C.U. Shah College of Pharmacy, SNDT University Santacruz (W), Mumbai 400 049, Maharashtra, India.
The plant Butea frondosa has been indicated in the Indian system of medicine as a plant augmenting memory and as a rejuvenator. The effect of oral administration of the aqueous and alcoholic extracts of the leaves was assessed on stress, cognitive function, and anxiety in albino rats. The antistress activity was evaluated using cold restraint induced ulcers and leukocyte count after subcutaneous injection of milk. The aqueous extract provides protection against stress-induced gastric lesions while both the alcoholic as well as the aqueous extract normalizes the white blood cell count. Effect on cognitive function was evaluated using Cook and Weidley's pole apparatus. The results indicate that the aqueous extract and the alcoholic extract when administered at a dose of 300 mg/kg for a period of 7 days augment both the acquisition as well as the retention of memory of learned task. The absence of an increase in the occupancy of the open arm in the elevated plus maze and in the number of head dips in the hole-board paradigms indicates that both the extracts are devoid of anxiolytic activity. Nootropic activity was compared using piracetam (100 mg/kg po) as the standard, while for anxiolytic and antistress activity, diazepam (1.0 mg/kg ip) was employed as the standard drug. It is concluded that the aqueous and alcoholic extract of B. frondosa possesses antistress and weak nootropic activity.
Ratchanaporn Chokchaisiri, Channarong Suaisom, Siriluk Sriphota, Anon Chindaduang, Thipphawan Chuprajob, Apichart Suksamrarn
Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, Ramkhamhaeng University, Bangkok, Thailand.
One new dihydrochalcone, dihydromonospermoside (7), was isolated from the flowers of Butea monosperma together with three known chalcones, butein (2), monospermoside (4) and isoliquiritigenin (8), one flavone, 7,3',4'-trihydroxyflavone (6), four flavanones,(-)-butin (1a),(-)-butrin (3a),(+)-isomonospermoside (5b) and (-)-liquiritigenin (9a), and three isoflavones, formononetin (10), afrormosin (11) and formononetin-7-O-beta-D-glucopyranoside (12). The structure of the new compound was elucidated by spectroscopic techniques whereas those of the known compounds were identified by comparisons of spectroscopic and some physical data with those of reported compounds. The absolute configurations at the 2-position of the flavanones 1a, 3a, 5b and 9a were established to be 2S, 2S, 2R and 2S, respectively, by circular dichroism spectral measurements and were confirmed by comparison of the optical rotations with those of reported values and by enzymic hydrolysis of the glucosides to the corresponding aglycones. The isolated flavonoids exhibited varying antimycobacterial activity with the chalcone 2 being the most active compound (MIC 12.5 microg/ml).
Effect of Convulvulus pluricaulis Choisy. on learning behaviour and memory enhancement activity in rodents.
Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar, M.P., India.
The present study was undertaken to investigate the effects of Convulvulus pluricaulis (CP), considered as Shankhpushpi on learning and memory in rodents. Nootropic activity using Cook and Weidley's Pole Climbing Apparatus, passive avoidance paradigms and active avoidance tests were used to test learning and memory. The ethanolic extract of CP and its ethyl acetate and aqueous fractions were evaluated for their memory enhancing properties. Two doses (100 and 200 mg kg(-1) p.o.) of the ethanolic extract and ethyl acetate and aqueous fractions were administered in separate groups of animals. Both the doses of all the extracts of CP significantly improved learning and memory in rats. Furthermore, these doses significantly reversed the amnesia induced by scopolamine (0.3 mg kg(-1) i.p.). Nootropic activity was compared using piracetam as the standard. Moreover, CP has exhibited potent memory-enhancing effects in the step-down and shuttle-box avoidance paradigms. Further studies are necessitated to identify the exact mechanism of action.
Influence of sex on the interaction between dizocilpine (MK-801) pretreatment and acute cold-restraint stress in epilepsy susceptibility in an animal study.
