Ethnopharmacological evaluation of the anticonvulsant, sedative and antispasmodic activities of Lavandula stoechas L

Lavandula stoechas L. (Lamiaceae) has been used for a long time in traditional medicine as an anticonvulsant and antispasmodic. The aqueous-methanolic extract of L. stoechas flowers (LS) was studied for its possible anticonvulsant and antispasmodic activities. When tested in mice, LS (600 mg/kg) significantly reduced the severity and increased the latency of convulsions induced by pentylene tetrazole (PTZ). LS likewise reduced PTZ's lethality. LS up to a dose of 600 mg/kg was found devoid of any hypnotic effect in mice, however, animals were found to be dull, calm and relaxed. The sedative effect of the plant extract was confirmed, as it prolonged the pentobarbital sleeping time in mice similar to that of diazepam. In isolated rabbit jejunum preparations, LS caused a dose-dependent (0.1-1.0 mg/ml) relaxation of spontaneous contractions. LS also inhibited K(+)-induced contractions in a similar dose range, thereby suggesting calcium channel blockade. This effect was confirmed when pretreatment of the jejunum preparation with LS produced a dose-dependent shift of the Ca(2+) dose-response curve to the right, similar to the effect of verapamil, a standard calcium channel blocker. These data indicate that the plant extract exhibits anticonvulsant and antispasmodic activities. Its calcium channel blocking property may be mechanistically related to these activities. Its usefulness in folk medicine appears thus to be based on a sound mechanistic background.     

Antimicrobial and anticonvulsant activities of Viscum capense

Dichloromethane, methanol and water extracts of Viscum sapense L.f., of the Loranthaceae family, were tested for antimicrobial activities against Staphylococcus aureus, Pseudomonas aeruginosa and Candida albicans. Methanol extract was also tested for activity against seizures in albino mice induced by pentylenetetrazole (PTZ), bicuculline and N-methyl-dl-aspartic acid (NMDLA). Methanol extract of V. capense inhibited the growth of S. aureus. Methanol extract also protected the mice against PTZ- and bicuculline-induced tonic seizures but did not significantly alter NMDLA-induced tonic seizures. The data indicate that the extract of V. capense has antibacterial activity against S. aureus and also anticonvulsant activity.     

Evaluation of the anti-stress and anticonvulsant activities of leaf extract of Alchornea cordifolia in mice

Aim of the study

The extract of the leaves of Alchornea cordifolia (AC) is extensively used in ethnomedicine for ulcers, rheumatic pains, febrile convulsions and for enhancing physical performance. In this study, the anti-stress and anticonvulsant activities of the aqueous leaf extract of Alchornea cordifolia were investigated in mice.

Materials and methods

The anti-stress activity was assessed based on the ability of the extract to alter the duration of immobility, in the forced swim endurance test, whilst a picrotoxin-treated animal, was employed as the model for convulsive seizures.

Results

The extract (100–400 mg/kg) given orally was found to significantly (p < 0.05) reduce the duration of immobility, which suggest an anti-stress/anti-fatigue property. However, AC when tested at doses between 100 and 400 mg/kg did not prevent convulsions induced by picrotoxin in mice. The acute toxicity study carried out in mice revealed that the extract was well tolerated by the animals, as no death was observed at oral doses of 500–4000 mg/kg.

Conclusions

The results of this preliminary study provide evidence, which may support the use of Alchornea cordifolia against stress or fatigue in ethnomedicine.     

Evaluation of hepatoprotective effect of Amalkadi Ghrita against carbon tetrachloride-induced hepatic damage in rats

Amalkadi Ghrita (AG), a polyherbal formulation, was evaluated for its hepatoprotective activity against carbon tetrachloride (CCl₄)-induced hepatic damage in rats. The hepatoprotective activity of AG was evaluated by measuring levels of serum marker enzymes like serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT), alkaline phosphatase (ALP), and acid phosphatase (ACP). The serum levels of total proteins and bilirubin were also estimated. The histological studies were also carried out to support the above parameters. Silymarin was used as standard drug. Administration of AG (100 and 300 mg/kg, p.o.) markedly prevented CCl₄-induced elevation of levels of serum GPT, GOT, ACP, ALP, and bilirubin. The decreased level of total proteins due to hepatic damage induced by CCl₄ was found to be increased in AG-treated group. The results are comparable to that of silymarin. A comparative histopathological study of liver exhibited almost normal architecture, as compared to CCl₄-treated group. Hepatoprotective effect of AG is probably due to combined action of all ingredients.     

