of in-use stability of the hydrogels showed that organoleptic characteristics, flow behavior, and pH values could be preserved for 3 months under ambient conditions. The rat ear test results suggested that the hydrogels are safe to be used on human skin. Both escin and ES-loaded hydrogels exerted significant, concentration-dependent antihyperalgesic effect in inflammatory pain model in rats. ES-loaded hydrogels were significantly more effective than those loaded with escin. This is a first report on the antihyperalgesic effect of topically applied escin as well as ES in a model of inflammatory pain.


Asunto(s)
Escina/química , Escina/farmacología , Hidrogeles/farmacología , Sitoesteroles/química , Sitoesteroles/farmacología , Administración Cutánea , Animales , Fenómenos Químicos , Relación Dosis-Respuesta a Droga , Composición de Medicamentos/métodos , Estabilidad de Medicamentos , Escina/efectos adversos , Hidrogeles/administración & dosificación , Hidrogeles/efectos adversos , Hidrogeles/química , Masculino , Dimensión del Dolor/efectos de los fármacos , Ratas , Sitoesteroles/efectos adversos
3.
Biochem J ; 474(17): 2993-3010, 2017 08 17.
Artículo en Inglés | MEDLINE | ID: mdl-28739601

RESUMEN

Arthritis is a chronic inflammatory disease which reduces the life quality of affected individuals. Therapeutic tools used for treating inflammatory pain are associated with several undesirable effects. Buddleja thyrsoides Lam., known as 'Barbasco' or 'Cambara', is mostly used in several disorders and possesses antirheumatic, anti-inflammatory, and analgesic properties. Here, we investigated the antinociceptive and anti-inflammatory effects of the B. thyrsoides crude extract applied orally and topically in acute pain models and an arthritic pain model induced by complete Freund's adjuvant (CFA) paw injection in male mice (25-30 g). The high-performance liquid chromatography (HPLC) of the B. thyrsoides extract crude revealed the presence of the lupeol, stigmasterol, and ß-sitosterol. The stability study of the B. thyrsoides gel did not show relevant changes at low temperatures. The oral treatment with the B. thrysoides extract prevented the capsaicin-induced spontaneous nociception and the acetic acid-induced abdominal writhing, but did not alter the thermal threshold in the tail immersion test. The B. thyrsoides antinociceptive effect was not reversed by naloxone in the capsaicin test. The B. thyrsoides oral or topical treatment reversed the CFA-induced mechanical allodynia and thermal hyperalgesia with maximum inhibition (Imax) of 69 ± 6 and 68 ± 5% as well as 78 ± 15 and 87 ± 12%, respectively. Moreover, the topical but not oral treatment inhibited the CFA-induced cell infiltration, but did not reduce the paw edema significantly. The oral treatment with B. thyrsoides did not cause adverse effects. These findings suggest that the oral or topical treatment with B. thyrsoides presents antinociceptive actions in an arthritic pain model without causing adverse effects.


Asunto(s)
Analgésicos no Narcóticos/uso terapéutico , Antiinflamatorios no Esteroideos/uso terapéutico , Artritis Experimental/tratamiento farmacológico , Buddleja/química , Extractos Vegetales/uso terapéutico , Hojas de la Planta/química , Dolor Agudo/tratamiento farmacológico , Administración Cutánea , Administración Oral , Analgésicos no Narcóticos/administración & dosificación , Analgésicos no Narcóticos/efectos adversos , Analgésicos no Narcóticos/química , Animales , Antiinflamatorios no Esteroideos/administración & dosificación , Antiinflamatorios no Esteroideos/efectos adversos , Antiinflamatorios no Esteroideos/química , Brasil , Buddleja/crecimiento & desarrollo , Estabilidad de Medicamentos , Almacenaje de Medicamentos , Etnofarmacología , Geles , Calor/efectos adversos , Masculino , Ratones , Triterpenos Pentacíclicos/administración & dosificación , Triterpenos Pentacíclicos/efectos adversos , Triterpenos Pentacíclicos/análisis , Triterpenos Pentacíclicos/uso terapéutico , Extractos Vegetales/administración & dosificación , Extractos Vegetales/efectos adversos , Extractos Vegetales/química , Hojas de la Planta/crecimiento & desarrollo , Sitoesteroles/administración & dosificación , Sitoesteroles/efectos adversos , Sitoesteroles/análisis , Sitoesteroles/uso terapéutico , Estigmasterol/administración & dosificación , Estigmasterol/efectos adversos , Estigmasterol/análisis , Estigmasterol/uso terapéutico , Viscosidad
4.
Medicine (Baltimore) ; 96(29): e7582, 2017 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-28723796

