Physiological Activities of Policosanol Extracted from Sugarcane Wax

Policosanol extracted from sugarcane wax is a generic term used for total fatty alcohols obtained from esterification of fatty acids. It has been approved as a health functional food by the Ministry of Food and Drug Safety of Korea in 2006. Policosanol is well-known to aid in lowering blood cholesterol level. Recently, several studies have reported the physiological activities of policosanol, such as anti-inflammatory effects, antioxidant effects, and lowering of the incidence of ageing-related diseases, for example, hypertension, stroke, among others. This review describes the physiological activities of policosanol and its applications in the field of health functional foods.

Validación de procesos con análisis inicial de criticidad aplicado a la obtención del principio activo policosanol (PPG) / Processes validation with initial analysis of criticality applied to obtaining the active ingredient policosanol (PPG)

Resumen Identificar cuáles son los activos que se someterán al proceso de validación es una tarea prioritaria para cualquier empresa que implemente un Sistema de Gestión de la Calidad, lo cual repercute de manera directa en el éxito de cualquier empresa. Como consecuencia de esto en septiembre de 2014 se diseñó un procedimiento en el departamento de Aseguramiento de la Calidad, dirección de Producción, CNIC; con el objetivo de determinar aquellos equipos o sistemas de apoyo auxiliar que serán sometidos al proceso de validación en la fabricación del principio activo del Policosanol (PPG). Para darle cumplimiento a nuestro objetivo el método utilizado se basa en la combinación de técnicas de riesgos tradicionales como son los métodos comparativos, diagramas lógicos de fallas, estudios de riesgo y operatividad, análisis de modos de falla y efectos, y otros. Como resultado se obtuvo un procedimiento general para la aplicación de la técnica de criticidad, la cual denominamos HAZID (HAZard-IDentification), basado en el análisis de riesgos. Como conclusión fundamental se obtiene un criterio de partida para justificar la inclusión de un equipo o sistema al proceso de validación.

Abstract Identifying the assets that will be submitted to the validation process is a priority task for any company that implements a Quality Management System, wicth has a direct impact on the success of any company. Taking into account the previous approach, it was designed in September 2014 a procedure in the department of Quality Assurance, Production Management, CNIC; with the aim of identifying those equipment or auxiliary systems that will be included in the validation process in the manufacture of the active ingredient Policosanol (PPG). To meet the principal goal, it was used a method based on the combination of techniques traditional risks such as comparative methods, fault logic diagrams, risk studies and operability, analysis of failure modes and effects, and others. As a result, it was obtained a general procedure for the implementation of the technique of criticality, it was named HAZID (HAZard-IDentification), based on risk analysis. As a fundamental conclusion, it was obtained a starting point to justify the inclusion of an equipment or auxiliary system to the validation process.

Meta-analysis of 10 mg policosanol versus an equal dose of atorvastatin on the lipid-lowering efficacy in patients with dyslipidemia / 药学实践杂志

Objective To evaluate the lipid-lowering effect of 10 mg policosanol versus an equal dose of atorvastatinin patients with dyslipidemia.Method Databases such as VIP,Wanfang,CNKI,Cochrance Library,PubMed,Web of Science and EMBASE were searched for random control trials(RCT) and controlled clinical trials (CCT) of 10 mg policosanol versus an equal dose of atorvastatinin their lipid-lowering effects.The quality was assessed by Cochrance Handbook 5.1.0 or Newcastle-Ottawa scale (NOS).The study related data were analyzed statistically with RevMan 5.2 software.4 RCTs were selected.257 patients were included in the trials.130 cases were in 10 mg policosanol group and 127 cases belonged to 10 mg atorvastatin group.Results Results of Meta-analysis show that TC[SMD=0.84,95%CI(0.41,1.27),P=0.000 1] and LDL-C[SMD=0.68,95%CI(0.28,1.09),P=0.001] were reduced more effectively in 10 mg atorvastatin group than in 10 mg policosanol group.HDL-C[SMD=0.27,95%CI(0.02,0.51),P=0.03] was elevated more in 10 mg policosanol group than 10 mg atorvastatin group.Both groups showed no statistic difference(P=0.42) in TG [SMD=0.10,95% CI:(-0.41,0.35),P=0.42].Conclusion The lipid-lowering efficacy of 10 mg atorvastatin is better than equal dose of policosanolin patients with dyslipidemia.Dose increase of policosanol should be considered to ensure the efficacy when policosanol was used tore place atorvastatin therapy.This study had some shortcomings, such as limited study numbers and small sample size.The reliability of this study should be verified from high-quality,multi-center RCTS with large samples.

