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Psychopharmacological properties of Ptychopetalum olacoides BENTHAM (Olacacea)
Pharmaceutical Biology
Abstract
Roots of Ptychopetalum olacoides Bentham (Olacaceae), known as Marapuama, are prepared in alcoholic infusion for treating “nervous weakness” by Amazonian Caboclos. “Nervous weakness” can be described as a syndrome having several symptoms, among which the following are emphasized: lassitude, depression, sexual impotence and tremors. Based on ethnopharmacological data, we have considered the hypothesis that PO may have psychopharmacological effects, by interacting with different neurotransmitter systems: (i) the dopaminergic system, considering its use as an appetite modulator and to counteract tremors, as well as for its alleged sexual arousing properties; (ii) the noradrenergic system, again for its use against tremors and/or depression; and/or (iii) the serotonergic system, also related to depression and sexual arousal. This paper reports that P. olacoides hydroalcoholic extract potentiated yohimbine-induced lethality, rever sed reserpine-induced ptosis and prevented apomorphine-induced stereotypy. The data indicates that P. olacoides has central nervous system effects and supports the hypothesis of its interaction with dopaminergic and/or noradrenergic systems.
... Although, the potentiation of yohimbine-induced lethality in aggregated mice is not commonly used today, it still serves as an additional animal model for the routine screening of compounds with antidepressant activity. Yohimbine, an alkaloid, obtained from Pausinystalia yohimbe have been reported to induce lethality in grouped mice through the release of catecholamines from the brain and adrenal glands as consequence of antagonism of presynaptic α 2 -adrenergic receptors [27][28][29]. In addition, antagonism of presynaptic α 2adrenergic receptors has been reported to promote the release of serotonin, which further contributes to the overall toxicity caused by yohimbine [27,29]. ...
... Yohimbine, an alkaloid, obtained from Pausinystalia yohimbe have been reported to induce lethality in grouped mice through the release of catecholamines from the brain and adrenal glands as consequence of antagonism of presynaptic α 2 -adrenergic receptors [27][28][29]. In addition, antagonism of presynaptic α 2adrenergic receptors has been reported to promote the release of serotonin, which further contributes to the overall toxicity caused by yohimbine [27,29]. The excess amounts of these amines have been implicated in yohimbine toxicity in aggregated mice [22]. ...
... The excess amounts of these amines have been implicated in yohimbine toxicity in aggregated mice [22]. Compounds with antidepressant property have been reported to potentiate the lethal effect of yohimbine by enabling the amines to reach the receptor sites in greater amounts, either by inhibiting their reuptake or by reducing their metabolic degradation [22,27,29]. The finding that CC potentiated the lethal effect of yohimbine further suggests antidepressant property. ...
Objectives Depression is a complex neuropsychiatric disorder, which affects the quality of life of the sufferers and treatment approach is associated with serious adverse effects and sometimes therapeutic failures. Cymbopogon citratus leaf (CC) has been reported to exert anti-depressant effect but its mechanism of action is yet to be elucidated hence, the need for this study.
Methods The anti-depressant-like effect of Cymbopogon citratus aqueous leaf was evaluated using forced swim test (FST), tail suspension test (TST) and yohimbine-induced lethality test (YLT) in aggregated mice. Interaction studies involving p-chlorophenylalanine (pCPA), an inhibitor of serotonin biosynthesis and yohimbine, α2-adrenergic receptor antagonist were carried out to evaluate the role of monoaminergic system in the anti-depressant-like effect of CC. The effect of CC on spontaneous motor activity (SMA) was also assessed using activity cage.
Results Cymbopogon citratus (25 and 50 mg/kg, p.o.) demonstrated antidepressant-like activity devoid of significant stimulation of the SMA in mice. However, the antidepressant-like property of CC was significantly (p<0.05) attenuated by pretreatment with yohimbine suggesting involvement of noradrenergic pathway in the action of the extract. Also, pCPA reversed the anti-immobility effect of CC, indicating the role of serotonergic system in the mediation of its antidepressant activity. Moreover, CC (25 and 50 mg/kg) potentiated the lethal effect of yohimbine in aggregated mice, which further suggest the involvement of monoaminergic systems in its action.