RESUMEN

BACKGROUND: Pressure ulcers often seriously affect the quality of life of patients. Moist Exposed Burn Ointment (MEBO) has been developed to treat patients with pressure ulcers. The present study aimed to evaluate the efficacy and safety of MEBO in the treatment of pressure ulcers in Chinese patients. METHODS: Seventy-two patients with pressure ulcers were randomly assigned to 2 groups who received a placebo or MEBO for 2 months. The primary outcomes included the wound surface area (WSA) and pressure ulcer scale for healing (PUSH) tool. The secondary outcomes included a visual analog scale (VAS), questionnaire of ulcer status, and adverse effects. RESULTS: Sixty-seven patients completed the study. After 2 months of treatment, the difference of mean change from the baseline was greater for MEBO (vs placebo) for WSA mean (SD) -6.0 (-8.8, -3.3), PUSH Tool -2.6 (-4.7, -1.5), and VAS score -2.9 (-4.4, -1.7). On the basis of the questionnaire, the pressure ulcers were "completely healed" (50.0% vs 16.7%) (P < .05) in patients after 2 months of treatment with MEBO versus placebo. No major adverse effects were found in the 2 groups. CONCLUSION: We showed that MEBO is effective and well tolerated for improving wound healing in Chinese patients with pressure ulcers.


Asunto(s)
Medicamentos Herbarios Chinos/uso terapéutico , Úlcera por Presión/tratamiento farmacológico , Sitoesteroles/uso terapéutico , Anciano , China , Medicamentos Herbarios Chinos/efectos adversos , Femenino , Humanos , Masculino , Dimensión del Dolor , Úlcera por Presión/patología , Índice de Severidad de la Enfermedad , Sitoesteroles/efectos adversos , Encuestas y Cuestionarios , Resultado del Tratamiento , Cicatrización de Heridas/efectos de los fármacos
5.
Food Funct ; 7(9): 3999-4011, 2016 Sep 14.
Artículo en Inglés | MEDLINE | ID: mdl-27711824

RESUMEN

Banana is an extensively cultivated plant worldwide, mainly for its fruit, while its ancillary product, the banana pseudostem, is consumed as a vegetable and is highly recommended for diabetics in the traditional Indian medicine system. The present study was aimed at elucidating the mechanism of antihyperglycaemia exerted by the ethanol extract of banana pseudostem (EE) and its isolated compounds viz., stigmasterol (C1) and ß-sitosterol (C2), in an alloxan-induced diabetic rat model. Diabetic rats which were administered with C1, C2 and EE (100 and 200 mg per kg b. wt.) for 4 weeks showed reduced levels of fasting blood glucose and reversal of abnormalities in serum/urine protein, urea and creatinine in diabetic rats compared to the diabetic control group of rats. Diabetic symptoms such as polyphagia, polydipsia, polyuria, urine glucose and reduced body weight were ameliorated in the diabetic group of rats fed with EE, C1 and C2 (100 mg per kg b. wt., once daily) for 28 days. The levels of insulin and Hb were also increased, while the HbA1c level was reduced. The altered activities of hepatic marker enzymes viz., aspartate transaminase (AST), alanine transaminase (ALT) and alkaline phosphatase (ALP); glycolytic enzyme (hexokinase); shunt enzyme (glucose-6-phosphate dehydrogenase); gluconeogenic enzymes (glucose-6-phosphatase, fructose-1,6-bisphosphatase and lactate dehydrogenase) and pyruvate kinase were significantly reverted to normal levels by the administration of EE, C1 and C2. In addition, increased levels of hepatic glycogen and glycogen synthase and the corresponding decrease of glycogen phosphorylase activity in diabetic rats illustrated the antihyperglycaemic potential of EE and its components. The histological observations revealed a marked regeneration of the ß-cells in the drug treated diabetic rats. These findings suggest that EE might exert its antidiabetic potential in the presence of C1 and C2, attributable to the enhanced glycolytic activity, besides increasing the hepatic glucose utilization in diabetic rats by stimulating insulin secretion from the remnant ß-cells.


