RESUMO
RATIONALE: Traditional remedies prepared from Ptychopetalum olacoides (PO) are used throughout the Amazon to alleviate age-related conditions. These formulas are mainly used by elders, and alleged effects may be related to the anticholinesterase properties identified in a standardized ethanol extract of this species [P. olacoides standardized ethanol extract (POEE)]. OBJECTIVES: To further characterize the potential of this extract for developing drugs useful to treat cognitive deficits, the effects of POEE on scopolamine (scop)- and MK801-induced amnesias (acquisition, consolidation, and retrieval) in mice were investigated. RESULTS: Scop (3.0 mg/kg, ip) significantly impaired memory (all three phases) in the step-down inhibitory avoidance protocol. As expected, MK801 (0.1 mg/kg, ip) was amnesic regarding acquisition and consolidation, but not retrieval. POEE (100 mg/kg, ip) reversed the scop-induced impairment in all three phases of long-term and short memories, whereas only the memory consolidation deficit was reversed with MK801-induced amnesia. CONCLUSIONS: This study complements previously reported promnesic properties of this plant extract and suggests that POEE may be further developed for treating conditions associated with cognitive deficits, especially those linked with cholinergic malfunction.
Assuntos
Amnésia/induzido quimicamente , Amnésia/tratamento farmacológico , Maleato de Dizocilpina , Antagonistas de Aminoácidos Excitatórios , Antagonistas Muscarínicos , Olacaceae/química , Escopolamina , Amnésia/psicologia , Animais , Aprendizagem da Esquiva/efeitos dos fármacos , Brasil , Eletrochoque , Injeções Intraperitoneais , Masculino , Memória/efeitos dos fármacos , Memória de Curto Prazo , Camundongos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/farmacologia , Raízes de Plantas/químicaRESUMO
Linalool is a monoterpene often found as a major component of essential oils obtained from aromatic plant species, many of which are used in traditional medical systems as hypno-sedatives. Psychopharmacological evaluations of linalool (i.p. and i.c.v.) revealed marked sedative and anticonvulsant central effects in various mouse models. Considering this profile and alleged effects of inhaled lavender essential oil, the purpose of this study was to examine the sedative effects of inhaled linalool in mice. Mice were placed in an inhalation chamber during 60 min, in an atmosphere saturated with 1% or 3% linalool. Immediately after inhalation, animals were evaluated regarding locomotion, barbiturate-induced sleeping time, body temperature and motor coordination (rota-rod test). The 1% and 3% linalool increased (p<0.01) pentobarbital sleeping time and reduced (p<0.01) body temperature. The 3% linalool decreased (p<0.01) locomotion. Motor coordination was not affected. Hence, linalool inhaled for 1h seems to induce sedation without significant impairment in motor abilities, a side effect shared by most psycholeptic drugs.
Assuntos
Hipnóticos e Sedativos/farmacologia , Monoterpenos/farmacologia , Atividade Motora/efeitos dos fármacos , Destreza Motora/efeitos dos fármacos , Extratos Vegetais/farmacologia , Sono/efeitos dos fármacos , Monoterpenos Acíclicos , Administração por Inalação , Animais , Temperatura Corporal/efeitos dos fármacos , Diazepam/farmacologia , Relação Dose-Resposta a Droga , Hipnóticos e Sedativos/administração & dosagem , Masculino , Camundongos , Monoterpenos/administração & dosagem , Pentobarbital/farmacologia , Extratos Vegetais/administração & dosagemRESUMO
Nootropic, antioxidant, and neuroprotective properties have been shown in a standardized ethanol extract of Ptychopetalum olacoides (POEE), a medicinal plant traditionally used by the Amazonian elderly population. It has been revealed that POEE mechanisms of action include anticholinesterase effects, and involve beta-adrenergic and dopamine D(1) receptors. The purpose of this study was to verify the role of serotonin receptors in the promnesic effects of this standardized extract. The step-down task in mice and selective serotonin antagonists were used. The study reveals that POEE promnesic effects on short-term (acquisition, consolidation and retrieval) and long-term (retrieval) declarative aversive memories are increased by 5HT(2A) (but not 5HT(1A)) serotonin antagonists (spiperone and pindolol, respectively). The observed synergism between POEE and spiperone can be interpreted as the combined effects of two subeffective doses of two 5HT antagonists, or the known synergism between an acetylcholinesterase inhibitor (POEE) and a 5HT antagonist. In conclusion it is suggested that 5HT(2A) serotonin receptors are relevant for the promnesic effects of this extract, adding to its multiple mechanisms of action.
Assuntos
Comportamento Animal/efeitos dos fármacos , Olacaceae/química , Extratos Vegetais/farmacologia , Receptores de Serotonina/metabolismo , Animais , Aprendizagem da Esquiva/efeitos dos fármacos , Relação Dose-Resposta a Droga , Interações Medicamentosas , Masculino , Memória/classificação , Memória/efeitos dos fármacos , Camundongos , Pindolol/farmacologia , Tempo de Reação/efeitos dos fármacos , Antagonistas da Serotonina/farmacologia , Espiperona/farmacologia , Estatísticas não ParamétricasRESUMO
The cholinergic hypothesis of Alzheimer disease (AD) has provided the rationale for the current pharmacotherapy of this disease, in an attempt to downgrade the cognitive decline caused by cholinergic deficits. Nevertheless, the search for potent and long-acting acetylcholinesterase (AChE) inhibitors that exert minimal side effects to AD patients is still an ongoing effort. Amazonian communities use traditional remedies prepared with Ptychopetalum olacoides (PO, Olacaceae) roots for treating various central nervous system conditions, including those associated with aging. The fact that PO ethanol extract (POEE) has been found to facilitate memory retrieval in the step down procedure in young and aged mice prompt us to evaluate its effects on AChE activity in memory relevant brain areas. POEE significantly inhibited AChE activity in vitro in a dose- and time-dependent manner in rat frontal cortex, hippocampus and striatum; a significant inhibition was also found in these same brain areas of aged (14 months) mice after acute administration of POEE (100 mg/kg ip). We propose that such AChE inhibitory activity is a neurochemical correlate of a number of therapeutic properties traditionally claimed for P. olacoides, particularly those associated with cognition.