[Show abstract][Hide abstract] ABSTRACT: GC/MS/FID analyses of volatile compounds from cladodes and inflorescences from male and female specimens of Baccharis trimera (Less.) DC. collected in the states of Paraná and Santa Catarina, Brazil, showed that carquejyl acetate was the primary volatile component (38% to 73%), while carquejol and ledol were identified in lower concentrations. Data were subjected to hierarchical cluster analysis and principal component analysis, which confirmed that the chemical compositions of all samples were similar. The results presented here highlight the occurrence of the same chemotype of B. trimera in three southern states of Brazil.
Química Nova 12/2012; 36(8):1096-1100. · 0.66 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Objective
To further characterize the acetylcholinesterase inhibitors (AChE-Is) pattern of Ptychopetalum olacoides ethanol extract (POEE) on the cytosolic globular monomer (G1) and membrane bound globular tetramer (G4) AChE isoforms in brain areas relevant for cognition.Methods
The G1 and G4 AChE isoforms were prepared according to the reported methods and the determination of AChE activity used was adapted from colorimetric method.ResultsPOEE mostly inhibited G1 in hippocampus (75%), and G4 in frontal cortex (58%) and striatum (75%) (P < 0.05). Kinetic analysis indicated that POEE-induced AChE inhibition in hippocampus was of a competitive nature for G1 but uncompetitive for G4.Conclusion
Considering the high density of cholinergic projection to the cortex and striatum, and the usefulness of conserving cytosolic acetylcholine to replenish synaptic vesicles in a highly active cognition site such as hippocampus, we argue that this could be a desirable profile for a clinically relevant AChE-I.
[Show abstract][Hide abstract] ABSTRACT: Essential oils (EOs) have been reported to possess pharmacological properties, of which those related to the central nervous system have been especially attributed to mono- and sesquiterpenes. Baccharis uncinella DC. (Asteraceae) is used by the Laklaño Indians (Santa Catarina, Brazil) for sedative purposes. Interestingly, the species does not seem to be used medicinally elsewhere in Brazil.
This study was designed to compare the composition and sedative properties of B. uncinella EOs obtained closer (BU-SC) and farther (BU-PR) to the Laklaño Indian Reserve.
BU-SC and BU-PR obtained by hydrodistillation were analyzed by CG-MS. Mice treated with BU-SC and BU-PR (50 and 100 mg/kg) were evaluated regarding pentobarbital-induced sleeping time, body temperature, and locomotion. Results: BU-SC presents a higher monoterpene/sesquitherpene ratio (0.31); α-pinene (6.42%), limonene (7.21%), caryophyllene (26.13%), spathulenol (13.39%) and caryophyllene oxide (13.26%) were identified as major components. BU-PR presents a low monoterpene/sesquitepene ratio (0.004); spathulenol (32.93%), caryophyllene oxide (27.78%), viridiflorol (5.29%) and α-cadinol (2.42%) were identified as the main components. Both samples significantly (p < 0.05, ANOVA) decreased locomotion and body temperature, as well as increased sleeping time. The hypnotic activity was sensitive to the differences in monoterpene composition.
In comparison with a sample collected in Paraná State, B. uncinella EO collected closer to the Laklaño Indians possess a composition that better justifies the claimed sedative properties. The study confirms the value of traditional information to guide bioactivity assessment in medicinal plants, and gives notice to the ecological factors that can interfere with the conclusions of such assessments.
[Show abstract][Hide abstract] ABSTRACT: This study aimed to evaluate the gastroprotective mechanism of action of the essential oil of Croton cajucara Benth. (Euphorbiaceae) stem bark in ethanol-induced gastric ulcers and its in vitro anti-Helicobacter pylori activity. The involvement of heat-shock protein-70, vasoactive intestinal peptide, glutathione, nitric oxide, and nonprotein sulfhydryl compounds in the gastroprotective effect was determined in male Wistar rats. The minimum inhibitory concentration against H. pylori was determined in vitro. The results were analyzed by analysis of variance followed by the Dunnett test, and a P value less than 0.05 was considered to represent a statistically significant difference. C. cajucara decreased ethanol-induced ulcer area in 100% of ulcers and decreased the histologic lesions. In the C. cajucara group, the area marked by heat-shock protein-70 was significantly higher than the area in the control group; this finding was not seen for vasoactive intestinal peptide. C. cajucara could not maintain glutathione levels close to those in the sham group. The gastric ulcer area of rats treated with the sulfhydryl compound blocker was decreased, but the ulcer area of rats treated with nitric oxide synthase inhibitor showed no alteration. The minimum inhibitory concentration obtained for C. cajucara was 125 μg/mL. These findings suggest that sulfhydryl compounds and heat-shock protein-70, but not nitric oxide, glutathione, or vasoactive intestinal peptide, are involved in the C. cajucara gastroprotective effect against ethanol-induced gastric ulcers.
