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Analgesic and anticonvulsant effects of Acorus calamus roots in mice

Authors:
Jayaraman Rajangam at AMITY Institute of Pharmacy, AMITY University
Jayaraman Rajangam
  • AMITY Institute of Pharmacy, AMITY University
T. Anitha
T. Anitha
T. Anitha
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Vishal D Joshi
Vishal D Joshi
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Acorus calamus has been used for a long time in traditional medicine as a remedy for pain, convulsion, inflammation, and ulcer. In the present work, the analgesic effects of methanolic extract of Acorus calamus roots (MEAC) have been evaluated using acetic acid induced Writhing response and Rat caudal immersion method. Whereas the anticonvulsant effect were investigated by utilizing pentylenetetrazol induced convulsion methods. MEAC administered orally at the doses of 100 and 200 mg/kg, exhibited protective effect against the pain models in mice. Also the methanolic extract of Acorus calamus roots significantly increased the latency period in seizures induced by PTZ in mice. These obtained results indicate the analgesic as well as anticonvulsant effect Acorus calamus roots.
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International Journal of PharmTech Research
CODEN (USA): IJPRIF ISSN : 0974-4304
Vol.2, No.1, pp 552-555, Jan-Mar 2010
ANALGESIC AND ANTICONVULSANT EFFECTS OF
ACORUS CALAMUS
ROOTS IN MICE
R. Jayaraman1*, T. Anitha2, Vishal D. Joshi1
1K.N.V. Pharmacy College - Metoda, Rajkot, Gujarat, India.
2Department of Biochemistry, Vivekananda college of Arts and Science for Women,
Tiruchengodu, India.
*Corros. Author: jayaraam81@gmail.com
ABSTRACT: Acorus calamus has been used for a long time in traditional medicine as a remedy for pain, convulsion,
infla mmation, and ulcer. In the present work, the analgesic effects of methanolic extract of Acorus calamus roots
(MEAC) have been evaluated using acetic acid induced Writhing response and Rat caudal immersion method. Whereas
the anticonvulsant effect were investigated by utilizing pentylenetetrazol induced convulsion methods. MEAC
administered orally at the doses of 100 and 200 mg/kg, exhibited protective effect against the pain models in mice. Also
the methanolic extract of Acorus calamus roots significantly increased the latency period in seizures induced by PTZ in
mice. These obtained results indicate the analgesic as well as anticonvulsant effect Acorus calamus roots.
KEY WORDS: Acorus calamus roots,Methanol extract, Analgesic, Anticonvulsant activity
INTRODUCTION
Drugs acting in the central nervous system
were among the first to be discovered by the primitive
human and are still the most widely used group of
pharmacological agents.The CNS acting drugs are
invaluable therapeutically, because they can produce
specific physiological and psychological effects. From
the vast array of materia medica of the indigenous
system so many plants have been reported to
have activity against CNS disorders and thus act as
very useful remedies for the alleviation of human
suffering 1.
Acorus calamus Linn. (Araceae) is commonly
known as “bath” or “ugragandha” in North India. The
roots and rhizomes of this plant have been used in the
Indian systems of medicine for hundreds of years.
While the drug is used in Ayurvedic medicine on a
regular basis for the treatment of insomnia,
melancholia, neurosis, epilepsy, hysteria, loss of
memory and remittent fevers2,3,4,5.
The plant has been extensively investigated
and a number of chemical constituents from the
rhizomes, leave and roots of the plant have previously
reported which includes β- Asarone,α- Asarone,
elemicine, cis-isoelemicine, cis and trans isoeugenol
and their methyl ethers, camphene, P-cymene, b-
gurjunene, a-selinene, b-cadinene, camphor,terpinen-4-
ol, aterpineol and a-calacorene, acorone, acrenone,
acoragermacrone, 2-deca –4,7 dienol, shyobunones,
linalool and preisocalamendiol are also present2
.Acoradin, galangin, 2, 4, 5- trimethoxy benzaldehyde,
2,5- dimethoxybenzoquinone, calamendiol,spathulenol
and sitosterol have been isolated from Acorus
calamus6,7. In the present study, we investigated the
Analgesic and anticonvulsant effects of methanol
extracts of Acorus calamus roots in rat and mice.
