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Anxiogenic properties of Ptychopetalum olacoides Benth. (Marapuama)


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Alcohol infusions of roots of Ptychopetalum olacoides Benth. (PO), known as Marapuama or Muirapuama, are used in the Brazilian Amazon as a 'nerve tonic'. Over the years PO has been found increasingly in phytoformulations and regarded as a stimulant, claimed to enhance physical and mental performances. This study determined that a P. olacoides ethanol extract (30, 100 and 300 mg/kg) decreased exploratory behaviour in the hole-board test, without interfering with locomotion or motor coordination (rota-rod test). The data are comparable to that obtained with pentylenetetrazol (40 mg/kg), suggesting an anxiogenic effect of P. olacoides.
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Anxiogenic Properties of Ptychopetalum
olacoides Benth. (Marapuama)
A. L. da Silva,
S. Bardini,
D. S. Nunes
and E. Elisabetsky
Curso de Po´s Graduac¸a
ˆncias Biolo´gicas-Bioquı´mica, Universidade Federaldo Rio Grande do Sul, Av. Ramiro Barcelos 2600,
90035-003, Porto Alegre, RS, Brazil
Laborato´rio de Etnofarmacologia, ICBS, Universidade Federal do Rio Grande do Sul, Av. Sarmento Leite 500/202, 90046-900, Porto
Alegre, RS, Brazil
Departamento de Quı´mica, Universidade Estadual de Ponta Grossa, Campus Uvaranas, Bloco M, 84030-310, Ponta Grossa, PR, Brazil
Alcohol infusions of roots of Ptychopetalum olacoides Benth. (PO), known as Marapuama or Muirapua-
ma, are used in the Brazilian Amazon as a ‘nerve tonic’. Over the years PO has been found increasingly
in phytoformulations and regarded as a stimulant, claimed to enhance physical and mental perfor-
mances. This study determined that a P. olacoides ethanol extract (30, 100 and 300mg/kg) decreased
exploratory behaviour in the hole-board test, without interfering with locomotion or motor coordination
(rota-rod test). The data are comparable to that obtained with pentylenetetrazol (40 mg/kg), suggesting
an anxiogenic effect of P. olacoides. Copyright #2002 John Wiley & Sons, Ltd.
Keywords: Ptychopetalum olacoides; Marapuama; Muirapuma; anxiogenic; hole-board; rota-rod.
Ethnopharmacological studies indicate that Amazonian
‘caboclos’ (Amazonian native rural inhabitants) use an
alcohol infusion of the roots of Ptychopetalum olacoides
Benth. (PO) (Olacacea), known as Marapuama, as a
‘nerve tonic’, aphrodisiac, appetite modulator and as an
anti-tremor agent (Elisabetsky, 1987; Grenand et al.,
1987). The concept of a ‘nerve tonic’ has been discussed
in detail elsewhere (Elisabetsky et al., 1992); relevant to
this study is to mention that the use of a ‘nerve tonic’
includes recovery of cognitive and motor functions after
brain injuries (such as stroke), and cognition improve-
ment (including alertness and memory) in the elderly. P.
olacoides is currently present in herbal products in
several American and European countries (Table 1).
Although little is known about the chemistry or
pharmacology of this species (Paiva et al., 1998; Uber
Bucek et al., 1987), we previously reported that a PO
ethanol extract (POEE) potentiated yohimbine-induced
lethality, reversed reserpine-induced ptosis, and pre-
vented apomorphine-induced stereotypy in mice (Si-
queira et al., 1998). These data support the hypothesis of
a PO modulatory effect on brain functions, suggesting the
involvement of cateholaminergic transmission.
Considering the therapeutic claims of the marketed P.
olacoides formulations, the purpose of this paper was to
investigate the effects of P. olacoides ethanol extract in
the hole-board model (exploratory behaviour) and the
rota-rod test (motor coordination).
Material and Methods
Plant material. Roots of Ptychopetalum olacoides
Benth. (Olacaceae) were collected in the State of Para´,
Brazil, and identified by Nelson Rosa. Voucher speci-
mens were deposited at the herbarium of the Museu
Paraense Emilio Goeldi (MPEG 108.036). The collection
was authorized by CNPq and is in line with the Brazilian
policy regarding access to genetic resources.