Conclusions The results of the study showed that C. citratus might be interacting with serotonergic and noradrenergic pathways to mediate its anti-depressant-like effect in mice.
... It is popularly known as muirapuama, marapuama, and miratã. The traditional use of alcoholic infusions of the roots and ethanolic extracts of P. olacoides (EEPO) suggests the presence of bioactive compounds that could present interactions with the dopaminergic system, that is, presenting aphrodisiac, antidepressant, antitremor, and appetite modulatory characteristics, among others [1]. ...
... Several muirapuama-based products are easily found in the market in different formulations such as powders, capsules, tinctures, and extracts mixture. For these formulations, different forms of plant preparation are used [1]. ...
This work reports on the preparation of a drying process from the ethanolic extract of Muirapuama and its characterization through green analytical techniques. The spray-drying processes were performed by using ethanolic extract in a ratio of 1:1 extract/excipient and 3 2 factorial design. The properties of dried powder were investigated in terms of total flavonoid content, moisture content, powder yield, and particle size distribution. An analytical eco-scale was applied to assess the greenness of the developed protocol. Ultra-high performance liquid chromatography (UHPLC)with reduced solvent consumption in the analysis was compared to the conventional HPLC method. A Fourier transform near-infrared (FT-NIR) spectroscopic method was applied based on the principal component scores for the prediction of extract/excipient mixtures and partial least squares regression model for quantitative analysis. NIR spectroscopy is an economic, powerful, and fast methodology for the detection of excipient in muirapuama dried extracts, generating no residue in the analysis. Scanning electron microscopy (SEM) images showed samples with a higher concentration of excipient, presenting better morphological characteristics and a lower moisture absorption rate. An eco-scale score value of 85 was achieved for UHPLC and 100 was achieved for NIR (excellent green analysis). Above all, these methods are rapid and green for the routine analysis of herbal medicines based on dried extracts.
... The potential efficacy of these extracts is based on their phytochemical composition, as there is a synergic effect of their components (flavonoids, alkaloids, tannins, aromatic oils, saponins, terpenes, steroids, fatty resins, behenic acid and lupeol) [12,13] which have been shown to have lipolytic action and prevent gynoid lipodystrophy [14]. Ptychopetalum olacoides Bentham, known as Marapuama (and/ or Muirapuama and Mirantã among others) in Brazil, contains alkaloids, phenolic compounds, tannins, saponins, flavonoids and terpenic compounds in the roots [15]. Because of their composition, Trichilia catigua A. Juss and Ptychopetalum olacoides Bentham extracts have the potential to improve cellulite appearence. ...
... Apresenta ação lipolítica e previne a hidrolipodistrofia ginóide [14]. Ptychopetalum olacoides Bentham conhecido como Marapuama (e/ou Muirapuama e Mirantã entre outros) no Brasil contém alcaloides, compostos fenólicos, taninos, saponinas, flavonoides e compostos terpênicos nas raízes [15]. Devido à sua composição, os extratos de Trichilia catigua A. Juss e Ptychopetalum olacoides Bentham apresentam potencial para melhorar o aspecto da celulite. ...
... The native communities have used its roots and barks as a treatment for depression, sexual dysfunction, and as a "nerve tonic" [259]. Roots are usually prepared in alcoholic infusion, but other formulations have also been employed (e.g., mixture of extracts, solutions, pills) [260]. ...
Sexual enhancers increase sexual potency, sexual pleasure, or libido. Substances increasing libido alter the concentrations of specific neurotransmitters or sex hormones in the central nervous system. Interestingly, the same pathways are involved in the mechanisms underlying many psychiatric and neurological disorders, and adverse reactions associated with the use of aphrodisiacs are strongly expected. However, sexual enhancers of plant origin have gained popularity over recent years, as natural substances are often regarded as a safer alternative to modern medications and are easily acquired without prescription. We reviewed the psychiatric and neurological adverse effects associated with the consumption of herbal aphrodisiacs Areca catechu L., Argemone Mexicana L., Citrus aurantium L., Eurycoma longifolia Jack., Lepidium meyenii Walp., Mitragyna speciosa Korth., Panax ginseng C. A. Mey, Panax quinquefolius L., Pausinystalia johimbe (K. Schum.) Pierre ex Beille, Piper methysticum G. Forst., Ptychopetalum olacoides Benth., Sceletium tortuosum (L.) N. E. Brown, Turnera diffusa Willd. ex. Schult., Voacanga africana Stapf ex Scott-Elliot, and Withania somnifera (L.) Dunal. A literature search was conducted on the PubMed, Scopus, and Web of Science databases with the aim of identifying all the relevant articles published on the issue up to June 2020. Most of the selected sexual enhancers appeared to be safe at therapeutic doses, although mild to severe adverse effects may occur in cases of overdosing or self-medication with unstandardized products. Drug interactions are more concerning, considering that herbal aphrodisiacs are likely used together with other plant extracts and/or pharmaceuticals. However, few data are available on the side effects of several plants included in this review, and more clinical studies with controlled administrations should be conducted to address this issue.
