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.     

Behavioral and anticonvulsant effects of the standardized extract of Ficus platyphylla stem bark

Ethnopharmacological relevance

Decoctions of Ficus platyphylla Del.-Holl (Family: Moraceae) are used in Nigeria?s folk medicine for the management of epilepsy and their efficacies are widely acclaimed among the rural communities of northern Nigeria. The aim of the study is to examine the behavioral and anticonvulsant properties of the standardized methanol extract of Ficus platyphylla (FP) stem bark, in order to scientifically describe its potential values in the management of convulsive disorders.

Materials and methods

High performance liquid chromatography (HPLC) and preliminary phytochemical analysis of the methanol extract were utilized and the intraperitoneal median lethal dose (LD₅₀) determined in mice. The effects of FP were investigated on some murine models of behavior and its anticonvulsant effects studied on pentylenetetrazole (PTZ)-, strychnine (STN)-, picrotoxin (PCT)-, isoniazid (INH)-, aminophylline (AMI)- and maximal electroshock (MES)-induced seizures in mice.

Results

The intraperitoneal oral LD₅₀ of FP was estimated to be 5000 mg/kg. FP significantly reduced the locomotor activities including the total distance covered, speed, active time and rearing counts. It shortened the onset and prolonged the duration of diazepam-induced sleep, but had no effect on motor coordination on the rota-rod treadmill or beam-walking assay in mice at the doses tested. The extract protected the mice against PTZ- and STN-induced seizures and significantly delayed the latencies of myoclonic jerks and tonic seizures induced by all the standard convulsant agents (PTZ, PCT, INH, STN and AMI) used in this study, but failed to protect the mice against MES seizures at the doses tested. The HPLC fingerprint of the extract shows a spectrum profile characteristic of Ficus platyphylla, while the preliminary phytochemical screening revealed the presence of saponins, flavonoids and tannins.

Conclusion

Our study provides scientific evidence that FP may contain psychoactive principles with potential anticonvulsant properties, thus supporting further development of the psychoactive components of this plant as anticonvulsant agents.     

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.     

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.     

Anticonvulsant activity of Benkara malabarica (Linn.) root extract: In vitro and in vivo investigation

Aim of the study

To systematically investigate the anticonvulsant activity of methanol extract of Benkara malabarica roots and to provide a biochemical basis elucidating its mode of action.

Methods

The median lethal dose (LD₅₀) of Benkara malabarica extract was determined. The anticonvulsant activity of the extract was assessed in strychnine-induced and isoniazide-induced convulsion models; phenytoin (20 mg/kg) and diazepam (1 mg/kg) were used as standards, respectively. Percentage protection provided by the drug was accounted as decrease in the number of convulsions within 8 h of observation. Mechanism of action was studied by performing GABA transaminase (GABA-T) assay, isolated from rat brain. Active constituent was isolated and characterized from the plant extract.

Results

The median lethal dose (LD50) of Benkara malabarica was found to be more than 500 mg/kg. It demonstrated 30% and 35% protection against strychnine-induced convulsions and 60% and 80% protection against isoniazide-induced convulsions, at doses of 25 mg/kg and 50 mg/kg, respectively. Enzyme assay results revealed that Benkara malabarica extract possesses GABA-T inhibitory activity (IC50 = 0.721 mg/ml). Scopoletin which was identified as the major constituent of the extract was found to be an inhibitor of GABA-T (IC50 = 10.57 μM).

Conclusions

The anticonvulsant activity of the plant extract is predominantly GABA mediated and may be due to the action of scopoletin alone or is a result of synergy of different compounds in the extract in which scopoletin is the major constituent.     

Antioxidant and anti-inflammatory activities of aqueous extract of Centipeda minima

Ethnopharmacological relevance

Centipeda minima (L.) is traditionally used in Chinese folk medicine for the treatments of rhinitis, sinusitis, relieving pain, reducing swelling, and treating cancer for a long history in Taiwan. However, there is no scientific evidence which supports the use in the literature.

Aim of the study

The aim of this study was to evaluate the antioxidant and anti-inflammatory activities of the aqueous extract of Centipeda minima (ACM).