MATERIALS AND METHODS
Plant material
The roots of Acorus calamus were procured
from the local market, rajkot, India and authenticated
by G.K.S Moorthy Botanical survey of India,
Coimbatore. The roots were dried under shade and
pulverized to coarse powder. The powder was passed
through 40-mesh sieve and exhaustively extracted with
90% v/v methanol in a soxhlet apparatus. The extract
was evaporated under reduced pressure until all the
solvent had been removed .The dried methanol extract
(MEAC) was stored in the refrigerator and a weighed
R. Jayaraman
et al
/Int.J. PharmTech Res.2010,2(1)
553
amount was dissolved in propylene glycol for the
present investigation.
Phytochemical investigation of the extracts
In order to detect the various constituents
present in the Methanolic extract of A. calamus were
subjected to Phytochemical screenings8,9.
Animals
Wistar albino mice of either sex (20–25 g)
were used for the study. They were housed in a quite
temperature of 25+10C and relative humidity of 45-
55%. A 12:12 light/dark cycle was maintained during
the experiment. They were given free access to food
and water, except during the test period. The mice
were acclimatized to laboratory condition for 10 days
before commencement of experiment .All experiments
were performed at the same time of the day and during
the light period. Each group consists of a 6
animals/dose and the experimental protocols were
approved by institutional animal ethics committee
(IAEC) and conducted according to the CPCSEA
guidelines for the use and care of experimental
animals, New Delhi, India.
Toxicological study
The acute toxicity study was done as per the
OECD guidelines (407). MEAC were administered
orally in different doses, where 24 h toxicit y was
recorded to identify the toxic doses. The doses of the
test compounds were then fixed on the basis of their
acute toxicity as 100 mg/kg and 200 mg/kg for
evaluation.
Analgesic study
Writhing test
Animals were divided in 4 groups of 6 mice
each. Group 1 served as negative control and was
treated with a mixture of 3% of DMSO and 3% of
Tween 20 (1 mL/100 g body weight). The second
group received indomethacin (10 mg/kg) and was used
as positive controls. The remaining groups received
the plant extracts at the doses of 100–200 mg/kg. One
hour after oral administration of these substances, each
animal was injected intraperitoneally with 0.6% acetic
acid, in a volume of 0.1 mL/10 g body weight. After
acetic acid injection, the number of stretchings or
writing responses per animal was recorded during a
subsequent 30 min10.
Rat caudal immersion method
Animals were divided into 4 groups of 6 mice
each. Group 1 served as negative control and was
treated with a mixture of 3% of DMSO and 3% of
Tween 20 (1 mL/100 g body weight). The second
group received indomethacin (10 mg/kg) and was used
as positive controls. The remaining groups received
the plant extracts at the doses of 100–200 mg/kg.
p.o. The reaction time for withdrawal of tail was
recorded after 60 min from the administration of test
compounds. It was determined by immersing the tail
up to the caudal portion (5 cm from the tip) in hot
water (55±0.5°) and by noting the time taken to
withdraw the tail clearly out of water11.
Anticonvulsant study
Pentylenetetrazol-induced seizures
Wistar albino mice of either sex (20–30 g)
were used for the anticonvulsant activity. Animals
were divided into four groups of six mice each. Group
1 served as control (saline 10 ml/kg) and second
groups is treated with carbamazepine
(50mg/kg).remaining two groups were given different
doses of the extract (100 and 200 mg/kg .p.o), 60 min
before the subcutaneous injection of pentylenetetrazole
(PTZ). Onset of convulsions and Duration of
convulsion were recorded. These two parameters were
compared with control animals, in order to assess the
anticonvulsant activity 12.
STATISTICAL ANALYSIS
The r esults wer e expressed as mean +S.E.M.
All statistical comparisons were made by means of
Student’s t-test, and a P< 0.05 was regarded as
significant.
RESULTS
Phytochemical investigation of the extracts
Phytochemical screening revealed the presence
of saponins, alkaloids, tannins, sugars and gums and
mucilages.
Analgesic activity
Writhing test
The oral administration of the MEAC extract
at the doses of 100 and 200 mg/kg significantly
reduced the writhing reaction induced by acetic acid.
