Anti-inflammatory and gastric effects of D-002, aspirin and naproxen and their combined therapy in rats with cotton pellet-induced granuloma

D-002, a mixture of six beeswax alcohols, with gastroprotective and anti-inflammatory effects, was compared with naproxen, aspirin and their combined therapy in rats with cotton pellet granuloma. After pellet implantation, rats were randomized into seven groups, a vehicle control and treated with (mg/kg): D-002 (50 and 200), naproxen (10 and 25) and aspirin (150 and 300). Other group of implanted rats was randomized into six groups, vehicle control and treated with D-002 50, naproxen 10, aspirin 150, D-002 50 + aspirin 150, or D-002 50 + naproxen 10. Granuloma weights decreased with all treatments, the effects of the highest doses were 38 % (D-002), 42 % (naproxen) and 42 % (aspirin). The combinations were not greater than those of each monotherapy. Aspirin and naproxen, not D-002, induced gastric ulceration. D-002 + naproxen or aspirin significantly decreased ulcers by 69.8 % and 67.3 %, respectively. Then, D-002, aspirin and naproxen were similarly effective for reducing the cotton granuloma in rats. The combination therapies D-002 + naproxen or aspirin did not produce greater anti-inflammatory effects, but reduced the NSAIDs-induced gastrotoxicity.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Effects of Grape Seed Extract, Vitamin C, and Vitamin E on Ethanol- and Aspirin-Induced Ulcers

Effects of GSE and vitamins C and E on aspirin- and ethanol-induced gastric ulcer and associated increases of lipid peroxidation in rats were compared. Two experiments were conducted. Rats were randomized into eight groups: a negative control and seven groups that received aspirin or ethanol for ulcer induction: one positive control (vehicle) and six with VC, VE, or GSE (25 and 250 mg/kg). Ulcer indexes and gastric levels of malondialdehyde (MDA) were quantified. VC, VE, and GSE (25 and 250 mg/kg) decreased aspirin, and ethanol-induced ulcers and MDA values compared with positive control group. The magnitude of aspirin ulcer reduction was comparable for all treatments, and MDA decrease with GSE was higher than with VC and tended to be greater, albeit none significantly, than with VE. GSE was more effective than VC and VE for lowering the ethanol ulcers, while the decrease of MDA levels with GSE was greater than with VC, but comparable to that achieved with VE. GSE protected against ethanol-induced gastric ulcers more effectively than VC or VE, while its protection against aspirin ulcers was comparable for all treatments. GSE produced the greatest reductions of gastric MDA in both models

Effects of single oral and topical administration of D-002 (beeswax alcohols) on xylene-induced ear edema in mice

D-002 (beeswax alcohols) contains triacontanol as most abundant component. Local application of triacontanol has been shown anti-inflammatory effects on chemically-induced dermatitis and oral treatment with D-002 produced anti-inflammatory effects in carrageenan-induced pleurisy and cotton granuloma in rats, but its effects on xylene-induced mouse ear edema had not been studied. This study investigated the effects of single oral and topical doses of D-002 on this model. Oral dosing groups were composed by one negative control and six xylene-treated, one positive control, four D-002-treated (25, 50, 200, 400 mg/kg), and one indomethacin-treated (10 mg/kg). Topical dosing groups were conformed by one negative control and four xylene- treated, one positive control and three D-002-treated (2.5, 5, 10 %). Single oral doses of D-002 significantly and dose-dependently reduced edema formation and myeloperoxidase activity, but single topical applications unchanged both variables. Concluding, acute oral treatment with D- 002 was effective to decrease xylene-induced mouse ear edema, but single topical doses were ineffective.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Comparison of the efficacy and tolerability of chondroitin plus glucosamine and D-002 (beeswax alcohols) in subjects with osteoarthritis symptoms

Background/AIMS: Osteoarthritis (OA), the commonest joint disorder, is a leading cause of disability. Symptomatic slow-acting drugs for OA (SYSADOA), particularly glucosamine plus chondroitin sulphate (GS/CS), are effective for symptom relief, protect joint cartilage and delay OA progression, with a good safety profile. D-002, a mixture of beeswax alcohols that inhibits both cyclooxygenase and 5-lipoxygenase activities, has been effective in experimental and clinical OA studies, showing also a chondroprotective effect.OBJECTIVES: To compare the effects of D-002 and GS/SC administered for 12 weeks on OA symptoms.METHODS: Participants were randomized to GS/CS (375/300 mg) or 50?mg D-002 once daily for 12 weeks. Symptoms were assessed by the Western Ontario and McMaster Individual Osteoarthritis Index (WOMAC) and the visual analogy scale (VAS) scores. The primary outcome was the reduction of the total WOMAC score. Secondary outcomes included WOMAC pain, stiffness and function scores, VAS score and rescue medication consumption.RESULTS: Of 60 randomized patients, 59 completed the study. D-002 and GS/SC reduced significantly total WOMAC score (72.1% and 78.5%, respectively), and pain, joint stiffness and physical function scores versus baseline. VAS scores decreased significantly with D-002 (76.6%) and GS/SC (76.8%). The reductions, significant from the second week, were enhanced over the trial. Rescue medications were consumed by 3/30 D-002 and 4/30 GS/SC patients. No differences between groups were found. Treatments were well tolerated.CONCLUSIONS: D-002 (50 mg/day) administered for 12 weeks was safe and comparable to GS/SC for alleviating OA symptoms (pain, stiffness, and functional limitation) (RPCEC00000180).</h4