Materials and methods

The following activities were investigated: antioxidant activities [2,2′-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), DPPH (1,1-diphenyl-2-picrylhydrazyl)], and anti-inflammatory [lipopolysaccharide (LPS) induced nitric oxide (NO) production in RAW264.7 macrophages and paw-edema induced by λ-carrageenan (Carr)]. We also investigated the anti-inflammatory mechanism of ACM via studies of the activities of catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPx) and the levels of malondialdehyde (MDA) in the edema paw. Serum NO, tumor necrosis factor α (TNF-α), and interleukin-1β (IL-1β) were also measured in vivo. In HPLC analysis, the fingerprint chromatogram of ACM was established.

Results

ACM showed the highest TEAC and DPPH radical scavenging activities, respectively. ACM also had highest contents of polyphenol and flavonoid contents. We evaluated that ACM and the reference compound of protocatechualdehyde and caffeic acid decreased the LPS-induced NO production in RAW264.7 cells. Administration of ACM showed a concentration dependent inhibition on paw edema development after Carr treatment in mice. The anti-inflammatory effects of ACM could be via NO, TNF-α, and IL-1β suppressions and associated with the increase in the activities of antioxidant enzymes. Western blotting revealed that ACM decreased Carr-induced inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expressions.

Conclusions

Anti-inflammatory mechanisms of ACM might be correlated to the decrease in the level of Malondialdehyde (MDA), iNOS, and COX-2 via increasing the activities of CAT, SOD, and GPx in the edema paw. Overall, the results showed that ACM demonstrated antioxidant and anti-inflammatory activity, which supports previous claims of the traditional use for inflammation and pain.     

Antimicrobial activities of methanol extract and compounds from stem bark of Vismia rubescens

Ethnopharmacological relevance

The plant, Vismia rubescens (Guttiferae) is popularly used in Cameroon and in several parts of Africa as febrifugal and for the treatment of various microbial infections (skin diseases, diarrhoea and venereal diseases).

Aim of the study

This study was mapped out to evaluate the antimicrobial activities of the methanol extract and compounds from the stem bark of Vismia rubescens.

Materials and methods

Structures of the compounds obtained after column chromatography of the methanol-soluble fraction were determined by spectroscopy and in comparison with published data. The broth micro-dilution method was used to evaluate the antimicrobial activities against three bacteria species (Salmonella typhi, Stahylococcus aureus and Pseudomonas aeruginosa) and four yeast species (Candida albicans, Candida tropicalis, Candida parapsilosis and Cryptococcus neoformans).

Results

Chemical analysis of the methanol extract from the stem bark of Vismia rubescens yielded five known compounds 1,4,8-trihydroxyxanthone (1), 1,7-dihydroxyxanthone (2), physcion (3), friedelin (4) and friedelanol (5). The crude extract and compounds 1, 2 and 3 exhibited both antibacterial and antifungal activities that varied between the microbial species (MIC = 3.12–1000 μg/ml). Compounds 2 and 3 were the most active (MIC = 3.12–100 μg/ml) while Stahylococcus aureus and Pseudomonas aeruginosa were sensitive to all the tested compounds. The antimicrobial activity of this plant as well as that of compounds 1 and 2 is being reported here for the first time.

Conclusion

These results provide promising baseline information for the potential use of this plant as well as some of the isolated compounds in the treatment of skin diseases and diarrhoea.     

Antimicrobial activity of the methanolic extract and compounds from Morus mesozygia stem bark

Aim of the study

This study was aimed at investigating the antimicrobial activity of the methanolic extract (MMB) and compounds isolated from the stem bark of Morus mesozygia, namely 3β-acetoxyurs-12-en-11-one (1), moracin Q (2), moracin T (3), artocarpesin (4), cycloartocarpesin (5), moracin R (6), moracin U (8), moracin C (9), and moracin M (10).

Materials and Methods

The liquid microdilution assay was used in the determination of the minimal inhibitory concentration (MIC) and the minimal microbicidal concentration (MMC), against nine bacterial and two fungal species.