Safety and efficacy of policosanol in elder patients with high on-treatment platelet reactivity after ;drug-eluting stent implantation:a subgroup analysis of the SPIRIT study / 中国介入心脏病学杂志

Objective To explore the safety and efficacy of policosanol in elder patients with high on-treatment platelet reactivity ( HPR) after drug-eluting stent ( DES) implantation. Methods This study was a prespecified subgroup analysis of the multicenter, randomized SPIRIT trial,in which there were a total of 169 elder patients (≥60 years old) with HPR. Among these patients, 30 patients were in group A ( given clopidogrel 75 mg/d for one year) , 75 patients in group B ( given clopidogrel 150 mg/d for 30 days followed by 75 mg/d until one year ) and 64 patients in group C ( given policosanol 40 mg/d for 6 month and clopidgrel 75 mg/d for one year ) . All patients were treated with aspirin at the same time. The primary endpoint was the reversion rate of HPR at 30 days (reversion was defined as platelet aggregation ﹤65%). The secondary endpoint was 2-year major adverse cardiac events ( MACE ) rate, which included cardiac death, non-fatal myocardial infarction and ischemic symptoms driven target vessel revascularization. The safety endpoint was any bleeding as defined by the Bleeding Academic Research Consortium ( BARC ) definition. Results At 30 days, the reversion rate of HPR in group C was numerically higher as compared with group A ( 42. 9% vs. 23. 3. 0%, P=0. 068 ) , and similar with group B ( 42. 9% vs. 49. 3%, P=0.447). MACE occurred in 4 (13.3%), 5(6.7%) and 3(4.7%) patients in group A, B and C respictively ( P=0. 352). Bleeding events in group A and group C were both markedly lower in comparison to group B (3. 3% vs. 17. 3% vs. 1. 6%, P=0. 001). At the 24-month follow-up, the MACE-free survival rates were not significantly different (95. 3% vs. 93. 3% vs. 86. 7%, P=0. 146). Conclusions For elder patients with HPR, policosanol reduced platelet reactivity to a similar extent in comparison of high maintenance dose of clopidogrel without increasing bleeding risk.

Effects of octacosanol and triacontanol alcohols on ciclooxygenase and 5-lipoxygenase enzyme activities in vitro / Efecto sobre la actividad in vitro de las enzimas cicloxigenasa y 5-lipoxigenasa de los alcoholes octacosanol y el triacontanol

INTRODUCTION: policosanol, a mixture of eight primary aliphatic alcohols purified from sugar cane wax, contains octacosanol as major component. D-002, a mixture of six primary aliphatic alcohols purified from beeswax, presents triacontanol as the main component. Although both substances are high molecular weight alcohol mixtures, they have different compositions and pharmacological effects such as their distinct effects on arachidonic acid metabolism enzymes; whereas policosanol inhibits cyclooxygenase (COX)-1, D-002 inhibits COX and 5-lipoxygenase (5-LOX) activities. OBJECTIVE: to study the effects of octacosanol and triacontanol, which are main components of policosanol and D-002, respectively on the COX and the 5-LOX enzyme in vitro activities. METHODS: triacontanol and octacosanol were suspended in a Tween-20/H2O (2 %) (0.6-5000 g/mL) vehicle. The effects of adding these alcohols on COX-1, COX-2 and 5-LOX enzymes activities were assessed in rat platelet microsomes, rat seminal vesicle microsomes and rat polymorphonuclear (PMN) preparations, respectively. Indomethacin (0.4µg/mL) was used as reference inhibitor of COX-1 and COX-2, and Lyprinol as 5-LOX inhibitor. RESULTS: octacosanol showed significant, marked (70% with highest concentration) (IC50=143.54 g/mL) and dose-dependent (r=0.991, p <0.001) inhibitory action on COX-1 activity. However, Triacontanol did not affect COX-1, but inhibited significantly, depending on dose (r=0.985, p <0.001) the COX-2 activity to 50 % with 1250 g/mL. In contrast, octacosanol did not change COX-2 activity. Indomethacin inhibited both COX-1 and COX-2 by 83 %. Octacosanol addition was ineffective whereas triacontanol had significant, dose-dependent (r=0.978, p<0.001) and marked effect (79 %) on the 5-LOX activity (IC50=58.74 g/mL). Lyprinol inhibited 5-LOX by 89 %. The inhibitions induced by octacosanol and triacontanol were competitive. CONCLUSIONS: in vitro addition of octacosanol and triacontanol caused differential effects on COX-1, COX-2 and 5-LOX enzyme activities. Whereas octacosanol markedly inhibited COX-1 activity and did not change those of COX-2 and 5-LO, triacontanol markedly inhibited 5-LOX activity, but had moderate effect on COX-2 and did not change COX-1 activity.

