Rosewood oil induces sedation and inhibits compound action potential in rodents

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.     

Sedative, hypnotic and anticonvulsant activities of the ethanol fraction from Rhizoma Pinelliae Praeparatum

Ethnopharmacological relevance

Rhizoma Pinelliae Praeparatum is the product of raw Rhizoma Pinellia processed with alkaline solution and Licorice, which had been widely used for treatment of insomnia in traditional Chinese medicine. The present study aimed to investigate the sedative, hypnotic and anticonvulsant activities of ethanol fraction from Rhizoma Pinelliae Praeparatum (EFRP) and to determine whether these effects were related to GABAergic mechanism.

Materials and methods

The sedative, hypnotic and anticonvulsant activities of EFRP were investigated with locomotion activity, pentobarbital-induced sleeping and nikethamide (NKTM)-induced convulsion tests, respectively. Additionally, the effects of flumazenil (an antagonist of GABA_A receptor) and l-malic acid (blocker of synthetic enzyme for GABA) on the hypnotic activity of EFRP were evaluated.

Results

EFRP at dose of 12 g/kg significantly inhibited the locomotion activity of mice. EFRP showed synergic effect on pentobarbital-induced sleeping by increased numbers of mice falling asleep, reduced the sleep latency and prolonged the sleeping time. l-malic acid and flumazenil inhibited the augment effects of EFRP on pentobarbital-induced sleeping. EFRP promoted a significant protection to NKTM-induced convulsion, by prolonged the death latency and decreased mortality.

Conclusion

EFRP possessed sedative, hypnotic and anticonvulsant activities and these activities may be related to the GABAergic system.     

CNS depressant and anticonvulsant activities of the alcoholic extract of leaves of Ziziyphus nummularia

Ethnopharmacological relevance

Ziziyphus nummularia (family: Rhamnaceae) is a xerophyte, grows in the grazing lands of the Thar Desert of Rajasthan. Ziziyphus nummularia (ZN) is used as sedative in ethnomedicine. The objective of this study is to investigate the anticonvulsant, anxiolytic and sedative activities of the alcoholic extract of leaves of Ziziyphus nummularia (EZN).

Materials and methods

The anticonvulsant effect of the EZN (100, 200 and 300 mg/kg) was evaluated in mice using the pentylenetetrazole and maximal electroshock induced seizure models. Its anxiolytic activity was evaluated using the elevated plus maze, hole board and open field models board methods, while the pentobarbital induced sleep was used to evaluate the sedative activity. The acute toxicity and effect on motor coordination were also assessed.

Results

EZN (100–300 mg/kg) protected the mice against the pentylenetetrazole induced convulsions; it causes a significant (P<0.05) dose dependent increase in latency of convulsion. Treatment with EZN reduced the duration of the tonic hind limb extension induced by electroshock. Mice treated with EZN preferred the open arm of the plus maze and were found to be devoid of open-arm avoidance. EZN potentiation the barbiturate induce sleep in mice, it causes a decrease in the sleep latency and increases the duration of sleep.

Conclusion

The results obtained from the experiments indicate that the EZN has CNS depressant and anticonvulsant activities.     

Hypnotic effect of jujubosides from Semen Ziziphi Spinosae

Ethnopharmacological significance

Semen Ziziphi Spinosae, the seed of Ziziphus jujuba Mill. var. spinosa (bunge) Hu ex H.F. Chow has been widely used in treating insomnia and anxiety.

Aim of the study

In this study, we investigated the hypnotic effect of jujubosides, one of the major components (saponin) of Semen Ziziphi Spinosae, in both day and night period.

Materials and methods

After the administration of jujubosides (9 mg/kg once per day for 3 days), sleep parameters were examined by EEG and EMG analysis in normal rats and the action of jujubosides on pentobarbital-induced sleep assessed by the loss-of righting reflex.