... Thus, the reversal of the locomotor decreasing effect and the potentiation of NIR and NIG actions of EETC by haloperidol in the OFT suggests that its neurobehavioral effect may be partly mediated via interaction with dopaminergic system; mechanism which might be related to enhancement of central GABAergic activity [22]. Also, yohimbine (α₂-noradrenergic receptor antagonist) and propranolol (βnoradrenergic receptor antagonist) are often used as a research tools for the elucidation of the possible involvement of noradrenergic pathway in the neurobehavioral effects of drugs [35,36]. Therefore, the blockades of anxiolytic, sedative or antidepressant property of test compounds by adrenergic antagonists (yohimbine, propranolol) serve as a pharmacological probe for the interaction of noradrenergic system [37]. ...
This study was carried out to investigate neurobehavioral properties and the underlying neural mechanisms of action of the ethanol extract of leaves of Triumfetta cordifolia (EETC) on behavioral models in mice. The acute toxicity test of EETC was assessed using Locke’s method. Thereafter, neurobehavioral property of EETC (4.4, 8.8 and 17.5 mg/kg) administered intraperitoneally (i.p.) was evaluated on novelty-induced rearing, grooming and locomotor using open-field test; cognitive enhancing effect was evaluated using Y-maze test. The anxiolytic and sedative effects were assessed using elevated-plus maze and hole board tests respectively. Moreover, the potential
underlying neural mechanisms of EETC was carried out using neurotransmitter receptor antagonists: haloperidol (0.2 mg/kg), yohimbine (1 mg/kg), propranolol (0.2 mg/kg), cyproheptadine (0.5 mg/kg) and atropine (0.5 mg/kg) on novelty-induced rearing, grooming, locomotor and hole board tests. Acute toxicity test carried out revealed the LD50 of the extract was estimated to be 282 mg/kg, i.p. EETC significantly (p < 0.05) reduced rearing, grooming and locomotor activity in the open-field test. Moreover, EETC reduced head dipping activity in the hole board test, suggesting sedation. EETC did not exhibit anxiolytic and memory enhancing effects in comparison to controls. Pretreatments with haloperidol, yohimbine, propranolol, cyproheptadine and atropine significantly potentiated the inhibitory effects of EETC on rearing and grooming, but reversed its effect on locomotion in the open-field test respectively. In conclusion, the findings suggest that EETC possesses central nervous system depressant activity and the effect might be related to modulation of dopaminergic, noradrenergic, serotoninergic and cholinergic neurotransmissions.
... Preliminary phytochemical screening of ethanol extract exhibited the presence of flavonoids, coumarin, amino acids, carbohydrates, and tannins which implies that this plant is rich in phenolic components. Plants with high flavonoid content have been traditionally used as cure for nervous disorders and now they have been identified as a new type of ligand with in vivo anxiolytic properties [24]. A report has suggested that neuroprotective action of flavonoids is highly enhanced by the general bioavailability of flavonoids, and particularly by their presence (in vivo) in the brain [25]. ...