Indomethacin inhibited pain sensation by 16.48 from
37.90 and the percentage of protection is 59.9%
Whereas the Methanolic extract of Acorus calamus at
the dose of 100 and 200mg/kg showed 38.09 and
45.02%respectively. (Table 1)
Rat caudal immersion method
In this method, the Methanolic extract of
Acorus calamus roots at the dose of 100 and 200mg/kg
exhibited significant analgesic activity (***P< 0.001)
which was confirmed by increased tail withdrawal
time of MEAC treated animals when compared to
control groups. (Table 2)
Anticonvulsive activity
Pentylenetetrazol-induced seizures
Single dose, subcutaneous administration of
pentylene tetrazole (PTZ; 90 mg:kg) caused clonic
convulsions as well as lethality in mice. Pretreat ment
of the mice with the plant extract caused a dose-
dependent protection against PTZ-induced convulsions
as shown in Table 3.
R. Jayaraman
et al
/Int.J. PharmTech Res.2010,2(1)
554
DISCUSSION
The results of the present study indicate that
methanol extract of Acorus calamus roots possesses
analgesic and anticonvulsant activity in mice. The
results of our study shows that extracts from the roots
of Acorus calamus have an analgesic effect against
writhing response induced by acetic acid.
Intraperitoneal injection of acetic acid produced pains
through activation of chemo sensitive nociceptors13 or
irritation of the visceral surface, which lead to the
liberation of histamine, bradikynin, prostaglandins and
serotonin14,15. Thus, analgesic activity of opioid
agonist, opioid partial agonist and non-steroidal anti-
inflammatory agents can be determined by writhing
test. Since Acorus calamus root extract were active in
this type of pain, they may belong to at least one of
these classes of analgesics.
It is now accepted that many anti-epileptic
drugs can have an analgesic effect in human
neuropathic pain16,17. Considering this, the extract of
Acorus calamus root was tested for its anticonvulsant
activity. The extract significantly increased the latency
period and reduced the duration of seizures induced by
PTZ. T wo mechanisms have been proposed for the
mode of PTZ-induced convulsion. It is proposed that
PTZ induces convulsion by either inhibiting gamma
amino butyric acid (GABA) pathway in CNS
18 or by
increasing the central noradrenergic activity19. The
effect of extract in this model can therefore suggest its
involvement in GABA-ergic or noradrenergic
pathways and its efficacy a gainst generalized Tonic-
clonic and partial seizures in mice.
CONCLUSION
In conclusion, the extracts from Acorus
calamus root seem to possess central analgesic
properties as well as anticonvulsant effects, which may
be mediated by the Potentiation of t he activity of
GABA.
Table1 :Effect of oral administration of Methanolic extract of Acorus calamus roots on pain
induced by intraperitoneal injection of acetic acid in mice.
Treatment Dose
(mg/kg)
Writhing Response % Inhibition
Control 1 mL/100 g 37.90±0.48 0.00
Indomethacin 10 16.48±0.89*** 59.9
MEAC 100 23.48±0.15*** 38.09
MEAC 200 21.37±0.79*** 45.02
Values are Mean ± S.E.M n=6.
** P< 0.01, *** P< 0.001, significant difference compared to control.
Table 2 : Effect of oral administration of Methanolic extract of Acorus calamus roots on
pain induced by caudal immersion method
Treatment Dose (mg/kg) Caudal immersion reaction
time (in sec)
Control 1 mL/100 g 3.40±0.48
Indamethacin 10 12.49±0.80***
MEAC 100 6.10±0.47**
MEAC 200 8.59±0.39***
Values are Mean ±S.E.M n=6.
** P< 0.01, *** P< 0.001, significant difference compared to control.
R. Jayaraman
et al
/Int.J. PharmTech Res.2010,2(1)
555
Table 3: The effect of Methanolic extract of Acorus calamus roots on pentylenetetrazole
induced seizure in Mice
Groups Treatment Dose (mg/kg
p.o.)
