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α-Terpineol (TPN) is a monoterpenoid alcohol present in the essential oils of several species of the Eucalyptus genus (Myrtaceae).TPN was assessed for its antinociceptive activity in rodents.The antinociceptive effect of TPN was examined using the acetic acid writhing reflex, formalin, glutamate, and capsaicin-induced nociception tests.TPN produced a significant (P 0.01 or P 0.001) analgesic effect by reduction at the early and late phases of paw licking and reduced the writhing reflex in mice (formalin and writhing tests, respectively). In the glutamate test, all doses of TPN produced significant (P 0.01) nociceptive protection. When the capsaicin-induced nociception test was conducted, TPN produced dose-related inhibition of the nociceptive behavior. In addition, the results of a hot plate test showed central analgesic properties for TPN (P 0.01 or P 0.001). Such results were unlikely to be provoked by motor abnormality.Our results suggest that TPN might represent an important tool for management and/or treatment of painful conditions.

Linalool oxide is a monoterpene that is found in some species of aromatic plants. The effects of the inhalation of linalool oxide (0.65%, 1.25%, 2.5% and 5.0% w/w) in the elevated plus-maze and light/dark box tests as animal models of anxiety were investigated in adult male mice and compared with the effects of the reference anxiolytic diazepam (0.5 and 2.0mg/kg), administered intraperitoneally. Additionally, the effects of inhaled linalool oxide were investigated in the rotarod test. Linalool oxide significantly increased the number of visits to the open arms of the elevated plus-maze and the amount of time spent there as well as the total number of entries. In the light/dark box test, inhalation of linalool oxide led to an increase in the time spent by the mice in the brightly-lit chamber and in the number of times the animal crossed from one compartment to another. Performance on the rotarod was unaffected. Thus, inhaled linalool oxide was found to have anxiolytic properties in both animal models, without causing any motor deficit. These results suggest that inhalation of linalool oxide may be a useful means of counteracting anxiety.

Acute treatment with the chloroform fraction ofDioclea virgata(Rich.) Amshoff (CFDv) in mice produced decreased ambulation and sedation in the behavioral pharmacological screening. Doses of 125 and 250 mg/kg CFDv decreased latency of sleep onset in the test of sleeping time potentiation. In the open field, animals treated with CFDv reduced ambulation and rearing (250 mg/kg), as well as defecation (125; 250 mg/kg). Regarding the antinociceptive activity, CFDv (125, 250, 500 mg/kg) increased latency to first writhing and decreased the number of writhings induced by acetic acid. In the formalin test, CFDv (250 mg/kg) decreased paw licking time in the first and second phases indicating antinociceptive activity that can be mediated both peripherally and at the central level. CFDv did not affect motor coordination until 120 minutes after treatment. CFDv shows psychopharmacological effects suggestive of CNS-depressant drugs with promising antinociceptive activity.

Hydroxydihydrocarvone (HC) is a synthetic intermediate obtained by hydration of the natural compound (R)-(-)-carvone. The aim of the present study was to investigate the possible anti-inflammatory activity of orally administered HC. Toxicity, motor coordination, tail immersion test, as well as carrageenan-induced paw edema and myeloperoxidase (MPO) activity or peritonitis were all evaluated in rodents. HC was force-fed to the animals 1 h before the stimulus. The lethal dose 50% (LD50) of orally administered HC was 1259 mg/kg. No changes in motor coordination were recorded in HC-treated mice in the rotarod test. The time of response to the thermoceptive stimulus in the tail immersion test was longer in HC-treated animals (50, 100, and 200 mg/kg) than in the vehicle-treated group. HC also significantly decreased the area under curve of carrageenan-induced rat paw edema at 100 and 200 mg/kg and MPO activity at 200 mg/kg. Carrageenan-induced neutrophil recruitment to the peritoneal cavity was significantly reduced by HC at doses of 100 or 200 mg/kg, but not 50 mg/kg. These findings demonstrate that orally administered HC exerts antinociceptive and anti-inflammatory activities in rats and mice.