INTRODUCCIÓN: el policosanol, mezcla de ocho alcoholes purificados de la cera de la caña de azúcar, contiene octacosanol como componente mayoritario. El D-002, mezcla de seis alcoholes alifáticos primarios purificada de la cera de abejas, presenta triacontanol como el componente mayoritario. Aunque ambas sustancias son mezclas de alcoholes de alto peso molecular, exhiben diferente composición y perfil farmacológico como son sus efectos sobre las enzimas del metabolismo del ácido araquidónico: mientras el policosanol inhibe la actividad de ciclooxigenasa (COX)-1, el D-002 inhibe las actividades de la COX y la 5-lipooxigenasa (5-LOX). OBJETIVO: investigar los efectos del octacosanol y el triacontanol, principales componentes del policosanol y el D-002, respectivamente, sobre las actividades de las enzimas COX y 5-LOX in vitro. MÉTODOS: el policosanol y el triacontanol se suspendieron en vehículo Tween-20/H2O (2 %) (0.6-5000g/mL). Los efectos de la adición de estos alcoholes sobre las actividades de las enzimas COX-1, COX-2 y 5-LOX se evaluaron en microsomas de plaquetas de ratas, microsomas de vesículas seminales de ratas y en preparaciones de polimorfonucleares (PMN) de ratas, respectivamente. Se utilizó indometacina (0.4 µg/mL) como inhibidor de referencia de COX-1 and COX-2 y Lyprinol como inhibidor de 5-LOX. RESULTADOS: la adición de octacosanol inhibió la actividad de COX-1 de modo significativo, marcado (70 % con la concentración mayor) (CI50=143.54 g/mL) y dependiente de la dosis (r=0.991, p <0.001). La adición de triacontanol, sin embargo, no afectó COX-1, pero inhibió de modo significativo y dependiente de la dosis (r=0.985, p <0.001) la actividad de la COX-2 hasta 50 % con 1250 g/mL. En contraste, el octacosanol no modificó la actividad de la COX-2. La indometacina inhibió COX-1 y COX-2 en un 83 %. Mientras la adición del octacosanol no fue efectiva, el triacontanol inhibió de modo significativo, dependiente de la dosis r=0.978, p <0.001) y marcadamente (79 %) la actividad de la 5-LOX (CI50=58.74 g/mL). El Lyprinol inhibió la 5-LOX en un 89 %. Las inhibiciones inducidas por el octacosanol y el triacontanol fueron competitivas. CONCLUSIONES: la adición in vitro de octacosanol y triacontanol produjo efectos diferenciales sobre las actividades enzimáticas de COX-1, COX-2 y 5-LOX. Mientras el octacosanol inhibió marcadamente la actividad de COX-1, sin afectar COX-2 y 5-LOX; el triacontanol inhibió marcadamente 5-LOX, pero moderadamente COX-2, y no cambió la actividad de COX-1.

Efectos del policosanol en la acción gastroprotectora del D-002 / Effects of policosanol on gastroprotective action of D-002