Onset of convulsion
(Sec)
Duration of
convulsion
(Min)
1PTZ + saline (90+ 10ml/kg) 67.20±1.25 463.48±11.39
2PTZ +Carbamazepine 50 79.20±1.56 205.37±17.49
3PTZ +MEAC 90 +100 72.39±2.49 210.59±13.49*
4PTZ + MEAC 90+200 91.20±2.55*** 163.44±17.04**
Values are Mean ±S.E.M n=6.
** P< 0.01, significant difference compared to control.
*** P< 0.001, significant difference compared to control.
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*****
... A. calamus has shown anticonvulsant activity against pentylenetetrazolinduced seizures. [37] A. calamus rhizome extract has shown neuromodulatory effect in mice. [38] Further, in a study, it is found that methanol and acetone extract significantly reversed the stereotypy induced by apomorphine in mice. ...
... Acorus calamus L. Rhizome extract [38] Neuromodulatory effect [38] Methanol and acetone extract [39] Significantly reversed the stereotypy induced by apomorphine [39] Methanol extract Anticonvulsant activity [37] Acetone extract, ethanol and hydroalcoholic extracts Antioxidant activity [53] Methanolic rhizome extract Antidepressant effect [53] ...
... In this regard, the observation and documentation of Acharya Kashyapa, by including medicinal herbs like Triphala, O. turpethum, and P. zeylanica under nootropic drugs, is path-breaking and remarkable. These properties increases the potency of drug in multifold by maintaining the healthy gut as [54] Diseases [54] Name of the drug B. monnieri, [9][10][11][12][13][14][15][16][17][18][19][20][21][22] C. asiatica, [23][24][25][26][27][28][29][30][31] A. calamus, [37][38][39] A. racemosus, [40][41][42][43] Triphala, [32] A. graveolens, [45] P. zelanica, [34,35] Panchagavya ghrita, [50] and Kalyanak ghrita [51] 2 Preschool (3-6 years) ...
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... As a result, studies report that phenolic acids may influence carbohydrate metabolism at various levels, improving postprandial glycemic levels, acute insulin secretion, fasting blood glucose levels and insulin sensitivity. The currently used medications that prevent the absorption of glucose have unpleasant side effects since they are not selective (Rajangam et al., 2010). In the present study, studies on the in vitro inhibition of AM showed that MeL and its constituent ingredients have demonstrated potent inhibitory activity. ...
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... The methanol extricate of A. calamus manifested anticonvulsant property, at the doses of 100 and 200 mg/kg, successfully by potentiating the effect of gammaaminobutyric acid (GABA) pathway in the nervous system (Jayaraman et al. 2010). The purified rhizome whose purification is done by boiling it in cow's urine as recommended in the Ayurvedic Pharmacopeia of India (API) before its curative use was analyzed in a maximal electroshock (MES) seizure model and the standard drug used was phenytoin. ...
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Chapter
  • Mar 2022
Capsella bursa-pastoris L. is widely found in countries such as Cyprus, Europe, Saudi Arabia, Turkey, Pakistan, India, Iraq, Iran, China, Azerbaijan, and in ethnomedical records of many other Asian countries. C. bursa-pastoris (L.) Medic—a traditional herb belongs to genus Capsella. Animal model-based preclinical studies have provided important comprehensive scientific data of its phytochemistry and phytopharmacology besides its various important uses. The main focus of this chapter aims to provide a detailed information about the traditional uses, scientific evidence-based pharmacological actions, and phytoconstituents from C. bursa-pastoris (L.) Medic based on the data available from the past 40 years. The data available shows that the plant’s crude extracts and some phytoconstituents have anti-inflammatory, smooth muscles contraction, infertility, antimicrobial, hepatoprotective, cardiovascular, anticancer, sedative, antioxidant, acetylcholinesterase inhibition potential. The data also showed that C. bursa-pastoris (L.) has a good nutritional value due to the presence of plethora of phytoconstituents which include flavonoids, phytosterols, phenolics, etc. Other than immense pharmacological potential, C. bursa-pastoris is a rich source of nutrients also. The available scientific data on ethnopharmacology, phytochemistry, and pharmacological actions of C. bursa-pastoris suggest that this plant can be a promising target for discovery and development of novel drugs for treating wide range of human ailments due to the safe and effective nature of C. bursa-pastoris. More scientific studies need to be carried out on this plant because different traditional uses and phytoconstituents.KeywordsEthnopharmacologyPhytochemistryPharmacological actionsPhytosterolsPhenolicsFlavonoidsAnti-inflammatory C. bursa-pastoris
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... The methanol extricate of A. calamus manifested anticonvulsant property, at the doses of 100 and 200 mg/kg, successfully by potentiating the effect of gammaaminobutyric acid (GABA) pathway in the nervous system (Jayaraman et al. 2010). The purified rhizome whose purification is done by boiling it in cow's urine as recommended in the Ayurvedic Pharmacopeia of India (API) before its curative use was analyzed in a maximal electroshock (MES) seizure model and the standard drug used was phenytoin. ...
