In vitro Evaluation of the Calcification Inhibitory Properties of Policosanol, Genistein, and Vitamin D (Reduplaxin®) either Alone or in Combination.

INTRODUCTION: The process of vascular calcification has severe clinical consequences in a number of diseases, including diabetes, atherosclerosis, and end-stage renal disease. In the present study, we investigated the effect of policosanol (Poli), genistein (Gen), and vitamin D (VitD) separately and in association to evaluate the possible synergistic action on inorganic phosphate (Pi)-induced calcification of vascular smooth muscle cells (VSMCs). METHODS: Primary human VSMCs were cultured with either growth medium or growth medium supplemented with calcium and phosphorus (calcification medium) in combination with Poli, Gen, and VitD. Alizarin Red staining, mineralization, and the protein expression of RUNX2 and superoxide dismutase-2 (SOD2) were investigated. RESULTS: All three substances tested were effective at reducing osteogenic differentiation of VSMCs in a dose-dependent manner. Poli+Gen, Poli+VitD, Gen+VitD treatment induced a greater inhibition of calcification and RUNX2 expression compared to single compounds treatments. Moreover, the association of Poli+Gen+VitD (Reduplaxin®) was more effective at inhibiting VSMCs mineralization and preventing the increase in RUNX2 expression induced by calcification medium but not modified SOD2 expression. CONCLUSIONS: The association of Pol, Gen, and VitD (Reduplaxin®) has an additive inhibitory effect on the calcification process of VSMCs induced in vitro by a pro-calcifying medium.

Bioactives from Crude Rice Bran Oils Extracted Using Green Technology.

Crude rice bran oils from different rice cultivars and extraction methods bear different contents of nutraceuticals. The health benefits of lowering cholesterol activity of rice bran oil being confirmed by many reports are partly attributed to non-nutrient nutraceuticals, especially γ-oryzanol, phytosterols, and policosanols. As the world has been facing the global warming crisis, green extraction technology is gaining attention from many sectors. The current study aims to compare the nutraceutical composition with respect to γ-oryzanol, phytosterol, and policosanol content as well as the antioxidant properties of crude rice bran oils extracted from white and red rice bran using three green technologies, comparing with conventional hexane extraction. The data show that the traditional solvent extraction gave the highest oil yield percentage (26%), but it was not significantly different from subcritical liquefied dimethyl ether extraction (24.6%). Subcritical liquefied dimethyl ether extraction gave higher oil yield than supercritical CO2 extraction (15.5-16.2%). The crude rice bran oil extracted using subcritical liquefied dimethyl ether extraction produced the highest total phenolic contents and antioxidant activities. The highest γ-oryzanol content of the crude rice bran oil was found in oil extracted by conventional cold press (1370.43 mg/100 g). The γ-oryzanol content of the oil obtained via subcritical liquefied dimethyl ether extraction was high (1213.64 mg/100 g) compared with supercritical CO2 extraction. The red rice bran yielded the crude rice bran oil with the highest total phytosterol content compared with the white bran, and the oil from red rice bran extracted with subcritical liquefied dimethyl ether generated the highest total phytosterol content (1784.17 mg/100 g). The highest policosanol content (274.40 mg/100 g) was also found in oil obtained via subcritical liquefied dimethyl ether extraction.

Recapsoma®: A Novel Mixture Based on Bergamot, Ipomoea Batatas, Policosanol Extracts and Liposomal Berberine for the Treatment of Hypercholesterolemia.

Cardiovascular disease (CVD) is considered one of the major causes of mortality worldwide. Epidemiological studies have shown that regular consumption of phenols is inversely associated with cardiovascular disease, and the use of nutraceuticals and functional foods can provide protective, preventive, and possibly curative effects in CVD. A novel mixture of different natural substances named Recapsoma® (bergamot, liposomal berberine, Ipomoea batatas, oleuropein, polycosanols, and vitamin E) has been produced, and its anti-dyslipidaemic efficacy has been tested, specifically studying the in vitro effects on the mechanisms of action underlying cholesterol synthesis, triglycerides, and LDL-cholesterol oxidation. The work has demonstrated the ability of this herbal extract mixture to inhibit the action of PCSK, ACAT, PAP, and HMGR and to increase the LDL receptor (LDLR), underlying the synergistic effect of the mixture over the single components. Such results suggest that the Recapsoma® mixture could be used as a tool for controlling hypercholesterolemia, and an alternative to statins, especially for those patients with metabolic syndrome.

