Cycloartane triterpenoid saponins from water soluble of Passiflora edulis Sims and their antidepressant-like effects

Ethnopharmacological relevance

Various species of genus Passiflora have been used as traditional folk medicines owing to their sedative and anti-hypertensive properties. Passiflora edulis Sims most widely grown in the warm temperate for their fragrant fruits and their twigs and leaves are used as a folk medicine for treating both anxiety and nervousness in American countries. The present study was to evaluate the antidepressant-like effect and the active components of this plant.

Materials and methods

The alcohol extracts of the stems (PES, 10 and 2 g/kg of the plant materials) and leaves (PEL, 10 and 2 g/kg of the plant materials) of Passiflora edulis Sims were orally administered to mice for 7 day. The animals were tested in the forced swim test (FST) and tail suspension test (TST). After behavioral assay of ethanol extract, phytochemical research of the stems and leaves (5.7 kg) of Passiflora edulis Sims were developed and further bioactive verification of monomeric compounds were conducted.

Results

There are mainly cycloartane triterpenoids and their saponins isolated from this plant, including two new cycloartane triterpenoid saponins named cyclopassifloside ХII (1) and ХIII (2), together with six known cycloartane triterpenoids, cyclopassifloic acids B and E, cyclopassiflosides II, VI, IX and XI. The ethanol extract of Passiflora edulis Sims together with isolated compounds cyclopassiflosides IX and XI may possess antidepressant-like effect.

Conclusions

Cycloartane triterpenoid was one of the main compositions of Passiflora edulis Sims and possess antidepressant-like activity.     

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.     

Antihistaminic and antiallergic actions of extracts of Solanum nigrum berries: Possible role in the treatment of asthma

Ethnopharmacological relevance

Berries of the plant Solanum nigrum Linn (Solanaceae) are used for the treatment of asthma in folk medicine and ancient books.

Aim of study

To evaluate potential of the plant berries in the treatment of asthma.

Materials and methods

Petroleum ether, ethanol and aqueous extracts of S. nigrum berries (50, 100 and 200 mg/kg, i.p.) were screened for the treatment of asthma by the various methods viz. effect on clonidine and haloperidol induced catalepsy, milk-induced leucocytosis and eosinophilia, mast cell stabilizing activity in mice and studies on smooth muscle preparation of guinea pig ileum (in vitro). Active petroleum ether extract was standardized by HPTLC.

Results

The petroleum ether extract of S. nigrum berries inhibited clonidine-induced catalepsy significantly but not haloperidol-induced catalepsy. Petroleum ether extract significantly inhibited increased leukocyte and eosinophil count due to milk allergen and showed maximum protection against mast cell degranulation by clonidine. Petroleum ether extract resisted contraction induced by histamine better than other extracts. All the results are dose dependant. Active petroleum ether extract showed presence of antiasthmatic compound, β-sitosterol.

Conclusion

The petroleum ether extract of S. nigrum berries can inhibits parameters linked to the asthma disease.     

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.     

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

Ethnopharmacological relevance

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

Materials and methods

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

Results

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

Conclusions

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

Anti-inflammatory and analgesic activities of methanolic extract of Kigelia pinnata DC flower

Ethnopharmacological relevance

Kigelia pinnata DC is extensively used in Indian traditional medicine for several diseases including inflammatory and painful disorders.

Aim of the study

The aim of the present study is to investigate the possible anti-inflammatory and analgesic activities of methanolic extract of Kigelia pinnata flower (MKFL) to support the medicinal uses claimed by folklore practitioners.

Materials and methods

MKFL is evaluated for its anti-inflammatory activity in carrageenan-induced paw edema model in rats and analgesic activity in acetic acid-induced writhing, hot plate and formalin-induced paw licking models in mice.

Results

MKFL exhibited a significant (P < 0.01) anti-inflammatory and analgesic activities with the doses of 100, 200 and 400 mg/kg b.w. in rats and mice respectively.

Conclusions

The results of the experimental study thus strongly support the traditional use of this plant for inflammatory and pain disorders.     

Screening of the topical anti-inflammatory activity of the bark of Acacia cornigera Willdenow, Byrsonima crassifolia Kunth, Sweetia panamensis Yakovlev and the leaves of Sphagneticola trilobata Hitchcock

Ethnopharmacological relevance

An investigation of topical anti-inflammatory activity was undertaken on plants used in Central America traditional medicine.