Results

During daytime (9:00–15:00), jujubosides significantly increased the total sleep and rapid eye movement (REM) sleep without significant influence on non-REM (NREM) sleep. During nighttime (21:00–3:00), jujubosides significantly increased the total sleep and NREM sleep especially the light sleep while showed no significant effect on REM sleep and slow wave sleep (SWS). In pentobarbital-treated mice, jujubosides significantly augmented the hypnotic effect of pentobarbital (45 mg/kg, i.p.), proved by increasing sleep time and this augmentative effect was potentiated by 5-hydroxytryptophan (2 mg/kg, i.p.). Furthermore, jujubosides inhibited the para-chlorophenylalanine-induced suppression of pentobarbital-induced hypnosis.

Conclusions

These results suggested that the hypnotic effect of jujubosides on normal rats may be influenced by circadian rhythm and the serotonergic system may involve in the hypnotic effect of jujubosides. Jujubosides may be good source of lead compounds for novel hypnotics.     

Antinociceptive and hypnotic properties of Celastrus orbiculatus

Ethnopharmacological relevance

Celastrus orbiculatus, a woody vine of the Celastraceae family, has been widely used as a traditional medicine for the treatment of many diseases, including rheumatoid arthritis and odontalgia. In this study, we assessed the sedative and antinociceptive activities of the methanolic extract of Celastrus orbiculatus (MCO).

Materials and methods

The antinociceptive effect of MCO was evaluated using several experimental pain models, including thermal nociception methods, such as the tail immersion and the hotplate tests, as well as chemical nociception induced by intraperitoneal acetic acid and subplantar formalin administration in mice. To verify the possible connection of the opioid receptor to the antinociceptive activity of MCO, we performed a combination test with naloxone, a nonselective opioid receptor antagonist. The sedative effect of MCO was studied using the pentobarbital-induced sleeping model.

Results

MCO demonstrated strong and dose-dependent antinociceptive activity compared to tramadol and indomethacin in various experimental pain models. The combination test using naloxone revealed that the antinociceptive activity of MCO is associated with activation of the opioid receptor. MCO also caused decreased sleep latency and increased sleeping time in the pentobarbital-induced sleeping model; however, MCO alone did not induce sleep.

Conclusions

In the present study, MCO showed potent antinociceptive and sedative activities. Based on these results, MCO may be considered a valuable anti-nociceptive and hypnotic agent for the treatment of various diseases.     

Sedative, antiepileptic and antipsychotic effects of Viscum album L. (Loranthaceae) in mice and rats

Ethnopharmacological relevance

Viscum album L. is claimed in traditional medical practice, to be useful in the treatment of epilepsy and insomnia in Himachal Pradesh, India.

Materials and methods

The effect of Viscum album L. on epilepsy, psychosis and sedative activity was evaluated in mice and rats using standard procedure.

Results

The aqueous leaf extract of Viscum album L. prolonged the pentobarbital induced sleeping time and reduced the locomotor activity in actophotometer. This suggests that reduced locomotor activity facilitate GABAergic transmission. In addition the extract reduced MES, INH and PTZ-induced convulsions which suggest that there may be possibility of blocking Na⁺ channels, opening of Cl⁻channels or enhancing the GABAergic system. The extract decreased the apomorphine-induced stereotyped behavior and potentiates the HAL-induced cataleptic score which suggests the extract possess antidopaminergic activity.

Conclusion

The results obtained in present study suggested that title plant exhibited sedative, antiepileptic and antipsychotic activity in mice and rats.     

Effects of Sini San used alone and in combination with fluoxetine on central and peripheral 5-HT levels in a rat model of depression

Objective

To investigate the effects of Sini San and fluoxetine on the levels of central and peripheral 5-HT in a rat model of depression, and provide new insight into the treatment of depression with integrated Chinese-Western Medicine.

Methods

A rat model of depression was established by chronic mild stress (CMS). Model rats received either Sini San, fluoxetine, a combination of the two drugs, or no drug treatment. Healthy naive rats were used as controls. Open field and sucrose preference tests were used to assess depression-like behavior. ELISA and immunohistochemistry were used to determine central and peripheral levelsof 5-HT.

Results

In the group with no drug treatment, central 5-HT expression decreased while peripheral 5-HT concentrations increased as CMS continued. Four weeks after CMS, Sini San alone was less effective in reducing depression-like behavior than fluoxetine alone or in combination with Sini San, but combined use was more effective than fluoxetine alone. Eight weeks after CMS, Sini San alone or in combination with fluoxetine was more effective in reducing depression-like behavior than fluoxetine alone. Furthermore Sini San and fluoxetine used alone or in combination notably increased central 5-HT expression and decreased peripheral 5-HT levels in the rat model.