Journal of medicinal food 04/2011; 14(9):1011-7. · 1.39 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Alzheimer's disease (AD) is expected to affect more than 22 million people worldwide by 2025, causing devastating suffering and enormous costs to families and society. AD is a multifactorial disease, with a complex pathological mosaic. In rodents, AD-like dementia can be induced by cerebral microinjection of Aβ peptide, leading to amyloid deposits, amnesia and various features of neurodegeneration. Marapuama (Ptychopetalum olacoides) is regarded as a "brain tonic" in the Amazon region and shows a nootropic profile in rodents.
Because a specific extract (POEE) of Marapuama was shown to possess promnesic and anti-amnesic properties, the aim of this study was to verify if POEE is also effective against Aβ(1-42)-induced cognitive deficit in mice. Additionally, Aβ deposits (Congo red), GFAP immunoreactivity (immunohistochemistry), and neurodegenerative changes in the hippocampal pyramidal layer (Nissl) were examined as measures of Aβ(1-42)-induced neurodegeneration.
CF1 mice were subjected to the experimental Alzheimer model with the Aβ(1-42) i.c.v. administration. The effects of POEE 800 mg/kg were evaluated over 14 consecutive days of treatment.
The data show that 14 days of oral treatment with POEE (800 mg/kg) was effective in preventing Aβ-induced cognitive impairment, without altering the levels of BDNF and with parallel reductions in Aβ deposits and astrogliosis. CA1 hippocampus loss induced by Aβ(1-42) was also diminished in POEE-treated mice.
This study offers evidence of functional and neuroprotective effects of two weeks treatment with a Ptychopetalum olacoides extract against Aβ peptide-induced neurotoxicity in mice. Given the multifactorial nature of neurodegeneration, the considerable potential for an AChE inhibitor displaying associated neuroprotective properties such as here reported warrants further clinic evaluation.
Phytomedicine: international journal of phytotherapy and phytopharmacology 02/2011; 18(4):327-33. · 2.97 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: The goal of acetylcholinesterase inhibitors (AChEIs) used to treat Alzheimer's patients is an improvement in cholinergic transmission. While currently available AChEIs have limited success, a huge impediment to the development of newer ones is access to the relevant brain areas. Promnesic, anti-amnesic and AChEI properties were identified in a standardized ethanol extract from Ptychopetalum olacoides (POEE), a medicinal plant favored by the elderly in Amazon communities. The purpose of this study was to provide conclusive evidence that orally given POEE induces AChE inhibition in brain areas relevant to cognition. Histochemistry experiments confirmed that the anticholinesterase compound(s) present in POEE are orally bioavailable, inducing meaningful AChE inhibition in the hippocampus CA1 (∼33%) and CA3 (∼20%), and striatum (∼17%). Ellman's colorimetric analysis revealed that G1 and G4 AChE isoforms activities were markedly inhibited (66 and 72%, respectively) in hippocampus and frontal cortex (50 and 63%, respectively), while G4 appeared to be selectively inhibited (72%) in the striatum. Western blotting showed that POEE did not induce significant changes in the AChE immunocontent suggesting that its synthesis is not extensively modified. This study provides definitive proof of meaningful anticholinesterase activity compatible with the observed promnesic and anti-amnesic effects of POEE in mice, reaffirming the potential of this extract for treating neurodegenerative conditions where a hypofunctioning cholinergic neurotransmission is prominent. Adequate assessment of the safety and efficacy of this extract and/or its isolated active compound(s) are warranted.