Department of Science, Tarsus American College, Tarsus, Mersin, Republic of Turkiye. email@example.com
BACKGROUND Stress is a part of our daily life, inducing neurochemical and neurophysiological changes in the central nervous system. OBJECTIVE The present study was designed to investigate the importance of sex differences in the interaction between dizocilpine (MK-801) pretreatment and acute cold-restraint stress (CRS) in pentylenetetrazole (PTZ)-induced seizures in Swiss albino mice. METHODS A CRS protocol was applied to mice to investigate the interaction between MK-801 pretreatment (30 min before CRS) and stress (followed by PTZ injection) in epilepsy susceptibility. For this purpose, 6 groups were designated:(1) PTZ control group (received only PTZ);(2) stress group (received stress and PTZ);(3) saline group (received saline and PTZ);(4) MK-801 group (received MK-801 and PTZ);(5) saline + stress group (received saline, stress, and PTZ); and (6) MK-801 + stress group (received MK-801, stress, and PTZ). RESULTS Pretreatment with MK-801 (0.125, 0.25, 0.50 mg/kg) significantly potentiated the protective effect of stress in PTZ-induced (65 mg/kg) seizures in both sexes by prolonging the onset of myoclonic jerks and clonic convulsions. Male mice had a significantly greater delay in the onset of myoclonic jerks (males, 66.7-295.5 sec; females, 54.0-247.5 sec; P < 0.05) and clonic convulsions (males, 123.5-789.8 sec; females, 94.5-757.2 sec; P < 0.05) compared with female mice in all groups (ie, PTZ control, stress, saline, MK-801, saline + stress, and MK-801 + stress groups). CONCLUSION The findings of this study in mice suggest the involvement of sex hormones in the interaction between MK-801 pretreatment and acute CRS in PTZ-induced seizures.
Nattaya Ngamrojanavanich, Aimon Loontaisong, Somchai Pengpreecha, Wichai Cherdshewasart, Surachai Pornpakakul, Khanitha Pudhom, Sophon Roengsumran, Amorn Petsom
Research Centre for Bioorganic Chemistry, Faculty of Science, Chulalongkorn University, Pyathai Road, Pathumwan, Bangkok, Thailand. firstname.lastname@example.org
A carpin (3-hydroxy-9-methoxypterocarpan)(Medicarpin)(1) and four isoflavones, 7-hydroxy-4'-methoxy-isoflavone (Formononetin)(2); 7,4'-dimethoxyisoflavone (3); 5,4'-dihydroxy-7-methoxy-isoflavone (Prunetin)(4) and 7-hydroxy-6,4'-dimethoxyisoflavone (5) were isolated from the tuber roots of Butea superba Roxb. Compounds 2 and 4 showed moderate cytotoxic activity on KB cell lines with IC(50)(microM) values of 37.3+/-2.5 and 71.1+/-0.8 and on BC cell lines with IC(50)(microM) values of 32.7+/-1.5 and 47.3+/-0.3, respectively.
Inhibition within the nucleus tractus solitarius (NTS) ameliorates environmental exploration deficits due to cerebellum lesions in an animal model for autism.
Department of Psychology, Georgetown University, Washington, DC 20057, USA. email@example.com
Clinical observations suggest that abnormalities within the cerebellum and/or the cerebellum--cholinergic forebrain connections may be key to explain the severe behavioral deficits and increases in seizures seen in autism. In order to explore functional relationships between brain areas implicated in many of the core behavioral features of autism, experiments utilizing animal models for specific autism-like behaviors have increased in recent years. In the current study, we used a rodent model for the autism-like behavior of environment exploration deficits to examine the role of the cerebellum and its connectivity to the forebrain. In addition, due to the possible common neural pathways between seizures and autism-like behaviors, we explored the possibility for limiting autism-like behaviors via antiseizure brainstem and cerebellar circuitry. In two experiments, adult male rats showed a significant decrease in exploration behavior following developmental cerebellar suction lesions (experiment 1) or i.c.v. saporin injections specifically targeting Purkinje cells, but not after the addition of saporin-induced cholinergic forebrain lesions (experiment 2). In both experiments, the anticonvulsant treatment of inhibition of the medullary nucleus tractus solitarius (NTS) restored exploration behavior to control levels. These findings suggest that specific neuronal populations within the cerebellum are responsible for mediating exploration behavior, and these neuronal populations are similar to the circuitry involved in limbic motor seizures in that they are sensitive to brainstem inhibition. Furthermore, these results suggest this connection could be utilized in order to control behavioral deficits seen in autism with treatments, such as vagal nerve stimulation, which are effective against pharmaco-resistant seizures.
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C.U. Shah College of Pharmacy, S. N. D. T. Women's University, Santacruz [W], Mumbai 400 049, India.
The present study deals with the investigation of standardized and phytochemically evaluated aqueous and hydroalcoholic extracts of the plant Eclipta alba for sedative, muscle-relaxant, anxiolytic, nootropic and anti-stress activities. The hydrolyzed fraction of the aqueous extract was also subjected to similar studies in rats. The aqueous and hydroalcoholic extracts were administered in a dose of 150 and 300 mg/kg, p.o., while the hydrolyzed fraction was administered in a dose of 30 mg/kg, p.o. The findings indicated nootropic activity of the aqueous extract (300 mg/kg, p.o.) and its hydrolyzed fraction (30 mg/kg, p.o.). The effect of the extracts on stress-induced alterations was evaluated. The aqueous extract and the hydrolyzed fraction provided protection against cold restraint induced gastric ulcer formation and also normalized the white blood cell count in the milk induced leukocytosis challenge model. The hydroalcoholic extract on the other hand demonstrated a significant effect only in the milk induced leukocytosis challenge model. The results point towards the potential neuropharmacological activity of the plant Eclipta alba as a nootropic and also having the property of attenuating stress induced alterations. Further neurochemical investigations can unravel the mechanism of action of the plant drug with respect to nootropic activity and help to establish the plant in the armamentarium of nootropic agents.