Results

The results of the MIC determination showed that the compounds 3, 4, 8 and 9 were able to prevent the growth of all tested microbial species. All other samples showed selective activities. Their inhibitory effects were noted on 90.9% studied organisms for the crude extract, 81.8% for compound 6, 72.7% for compound 10, 63.6% for compound 1, 54.5% for compound 5, and 45.5% for compound 2. The lowest MIC value of 39 μg/ml was obtained with the crude extract against Escherichia coli. The corresponding value for compounds (5 μg/ml) was registered with compound 9 on Shigella dysenteriae and compound 3 on E. coli, S. dysenteriae, Pseudomonas aeruginosa, Salmonella typhi and Bacillus cereus. The lowest MIC value (39 μg/ml) observed with the crude extract (on E. coli) was only eightfold greater than that of gentamycin used as reference antibiotic (RA) while the corresponding value (5 μg/ml) recorded with compounds 3 and 9 was equal to that of RA on the corresponding microorganisms.

Conclusions

The obtained results highlighted the interesting antimicrobial potency of M. mesozygia as well as that of the studied compounds, and provided scientific basis for the traditional use of this species.     

Mutagenic and antimutagenic activities of aqueous and methanol extracts of Euphorbia hirta

Euphorbia hirta (E. hirta) is a weed commonly found in tropical countries and has been used traditionally for asthma, bronchitis and conjunctivitis. However, one of the constituents in this plant, quercetin, was previously reported to be mutagenic. This work aimed to determine the level of quercetin in the aqueous and methanol plant extracts and to investigate the mutagenic effects of quercetin and the extracts in the Ames test utilising the mutant Salmonella typhimurium TA98 and TA100 strains. The antimutagenic activity of Euphorbia hirta aqueous and methanol extracts was also studied in Salmonella typhimurium TA98. HPLC analyses showed that quercetin and rutin, a glycosidic form of quercetin, were present in the acid-hydrolysed methanol extract and non-hydrolysed methanol extract respectively. The quercetin concentration was negligible in both non-hydrolysed and acid-hydrolysed aqueous extracts. The total phenolic contents in Euphorbia hirta were determined to be 268 and 93 mg gallic acid equivalent (GAE) per gram of aqueous and methanol extracts, respectively. Quercetin (25 μg/mL) was found to be strongly mutagenic in Salmonella typhimurium TA98 in the absence and presence of S-9 metabolic activation. However, both the aqueous and methanol extracts did not demonstrate any mutagenic properties when tested with Salmonella typhimurium TA98 and TA100 strains at concentrations up to 100 μg/mL in the absence and presence of S-9 metabolic activation. In the absence of S-9 metabolic activation, both the extracts were unable to inhibit the mutagenicity of the known mutagen, 2-nitrofluorene, in Salmonella typhimurium TA98. On the other hand, the aqueous extracts at 100 μg/mL and methanol extracts at 10 and 100 μg/mL exhibited strong antimutagenic activity against the mutagenicity of 2-aminoanthracene, a known mutagen, in the presence of S-9 metabolic activating enzymes. The results indicated that these extracts could modulate the xenobiotic metabolising enzymes in the liver at the higher concentrations.     

Antiinflammatory and antinociceptive activities of Blechnum occidentale L. extract

Aim of study

Blechnum occidentale L. is a terrestrial fern that ranges from the United States to South America, and is employed in Brazilian folk medicine. In the present study we investigated the antinociceptive and antiinflammatory activities of the methanolic extract of Blechnum occidentale L. (MEB) in animal models of pain and inflammation to support its medicinal use in treatment of inflammatory and pulmonary diseases, urinary infections and liver diseases.

Materials and methods

The antinociceptive activity of MEB was evaluated using the writhing, formalin, and tail flick tests. The antiinflammatory activity of MEB was evaluated in carrageenan-induced paw oedema and neutrophil migration. In order to discard possible non-specific muscle relaxant or sedative effects of MEB, mice motor performance was evaluated in the rota rod test and its toxicity evaluated over 14 days.