Phytomedicine: international journal of phytotherapy and phytopharmacology 10/2010; 17(12):956-62. · 2.97 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: With the recognition that high levels of sustained stress are associated with the natural course of countless illnesses, effective anti-stress agents have gained importance. Improved endurance to particularly stressful periods is one of the medicinal claims for Marapuama (Ptychopetalum olacoides Bentham, PO), a popular Amazonian herbal. The purpose of this study was to evaluate if PO possesses anti-stress properties. To this end, an extract from PO (POEE) was evaluated on anxiety and glucose levels in mice submitted to the unpredictable chronic mild stress (UCMS) paradigm. POEE did not present anxiolytic effects, but was able to prevent (p<0.01) the UCMS-induced anxiety as assessed by the light/dark test (time spent in the lit area, POEE 100 and 300mg/kg 235.9+/-20.6s and 250.4+/-17.4s, respectively, compared to DMSO 104.7+/-24.4s). Likewise, although POEE did not induce noticeable effects on glycemia, it effectively (p<0.01) prevented the UCMS-induced hyperglycemia (POEE 100 and 300mg/kg 106.4+/-6.7mg/dl and 107.3+/-3.3mg/dl, respectively, compared to DMSO 134.6+/-5.9mg/dl). Additionally, POEE (50-200mg/kg i.p. and 800mg/kg p.o.) significantly (p<0.01 and p<0.05, respectively) increased the time to hypoxia-induced convulsion (by 38%, 51%, 59% and 27%, respectively for i.p. and p.o. treatments). The data indicate that POEE counteracts some of the effects brought about by chronic stress. This study combined with the identified antioxidant and neuroprotective properties, as well as the claimed benefits associated with stressful periods suggest that Ptychopetalum olacoides (Marapuama) might possess adaptogen-like properties.
Phytomedicine: international journal of phytotherapy and phytopharmacology 09/2009; 17(3-4):248-53. · 2.97 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Depression has become of universal major importance, and it is therefore vital to expand the armamentarium for treating the condition. Lack of motivation and lassitude are major symptoms treated with the use of Marapuama (Ptychopetalum olacoides, PO) remedies by communities in the Brazilian Amazon. Considering the prominence of such symptoms in depression, the present study was designed to verify the effects of a standardized PO ethanol extract (POEE) on the forced swimming (FST) and tail suspension tests (TST). POEE i.p. (15-100 mg/kg) and oral (300 mg/kg) resulted in a significant and dose-related anti-immobility effect. We further examined the involvement of dopamine, noradrenaline and serotonin in these antidepressant-like effects. POEE effects were prevented when catecholamine synthesis was inhibited by -alpha-methyl-rho-tyrosine (AMPT) (100 mg/kg, i.p.), while inhibition of serotonin synthesis with rho-chlorophenylalanine methyl ester hydrochloride (PCPA) (100 mg/kg, i.p.) was devoid of effect. The blockade of beta-adrenergic (propranolol 2 mg/kg, i.p.) and D(1) dopamine (SCH 23390 0.5 mg/kg, i.p.) receptors prevented POEE anti-immobility effects; by contrast, blockade of D(2) dopamine (sulpiride 2 and 50 mg/kg, i.p.) receptors was ineffective. Consistent with traditional use, the results indicate that POEE possesses antidepressant-like effects, possibly mediated by beta-adrenergic and D(1) dopamine receptors.
Phytotherapy Research 04/2009; 23(4):519-24. · 2.40 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: 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.
Phytomedicine: international journal of phytotherapy and phytopharmacology 10/2008; 16(4):303-7. · 2.97 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Alcohol infusions of roots from Ptychopetalum olacoides Bentham (PO; Olacaceae) have been used for treating many diseases in which free radicals are likely to be implicated. Of particular interest are the uses amongst the elderly (to ameliorate cognitive functions), and by patients recovering from pathologies associated with damage to the central nervous system (such as stroke). The aim of this study was to evaluate the antioxidant properties of a PO ethanol extract (POEE) by using various in vitro systems. POEE acted as a scavenger of nitrogen oxides as well as superoxide generated by the xanthine-xanthine oxidase system. The extract also showed a high antioxidant capacity using a luminol chemiluminescence derived from a thermolabile diazocompound. We suggest that the therapeutic effects attributed to P. olacoides could be in part associated to its oxygen free radical scavenging capacity.
[Show abstract][Hide abstract] ABSTRACT: 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)].
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.
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.
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.
[Show abstract][Hide abstract] ABSTRACT: ETHNOPHARMACOLOGY RELEVANCE: Ptychopetalum olacoides Bentham (PO) (Olacaceae), known as Marapuama, is regarded as a "nerve tonic" in the Amazon. Traditional uses include states of lassitude with noticeable lack of desire/motivation, and to manage particularly stressful (physical and/or psychological) circumstances. Suggestive of antidepressant activity, we have established that a specific PO ethanol extract (POEE) significantly decreases immobility in the tail suspension and forced swimming tests.
The aim of this study was to verify the effects of POEE in the unpredictable chronic mild stress (UCMS) depression model in mice, given the construct and face values of the UCMS as an experimental model of depression and the traditional use of this species.
Over 6 weeks BALB/c mice were subjected to the UCMS protocol. The effects of POEE (50, 100, 300mg/kg, p.o.) and imipramine (20mg/kg, i.p.) were evaluated in relation to coat state, splash-test grooming, and corticosterone levels.