Natural Products Laboratory, MVP Samaj's College of Pharmacy, Nashik 422 002, India.
The present investigation was aimed at determining the spectrum of activity of the methanolic extract of Clitoria ternatea (CT) on the CNS. The CT was studied for its effect on cognitive behavior, anxiety, depression, stress and convulsions induced by pentylenetetrazol (PTZ) and maximum electroshock (MES). To explain these effects, the effect of CT was also studied on behavior mediated by dopamine (DA), noradrenaline, serotonin and acetylcholine. The extract decreased time required to occupy the central platform (transfer latency, TL) in the elevated plus maze (EPM) and increased discrimination index in the object recognition test, indicating nootropic activity. The extract was more active in the object recognition test than in the EPM. The extract increased occupancy in the open arm of EPM by 160% and in the lit box of the light/dark exploration test by 157%, indicating its anxiolytic activity. It decreased the duration of immobility in tail suspension test (suggesting its antidepressant activity), reduced stress-induced ulcers and reduced the convulsing action of PTZ and MES. The extract exhibited tendency to reduce the intensity of behavior mediated via serotonin and acetylcholine. The effect on DA- and noradrenaline-mediated behavior was not significant. In conclusion, the extract was found to possess nootropic, anxiolytic, antidepressant, anticonvulsant and antistress activity. Further studies are necessary to isolate the active principle responsible for the activities and to understand its mode of action.
N.D.M.V.P. Samaj's College of Pharmacy, Nashik - 422 002, India.
The benzene fraction (BF) of a petroleum ether extract of dried rhizomes of ginger, which contained anticonvulsant principle(s), was screened for anxiolytic and antiemetic activity. Motor coordination was not affected by BF per se, but diazepam-induced motor incoordination was potentiated. Animals treated with BF showed decreased occupancy in the closed arm of the elevated plus maze suggesting the presence of anxiolytic principles in the BF. BF also blocked lithium sulphate-induced conditioned place aversion indicating antiemetic activity. These findings suggest that the fraction (BF) possesses anticonvulsant, anxiolytic and antiemetic activity.
Department of Pharmacology, M.V.P. Samaj's College of Pharmacy, Nashik 422 002, Maharashtra, India.
The effect of saponin containing n-butanolic fraction (BF) extracted from dried leaves of Albizzia lebbeck on learning and memory was studied in albino mice using passive shock avoidance paradigm and the elevated plus maze. Significant improvement was observed in the retention ability of the normal and amnesic mice as compared to their respective controls. We have also studied the effects of BF on the behavior influenced by serotonin (5-HT), noradrenaline and dopamine. The brain levels of serotonin, gamma-aminobutyric acid (GABA) and dopamine were also estimated to correlate the behavior with neurotransmitter levels. The brain concentrations of GABA and dopamine were decreased, whereas the 5-HT level was increased. The data indicate the involvement of monoamine neurotransmitters in the nootropic action of BF of A. lebbeck.
Natural Products Laboratory, NDMVP Samaj's College of Pharmacy, Nāshik, India. firstname.lastname@example.org
The bioassay-guided fractionation of dried flowers of Butea monosperma (BM) was carried out to isolate the active principle responsible for its anticonvulsant activity. The petroleum ether extract was fractionated by column chromatography using solvents of varying polarity such as n-hexane, n-hexane:ethyl acetate, ethyl acetate, and methanol. The anticonvulsive principle of B. monosperma was found to be a triterpene (TBM) present in the n-hexane:ethyl acetate (1:1) fraction of the petroleum ether extract. TBM exhibited anticonvulsant activity against seizures induced by maximum electroshock (MES) and its PD(50) was found to be 34.2+/-18.1 mg/kg. TBM also inhibited seizures induced by pentylenetetrazol (PTZ), electrical kindling, and the combination of lithium sulfate and pilocarpine nitrate (Li-Pilo). However, TBM was not effective against seizures induced by strychnine and picrotoxin. TBM exhibited depressant effect on the central nervous system. After repeated use for 7 days, the PD(50)(MES) of TBM increased to 51.5+/-12.1 mg/kg. Similarly, after repeated use of TBM, the duration of sleep induced by pentobarbital was not reduced significantly. Further studies are required to investigate its usefulness in the treatment of epilepsy.
