Stroke is the third cause of death and the first of permanent adult disability. Pretreatment with... more Stroke is the third cause of death and the first of permanent adult disability. Pretreatment with policosanol and atorvastatin has been effective in experimental models of cerebral ischaemia in rodents. The objective was to compare the therapeutic effects of policosanol and atorvastatin in a model of global cerebral ischaemia in gerbils. Gerbils were distributed into seven groups, a negative control and six with ischaemia-reperfusion-induced global cerebral ischemia (one vehicle positive control, two policosanol (100 and 200 mg/kg), two atorvastatin (10 and 20 mg/kg) and one aspirin (60 mg/kg) group). Treatments were given 4 h after ischaemia induction. Effects on ischemia-reperfusion-induced symptoms, hyperlocomotion, damage of pyramidal hipoccampal neurons and increased plasma oxidative markers were investigated. Positive, not negative controls, exhibited clinical symptoms, hyperlocomotion, neuronal damage and increased plasma oxidative markers. Policosanol (100 and 200 mg/kg) red...
Osteoarthritis (OA) is characterized by degeneration, pain and inflammation of joint cartilage. T... more Osteoarthritis (OA) is characterized by degeneration, pain and inflammation of joint cartilage. The effects of D-002, a mixture of beeswax alcohols with anti-inflammatory action, on monosodium iodoacetate (MIA)-induced OA were investigated. Rats were distributed into a negative control group (vehicle) and five groups with MIA-induced OA and treated orally with vehicle (positive control), D-002 (50, 200 and 400 mg/kg) or ibuprofen (30 µmol/kg) for 10 days after OA induction. Joint damage was assessed using histological analysis. MIA injection increased the depth, extent and histological scores of cartilage damage. D-002 (50-200 mg/kg) reduced the MIA-induced injury on joint cartilage (loss of chondrocytes and proteoglycans, pannus formation and joint inflammation) but unaffected bone destruction. Ibuprofen reduced the inflammation degree and the depth of cartilage damage, but not the other parameters. These results indicate a protective effect of D-002 against joint damage in MIA-ind...
Osteoarthritis (OA), a degenerative joint disease affecting the cartilage and surrounding tissues... more Osteoarthritis (OA), a degenerative joint disease affecting the cartilage and surrounding tissues, causes pain, reduces mobility, and deteriorates quality of life in adults, mainly the elderly. Most treatments for OA, such as non-steroidal anti-inflammatory drugs and analgesics, induce adverse side effects, supporting the search for effective, but safer treatments. Green-lipped mussel (Perna canaliculus) extracts (GME) have been useful for managing OA. D-002, a mixture of beeswax alcohols, has been shown to ameliorate experimental OA and to reduce OA symptoms. This study investigated whether administering D-002 together with GME may improve the efficacy of GME on OA symptoms. Subjects with OA symptoms were double-blindly randomized to GME capsules (50 mg of the extract/capsule) + placebo or D-002 (50 mg) tablets for 6 weeks. Symptoms were assessed by the Western Ontario and McMaster Individual Osteoarthritis Index (WOMAC) and the visual analogy scale (VAS) scores. The primary outcom...
The rheumatoid arthritis, is the inflammatory polyarthritis commonest in adults affecting about t... more The rheumatoid arthritis, is the inflammatory polyarthritis commonest in adults affecting about the 1 % of world population, more predominant in women than men and more frequent in those aged 30 and 50 and entails a high level of inability of patient. It is characterized by a symmetrical erosive synovitis with proliferation of conjunctival tissue (pannus), invading and eroding the cartilage and joint bones, and sometimes, by a multisystem affection. In most patients the disease follows a fluctuating chronic course, which it is not treated, provoke a progressive destruction, deformity and inability of involved joints. The disease evolves with high figures of rheumatoid factor and/or anticitrulline antibodies. These are essential features of an optimal treatment of this entity include: early differential diagnosis, initial treatment with non-steroidal anti-inflammatory drugs (NSAIDs), the use of disease course modifying drugs, the potential use of oral low-dose glucocorticoid agents o...