Asunto(s)
Diabetes Mellitus Experimental/dietoterapia , Suplementos Dietéticos , Hipoglucemiantes/uso terapéutico , Musa/química , Extractos Vegetales/uso terapéutico , Sitoesteroles/uso terapéutico , Estigmasterol/uso terapéutico , Aloxano , Animales , Biomarcadores/sangre , Línea Celular Tumoral , Diabetes Mellitus Experimental/sangre , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Experimental/patología , Etnofarmacología , Femenino , Hiperglucemia/prevención & control , Hipoglucemiantes/administración & dosificación , Hipoglucemiantes/efectos adversos , Hipoglucemiantes/aislamiento & purificación , Insulina/metabolismo , Secreción de Insulina , Células Secretoras de Insulina/metabolismo , Células Secretoras de Insulina/patología , Masculino , Medicina Ayurvédica , Musa/crecimiento & desarrollo , Extractos Vegetales/administración & dosificación , Extractos Vegetales/efectos adversos , Hojas de la Planta/química , Hojas de la Planta/crecimiento & desarrollo , Ratas , Ratas Wistar , Sitoesteroles/administración & dosificación , Sitoesteroles/efectos adversos , Sitoesteroles/aislamiento & purificación , Estigmasterol/administración & dosificación , Estigmasterol/efectos adversos , Estigmasterol/aislamiento & purificación , Pruebas de Toxicidad Aguda
6.
Br J Nutr ; 113(5): 794-802, 2015 Mar 14.
Artículo en Inglés | MEDLINE | ID: mdl-25683704

RESUMEN

Plant sterols and stanols inhibit intestinal cholesterol absorption and consequently lower serum LDL-cholesterol (LDL-C) concentrations. The underlying mechanisms are not yet known. In vitro and animal studies have suggested that changes in intestinal sterol metabolism are attributed to the LDL-C-lowering effects of plant stanol esters. However, similar studies in human subjects are lacking. Therefore, we examined the effects of an acute intake of plant stanol esters on gene expression profiles of the upper small intestine in healthy volunteers. In a double-blind cross-over design, fourteen healthy subjects (eight female and six male; age 21-55 years), with a BMI ranging from 21 to 29 kg/m², received in random order a shake with or without plant stanol esters (4 g). At 5 h after consumption of the shake, biopsies were taken from the duodenum (around the papilla of Vater) and from the jejunum (20 cm distal from the papilla of Vater). Microarray analysis showed that the expression profiles of genes involved in sterol metabolism were not altered. Surprisingly, the pathways involved in T-cell functions were down-regulated in the jejunum. Furthermore, immunohistochemical analysis showed that the number of CD3 (cluster of differentiation number 3), CD4 (cluster of differentiation number 4) and Foxp3⁺ (forkhead box P3-positive) cells was reduced in the plant stanol ester condition compared with the control condition, which is in line with the microarray data. The physiological and functional consequences of the plant stanol ester-induced reduction of intestinal T-cell-based immune activity in healthy subjects deserve further investigation.


Asunto(s)
Anticolesterolemiantes/administración & dosificación , Inmunidad Mucosa , Inmunomodulación , Mucosa Intestinal/inmunología , Yeyuno/inmunología , Sitoesteroles/administración & dosificación , Linfocitos T/inmunología , Adulto , Anticolesterolemiantes/efectos adversos , Antígenos de Superficie/sangre , Antígenos de Superficie/genética , Antígenos de Superficie/metabolismo , Bebidas , Estudios Cruzados , Método Doble Ciego , Regulación hacia Abajo , Duodeno/citología , Duodeno/inmunología , Duodeno/metabolismo , Femenino , Factores de Transcripción Forkhead/sangre , Factores de Transcripción Forkhead/genética , Factores de Transcripción Forkhead/metabolismo , Regulación de la Expresión Génica , Humanos , Mucosa Intestinal/citología , Mucosa Intestinal/metabolismo , Yeyuno/citología , Yeyuno/metabolismo , Masculino , Persona de Mediana Edad , Sitoesteroles/efectos adversos , Linfocitos T/citología , Linfocitos T/metabolismo , Adulto Joven
7.
J Pharm Pharmacol ; 66(3): 428-36, 2014 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-24237052

RESUMEN

OBJECTIVES: Plant sterols are thought to treat hypercholesterolemia via inhibiting intestinal cholesterol absorption. The aim of this study was to evaluate the contribution of impaired ATP-binding cassette transporter G5/8 (ABCG5/8) expression by diabetes to the increased ß-sitosterol (BS) exposure and impact of increased BS on integrity of blood-brain barrier (BBB). METHODS: Basal BS level in tissues of streptozotocin-inducted rats and ABCG5/8 protein levels in liver and intestine were investigated; pharmacokinetics of BS was studied following oral dose; and primarily cultured rat brain microvessel endothelial cells (rBMECs) were used to study BS transportation across BBB and effect of BS on BBB integrity. KEY FINDINGS: Diabetic rats showed greatly upgraded basal levels of BS in plasma, intestine, cerebral and hippocampus, accompanied by impairment of ABCG5/8 protein expression in liver and intestine. Pharmacokinetics studies demonstrated higher AUC0-48 and Cmax , and lower faecal recoveries of BS after oral administration, indicating enhancement of absorption or efflux impairment. In-vitro data showed increased ratio of BS/cholesterol in high levels BS-treated rBMECs was associated with increased BBB permeability of some biomarkers including BS itself. CONCLUSIONS: Impaired ABCG5/8 protein expression by diabetes led to increase in BS exposure, which may be harmful to BBB function.