Conclusion

The results of the present study indicate that there is a synergistic action between the two medicines in the treatment of depression. Sini San exhibited a relatively long lag before its effects were observed; however, by eight weeks the Traditional Chinese Medicine appeared at least as effective as fluoxetine. We suggest that Sini San can replace fluoxetine in the later stages of depression treatment to minimize side effects observed with long-term fluoxetine administration.     

Depressant effects of Clinopodium mexicanum Benth. Govaerts (Lamiaceae) on the central nervous system

Ethnopharmacological relevance

The decoction of leaves of Clinopodium mexicanum Benth. Goaverts (Lamiaceae), commonly known as “Toronjil de Monte”, is used in the Mexican traditional medicine to induce sleep, as well as sedative and analgesic remedy.

Aim of the study

To evaluate the putative depressant effects of an aqueous extract of the medicinal plant Clinopodium mexicanum on the central nervous system (CNS).

Materials and methods

The effects of the extract (AECM) on mice were tested in several animal paradigms, including sodium pentobarbital-induced sleep, open field tests, and hole-board tests. The effects of AECM on pentylenetetrazole- and picrotoxin-induced convulsions in mice and on the antithermonociceptive response in the hot-plate paradigm were also tested. Additionally, the active extract (AECM) was analyzed with HPLC–ESI-MS techniques.

Results

Mice acutely treated with AECM at 100, 200, 500 and 1000 mg/kg doses prolonged the sleeping time induced by sodium pentobarbital (42 mg/kg). This extract, at 100 and 200 mg/kg doses, showed a sedative effect in the hole-board paradigm and decreased spontaneous activity in mice. AECM at 10, 100 and 200 mg/kg prolonged the onset of seizures induced by pentylenetetrazole (90 mg/kg) and antagonized tonic convulsions induced by picrotoxin (10 mg/kg). Additionally, AECM inhibited the response to a thermonociceptive stimulus. The intraperitoneal AECM treatment produced mortality with an LD₅₀ = 2154 mg/kg. Chemical analysis showed that the flavanone glycosides neoponcirin, poncirin, and isonaringenin are the main compounds of the active extract.

Conclusions

This study demonstrates that an acutely administered single dose of an aqueous extract of Clinopodium mexicanum can exert depressant effects on the CNS. These findings are in agreement with the traditional use of Clinopodium mexicanum to induce sleep as well as sedative and analgesic remedy. The chemical analysis of AECM revealed the presence of the flavanone glycosides neoponcirin, poncirin, and isonaringin.     

Isolation of jacaranone,a sedative constituent extracted from the flowers of the Mexican tree Ternstroemia pringlei

Ethnopharmacological relevance

Ternstroemia pringlei represents one of the most widely employed and commercially exploited medicinal plant in Mexico, used popularly as a tranquilizer and for the treatment of insomnia.

Aim of the study

To investigate the sedative constituents of the plant through a bio-guided fractionation of extracts derived from calyx and fruits.

Materials and methods

Crude extracts with different polarities (CHCl₃, AcOEt, MeOH, aqueous) were prepared and subjected to chromatographic fractionation, leading to the isolation of the sedative compound (1) from the MeOH crude extract. The identity of 1 was unequivocally established by means of 1D and 2D NMR spectroscopic analysis. The sleeping time induced by sodium pentobarbital and the elevated plus-maze models were performed on mice to determine the sedative and anxiolytic activities, respectively. Bioactivity was also investigated though in vitro GABA release experiments using mice brain slices.

Results

The sedative compound was established as jacaranone (1), and its effect was clearly demonstrated through a dose-dependent response analysis (ED₅₀ = 25 mg/kg mouse weight). When tested in the elevated plus-maze model, none of the extracts from Ternstroemia pringlei displayed anxiolytic activity. GABA release experiments showed that the MeOH and aqueous crude extracts released this neurotransmitter at a ratio of 217 and 179 pmol/g protein, respectively, evidencing the presence of other bioactive constituents in the extracts apart of 1, whose activity was absent in this model.