Oral supplementation of policosanol alleviates carbon tetrachloride-induced liver fibrosis in rats.

Liver fibrosis is a prevalent liver disease that requires rapid and effective treatment prior to its progression to cirrhosis and liver damage. Recently, several reports have investigated the efficacy of phytotherapy using natural herbal extracts rather than synthetic drugs to treat several liver diseases. Policosanol is a herbal extract used to treat patients with cardiovascular. However, its therapeutic effect on liver fibrosis is still unknown. Therefore, the present study aimed to assess the potential antifibrotic effect of policosanol compared to silymarin and the possible underlying molecular mechanisms. Rats were categorized into four groups; negative control group "NCG", the fibrotic group "FG", silymarin treated group "STG", and policosanol treated group "PTG". Serum liver enzymes, oxidative stress markers, angiogenic growth factors, and pro-inflammatory cytokines were measured biochemically. The relative mRNA expressions of liver caspase-3 and alpha-smooth muscle actin (α-SMA) were assessed. Immunohistochemical staining was carried out using anti- α-SMA, and anti-caspase-3 antibodies. Compared to NCG, the FG group demonstrated a significant decrease in the level of serum liver enzymes "GSH, TAC, and SDF. Nevertheless, it demonstrateda significant increase in the level of pro-inflammatory cytokines "Il-6, TNF"; oxidative stress markers "NO, MDA", and angiogenic growth factors "VEGF and PDGF" and the expression of α-SMA, and Caspase-3. Interestingly, the values of these measurements were restored to normal levels in the treated groups, particularly the PTG. In conclusion, our data revealed the beneficial effects of co-administration of policosanol or silymarin on the fibrotic liver rat model and thus could be a promising natural therapeutic drug.

Effect of policosanol from insect wax on amyloid ß-peptide-induced toxicity in a transgenic Caenorhabditis elegans model of Alzheimer's disease.

BACKGROUND: Alzheimer's disease (AD), an age-related neurodegenerative disorder and a serious public health concern, is mainly caused by ß-amyloid (Aß)-induced toxicity. Currently, a limited number of drugs are effective against AD, and only a few are used for its treatment. According to traditional Chinese medicine, white wax is mainly composed of policosanol, hexacosanol, and octacosanol. Policosanol has been shown to reduce lipid levels in blood and alleviate the symptoms associated with diabetic complications and neurodegenerative disorders, such as Parkinson's disease and AD. However, the efficacy of policosanol depends on the purity and composition of the preparation, and the therapeutic efficacy of policosanol derived from insect wax (PIW) in AD is unknown. METHODS: Here, we identified the main components of PIW and investigated the effects of PIW on Aß-induced toxicity and life-span in a transgenic Caenorhabditis elegans model of AD, CL4176. Furthermore, we estimated the expression of amyloid precursor-like protein (apl-1) and the genes involved in various pathways associated with longevity and alleviation of AD-related symptoms in PIW-fed CL4176. RESULTS: PIW mainly consists of tetracosanol, hexacosanol, octacosanol, and triacontanol; it could decrease the Aß-induced paralysis rate from 86.87 to 66.97% (P < 0.01) and extend the life-span from 6.2 d to 7.8 d (P < 0.001) in CL4176 worms. Furthermore, PIW downregulated apl-1, a gene known to be associated with the levels of Aß deposits in C. elegans. Additionally, our results showed that PIW modulated the expression of genes associated with longevity-related pathways such as heat shock response, anti-oxidative stress, and glutamine cysteine synthetase. CONCLUSION: Our findings suggest that PIW may be a potential therapeutic agent for the prevention and treatment of AD. However, its effects on murine models and patients with AD need to be explored further.

Nanoemulsification of Rice Bran Wax Policosanol Enhances Its Cardio-protective Effects via Modulation of Hepatic Peroxisome Proliferator-activated Receptor gamma in Hyperlipidemic Rats.