Preparation of extract. Ptychopetalum olacoides etha-
nol extract (POEE) was prepared as detailed elsewhere
(Elisabetsky and Siqueira, 1998). Briefly, the dried roots
(2.5 kg) were peeled, ground and extracted with ethanol
(12 L), using a Soxhlet apparatus (40 h). The extract was
evaporated under reduced pressure resulting in the POEE
(150 g; 6% yield).
Animals. Experiments were performed with male adult
mice, CF1 strain, received from Fundac¸a
˜o Estadual de
˜o e Produc¸a
˜o da Sau
´de (FEEPS) immedi-
ately after weaning (21 days). Animals were maintained
in our own animal facilities under a controlled environ-
ment (22°1°C, 12 h light/dark cycle, free access to
food [Nuvilab CR1] and water) up to 10 weeks old
(25–40 g). All procedures were carried out according
to institutional policies on experimental animal hand-
Drugs. Diazepam and propylene glycol (PPG) were
acquired from Sigma; dimethyl sulphoxide (DMSO)
from Delaware and pentylenetetrazol (PTZ) from Knoll
A.G-Ludwingshafen/Rheno. Diazepam (0.5 mg/kg) was
suspended in propylene glycol 10% (v/v). POEE (30, 100
and 300mg/kg) was dissolved in DMSO 20%(v/v). PTZ
was dissolved in saline.
Phytother. Res. 16, 223–226 (2002)
Published online in Wiley InterScience ( DOI: 10.1002/ptr.825
Copyright #2002 John Wiley & Sons, Ltd.
* Correspondence to: Dr E. Elisabetsky, CP 5072, 90041-970, Porto Alegre,
RS, Brazil.
Contract/grant sponsor: FAPERGS; Contract/grant number: 98/1610-3.
Contract/grant sponsor: CNPq.
Contract/grant sponsor: CAPES.
Received 7 January 2001
Accepted 11 January 2001
Hole-board. The hole-board apparatus (Ugo Basile,
Italy) consisted of a grey Perspex panel (40 40
40 cm, 2.2 cm thick) with 16 equidistant holes (3 cm in
diameter) in the floor. Photocells below the surface of the
holes provided measures of the number of head-dips. The
board was positioned 15cm above the table and divided
(with black water-resistant marker) in 9 squares of
10 10cm. The method was adapted from Takeda et
al. (1998). Mice were transported to the dimly lit
laboratory at least 1 h prior to testing. Each animal was
individually placed in the centre of the board (facing
away from the observer) and the following parameters
were noted for 5 min: the latency to the first head-dip,
measured using a stopwatch; the number of rearings and
spontaneous movements (number of squares crossed
with all four paws). The animals were divided into eight
groups (15–30 animals) and treatments (saline, PPG,
DMSO, diazepam, POEE and PTZ) administered in-
traperitoneally (i.p, 10 mL/kg) 30 min prior to the
Rota-rod. The rota-rod apparatus (Ugo Basile, Italy)
consisted of a rotating bar which is suitably machined to
provide grip. Six flanges divide the bar, enabling five
mice to be at the treadmill simultaneously. Latency to fall
from the bar is automatically recorded in seconds. The
method was adapted from Dalmmeier and Carlini (1981).
Mice were initially selected for their ability to remain in
the rota-rod (18 rpm) for at least two of three consecutive
90 s trials. On the test day (24 h after selection), the
latency to fall from the rota-rod (one trial of 60 s) was
determined 30 and 60 min after treatments.
Statistical analysis. The results are expressed as mean
SEM, and were analysed by ANOVA followed by
Student–Newman–Keuls test.
The POEE (30,100 and 300 mg/kg) significantly reduced
the number of head-dips, as did PTZ (40 mg/kg) (Fig.
1A). POEE increased the latency to the first head-dip at
100 and 300 mg/kg (Fig. 1B), while reducing locomotion
only at 300 mg/kg (Fig. 1C). POEE significantly reduced
the number of rearings at 100 and 300 mg/kg (Fig. 1D).
Diazepam 0.5 mg/kg increased the number of head-dips
(Fig. 1A) and locomotion (Fig. 1C).
There were no deficits nor differences in the rota-rod
performance with any POEE doses, nor with DMSO
compared with saline (data not shown).