Conclusions

Although 1 has been isolated and identified in a number of plant species, this is the first time that its sedative effect has been demonstrated. No previous record exists of other sedative compounds having been isolated from Ternstroemia pringlei.     

双夏汤不同洗脱液镇静催眠作用研究

目的：研究双夏汤不同洗脱液的镇静催眠作用。方法：通过测定小鼠自主活动和对戊巴比妥钠阈下剂量诱导睡眠的作用,观察双夏汤水煎液、水洗液、20%、70%和95%醇洗液的镇静催眠作用。结果：双夏汤水煎液、20%和95%醇洗液显著降低小鼠的站立次数,分别为78.5%,78.3%和62.5%;双夏汤水洗液和70%醇洗液能显著降低小鼠自主活动次数（P<0.01）、站立次数（P<0.01）和修饰时间（P<0.05）。双夏汤水煎液能明显缩短小鼠睡眠的潜伏期（P<0.05）,延长小鼠睡眠时间（P<0.05）,增加小鼠的入睡率。双夏汤水洗液能显著缩短小鼠睡眠潜伏期（P<0.05）,增加小鼠的入睡率。结论：双夏汤水煎液和水洗液的镇静催眠作用优于醇洗液。     

Anti-hypoxic activity of the ethanol extract from Portulaca oleracea in mice

Aim of the study

To investigate the effects of the ethanol extract from Portulaca oleracea (EEPO) on hypoxia models mice and to find the possible mechanism of its anti-hypoxic actions so as to elucidate the anti-hypoxia activity and provide scientific basis for the clinical use of Portulaca oleracea.

Materials and methods

EEPO was evaluated on anti-hypoxic activity in several hypoxia mice models, including closed normobaric hypoxia and sodium nitrite or potassium cyanide toxicosis. To verify the possible mechanism(s), we detected the activities of pyruvate kinase (PK), phosphofructokinase (PFK), lactate dehydrogenase (LDH) and the level of adenosine triphosphate (ATP) in mice cortices.

Results

Given orally, the EEPO at doses of 100, 200, 400 mg/kg could dose-dependently enhance the survival time of mice in both of the normobaric and chemical hypoxia models. The activity of the glycolysis enzymes and the level of ATP were higher than those of the control. In the pentobarbital sodium-induced sleeping time test and the open-field test, EEPO neither significantly enhanced the pentobarbital sodium-induced sleeping time nor impaired the motor performance, indicating that the observed anti-hypoxic activity was unlikely due to sedation or motor abnormality.

Conclusions

These results demonstrated that the EEPO possessed notable anti-hypoxic activity, which might be related to promoting the activity of the key enzymes in glycolysis and improving the level of ATP in hypoxic mice.     

Pharmacological evaluation of sedative–hypnotic activity and gastro-intestinal toxicity of Rhizoma Paridis saponins

Ethnopharmacological relevance

Rhizoma Paridis saponins (RPS) have been well studied for antimicrobial, anti-hemorrhagic, and anticancer effects. However, scientific information on RPS regarding the toxic and neuropharmacological effects is limited. In this study, the acute oral toxicity, sedative–hypnotic activity and gastro-intestinal toxicity of RPS were investigated.

Materials and methods

The acute toxicity was carried out by administering single doses (800–5000 mg/kg) of RPS to adult mice. Rotarod test and sodium pentobarbital-induced hypnosis activity were used to evaluate the neuropharmacological effects on mice. Gastric emptying and intestinal transit were used to investigate the gastric–intestinal system effects.

Results

A single oral administration of RPS dose-dependently caused adverse effects on the general behavior and mortality rate of mice. LD₅₀ value of oral acute toxicity was 2182.4 mg/kg, with 95% confidence limit of 1718.4–2807.8 mg/kg. In the test of sleeping mice, RPS acted in synergy with sodium pentobarbital at doses 250 and 500 mg/kg while motor coordination was not influenced within 120 min after treatment with RPS. Regarding the gastric–intestinal toxicity, RPS (100, 250, and 500 mg/kg) significantly inhibited gastric emptying but did not affect the intestinal transit.