INTRODUCTION: policosanol, a mixture of higher aliphatic alcohols purified from sugar cane wax, is used to treat hypercholesterolemia. D-002 (Abexol), a mixture of higher aliphatic alcohols from beeswax, is an antioxidant supplement with gastroprotective effects. Then, concomitant intake of D-002 and policosanol may occur in routine practice, so potential pharmacological interactions between them should be researched on. OBJECTIVE: to find out the influence of policosanol on the gastroprotective effect of D-002 on the ethanol-induced gastric ulcer model. METHODS: rats were randomized into eight groups: one treated with the vehicle (control), two with D-002 (25 and 200 mg/kg), two with policosanol (25 and 200 mg/kg), two with the same doses of D-002 + policosanol and other with sucralfate (100 mg/kg). Treatments were given as single oral doses. One hour after treatment, rats received 60 percent ethanol orally and one hour later they were killed and their stomachs exposed. Effects on ulcer indexes (UI) were assessed. RESULTS: acute oral administration of D-002 (25 and 200 mg/kg) significantly reduced the ulcer indexes by 40 percent and 68 percent, respectively, as compared to the control group, and policosanol by 26 percent and 47 percent, respectively. The concomitant administration of the same doses of D-002 and policosanol significantly decreased ulcer indexes by 64 percent or ciento (both given at 25 mg/kg) and by 92 percent (both given at 200 mg/kg) as compared to the respective monotherapies. Sucralfate (100 mg/kg) significantly reduced ( 99 percent) ulcer indexes compared to the control group. CONCLUSIONS: the concomitant oral administration of policosanol with D-00 2 gives greater gastroprotection than D-002 monotherapy, so both products can be taken together(AU)

INTRODUCCIÓN: el policosanol, mezcla de alcoholes alifáticos de alto peso molecular obtenida de la cera de caña de azúcar (Saccharum officinarum L), se emplea en el tratamiento de la hipercolesterolemia. El D-002 (Abexol), mezcla de alcoholes alifáticos obtenida de la cera de abejas, es un suplemento antioxidante con efectos gastroprotectores. Así, el consumo concomitante de D-002 y policosanol puede ocurrir en la práctica rutinaria, por lo cual algunas interacciones entre ellos deben ser investigadas. OBJETIVO: determinar la influencia del policosanol sobre el efecto gastroprotector del D-002 en el modelo de úlcera gástrica inducida por etanol MÉTODOS: las ratas se distribuyeron en ocho grupos: uno tratado con el vehículo (control), dos con D-002 (25 y 200 mg/kg), dos con policosanol (25 y 200 mg/kg), dos con las mismas dosis de D-002 + policosanol, y otro con sucralfato (100 mg/kg). Los tratamientos se administraron como dosis únicas orales. Una hora después las ratas recibieron por vía oral etanol 60 por ciento y se sacrificaron; los estómagos se extrajeron y se cuantificó el índice de úlceras. RESULTADOS: la administración oral aguda de D-002 (25 y 200 mg/kg) redujo significativamente el índice de úlceras en un 40 por ciento y un 68 por ciento, respectivamente, con respecto al grupo control y el policosanol en un 26 por ciento y un 47 por ciento, respectivamente. La administración concomitante de D-002 y policosanol redujo significativamente el índice de úlceras en un 64 por ciento ambos administrados a 25 mg/kg) y un 92 por ciento (ambos administrados a 250 mg/kg) al compararse con las respectivas monoterapias. Sucralfato (100 mg/kg) redujo significativa y marcadamente ( 99 por ciento el índice de úlceras con respecto al grupo control. CONCLUSIONES: la administración oral concomitante de policosanol más D-002 confiere una gastroprotección mayor que las respectivas monoterapias, de modo que pueden ser administrados conjuntamente(AU)

Efecto in vitro del policosanol (alcoholes de la cera de Saccharum officinarum L) sobre la enzima 5-lipooxigenasa / In vitro effects of policosanol (Saccharum officinarum L wax alcohols) on the 5-lipooxygenase enzyme

INTRODUCTION: policosanol, a mixture of high molecular weight aliphatic alcohols purified from sugarcane with octacosanol as the main component, shows cholesterol-lowering and antiplatelet effects in addition to an inhibitory effect on type I cicloxygenase. OBJECTIVE: to determine whether policosanol may inhibit 5-LOX enzyme activity in vitro. METHODS: effects on 5-LOX enzyme activities were assessed in rat blood polymorphonuclear leukocytes. Vehicle or Policosanol suspensions (0.6 to 6 000 µg/mL) were added to tubes containing the reaction mix and then absorbance changes at 234 nm were measured. RESULTS: added Policosanol inhibited in vitro 5-LOX activity by 30 percent, which was not a significant figure but depended on the concentration(r= 0.992; p< 0.05); it was 1 250 µg/mL. CONCLUSIONS: policosanol did not significantly inhibit 5-LOX enzyme activity in rat PMNL preparations, so that it does not seem to be a dual inhibitor of COX and-LOX enzymes. This result differs from that found for beeswax alcohols and underlines the different effects of the mixtures of long-chain fatty alcohols purified from the sugarcane and the beeswax(AU).