Anxiety, a symptom accompanying various central
nervous system disorders and a disorder by itself, is
characterized in humans by a tense and physically
Table 1. Some herbal products containing Ptychopetalum olacoides
Product Description of Contents Country Reference
X-Action Pack or Ptychopetalum olacoides (Muira puama) USA
Men X Action Pausinystalia yohimbe (yohimbe bark) /xaction.html
Damiana leaves
Oat straw leaves concentrate
Saw palmetto berries
Touch®re HIS Ptychopetalum olacoides (Potency Wood) USA
Juniperis brasiliensis (Catuaba) Canada /his®re.html
Turnera aphrodisiaca (Damiana)
Smilax papyracea (salsaparilla)
Urtica dioica (Nettle Root)
Doctor's Choice Essential vitamins and minerals USA
for Men Zingiber of®cinale (Ginger Root extract) /individual/eprod004.html
Camellia sinensis (Green Tea Extract)
Ptychopetalum olacoides (Muira puama extract)
Serenoa repens (Saw Palmeto extract)
Panax Ginseng (Korean Ginseng Root Extract)
Masculex Vitamin E USA
Ptychopetalum olacoides (Muira puama extract) /individual/eprod149.html
Turnera diffusa (Mexican Damiana leaves extract)
Serenoa repens (Saw Palmeto extract)
Cola nitida (Cola Nut extract)
Panax Ginseng (Korean Ginseng Root Extract)
Ginkgo biloba Extract
Potency Wood Ptychopetalum olacoides (Muira puama extract) USA
Marapuanatus Ptychopetalum olacoides (Marapuama extract) Brazil
Guaracola Paullinia cupana Brazil
Sterculia acuminata
Anemopaegma mirandum
Ptychopetalum olacoides
Copyright #2002 John Wiley & Sons, Ltd. Phytother. Res. 16, 223–226 (2002)
exhaustive alertness (Treit, 1985). Other animal species
display a variety of defensive reactions in response to
predators, some understood as animal correlates of
anxiety states (Rodgers et al., 1995). Rodents demon-
strate anxiety, fear and curiosity when placed in a new
environment, and an overall assessment of behaviour can
be determined by observing freezing, grooming (fear) or
rearing, head-dips (curiosity) and the number of faecal
pellets (stress) (File, 1987a; Kennedy, 1978; Dalvi and
Rodgers, 1999).
The so-called hole-board model has become increas-
ingly the most frequently used test to detect and evaluate
the anxiolytic/anxiogenic properties of drugs (File and
Wardill, 1975; Durcan and Lister, 1988; Moreira et al.,
1996; Takeda et al., 1998). The present study demon-
strated that the P. olacoides ethanol extract reduced the
number of head-dips and rearings, and increased the
latency to the first head-dip; these behaviour alterations
are compatible with the profile of anxiogenic drugs
(Moreira et al., 1996; Takeda et al., 1998). Accordingly,
pentylenetetrazol, a known anxiogenic agent, reduced the
number of head-dips.
A decrease in locomotion was observed only with the
highest POEE dose studied, and the extract did not induce
motor deficits in the rota-rod.
Changes in emotional states of animals are associated
with benzodiazepine and non-benzodiazepine associated
mechanisms. Yohimbine, an a
-adrenergic antagonist,
causes anxiety in humans, and in animal models (File,
1987b). Buspirona, a 5-HT
agonist, and ritanserine, a
antagonist, possess anxiolytic proprieties in the
human as well as animal models. Adrenocorticotrophic
hormone (ACTH) has anxiogenic effects in the social
interaction test, being antagonized by chlordiazepoxide
(File, 1987b).
In this study, diazepam (0.5 mg/kg) increased the
number of head-dips and locomotion, without interfering
with rearing. Takeda et al. (1998) reported that diazepam
increases head-dipping behaviour at doses similar to those
used in this study, but did not observe modifications in
locomotion or rearings. Nevertheless, several studies
reported that diazepam increased locomotor activity in
the open field (Bhattacharya and Mitra, 1991; Wieland et
al., 1991; Ramanathan et al., 1998). Moreover, increases in
the number of squares crossed in the open field and in head-
dips in the hole-board were obtained with desmethyldia-
zepam and chlordesmethyldiazepam (De Angelis et al.,
1982). Our results indicate that a non-sedative but
anxiolytic dose of diazepam facilitates exploratory beha-
viour, expressed in increased head-dips and locomotion.
