Efecto a largo plazo del policosanol en la recuperación funcional de pacientes con ictus isquémico no cardioembólico: estudio de un año / Long-term eff ect of policosanol on the functional recovery of non-cardioembolic ischemic stroke patients: a one year study

Introducción. El ictus es una causa principal de mortalidad y discapacidad. El policosanol ha sido efi caz en modelos de isquemia cerebral. Este estudio investiga si el tratamiento a largo plazo con policosanol, añadido a la terapia con ácido acetilsalicílico (AAS), dentro de los 30 días posteriores a un ictus, es mejor que el placebo + AAS en la recuperación de los pacientes. Pacientes y métodos. Estudio aleatorizado, doble ciego, controlado con placebo. Se incluyeron 80 pacientes (edad media: 69 años) que sufrieron un ictus en los 30 días previos y con una puntuación de 2-4 en la escala de Rankin modifi cada(mRS). Se distribuyeron aleatoriamente en dos grupos y recibieron policosanol + AAS o placebo + AAS durante 12 meses. Resultados. El tratamiento con policosanol + AAS disminuyó signifi cativamente la puntuación en la mRS desde el primer control intermedio (1,5 meses). El efecto del tratamiento incluso mejoró con la terapia a largo plazo. El número de pacientes que alcanzaron valores de mRS menores o iguales a 1 fue superior en el grupo de policosanol + AAS (87,5%) que en el de placebo + AAS (0%). El tratamiento con policosanol + AAS aumentó signifi cativamente el índice de Barthel, disminuyó el colesterol LDL y aumentó el colesterol HDL frente a placebo + AAS. Conclusiones. El tratamiento a largo plazo (12 meses) con policosanol + AAS fue más efectivo que el tratamiento con placebo + AAS en la recuperación funcional de los pacientes después de sufrir un ictus isquémico no cardioembólico de moderada gravedad (AU)

Introduction. Stroke is a leading cause of mortality and disability. Policosanol has been eff ective in brain ischemia models. The aim of this study is to investigate whether policosanol, added to aspirin therapy within 30 days of stroke onset, is better than placebo + aspirine for the long-term recovery of non-cardioembolic ischemic stroke subjects. Patients and methods. Randomized, double-blind, placebo-controlled study. Eighty patients (mean age: 69 years) within 30 days of onset, with a modifi ed Rankin Scale score (mRS) 2 to 4, were included. They were randomized in two groups (policosanol + aspirine or placebo + aspirine) for 12 months. Results. Policosanol + aspirine decreased signifi cantly mean mRS from the fi rst interim check-up (1.5 months). The treatment even improved after long-term therapy. More policosanol + aspirin (87.5%) than placebo + aspirine (0%) patients achieved mRSs ≤ 1. Policosanol + aspirine increased signifi cantly Barthel Index, lowered LDL-cholesterol and increased HDL-cholesterol versus placebo + aspirin. Conclusions. Long-term (12 months) administration of policosanol + aspirin given after suff ering non-cardioembolic ischemic stroke was shown to be better than placebo + aspirin in improving functional outcomes when used among patients with non-cardioembolic ischemic stroke of moderate severity (AU)

Effects of D-002, a mixture of high molecular weight beeswax alcohols, on patients with nonalcoholic fatty liver disease.

BACKGROUND/AIMS: Nonalcoholic fatty liver disease (NAFLD) is intimately related to insulin resistance and ranges from a benign course to liver fibrosis and cirrhosis. NAFLD management mainly involves dietary modification and weight loss. Although no fully successful pharmacological intervention is available, alternative therapies to treat NAFLD have shown promising results. Experimental studies have shown that D-002, a mixture of beeswax alcohols with antioxidant effects, is hepatoprotective. The aim of this study was to investigate the efficacy and safety of D-002 in patients with NALFD. METHODS: Fifty patients with NAFLD were randomized to receive a placebo or D-002 (100 mg/day) for 24 weeks. The primary endpoint was a significant ultrasonography-detected reduction of liver fat infiltration versus a placebo. Secondary endpoints were decreases in the homeostatic model assessment (HOMA) index, insulin levels, serum liver enzymes, increases in plasma total antioxidant status (TAS) and improved clinical symptoms versus the placebo recipients. RESULTS: At randomization, all indicators were comparable in both groups. At study completion, seven (28.0%) D-002-patients, but none of the placebo recipients, exhibited a normal liver echo pattern on ultrasonography (p < 0.01). Also, D-002 significantly reduced (p < 0.01 vs. baseline and placebo) the HOMA index and insulin levels and increased the TAS, but did not affect other parameters. The proportion of D-002-patients (12/25, 48.0%) showing symptom improvement was higher (p < 0.001) than that of the placebo group (1/25, 4.0%). The treatment was safe and well tolerated. Three patients in each group withdrew from the study. CONCLUSIONS: D-002 (100 mg/day) improved ultrasonographic findings, indicators of insulin resistance, plasma TAS and clinical evolution on NAFLD patients. Further studies, however, are needed to confirm these results.