Aim of study

Four herbal drugs used in the folk medicine of Central America to treat inflammatory skin affections (Acacia cornigera bark, Byrsonima crassifolia bark, Sphagneticola trilobata leaves and Sweetia panamensis bark) were evaluated for their topical anti-inflammatory activity.

Materials and methods

Petroleum ether, chloroform and methanol extracts were obtained for herbal medicines and then extracts were tested on Croton oil-induced ear dermatitis model in mice.

Results

Almost all the extracts reduced the Croton oil-induced ear dermatitis in mice and the chloroform ones showed the highest activity, with ID₅₀ (dose giving 50% oedema inhibition) values ranging from 112 μg/cm² (Byrsonima crassifolia) to 183 μg/cm² (Sphagneticola trilobata). As reference, ID₅₀ of the non-steroidal anti-inflammatory drug indomethacin was 93 μg/cm².

Conclusions

Lipophilic extracts from these species can be regarded as potential sources of anti-inflammatory principles.     

Citrus limetta leaves extract antagonizes the hypertensive effect of angiotensin II

Ethnopharmacological relevance

Citrus limetta Risso (Rutaceae) is widely used in Mexico for healing purposes, among them as antihypertensive treatment.

Aim of the study

To assess the antihypertensive effect of C. limetta leaves as one of its ethnomedical uses.

Materials and methods

The acute response of blood pressure to angiotensin II administration was measured in mice. Additionally, the acute oral toxicity profiles were determined.

Results

The findings of the current investigation showed that different concentrations of the aqueous extract prevented the raise of systolic blood pressure (p ≤ 0.001 vs. vehicle), diastolic blood pressure (p ≤ 0.0002 vs. vehicle) and mean blood pressure (p ≤ 0.0000 vs. vehicle); with a dose dependent effect for diastolic pressures at 125–500 mg/kg dosages. The 500 and 1000 mg/kg doses inhibited the action of Ang II in similar extent to telmisartan. Toxic signs or deaths were not observed in mice treated at 2000 mg/kg of C. limetta extract.

Conclusions

All doses of C. limetta aqueous extract, used in this assay, were safe and effective.     

In vivo antimalarial activities of Enantia polycarpa stem bark against Plasmodium berghei berghei in mice

Ethnopharmacological relevance

Enantia polycarpa (PC) Engl. Et Diels (Annonaceae) is used in traditional medicine as an antimalarial remedy in Southern Nigeria.

Aim of the study

The antimalarial activities of ethanolic stem bark extracts of Enantia polycarpa was studied in vivo, in mice infected with Plasmodium berghei berghei.

Materials and methods

The ethanolic stem bark extract of Enantia polycarpa was administered at doses ranging from 200 to 600 mg/kg/day to Plasmodium berghei infected mice in both early and established models of antiplasmodial studies.

Results

The extract of Enantia polycarpa exhibited promising antimalarial activity against both early and established infections. At a dose of 600 mg/kg the extract achieved a 75.8% and 72% chemosuppression of parasitaemia in the study of acute and established infections, respectively. The extract also prolonged mean survival time of Plasmodium berghei infected mice during the study of established infection. The mean survival time of mice administered Enantia polycarpa extract at 600 mg/kg/day (27 days) was significantly longer than infected/untreated control (12 days). For the acute toxicity study the extract had an intraperitoneal LD₅₀ of 186 mg/kg but caused no mortality when administered orally at doses as high as 2,000 and 4,000 mg/kg.

Conclusions

Collectively, the results indicate that Enantia polycarpa is safe when administered orally and possesses promising antimalarial activity, thus supporting its use in traditional medicine for the treatment of malaria.     

Effect of Laggera alata on hepatocyte damage induced by carbon tetrachloride in vitro and in vivo

Ethnopharmacological relevance

Laggera alata, as a traditional Chinese herbal medicine, has been widely used to ameliorate some ailments associated with inflammation including hepatitis in folk.

Aim of the study

Based on anti-inflammatory activity of total phenolics from Laggera alata (TPLA), to further validate the remarkable curative effect Laggera alata in hepatitis, hepatoprotective effect of TPLA was examined.

Materials and methods

TPLA was prepared and its principle components were quantificationally analyzed. The hepatoprotective effects of TPLA were studied using a CCl₄-induced injury model in primary cultured neonatal rat hepatocytes, and a CCl₄-induced acute and chronic damage model in vivo.