Natural Products Laboratory, M.V.P. Samaj's College of Pharmacy, Nashik 422-002, India.
In the present study, the n-hexane extract of Myristica fragrans (MF) seeds, acetone-insoluble part of the n-hexane extract (AIMF) and trimyristin (TM) were assessed for their anxiogenic activity. The MF (10 and 30 mg/kg), AIMF (30, 100, and 300 mg/kg), and TM (10, 30, and 100 mg/kg) administered intraperitoneally exhibited anxiogenic activity in elevated plus-maze (EPM) paradigm. The open-field test and hole-board test were also used to assess anxiogenic activity of AIMF and TM. In the EPM test, MF, AIMF, and TM decreased the time spent by mice in the open arm and the entries in the open arm. Further, the effect of diazepam (1 mg/kg i.p.), serotonin 5-HT3 receptor antagonist, ondansetron (1 mg/kg i.p.), and 5-HT1A receptor agonist, buspirone (1 mg/kg i.p.), on the occupancy in open arm and entries in open arm was significantly reduced by TM. In the open-field test, AIMF as well as TM reduced the number of rearing and locomotion. Both TM and AIMF reduced the number of head pock in the hole-board test. Inhibition of anxiolytic activity of ondansetron (5-HT3 receptor antagonist), buspirone (5-HT1A receptor agonist), and diazepam [acting on gamma-aminobutyric acid (GABAA) receptor] suggests a nonspecific anxiogenic activity of TM and also a link between 5-HT and GABA systems in the anxiogenic activity of TM.
Department of Pharmacology, MVP Samaj's College of Pharmacy, Nashik 422 002, Maharashtra State, India.
The effect of saponin containing, n-butanolic fraction (BF), extracted from dried leaves of Albizzia lebbeck, was studied on cognitive behavior and anxiety in albino mice. The elevated plus maze was used for assessment of both nootropic and anxiolytic activity. The nootropic activity was evaluated by recording the effect of BF (0, 10, 25, and 50 mg/kg) on the transfer latency, whereas anxiolytic activity was assessed by studying its effect on the duration of occupancy in the closed arm. Results showed significant improvement in the retention ability of the normal and amnesic mice as compared to their respective controls. Animals treated with BF (25 mg/kg) spent more time in the open arm in a dose-dependent manner. The BF was without any significant effect on motor coordination. However, it significantly inhibited passivity and hypothermia induced by baclofen (10 mg/kg), a GABA(B) agonist. The data emanated in the present study suggests involvement of gamma-aminobutyric acid (GABA) in the nootropic and anxiolytic activity of saponins obtained from A. lebbeck.
Effect of drugs influencing central serotonergic mechanisms on pentazocine-induced catalepsy in mice.
Department of Pharmacology, College of Pharmacy, Nashik, India.
Cataleptic effect of pentazocine in mice was affected by pretreatment with dexfenfluramine, fluoxetine, buspirone, p-chlorophenylalanine, cyproheptadine, mianserin, cisapride, ondansetron, pindolol and propranolol. The results suggest that drugs which influence the activity of central serotonergic systems do modulate pentazocine-induced catalepsy in mice.
Comparative evaluation of Butea frondosa and flurbiprofen for ocular anti-inflammatory activity in rabbits.
C. U. Shah College of Pharmacy, Women's University, Bombay, India.
The roots and leaves of the plant Butea frondosa were evaluated for ocular anti-inflammatory activity on the subacute model of ocular inflammation in rabbits. The arkas (liquid preparations obtained by distillation of certain liquids or drugs soaked in water, using the Arka-Yantra or any other convenient modern distillation apparatus) were prepared using the roots and leaves of the plant. The arkas were formulated as gels using Pluronic F-127 (PF-127) 30% w/w as the polymer. The anti-inflammatory activity of the preparations were assessed by determining their effects on elevated intraocular pressure consequent to breakdown of blood/aqueous humour barrier. A commercial eyedrop of flurbiprofen 0.03% w/w was used to compare the ocular anti-inflammatory activity of the arkas of the plant. A marketed root arka was included in the study for comparison. The anti-inflammatory activity of the arkas formulated as gels were compared with flurbiprofen gel prepared using the same polymer. The changes in intraocular pressure were monitored at various time intervals after a single dose administration of the aqueous as well as gel formulations. In multiple dose studies the aqueous preparations were administered three times a day, while the gels were administered once a day up to day 30 and the intraocular pressure was monitored on different days post-administration. The findings reveal statistically significant differences (P < 0.05) between the arkas of the plant and the commercial eyedrop of flurbiprofen. The arkas of the plant proved to be better than the eyedrop of flurbiprofen, while with respect to gels, the intraocular pressure monitored at various time intervals revealed no statistically significant difference (P > 0.05) between the gel formulations. However, the changes in intraocular pressure monitored on different days post-administration until day 30, demonstrated that the gel produced from B. frondosa leaves arka was superior to all the other gels with respect to the extent of reduction of elevated intraocular pressure elicited experimentally.