Acorus calamus: A Review on Its Phytochemical and Pharmacological Profile
Chapter
  • Mar 2022
By systematizing and analyzing the vigor of potent plant-derived compounds, herbal drugs can assist the exposure of a replacement period of the healthcare system to nurse human diseases within the future. Perception of lore and remedial plants can play a vital role within the utilization and revelation of natural plant resources. Acorus calamus is a tall perennial marshland monocot plant, being the member of the family Acoraceae. A. calamus habitually known as sweet flag It is also known by different names, including sweet sedge, sweet root, sweet rush, sweet cane, sweet myrtle, myrtle grass, myrtle sedge, gladdon, myrtle flag, flag root, and cinnamon sedge. This medicinal herb is perhaps native to India and located across China, Europe, northern Asia Minor, southern Russia, Japan, northern USA, Sri Lanka, Burma, and Japan. The rhizomes of calamus and aromatic leaves are conventionally employed as a drug and therefore the dried and powdered rhizome features a tangy flavor and is employed as an alternate for nutmeg, cinnamon and ginger for its odor. The rhizomes are examined to have carminative, expectorant, nauseate, nervine, sedative, stimulant, aromatic, anthelmintic, and antispasmodic properties, and also employed for the medicaments of mental ailments, epilepsy, antidiabetic, antioxidant, anticonvulsant, long-term diarrhea, dysentery, glandular and abdominal tumors, fevers, and bronchial catarrh. The prehistoric people of China employed it for constipation and to reduce swelling. In Ayurvedic School of medicine from India, the rhizomes are wont to treat various diseases like bronchitis, fever, asthma, and as a sedative. Indigenous tribes employed it to treat a cough. As a carminative they employed it to make a decoction from it and as an infusion for colic. Perception of lore and remedial plants can take part in vital role within the utilization and unearthing of natural plant assets. Encyclopedic approach and association are needed to take care of ancient documentation on medicinal plants and utilizing these assets in benefit of citizenry. The present review gives a brief introduction about the medicinal, phytochemical, and pharmacological related aspects of the plant. Keywords: Acorus calamus · Expectorant · Ayurvedic · Antispasmodic · Aromatic
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... calamendiol, galangin, 2, 4, 5-trimethoxy benzaldehyde, pathulenol, 2,5-dimethoxybenzoquinone and sitosterol (Mazza, 1985;Williamson et al.,1988). It has also been used to arrest pain and convulsions (Jayaraman et al., 2010). The plant proved to be helpful in specific diagnosis of schizophrenic and improved clarity of speech in children (Fozdar et al.,1962). ...
Cognitive Enhancement and Neuroprotective Abilities of Plants: Ethnobotanical and Pharmacological Importance of These Plants
Chapter
  • Jan 2022
Extensive research suggests that a number of plant-derived chemicals and traditional Oriental herbal remedies possess cognition-enhancing properties. Widely used current treatments for dementia include extracts of Ginkgo biloba and several alkaloidal, and therefore toxic, plant-derived cholinergic agents. Several non-toxic, European herbal species have pan-cultural traditions as treatments for cognitive deficits, including those associated with aging. Acute administration has also been found to reliably improve mnemonic performance in healthy young and elderly cohorts, whilst a chronic regime has been shown to attenuate cognitive declines in sufferers from Alzheimer's disease. The present chapter looks at the ethnobotanical and pharmacological importance of various plants cognitive enhancing and other neuroprotective abilities.