Asunto(s)
Transportadoras de Casetes de Unión a ATP/metabolismo , Barrera Hematoencefálica/efectos de los fármacos , Permeabilidad Capilar , Diabetes Mellitus Experimental/metabolismo , Mucosa Intestinal/metabolismo , Hígado/metabolismo , Sitoesteroles/farmacocinética , Administración Oral , Animales , Transporte Biológico , Encéfalo/metabolismo , Colesterol/sangre , Diabetes Mellitus Experimental/complicaciones , Heces/química , Masculino , Ratas , Ratas Sprague-Dawley , Sitoesteroles/efectos adversos , Sitoesteroles/metabolismo
8.
Atherosclerosis ; 225(2): 521-33, 2012 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-23083678

RESUMEN

Abundant evidence over past decades shows that foods with added plant sterols and plant stanols lower serum LDL cholesterol concentrations. However, despite the overwhelming data, numerous scientific questions still remain. The objective of this paper is to summarize the considerations of 60 academic and industrial experts who participated in the scientific meeting in Maastricht, the Netherlands, on issues related to the health effects of plant sterols and plant stanols. The meeting participants discussed issues including efficacy profiling, heterogeneity in responsiveness, effects beyond LDL-C lowering, and food formulation aspects of plant sterol and stanol consumption. Furthermore, aspects related to the potential atherogenicity of elevated circulatory plant sterol concentrations were discussed. Until the potential atherogenicity of plant sterols is resolved, based on the results >200 clinical trials, the risk to benefit of plant sterol use is favorable. Evidence on these topics in plant sterol and plant stanol research was presented and used to reach consensus where possible. It was concluded that endpoint studies looking at plant sterol and plant stanol efficacy are needed, however, there was no clear opinion on the best marker and best design for such a study. Based on the current scientific evidence, plant sterols and plant stanols are recommended for use as dietary options to lower serum cholesterol.


Asunto(s)
Anticolesterolemiantes/uso terapéutico , Suplementos Dietéticos , Hipercolesterolemia/tratamiento farmacológico , Fitosteroles/uso terapéutico , Sitoesteroles/uso terapéutico , Animales , Anticolesterolemiantes/efectos adversos , Anticolesterolemiantes/química , Anticolesterolemiantes/metabolismo , Aterosclerosis/etiología , Biomarcadores/sangre , Química Farmacéutica , Colesterol/sangre , Dieta/efectos adversos , Suplementos Dietéticos/efectos adversos , Humanos , Hipercolesterolemia/sangre , Política Nutricional , Fitosteroles/efectos adversos , Fitosteroles/química , Fitosteroles/metabolismo , Medición de Riesgo , Factores de Riesgo , Sitoesteroles/efectos adversos , Sitoesteroles/química , Sitoesteroles/metabolismo , Resultado del Tratamiento , Triglicéridos/sangre
9.
Maturitas ; 73(3): 180-5, 2012 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-22883375

RESUMEN

Benign prostatic hyperplasia (BPH) is a common chronic condition in older men. The aim of this overview of systematic reviews (SRs) is to summarise the current evidence on the efficacy and adverse effects of dietary supplements for treating BPH with lower urinary tract symptoms. We searched 5 electronic databases and relevant overviews without limitations on language or publication status. Six SRs of 195 articles were included in this overview. Serenoa repens was reviewed in 3 studies and no specific effect on BPH symptoms and urinary flow measures was observed. However, ß-sitosterol, Pygeum africannum and Cernilton were reviewed in one study each, and significant improvement was observed for all three. All the included compounds have mild and infrequent adverse effects. SRs on ß-sitosterol, Pygeum africannum and Cernilton have not been updated since 2000, thus an update of reviews on these compounds will be necessary in the future.