IINTRODUCCIÓN: el policosanol es una mezcla de alcoholes alifáticos aislados y purificados de la caña de azúcar cuyo componente mayoritario es el octacosanol, con efecto sobre la reducción de colesterol y antiagregante plaquetario, además inhibe la ciclooxigenasa (COX) tipo 1. OBJETIVO: determinar el poder de inhibición del policosanol en la actividad de la enzima 5-LOX in vitro. MÉTODOS: el efecto sobre la actividad de la enzima 5-LOX se determinó en leucocitos polimorfonucleares obtenidos de sangre de ratas. Se añadieron vehículo o suspensiones de policosanol (0,6 a 6 000 µg/mL) a tubos que contenían la mezcla de reacción y se medió el cambio de absorbancia a 234 nm. RESULTADOS: la adición de policosanol inhibió in vitro la actividad de la 5-LOX en un 30 por ciento que no fue significativo pero sí dependiente de la concentración (r= 0,992; p< 0,05), inhibición esta que alcanzó 1 250 µg/mL. CONCLUSIÓN: el policosanol no inhibió significativamente la actividad de la enzima 5-LOX en preparación de polimorfonucleares de ratas, por lo que no es un inhibidor dual de las enzimas. Este resultado difiere del encontrado para los alcoholes de la cera de abeja y subraya la diferencia de los efectos hallados entre las mezclas de alcoholes alifáticos de cadenas largas purificados de la caña de azúcar y la cera de abeja(AU)

Efectos del policosanol en los modelos de pleuresía inducida por carragenina y granuloma por algodón / Effects of policosanol on carrageenan-induced pleurisy and cotton pellet granuloma models

Introducción: el policosanol, mezcla de alcoholes alifáticos primarios superiores purificada de la cera de caña, inhibe la actividad de la cicloxigenasa-1 (COX-1) in vitro, efecto que pudiera sustentar su acción antiagregante plaquetaria. Sin embargo, sus posibles efectos en modelos experimentales de inflamación no se habían investigado. Objetivo: determinar el efecto antinflamatorio in vivo del policosanol en un modelo de inflamación aguda (pleuresía por carragenina) y crónico (granuloma por algodón). Métodos: se distribuyeron las ratas Sprague Dawley en siete grupos para el modelo de inflamación aguda: un control negativo (vehículo) y seis a los que se les indujo la inflamación: un control positivo (vehículo), cuatro tratados con policosanol (50-800 mg/kg) y uno con aspirina (100 mg/kg). Se cuantificaron a las 5 h el volumen de exudado pleural, la concentración de proteínas y actividad de la enzima mieloperoxidasa. Se distribuyeron las ratas en seis grupos para el modelo crónico: un control (vehículo), cuatro tratados con policosanol (50-800 mg/kg) y uno con aspirina (100 mg/kg). Se extrajo el granuloma para determinar los pesos húmedo y seco seis días después de implantado el pellet. Resultados: dosis orales únicas de policosanol (200, 400 y 800 mg/kg) redujeron significativa y moderadamente el volumen, la actividad de la enzima mieloperoxidasa (¼ 12 por ciento) y la concentración de proteínas (¼ 20 por ciento) del exudado pleural, mientras la aspirina redujo estos indicadores en un 35,3, 19,9 y 19,1 por ciento, respectivamente. La administración oral de policosanol (400 y 800 mg/kg) durante 6 días disminuyó significativa y moderadamente el peso húmedo del granuloma (16,4 y 16,2 por ciento), y el peso seco (28,4 y 34,4 por ciento). La aspirina 100 mg/kg redujo estas variables en un 18,5 por ciento (peso húmedo) y 34,4 por ciento (peso seco). Ambos tratamientos produjeron mayores reducciones del peso seco que del peso húmedo del granuloma. Conclusiones: la administración oral de policosanol produjo un moderado efecto antinflamatorio in vivo en modelos de inflamación aguda y crónica(AU)