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... Antioxidant shows that ameliorative effect induced painful neuropathy by tibial and sural nerve transection, neuroprotective action Significant acetylcholinesterase (Ach) inhibitory potential Anti-convulsant Sedative and hypothermic effects Used in schizophrenic psychosis [57][58][59][60][61] 9 Jatamansi (Nardostachys jatamansi (D.Don) DC) Useful part: roots and rhizomes ...
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... Hence by reducing the dose of sodium valproate, its adverse effects can also be limited. Phytochemical investigations revealed that methanolic extract of Acorus calamus leaves contain triterpenoids, flavonoids, saponins and tannins 29 . A number of scientific reports indicate that triterpenoids produce CNS depressant action. ...
Anticonvulsant Activity of Methanolic Extract of Acorus Calamus Leaves in Albino Mice
Article
Full-text available
Acorus calamus , commonly known as sweet flag, has a long history of use in the treatment of a variety of ailments including inflammation, chest pain, digestive disorders and some mental illnesses. Its effects on the neurological conditions have been well documented for axinolytic and antidepressant activities. With this background, the aim of the present study is evaluate the anticonvulsant activity of methanolic extract of Acorus calamus leaves in albino mice. The study included albino mice divided into 8 groups of 6 mice each. Maximum electroshock induced seizures (MES) and Pentylenetetrazole (PTZ) tests were performed on the animal models to evaluate the antiepileptic activity (4 groups were allocated to MES and 4 to PTZ). The methanolic extract of Acorus calamus leaves exhibited a significant reduction in the duration of hind limb extensor phase in MES model (7.116±0.501 seconds for control and 9.116± 0.527 seconds for extract) and delayed the latency of seizures induced by PTZ (485.500±14.941 seconds) when compared with that of the control group (297.000±21.918 seconds). In addition, the groups administered with the extract and sodium valproate in combination exhibited significant results in both MES and PTZ models (T2- 92.61% and T4- 21.95 %, respectively). Preliminary phytochemical screening performed in several studies has shown the presence of triterpenoids, flavonoids, saponins and tannins. The anticonvulsant activity of Acorus calamus may be mediated by its GABA potentiating activity. It can thus be concluded that the observed anticonvulsant effects could be the resultant of a synergistic action of these phytochemicals. Further studies should be undertaken to substantiate these results on various animal models along with a thorough phytochemical analysis and in silico studies to understand the mode of action of these phytochemicals on various GABA receptor-mediated signaling
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... Flavonoïds, alkaloids or terpenes might be responsible for the anticonvulsant activity of A. conyzoides hydroalcoholic extract. As reported by Rasilingam et al. (2009), gossypin, a flavonoid isolated from Hibiscus vitifolius L. (Malvaceae) protects mice from MES-induced seizure; similarly flavonoids isolated from Nauclea latifolia Sm. (Rubiaceae) protect mice against MES-induced seizures through GABA or by inhibiting sodium channels (Bum et al.,2009), and the flavonoid, galangin, isolated from Acorus calamus L. (Acoraceae) act through GABA receptor (Jayaraman et al., 2010). Alkaloids also have been reported to be responsible for anticonvulsant activity. ...
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Swarna Prashana – faith in the embrace of research
Article
  • Nov 2021
Childhood needs diverse nutritional requirements. Poor appetite, lifestyle changes, and poor digestion affects child immunity and make them prone to diseases. Kaumarabhritya, a branch of Ayurveda which deals in child and adolescent health care, has a unique concept of Swarna Prashana (SP) to promote generalized immunity and intellect. SP is commonly recommended to children between 0-12yrs of age and given as a general health promoter to improve intellect, digestion, strength, immunity, longevity, and complexion. Multiple benefits of SP are mentioned in different Samhitas which needs to be explored on scientific background. Authors have highlighted content variabilities, plausible mechanisms, research tasks and potentials, lacunae, and future prospects about SP. This manuscript is a spotlight on current social, clinical, marketing, and scientific information of Swarna Prashana. SP can be a cost-effective, safe, infrastructure compatible, and prevention-centric approach to improve children's overall health status and has the potential to serve as a positive health care program for children.