Analgesic and sedative activities of lactucin and some lactucin-like guaianolides in mice

Lactucin (1) and its derivatives lactucopicrin (2) and 11beta,13-dihydrolactucin (3), which are characteristic bitter sesquiterpene lactones of Lactuca virosa and Cichorium intybus, were evaluated for analgesic and sedative properties in mice. The compounds showed analgesic effects at doses of 15 and 30 mg/kg in the hot plate test similar to that of ibuprofen, used as a standard drug, at a dose of 30 mg/kg. The analgesic activities of the compounds at a dose of 30 mg/kg in the tail-flick test were comparable to that of ibuprofen given at a dose of 60 mg/kg. Lactucopicrin appeared to be the most potent analgetic of the three tested compounds. Lactucin and lactucopicrin, but not 11beta,13-dihydrolactucin, also showed sedative properties in the spontaneous locomotor activity test.     

UPLC-TOF-MS analysis of Galium spurium towards its neuroprotective and anticonvulsant activities

Ethnopharmacological relevance

Galium species have been reported to be used against epilepsy in traditional Turkish folk medicine.

Aim of study

The present work was undertaken to evaluate the in vivo anticonvulsant and in vitro neuroprotective effects of Galium spurium L. and to determine the major constituents by UPLC–TOF-MS.

Materials and methods

Anticonvulsant activity of the aerial parts of Galium spurium was investigated using pentylenetetrazole, picrotoxin, and maximal electroshock-induced seizure animal models. In order to evaluate the safety, neurotoxicity (Rota rod test) of the ethanol extract was also determined. In vitro neuroprotective effect of the ethanol extract of Galium spurium was assessed by acetylcholinesterase and butrylcholinesterase inhibitions. Ultra Performance Liquid Chromatography–Time of Flight Mass Spectrometer (UPLC–TOF-MS) was used to identify the major compounds in the extract.

Results

In pentylenetetrazole-induced seizure, the ethanol extract at doses of 250 and 1000 mg/kg prolonged the onset of seizures. Similarly, Galium spurium (250 and 500 mg/kg) significantly delayed the onset of picrotoxin-induced seizures in mice and these doses also exhibited 12.5% and 17% protection, respectively, against picrotoxin-induced seizures. Furthermore, Galium spurium extract showed a significant protective effect against maximal electroshock-induced seizures at doses of 250 and 1000 mg/kg (50% and 37.5%, respectively) and also all tested doses prolonged the onset of seizures. No motor co-ordination was observed with intraperitoneal injection of Galium spurium extract at doses of 500 and 1000 mg/kg. The extract exhibited 16.2% inhibition against butrylcholinesterase at 200 μg/mL concentration, whereas it did not inhibit acetylcholinesterase. Phytochemical analysis of the extract based on the MS data by UPLC–TOF-MS, ten major compounds (phenolic and triterpenic acids, flavonoids and iridoids) were determined.

Conclusions

The results indicate that Galium spurium may have anticonvulsant activity against picrotoxin and maximal electroshock-induced seizures in mice. Phenolic acids, flavonoids and iridoids might be responsible for anticonvulsant activity. The results offer possible beneficial effects by the plant's aerial parts and may suggest a realistic explanation for its traditonal usage in epilepsy.     