Fibromyalgia is a chronic painful syndrome that affects up to 5% of the world population. It is associated with sleep and mood disorders, fatigue, and functional disability. Its pathogenesis involves a disorder of the central modulation of pain, impairment of the descending inhibitory system, and hyperactivity of substance P. Because of the extensive symptomatology of patients with fibromyalgia and its multifactorial pathogenesis, its ideal treatment requires a multidisciplinary approach including the association of pharmacological and non-pharmacological therapies. The pharmacological therapy currently recommended for the syndrome includes antidepressants, calcium-channel modulators, muscle relaxants, and analgesics. In most cases, the non-pharmacological treatment consists of patient education, supervised aerobic physical activity, and cognitive-behavioral therapy. However, many patients do not respond satisfactorily, or have side effects associated with the long-term use of drugs, in addition to reporting difficulties in adhering to a therapy based on exercises and physical medicine. Thus, physicians and patients are increasingly interested in an alternative and complementary therapy for fibromyalgia. This review approaches the different therapeutic modalities used in fibromyalgia, emphasizing the evidence of non-pharmacological therapy and use of alternative and complementary medicine for these patients.

A new flavanone with the relatively rare 2′,5′-dioxygenation at ring B has been isolated from the roots of Dioclea grandiflora and its structure established as 5,2′, 5′-trihydroxy-6,7-dimethoxyflavanone, mainly with the aid of spectroscopic methods.

The Aim of this study was to evaluated the effects of the ethanol extract of Rauvolfia ligustrina Willd. ex Roem. & Schult., Apocynaceae, roots (EER) in animal models of epilepsy. The EER increased the latency for convulsions significantly different from control (p

The acute treatment of mice with an ethanolic extract from the seed pod ofDioclea grandiflora(EDgP) at doses of 75, 150 and 300 mg/kg by intraperitoneal administration produced a significant antinociceptive effect as displayed by the acetic acid-induced writhing test and the formalin test. The antinociception was observed through the first (neurogenic pain) and second (inflammatory pain) phases in the formalin test. The hot plate test did not show an increase in the antinociceptive latency whereas the motor performance was affected by the administration at 300 mg/kg at the beginning (30 minutes) of the observation period but not at later periods (60 and 120 minutes). These results suggest that EDgP has a central antinociceptive action and a possible anti-inflammatory activity in mice.

We investigated the antinociceptive and nerve excitability effects of theN-salicyloyltryptamine (NST) NST-treated mice exhibited a significant decrease in the number of writhes when 100 and 200 mg/kg (i.p.) were administered (i.p.). This effect was not antagonized by naloxone (1.5 mg/kg, i.p.). NST inhibited the licking response of the injected paw when 100 and 200 mg/kg were administered (i.p.) to mice in the first and second phases of the formalin test. Because the antinociceptive effects could be associated with neuronal excitability inhibition, we performed the single sucrose gap technique and showed that NST (3.57 mM) significantly reduced (29.2%) amplitude of the compound action potential (CAP) suggesting a sodium channel effect induced by NST. Our results demonstrated an antinociceptive activity of the NST that could be, at least in part, associated to the reduction of the action potential amplitude. NST might represent an important tool for pain management.

The orange essential oil (OEO) and its components obtained from Citrus aurantium L. (Rutaceae) has been attracting interest due to its sedative and relaxing actions. In the present study, rats previously exposed to OEO at the concentrations of 1.0%; 2.5% and 5.0%, w/w, by inhalation during 7 minutes in acrylic boxes were evaluated in two anxiety models: elevated plus maze (EPM) and open-field. The OEO at the concentration of 2.5% increased both the time of the animals in the open arms of the EPM and the time of active social interaction in the open-field being longer than that of the diazepam group (1.5 mg/kg i.p). In conclusion, the decrease in the level of emotionality of the animals observed in the two experimental models suggests a possible central action, which is in agreement with the phytochemical profile of the oil under study, since it showed the presence of limonene (96.24%) and mircene (2.24%), components with a well-known depressant activity on the central nervous system. O óleo essencial de laranja (OEL) e seus constituintes obtidos da Citrus aurantium L. (Rutaceae) têm despertado interesse pela sua ação sedativa e relaxante. No presente estudo, ratos previamente expostos à inalação do OEL nas concentrações de 1,0%; 2,5% e 5,0%, p/v, durante 7 minutos em caixas de acrílico, foram avaliados em dois modelos de ansiedade: labirinto em cruz elevado (LCE) e campo aberto. O OEL na concentração de 2,5% aumentou tanto o tempo de permanência dos animais nos braços abertos do LCE, como o tempo de interação social ativa no campo aberto, tendo sido superior ao grupo padrão diazepam (1,5 mg/kg) ip. A diminuição do grau de emocionalidade dos animais observada nos dois modelos experimentais sugere uma possível ação central, o que está de acordo com o perfil fitoquímico do óleo em estudo o qual mostrou a presença de limoneno (96,24%) e mirceno (2,24%), constituintes com comprovada atividade depressora sobre o sistema nervoso central.