M. V. P. Samaj's College of Pharmacy, Nashik, India.
Baclofen, a GABAB receptor agonist can induce catatonia in rats. This catatonia may serve as a tool for the study of GABAB receptor function. Reciprocal interactions between serotonin (5-HT) and GABAB receptors in the CNS are known to occur. In the present study we examined the effect of various agents that influence serotonergic neurotransmission on baclofen-induced catatonia in rats. The catatonia was rated by means of a scoring method, according to the severity of motor symptoms produced by baclofen (10-15 mg/kg, i.p.). All serotonergic drugs were injected intraperitoneally 30 min prior to baclofen, except the 5-HT synthesis inhibitor p-chlorophenylalanine (PCPA), which was injected 72 and 48 hr prior to baclofen. The 5-HT releaser fenfluramine (10 mg/kg) and the uptake inhibitor fluoxetine (10 mg/kg) reversed, whereas the 5-HT1A agonist buspirone (3 mg/kg) potentiated baclofen-induced catatonia. The 5-HT synthesis inhibitor PCPA (150 x 2 mg/kg), the non-specific 5-HT antagonist cyproheptadine (5 mg/kg), the 5-HT1A/1B antagonist pindolol (3 mg/kg) and the 5-HT2 antagonist sulpiride (20 mg/kg) enhanced baclofen-induced catatonia. It is concluded that the manipulations of central serotonergic mechanisms modulate baclofen-induced catatonia.
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Ayu. 2011 Jul ;32 (3):375-9 22529654
Evaluation of anti-depressant and anxiolytic activity of Rasayana Ghana Tablet (A compound Ayurvedic formulation) in albino mice.
Lecturer, Department of Kayachikitsa, GJ Patel Ayurveda College and Research Centre, New Vallabh Vidya Nagar, India.
In recent years, many Ayurvedic formulations are being researched to provide an effective antidepressant and anxiolytic drug in the field of psycho-pharmacology. The present study was planned to evaluate the anti-depressant and anxiolytic activity of Rasayana Ghana Tablet comprising three herbs Guduchi (Tinospora cordifolia Miers), Aamalaki (Emblica officinalis Garten)(RGT) and Gokshura (Tribulus terrestris Linn). Swiss albino mice were divided into four groups of six animals each, comprising of both male and female in each group. Group I received water served as normal control (WC), group II received vehicle and served as vehicle control (VC), group III received Rasayana Ghana tablet and group IV received standard drug diazepam (2 mg/kg) for anxiolytic study in elevated plus maze and standard antidepressant imipramine (5 mg/kg) for anti-depressant activity in behavior despair test. Rasayana Ghana tablet along with ghee and honey as vehicle is found to be having antidepressant and anxiolytic activity in experimental animals. Thus, this formulation can be used in prevention and treatment of depression and anxiety.
Pharm Biol. 2012 Jul ;50 (7):878-82 22489538
L.R. Institute of Pharmacy , Solan, Himachal Pradesh , India.
Context: Medicago sativa Linn.(Leguminosae) has a long tradition of use as an Ayurvedic and Homoeopathic medicine in a variety of central nervous system (CNS) disorders. Traditionally, M. sativa is used to improve the memory, as a rejuvenator, antidiabetic, antioxidant, anti-inflammatory, and in CNS disorders. Despite a long tradition of use, no systematic phytochemical and pharmacological work has been carried out on this potential plant. M. sativa was subjected to preliminary anti-anxiety screening studies, with a view to ascertain the verity of its traditional use as an anxiolytic. Objective: Various extracts, viz., petroleum ether, chloroform, methanol and aqueous extract from the aerial parts of M. sativa was subjected to preliminary anti-anxiety screening studies, with a view to ascertain the truth on evidence of its traditional use as an anxiolytic. Materials and methods: The aerial parts of the plant were extracted using solvents in order of increasing polarity, viz., petroleum ether (60-80°C), chloroform, methanol and distilled water. All the crude extracts were evaluated for anti-anxiety activity in mice using elevated plus-maze apparatus. Diazepam was used as the standard drug. Results: Among all extracts, only the methanol extract exhibited significant (p < 0.05) anti-anxiety activity by increasing the average time spent, and number of entries in open arms at a dose of 100 mg/kg in mice with respect to the vehicle treated control as well as the standard (2 mg/kg). Conclusion: These results suggest that administration of M. sativa exerts anxiolytic effect on mice, and it could serve as a new approach for the treatment of anxiety.