Policosanol, a mixture of long-chain alcohols found in animal and plant waxes, has several biological effects including lipid-lowering that have been extensively studied. However, its bioavailability is low. To investigate the effect of nanoemulsified rice bran wax policosanol (NPOL) on plasma homocysteine, heart and liver histology in hyperlipidemic rats, high-fat diet containing 2.5% cholesterol was used to induce hyperlipidemia in Sprague Dawley rats. The hyperlipidemic rats were treated with NPOL and rice bran wax policosanol (POL) in comparison with normal diet (ND), high-cholesterol diet (HCD) and simvastatin-treated rats. Plasma homocysteine, heart and liver histology, and hepatic mRNA expression of peroxisome proliferator-activated receptor gamma (PPARG) were evaluated. The NPOL group, similar to the simvastatin group, showed reduced plasma homocysteine, preserved heart and liver histology, and down-regulated hepatic PPARG mRNA in comparison to the control group, and was better than the POL group. The results suggest that the modest effect of NPOL on homocysteine and preservation of heart and liver histology could be through the regulation of PPARG expression on a background of increased assimilation of rice bran wax policosanol.

Policosanol profiles and adenosine 5'-monophosphate-activated protein kinase (AMPK) activation potential of Korean wheat seedling extracts according to cultivar and growth time.

Policosanols is a health promoting aliphatic alcohol known as lipid-lowing agent. To enable maximising the functional properties of wheat, this research investigates the policosanol profiles and adenosine 5'-monophosphate-activated protein kinase (AMPK) activation potential of Korean wheat seedlings according to cultivars and growth times. GC-MS revealed six policosanols that differed markedly in content between 17 cultivars, especially, octacosanol (8) showed the most predominant component (49-83%), varying significantly in average concentrations with growth times as 361.4 (3 days) â†’ 613.0 (6 days) â†’ 203.1 (9 days) â†’ 196.5 (12 days) â†’ 50.9 mg/100 g (19 days). The highest average policosanol (738.7 mg/100 g) exhibited after 6 days, while the lowest was 104.4 mg/100 g on 19 days. Moreover, the wheat cultivars including Shinmichal 1, Anbaek, Namhae, and Joah at 6 days may be recommended as potential sources because of high policosanols (921.7-990.6 mg/100 g). Western blot analysis revealed markedly higher AMPK activation in cells treated with the hexane extracts (150-370% at 100 µg/ml) and octacosanol (8) possessed potent AMPK activator (control; 100 â†’ 280% at 200 µg/ml). It is confirmed that the AMPK activation by wheat seedlings are positively related to the highest policosanol content at the 6 days of growth time, independent of the cultivar. Our results may be contributed to enhance the wheat value regarding development of new cultivars and functional foods.

Policosanol Attenuates Cholesterol Synthesis via AMPK Activation in Hypercholesterolemic Rats.

This study was carried out to investigate the effects of policosanol on high-fat and high-cholesterol diet-induced hypercholesterolemic rats to provide strong evidence in support of its hypocholesterolemic effect. The hypercholesterolemic rats showed elevations in liver weight, total triglycerides, total cholesterol, and low-density lipoprotein (LDL) cholesterol in serum; however, policosanol supplementation reduced these markers significantly. In addition, we found that policosanol supplementation stimulated an increase in fecal cholesterol and bile acid contents and deactivated 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase by AMP-activated protein kinase (AMPK) phosphorylation during high-fat and high-cholesterol-containing diet-induced development of hypercholesterolemia. Policosanol supplementation decreased ApoB levels and increased LDL-receptor expression, but it did not affect the hepatic ACAT2 level in livers from hypercholesterolemic rats. Moreover, supplementation with policosanol significantly decreased aortic wall thickness and levels of P-selectin and soluble vascular cell adhesion molecule (sVCAM-1) in serum. In conclusion, we suggest that policosanol supplementation induces antihypercholesterolemia by inhibiting cholesterol biosynthesis, LDL cholesterol uptake, and cholesterol excretion.

Policosanol supplementation significantly improves blood pressure among adults: A systematic review and meta-analysis of randomized controlled trials.