The present results add to previously reported data
obtained with POEE (Elisabetsky and Siqueira, 1998)
indicating a central stimulant profile. An anxiogenic
effect is in line with traditional therapeutic claims for
Ptychopetalum olacoides, since moderate anxiogenesis is
associated with alertness and increased physical and
Figure 1. Effects of Ptychopetalum olacoides ethanol extract (POEE) in the hole-board test. Number of head-dips (A), latency for
the ®rst head-dip (B), number of squares crossed (C) and number of rearings (D). PTZ, pentylenetetrazol; PPG, Propylene glycol
10%; DZP, diazepam 0.5 mg/kg; DMSO, Dimethyl sulphoxide 20%. Each column represents the mean SEM. ANOVA * = p<0.05
and ** p<0.01 compared with saline.
Copyright #2002 John Wiley & Sons, Ltd. Phytother. Res. 16, 223–226 (2002)
psychological endurance (Jaffe, 1990). Further studies
are necessary to complete the psychopharmacological
profile of PO and unveil the mechanism(s) that underlie
the central effects of POEE.
This study was supported by FAPERGS (grant 98/1610.3), CNPq (EE)
and CAPES (ALS). Authors wish to thank Patricia Shanley for her
crucial assistance in collecting plant material.
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... which the root of the plant is macerated in an alcoholic spirit or wine and consumed daily before meals (Siqueira et al. 1998;Piato et al. 2010). The plant drug is part of many commercially available herbal products, either as a single constituent (Testor-Plus ® ) or in combination with other plants (Catuama ® , Herbal vX ® , Masculex ® ) (Vaz et al. 1997;Bonnard 1999;Waynberg and Brewer 2000;Da Silva et al. 2002). The plant drug also was part of a nervine tonic called Esthenol (Silva 1925), no longer found in the market. ...
... The psychopharmacological profile of the hydroalcoholic extract of the roots or rootbark indicated that the plant could interact with cholinergic, dopaminergic, and serotonergic systems (Siqueira et al. 1998). Da Silva et al. (2002) observed a moderate anxiogenic effect for doses from 30 to 300 mg/kg (ip) of muirapuama root ethanolic extract in the hole board test, without observing the decreased motor activity or motor incoordination in the rota-rod. The authors suggested that moderate anxiogenic action can be associated with the stimulating action of P. olacoides, contributing to an increased alertness as well as to physical and psychological resistance. ...
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.
... Infusões das raízes desta planta têm sido utilizadas para o tratamento de muitas doenças em que os radicais livres são susceptíveis de serem implicados. De particular interesse são os usos entre os idosos e por pacientes em recuperação de patologias associadas com danos ao sistema nervoso central (Silva, et al., 2002). ...
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A descoberta e o manejo de recursos naturais são essenciais no processo de desenvolvimento social. Por milhares de anos, a humanidade tem se utilizado de plantas com os mais diversos intuitos, como, por exemplo, para o alívio e a cura de enfermidades. A diversidade florística brasileira também possibilitou que as comunidades nativas adquirissem e desenvolvessem conhecimentos associados ao uso de inúmeros vegetais. Esta breve revisão da literatura tem por objetivo fazer um levantamento das propriedades de quatro espécies vegetais – guaraná (Paullinia cupana Kunth), marapuama (Ptychopetalum olacoides Benth.), genciana (Gentiana lutea L.), quassia (Quassia amara L.) – amplamente utilizadas pelos nativos da região amazônica, especialmente devido as suas propriedades terapêuticas. Destaca-se, por fim, a existência de grande potencial para o aprofundamento de pesquisas nas espécies vegetais revisadas, principalmente no que se refere ao uso fitoterápico – uma vez que essas tem mostrado, de acordo com fontes consultadas, auxiliar nos mais diversos quadros de saúde.
... In addition, higher doses, either acutely or subchronically (15 days), did not cause a worsening of adverse effects [263]. A few neurological side effects were reported in preclinical studies, including impairment of both shortand long-term memory and reduced locomotion [151,152] (Table 1). ...
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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.
... Several studies have provided evidence of the effects of this plant drug on the central nervous system. Initially it was found to show effects as an anxiogenic (Silva et al., 2002), anticholinesterase (Siqueira et al., 2003), neuroprotective (Siqueira et al., 2004), facilitation of memory recovery in young and old mice (Silva et al., 2004), antioxidant (Siqueira et al., 2007), antidepressant (Paiva et al., 1998;Piato et al., 2009), and anti-stress (Piato et al., 2010). Its aphrodisiac potential has not been confi rmed experimentally or clinically, although some of its effects, such as antidepressant and antioxidant activity, may improve sexual performance (Feldman et al., 1994). ...