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Anticonvulsant drugs for management of pain: A systematic review
Article
Full-text available
  • Nov 1995
To determine effectiveness and adverse effects of anticonvulsant drugs in management of pain. Systematic review of randomised controlled trials of anticonvulsants for acute, chronic, or cancer pain identified by using Medline, by hand searching, by searching reference lists, and by contacting investigators. Between 1966 and February 1994, 37 reports were found; 20 reports, of four anticonvulsants, were eligible. Numbers needed to treat were calculated for effectiveness, adverse effects, and drug related withdrawal from study. The only placebo controlled study in acute pain found no analgesic effect of sodium valproate. For treating trigeminal neuralgia, carbamazepine had a combined number needed to treat of 2.6 for effectiveness, 3.4 for adverse effects, and 24 for severe effects (withdrawal from study). For treating diabetic neuropathy, anticonvulsants had a combined number needed to treat of 2.5 for effectiveness, 3.1 for adverse effects, and 20 for severe effects. For migraine prophylaxis, anticonvulsants had a combined number needed to treat of 1.6 for effectiveness, 2.4 for adverse effects, and 39 for severe effects. Phenytoin had no effect on the irritable bowel syndrome, and carbamazepine had little effect on pain after stroke. Clonazepam was effective in one study for temporomandibular joint dysfunction. No study compared one anticonvulsant with another. Anticonvulsants were effective for trigeminal neuralgia and diabetic neuropathy and for migraine prophylaxis. Minor adverse effects occurred as often as benefit.
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Gas chromatographic and mass spectrometric studies of the constituents of the rhizome of calamus. I. The volatile constituents of the essential oil
Article
The composition of the volatile oil of European calamuse (Acorus calamus L.) was investigated by liquid—solid chromatography and gas chromatography—mass spectrometry (GC—MS). A total of 184 volatile components were detected, including 67 hydrocarbons, 35 carbonyl compounds, 56 alcohols, 8 phenol, 2 furans and 4 oxido-compounds. The essential oil of Indian calamus was also analyzed by GC—MS and 93 volatile components were detected, β-asarone being the major component. A probable oxidation scheme for β-asarone is shown and the importance of minor components for the development of calamus aroma is also discussed. Of the 125 and 79 components identified in the European and Indian oils, respectively 72 and 39 had not been reported previously in calamus oil.
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Decrease in the Function of the ?-Aminobutyric Acid-Coupled Chloride Channel Produced by the Repeated Administration of Pentylenetetrazol to Rats
Article
  • Nov 1990
The acute administration of pentylenetetrazol (PTZ; 25-75 mg/kg i.p.) failed to modify the specific binding of t-[35S]butylbicyclophosphorothionate ([35S]TBPS) to membrane preparations from the cerebral cortex of the rat. In contrast, the repeated administration of PTZ (30 mg/kg i.p., three times a week for 12 weeks) reduced by 26% the density of [35S]TBPS binding sites without modifying the dissociation constant. This effect was observed 3 days after the last PTZ administration. A parallel reduction of gamma-aminobutyric acid (GABA)-stimulated 36Cl- uptake was measured in the cerebral cortex of PTZ-treated rats 3 days after the last injection. The repeated administration of PTZ produced sensitization to the drug, or chemical kindling. In fact, no convulsions were observed in the first week of treatment, but all the animals became sensitized to PTZ by the 12th week. The results are consistent with the hypothesis that chronic treatment with PTZ at a subconvulsant dose causes a decrease in GABA-coupled chloride channel activity that may be related to the chemical kindling produced by this compound.
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Neuropharmacological profile of Barleria lupulina Lindl. Extract in animal models
Article
Barleria lupulina Lindl. is a popular medicinal plant distributed in mountains of southern and western India. In the present work, the effect of methanolic extract of aerial parts of B. lupulina on CNS activity has been evaluated. The CNS activity was tested in several experimental models, in mice and rats: general behavior, exploratory behavior, muscle relaxant activity, conditioned avoidance response and phenobarbitone sodium-induced sleeping time tests. The aerial parts of the plant B. lupulina was extracted with methanol and the solvent was removed by vacuum distillation. The methanol extract (100, 200 and 300 mg/kg) showed reduction in general behavioral pattern (spontaneous activity, alertness, awareness, pain response and touch response) in a dose dependent manner. The extract was found to produce a significant reduction of the exploratory behavioral profile (Y-maze test, head dip test) and conditioned avoidance response with all the tested doses. The methanolic extract showed significant motor incoordination and muscle relaxant activity. The extract also potentiated phenobarbitone sodium induced sleeping time. Preliminary investigation showed that the methanol extract of B. lupulina has significant psychopharmacological activity.