Conclusions

RPS, which is a hypotoxic anticancer drug, possesses the sedative–hypnotic activity and gastric stimulus side effect.     

Sedative and anticonvulsant activities of methanol extract of Dorstenia arifolia in mice

Ethnopharmacological relevance

Dorstenia arifolia is a plant that has been used in the folk medicine to produce hypnotic, sedative and ansiolitic effects but the pharmacological properties have not yet been studied. In addition, the smoke of its rhizome is reputed to induce lethargic sensation.

Aims of the study

The present study investigated possible activities of the methanol extract (ME) of Dorstenia arifolia rhizome on the central nervous system (CNS).

Materials and methods

ME was tested for sedative, hypnotic and anticonsulsant effects using locomotor activity evaluation, pentobarbital-induced sleeping time and pentylenetetrazol (PTZ)-induced convulsion, respectively.

Results

Intraperitoneal administration of ME (10 and 50 mg/kg) significantly decreased locomotor activity from 205.2 ± 25.6 movements/min (DMSO) to 112.1 ± 18.4 (P < 0.05) and 114.9 ± 16.9 (P < 0.05), respectively. Flumazenil (10 mg/kg), an antagonist of GABA_A receptor, prevented the ME-induced sedation. Treatment with ME (50 mg/kg) significantly increased the duration of pentobarbital-induced sleeping time from 41.0 ± 2.3 to 57.9 ± 2.9 min (P < 0.05). The latencies to seizures after intraperitoneal injection of PTZ was recorded and compared between groups. ME promoted a significant protection of PTZ-induced seizures and mortality in a dose-dependent manner.

Conclusions

Our findings indicate that ME of Dorstenia arifolia rizhome has pronounced central effects, and that the sedative and anticonvulsant activities may be related to a facilitation of the GABAergic transmission.     

Antipsychotic and sedative effects of the leaf extract of Crassocephalum bauchiense (Hutch.) Milne-Redh (Asteraceae) in rodents

Ethnopharmacological relevance

Crassocephalum bauchiense (Hutch.) Milne-Redh (Asteraceae) has been used as a medicine for the treatment of epilepsy, insomnia, dementia and psychotic disorders in Cameroonian traditional medicine.

Aim of the study

This study was designed to examine whether the aqueous extract and the alkaloid fraction prepared from the leaves of Crassocephalum bauchiense possess antipsychotic and sedative properties in rodents.

Materials and methods

The rectal temperature of mice was recorded with a probe thermometer at a constant depth. Novelty-induced rearing behavior is used to evaluate a central excitatory locomotor behavior in mice. The antipsychotic effects of the extracts were assessed using the apomorphine animal model of psychosis. The catalepsy test was tested based on the ability of the leaves extracts of Crassocephalum bauchiense to alter the duration of akinesia by placing the naive mice with both forelegs over a horizontal bar. The extracts of Crassocephalum bauchiense effects were evaluated on sodium pentobarbital-induced sleeping time. In addition, gamma-aminobutyric acid concentrations in the brain treated mice were also estimated.

Results

The aqueous extract and the alkaloid fraction from Crassocephalum bauchiense caused dose-dependent inhibition of novelty-induced rearing behavior, decreased the apomorphine-induced stereotypy and fighting, and had significant fall of the body temperature. The aqueous extract prolonged the sodium pentobarbital sleeping time. This prolongation was not reversed by bicuculline, a light-sensitive competitive antagonist of GABA_A receptors complex. However, the effect of the aqueous extract on sodium pentobarbital-induced sleeping time was blocked by N-methyl-β-carboline-3-carboxamide, a partial inverse agonist of the benzodiazepine site in the GABA_A receptor complex and flumazenil, a specific antagonist of the benzodiazepine site in the GABAA receptor complex. In biochemical experiments, the concentration of the inhibitory amino acid, gamma-aminobutyric acid, was significantly increased in the brain of animals treated with the aqueous extract of Crassocephalum bauchiense and sodium valproate.