Latin American and Caribbean Bulletin of Medicinal and Aromatic Plants, 2017
El objetivo de este estudio fue investigar si el extracto lipidico de los frutos de Acrocomia cri... more El objetivo de este estudio fue investigar si el extracto lipidico de los frutos de Acrocomia crispa (D - 005) inhibe in vitro las actividades de las enzimas COX y 5 - LOX. Este estudio demuest ra que el D - 005 inhibe marcadamente y de manera dosis dependiente las actividades de la COX - 2 y 5 - LOX. La inhibicion dual de la COX - 2 y 5 - LOX soportan futuras investigaciones sobre el potencial efecto anti - inflamatorio del D - 005
Both policosanol and D-003 are mixtures of higher aliphatic alcohols and acids, respectively, pur... more Both policosanol and D-003 are mixtures of higher aliphatic alcohols and acids, respectively, purified from sugarcane wax, whose main components are octacosanol and octacosanoic acid (an active metabolite of octacosanol), respectively. Both substances share some, not all, pharmacological effects, like cholesterol-lowering, antiplatelet and antioxidant effects. The mechanisms whereby they exhibit cholesterol-lowering have been investigated, but those supporting their antiplatelet effects remain unknown. We hypothesized that these substances could inhibit cyclooxygenase (COX) activity. The aim of this study was to investigate whether policosanol and D-003 may inhibit COX-1 and COX-2 enzyme activities, effects assessed in cytosolic microsomes from rat platelets and seminal vesicles, respectively. Vehicle, Policosanol or D-003 suspensions (0.6 to 6000 g/mL) were added to tubes containing a mixture of reactions and absorbance changes at 480 nm were measured. Both policosanol and D-003 i...
Osteoarthritis (OA) is a syndrome that affects hundreds of millions around the world. The treatme... more Osteoarthritis (OA) is a syndrome that affects hundreds of millions around the world. The treatment of OA is addressed to pain alleviation and functional status improvement. Non-steroidal anti-inflammatory drug are widely prescribed for OA, but produce gastrointestinal (non selective) and cardiovascular (ciclooxygenase–2 inhibitors) adverse effects. Then, the search for new substances is justified. D-003 is a mixture of higher aliphatic sugarcane wax acids with antiresorptive and antioxidants effects. The aim of this study was to investigate the effects of D-003 on formaldehyde-induced OA in rats. OA Animals were orally dosed with either D-003 (100 and 400 mg/kg) or naproxen (NAP) (3 mg/kg), as reference drug. Controls comprised negative and vehicle-treated rats. Treatments were administered for 10 days. The effects were assessed by measuring the changes on the diameters of rat ankle and paw. The formaldehyde injection significantly increased the diameters of rat paw and ankle as co...
The effect of policosanol on circulating endothelial cells has been studied in different experime... more The effect of policosanol on circulating endothelial cells has been studied in different experimental models with endothelium damage. Oral administration of 25 mg kg− policosanol to Sprague-Dawley rats resulted in significant protection of the endothelial lining against the desquamating effect of citrate. Oral administration of 5 mg kg− policosanol to spontaneously hypertensive rats (SHR) resulted in a significant reduction of circulating endothelial cells compared with controls. Moreover, comparison between groups revealed a lower frequency of aortic lesions in policosanol-treated animals than in controls. On the other hand, administration of 5 mg kg− policosanol to rabbits with intimal hyperplasia induced by cuff placement in the carotid artery resulted in levels of circulating endothelial cells significantly lower than in controls. These results demonstrate the protective effect of policosanol in different experimental models and suggest its potential for endothelial protection.
Canadian Journal of Physiology and Pharmacology, 2002
Previous results have demonstrated that policosanol, a mixture of aliphatic primary alcohols isol... more Previous results have demonstrated that policosanol, a mixture of aliphatic primary alcohols isolated and purified from sugar cane wax, whose main component is octacosanol, inhibited lipid peroxidation in experimental models and human beings. D003 is a defined mixture of very long-chain saturated fatty acids, also isolated and purified from sugar cane wax, whose main component is octacosanoic acid followed by traicontanoic, dotriacontanoic, and tetracontanoic acids. Since very long-chain fatty acids are structurally related to their corresponding alcohols, we investigated the effect of oral treatment with D003 (0.5, 5, 50, and 100 mg/kg) over 4 weeks in reducing the susceptibility of rat lipoprotein to oxidative modification. The combined rat lipoprotein fraction VLDL + LDL was subjected to several oxidation systems, including those containing metal ions (CuSO4), those having the capacity to generate free radicals 2,2-azobis-2-amidinopropane hydrochloride (AAPH), and a more physiolo...