Gut modulatory, blood pressure lowering, diuretic and sedative activities of cardamom

ETHNOPHARMACOLOGICAL RELEVANCE: Cardamom (Elettaria cardamomum) is traditionally used in various gastrointestinal, cardiovascular and neuronal disorders. AIM OF THE STUDY: To rationalize cardamom use in constipation, colic, diarrhea, hypertension and as diuretic. MATERIALS AND METHODS: Cardamom crude extract (Ec.Cr) was studied using in vitro and in vivo techniques. RESULTS: Ec.Cr caused atropine-sensitive stimulatory effect in isolated guinea-pig ileum at 3-10mg/ml. In rabbit jejunum preparations, Ec.Cr relaxed spontaneous and K+ (80 mM)-induced contractions as well as shifted Ca++ curves to right, like verapamil. Ec.Cr (3-100mg/kg) induced fall in the arterial blood pressure (BP) of anaesthetized rats, partially blocked in atropinized animals. In endothelium-intact rat aorta, Ec.Cr relaxed phenylephrine (1 microM)-induced contractions, partially antagonized by atropine and also inhibited K+ (80 mM) contractions. In guinea-pig atria, Ec.Cr exhibited a cardio-depressant effect. Ec.Cr (1-10mg/kg) produced diuresis in rats, accompanied by a saluretic effect. It enhanced pentobarbital-induced sleeping time in mice. Bio-assay directed fractionation revealed the separation of spasmogenic and spasmolytic components in the aqueous and organic fractions respectively. CONCLUSION: These results indicate that cardamom exhibits gut excitatory and inhibitory effects mediated through cholinergic and Ca++ antagonist mechanisms respectively and lowers BP via combination of both pathways. The diuretic and sedative effects may offer added value in its use in hypertension and epilepsy.     

Anxiolytic and sedative activities of Passiflora edulis f. flavicarpa

Aim of the study

Many plants in the genus Passiflora have long been used in traditional folk medicines as a remedy for many neurogenic diseases in many countries. A number of species of the genus was studied about their neuropharmacological activities, but the results were inconsistent. No literature reported neuropharmacological studies on Passiflora edulis f. flavicarpa as yet. The present study was aimed at evaluating the anxiolytic and sedative activities of Passiflora edulis f. flavicarpa.

Materials and methods

Swiss albino mice were used as experimental animals in elevated plus-maze (EPM) test and spontaneous activity (SA) test to assay the behavioral effects of ethanolic extract (EE) of the aerial part of Passiflora edulis f. flavicarpa and its fractions, viz. petrol ether extract (PEE), ethyl acetate extract (EAE), n-BuOH extract (BE) and aqueous extract (AE), together with subfractions of BE, viz. BEF-I, BEF-II, BEF-III, BEF-IV and isoorientin, a flavonoid component isolated from BEF-III.

Results

In the EPM test, single-dose oral administration of EE (300 mg/kg and 400 mg/kg), BE (125 mg/kg and 200 mg/kg), AE (200 mg/kg and 300 mg/kg), BEF-I (200 mg/kg), BEF-II (200 mg/kg), BEF-III (100 mg/kg), or isoorientin (20 mg/kg) resulted in anxiolytic-like effects, but a sedative-like activity was produced at higher doses, such as 300 mg/kg of BE, 200 mg/kg of BEF-III, or 40 mg/kg and 80 mg/kg of isoorientin. The results of the SA test manifested that treatment with 400 mg/kg of EE, 300 mg/kg of BE, or 40 mg/kg and 80 mg/kg of isoorientin compromised motor activity in mice, which are in line with the results of the EPM test.

Conclusions

The aerial part of Passiflora edulis f. flavicarpa was anxiolytic at low dose but sedative at high dose. Flavonoids are important active constituents. Since AE contained little flavonoids, it was conjectured that there were other components responsible for the anxiolytic effect of Passiflora edulis f. flavicarpa besides flavonoids.     

Sedative and anticonvulsant activities of goodyerin,a flavonol glycoside from Goodyera schlechtendaliana

Goodyerin is a flavonol glycoside isolated from the whole plants of Goodyera schlechtendaliana which has been used as a substitute for the crude drug, Anoectochilus formosanus. The pharmacological properties of goodyerin were assayed for effects on spontaneous locomotor activity, on pentobarbital-induced hypnosis, and on anticonvulsant activity against picrotoxin-induced seizures in rodents. Goodyerin exhibited a significant and dose-dependent sedative and anticonvulsant 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.     

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.     

Anticonvulsant,anxiolytic and sedative activities of the aqueous root extract of Securidaca longepedunculata Fresen.

Aim of the study

The objective of this study is to investigate the anticonvulsant, anxiolytic and sedative activities of the aqueous root extract of Securidaca longepedunculata.