Conclusions

The results show that the antipsychotic and sedative properties of Crassocephalum bauchiense are possibly mediated via the blockade of dopamine D-2 receptors and GABAergic activation, respectively. However, pharmacological and chemical studies are continuing in order to characterize the mechanism(s) responsible for these neuropharmacological actions and also to identify the active substances present in the extracts of Crassocephalum bauchiense.     

赤灵芝孢子粉水溶性提取物(肌生注射液)对小鼠的催眠镇静作用

目的：研究赤灵芝孢子粉水提物（肌生注射液）对小鼠中枢神经系统的作用。方法：以翻正反射消失出现时间作为睡眠时间,观察不同剂量和给药方式下肌生液对小鼠戊巴比妥钠和巴比妥钠睡眠时间及自主活动等的影响。结果：皮下注射肌生液可明显延长小鼠戊巴比妥钠和巴比妥钠睡眠时间,且有剂量效应关系。肌生液亦可诱导注射阈下剂量的戊巴比妥的小鼠入睡。每日注射具有镇静作用剂量的肌生液一次连续8天不产生依赖性,而安定连续给药8天后产生依赖性。肌生液可明显减少小鼠的自主活动。结论：灵芝孢子粉水提物对小鼠中枢神经系统具有镇静催眠的效果。     

天王补心丸镇静安神作用的研究

目的:观察天王补心丸镇静催眠的药理作用。方法:选用ICR小鼠,随机分为5组:天王补心丸高、中、低剂量组,空白对照组,安神健脑液组。天王补心丸剂量组分别在(生药)3.24,1.62,0.81 g.kg-1剂量下连续ig给药7 d,测定药物对正常和阴虚模型小鼠自主活动的影响,以及对阈下、阈剂量戊巴比妥钠对催眠作用的影响。结果:测定5 min内小鼠自主活动数/次、睡眠率/%、睡眠潜伏期、维持睡眠时间。小鼠ig天王补心丸,对正常小鼠的自主活动没有明显影响,但能减少阴虚模型小鼠自主活动次数。对戊巴比妥钠所致睡眠有一定的协同作用,缩短小鼠睡眠潜伏期,延长小鼠睡眠时间。结论:天王补心丸具有一定的镇静安神作用。     

Evaluation of anxiolytic and sedative effects of 80% ethanolic Carica papaya L. (Caricaceae) pulp extract in mice

Ethnopharmacological relevance

Carica papaya has been used in the Ethiopian traditional medicine to relieve stress and other disease conditions.

Aim of the study

The present study was undertaken to evaluate the anxiolytic and sedative effects of 80% ethanolic Carica papaya (Caricaceae) pulp extract in mice.

Materials and methods

Carica papaya pulp extract was screened for anxiolytic effect by using elevated plus maze, staircase and open field tests, and ketamine-induced sleeping time test for sedation at doses of 50, 100, 200, 400 mg/kg. Distilled water and Diazepam were employed as negative and positive control groups, respectively.

Results

Carica papaya pulp extract 100 mg/kg significantly increased the percentage of open arm time and entry, and reduced the percentage of entry and time spent in closed arm in elevated plus maze test; reduced the number of rearing in the staircase test; and increased the time spent and entries in the central squares while the total number of entries into the open field were not significantly affected, suggesting anxiolytic activity without altering locomotor and sedative effects. A synergistic reduction in the number of rearing and an inverted U-shaped dose response curves were obtained with important parameters of anxiety

Conclusions

The results of this study established a support for the traditional usage of Carica papaya as anxiolytic medicinal plant.     

Central effects of isolated fractions from the root of Petiveria alliacea L. (tipi) in mice

Ethnopharmacological relevance

Petiveria alliacea L. (tipi) a shrub from Phytolaccaceae family is popularly used in folk medicine for treating a wide variety of disorders in South and Central America.

Aim of the study

To investigate the neuropharmacological properties on experimental animals.

Materials and methods

The acetate (FA), hexanic (FH), hydroalcoholic (FHA) and precipitated hydroalcoholic (FHAppt) fractions from the root of tipi were studied to investigate its pharmacological properties in the classical behavioral models (open-field, elevated plus maze-EPM, rotarod, barbiturate-induced sleeping time, forced swimming and pentylenetetrazole (PTZ)-induced convulsions tests) using mice. These fractions were administered intraperitoneally and orally to female mice at single doses of 100 and 200 mg/kg.