(−)-Carvone is a monoterpene ketone that is the main active component of Mentha plant species like Mentha spicata. This study aimed to investigate the antinociceptive activity of (−)-carvone using different experimental models of pain and to investigate whether such effects might be involved in the nervous excitability elicited by others monoterpenes. In the acetic acid-induced writhing test, we observed that (−)-carvone-treated mice exhibited a significant decrease in the number of writhes when 100 and 200 mg/kg was administered. It was also demonstrated that (−)-carvone inhibited the licking response of the injected paw when 100 and 200 mg/kg was administered (i.p.) to mice in the first and second phases of the formalin test. Since naloxone (5 mg/kg, s.c.), an opioid antagonist, showed no influence on the antinociceptive action of (−)-carvone (100 mg/kg), this suggested nonparticipation of the opioid system in the modulation of pain induced by (−)-carvone. Such results were unlikely to be provoked by motor abnormality, since (−)-carvone-treated mice did not exhibit any performance alteration on the Rota-rod apparatus. Because the antinociceptive effects could be associated with neuronal excitability inhibition, we performed the single sucrose gap technique and observed that (−)-carvone (10 mM) was able to reduce the excitability of the isolated sciatic nerve through a diminution of the compound action potential amplitude by about 50% from control recordings. We conclude that (−)-carvone has antinociceptive activity associated with decreased peripheral nerve excitability.

Aim of the study Aniba rosaeodora is an aromatic plant which has been used in Brazil folk medicine due to its sedative effect. Therefore, the purpose of the present study was to evaluate the sedative effect of linalool-rich rosewood oil in mice. In addition we sought to investigate the linalool-rich oil effects on the isolated nerve using the single sucrose-gap technique. Materials and methods Sedative effect was determined by measuring the potentiation of the pentobarbital-induced sleeping time. The compound action potential amplitude was evaluated as a way to detect changes in excitability of the isolated nerve. Results The results showed that administration of rosewood oil at the doses of 200 and 300 mg/kg significantly decreased latency and increased the duration of sleeping time. On the other hand, the dose of 100 mg/kg potentiated significantly the pentobarbital action decreasing pentobarbital latency time and increasing pentobarbital sleeping time. In addition, the effect of linalool-rich rosewood oil on the isolated nerve of the rat was also investigated through the single sucrose-gap technique. The amplitude of the action potential decreased almost 100% when it was incubated for 30 min at 100 μg/ml. Conclusions From this study, it is suggested a sedative effect of linalool-rich rosewood oil that could, at least in part, be explained by the reduction in action potential amplitude that provokes a decrease in neuronal excitability.

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) O monoterpeno alfa,beta-epóxi-carvona (EC) nas doses de 200, 300 e 400 mg/kg administrado por via i.p. em camundongos diminuiu significativamente a atividade motora dos animais, quando comparado aos controles, até 120 minutos após a administração. As doses de 300 e 400 mg/kg induziram um aumento significativo do tempo de sono dos animais não alterando, no entanto, a sua latência. O EC na dose de 400 mg/kg induziu uma redução no tempo de permanência dos animais na barra giratória (teste do rotarod). Os resultados sugerem um possível efeito central. The monoterpene alpha,beta-epoxy-carvone (EC) in doses of 200, 300 or 400 mg/kg injected by i.p. route in mice caused a significant decrease in the motor activity of animals when compared with the control group, up to 120 minutes after the administration. The doses of 300 or 400 mg/kg had induced a significant increase of in the sleeping time of animals not having modified, however, the latency. The EC in the dose of 400 mg/kg reduced the remaining time of the animals on the rotating rod (Rotarod test). These results suggest a possible central effect. Universidade Federal de Sergipe Departamento de Fisiologia Universidade Federal da Paraíba Laboratório de Tecnologia Farmacêutica Universidade Federal de São Paulo (UNIFESP) Departamento de Psicobiologia UNIFESP, Depto. de Psicobiologia SciELO