Introduction: policosanol, a mixture of higher aliphatic alcohols purified from sugarcane wax, inhibits cyclooxygenase-1 (COX-1) activity in vitro, an effect that could support its anti-platelet action. Its putative effects on experimental models of inflammation had not been yet investigated. Objective: to determine the in vivo effect of policosanol on acute (carrageenan-induced pleurisy) and chronic inflammation (cotton-pellet granuloma) in vivo models. Methods: in the acute model, rats were randomly distributed into seven groups: a negative vehicle control, and six with carrageenan-induced pleurisy: a positive control (vehicle), four treated with policosanol (50-800 mg/kg) and one with aspirin (100 mg/kg). Five hours later, volume of pleural exudate, protein concentration and myeloperoxidase activity were quantified. For the chronic model, rats were distributed into six groups: a control (vehicle), four treated with policosanol (50-800 mg/kg) and one group with aspirin (100 mg/kg). The cotton pellet was implanted and six days after treatment, it was extracted to determine the dry and the wet weights. Results: single oral doses of policosanol (200, 400 and 800 mg/kg) reduced significantly and moderately the volume (¼ 20 percent), the myeloperoxidase activity (¼ 12 percent) and the protein concentration (¼ 20 percent) in pleural exudates, whereas aspirin 100 mg/kg decreased significantly these indicators by 35.3, 19.9 and 19.1 percent, respectively. Oral administration of policosanol (400 and 800 mg/kg) for 6 days reduced significantly and moderately the wet (16.4 and 16.2 percent, respectively) and dry (28.4 and 34.4 percent, respectively) granuloma weights. Treatment with 100 mg/kg aspirin reduced these variables by 18.5 percent (wet weight) and 34.4 percent (dry weight), respectively. Both treatments reduced the dry more than the wet granuloma weight. Conclusion: oral administration of policosanol produced a moderate anti-inflammatory effect in vivo on models of acute and chronic inflammation(AU)

Efectos del policosanol, el extracto de semillas de uva y su terapia combinada sobre marcadores oxidativos en ratas / Effect of polycosanol, a grape seed extract and its combined therapy on oxidation markers in rats

El policosanol, mezcla de alcoholes alifáticos primarios superiores obtenida de la cera de caña de azúcar (Saccharum officinarum, L) y el extracto de semillas de uva (Vitis vinífera, L), producen efectos antioxidantes demostrados experimental y clínicamente. El objetivo del trabajo consistió en comparar los efectos del policosanol, el extracto de semilla de uva y su terapia combinada sobre marcadores oxidativos en plasma e hígado de ratas. Las ratas se distribuyeron en 4 grupos: un control y 3 tratados con policosanol, extracto de semilla de uva y su terapia combinada, respectivamente, todos a dosis de 25 mg/kg, durante 4 semanas. Las monoterapias redujeron significativamente las concentraciones plasmßticas de malondialdehído y de grupos carbonilos asociados a proteínas con respecto al control, lo que mostró similar eficacia. La terapia combinada redujo (p < 0,001) las concentraciones de malondialdehído màs efectivamente (p < 0,05) que cada una de las monoterapias, y también disminuyó (p < 0,01) las concentraciones de grupos carbonilos, pero no màs que las monoterapias. Cada monoterapia redujo las concentraciones de malondialdehído generadas por el sistema oxidante espontàneo en homogenato de hígado. El efecto de la terapia combinada fue mayor (p < 0,05) que el del extracto de semilla de uva, pero no que el del policosanol. En conclusión, las monoterapias orales con policosanol y extracto de semilla de uva, administradas durante 4 semanas, redujeron similarmente la peroxidación lipídica en plasma e hígado de ratas. La terapia combinada resultó más efectiva para inhibir la peroxidación lipídica en plasma que cada monoterapia por separado.

The Polycosanol, a mixture of superior primary aliphatic alcohols obteined from the sugarcane wax (Sacharum officinarum, L) and the grape seeds extract (Vitis vinífera, L) produces antioxidant effects experimentally and clinically demonstrated. The aim of present paper was to compare the effects of Polycosanol, the grape seed extract, and its combined therapy on oxidative markers in plasma and liver of rats. The rats were distributed into 4 groups: a control one and three treated with Polycosanol, grape seed extract and its combined therapy, respectively, using a 25 mg/kg dose over 4 weeks. The single-therapies significantly reduced the plasmatic concentrations of malonyldialdehyde and of proetin-associated carbonyl groups regarding the control, showing a similar efficacy. Combined therapy reduced in a more effective way (p < 0,001) the malonyldialdehyde concentrations of carbonyl groups, and also decreased (p < 0,01) the concentrations of carbonyl groups, but no more than the single-therapies. Each single-therapy reduced the malonyldialdehyde concentrations generated by spontaneous oxidant system in liver homogenate. The effect of combined therapy was higher (p < 0,05) than the grape seed extract, but no more than that of polycosanol. We concluded that oral single-therapies using polycosanol and grape seed extract, administered during 4 weeks, decreased in a similar way, the lipid peroxidation in plasma and liver of rats. Combined therapy was more effective to inhibits the lipid peroxidation in plasma than each single-therapy, separately.