Results

TPLA significantly reduced cellular leakage of hepatocyte aspartate aminotransferase (AST) and alanine aminotransferase (ALT) and improved cell viability in vitro. TPLA markedly decreased the serum AST and ALT levels of the mice, the levels of AST, ALT, total protein, albumin, and sialic acid in rat serum, and the hydroxyproline level in rat liver. Meanwhile, severe hepatic lesions induced by CCl₄ in mice/rats were remarkably improved by the administration of TPLA.

Conclusions

This investigation verifies the hepatoprotective effect of TPLA in vitro/in vivo and clarifies its active components dicaffeoylquinic acids responsible for hepatoprotective potential.     

Anxiolytic-like effect of Sonchus oleraceus L. in mice

Ethnopharmacological relevance

Sonchus oleraceus L. has been used as a general tonic in Brazilian folk medicine. Nevertheless, available scientific information regarding this species is scarce; there are no reports related to its possible effect on the central nervous system.

Aim of the study

This study was conducted to establish the anxiolytic effect of extracts from the aerial parts of Sonchus oleraceus.

Materials and methods

This study evaluated the effect of hydroethanolic and dichloromethane extracts of Sonchus oleraceus in mice submitted to the elevated plus-maze and open-field tests. Clonazepam was used as the standard drug.

Results

In the elevated plus-maze test, the Sonchus oleraceus extracts increased the percentage of open arm entries (P < 0.05) and time spent in the open-arm portions of the maze (P < 0.05). The extracts induce an anti-thigmotactic effect, evidenced by increased locomotor activity into the central part of the open field set-up (P < 0.05). The extracts administered at 30–300 mg/kg, p.o. had a similar anxiolytic effect to clonazepam (0.5 mg/kg, p.o.).

Conclusion

These data indicate that Sonchus oleraceus extract exerts an anxiolytic-like effect on mice.     

Anti-inflammatory and analgesic properties of Heracleum persicum essential oil and hydroalcoholic extract in animal models

Ethnopharmacological relevance

Fruits of Heracleum persicum (Apiaceae) are used as pain killer in Iranian folkloric medicine.

Aims of study

To evaluate the anti-inflammatory and analgesic effects of the hydroalcoholic extract and essential oil of the plant fruits and analyzing the essential oil.

Materials and methods

Essential oil and hydroalcoholic extracts of the fruits were prepared according to standard methods and the components of essential oil were identified using GC–MS method. The acetic acid-induced writhing response and formalin test were used in male mice to assess analgesic activity. For evaluation of anti-inflammatory effect, carrageenan-induced rat paw edema was used.

Results

Hexyl butyrate (56.5%), octyl acetate (16.5%), hexyl 2-methylbutanoate (5.2%) and hexyl isobutyrate (3.4%) were identified as the major constituents of the oil. Oral or intraperitoneal administration of Heracleum persicum essential oil (HPEO) at doses of 50–200 mg/kg and Heracleum persicum hydroalcoholic extract (HPHE) at doses of 250 and 500 mg/kg significantly reduced acetic acid-induced abdominal constrictions. HPEO and HPHE also significantly attenuated the pain response of the second phase of formalin test.In carrageenan test HPEO at doses of 100 and 200 mg/kg and HPHE at a dose of 400 mg/kg induced a significant reduction of paw edema.

Conclusions

These results clearly show the analgesic and anti-inflammatory effects of the plant essential oil and hydroalcoholic extract. Further studies are needed to clarify the mechanism of action and the components responsible for these pharmacological effects.     

Anti-inflammatory and antinociceptive activities of Campomanesia adamantium

Ethnopharmacological relevance

Campomanesia species are used in folk medicine as anti-inflammatory, anti-rheumatic, anti-diarrheal and hypocholesterolemic.

Aim of the study

The present study investigated the in vivo anti-inflammatory and antinociceptive properties of ethyl acetate (AE) and aqueous (Aq) extracts from leaves of Campomanesia adamantium and in vitro anti-inflammatory activity of AE and its isolated flavonols, myricitrin and myricetin.

Materials and methods

The antinociceptive activity of AE and Aq was evaluated using acetic acid-induced writhing and formalin methods. The in vivo anti-inflammatory effect of AE and Aq was evaluated using carrageenan-induced paw oedema in mice. AE, myricitrin and myricetin were evaluated for their abilities to modulate the production of NO, TNF-α and IL-10 in LPS/IFN-γ stimulated J774.A1 macrophages.