Mohammed Garba Magaji, Abdullahi Hamza Yaro, Aliyu Muhammad Musa, Joseph Akponso Anuka, Ibrahim Abdu-Aguye, Isa Marte Hussaini
Department of Pharmacology and Therapeutics, Ahmadu Bello University, Zaria, Nigeria.
ETHNOPHARMACOLOGICAL RELEVANCE Securinega virosa is a commonly used medicinal plant in African traditional medicine in the management of epilepsy and mental illness. Previous studies in our laboratory showed that the crude methanol root bark extract of the plant possesses significant behavioral effect in laboratory animals. In an attempt to isolate and characterize the biological principles responsible for the observed activity, this study is aimed at evaluating the central depressant activity of the butanol fraction of the methanol root bark extract of Securinega virosa. MATERIALS AND METHODS The medial lethal dose of the butanol fraction was estimated using the method of Lorke. Preliminary phytochemical screening was conducted on the butanol fraction using standard protocol. The behavioral effect of the butanol fraction (75, 150 and 300mg/kg) was evaluated using diazepam induced sleep test, hole-board test, beam walking assay, staircase test, open field test and elevated plus maze assay, all in mice. RESULTS The median lethal dose of the butanol fraction was estimated to be 1256.9mg/kg. The preliminary phytochemical screening revealed the presence of tannins, saponins, alkaloids, flavonoids, cardiac glycosides, similar to those found in the crude methanol extract. The butanol fraction significantly (P<0.001) reduced the mean onset of sleep in mice and doubled the mean duration of sleep in mice at the dose of 75mg/kg. The butanol fraction and diazepam (0.5mg/kg) significantly (P<0.01-0.001) reduced the number of head dips in the hole-board test suggesting sedative effect. The sedative effect of the butanol fraction was further corroborated by its significant (P<0.01-0.001) reduction of the number of step climbed and rearing in the staircase test. The butanol fraction did not significantly increase the time taken to complete the task and number of foot slips in the beam walking assay, suggesting that it does not induce significant motor coordination deficit. Diazepam (2mg/kg), the standard agent used significantly (P<0.01) increased the number of foot slips. In the open field test, the butanol fraction significantly reduced the number of square crossed as well as the number of rearing. However, the butanol fraction did not significantly alter the behavior of mice in the elevated plus maze assay, while diazepam (0.5mg/kg) significantly (P<0.05) increased the time spent in the open arm and reduced the number of closed arm entry. CONCLUSION The findings of this study suggest that the butanol fraction of Securinega virosa root bark contains some bioactive principles that are sedative in nature.
Sedative and Hypnotic Activities of the Methanolic and Aqueous Extracts of Lavandula officinalis from Morocco.
Laboratory of Genetic Immunology and Biochemistry, Department of Biology, Faculty of Science, Mohammed V Agdal University, BP 6203, Rabat Instituts, Agdal, Rabat, Morocco.
We evaluate the sedative and hypnotic activities of the methanolic and aqueous extract of Lavandula officinalis L. on central nervous system (CNS). In this study, the effect of the methanolic and aqueous extracts of this plant was investigated in a battery of behavioural models in mice. Stems and flowers of Lavandula officinalis L. have several therapeutic applications in folk medicine in curing or managing a wide range of diseases, including insomnia. The methanolic extract produced significant sedative effect at the doses of 200, 400, and 600 mg/kg (by oral route), compared to reference substance diazepam (DZP), and an hypnotic effect at the doses of 800 and 1000 mg/kg while the treatment of mice with the aqueous extract at the doses of 200 and 400 mg/kg via oral pathway significantly reduced in both the reestablishment time and number of head dips during the traction and hole-board tests. In conclusion, these results suggest that the methanolic and aqueous extracts of Lavandula officinalis possess potent sedative and hypnotic activities, which supported its therapeutic use for insomnia.
Protective effects of total alkaloidal extract from Murraya koenigii leaves on experimentally induced dementia.