Tratamientos más utilizados en la colitis ulcerativa

Teniendo en cuenta la importancia de la colitis ulcerativa, el objetivo de esta revisión consiste en la aproximación al manejo de enfermedad haciendo énfasis en los tratamientos. La colitis ulcerativa (CU) es una enfermedad inflamatoria crónica caracterizada por la inflamación de la mucosa del colon y el recto. Es una enfermedad multifactorial, con una interacción compleja de factores genéticos y ambientales. Los síntomas más frecuentes son diarrea, dolor abdominal y heces con sangre, sin embargo, a pesar de los avances terapéuticos, la morbilidad de esta enfermedad es alta, afectando la calidad de vida de los pacientes. La elección del tratamiento depende de la severidad, localización y el curso de la enfermedad. La primera línea terapéutica para inducir y mantener la remisión en pacientes con colitis ulcerativa de media a moderada corresponde a los derivados del 5-ASA, los aminosalicila tos (ácido 5-aminosalicilato), también denominados mesalamina. La sulfasalazina fue el primer medicamento de este grupo utilizado pero resultó tóxico debido a la sulfapiridina molécula utilizada como transportadora. Otras formulaciones (olsalazida, balsala zida, salofalk, pentasa), con menos efectos adversos han sido ensayadas con buenos resultados. En pacientes refractarios a la mesalamina se utilizan los esteroides (prednisolona, hidrocortisona, beclometasona y budesonida), los inmunomoduladores (azatiop rina, 6-mercaptopurina, ciclosporina A, metotrexate) y los inhibidores del FNT-α como el infliximab, adalimumab y certolizumab pegol). Nuevos tratamientos están siendo ensayados para lograr una remisión más efectiva de la enfermedad

Protective effect of D-003 on renal ischemia-reperfusion in rats

The effects of D-003, a mixture of higher aliphatic acids purified from sugarcane wax with antioxidant effects, and a grape seed extracts (GSE) on serum creatinine levels and on histological damage, were evaluated in a rat model of renal ischemia-reperfusion (I/R). Rats were subjected to sham operation or renal I/R. One group was treated orally with the vehicle, two were treated with D-003 (250 and 500 mg/kg) and other with GSE (200 mg/kg). Renal morphological alterations were assessed by histopathological examination of haematoxylin-eosin stained. After 24 h of post-ischemic acute renal failure, serum creatinine levels was increased, effect that was significantly decreased by about 30 % and 60 % with D-003 and with GSE, respectively. Compared with sham rats, ischemic controls demonstrated severe damage of renal function and morphology, while both D-003 and GSE treatments protected against these I/R-induced histological abnormalities too. D-003 protected moderately against the increase of serum creatinine and histological findings of I/R-induced renal injury in rats.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Different ripening stages of Roystonea regia fruits influence: their effects on testosterone-induced prostate enlargement in rats

En este trabajo se han comparado los efectos de extractos lipídicos obtenidos de los frutos de Roystonea regia de diferentes estados de maduración sobre la hiperplasia prostática inducida por testosterona en ratas. Frutos maduros, pintones y verdes fueron colectados y procesados para la obtención de extractos lipídicos, cuyo contenido de ácidos grasos fue analizado por cromatografía gaseosa. A medida que los frutos maduran la concentración de ácido láurico aumenta y el oleico disminuye, mientras que los otros ácidos presentaron pocos cambios en sus concentraciones. Los extractos con mayores concentraciones de ácido láurico fueron más efectivos en reducir el incremento del tamaño de la próstata inducido por testosterona.The effects of lipid extracts from Roystonea regia fruits at different ripening stages on prostate hyperplasia induced with testosterone in rats were compared . Ripe, medium ripe and unripe fruits were collected and processed to obtain lipid extracts whose fatty acid contents were determined by gas chromatography. Lauric acid increased while oleic acid concentrations decreased, as per fruit ripening, while other fatty acids had little changes. Higher concentrations of lauric acid reduced prostate enlargement, meanwhile batches with low concentrations were ineffective.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Different ripening stages of Roystonea regia fruits influence: their effects on testosterone-induced prostate enlargement in rats

En este trabajo se han comparado los efectos de extractos lipídicos obtenidos de los frutos de Roystonea regia de diferentes estados de maduración sobre la hiperplasia prostática inducida por testosterona en ratas. Frutos maduros, pintones y verdes fueron colectados y procesados para la obtención de extractos lipídicos, cuyo contenido de ácidos grasos fue analizado por cromatografía gaseosa. A medida que los frutos maduran la concentración de ácido láurico aumenta y el oleico disminuye, mientras que los otros ácidos presentaron pocos cambios en sus concentraciones. Los extractos con mayores concentraciones de ácido láurico fueron más efectivos en reducir el incremento del tamaño de la próstata inducido por testosterona.The effects of lipid extracts from Roystonea regia fruits at different ripening stages on prostate hyperplasia induced with testosterone in rats were compared . Ripe, medium ripe and unripe fruits were collected and processed to obtain lipid extracts whose fatty acid contents were determined by gas chromatography. Lauric acid increased while oleic acid concentrations decreased, as per fruit ripening, while other fatty acids had little changes. Higher concentrations of lauric acid reduced prostate enlargement, meanwhile batches with low concentrations were ineffective.Colegio de Farmacéuticos de la Provincia de Buenos Aire