Rotundifolone, a monoterpene isolated from the essential oil of the leaves of Mentha x villosa, is a constituent of several essential oils and known to have antinociceptive activity. Our recent study demonstrated that the analogues of rotundifolone showed also a significant antinociceptive effect. In the present report, to investigate the correlation between the structure and antinociceptive activity, rotundifolone and its analogues were evaluated in the acetic acid-induced writhing test in mice. All compounds showed to be more antinociceptive than rotundifolone against the pain response induced by acetic acid. Comparing the antinociceptive effect of rotundifolone with limonene oxide and (+)-pulegone, the results demonstrated that the epoxide group contributes as much as the ketone group to the antinociceptive activity of rotundifolone. Similarly, pulegone oxide and carvone epoxide were more antinociceptive than rotundifolone, thereby suggesting that the position of the functional group on the ring also influences the antinociceptive activity. (D)-Carvone produced maximal inhibition of the writhing response and was slightly more active than (+)-carvone. The study showed that by appropriate structural modification it may be possible to develop novel antinociceptive agents.

Inhibition of Angiotensin Converting Enzyme (ACE) is a modern therapeutic target in the treatment of hypertension. Within the enzyme cascade of the renin-angiotensin system, ACE removes histidyl-leucine from angiotensin I to form the physiologically active octapeptide angiotensin II, one of the most potent known vasoconstrictors. Therefore, a rationale for treating hypertension would be to administer drugs or natural compounds which selectively inhibit ACE. The present work constitutes a review of the literature of plants and chemically defined molecules from natural sources with in vitro anti-hypertensive potential based on the inhibition of ACE. The review refers to 321 plants, the parts utilized, type of extract and whether they are active or not. It includes also the names of 158 compounds isolated from higher plants, marine sponges and algae, fungi and snake venom. Some aspects of recent research with natural products directed to produce anti-hypertensive drugs are discussed. In this review, 148 references were cited. A inibição da Enzima Conversora da Angiotensina (ECA) é um alvo terapêutico moderno e eficaz no tratamento da hipertensão arterial. Na cascata enzimática que envolve o sistema renina-angiotensina, a ECA promove a remoção dos aminoácidos histidil-leucina da angiotensina I para formar o octapeptídio angiotensina II, a qual é fisiologicamente ativa em diversos sistemas, e considerado como um dos mais potentes vasoconstrictores endógenos conhecido. Portanto, uma racionalidade no tratamento da hipertensão seria administrar drogas ou compostos de origem natural que inibam seletivamente a ECA. O presente estudo constitui uma revisão da literatura sobre plantas e moléculas de origem natural com potencial anti-hipertensivo, baseado na inibição in vitro da ECA. A revisão referencia 321 plantas, partes usadas, tipo de extrato e se é ativo ou não. Inclui ainda o nome de 158 compostos isolados de plantas superiores, esponjas e algas marinhas, fungos e venenos de cobra. Alguns aspectos de pesquisa recente com produtos naturais direcionados à produção de drogas anti-hipertensivas também são discutidos. Nesta revisão 148 referências foram consultadas.