BACKGROUND AND AIMS: Policosanol contains a mixture of concentrated primary aliphatic alcohols extracted from sugar cane wax and is recognized as a cholesterol-lowering drug but previous studies reported that it could be helpful for reducing blood pressure as well. We aimed to systematically review all randomized control trials (RCTs) evaluating the efficacy of policosanol supplementation for lowering high blood pressure. METHODS AND RESULTS: The following databases were searched up to March 2019: PubMed, Scopus, ISI Web of Science and the Cochrane library. Eligible RCTs were included if they investigate the effects of policosanol supplementation on systolic (SBP) and diastolic (DBP) blood pressure. Pooled effect size was measured using random effect model (DerSimmonon method). A total of nineteen studies with twenty-four arms were considered. Pooled effect size showed that SBP (WMD: -3.423 mmHg, 95% CI: -5.315, -1.531; p < 0.001) and DBP (WMD: -1.468 mmHg 95% CI: -2.632, -0.304, p = 0.013). decrease significantly after policosanol supplementation with significant heterogeneity among included studies (I2 = 78.5% and 78.9% for SBP and DBP respectively). All subgroups showed a significant effect of policosanol supplementation except patients with mixed dyslipidemia for SBP and DBP and overweight subjects for DBP. CONCLUSION: Policosanol could lower SBP and DBP significantly; future long term studies are required to confirm these findings in the general population.

Policosanol composition, antioxidant and anti-arthritic activities of milk thistle (Silybium marianum L.) oil at different seed maturity stages.

BACKGROUND: Several anti-arthritic drugs and synthetic antioxidants have wide pharmaceutical uses and are often associated with various side effects on the human health. Dietary seed oils and their minor components like policosanol may offer an effective alternative treatment for arthritic and oxidative-stress related diseases. The biological effects of seed oils were affected by different parameters such as the stage of seed maturity. Hence, this study seeks to determine the policosanol content, antioxidant and anti-arthritic activities of milk thistle (Silybium marianum L.) oil extracted at various stages of seed maturation. METHODS: Milk thistle oil samples were extracted from seeds collected at three maturation stages (immature, intermediate, and mature). The 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethyl-benzthiazoline-6-sulfonic acid) (ABTS) radical scavenging assays were used to determine the antioxidant activity of the extracted oils. The anti-arthritic activity of oil samples was evaluated with bovine serum protein denaturation and egg albumin denaturation methods. Gas chromatography coupled to mass spectrometry (GC-MS) was employed to determine the policosanol profile. RESULTS: Policosanol profile, antioxidant and anti-arthritic activities of milk thistle oil were influenced by the seed maturity stages. The oil extracted from the immature seeds had the highest total policosanol content (987.68 mg/kg of oil) and displayed the maximum antiradical activity (96.42% and 90.35% for DPPH test and ABTS assay, respectively). Nine aliphatic alcohols were identified in the milk thistle oil. The dominant poliosanol in the mature seed oil was octacosanol (75.44%), while triacontanol was the major compound (40.25%) in the immature seed oil. Additionally, the maximum inhibition of bovine serum protein denaturation (92.53%) and egg albumin denaturation (86.36%) were observed in immature seed oil as compared to mature seed oil. A high correlation was found between the total policosanol content, anti-arthritic activity and antioxidant capacity of oil. CONCLUSIONS: The milk thistle oil exhibited a potential anti-arthritic and antioxidant activities and that it might contribute to the protection of humans from a variety of diseases like rheumatoid arthritis. Also, it could serve as natural antioxidant and anti-arthritic agents for application in the food industries and pharmaceutic. Policosanol level in the seed oils might contribute to their anti-arthritic and antioxidant activities.

Hair growth promoting effect of white wax and policosanol from white wax on the mouse model of testosterone-induced hair loss.