Results

Intraperitoneal (IP) administration of MEB (0.01–100 mg/kg) produced a dose-related antinociception on acetic acid-induced writhing in mice. Oral administration of MEB, at a different range of doses (100–400 mg/kg), also produced significant antinociceptive effect on the writhing test. Furthermore, treatment with MEB (100 and 200 mg/kg IP) inhibited significantly both the early and late phases of formalin-induced hypernociception in rats. In contrast, treatment with MEB (100 and 200 mg/kg IP) did not prevent the thermal nociception in the tail flick test. The IP administration of MEB (100 and 300 mg/kg) significantly reduced the paw oedema induced by carrageenan. Moreover, systemic treatment with MEB (11–300 mg/kg) reduced the neutrophil migration in the carrageenan-induced migration to the peritoneal cavity. In the rota rod test, MEB-treated mice did not show any significant motor performance alterations with the dose of 300 mg/kg. In addition, over the study duration of 14 days, there were no deaths or toxic signs recorded in the mice given 100 or 1000 mg/kg of MEB.

Conclusion

The results described here are the first report of pharmacological studies of Blechnum occidentale L. and indicate that this plant has antinociceptive and antiinflammatory activities which support its folk medicine use.     

Antimicrobial activity of the crude extract,fractions and compounds from stem bark of Ficus ovata (Moraceae)

Aim of the study

This study was designed to investigate the antimicrobial activities of the methanol extracts from the stem bark of Ficus ovata (FOB), fractions (FOB1–6) and compounds isolated following bio-guided fractionation [3-friedelanone (1), taraxeryl acetate (2), betulinic acid (3), oleanoïc acid (4), 2-hydroxyisoprunetin (5), 6,7-(2-isopropenyl furo)-5,2,4-trihydroxyisoflavone (6), Cajanin (7) and protocatechuic acid (8)].

Materials and Methods

The micro-dilution method was used for the determination of the minimal inhibition concentration (MIC) and the minimal microbicidal concentration (MMC) against fungi (two species), Gram-positive (three species) and Gram-negative bacteria (five species).

Results

The results of the MIC determinations indicated that the crude extract (FOB), fractions FOB2 and FOB4 as well as compound 5 were active on the entire studied organisms. Other samples showed selective activity, fractions FOB1, FOB3 and FOB5 being active against 50% of the tested microbial species while FOB6 was active on 40%. Compounds 8, 6, 2 and 7 prevented the growth of 80%, 70%, 50% and 20% of the organisms respectively. The lowest MIC value (156g/ml) observed with the crude extract was recorded on Streptococcus faecalis, Candida albicans and Microsporum audouinii. The corresponding value for fractions (39 μg/ml) was noted with FOB4 against Staphylococcus aureus, while that of the tested compounds (10 μg/ml) was observed with compound 8 on Microsporum audouinii. The results of the MMC determination suggested that the cidal effect of most of the tested samples on the studied microorganisms could be expected.

Conclusions

The overall results provided evidence that the studied plant extract, as well as some of the isolated compounds might be potential sources of new antimicrobial drug.     

Investigation for anti-inflammatory and anti-thrombotic activities of methanol extract of Capparis ovata buds and fruits

Ethnopharmacological relevance

Capparis ovata Desf. has wide natural distribution in Turkey and it is consumed in pickled form. Flower buds, root bark, and fruits of the plant are used traditionally due to their analgesic, anti-inflammatory, wound healing, anti-rheumatismal, tonic, and diuretic effects.

Aim of the study

The aim of this study was to investigate the possible anti-inflammatory and anti-thrombotic effects of methanol extracts prepared from flower buds (CBE) and fruits (CFE) of C. ovata.

Materials and methods

Anti-inflammatory effects of CBE and CFE were assessed using carrageenan-induced and prostaglandin E₂-induced mouse paw edema models. For the anti-thrombotic effect evaluation, carrageenan-induced tail thrombosis model was performed in mice. The extracts were administered intraperitonally (i.p.) at the doses of 100, 200, and 300 mg/kg. The anti-inflammatory effect of Capparis extracts were tested in comparison to 10 mg/kg diclofenac and anti-thrombotic activity to 10 and 100 IU heparin.