N-Benzoyltryptamine (3), previously isolated from Myrtopsis myrtoidea and a new analogue, N-salicyloyltryptamine (5), were prepared by coupling tryptamine with benzoylchloride and methyl salicylate, respectively. Their structural elucidation was made by the usual spectroscopic methods and two-dimentional NMR techniques COSY, COBY and HMBC. N-salicyloyltryptamine (5) was submitted to pharmacological screening behavior, showing depressant effects

The central effects of hydroxydihydrocarvone (HC), an analogue of several monoterpenes, were evaluated in animal models. General behavior, locomotor activity, pentobarbital-induced sleeping time, pentylenetetrazol (PTZ)-induced convulsions, and acetic acid-induced writhing were evaluated in mice. The compound caused palpebral ptosis, decreased the response to touch, and increased sedation (general behavioral profile). HC (50-200 mg/kg) caused a significant dose-dependent decrease in the spontaneous motor activity of mice. This compound (100, 200 mg/kg) potentiated the pentobarbital sleeping time, indicating a depressant action. HC also protected the mice against PTZ-induced convulsions at 400 mg/kg. In the acetic acid-induced writhing, the antinociceptive activity of HC was demonstrated with a significant dose-dependent response at a dose range of 25-400 mg/kg. The present results provide evidence that HC has significant psychopharmacologic activity with depressant effects.

Further investigation of the root-bark of Dioclea grandiflora resulted in the isolation of a minor constituent, dioclenol. The structure of dioclenol was determined to be 3,5,7-trihydroxy-8-methoxy-6-prenylflavanone on the basis of its spectral characteristics. The 13 C NMR assignments have been confirmed by a selective INEPT experiment.

Citronellol is one monoterpene alcohol, which is present in the essential oils of various aromatic plant species. This study evaluated the neuroprotective activity of citronellol on pentylenetetrazol- and picrotoxin-induced convulsions and maximal electroshock-induced seizures in mice. Administration of citronellol significantly reduced the number of animals of convulsion induced by pentylenetetrazol and eliminated the extensor reflex of maximal electroshock-induced seizures test in about 80% of the experimental animals. In addition, administration of citronellol showed protection in the pentylenetetrazol and picrotoxin tests by increasing the latency of clonic seizures. We also investigated the effect of citronellol in the rat isolated nerve using the single sucrose-gap technique. We showed that the amplitude of the compound action potential decreased more than 90% when the monoterpene was incubated for 30 min at 6.4 mM and we did not verify any effect on the repolarization of the compound action potential. Taken together, our results demonstrated an anticonvulsant activity of the citronellol that could be, at least in part, explained by the diminution of the action potential amplitude.

Sida cordifolia L. (Malvaceae), known as “malva branca”, is a plant used in the popular medicine for the treatment stomatits, of asthma and nasal congestion. This work researched the acute toxicity of Sida cordifolia and its action on the central nervous system (CNS) because no data in the literature have been found about of pharmacological activity of this plant in the CNS. The hydroalcoholic extract of Sida cordifolia leaves (HESc) was used and the psychopharmacology approach began with the determination of LD 50 , where a low toxicity was observed in mice. Depressive activity on CNS was demonstrated by several alterations in mice's behavior in the pharmacological screening. In the motility test, the HESc showed significant reduction of spontaneous activity at a dose of 1000 mg/kg (i.p.) at 30 and 60 min. The same form the HESc also decreased the ambulation and rearing in open-field test at 30, 60 and 120 min at a dose of 1000 mg/kg (i.p.).