Asunto(s)
Suplementos Dietéticos , Fitoterapia , Extractos Vegetales/uso terapéutico , Hiperplasia Prostática/tratamiento farmacológico , Prunus africana , Serenoa , Sitoesteroles/uso terapéutico , Suplementos Dietéticos/efectos adversos , Humanos , Masculino , Extractos Vegetales/efectos adversos , Hiperplasia Prostática/complicaciones , Prunus africana/efectos adversos , Secale/efectos adversos , Serenoa/efectos adversos , Sitoesteroles/efectos adversos , Resultado del Tratamiento , Enfermedades Urológicas/tratamiento farmacológico , Enfermedades Urológicas/etiología
10.
J Agric Food Chem ; 60(16): 4060-6, 2012 Apr 25.
Artículo en Inglés | MEDLINE | ID: mdl-22490085

RESUMEN

Oxysterols, found in some commonly consumed foods, can induce a wide range of cytotoxic effects, which have been extensively studied. On the other hand, the side effects of phytosterols and oxyphytosterols are less well-known. Over the past few years, different types of foods have been enriched with phytosterols on the basis of the properties of these compounds that reduce circulating cholesterol levels in certain experimental conditions. It is therefore important to gain better knowledge of the risks and benefits of this type of diet. In this study, conducted in human monocytic U937 cells, the ability of phytosterols (sitosterol, campesterol) and oxyphytosterols (7ß-hydroxysitosterol, 7-ketositosterol) to induce cell death, polar lipid accumulation, and pro-inflammatory cytokine (MCP-1; IL-8) secretion was determined and compared to that of oxysterols (7-ketocholesterol, 7ß-hydroxycholesterol). Phytosterols and oxyphytosterols had no significant effects on the parameters studied; only 7ß-hydroxysitosterol slightly increased cell death, whereas at the concentration used (20 µg/mL), strong cytotoxic effects were observed with the oxysterols. With sitosterol, campesterol, and 7-ketositosterol, IL-8 secretion was decreased, and with campesterol the intracellular polar lipid level was reduced. The data show that phytosterols and oxyphytosterols have no oxysterol-like side effects, and they rather argue in favor of phytosterols' beneficial effects.


Asunto(s)
Monocitos/efectos de los fármacos , Fitosteroles/farmacología , Sitoesteroles/farmacología , Apoptosis/efectos de los fármacos , Muerte Celular/efectos de los fármacos , Humanos , Monocitos/citología , Fitosteroles/efectos adversos , Sitoesteroles/efectos adversos , Células U937
11.
Complement Ther Med ; 19(1): 37-46, 2011 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-21296266

RESUMEN

Recommendations about the use of plant stanol/sterol esters have not been updated since 2001. There have been many developments in medicines for lipid-lowering since 2001. In this review, the use of margarines containing stanol or sterol esters, to lower LDL cholesterol is considered in the 2011 setting. Firstly, there is a brief overview of the effects of the stanols/sterols on LDL cholesterol, which shows that these agents have a modest ability to lower LDL cholesterol, and are not effective in all conditions. Secondly, the relevance of the stanols/sterols in 2010/1 is questioned, given they have not been shown to reduce clinical endpoints, and have no effects on HDL cholesterol or triglyceride levels. Finally, there is a section comparing the stanols/sterols with the present day prescription lipid lowering medicines. Prescription drugs (statins, ezetimibe, and niacin) have a much greater ability to lower LDL cholesterol than the stanol/sterol esters, and also increase levels of HDL cholesterol and decrease levels of triglycerides. The statins and niacin have been shown to reduce cardiovascular clinical endpoints. Except in borderline normo/hypercholesterolemia, prescription drugs should be preferred to stanol/sterol esters for lowering LDL cholesterol in 2011.


Asunto(s)
Anticolesterolemiantes/farmacología , Anticolesterolemiantes/uso terapéutico , Enfermedades Cardiovasculares/dietoterapia , Enfermedades Cardiovasculares/tratamiento farmacológico , LDL-Colesterol/efectos de los fármacos , Margarina , Fitosteroles/farmacología , Fitosteroles/uso terapéutico , Azetidinas/farmacología , HDL-Colesterol/efectos de los fármacos , LDL-Colesterol/genética , Diabetes Mellitus/dietoterapia , Diabetes Mellitus/tratamiento farmacológico , Ezetimiba , Ácidos Fíbricos/farmacología , Humanos , Inhibidores de Hidroximetilglutaril-CoA Reductasas/farmacología , Inhibidores de Hidroximetilglutaril-CoA Reductasas/uso terapéutico , Hipercolesterolemia/dietoterapia , Hipercolesterolemia/tratamiento farmacológico , Hiperlipoproteinemia Tipo II/dietoterapia , Hiperlipoproteinemia Tipo II/tratamiento farmacológico , Enfermedades Intestinales/dietoterapia , Enfermedades Intestinales/tratamiento farmacológico , Errores Innatos del Metabolismo Lipídico/dietoterapia , Errores Innatos del Metabolismo Lipídico/tratamiento farmacológico , Micronutrientes/sangre , Niacina/farmacología , Fitosteroles/efectos adversos , Sitoesteroles/efectos adversos , Sitoesteroles/farmacología , Sitoesteroles/uso terapéutico , Triglicéridos/metabolismo
12.
J Agric Food Chem ; 58(18): 10064-9, 2010 Sep 22.
Artículo en Inglés | MEDLINE | ID: mdl-20731356