Results

CBE at the doses of 200, and 300 mg/kg and CFE at the doses of 100, 200, and 300 mg/kg showed significant anti-inflammatory activity and CFE reached therapeutic concentration early than CBE in carrageenan inflammation model. In prostaglandin E₂ inflammation model, CBE and CFE exhibited significant inhibitory effects. The C. ovata extracts did not show remarkable anti-thrombotic effect.

Conclusions

Based on the results obtained, it can be concluded that fruits of C. ovata have more potent anti-inflammatory effect than flower buds. It has been suggested that inhibition of cyclooxygenase pathway is one of the mechanisms of the activity. C. ovata may be potentially used as therapeutic agents for inflammatory diseases.     

Anticonvulsant effect of Rhus chirindensis (Baker F.) (Anacardiaceae) stem-bark aqueous extract in mice

Extracts of Rhus chirindensis stem-bark are used extensively in South African traditional medicines for the treatment, management and/or control of an array of human ailments, including childhood convulsions and epilepsy. In this study, we investigated the anticonvulsant activity of the plant's stem-bark aqueous extract (RCE, 50-800 mg/kg i.p.) against pentylenetetrazole (PTZ)-, picrotoxin (PCT)- and bicuculline (BCL)-induced seizures in mice. Phenobarbitone and diazepam were used as reference anticonvulsant drugs for comparison. Single intraperitoneal injections of PTZ (90 mg/kg), PCT(10 mg/kg) or BCL (30 mg/kg) produced tonic-clonic seizures. Like the standard antiseizure drugs used, Rhus chirindensis stem-bark aqueous extract (RCE, 100-800 mg/kg i.p.) significantly delayed (p<0.05-0.001) the onset of, and antagonized pentylenetetrazole-induced seizures. The plant's stem-bark aqueous extract (RCE, 100-800 mg/kg i.p.) also profoundly antagonized picrotoxin-induced seizures, but only weakly antagonized bicuculline-induced seizures. Although the data obtained in the present study do not provide conclusive evidence, it would appear that RCE produces its antiseizure effect by enhancing GABAergic neurotransmission and/or action in the brain. The results of this laboratory animal study indicate that RCE possesses anticonvulsant activity in the mammalian experimental model used, and thus suggest that the plant may be used as a natural supplementary remedy in the management, control and/or treatment of childhood convulsions and epilepsy. In conclusion, the findings of this study lend pharmacological credence to the suggested folkloric, ethnomedical uses of Rhus chirindensis in the management of childhood convulsions and epilepsy in some rural communities of South Africa.     

Toxicology evaluation of standardized methanol extract of Gynura procumbens

Aims of the study

Gynura procumbens (Merr.), which is known as “Sambung nyawa”, is widely used in South East Asian countries in the traditional treatment of many ailments. However, there is little toxicological information available regarding safety following repeated exposure.The present investigation describes the toxicity of a methanol extract of Gynura procumbens leaves in rats.

Materials and methods

For acute toxicity studies, a methanol extract of Gynura procumbens was orally administered to Sprague–Dawley rats (female and male) at a dose range of 1000–5000 mg/kg. For sub-chronic toxicity studies, the rats were orally administered the methanol extract of Gynura procumbens at the doses of 125, 250, and 500 mg/(kg day) for a period of 13 weeks. The animals were sacrificed, followed by examination of their organs and blood serum.

Results and conclusions

Administration of the methanol extract from Gynura procumbens leaves at 1000–5000 mg/kg did not produce mortality or significant changes in the general behaviour, body weight, or organ gross appearance of rats. There were no significant differences in the general condition, growth, organ weights, haematological parameters, clinical chemistry values, or gross and microscopic appearance of the organs from the treatment groups as compared to the control group. Therefore, the NOAEL for the Gynura procumbens methanol extract is 500 mg/(kg day) administered orally for 13 weeks.     