Objective: Anxiety is one of the most common and serious mental illness affecting humankind and its extensiveness is on the rise at an alarming rate. Anxiolytic substances are highly acclaimed in the ranking of the most utilized drugs by human. The clinical applications of most widely used anxiolytic agents, that is, benzodiazepines are restricted by their undesirable side effects. Therefore, the development of new pharmacological agents for the treatment of this problem is well justified. Among medicinal plants, Melilotus officinalis (yellow sweet clover) has been recommended for relief of insomnia, convulsions, and as nervine tonic in traditional system of medicine. Nevertheless, no pharmacological studies have thus far evaluated its anxiolytic effect. Therefore, the aim of this study was to evaluate antianxiety effect of different extracts of M. officinalis in mice.Methods: The extracts of roots and aerial parts of the plant were prepared according to the polarity, that is, petroleum ether, chloroform, ethanol, and water. The anxiolytic effects of petroleum ether, chloroform, ethanol, and aqueous extract of aerial parts and roots of the plant (50, 100, and 200 mg/kg, p.o) were examined in albino mice using elevated plus maze (EPM) and mirror-chamber models of anxiety. High-performance thin layer chromatography (HPTLC) studies were carried out using toluene: Acetone: Formic acid as mobile phase.Results: Various extracts prepared from roots did not produce significant effect in both the models, whereas the ethanol extract prepared from aerial parts at 100 and 200 mg/kg showed a significant anxiolytic effect as compared to control and standard group. The petroleum ether, chloroform, and water extracts (50, 100, and 200 mg/kg) of the aerial parts of the plant did not produce meaningful effects in this study. HPTLC analysis of the ethanol extract revealed the presence of nine components.Conclusion: These results suggest that the ethanol extract of aerial parts of M. officinalis plant has statistically significant dose-dependent antianxiety activity which can be attributed to the presence of coumarin, and flavonoid compounds in it.
Aphrodisiacs, libido or erection-enhancing supplements are widely available on the internet. The beneficial effects are controversial. Forensic toxicologists should be aware of the potential toxicities of these products because they could be given in cases of drug-facilitated sexual assault. This article presents a case report in which the defendant claimed to have administered an aphrodisiac to several women who showed strong symptoms of intoxication after consumption in an alcoholic drink. A literature research was carried out for potential substances sold in these aphrodisiac products. Synthetic substances as well as products of herbal or animal origin can be the ingredients. The main products that could cause intensive side effects and intoxication are phosphodiesterase V inhibitors (declared or undeclared on packaging), yohimbine, steroid hormones, flibanserin, gamma-hydroxybutyric acid, Tribulus terrestris, Bufo Toad, Spanish fly or Horny Goat Weed. All other products used as aphrodisiacs and described herein show less potential side effects or no studies on side effects in humans were carried out.
The Ptychopetalum olacoides Benth. (Olacaceae) is an Amazonian tree popularly known as muirapuama or marapuama, among other names, which is used for several central nervous system related problems. The roots and occasionally the bark roots are the main medicinal parts employed and are prepared as an alcoholic infusion, tinctures, and tea. Phytochemical studies revealed that the roots contain tannins, flavonoids, and several terpenoids, while the presence of alkaloids is not clear. Most studies used ethanolic or hydroalcoholic extracts prepared with the roots of the plant. These studies indicate that the species has promising potential for treating central nervous system disorders, acting as an antidepressant, an anti-stress, a neuroprotective agent, and improving cognition. Although some herbal products contain P. olacoides in their composition, clinical studies are still needed to confirm the effects observed in pre-clinical studies.
Small molecule natural products (NPs) have a long and successful track record of providing first-in-class drugs and pharmacophore (scaffolds) in all therapeutic areas, serving as a bridge between modern and traditional medicine. This trajectory has been remarkably successful in three key areas of modern therapeutics: cancers, infections and CNS diseases. Beginning with the discovery of morphine 200 years ago, natural products have remained primary source of new drugs/scaffolds for CNS diseases. In this perspective, we address the question; why are majority of active compounds in the CNS domain natural products? Our analysis indicates that ~84% approved drugs for CNS diseases are NPs or NP-inspired, and interestingly, 20 natural products provided more than 400 FDA approved CNS drugs. We have discussed unique physicochemical properties of NPs and NP-inspired vis-à-vis synthetic drugs, isoform selectivity, evolutionary relationship providing rationale for increasing focus on natural product driven discovery for next generation drugs for neurodegenerative diseases.