RESUMEN

Abnormal proliferation of vascular smooth muscle cells (VSMCs) plays a central role in the pathogenesis of atherosclerosis. ß-Sitosterol, an important phytosterol found in plant food, is known to exert antiatherosclerosis activity. However, the molecular mechanisms underlying ß-sitosterol-induced antiproliferation of VSMCs were still not clear. This study demonstrated that ß-sitosterol (1-20 µM) concentration-dependently inhibited proliferation of rat aortic smooth muscle cells (RASMCs) without cytotoxic effect. Flow cytometric analysis revealed that ß-sitosterol arrested cell cycle progression through down-regulation of cyclin E and cyclin-dependent kinase (CDK)2 and up-regulation of p21cip1. In the ß-sitosterol-treated RASMCs, the formation of the CDK2-p21cip1 complex was increased and the assayable CDK2 activity was decreased. Knockdown of the expression of p21cip1 gene prevented ß-sitosterol-induced cell cycle arrest in RASMCs. In conclusion, ß-sitosterol inhibited VSMC proliferation by increasing the levels of p21cip1 protein, which in turn inhibited the CDK2 activity, and finally interrupted the progress of the cell cycle.


Asunto(s)
Aorta Torácica/efectos de los fármacos , Ciclo Celular/efectos de los fármacos , Inhibidor p21 de las Quinasas Dependientes de la Ciclina/metabolismo , Hipolipemiantes/farmacología , Músculo Liso Vascular/efectos de los fármacos , Sitoesteroles/farmacología , Regulación hacia Arriba/efectos de los fármacos , Animales , Aorta Torácica/citología , Aorta Torácica/metabolismo , Aterosclerosis/prevención & control , Proliferación Celular/efectos de los fármacos , Células Cultivadas , Inhibidor p21 de las Quinasas Dependientes de la Ciclina/genética , Hipolipemiantes/efectos adversos , Masculino , Músculo Liso Vascular/citología , Músculo Liso Vascular/metabolismo , Ratas , Ratas Sprague-Dawley , Sitoesteroles/efectos adversos
13.
J Eur Acad Dermatol Venereol ; 21(1): 100-3, 2007 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-17207176

RESUMEN

BACKGROUND: Sitosterolaemia is a lipid disorder in which plasma plant sterol levels are extremely elevated. Sitosterolaemia is clinically characterized by tuberous and tendon xanthomas, premature vascular disease and arthritis. OBJECTIVE: To report a case of sitosterolaemia diagnosed by cutaneous manifestations and to review this rare disease. METHODS: We report the case of a 60-year-old woman who presented with cutaneous xanthomas, arterial hypertension and polyarthralgias. The patient had had hypercholesterolaemia for many years without reduction of serum cholesterol, despite treatment with fenofibrate. RESULTS: Ezetimibe therapy was started, decreasing sitosterol plasmatic levels and tuberous xanthomas after 3 months of treatment. CONCLUSION: It is important to detect levels of sitosterol in plasma in patients with premature vascular disease, presence of xanthomas, and uncontrolled hypercholesterolaemia. Ezetimibe therapy is effective.


Asunto(s)
Azetidinas/uso terapéutico , Hipolipemiantes/efectos adversos , Sitoesteroles/efectos adversos , Xantomatosis/diagnóstico , Ezetimiba , Femenino , Humanos , Persona de Mediana Edad , Xantomatosis/inducido químicamente , Xantomatosis/tratamiento farmacológico , Xantomatosis/patología
14.
Environ Pollut ; 144(3): 833-9, 2006 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-16584819

RESUMEN

We investigated the behavioral effects of exposure to waterborne phytoestrogens in male fighting fish, Betta splendens. Adult fish were exposed to a range of concentrations of genistein, equol, beta-sitosterol, and the positive control 17beta-estradiol. The following behaviors were measured: spontaneous swimming activity, latency to respond to a perceived intruder (mirror reflection), intensity of aggressive response toward a perceived intruder, probability of constructing a nest in the presence of a female, and the size of the nest constructed. We found few changes in spontaneous swimming activity, the latency to respond to the mirror, and nest size, and modest changes in the probability of constructing a nest. There were significant decreases, however, in the intensity of aggressive behavior toward the mirror following exposure to several concentrations, including environmentally relevant ones, of 17beta-estradiol, genistein, and equol. This suggests that phytoestrogen contamination has the potential to significantly affect the behavior of free-living fishes.