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Croton echioides Baill., Euphorbiaceae, is a small tree found in Bahia, Northeastern Brazil. Its stem bark has been widely sold as an aphrodisiac and tonic, as a substitute for the roots of Ptychopetalum olacoides Benth. Olacaceae, the Amazon Muira Puama or Marapuama, and C. echioides is characterized as the "Northeastern Marapuama". This contribution describes a morphoanatomical analysis and pharmacognostic study of stem bark of this species. The stem has a thick cortex with compound starch grains and laticifers; a sclerenchymatic sheath which consists of brachysclereids with large crystals externally to the phloem, and abundant fiber in the secondary xylem, as the main features of the species. The data obtained for water content (9.26±0.07%), water-soluble extractives (3.92±0.19%), total ash (1.24±0.06%) and acid-insoluble ash (0.16±0.01%), together with the chromatographic profile obtained by TLC, contribute to the quality control and standardization for the plant drug. The pharmacological screening indicated LD50 values above 500 mg/kg orally and equal to 500 mg/kg by the i.p. route, as well as some stimulant potential, depending on the dose.
... The traditional uses of P. olacoides have been extensively exploited by herbal industries in several American and European countries, and the native herb or its extracts are constituents of various phytomedicines supplied in the form of pills, tinctures, tablets, multivitamin supplements or compound extracts (Silva et al., 2002;Siqueira et al., 2003Siqueira et al., , 2007. The plant is also a component of the medication Catuama®, which is widely used in several parts of Brazil as a general tonic and to alleviate physical and mental fatigue (Antunes et al., 2001). ...
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Ptychopetalum olacoides Benth., Olacaceae, popularly known as marapuama or muirapuama or miriantã, is a species native to the Amazonian region of Brazil. Extracts of the bark of the plant have been used traditionally for its stimulating and aphrodisiac properties and currently commercialised by the herbal industry as constituents in a wide range of phytomedicines. Fractionation by open column chromatography followed by preparative HPLC-UV/PAD of the stem bark and of three commercial extracts of P. olacoides allowed the isolation of three components that were common to all extracts analysed, and these were identified by NMR to be vanillic acid, protocatechuic acid and theobromine. Vanillic acid, which has been proposed as a phytochemical marker for P. olacoides, was employed as an external standard in the development and validation of a rapid qualitative and quantitative HPLC assay for the analyte. The recoveries values of the developed method were 99.02% and the LOD and LOQ values were 0.033 and 0.11 mg.L-1, respectively. The described method may be applied to the standardisation of herbs, extracts or phytomedicines commercialised as marapuama.
Ethnopharmacological relevance: Sexual dysfunction is a multifactorial health condition characterized by distressing disturbances in the sexual response and libido, leading to an inability to maintain penile erection and achieve pleasure. Considering the huge Brazilian biodiversity, many plants are traditionally used for aphrodisiac purposes. However, the use of native medicinal plants as sexual boosters in Brazil has been poorly studied. Aim of the study: This review focuses on the composition, pharmacology, and results of experimental trials of the main native plants used in Brazilian folk medicine with alleged aphrodisiac effects. We aimed to provide a state-of-the-art reference for research on herbs for the treatment of male sexual dysfunction by summarizing and discussing the main studies found. Materials and methods: The relevant information was collected by searching keywords (aphrodisiac, sexual tonic, sexual stimulant, sexual vigor stimulant, sexual impotency, erectile dysfunction, etc.) from books containing primary surveys conducted in the original communities and bibliographic surveys prepared by authors linked to the national academic and scientific environment edited in Brazil. Preclinical and clinical studies of the compiled plant species were performed using scientific databases (Scopus, PubMed, SciELO, and SciFinder). Results: Seventy-four plant species belonging to 44 families used in Brazil to treat sexual dysfunction were compiled from ethnopharmacological literature. Fourteen plants, including Pfaffia glomerata (Spreng.) Pedersen, Aspidosperma quebracho-blanco Schltdl., Anemopaegma arvense (Vell.) Stellfeld ex de Souza, Mimosa pudica L., Heteropterys tomentosa A. Juss., Trichilia catigua A. Juss., and Turnera diffusa Willd. ex Schult. were pharmacologically studied to confirm these therapeutic properties. Probable modes of action include antioxidant and androgenic activities, inhibition of the PDE5 enzyme, increase in NO levels, and activation of dopaminergic and noradrenergic pathways. In addition, several different species popularly known as "catuaba" were identified, leading to adulterations and controversial effects. Conclusion: The overall results of the present review of Brazilian folk literature reveal that Brazil has a long tradition of using plants with potential aphrodisiac effects. However, further research is required to identify, characterize, and standardize the active ingredients and herbal preparations used in aphrodisiacs.