The coat state degradation, decreased grooming and increased serum corticosterone induced by UCMS were prevented by POEE and imipramine treatments.
In addition to supporting traditional claims and previously reported antidepressant properties for POEE, this study shows that POEE prevents stress-induced HPA hyperactivity.
Journal of Ethnopharmacology 08/2008; 118(2):300-4. · 2.94 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: 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.
[Show abstract][Hide abstract] ABSTRACT: Ptychopetalum olacoides (PO) roots are used by Amazonian peoples to prepare traditional remedies for treating various central nervous system conditions in which free radicals are likely to be implicated. Following the identification of PO ethanol extract (POEE) free-radical scavenging properties in vitro, the aim of this study was to verify the in vivo antioxidant effect of POEE. Aging mice (14 months) were treated (i.p.) with saline, DMSO (20%) or POEE (100mg/kg body wt.), and the hippocampi, cerebral cortex, striata, hypothalamus and cerebellum dissected out 60 min later to measure antioxidant enzyme activities, free-radical production and damage to macromolecules. POEE administration reduced free-radical production in the hypothalamus, lead to significant decrease in lipid peroxidation in the cerebral cortex, striatum and hypothalamus, as well as in the carbonyl content in cerebellum and striatum. In terms of antioxidant enzymes, catalase activity was increased in the cortex, striatum, cerebellum and hippocampus, while glutathione peroxidase activity was increased in the hippocampus. This study suggests that POEE contains compounds able to improve the cellular antioxidant network efficacy in the brain, ultimately reducing the damage caused by oxidative stress.
[Show abstract][Hide abstract] ABSTRACT: Homemade remedies with Ptychopetalum olacoides (PO) roots are used by Amazonian peoples for treating various age-related conditions. We previously reported that Ptychopetalum olacoides ethanol extract significantly improved step-down inhibitory avoidance long-term memory in adult and reversed memory deficits in aging mice. Adding to previous data, this study shows that a single i.p. administration of Ptychopetalum olacoides ethanol extract (POEE 50 and 100 mg/kg) improved step-down inhibitory avoidance short-term memory (STM) 3 h after training in adult (2.5 month) mice; comparable results were obtained with POEE given p.o. at 800 mg/kg. Moreover, memory improvement was also observed in aging (14 months) mice presenting memory deficit as compared to adult mice. Furthermore, POEE (100 mg/kg) improved non-aversive memory systems in adult mice in an object recognition paradigm. Consistently with its traditional use this study add to previously reported data and reinforces that POEE facilitates memory processes. Although the acetylcholinesterase inhibitory properties described for this extract may be of relevance for improving memory processes, the molecular mechanism(s) underlying the memory improvement here reported needs further scrutiny.
Journal of Ethnopharmacology 03/2007; 109(3):449-57. · 2.94 Impact Factor
[Show abstract][Hide abstract] ABSTRACT: Amazonian peoples use traditional remedies prepared with Ptychopetalum olacoides (PO) roots for treating various age-related conditions. This study shows that a single intraperitoneally (i.p.) administration of Ptychopetalum olacoides ethanol extract (POEE, 50 and 100mg/kg) improved memory retrieval in step-down inhibitory avoidance (P <or= 0.05 and P <or= 0.01, test session latency 102 [19.38-300] and 192 [91.3-300]s, respectively versus control 24.7 [12.9-89.6]), without interfering with acquisition or consolidation in adult (2.5-month-old) mice. Comparable results were obtained with POEE given p.o. at 800 and 1000mg/kg (P <or= 0.05 and P <or= 0.01, 52.7 [19.5-297.2] and 85.7 [44.4-260.4] versus control 20.5 [8-92.6]). Moreover, memory amelioration was also observed (P <or= 0.01) in aging (14 months) mice presenting memory deficit (14.95 [10.8-41]) as compared to adult (2.5 months) mice (57 [15.7-141.2]), with the extract given acutely i.p. 100 mg/kg (300 [133.1-300] versus control 14.95 [10.8-41]) or p.o. 800 mg/kg (28.4 [15.1-84.6] versus control 11.5 [7.8-23.3]). Indeed, aging mice treated with POEE (800 mg/kg, p.o.) performed as well as adult mice. Consistently with its traditional use, the data suggest that POEE facilitates memory retrieval. Although the antioxidant and acetylcholinesterase inhibitory properties previously described for this extract may be of relevance, the molecular mechanism(s) underlying the improvement in memory retrieval here reported merit further scrutiny.
Journal of Ethnopharmacology 01/2005; 95(2-3):199-203. · 2.94 Impact Factor