White wax (WW) has been traditionally used to treat hair loss in China. However there has been no reporter WW and its extract responsible for hair growth-promoting effect on androgenetic alopecia. In this paper, we examined the hair growth-promoting effects of WW and policosanol of white wax (WWP) on model animal of androgenetic alopecia and the potential target cell of WW and WWP. WW (1, 10 and 20%) and WWP (0.5, 1 and 2%) were applied topically to the backs of mice. Finasteride (2%) was applied topically as a positive control. MTS assays were performed to evaluate cell proliferation in culture human follicle dermal papilla cells (HFDPCs). The inhibition of WW and WWP for 5α- reductase were tested in Vitro. Results showed more lost hairs were clearly seen in mice treated with TP only and TP plus vehicle. Mice which received TP plus WW and WWP showed less hair loss. WW and WWP showed an outstanding hair growth-promoting activity as reflected by the follicular length, follicular density, A/T ratio, and hair bulb diameter. The optimal treatment effect was observed at 10% WW and 1% WWP, which were better than 2% finasteride treatment. MTS assay results suggested that WW and WWP remarkably increased the proliferation of HFDPCs. Inhibitor assay of 5α- reductase showed that WW and WWP inhibited significantly the conversion of testosterone to dihydrotesterone, and the IC50 values of WW and WWP were higher than that of finasteride. In Conclusion, WW and WWP could act against testosterone-induced alopecia in mice, and they promoted hair growth by inhibiting 5α-reductase activity and HFDPCs proliferation. DPCs is the target cell of WW and WWP.

Joint position statement on "Nutraceuticals for the treatment of hypercholesterolemia" of the Italian Society of Diabetology (SID) and of the Italian Society for the Study of Arteriosclerosis (SISA).

AIM: Evidence showed that LDL-cholesterol lowering is associated with a significant cardiovascular risk reduction. The initial therapeutic approach to hypercholesterolemia includes dietary modifications but the compliance to recommendations is often inadequate. Some dietary components with potential cholesterol-lowering activity are present in small amounts in food. Therefore, in recent years the use of "nutraceuticals" (i.e., nutrients and/or bioactive compounds with potential beneficial effects on human health) has become widespread. Such substances may be added to foods and beverages, or taken as dietary supplements (liquid preparations, tablets, capsules). In the present manuscript, the cholesterol-lowering activity of some nutraceuticals (i.e. fiber, phytosterols, soy, policosanol, red yeast rice and berberine) will be discussed along with: 1) the level of evidence on the cholesterol-lowering efficacy emerging from clinical trial; 2) the possible side effects associated with their use; 3) the categories of patients who could benefit from their use. DATA SYNTHESIS: Based on the current literature, the cholesterol-lowering effect of fiber, phytosterols and red yeast rice is consistent and supported by a good level of evidence. Over berberine, there is sufficient evidence showing significant cholesterol-lowering effects, although the results come from studies carried out almost exclusively in Asian populations. Data on the effects of soy are conflicting and, therefore, the strength of recommendation is quite low. The evidence on policosanol is inconclusive. CONCLUSION: Although health benefits may arise from the use of nutraceuticals with cholesterol-lowering activity, their use might be also associated with possible risks and pitfalls, some of which are common to all nutraceuticals whereas others are related to specific nutraceuticals.

The effects of intermolecular interactions on the physical properties of organogels in edible oils.

The microstructure of organogels based on monoglycerides of fatty acids (MAGs) and policosanol and on different edible oils was investigated by using different techniques (calorimetry, nuclear magnetic resonance, infrared spectroscopy, rheology, polarized light microscopy) towards a better understanding and control of the oil gelation phenomena. Dynamic moduli were related via a fractal model to microstructural information such as solid content and fractal dimension. Infrared spectroscopy evidenced that network structure in MAGs gel is mainly due to hydrogen bonding, whereas in policosanol system is mainly given by van der Waals interactions. Because of the different relative contribution of molecular interactions, the investigated organogelators exhibit a distinguished macroscopic behavior. MAGs are sensitive to the utilized oil and structuration occurs quickly, even though at a temperature lower than policosanol. Policosanol organogels exhibit a behavior independent of the used oil and a slower gelation rate, as a result of the weaker van der Waals interactions. Nevertheless, at lower concentration a stronger final gel is obtained, probably due to of the large number of interactions arising among the long alkyl chains of the fatty alcohols. Obtained results evidenced that policosanol is very effective in gelation of different oils and seems promising for potential commercial uses.