Stroke is the third cause of death and the first of permanent adult disability. Pretreatment with... more Stroke is the third cause of death and the first of permanent adult disability. Pretreatment with policosanol and atorvastatin has been effective in experimental models of cerebral ischaemia in rodents. The objective was to compare the therapeutic effects of policosanol and atorvastatin in a model of global cerebral ischaemia in gerbils. Gerbils were distributed into seven groups, a negative control and six with ischaemia-reperfusion-induced global cerebral ischemia (one vehicle positive control, two policosanol (100 and 200 mg/kg), two atorvastatin (10 and 20 mg/kg) and one aspirin (60 mg/kg) group). Treatments were given 4 h after ischaemia induction. Effects on ischemia-reperfusion-induced symptoms, hyperlocomotion, damage of pyramidal hipoccampal neurons and increased plasma oxidative markers were investigated. Positive, not negative controls, exhibited clinical symptoms, hyperlocomotion, neuronal damage and increased plasma oxidative markers. Policosanol (100 and 200 mg/kg) red...
Osteoarthritis (OA) is characterized by degeneration, pain and inflammation of joint cartilage. T... more Osteoarthritis (OA) is characterized by degeneration, pain and inflammation of joint cartilage. The effects of D-002, a mixture of beeswax alcohols with anti-inflammatory action, on monosodium iodoacetate (MIA)-induced OA were investigated. Rats were distributed into a negative control group (vehicle) and five groups with MIA-induced OA and treated orally with vehicle (positive control), D-002 (50, 200 and 400 mg/kg) or ibuprofen (30 µmol/kg) for 10 days after OA induction. Joint damage was assessed using histological analysis. MIA injection increased the depth, extent and histological scores of cartilage damage. D-002 (50-200 mg/kg) reduced the MIA-induced injury on joint cartilage (loss of chondrocytes and proteoglycans, pannus formation and joint inflammation) but unaffected bone destruction. Ibuprofen reduced the inflammation degree and the depth of cartilage damage, but not the other parameters. These results indicate a protective effect of D-002 against joint damage in MIA-ind...
Osteoarthritis (OA), a degenerative joint disease affecting the cartilage and surrounding tissues... more Osteoarthritis (OA), a degenerative joint disease affecting the cartilage and surrounding tissues, causes pain, reduces mobility, and deteriorates quality of life in adults, mainly the elderly. Most treatments for OA, such as non-steroidal anti-inflammatory drugs and analgesics, induce adverse side effects, supporting the search for effective, but safer treatments. Green-lipped mussel (Perna canaliculus) extracts (GME) have been useful for managing OA. D-002, a mixture of beeswax alcohols, has been shown to ameliorate experimental OA and to reduce OA symptoms. This study investigated whether administering D-002 together with GME may improve the efficacy of GME on OA symptoms. Subjects with OA symptoms were double-blindly randomized to GME capsules (50 mg of the extract/capsule) + placebo or D-002 (50 mg) tablets for 6 weeks. Symptoms were assessed by the Western Ontario and McMaster Individual Osteoarthritis Index (WOMAC) and the visual analogy scale (VAS) scores. The primary outcom...
The rheumatoid arthritis, is the inflammatory polyarthritis commonest in adults affecting about t... more The rheumatoid arthritis, is the inflammatory polyarthritis commonest in adults affecting about the 1 % of world population, more predominant in women than men and more frequent in those aged 30 and 50 and entails a high level of inability of patient. It is characterized by a symmetrical erosive synovitis with proliferation of conjunctival tissue (pannus), invading and eroding the cartilage and joint bones, and sometimes, by a multisystem affection. In most patients the disease follows a fluctuating chronic course, which it is not treated, provoke a progressive destruction, deformity and inability of involved joints. The disease evolves with high figures of rheumatoid factor and/or anticitrulline antibodies. These are essential features of an optimal treatment of this entity include: early differential diagnosis, initial treatment with non-steroidal anti-inflammatory drugs (NSAIDs), the use of disease course modifying drugs, the potential use of oral low-dose glucocorticoid agents o...