Vasudevan Mani, Kalavathy Ramasamy, Aliya Ahmad, Milind Parle, Syed Adnan Ali Shah, Abu Bakar Abdul Majeed
Brain Research Laboratory, Faculty of Pharmacy, Puncak Alam Campus, Universiti Teknologi MARA (UiTM), 42300 Bandar Puncak Alam, Selangor, Malaysia. email@example.com
Dementia is a syndrome of gradual onset and continuous decline of higher cognitive functioning. It is a common disorder in older persons and has become more prevalent today. The fresh leaves of Murraya koenigii are often added to various dishes in Asian countries due to the delicious taste and flavor that they impart. These leaves have also been proven to have health benefits. In the present study, the effect of total alkaloidal extract from M. koenigii leaves (MKA) on cognitive functions and brain cholinesterase activity in mice were determined. In vitro β-secretase 1 (BACE1) inhibitory activity was also evaluated. The total alkaloidal extract was administered orally in three doses (10, 20 and 30 mg/kg) for 15 days to different groups of young and aged mice. Elevated plus maze and passive avoidance apparatus served as the exteroceptive behavioral models for testing memory. Diazepam-, scopolamine-, and ageing-induced amnesia served as the interoceptive behavioral models. MKA (20 and 30 mg/kg, p.o.) showed significant improvement in memory scores of young and aged mice. Furthermore, the same doses of MKA reversed the amnesia induced by scopolamine (0.4 mg/kg, i.p.) and diazepam (1 mg/kg, i.p.). Interestingly, the brain cholinesterase activity was also reduced significantly by total alkaloidal extract of M. koenigii leaves. The IC50 value of MKA against BACE1 was 1.7 μg/mL. In conclusion, this study indicates MKA to be a useful remedy in the management of Alzheimer's disease and dementia.
J Med Food. 2011 Sep ;14 (9):912-9 21812651
Ocimum sanctum Linn. leaf extracts inhibit acetylcholinesterase and improve cognition in rats with experimentally induced dementia.
Vijayasree Vayalanellore Giridharan, Rajarajan Amirthalingam Thandavarayan, Vasudevan Mani, Taranalli Ashok Dundapa, Kenichi Watanabe, Tetsuya Konishi
Department of Functional and Analytical Food Sciences, Niigata University of Pharmacy & Applied Life Sciences (NUPALS), Niigata, Japan.
Cognitive disorders such as dementia, attention deficits, and Alzheimer's disease (AD) have been well investigated. However, effective interventions for the promotion and progression of AD are unavailable to date. The present work was undertaken to investigate the effects of the aqueous (300 and 500 mg/kg) and alcoholic (300 and 500 mg/kg) extracts of Ocimum sanctum Linn. leaves as an antidementic and anticholinesterase agent and also as an immunostimulant in rats. Maximal electroshock, atropine, and cyclosporine were used to induce dementia. The passive avoidance task was used for assessing memory. Acetylcholinesterase (AChE) activity was estimated in different parts of the brain, and immune status was studied using dinitrochlorobenzene (DNCB) skin sensitivity tests. In all the three models both aqueous and alcoholic O. sanctum extracts decreased the time taken to reach the shock-free zone and the number of mistakes and significantly decreased the AChE activity in rats. O. sanctum treatment significantly increased the induration in the DNCB skin test. Therefore, O. sanctum was shown to be useful for the management of experimentally induced cognitive dysfunctions in rats.
Department of Pharmacology, Institute of Post Graduate Medical Education and Research, Kolkata, India.
The present study was undertaken to explore the protective effects of tuberous root extract of Pueraria tuberosa on chronic foot shock stress (CS) induced physiological, neurobehavioral and neuropathological alterations. Male Wistar rats (120-150 g) were divided into seven groups, consisting of ten animals in each. Group I served as normal, group II as positive control, while group III-VII as test drug treated. P tuberosa tuber extract (PTE) was given to rats of groups III-VI at the doses of 50, 100, 200 and 400 mg/kg respectively, while group VII treated with Withania somnifera rhizome extract (WSE)(100 mg/kg) as reference drug. Group II (stress control) received only equivalent volume of distilled water (0.5 ml/100 g) orally. All the drugs were given orally once/day for 14 consecutive days. The last dose was given 1 h before study. Simultaneously, all the animals (except group I) were subjected to 1 h of foot-shock (2 mA) through a grid floor for those 14 days in a standard conditioning chamber with the escape route closed [Chronic stress (CS)]. Thereafter, the rats were placed on open-field and plus maze apparatus for studying the behavioral patterns of them, and the anxiolytic effects of the putative drug. Sexual activities of the animals were also studied. Finally, the animals were sacrificed and their ulcer formation in gastric mucosa was noted. Weights of adrenals and spleen were also taken. Further, plasma corticosterone levels were estimated spectroflurometrically. Results indicated that, CS significantly altered the behavioral patterns, decreased the sexual urge and activities, damaged the gastric mucosal layers, enhanced plasma corticosterone levels and increased adrenal glands and spleen weights. PTE and WSE showed significant anxiolytic activity, protected the gastric mucosa, lowered plasma corticosterone level (indicating HPA axis inhibition) and negated the hypertrophy of adrenals and spleen. PTE also enhanced the sexual urge and activities in animals exposed to chronic stress. The findings suggest significant anxiolytic and anti-stress properties of PTE, confirming the clinical efficacy of the plant mentioned in Ayurveda (Indian system of traditional medicine).