Effects of policosanol on serum cholesterol levels in hyperlipidemia rats / 中国药理学与毒理学杂志

AIM To explore effects of policosanol on depressing cholesterol in hyperlipidemia rats and the correlated biochemistry mechanism. METHODS The rats were randomly divided into normal control, policosanol 4 mg·kg~(-1) prevention, hyperlipidemia model, policosanol 4, 6 and 8 mg·kg~(-1) and lovastatin positive control groups. The later 5 group rats were fed with high-cholesterol diets for 4 weeks in order to make hyperlipidemia model and beginning from the 5th week, in addition to the normal control and model groups, other groups were ig given policosanol or lovastatin once a day for 6 weeks, respectively, and policosanol protection group rats were ig given with policosanol 4 mg·kg~(-1) once a day for 10 weeks, together with high-cholesterol diets everyday. Total cholesterol(TC), triglycerides (TG), low density lipoprotein cholesterol (LDL-C) and high density lipoprotein cholesterol (HDL-C) concentrations in the serum and fecal bile acid (FBA) in the exrement were determined by auto-biochemistry analyzer. The activity of 3-hydroxy-3-methyl-glutaryl coenzyme A (HMG-CoA) reductase in hepatocellular microsomes was detected by ultraviolet spectrophotometric analysis and activity of low density lipoprotein receptor (LDL-R) in peripheral blood lymphocyte was detected by fluorescence labelled integrator method. RESULTS Compared with hyperlipemia model group, the levels of TC decreased (39.1%-46.4%), LDL-C decreased (66.6%-80.7%), and FBA increased (9.7%-19.0%), the activity of HMG-CoA reductase decreased （13.8%-23.6%）, and activity of LDL-R increased (27.5%-129.6%) in policosanol prevention, policosanol 4, 6 and 8 mg·kg~(-1) and lovastatin groups, respectively; HDL-C increased （12.2%-16.7%） in policosanol prevention and policosanol 8 mg·kg~(-1) groups; TG decreased in lovastatin group. CONCLUSION Policosanol has significant effects on decreasing cholesterol. The decreasing cholesterol mechanism should include: ① increasing FBA excretion; ② decreasing the activity of HMG-CoA reductase; ③ increasing activity of LDL-R.

Validación de un nuevo método analítico por CG con columna capilar para la determinación de alcoholes de alto peso molecular en policosanol ingrediente activo / Validation of a new capillary column GC analytical method for determining long chain fatty alcohols in policosanol active ingredient

El policosanol es una mezcla de 8 alcoholes alifáticos primarios (C24-C34), aislada y purificada a partir de la cera de la caña de azúcar (Saccharum officinarum L.), cuya eficacia como reductor del colesterol, tolerabilidad y seguridad han sido demostradas. Diversos métodos han sido previamente validados para determinar policosanol mediante cromatografía gaseosa (CG) con columna empacada. Sin embargo, las ventajas logradas con la CG capilar la hacen superior y mundialmente extendida en la actualidad respecto a las empacadas. Se desarrolló y validó un nuevo método por CG utilizando una columna capilar para determinar los alcoholes grasos que componen el policosanol ingrediente activo. Los alcoholes fueron analizados como derivados trimetilsil. Se comprobó que el método tuvo una buena linealidad (r2 = 0,9954, CVrespuesta=1,07%, CVpendiente=1,89% y el intervalo de confianza del intercepto incluyó el cero, por lo que no hubo sesgos) y exactitud (recobrado promedio = 100,45%) en todo el intervalo de concentración estudiado de 80-120%. También se demostró su selectividad con muestras sometidas a condiciones de estrés. La repetibilidad y precisión intermedia a la concentración nominal cumplieron los criterios de aceptación (< 2%). La robustez se evaluó mediante un diseño experimental intralaboratorio, en el cual se realizaron siete cambios operacionales, y no se encontraron efectos significativos sobre los resultados observados. El método fue exitosamente validado, y fue apropiado para el control de la calidad y para estudios de estabilidad de este ingrediente activo.