Anticonvulsant activity of aqueous root extract of Ficus religiosa

Ethnopharmacological relevance

Ficus religiosa Linn is frequently used for the treatment of nervous disorders among Pawara tribe of the Satpuda range, India.

Aim of the study

This study aimed to investigate the anticonvulsant activity of the aqueous aerial root extract of Ficus religiosa in chemoconvulsant-induced seizures in mice.

Materials and methods

The anticonvulsant activity of the extract (25, 50 and 100 mg/kg, p.o.) was investigated in strychnine-, pentylenetetrazole-, picrotoxin- and isoniazid-induced seizures in mice. Rat ileum and fundus strip preparations were used to study the effect of the extract on acetylcholine (Ach)- and serotonin (5-HT)-induced contractions, respectively.

Results

The extract showed no toxicity and protected the animals in the strychnine and pentylenetetrazole tests in a dose-dependent manner. Its effect in the picrotoxin and isoniazid tests, however, was less potent. The extract also exhibited dose-dependent potentiation of Ach in rat ileum but failed to potentiate the effect of 5-HT in rat fundus strip preparation.

Conclusions

The results suggest that an orally administered aqueous root extract of Ficus religiosa has dose-dependent and potent anticonvulsant activities against strychnine- and pentylenetetrazole-induced seizures. The observed activities may be ascribed to the appreciable content of zinc and magnesium in the extract.     

In vitro and in vivo hepatoprotective and antioxidant activity of ethanolic extract from Meconopsis integrifolia (Maxim.) Franch

Ethnopharmacological relevance

Meconopsis integrifolia (Maxim.) Franch is a high mountain endemic species used as a traditional Tibetan and Mongolian herb to treat hepatitis, pneumonia, and edema. This study aims to investigate the hepatoprotective and antioxidant effects of Meconopsis integrifolia ethanolic extract (MIE) in vitro and in vivo.

Materials and methods

The in vitro antioxidant property of MIE was investigated by employing various established systems. Rats with carbon tetrachloride (CCl₄)-induced liver injury were used to assess the hepatoprotective and antioxidant effect of MIE in vivo. The level or activity of alkaline phosphatase (ALP), glutamate pyruvate transaminase (ALT), aspartate aminotransferase (AST), and total bilirubin (TB) in the blood serum and thiobarbituric acid reactive substances (TBARS), superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH) in the liver and kidney of the rats were assayed using standard procedures.

Results

MIE exhibited strong antioxidant ability in vitro. In the rats with CCl₄-induced liver injury, the groups treated with MIE and silymarin showed significantly lower levels of ALT, AST, ALP, and TB. MIE demonstrated good antioxidant activities in both the liver and kidney of the rats in vivo.

Conclusions

MIE exhibits excellent hepatoprotective effects and antioxidant activities in vitro and in vivo, supporting the traditional use of Meconopsis integrifolia in the treatment of hepatitis.     

Antimicrobial activity of the methanolic extracts and compounds from Treculia obovoidea (Moraceae)

The crude extract from Treculia obovoidea was subjected to purification by repeated chromatography. Eight compounds were isolated from Treculia obovoidea and identified as Psoralen (1), Bergapten (2), 7-methoxycoumarin (3), 7-hydroxycoumarin (4), 4,2′,4′-trihydroxychalcone (5), 4,2′,4′-trihydroxy-3-prenylchalcone (6), 3-hydroxy-4-methoxybenzoic acid (7) and O-[3-(2,2-dimethyl-3-oxo-2H-furan-5-yl) butyl] bergaptol (8). These compounds together with the extract were tested for their antimicrobial activity against Gram-positive bacteria (six species), Gram-negative bacteria (12 species) and three Candida species using micro-dilution methods for the determination of the minimal inhibition concentration (MIC) and the minimal microbicidal concentration (MMC). The MIC values obtained with the crude extracts varied from 78.12 to 156.25 μg/ml against 17 (80.95%) of the 21 tested microorganisms. All the isolated compounds showed selective activity. The antimicrobial activity of this plant as well as that of compounds 6 and 8 is being reported for the first time. The obtained results provide promising baseline information for the potential use of these crude extract as well as some of the isolated compounds in the treatment of bacterial and fungal infections.     