Latin American and Caribbean Bulletin of Medicinal and Aromatic Plants, 2017
El objetivo de este estudio fue investigar si el extracto lipidico de los frutos de Acrocomia cri... more El objetivo de este estudio fue investigar si el extracto lipidico de los frutos de Acrocomia crispa (D - 005) inhibe in vitro las actividades de las enzimas COX y 5 - LOX. Este estudio demuest ra que el D - 005 inhibe marcadamente y de manera dosis dependiente las actividades de la COX - 2 y 5 - LOX. La inhibicion dual de la COX - 2 y 5 - LOX soportan futuras investigaciones sobre el potencial efecto anti - inflamatorio del D - 005
Both policosanol and D-003 are mixtures of higher aliphatic alcohols and acids, respectively, pur... more Both policosanol and D-003 are mixtures of higher aliphatic alcohols and acids, respectively, purified from sugarcane wax, whose main components are octacosanol and octacosanoic acid (an active metabolite of octacosanol), respectively. Both substances share some, not all, pharmacological effects, like cholesterol-lowering, antiplatelet and antioxidant effects. The mechanisms whereby they exhibit cholesterol-lowering have been investigated, but those supporting their antiplatelet effects remain unknown. We hypothesized that these substances could inhibit cyclooxygenase (COX) activity. The aim of this study was to investigate whether policosanol and D-003 may inhibit COX-1 and COX-2 enzyme activities, effects assessed in cytosolic microsomes from rat platelets and seminal vesicles, respectively. Vehicle, Policosanol or D-003 suspensions (0.6 to 6000 g/mL) were added to tubes containing a mixture of reactions and absorbance changes at 480 nm were measured. Both policosanol and D-003 i...
Osteoarthritis (OA) is a syndrome that affects hundreds of millions around the world. The treatme... more Osteoarthritis (OA) is a syndrome that affects hundreds of millions around the world. The treatment of OA is addressed to pain alleviation and functional status improvement. Non-steroidal anti-inflammatory drug are widely prescribed for OA, but produce gastrointestinal (non selective) and cardiovascular (ciclooxygenase–2 inhibitors) adverse effects. Then, the search for new substances is justified. D-003 is a mixture of higher aliphatic sugarcane wax acids with antiresorptive and antioxidants effects. The aim of this study was to investigate the effects of D-003 on formaldehyde-induced OA in rats. OA Animals were orally dosed with either D-003 (100 and 400 mg/kg) or naproxen (NAP) (3 mg/kg), as reference drug. Controls comprised negative and vehicle-treated rats. Treatments were administered for 10 days. The effects were assessed by measuring the changes on the diameters of rat ankle and paw. The formaldehyde injection significantly increased the diameters of rat paw and ankle as co...
The effect of policosanol on circulating endothelial cells has been studied in different experime... more The effect of policosanol on circulating endothelial cells has been studied in different experimental models with endothelium damage. Oral administration of 25 mg kg− policosanol to Sprague-Dawley rats resulted in significant protection of the endothelial lining against the desquamating effect of citrate. Oral administration of 5 mg kg− policosanol to spontaneously hypertensive rats (SHR) resulted in a significant reduction of circulating endothelial cells compared with controls. Moreover, comparison between groups revealed a lower frequency of aortic lesions in policosanol-treated animals than in controls. On the other hand, administration of 5 mg kg− policosanol to rabbits with intimal hyperplasia induced by cuff placement in the carotid artery resulted in levels of circulating endothelial cells significantly lower than in controls. These results demonstrate the protective effect of policosanol in different experimental models and suggest its potential for endothelial protection.
Canadian Journal of Physiology and Pharmacology, 2002
Previous results have demonstrated that policosanol, a mixture of aliphatic primary alcohols isol... more Previous results have demonstrated that policosanol, a mixture of aliphatic primary alcohols isolated and purified from sugar cane wax, whose main component is octacosanol, inhibited lipid peroxidation in experimental models and human beings. D003 is a defined mixture of very long-chain saturated fatty acids, also isolated and purified from sugar cane wax, whose main component is octacosanoic acid followed by traicontanoic, dotriacontanoic, and tetracontanoic acids. Since very long-chain fatty acids are structurally related to their corresponding alcohols, we investigated the effect of oral treatment with D003 (0.5, 5, 50, and 100 mg/kg) over 4 weeks in reducing the susceptibility of rat lipoprotein to oxidative modification. The combined rat lipoprotein fraction VLDL + LDL was subjected to several oxidation systems, including those containing metal ions (CuSO4), those having the capacity to generate free radicals 2,2-azobis-2-amidinopropane hydrochloride (AAPH), and a more physiolo...
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