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A Note on the Preliminary Studies of Certain Pharmacological Actions of Acorns Calamus L*
Article
The alcoholic extract of Acorus calamus roots and rhizomes was screened for pharmacological activities. It was found to possess sedative and analgetic properties and caused a moderate depression in the blood pressure and respiration. The water-soluble fraction of the de-alcoholized extract relaxed the intestine and caused negative inotropic action on frog's heart. Anti-epileptic activity was absent.
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Does SPM 927 have an analgesic effect in human neuropathic pain? An open label study
Article
The aim of the study is to establish if the putative anticonvulsant SPM 927 has an analgesic effect in human neuropathic pain and to assess its tolerability. This is an open label study of 25 adult human subjects with resistant neuropathic pain. Subjects were treated with SPM 927 in a dose-escalating scheme to 600 mg daily, if tolerated. Treatment was continued for 4 weeks then withdrawn without tapering. Pain scores were recorded using a 11-point Likert score and a categorical pain-rating scale. Laboratory parameters and, electrocardiographs (ECGs) were collected; side effects were noted. Of the 25 enrolled subjects, 12 completed the study according to the protocol. The remaining subjects dropped out due to adverse events (n=12) or withdrawn consent. Mean daily pain scores (Likert score) fell by 0.83 (95% CI -1.77, +0.11) at the end of maintenance and rose by 0.58 (95% CI -0.23, +1.40) after withdrawal of SPM 927. Similar changes were seen in the categorical pain-rating scores. There were decreases in the mean scores for shooting pain, paraesthesia, and allodynia, but much less change in the numbness and burning-pain scores. The most common side effects were nausea, dizziness, leukocytosis, and increased ALT. No consistent changes in ECG recordings or haemodynamic variables were observed. SPM 927 may have an analgesic effect in human neuropathic pain and was reasonably well tolerated in this study. These data support the continued clinical development of SPM 927 for neuropathic pain.
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Antinociceptive and anti-inflammatory effect of the aqueous extract from leaves of Pimenta racemosa var: Ozua (Myrtaceae)
Article
The leaves of Pimenta racemosa var. ozua (Urban & Ekman) Landrum L. (Myrtaceae) are used against the pain and the inflammation in popular medicine of the Caribe area. In the present work, the antinociceptive, anti-inflammatory effect, and acute toxicity of the aqueous extract from leaves of Pimenta racemosa have been investigated. The antinociceptive action was assayed in several experimental models in mice: acetic acid, formalin, and hot plate tests. The aqueous extract (125 and 250 mg/kg) significantly and in a dose-dependent manner reduced the nociception induced by the acetic acid intraperitoneal injection (P<0.001). In the formalin test, the extract also significantly reduced the painful stimulus in both phases of the test (P<0.001). On the contrary, the extract neither significantly increased the latency time of licking nor jumping in the hot plate test. In the anti-inflammatory study, the plant also showed an interesting effect. Aqueous extract (125 and 250 mg/kg) orally administered, significantly reduced the carrageenan-induced edema in rat paw at 1, 3, and 5 h (P<0.001). In the TPA test the edema was dose-dependent and significantly reduced by the extract (0.5, 1, and 3 mg per ear) when it was topically applied (P<0.01; P<0.001). The levels of myeloperoxidase enzyme also were reduced in the inflamed tissue by the extract. Acute toxicity also was investigated and the results indicated a moderate toxicity (LD50: 287 +/- 12.9 mg residue/kg; 1.854 +/- 0.083 g plant/kg). These results revealed that the extract from leaves of Pimenta racemosa var. ozua exerts an important antinociceptive activity, associated to an anti-inflammatory effect which to appear be markedly influenced by the inhibition of neutrophil migration into inflamed tissue and that lack of toxic effects at usual doses.
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