The cardiovascular effects of reticuline, isolated in a pure form from the stem of Ocotea duckei Vattimo, were studied in rats by using a combined in vivo and in vitro approach. In normotensive rats, reticuline (5, 10 and 20 mg/kg, i. v., randomly) injections produced an intense hypotension. This hypotensive response was attenuated after either, L-NAME (20 mg/kg, i. v.), a nitric oxide (NO) synthase inhibitor, or atropine (2 mg/kg, i. v.), a muscarinic receptor antagonist. In isolated rat aortic rings with intact endothelium, reticuline (3 x 10 ( - 6), 3 x 10 ( - 5), 3 x 10 ( - 4), 9 x 10 ( - 4) and 1.5 x 10 ( - 3) M) inhibited in a concentration-dependent manner the contractions induced by phenylephrine (1 microM), KCl (80 mM) and KCl (30 mM), [IC (50) = (0.4 +/- 0.1, 2.4 +/- 0.4 and 3 +/- 0.4) x 10 ( - 4) M, respectively). The effect of reticuline on phenylephrine-induced contractions was attenuated by removal of the vascular endothelium [IC (50) = (2.5 +/- 0.7) x 10 ( - 4) M]. Similar results were obtained after pretreatment of the rings with L-NAME 100 microM [IC (50) = (1.3 +/- 0.1) x 10 ( - 4) M], L-NAME 300 microM [IC (50) = (3 +/- 0.3) x 10 ( - 4) M] or atropine 1 microM [IC (50) = (1.2 +/- 0.2) x 10 ( - 4) M]. On the other hand, the effect of reticuline on phenylephrine-induced contractions was not affected by indomethacin 1 microM [IC (50) = (0.7 +/- 0.3) x 10 ( - 4) M]. Reticuline (3 x 10 ( - 6), 3 x 10 ( - 5), 3 x 10 ( - 4), 9 x 10 ( - 4) and 1.5 x 10 ( - 3) M) antagonized CaCl (2)-induced contractions, and also inhibited the intracellular calcium dependent transient contractions induced by norepinephrine (1 microM), but not those induced by caffeine (20 mM). These results suggest that the hypotensive effect of reticuline is probably due to a peripheral vasodilation in consequence of: 1) muscarinic stimulation and NOS activation in the vascular endothelium, 2) voltage-dependent Ca (2+) channel blockade and/or 3) inhibition of Ca (2+) release from norepinephrine-sensitive intracellular stores.

1. The aim of this work was to study the effects of N-salicyloyltryptamine (STP), a novel anticonvulsant agent, on voltage-gated ion channels in GH3 cells. 2. In this study, we show that STP at 17 microM inhibited up to 59.2+/-10.4% of the Ito and 73.1+/-8.56% of the IKD K+ currents in GH3 cells. Moreover, the inhibitory activity of the drug STP on K+ currents was dose-dependent (IC50=34.6+/-8.14 microM for Ito) and partially reversible after washing off. 3. Repeated stimulation at 1 Hz (STP at 17 microM) led to the total disappearance of Ito current, and an enhancement of IKD. 4. In the cell-attached configuration, application of STP to the bath increased the open probability of large-conductance Ca2+-activated K+ channels. 5. STP at 17 microM inhibited the L-type Ca2+ current by 54.9+/-7.50% without any significant changes in the voltage dependence. 6. STP at 170 microM inhibited the TTX-sensitive Na+ current by 22.1+/-2.41%. At a lower concentration (17 microM), no effect on INa was observed. 7. The pharmacological profile described here might contribute to the neuroprotective effect exerted by this compound in experimental 'in vivo' models.

The present communication constitutes a global review on plant analgesic activity with special emphasis on those found in different parts of the world, including Brazil, which act on the central nervous system. One hundred and sixty six plants belonging to 79 families are reported.

α-Terpineol, a monoterpenoid alcohol, was investigated for its anticonvulsant activity. This compound increased the latency to convulsions induced by pentylenetetrazole at doses of 100 and 200 mg/kg and decreased the incidence of hindlimb extension produced by MES in a dose-related manner at doses of 200 and 400 mg/kg.

The anticonvulsant activity of the racemate and enantiomers of linalool have been evaluated. Pretreatment of the mice with ( S)-(+)-, ( R)-(-)- and rac-linalool increased the latency of convulsions significantly in the PTZ model. Only rac-linalool had an effect at the dose of 200 mg/kg. The enantiomers and their racemic mixture were effective in inhibiting the convulsant effect of PTZ at the dose of 300 mg/kg. The linalools presented pharmacological activity close to that of diazepam. In the PIC seizure model, ( R)-(-)-linalool and rac-linalool presented activity at the dose of 200 mg/kg, but the rac-linalool was more potent than ( R)-(-)-linalool; ( S)-(+)-linalool had no effect at this dose. On the other hand, at the dose of 300 mg/kg this enantiomer was effective, but less potent than ( R)-(-)-linalool and rac-linalool. In the MES model, linalools decreased the convulsion time of the mice in the doses of 200 and 300 mg/kg. rac-Linalool presented maximum effect at 300 mg/kg. Surprisingly, it increased significantly the convulsion time at a dose of 100 mg/kg. Using the parameter of tonic hind convulsions, only ( R)-(-)-linalool produced protection from tonic extension at the dose of 200 mg/kg. When the (+)- and (-)-enantiomers, and rac-linalool were administered at the dose of 300 mg/kg they were also effective in preventing tonic convulsions induced by transcorneal electroshock in the animals. The (+)- and (-)-forms were equipotent and the rac-linalool was more effective than phenytoin. We have demonstrated that the two enantiomers have similar qualitative anticonvulsant activity, but show different potencies.