Asunto(s)
Conducta Animal/efectos de los fármacos , Peces/fisiología , Fitoestrógenos/efectos adversos , Contaminantes Químicos del Agua/efectos adversos , Agresión/efectos de los fármacos , Animales , Equol , Estradiol/efectos adversos , Femenino , Genisteína/efectos adversos , Isoflavonas/efectos adversos , Masculino , Comportamiento de Nidificación/efectos de los fármacos , Conducta Sexual Animal/efectos de los fármacos , Sitoesteroles/efectos adversos , Natación
16.
Am J Cardiol ; 96(1A): 15D-22D, 2005 Jul 04.
Artículo en Inglés | MEDLINE | ID: mdl-15992511

RESUMEN

Incorporation of plant stanol esters into margarine is among the first examples of a functional food with proven low-density lipoprotein (LDL) cholesterol-lowering effectiveness. Recently, there have been many studies on the effects of plant stanols/sterols on cholesterol metabolism. It has been found that the serum LDL cholesterol-lowering effect of plant stanols/sterols originates from reduced intestinal cholesterol absorption, a process in which changes in micellar composition are thought to play a major role. However, recent findings suggest that there is an additional process in which plant stanols/sterols actively influence cellular cholesterol metabolism within intestinal enterocytes. Furthermore, in response to the reduced supply of exogenous cholesterol, receptor-mediated lipoprotein cholesterol uptake is probably enhanced, as shown by increased LDL receptor expression. At recommended intakes of about 2 to 2.5 g/day, products enriched with plant stanol/sterol esters lower plasma LDL cholesterol levels by 10% to 14% without any reported side effects. Thus, plant stanols/sterols can be considered to be effective and safe cholesterol-lowering functional food ingredients.


Asunto(s)
LDL-Colesterol/metabolismo , Hipercolesterolemia/tratamiento farmacológico , Fitosteroles/efectos adversos , Fitosteroles/farmacología , Sitoesteroles/efectos adversos , Sitoesteroles/farmacología , Humanos , Absorción Intestinal , Fitosteroles/uso terapéutico , Fitoterapia , Sitoesteroles/uso terapéutico
18.
Arzneimittelforschung ; 53(10): 708-13, 2003.
Artículo en Inglés | MEDLINE | ID: mdl-14650363

RESUMEN

Feeding of margarines containing sitostanol (CAS 19466-47-8), sitostanol acetate (CAS 73052-08-1), sitostanol oleate (CAS 107615-79-2), or placebo (equivalent of 0.5 g of sitostanol t.i.d) on cholesterol absorption and serum lipids were studied in 10 normolipemic volunteers in a randomized double blind cross-over trial. The study was divided into an open one-week run-in phase and four one-week treatment periods. Each treatment week was followed by a two-week washout period. Measurements of cholesterol absorption was performed by the continuous isotope feeding method using stable isotope labeled cholesterol and sitostanol. Cholesterol absorption during placebo, sitostanol, sitostanol acetate and sitostanol oleate feeding averaged 41.6 +/- (SD) 8.0, 10.2 +/- 6.6, 17.0 +/- 6.7, and 20.5 +/- 5.3%, respectively (p < 0.001 for all against placebo). Low density lipoprotein (LDL) cholesterol was proportionally reduced by 22 (p < 0.001), 14 (p < 0.05), and 8% (ns). Absorption efficiency was significantly lower with free sitostanol than with sitostanol acetate or oleate (p < 0.01). Percent reduction in cholesterol absorption with all preparations compared to placebo correlated positively with the percent reduction in LDL cholesterol (r = 0.404; p < 0.03). The results indicate that unesterified sitostanol is more effective in inhibiting cholesterol absorption and reducing LDL cholesterol than the acetate or oleate esters.


Asunto(s)
Colesterol en la Dieta/farmacocinética , Absorción Intestinal/efectos de los fármacos , Sitoesteroles/farmacología , Acetatos/farmacología , Adulto , Estudios Cruzados , Método Doble Ciego , Humanos , Lipoproteínas/sangre , Masculino , Margarina , Ácidos Oléicos/farmacología , Fitosteroles/farmacología , Sitoesteroles/efectos adversos
19.
Nutrition ; 19(4): 369-74, 2003 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-12679174