Ptychopetalum olacoides is a folk medicinal plant for health care in market, especially in Brazil. Fourteen known compounds were isolated from P. olacoides and their chemical structures were elucidated by extensive spectroscopic data, including 1D NMR, 2D NMR, UV, IR and HR-ESI-MS. The 14 known compounds were identified as N-trans-feruloyl-3,5-dihydroxyindolin-2-one (1), magnoflorine (2), menisperine (3), 4-coumaroylserotonin (4), moschamine (5), luteolin (6), 4′-methoxyluteolin (7), 3-methoxyluteolin (8), 3, 7-dimethoxyluteolin (9), caffeic acid (10), ferulic acid (11), vanillic acid (12), syringic acid (13) and ginsenoside Re (14). To our knowledge, compounds (1–6, 13–14) were isolated from the plant for the first time. Additionally, quantitative analysis results indicated that calibration equations of compounds (1–3, 6, 9, 11–13) exhibited good linear regressions within the test ranges (R² ≥ 0.9990) and magnoflorine and menisperine were the major constituents in the barks of P. olacoides. The contents of magnoflorine and menisperine accounted for 75.96% of all analytes. However, the content of phenolic components was smaller and the highest content was no more than 1.04 mg/g. Collectively, these results suggested that alkaloids are the dominant substances in P. olacoides, which can make a difference for the quality control and further use of P. olacoides.
A collection of traditional medicine substances have been used as tonics or stimulants by indigenous people of Brazil for thousands of years. Since such substances may represent a source of potentially active drugs for treating various mental diseases, natural products used by the Caboclos, a population native to the Amazon, were reviewed. Special attention has been paid to Chaunochiton kappleri (Sagot ex Engler) Ducke, a species observed in the upland rain forests and savanna forests in the Brazilian portion of Amazonia. This plant, considered highly effective, is used as treatment for "nerve weakness," a traditional syndrome that resembles depressive disorders.
The term adaptogen has not yet been accepted in medicine. This is probably due to the difficulties in discriminating adaptogenic drugs from immunostimulators, anabolic drugs, nootropic drugs, and tonics. There can be not doubt, however, that, at least in animal experiments, there are plant drugs capable of modulating distinct phases of the adaptation syndrome as defined by Seyle. These drugs either reduce stress reactions in the alarm phase or retard / prevent the exhaustion phase and thus provide a certain degree of protection against long-term stress. The small number of drugs the antistress activity of which has been proven or reported includes, among others, the plant drugs Ginseng, Eleutherococcus, Withania, Ocimum, Rhodiola, and Codonopsis. This review summarizes the major findings of pharmacological tests and human studies carried out with these drugs. Currently used assay systems allowing detection of antistress activities are also reported. At present the most likely candidates responsible for the putative antistress activity of plant drugs are special steroids, phenylprogane compounds and lignanes, respectively. Apart from influencing activities of the pituitary-adrenal axis and inducing stress proteins, many adaptogens also possess immunomodulatory and / or anabolic activities.
The ability of antidepressant agents to potentiate the lethal or toxic effects of yohimbine in mice was evaluated. With very few exceptions, the antidepressants were the only agents that significantly enhanced yohimbine-induced lethality. All of the clinically effective antidepressants, both typical (e.g., amine reuptake inhibitors, monoamine oxidase inhibitors) and atypical (e.g., mianserin, iprindole, bupropion, quipazine) drugs, produced a dose-related potentiation of yohimbine in mice. Representative anxiolytics and antipsychotics failed to potentiate yohimbine over a wide range of doses. Although several possible “false positives” (e.g., atropine, chlorpheniramine, and d-amphetamine) would be detected in this procedure, these same agents would be detected in other models (e.g., tetrabenazine antagonism, behavioral despair) considered predictive of antidepressant potential. Thus, the potentiation of yohimbine-induced lethality test in mice appears to represent a useful screening procedure for discovering potential antidepressant drugs.
The pathophysiology of major affective illness is poorly understood. However, several lines of preclinical and clinical evidence indicate that an enhancement of 5-HT-mediated neurotransmission might underlie the therapeutic effect of most antidepressant treatments. This net effect would, however, be obtained via different mechanisms. A better understanding of the neurobiological basis for the delayed onset of action of antidepressant treatments has led to the elaboration of strategies that could accelerate the antidepressant response. These strategies are discussed in this article by Pierre Blier and Claude de Montigny.
Incluye un Database Manual of Biologically active phytochemicals and their activities Incluye bibliografía