The analgesic activity of dioflorin and dioclenol, two constituents of Dioclea grandiflora Mart., has been studied in mice. It was found that dioclenol (10 mg/kg, i.p.) and dioclenol (10 mg/kg, i.p.) were effective in the acetic acid-induced writhing and tail immersion tests. These observations suggest that dioflorin and dio-clenol possesses central antinociceptive activity.

Dioflorin (1) was isolated as a minor constituent from the rootbark of Dioclea grandiflora, the crude extract of which demonstrated analgesic activity. The structure of 1 has been determined to be 5,7,2'-trihydroxy-8-methoxy-6-(3-methyl-2-butenyl)flavanone on the basis of spectral analysis.

A new flavanone with the relatively rare 2′,5′-dioxygenation at ring B has been isolated from the roots of Dioclea grandiflora and its structure established as 5,2′, 5′-trihydroxy-6,7-dimethoxyflavanone, mainly with the aid of spectroscopic methods.

Bumelia sartorum has been mentioned in Brazilian folklore for its reputed use in the treatment of diabetes mellitus and inflammatory disorders. An ethanol extract of root bark elicited a hypoglycemic effect in normal and alloxan-induced diabetic rats. In addition, the extract altered glucose tolerance in alloxan-induced diabetic rats, enhanced glucose uptake in skeletal muscle and significantly inhibited glycogenolysis in the liver. These results indicate that the hypoglycemic effect may be similar to chlorpropamide and possibly due to an enhanced secretion of insulin from the islets of Langerhans or an increased utilization of glucose by peripheral tissues. Besides hypoglycemic activity, the ethanol extract also elicited significant anti-inflammatory activity, but did not show any significant effects on blood pressure, respiration or on the various isolated tissue preparations studied. Basic acid has been isolated from the ethanol extract and this component may be responsible for the observed anti-inflammatory activity. However, it is yet to be established whether basic acid is responsible for the observed hypoglycemic activity of the ethanol extract.

Marine algae have been the focus of important studies over the past fifty years, with a considerable number of components important to chemists and taxonomists having been isolated and characterized. The scientific data available on Sargassum polyceratium are extremely limited. The objective of the present study was to evaluate the antinociceptive activity of an ethanol extract of S. polyceratium and to isolate its components. Intraperitoneal treatment with ethanol extract of S. polyceratium reduced the number of acetic acid-induced writhes and the amount of time spent in paw-licking in the second phase of the formalin test. Ethanol extract of S. polyceratium also reduced the amount of time spent in paw-licking in the glutamate test; however, there was no difference in the reaction time in the hot plate test at any of the doses tested. The chemical components isolated from ethanol extract of S. polyceratium were identified using one- and two-dimensional spectroscopic methods such as infrared spectroscopy, mass spectrometry and 1H and 13C nuclear magnetic resonance spectroscopy. The analytical results were also compared with data obtained in the literature. The following porphyrin derivatives were isolated from S. polyceratium: 132-hydroxy-(132-R)-pheophytin-a, 132-hydroxy-(132-S)-pheophytin-a, pheophytin-a, and the steroid fucosterol. The present results indicate that the ethanol extract of S. polyceratium has antinociceptive activity. In addition, four new substances were isolated from the species evaluated. Keywords: Antinociceptive, Sargassum polyceratium, Marine algae, Pain, Porphyrin compounds