Anxiolytic activity of a supercritical carbon dioxide extract of Souroubea sympetala (Marcgraviaceae).
Martha Mullally, Kari Kramp, Chris Cayer, Ammar Saleem, Fida Ahmed, Calum McRae, John Baker, Andrew Goulah, Marco Otorola, Pablo Sanchez, Mario Garcia, Luis Poveda, Zul Merali, Tony Durst, Vance L Trudeau, John Thor Arnason
Centre for Research in Biopharmaceuticals and Biotechnology, Department of Biology, University of Ottawa, Ottawa, ON, Canada, K1N 6N5.
The purpose of this work was to develop an extraction technique to yield a betulinic acid-(BA) enriched extract of the traditional anti-anxiety plant Souroubea sympetala Gilg (Marcgraviaceae). Five extraction techniques were compared: supercritical carbon dioxide extraction (SCE), conventional solvent extraction with ethyl acetate (EtOAc), accelerated solvent extraction (ASE), ultrasonic assisted extraction (UAE) and soxhlet extraction (Sox). The EtOAc and SCE extraction methods resulted in BA-enriched extracts, with BA concentrations of 6.78 ± 0.2 and 5.54 ± 0.2 mg/g extract, respectively, as determined by HPLC-APCI-MS. The bioactivity of the BA-enriched extracts was compared in the elevated plus maze (EPM), a validated rodent anxiety behaviour assay. Rats orally administered a 75 mg/kg dose of SCE extract exhibited anxiolysis as compared with vehicle controls, with a 50% increase in the percent time spent in the open arms, a 73% increase in unprotected head dips and a 42% decrease in percent time spent in the closed arms. No significant differences were observed between the SCE and EtOAc extracts for these measures, but the animals dosed with SCE extract had significantly more unprotected head dips than those dosed with the EtOAc extract. The SCE extract demonstrated a dose-response in the EPM, with a trend toward decreased anxiety at 25 mg/kg, and significant anxiolysis was only observed at 75 mg/kg dose. This study demonstrates that SCE can be used to generate a betulinic acid-enriched extract with significant anxiolysis in vivo. Further, the study provides a scientific basis for the ethnobotanical use of this traditional medicine and a promising lead for a natural health product to treat anxiety.
Department of Pharmacology, Government College of Pharmacy, Bengaluru, Karnataka, India. firstname.lastname@example.org
The effect of Celastrus paniculatus Willd.(Celastraceae) seed aqueous extract on learning and memory was studied using elevated plus maze and passive avoidance test (sodium nitrite induced amnesia rodent model). The aqueous seed extract was administered orally in two different doses to rats (350 and 1050 mg/kg) and to mice (500 and 1500 mg/kg). The results were compared to piracetam (100 mg/kg, p.o.) used as a standard drug. Chemical hypoxia was induced by subcutaneous administration of sodium nitrite (35 mg/kg), immediately after acquisition training. In elevated plus maze and sodium nitrite-induced amnesia model, Celastrus paniculatus extract has showed statistically significant improvement in memory process when compared to control. The estimation of acetylcholinesterase enzyme in rat brain supports the plus maze and passive avoidance test by reducing acetylcholinesterase activity which helps in memory performance. The study reveals that the aqueous extract of Celastrus paniculatus seed has dose-dependent cholinergic activity, thereby improving memory performance. The mechanism by which Celastrus paniculatus enhances cognition may be due to increased acetylcholine level in rat brain.
Department of Psychology, Eastern Oregon University, LaGrande, OR 97850, USA.
Valerian root (Valeriana officinalis) is a popular and widely available herbal supplement, primarily used to treat insomnia and anxiety. Until recently, its mechanism of action has remained unknown. Neurobiological research has begun to show that the herb, with its active valerenic acid, interacts with the GABA(A)-ergic system, a mechanism of action similar to the benzodiazepine drugs. This series of experiments sought to corroborate these findings with behavioral measures, compare them to the benzodiazepine diazepam, and to analyze the chemical composition of Valeriana officinalis. Rats were administered either ethanol (1 ml/kg), diazepam (1mg/kg), valerian root extract (3 ml/kg), valerenic acid (3mg/kg), or a solution of valerenic acid and exogenous GABA (75 microg/kg and 3.6 microg/kg, respectively) and assessed for the number of entries and time spent on the open arms of an elevated plus maze. Results showed that there was a significant reduction in anxious behavior when valerian extract or valerenic acid exposed subjects were compared to the ethanol control group. The evidence supports Valeriana officinalis as a potential alternative to the traditional anxiolytics as measured by the elevated plus maze.