In vitro antigonococcal activity of Coscinium fenestratum stem extract

Ethnopharmacological relevance

Gonorrhea is a sexually transmitted disease (STD), which originates from bacteria, Neisseria gonorrhoeae. It is still one of the major health problems worldwide in both men and women. Many medicinal plants have been recorded in Thai folk medicine for relieving STD but there is no scientific report of these plants for antigonococcal activity.

Aim of the study

This study was conducted to evaluate antigonococcal activity of 22 Thai medicinal plants selected from the plants popularly used in Thai folk medicine for treatment of gonorrhea.

Materials and methods

This study was performed by disc diffusion and agar dilution methods against Neisseria gonorrhoeae. Active compound was investigated by bioautographic assay.

Results

Among the selected plants, Coscinium fenestratum (Gaertn.) Colebr. extract showed the most effective activity against Neisseria gonorrhoeae ATCC 49226 with MIC value of 47.39 μg/ml. Bioautographic assay revealed that berberine was the active compound of Coscinium fenestratum against Neisseria gonorrhoeae. The average MIC values of purified berberine against Neisseria gonorrhoeae ATCC 49226 and 11 clinical isolates were 13.51 and 17.66 μg/ml, respectively while average MIC value of the crude extract of Coscinium fenestratum against all clinical isolates was about 56.39 μg/ml. There was no acute toxicity detected at the dose of 5 g of Coscinium fenestratum crude extract per kilogram.

Conclusions

These results provide theoretical support for ethnopharmacological relevance of antigonococcal activity of Coscinium fenestratum and its active compound.     

Analgesic and antimalarial activities of crude leaf extract and fractions of Acalypha wilkensiana

Aim of the study

Antiplasmodial and analgesic activities of leaf extract and fractions of Acalypha wilkensiana were evaluated to ascertain the folkloric claim of its antimalarial and analgesic activities.

Materials and methods

The crude leaf extract (220–659 mg/kg) and fractions (chloroform and aqueous; 440 mg/kg) of Acalypha wilkensiana were investigated for antiplasmodial activity against chloroquine sensitive Plasmodium berghei infections in mice and for analgesic activity against chemical and heat-induced pains. The antiplasmodial activity during early and established infections as well as prophylactic activity were investigated. Chloroquine (5 mg/kg) and pyrimethamine (1.2 mg/kg) were used as positive controls. Thin films made from tail blood of each mouse were used to assess the level of parasitaemia of the mice. Analgesic activity of the crude extract was also evaluated against acetic acid, formalin and heat-induced pains.

Results

The extract and its fractions dose-dependently reduced parasitaemia induced by chloroquine sensitive Plasmodium berghei infection in prophylactic, suppressive and curative models in mice. These reductions were statistically significant (p < 0.001). They also improved the mean survival time (MST) from 16 to 22 days relative to control (p < 0.01–0.001). The activities of extract/fractions were incomparable to that of the standard drugs used (chloroquine and pyrimethamine). On chemically and thermally induced pains, the extract inhibited acetic acid and formalin-induced inflammation as well as hot plate-induced pain in mice. These inhibitions were statistically significant (p < 0.001) and in a dose-dependent fashion.

Conclusion

The antiparasitaemic and analgesic effects may in part be mediated through the chemical constituents of the plant.     

Assessment of antidiarrhoeal activity of the methanol extract of Xylocarpus granatum bark in mice model

The methanol extract of Xylocarpus granatum bark was studied for its antidiarrhoeal properties in experimental diarrhoea, induced by castor oil and magnesium sulphate in mice. At the doses of 250 and 500 mg/kg per oral, the methanol extract showed significant and dose-dependent antidiarrhoeal activity in both models. The extracts also significantly reduced the intestinal transit in charcoal meal test when compared to atropine sulphate (5 mg/kg; i.m.). The results showed that the extracts of Xylocarpus granatum bark have a significant antidiarrhoeal activity and supports its traditional uses in herbal medicine.