Evaluation of anti-inflammatory and antinociceptive effects of D-002 (beeswax alcohols).

D-002, a mixture of six higher aliphatic alcohols purified from beeswax, displayed anti-inflammatory effects in carrageenan-induced pleurisy and cotton pellet granuloma in rats. The aim of the present study was to confirm the anti-inflammatory properties of D-002 and to explore its potential analgesic effects. Xylene-induced mouse ear oedema was used to assess the anti-inflammatory effect, acetic acid-induced writhing and hot plate responses for the analgesic activity, and the open field and horizontal rotarod tests for motor performance. For anti-inflammatory tests, mice were randomised into a negative vehicle control and five xylene-treated groups: the vehicle, D-002 (25, 50 and 200 mg/kg) and indomethacin 1 mg/kg (reference drug). Treatments were given for 15 days. Effects on oedema formation and myeloperoxidase (MPO) activity were tested. For analgesia and motor performance tests, mice were randomised into a vehicle control and D-002-treated groups (25, 50 and 200 mg/kg). Two sets of experiments were done, which included acute and repeat (15 days) dosing. D-002 (25, 50 and 200 mg/kg) significantly decreased xylene-induced ear oedema (44.7, 60.8 and 76.4%, respectively) and the increase of MPO activity induced by xylene (38.0, 47.0 and 57.0%, respectively), while indomethacin significantly inhibited xylene-induced oedema (59.9%) and MPO activity (57.5%). Single and repeat doses of D-002 (25, 50 and 200 mg/kg) decreased the acetic acid-induced writhing responses by 21.2, 28.2 and 40.1%, for the single doses; 25.2, 35.1 and 43.2%, respectively, for the repeat doses, but did not affect the hot plate, open field and rotarod behaviours. Aspirin 100 mg/kg significantly decreased acetic acid-induced abdominal constrictions and morphine (5 mg/kg) significantly increased the latency of the hot plate response. This study confirmed the anti-inflammatory effects of D-002 and demonstrated its analgesic effects on the acetic acid-induced writhing, but not on the hot plate response, which suggests that the antinociceptive effects of D-002 could be related to its anti-inflammatory activity.

Antioxidant effects of D-004, a lipid extract from the Roystonea regia fruit, on the plasma of healthy men

The aim of this study was to conduct a randomized, double-blind and placebo-controlled study to investigate the effects of D-004, a lipid extract of the Roystonea regia fruit that prevents testosterone- and phenylepinephrine-induced prostate hyperplasia in rodents, on plasma oxidative markers in healthy men. We enrolled male volunteers (20–55 years) in good health and without lower urinary tract symptoms. Thirty-four eligible participants were randomized to placebo or D-004 (320 mg) capsules administered daily for 6 weeks. An interim check-up and a final visit were conducted after 3 and 6 weeks of therapy, respectively. Physical examinations were performed at each visit, and laboratory tests were performed at baseline and at treatment completion. Oxidative variables included plasma malondialdehyde (MDA), total hydroxyperoxides (TOH), sulphydryl (SH) groups and total antioxidant status (TAS). We assessed treatment compliance and addressed adverse experiences (AEs) at weeks 3 and 6. At week 6, with D-004, the mean reductions of plasma MDA (26.7 percent), TOH (18.8 percent) and SH groups (31.6 percent), and the mean increase of TAS (35.3 percent) were significantly different from those of placebo (P < 0.001 for plasma TAS, P < 0.0001 for all other comparisons). D-004 did not differ from the placebo in safety indicators. There were two withdrawals (both in the D-004 group), with one due to dyspepsia (the only AE during the trial). In conclusion, D-004 displayed antioxidant effects on plasma oxidative markers in healthy men, which was consistent with findings from laboratory experimental studies(AU)

Antioxidant effects of D-004, a lipid extract from the Roystonea regia fruit, on the plasma of healthy men.