Materials and methods

The anticonvulsant effect of the aqueous root extract (100, 200 and 400 mg/kg) was evaluated in mice using the strychnine- and picrotoxin-induced seizure models. Its anxiolytic activity was evaluated using the elevated plus maze (EPM) and the Y maze (YM) methods (14 and 32) while the hexobarbitone induced sleep and the hole board models were used to evaluate the sedative and exploratory activities in mice respectively. The acute toxicity studies and phytochemical analysis of the extract were also carried out.

Results

The extract (100–400 mg/kg) produced a significant (P < 0.01) dose dependent increase in onset of convulsion compared to the control for strychnine- and picrotoxin-induced seizures. It also produced a significant (P < 0.01) dose dependent prolongation of the cumulative time spent in the open arms of the elevated plus maze and Y maze compared with the control. The extract (100–400 mg/kg) produced significant (P < 0.01) reduction in the time of onset of sleep induced by hexobarbitone. The prolongation of hexobarbitone sleeping time by the extract (200 mg/kg) was comparable to that produced by diazepam (3 mg/kg). At doses of 100–400 mg/kg, the extract produced a dose dependent decrease in exploratory activity of the mice. The reduction in exploratory activity produced by the extract (400 mg/kg) was greater than that of chlorpromazine (1 mg/kg). The results obtained from the experiments indicate that the extract has central nervous system depressant and anxiolytic activities. The LD₅₀ obtained for the acute toxicity studies using both oral and intraperitoneal routes of administration were 1.74 g/kg and 19.95 mg/kg respectively.

Conclusion

These findings justify the use of Securidaca longepedunculata in traditional medicine for the management of convulsion and psychosis.     

Sedative and anticonvulsant activities of the aqueous root extract of Sanseviera liberica Gerome & Labroy (Agavaceae)

The central nervous system (CNS) depressant and anticonvulsant activities of the aqueous root extract of Sanseviera liberica (ASL) were investigated on various animal models including pentobarbitone sleeping time and hole-board exploratory behaviour for sedation tests, and strychnine, picrotoxin, bicuculline and pentylenetetrazole-induced convulsions in mice. ASL (100-400mg/kg, p.o.), like chlorpromazine HCl (1mg/kg, i.m.), produced a dose-dependent prolongation of pentobarbitone sleeping time and suppression of exploratory behaviour. ASL (100 and 200mg/kg) produced dose-dependent and significant (P<0.05) increases in onset to clonic and tonic convulsions, and at 400mg/kg, showed complete protection against seizures induced by strychnine, picrotoxin and bicuculline, but not with pentylenetetrazole. ASL up to 10 g/kg, p.o. did not produce death, but i.p. treatment produced mortalities with LD(50) of 668.3+/-47.6 mg/kg. Preliminary phytochemical investigations of ASL revealed the presence of carbohydrates, alkaloids, saponins, reducing sugars and oils. The results indicate that ASL has sedative and anticonvulsant activities, therefore, justifying its use in traditional African medicine.     

安神类中药及其有效成分对神经递质镇静催眠机制的研究进展

安神类中药应用于临床治疗失眠历史悠久。现代药理作用主要为镇静、催眠以及抗焦虑和抗抑郁作用。现代分子生物学研究表明,失眠症与神经递质、细胞因子等有关。该文对中药单体成分、单味中药提取物、复方安神中药提取物以及复方安神中成药通过调节神经递质而发挥镇静催眠作用进行综述。该文所涉及到的神经递质包括γ-氨基丁酸(GABA)、谷氨酸(Glu)、5-羟色胺(5-HT)、多巴胺(DA)、去甲肾上腺素(NE)及其代谢物5-吲哚乙酸(5-HIAA)、高香草酸(HVA)、二羟苯乙酸(DOPAC)。研究结果表明,目前安神药研究最多的是5-HT和GABA能神经系统。研究最多的安神药是酸枣仁,包括其单体成分、单味中药提取物、复方中药提取物及复方中成药,涉及到的安神药还有五味子、合欢花、远志、龙眼肉、灵芝等。这为安神类中药的临床研究提供参考,进而为其开发利用提供依据。     

The sedative effect of acupuncture

Eight patients with diagnosis of anxiety neurosis were treated with acupuncture. Six of them showed good to moderate response while 2 had no change. The endorphin theory in applying acupuncture is discussed.     