A phytochemical component investigation of the bark of Ptychopetalum olacoides led to the isolation of 4 new clerodane-type diterpenoids, namely, ptycholide V (1), 7α,20-dihydroxykolavelool (2), ptycholide VI (3), and ptycholide VII (4). Their structures were elucidated by extensive spectroscopic data and comparison of NMR data with that obtained for known compounds.
Common name: Silver wattle, French mimosa.
Bilirubin, a by-product of heme degradation, has an important role in cellular protection. Therefore, we speculated that bilirubin could be of potential therapeutic value in wound healing. To validate the hypothesis, we used a full-thickness cutaneous wound model in rats. Bilirubin (30 mg/kg) was administered intraperitoneally every day for 9 days. The surface area of the wound was measured on days 0, 2, 4, 7 and 10 after the creation of the wound. The granulation tissue was collected on day 10 post-wounding for analysing various parameters of wound healing. Bilirubin treatment accelerated wound contraction and increased hydroxyproline and glucosamine contents. mRNA expression of pro-inflammatory factors such as intercellular cell adhesion molecule-1 (ICAM-1) and tumour necrosis factor-α (TNF-α) were down-regulated and that of anti-inflammatory cytokine interleukin-10 (IL-10) was up-regulated. The findings suggest that bilirubin could be a new agent for enhancing cutaneous wound healing.
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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.
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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 it is widely believed that benzodiazepines reduce anxiety through positive allosteric modulation of the GABAA–chloride channel complex, this is not the only mechanism through which agents of this class can modify CNS function. Furthermore, a significant number of reports of apparent flumazenil blockade of diazepam anxiolysis in animal models have paid limited attention to possible intrinsic behavioral actions of the antagonist per se. In the present study, ethological methods were employed to assess in detail the effects of diazepam, flumazenil, and their combination on the behavior of male DBA/2 mice in the elevated plus-maze paradigm. In two experiments, diazepam (1.5 mg/kg) alone reduced open-arm avoidance and increased head dipping, whereas flumazenil (10–40 mg/kg) alone was without significant behavioral effect. However, with the sole exception of head dipping, prior administration of flumazenil (10 and 40 mg/kg) failed to block the behavioral effects of diazepam under present test conditions. These findings imply that the anxiolytic effects of diazepam in the mouse plus-maze are not mediated through flumazenil-sensitive benzodiazepine receptors and that alternate mechanisms must be considered.
Ptychopetalum olacoides (Olacaceae) is a popular Amazonian medicinal plant in Brazil claimed to be aphrodisiac and to cure male impotence. In the present study, we have evaluated the hydroalcohol extract prepared from stem bark on the behaviour in mice using forced swimming-induced immobility and open field as test models. The plant extract was found to possess both motor depressant and stimulant properties depending on the test model used. While it diminished locomotor activity in the open field test, it caused a reduction of immobility time in the forced swimming test. Also, these effects were found to be similar to those produced by clonidine, an α2-adrenoceptor agonist and were abolished by yohimbine, an α2-adrenergic antagonist. The findings obtained suggest a clonidine-like effect of P. olacoides bark extract. © 1998 John Wiley & Sons, Ltd.
The clinical efficacy of the benzodiazepines in reducing anxiety is widely accepted. However, the search for novel anxiolytics continues, motivated by the hope of finding a non-sedative anxiolytic. This article reviews the pre-clinical evidence for new compounds as it relates both to their anxiolytic actions in animal tests and to their sedative potential. Drugs acting at sites on the GABA-benzodiazepine receptor complex are discussed, as well as the potential importance of aminergic and peptidergic pathways.