The aim of this study was to conduct a randomized, double-blind and placebo-controlled study to investigate the effects of D-004, a lipid extract of the Roystonea regia fruit that prevents testosterone- and phenylepinephrine-induced prostate hyperplasia in rodents, on plasma oxidative markers in healthy men. We enrolled male volunteers (20-55 years) in good health and without lower urinary tract symptoms. Thirty-four eligible participants were randomized to placebo or D-004 (320 mg) capsules administered daily for 6 weeks. An interim check-up and a final visit were conducted after 3 and 6 weeks of therapy, respectively. Physical examinations were performed at each visit, and laboratory tests were performed at baseline and at treatment completion. Oxidative variables included plasma malondialdehyde (MDA), total hydroxyperoxides (TOH), sulphydryl (SH) groups and total antioxidant status (TAS). We assessed treatment compliance and addressed adverse experiences (AEs) at weeks 3 and 6. At week 6, with D-004, the mean reductions of plasma MDA (26.7%), TOH (18.8%) and SH groups (31.6%), and the mean increase of TAS (35.3%) were significantly different from those of placebo (P<0.001 for plasma TAS, P<0.0001 for all other comparisons). D-004 did not differ from the placebo in safety indicators. There were two withdrawals (both in the D-004 group), with one due to dyspepsia (the only AE during the trial). In conclusion, D-004 displayed antioxidant effects on plasma oxidative markers in healthy men, which was consistent with findings from laboratory experimental studies.

Effects of D-002, a product isolated from beeswax, on gastric symptoms of patients with osteoarthritis treated with piroxicam: a pilot study.

Non-steroidal anti-inflammatory drugs (NSAIDs) are indicated for treatment of rheumatoid arthritis and osteoarthritis, but often induce gastric adverse experiences (AE), including gastric ulcers and complications. Inhibitors of proton pump and H(2) antagonists are very effective for duodenal ulcer; meanwhile, cytoprotective drugs are more effective for gastric ulcer. D-002 is a mixture of higher aliphatic alcohols obtained from beeswax, wherein triacontanol is the most abundant. D-002 induces anti-ulcer effects through a cytoprotective mechanism, being more effective in protecting against ethanol- and NSAID-induced ulcers. The present double-blind, placebo-controlled clinical study was undertaken to investigate the effects of D-002 on gastric symptoms associated to piroxicam use on patients suffering osteoarthritis. Fifty-nine patients, all taking piroxicam, 20 mg/day, were randomized to placebo or D-002 (40 or 100 mg/day) for 14 days. The primary efficacy variable was the reduction on the frequency of patients with gastric AE compared with placebo. Pain evolution was investigated to discard any influence on D-002 on the analgesic effect of piroxicam. The frequency of patients treated with D-002, 40 and 100 mg/day, reporting acidity [0 of 18 (0%) and 1 of 21 (4.8%), respectively] was lower (P < .05) than in placebo [6 of 20 (30%)]. Also, the frequency of patients treated with 100 mg/day reporting some gastric AE [5 of 21 (23.8%)] was lower (P < .05) than in placebo [13 of 20 (65.0%)]. The analgesic effect of piroxicam was unaffected with D-002. Treatment was well tolerated. Two patients discontinued from the study because of gastrointestinal AE: one in the placebo group and the other treated with D-002, 40 mg/day. Other three patients discontinued because of other AE: mildly uncontrolled hypertension (one in the placebo group, one treated with D-002, 40 mg/day) and headache (one treated with D-200, 100 mg/day). It is concluded that D-002 could be useful for controlling gastric AE of patients treated with NSAIDs, although further studies with a larger sample size and longer follow-up are needed for definitive conclusions.

Evaluación preliminar de los efectos neurofarmacológicos de Justicia pectoris / Preliminary evaluation of neuropharmacological effects of Justicia pectoris

Se realizaron ensayos preliminares de la decocción de Justicia pectoralis en ratones de la cepa C-57, donde se evaluaron los posible efectos de dichas decocciones sobre la conducta exploratoria, la conducta agresiva y las convulsiones inducidas por pentilentetrazol en ratones. También se estudió el efecto de J. pectoralis sobre la excitación producida por fenciclidina (droga esquizofrenomimética) en ratas infantiles. Los resultados obtenidos sugieren que Justicia pectoralis reduce la conducta agresiva y la actividad exploratoria en ratones, bloquea la excitación inducida por fenciclidina en ratas infantiles y no previene las convulsiones inducidas por pentilentetrazol

Evaluación preliminar de los efectos neurofarmacológicos de Justicia pectoris / Preliinary evaluation of neuropharmacological effects of Justicia pectoris

Se realizaron ensayos preliminares de la decocción de Justicia pectoralis en ratones de la cepa C-57, donde se evaluaron los posible efectos de dichas decocciones sobre la conducta exploratoria, la conducta agresiva y las convulsiones inducidas por pentilentetrazol en ratones. También se estudió el efecto de J. pectoralis sobre la excitación producida por fenciclidina (droga esquizofrenomimética) en ratas infantiles. Los resultados obtenidos sugieren que Justicia pectoralis reduce la conducta agresiva y la actividad exploratoria en ratones, bloquea la excitación inducida por fenciclidina en ratas infantiles y no previene las convulsiones inducidas por pentilentetrazol