RESUMEN

OBJECTIVE: The ester of plant stanols significantly reduces plasma levels of total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C) in Western people. Effects of plant stanol ester-containing spread on plasma levels of TC, LDL-C, and apolipoprotein B (apoB) were studied in a randomized, placebo-controlled trial in Japanese subjects whose diet is low in fat and cholesterol. The effects of plant stanol ester on plasma levels of arteriosclerosis-promoting factors, namely remnants of triacylglycerol (TG)-rich lipoproteins, cholesteryl ester transfer protein (CETP), and oxidized LDL (Ox-LDL), were also studied. The assessment of safety was also made. METHODS: One hundred and five healthy volunteers were assigned randomly to one of three groups: placebo spread (n = 35), 2 g/d of plant stanol (3.4 g of stanol ester; n = 34), and 3 g/d of plant stanol (5.1 g of stanol ester; n = 36). Plasma levels of lipids were measured at start of the study, at 2 and 4 wk (end of trial), and at 8 wk (+4 wk). Plasma apoproteins, cholesterol in remnant-like particles which are equivalent to remnants of TG-rich lipoproteins (RLP-C), CETP mass, and Ox-LDL were measured at the beginning and the end of the trial. Plasma levels of plant steroids and fat-soluble vitamins were also measured for the assessment of safety. RESULTS: Background and dietary composition did not differ among groups. Plasma levels of TC, LDL-C, apoB, apoE, CETP mass, and Ox-LDL were reduced significantly by 6.5%, 9.6%, 8.3%, 4.5%, 6.1%, and 20%, respectively, in the 2 g/d plant stanol group. Plasma levels of TC, LDL-C, apoB, CETP mass, and Ox-LDL were decreased significantly by 5.5%, 7.3%, 5.6%, 3.3%, and 19%, respectively, in the 3 g/d plant stanol group. Plasma levels of plant stanols, plant sterols, retinol, beta-carotene, and alpha-tocopherol did not change in any group, but levels of campestanol increased and alpha-tocopherol decreased slightly in the sitostanol groups. CONCLUSION: Plasma levels of TC and LDL-C were significantly reduced by the plant stanol ester-containing spread. The smaller reduction than in Western studies and the lack of dose dependency in this study might be due to the different basal diets. We concluded that plant stanol ester-containing spread is efficacious in reducing plasma LDL-C, apoB, CETP, and Ox-LDL and that 2 g/d plant stanol is adequate for Japanese people. No significant side effects were observed in any group.


Asunto(s)
Apolipoproteínas B/sangre , Proteínas Portadoras/sangre , Glicoproteínas , Hipercolesterolemia/dietoterapia , Lipoproteínas LDL/sangre , Sitoesteroles/administración & dosificación , Proteínas de Transferencia de Ésteres de Colesterol , LDL-Colesterol/sangre , Dieta , Relación Dosis-Respuesta a Droga , Femenino , Humanos , Hipercolesterolemia/sangre , Japón , Masculino , Persona de Mediana Edad , Placebos , Sitoesteroles/efectos adversos
20.
Nutr Metab Cardiovasc Dis ; 11(1): 31-40, 2001 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-11383323

RESUMEN

Functional foods enriched with plant sterols and stanols are on sale in many countries. Due to their structural similarity with cholesterol, these additives lower intestinal absorption of cholesterol, resulting in a 10-15% reduction in LDL-cholesterol when their daily intakes are 2-3 g. They are also effective as part of a cholesterol-lowering diet and in combination with cholesterol-lowering drugs. Estimates for the absorption of plant sterols (sitosterol and campesterol) and of campestanol are around 10%, and for sitostanol less than 5%. Lipid-standardized plasma levels are very low, but increase when statins are used. Extensive toxicological evaluation studies have not revealed any harmful side-effects. In human studies, side-effects were comparable to placebo treatment. However, lipid-standardized levels of the hydrocarbon carotenoids may decrease, without leaving the normal range. Together, these findings indicate that these functional foods have great potential in the prevention of coronary heart disease. However, post-marketing surveillance for example for functional foods in general is necessary to monitor possible adverse effects and describe consumers and consumption patterns.


Asunto(s)
Anticolesterolemiantes/farmacología , Enfermedades Cardiovasculares/metabolismo , Metabolismo de los Lípidos , Fitosteroles/farmacología , Anticolesterolemiantes/efectos adversos , Anticolesterolemiantes/farmacocinética , Enfermedades Cardiovasculares/prevención & control , Colesterol/metabolismo , Dieta , Alimentos Orgánicos , Humanos , Absorción Intestinal , Fitosteroles/efectos adversos , Fitosteroles/farmacocinética , Factores de Riesgo , Seguridad , Sitoesteroles/efectos adversos , Sitoesteroles/farmacocinética , Sitoesteroles/farmacología
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