3α-hydroxylated pregnane steroids have been shown to possess anesthetic, hypnotic, anticonvulsant and anxiolytic properties. In this study, metabolites of progesterone and deoxycorticosterone, 5α-pregnan-3α-ol-20-one (3α-OH-DHP) and 5α-pregnan-3α,21-diol-20-one (5α-THDOC), respectively, were tested for anxiolytic effects in N.I.H. Swiss-Webster mice using the light/dark transition, open-field and lick-suppression tests. Similar to the benzodiazepine (BZ) diazepam, 3α-OH-DHP (5–40 mg/kg) and 5α-THDOC (5–40 mg/kg) significantly increased the number of light/dark transitions. 3α-OH-DHP's effects were stereospecific as its diasteriomer, 3β-OH-DHP was devoid of activity. The benzodiazepine antagonist CGS-8216 (10 mg/kg) blocked diazepam's (1.0 mg/kg) anxiolytic effects, but did not have any effect against 3α-OH-DHP (20 mg/kg). The data indicate that the pregnane steroids produce their anxiolytic effects through a separate mechanism than the BZs. 3α-OH-DHP (20 mg/kg), 5α-THDOC (20 mg/kg) and diazepam (1.0 mg/kg) increased activity in a open-field test. 3β-OH-DHP had no effect in the open-field test. Furthermore, 3α-OH-DHP produced a 235% increase in punished responding in a lick-suppression test. These results demonstrate that the endogenous pregnane steroids possess anxiolytic effects that may be clinically relevant.
The anxiolytic activity of diazepam (DZP) (0.25-1 mg/kg) was investigated in streptozotocin (STZ)-induced diabetic adult Charles Foster albino rats of either sex. Diabetes was induced by injecting STZ IP (50 mg/kg; in citrate buffer, pH 4.5). Experiments were performed 72 h later. The rats were subjected to various anxiety paradigms, including the open-field exploratory behaviour, elevated plus maze and elevated zero maze behaviours and the social interaction tests. In addition, rat brain tribulin activity was also assessed as a biochemical marker of anxiety. The results indicate that diabetic rats showed significantly more anxiogenic activity in comparison to non-diabetic rats on open-field, elevated plus maze, zero maze and social interaction tests. In diabetic rats, brain tribulin activity (MAO-A inhibitory component) was significantly increased. DZP dose dependently produced anxiolytic activity on the various behavioural parameters in non-diabetic rats. DZP (0.5 and 1 mg/kg) partially reversed the anxiogenic behaviour of STZ diabetic rats in elevated plus maze and zero maze tests. However, in open field behaviour and social interaction tests significant anxiolytic activity was observed only at a higher dose of DZP (1 mg/kg). The findings indicate that STZ-induced diabetic rats exhibited augmented anxiety on various experimental paradigms and that the anxiolytic effect of diazepam was less marked in diabetic rats as compared to their euglycaemic counterparts.
Four different behavioural tests, the holeboard, faecal counts, food preference, and operant behaviour were assessed for their ability to detect anxiolytic activity in the rat. In evaluating each of these tests, varying doses of a single anxiolytic and/or different types of anxiolytic compounds were given to the rats and the resulting behavioural changes recorded. Anxiolytics did not significantly alter behaviour on the holeboard, nor did they change food preference in accordance with expectations. At high doses anxiolytic did reduce faecal counts. While this may be a consequence of the anxiolytic activity of these drugs, their effect on gastric motilityper se was not assessed. During the extinction of an operant response (performed over a number of trials on successive days) anxiolytics consistently shortened the latency before the onset of pressing. It is suggested that this test may be of value in th edetection of anxiolytic activity in the rat.
To determine whether head-dipping could be validated as a measure of exploration a modified hole-board was developed with four holes in the floor, under which novel objects could be placed. Two criteria for considering head-dipping as a measure of exploration were proposed: firstly that it should reflect novel aspects of the environment; secondly, that exposure to the hole-board should result in information storage. That head-dipping reflected novelty was indicated by the longer duration of head-dips on initial exposure if objects were present, and also on a second exposure when objects were introduced for the first time. Information storage was indicated by habituation on re-exposure to the hole-board. A significant positive correlation between head-dipping in the "four" and "sixteen" hole-boards was obtained for rats, but not for mice. This provided some indirect evidence that rat head-dipping in the "sixteen hole-board" also reflects exploration. (+)Amphetamine and alcohol were tested in the modified hole-board, and (+)amphetamine decreased and alcohol increased the frequency and duration of head-dips.