The purpose of the present study was to evaluate the effects of total tertiary alkaloid fraction (TTAF) of Cissampelos sympodialis Eichler (Menispermaceae) on two animal models of depression: a) forced swim test and b) reserpine test. Treatment of mice with TTAF (12.5 mg/kg) reduced the total immobility time. It also reversed the reserpine-induced hypothermia, demonstrating an antidepressant effect in both models. Additionally, TTAF treatment did not modify the ambulation and rearing evaluated in open field test in order to investigate if the immobility time reduction found in the forced swimming test was caused by locomotive activity stimulation. Since warifteine is one of the main alkaloids present in the TTAF of C. sympodialis, and it has inhibitory activity of the phosphodiesterase enzyme, it may be responsible by the antidepressant effect found in the fraction studied. A proposta deste trabalho foi de avaliar os efeitos da fração de alcalóides terciários totais (TTAF) de Cissampelos sympodialis Eichler (Menispermaceae) em dois modelos animais de depressão: a) teste do nado forçado e b) teste da reserpina. O tratamento de camundongos com TTAF (12,5 mg/kg) reduziu o tempo total de imobilidade dos animais. Também reverteu a hipotermia induzida por reserpina, demonstrando um efeito antidepressivo nos dois modelos. Adicionalmente, o tratamento com TTAF não modificou a ambulação e o comportamento de levantar das patas dianteiras dos animais avaliados no teste do campo aberto, realizado no intuito de investigar se a redução no tempo de imobilidade apresentada no teste do nado forçado foi causada por estimulação na atividade locomotora. Como a warifteína é um dos principais alcalóides presente na TTAF da C. sympodialis, e tem atividade inibidora da enzima fosfodiesterase, ela pode ser responsável pelo efeito antidepressivo observado na fração estudada.

The traditional use of essential oils in aromatherapy has offered numerous health benefits. However, few scientific studies have been conducted with these oils to confirm their therapeutic efficacy. (+)-Limonene is a chemical constituent of various bioactive essential oils. The present study reports on the anxiolytic-like effects of (+)-limonene in an elevated maze model of anxiety in mice. At concentrations of 0.5% and 1.0%, (+)-limonene, administered to mice by inhalation, significantly modified all the parameters evaluated in the elevated plus maze test. The pharmacological effect of inhaled (+)-limonene (1%) was not blocked by flumazenil. Analysis of (+)-limonene using gas chromatography–mass spectrometry (GC–MS) showed its volatility to be high. These data suggest possible connections between the volatility of (+)-limonene and its anxiolytic-like effect on the parameters evaluated in the elevated plus maze test. The data indicate that (+)-limonene could be used in aromatherapy as an antianxiety agent.

Seizures are resistant to treatment with currently available anticonvulsant drugs in about 1 out of 3 patients with epilepsy. Thus, there is a need for new, more effective anticonvulsant drugs for intractable epilepsy. However, nature is a rich source of biological and chemical diversity and a number of plants in the world have been used in traditional medicine remedies, i.e., anticonvulsant, anxiolytic, analgesic, antidepressant. This work constitutes a literature review on medicinal plants showing anticonvulsant properties. The review refers to 16 Brazilian plants and a total 355 species, their families, geographical distribution, the utilized parts, method and references. Some aspects of research on medicinal plants and a brief review of the most common animal models to discover antiepileptic drugs are discussed. For this purpose over 170 references were consulted. Cerca de um terço dos pacientes epilépticos não conseguem ter um tratamento adequado com as drogas anticonvulsivantes atuais. Nesse sentido, as plantas medicinais surgem como uma fonte promissora de novas moléculas químicas com propriedades biológicas apreciáveis. Muitas plantas ou produtos de origem naturais têm sido propostos para o tratamento de várias patologias, tais como: epilepsia, diabetes, ansiedade, depressão, dentre outras. O presente trabalho realizou um extenso levantamento na literatura especializada de plantas medicinais com propriedades anticonvulsivantes. Um total de 355 espécies vegetais foi identificado, sendo 16 plantas encontradas na flora brasileira, com indicação para o tratamento de quadros convulsivos. Características como nome da espécie, família, partes utilizadas, país do estudo e /ou publicação, métodos e referências foram sumarizados. Além disso, os principais apectos dos modelos animais mais utilizados no estudo de plantas/substâncias com propriedades anticonvulsivantes foram revisados. Mais de 170 referências foram consultadas.