Policosanol as a new inhibitor candidate for vascular calcification in diabetic hyperlipidemic rats.

This work mainly aimed to investigate the probable changes of aortic calcification by policosanol, omega-3 fatty acids in comparison with atorvastatin and subsequent progression of atherosclerosis in diabetic hyperlipemic rat model. Adult male albino rats of wistar strain (30) were divided into five groups (n = 6/group); one was fed normal diet and was used as a normal group, the other groups received alloxan, atherogenic diet (CCT - rat chow diet supplemented with 4% cholesterol, 1% cholic acid, and 0.5% thiouracil) and categorized as follows: the second group received no treatment and kept as control (diabetic hyperlipidemic control group (DHC)). The other groups received daily oral doses of atorvastatin, policosanol (10 mg/kg body weight) and ω-3 (50 mg/kg body weight), respectively, for eight weeks. Different biomarkers were used for the evaluation that included inflammatory (C reactive protein (CRP), tumor necrosis factor α (TNF-α)), oxidative stress (glutathione (GSH), malondialdehyde (MDA)) bone calcification markers (alkaline phosphatase (ALP), Vitamin D, parathyroid hormone (PTH)), lipogram pattern in addition to histochemical demonstration of calcium in the aorta. Diabetic hyperlipemic group demonstrated significant hyperglycemia, hyperlipidemia, and increased inflammation, oxidative stress, calcification, and finally atherogenesis progression. Treatment of diabetic hyperlipemic rats with, policosanol, omega-3 fatty acids (natural products) and atorvastatin for eight weeks significantly increased high-density lipoprotein cholesterol (HDL-C), Vitamin D, decreased aortic vacuoles number, and inhibited calcification process. Policosanol induced more remarkable reduction in the density and number of foam cells and improved the intimal lesions of the aorta as compared to atorvastatin. Drugs under study exerted hypoglycemic effect along with an inhibition of inflammation, oxidative stress, and calcium deposition with certain variations but policosanol effect was remarkable in comparison with other drugs.

Effects of a nutraceutical combination containing berberine (BRB), policosanol, and red yeast rice (RYR), on lipid profile in hypercholesterolemic patients: A meta-analysis of randomised controlled trials.

BACKGROUND AND AIM: A nutraceutical combination containing berberine, policosanol, and red yeast rice, largely marketed in Europe (Armolipid Plus(®)) (AP), has been reported to induce significant improvements in plasma lipids, insulin resistance and other components of the metabolic syndrome. However, literature study designs and results were heterogeneous and it was thus necessary to systematically review and meta-analyse all relevant randomised clinical trials (RCTs) to explore and quantify the effects of the dietary supplement AP on lipid profile. The aim of our meta-analysis was the evaluation of the effect of AP on lipid profile. METHODS AND RESULTS: We conducted a structures search on PubMed and Google Scholar to identify eligible articles published prior to 2015. Eleven RCTs were subjected to meta-analysis by means of random effects models using the Standardised Mean Differences approach (Hedges' method) and the Mean Differences approach as a sensitivity analysis. Data from 11 randomised clinical trials, corresponding to 1970 nutraceutical combination and 1954 control patients (3924 total patients), were included after the peer evaluation and data extraction of two independent evaluators. Heterogeneity was significant in all models. A significant effect was found for all lipid parameters. The effect size (relative change from baseline (%)) was -1.3 (9.9%) for total cholesterol, -1.17 (-13.7%) for LDL-c, +0.17 (+3.7%) for HDL-c and -0.24 (-7.0%) for Triglycerides. CONCLUSION: This meta-analysis confirms that the nutraceutical combination containing berberine, policosanol, and red yeast rice has shown to be an effective product for the improvement of the lipid profile.

Triacylglycerols and aliphatic alcohols from fruits of three Tunisian Pistacia lentiscus populations.