Results

All these fractions decreased the locomotor activity, rearing and grooming in the open-field test, suggesting a possible central depressant action. No significant effect was evident on motor coordination of the animals in the rotarod test. On EPM, all the fractions of tipi presented a significant reduction on the time of permanence in the open arms, indicating an absence of anxiolytic-like effect. In addition, the fractions increased the immobility time in the forced swimming test and potentiated pentobarbital-induced sleeping time in mice, confirmed a probable sedative and central depressant effect. Furthermore, the fractions increased the latency to the first convulsion and the lethal time of the PTZ-induced convulsions test in the animals, confirmed its popular use as anticonvulsant.

Conclusion

Our results suggest that the fractions of P. alliacea L. contains biologically active substance(s) that might be acting in the CNS and have significant depressant and anticonvulsant potentials, supporting folk medicine use of this plant.     

茯苓及其化学拆分组分学习记忆及镇静催眠的性味药理学研究

目的 评价茯苓及其拆分组分的活性,并结合中医传统理论对其进行性味归属。方法 采用东莨菪碱造成小鼠记忆障碍并应用Morris水迷宫实验,观察茯苓及其组分对学习记忆的影响,同时应用抖笼法及戊巴比妥钠协同催眠实验来观察茯苓及其组分的镇静催眠作用。结果 茯苓水煎液（生药8.56 g/kg）、醋酸乙酯组分、石油醚组分、粗多糖组分及精制多糖组分均能明显缩短小鼠到达平台的潜伏期,并且降低东莨菪碱所致记忆障碍小鼠大脑乙酰胆碱酯酶（AchE）活性,醇洗物与水洗物对潜伏期的影响不明显,各个组分对于小鼠的脑指数均有不同程度的增加;生药42.8 g/kg茯苓水煎液可显著延长阈上剂量戊巴比妥钠引起小鼠睡眠时间,而对小鼠睡眠潜伏期没有影响;茯苓粗多糖能显著缩短小鼠的睡眠潜伏期,并且与精制多糖组分均能显著延长小鼠睡眠时间,醋酸乙酯组分作用次之。结论 茯苓改善学习记忆和镇静催眠作用都与其味甘入脾能健脾宁心相关,其醋酸乙酯、石油醚及多糖拆分组分可能为其甘味的物质基础。     

Hypericum grandifolium Choisy: A species native to Macaronesian Region with antidepressant effect

Aim of the study

Various species of Hypericum genus have been used in the Canary Islands as sedative, diuretic, vermifuge, wound healing, antihysteric and antidepressant agent. Studies have shown that methanol extract of Hypericum grandifolium Choisy is active in tetrabenazine-induced ptosis and forced swimming tests. In the current study, the aqueous, butanol and chloroform fractions obtained from the methanol extract as well as three sub-fractions derived from the chloroform fraction were evaluated for their central nervous effects in mice, particularly their antidepressant activity.

Materials and methods

The central nervous effect of different fractions and sub-fractions of Hypericum grandifolium was evaluated in mice using various behavioural models including locomotor and muscle relaxant activity, forced swimming test, effect on normal body temperature, barbiturate-induced sleep, tetrabenazine-induced syndrome and 5-hydroxytryptohan-induced head twitches and syndrome.

Results

We found that the butanol and chloroform fractions and all sub-fractions showed an antidepressant effect in the forced swimming test, the chloroform fraction being the most active. They produced no effects or only a slight depression of locomotor activity. Chloroform fraction significantly increased the pentobarbital-induced sleeping time, produced a slight but significant hypothermia and antagonized tetrabenazine-induced ptosis, whereas the butanol fraction produced a slight potentiation of 5-HTP-induced head twitches and syndrome.

Conclusions

The present results, together with previous pharmacological and phytochemical data, indicated that Hypericum grandifolium possess antidepressant-like effects in mice and that different constituents, such as the flavonoids and the benzophenone derivatives, could be responsible at least in part for the antidepressant effects observed for this species.