Evaluation of the anticonvulsant activity of the essential oil of Eugenia caryophyllata in male mice

In this study, the effect of an essential oil of Eugenia caryophyllata (Myrtaceae), an antiepileptic remedy in Iranian folk medicine, against seizures induced by maximal electroshock (MES) or pentylenetetrazole (PTZ) in male mice was studied. The essential oil exhibited anticonvulsant activity against tonic seizures induced by MES. Although it was not effective against clonic convulsions induced by intraperitoneal administration of PTZ, the seizure threshold which was determined by an increase in the dose of intravenously infused PTZ required to induce clonus, was elevated by the essential oil. In addition, at some anticonvulsant doses, the essential oil produced motor impairment on the rotarod.     

Evaluation of antimicrobial activities of Satureja hortensis L

The present study was designated to evaluate the antimicrobial activities of methonol and hexane extracts of Satureja hortensis L. which is an annual herb used as traditional folk medicine in Eastern Anatolia region of Turkey for the treatment of different infectious diseases and disorders. The antimicrobial activities of the extracts against 147 laboratory strains belong to 55 bacterial species, and 31 isolates of 1 yeast and 4 fungi species were tested by using disc diffusion assay. The results showed that hexane extract of Satureja hortensis had no antifungal, but antibacterial activity against four strains of three Bacillus species whereas methanol extract of Satureja hortensis had both anticandidal and antibacterial effects. It inhibited the growth of 23 strains of 11 bacterial species and 6 isolates of Candida albicans, at the concentration of 300microg/ml. Satureja hortensis did not show antimicrobial activity against the remaining microorganisms (83%) tested including most and all of the clinic and plant pathogenic microorganisms, respectively. Methanol extract showed stronger and broader spectrum of antimicrobial activity as compared to hexane extract.     

生黄连或酒制黄连对交泰丸镇静催眠作用的影响

目的:观察生品黄连或酒制黄连组成的交泰丸镇静催眠活性的强弱。方法:采用戊巴比妥钠阈上剂量、阈下剂量诱导小鼠睡眠和小鼠自发活动实验,比较生黄连或酒制黄连组成的交泰丸镇静催眠作用,并初步探讨后者时效特点。结果:生品黄连与酒制黄连组成的交泰丸5g/kg单次灌胃给药,均可明显缩短阈上剂量戊巴比妥钠小鼠入睡潜伏期,延长其睡眠时间,增加阈下剂量戊巴比妥钠小鼠的入睡个数,并抑制小鼠自发活动;酒制黄连组成的交泰丸作用总体强于等剂量的生品黄连组成的交泰丸,给药半小时即呈现明显活性,2小时达到作用高峰,作用持续到3小时。结论:酒制黄连组成的交泰丸镇静催眠活性较同生药量生品黄连组成的交泰丸强,且具有起效快、维持时间短的时效特点。     

Evaluation of oriental medicinal herbs for estrogenic and antiproliferative activities

Herb extracts commercially used in Asia were screened for their estrogenic activity with a recombinant yeast system with both a human estrogen receptor (ER) expression plasmid and a reporter plasmid. Pueraria lobata (flower) had the highest estrogenic relative potency (RP, 17-estradiol = 1.00) (7.8e-3) (RP for + control), followed by Amomum xanthioides (1.3e-3), Glycyrrhiza uralensis, Zingiber officinale, Rheum palmatum, Curcuma aromatica, Eriobotrya japonica, Sophora flavescens, Anemarrhena asphodeloides, Polygonum multiflorum and Pueraria lobata (root) (9.5e-4-1.0e-4), and Prunus persica, Lycoppus lucidus and Adenophora stricta (9.0e-5-8.0e-5). In the antiproliferative assay, five human cancer cell lines representing different tissues (breast, lung and ovary) were used. Eriobotrya japonica showed strong cytotoxicity in ER-negative breast cancer (MDA-MB-231), cervix epitheloid (HeLa) and lung (A549) carcinoma cell lines.