Policosanol is a mixture of 8 long chain primary aliphatic alcohols (C24-C34), isolated and purified from sugar cane (Saccharum officinarum L.) wax, wich cholesterol-lowering efficacy, safety and tolerability has been demonstrated. Several methods for determing policosanol by packed GC column have been previously validated. However, the advantages achieved with the capillary GC make it worldwide currently extended and overcome to the packed ones. A new gas chromatographic method using a capillary column was developed and validated for the determination of the fatty alcohols that compose policosanol active ingredient. The alcohols were analyzed as trimethylsilyl derivatives. Good linearity (r2 = 0,9954, CVresponse=1,07%, CVslope=1,89% and the confidence interval included the zero, then there was no bias) and accuracy (mean recovery = 100,45%) of the method were proven over a range of 80-120% of the nominal concentration. It was also proved its specificity even when samples were subject to stress conditions. Repeatablility and intermediate precision at the nominal 100% value fulfilled the acceptance criteria (< 2%). Ruggedness was evaluated through an intralaboratory experimental design, in which seven operational changes were made, and there was not found any effect on the observed results. The method was sussefully validated being suitable for the quality control process and the stability studies of this active ingredient.

Effect of policosanol on activity of LDL-R / 中国药理学通报

Aim To identify the effect of policosanol on LDL-R activity.Methods In vitro cell culture experiments conventional methods were used to observe the direct effect of policosanol on mononuclear cells LDL-R.In vivo experiments self-control and negative-control group design methods were used to observe the effect of policosanol on LDL-R activity in the patients with hypercholesterolemia.LDL-R activity was analysed by fluorescence flow cytometry and labeled by the fluorescent reagent DiI.Results Policosanol 5~20 mg?L-1 obviously activated the activity of LDL-R in human mononuclear cells,policosanol levels and the activity of LDL-R in human mononuclear cells showed significantly dose-effect relationship in vitro study.These tendency could also be seen in the patients with hypercholesterolemia after policosanol treatment for four weeks in vivo study.As the increasing of policosanol dose,the activity of LDL-R in human mononuclear cells remarkably increased in the patients with hypercholesterolemia Conclusions Policosanol up-regulates the activity of the LDL-R in the mononuclear cells and reduce cholesterol level in the body.Policosanol reduce lipids through multiple ways including LDL-R.

Clinical assessment of policosanol-a new vegetal drug for regulating serum lipid / 中国实用内科杂志

Policosanol is a new drug for regulating lipid,which can inhibit cholesterin synthesis and increase blood clearance of low-density lipoprotein(LDL).It has similar effect as statins and its clinical efficiency,safety and tolerance for special people such as the old and those with hepatopath have been confirmed by many clinical studies.Policosanol combined with statins or fibrates is also safe,which can be used as primary prevention for the patients with hypercholesterinemia,high low-density lipoprotein-cholesterolor low high-density lipoprotein-cholesterol and as secondary prevention for the patients who could not tolerate other lipid-regulating drugs.The long-term clinical effect of Policosanol on the risk factors of atherosclerosis need further researches.

Effects of Policosanol on Activity of Lipoprotein Metabolism Key Enzyme in Hyperlipoidemia Rats / 中国药房

OBJECTIVE:To investigate the regulation effects of policosanol on lowering cholesterol and its enzymatic mechanism.METHODS:The rats were randomly assigned into control group,policosanol prevention group (4.0 mg?kg-1?d-1),policosanol low-dose,medium-dose and high-dose groups (4.0 mg?kg-1?d-1,6.0 mg?kg-1?d-1,8.0 mg?kg-1?d-1),lovastatin group (positive control) and hyperlipoidemia model group.The last five groups were induced hyperlipoidemia model for 4 weeks.Blood samples were collected after 6 weeks administration (i.g.).The levels of TC,TG,LDL-C and HDL-C in the serum were determined.Body weight and liver weight were measured and hepatic index was calculated.The activity of lecithin cholesterol acyl transferase (LCAT) in serum,hepatic lipoprotein lipase (LPL) and hepatic lipase (HL) were detected.RESULTS:Policosanol remarkably decreased the levels of TC (ranged from 39.1% to 43.3%) and LDL-C (ranged from 66.6% to 80.7%) in serum and hepatic index (ranged from 11.1% to 11.8%) (P