BACKGROUND: The search for other sources of vegetable oils by the exploitation and the enhancement of other oil plants will be needed to meet the demands of the international market. This study aims to determine the triacylglycerol (TAG) molecular species and aliphatic alcohol compositions of unexploited fruits of three Tunisian Pistacia lentiscus (lentisc) populations from the Korbous, Tebaba and Rimel areas of Tunisia. RESULTS: Results show that the content of total TAG varies from 738.32 mg g(-1) of total lipid in the Tebaba population to 981.15 mg g(-1) of total lipid in the Korbous population. Furthermore, 14 species of TAG were detected in the three studied populations. In addition, 13 aliphatic compounds were identified and classified into two groups: (1) aliphatic alcohols with fewer than 20 carbon atoms (hexadecanol, heptadecanol, (Z)-octadec-9-en-1-ol, octadecanol and nonadécanol); and (2) the policosanol group (eicosenol, docosenol, docosanol tetracosanol, hexacosanol octacosanol and triacontanol). The Tebaba population showed a distinct composition compared to Korbous and Rimel where heptadecanol is the major compound. CONCLUSION: Quantitatively, the most abundant TAG species are those constituted by palmitic, oleic and/or linoleic acid. Furthermore, the significant difference observed at the oil composition is associated with a remarkable station effect.

Characterization of rice bran wax policosanol and its nanoemulsion formulation.

Policosanol, a mixture of long-chain alcohols found in animal and plant waxes, has several biological effects; however, it has a bioavailability of less than 10%. Therefore, there is a need to improve its bioavailability, and one of the ways of doing this is by nanoemulsion formulation. Different droplet size distributions are usually achieved when emulsions are formed, which solely depends on the preparation method used. Mostly, emulsions are intended for better delivery with maintenance of the characteristics and properties of the leading components. In this study, policosanol was extracted from rice bran wax, its composition was determined by gas chromatography mass spectrophotometry, nanoemulsion was made, and the physical stability characteristics were determined. The results showed that policosanol nanoemulsion has a nanosize particle distribution below 100 nm (92.56-94.52 nm), with optimum charge distribution (-55.8 to -45.12 mV), pH (6.79-6.92) and refractive index (1.50); these were monitored and found to be stable for 8 weeks. The stability of policosanol nanoemulsion confers the potential to withstand long storage times.

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

Introducción: 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)

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)

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)

Long-chain fatty alcohols from evening primrose oil inhibit the inflammatory response in murine peritoneal macrophages.

ETHNOPHARMACOLOGICAL RELEVANCE: Evening primrose (Oenothera biennis L., Onagraceae) is a wild medicinal plant of Central American origin that is now one of the most widely used herbal medicines in different parts of the world. Oil extracted from it seeds is traditionally used in the treatment of eczema, asthma, rheumatoid arthritis, breast problem, premenstrual and menopausal syndrome, all they have an inflammatory component. The present study demonstrates the in vitro anti-inflammatory effect of long-chain fatty alcohols, minor compounds isolated from Evening primrose oil (EPO). MATERIAL AND METHODS: A mixture of long chain fatty alcohols (LCFAs) was isolated from the non-triacylglycerol fraction of the EPO. Hexacosanol (C26OH: 38.65%), tetracosanol (C24OH: 31.59%), docosanol (C22OH: 11.36%) and octocosanol (C28OH: 7.64%), were the major constituents, identified and quantified by GC and GC-MS. LCFA was tested with LPS stimulated murine peritoneal macrophage. This fraction, significantly and dose-dependently decreased nitric oxide production induced by LPS (P<0.001) and the inhibitory effect seems to be consequence of an action at the level of the inducible nitric-oxide synthethase (iNOS) gene enzyme expression rather than to a direct inhibitory action on enzyme activity. The release of PLA2 and TXB2 also was significantly inhibited by LCFAs (P<0.001) although LCFAs did not affect to PGE2 generation, however the western blot assay showed that LCFAs reduced cyclooxygenase-2 enzyme gene expression at all doses assayed. In the same way, the secretion of inflammatory cytokines interleukin 1ß (IL-1ß) and tumour necrosis factor α (TNF-α) from LPS-stimulated murine macrophage, were also significantly reduced (P<0.001). CONCLUSION: These results demonstrates the anti-inflammatory activity of LCFAs, providing an additional value about the role of bioactive minor compounds in the beneficial effect of EPO and supports its traditional uses in inflammatory processes management.