Results

It was found that orally administrated AE and Aq (125 and 250 mg/kg) inhibited carrageenan-induced paw oedema in mice. AE (125 and 250 mg/kg) and Aq (125 mg/kg) reduced the time to licking at the second phase of the formalin method in vivo in mice. AE (250 mg/kg) and Aq (125 mg/kg) also reduced the number of writhes. AE, myricitrin and myricetin inhibited NO (320 μg/mL and 6.25–100 μM, respectively) and TNF-α production by macrophages (320 μg/mL for AE, 100 μM for myricitrin and 25–100 μM for myricetin). AE (160 and 320 μg/mL), myricitrin (50 and 100 μM) and myricetin (25–100 μM) increased IL-10 production by macrophages.

Conclusions

The ethyl acetate and aqueous extracts from Campomanesia adamantium showed antinociceptive and anti-inflammatory effects supporting the use of the plant in folk medicine. The results suggest that anti-oedematogenic effect promoted by aqueous extract involves several anti-inflammatory mechanisms of action. The antinociceptive effect shown by aqueous extract can be due to the modulation of release of inflammatory mediators involved in nociception. The anti-inflammatory effects of AE and of its isolated flavonols may be attributed to inhibition of pro-inflammatory cytokines production, TNF-α and NO and to the increased of IL-10 production.     

Dual protective effect of Passiflora incarnata in epilepsy and associated post-ictal depression

Ethnopharmacological relevance

Passiflora incarnata L. (Passifloraceae) has been used for the treatment of epilepsy in several traditional systems of medicine.

Aim of the study

The aerial parts of Passiflora incarnata contain multiple bioactive metabolites such as, flavonoids (like, chrysin that show CNS depressant activity by agonizing GABA-benzodiazepine receptor), amino acids (like, GABA), harmala alkaloids (reversible monoamine oxidase-A inhibitor), etc. In view of this, the present study was designed to investigate dual protective effect of the hydroethanolic extract of Passiflora incarnata in pentylenetetrazol (PTZ)-induced seizure and associated post-ictal depression.

Materials and methods

Different groups of mice were administered with repeated subconvulsive doses of PTZ (50 mg/kg; i.p.) at an interval of 5 days for 15 days. From 5th to 15th day the animals in different groups were administered daily with varying doses of hydroethanolic extract of Passiflora incarnata (150, 300, and 600 mg/kg; i.p.), diazepam (2 mg/kg; i.p.) and vehicle. On every 5th day, after PTZ treatment, seizure severity (score) was noted. Following convulsive episodes the locomotor activity (using actophotometer) and immobility period (using forced swim test) were also determined. On 15th day after behavioral assessment, the brain serotonin and noradrenaline levels were determined using spectrofluorometric methods.

Results

Treatment with the extract significantly (p < 0.05) reduced the seizure severity and immobility period as compared to vehicle control, in a dose and time-dependent manner. Moreover, the extract treatment retained the serotonin and noradrenaline levels of the brain.

Conclusions

The results of present study concluded that the hydroethanolic extract of Passiflora incarnata suppress PTZ-induced seizures, and ameliorates its associated post-ictal depression, which has been found to be get worsened with the standard antiepileptic drug, diazepam.     

Prophylactic and curative activities of extracts from Warburgia ugandensis Sprague (Canellaceae) and Zanthoxylum usambarense (Engl.) Kokwaro (Rutaceae) against Plasmodium knowlesi and Plasmodium berghei

Ethnopharmacological relevance

This work reports the anti-plasmodial activities of Warburgia ugandensis and Zanthoxylum usambarense commonly used as phytomedicines against malaria by some Kenyan communities.

Aim of study

To determine the anti-plasmodial activities of extracts from Warburgia ugandensis and Zanthoxylum usambarense against Plasmodium knowlesi and Plasmodium berghei.

Materials and methods

Eight plant extracts were screened for in vitro anti-plasmodial activity against Plasmodium knowlesi, in a 96-well plate incubated at 37 °C on a RPMI culture medium supplemented with baboon serum. Of the eight, three were investigated for prophylactic and curative activities in BALB/c mice against drug-sensitive Plasmodium berghei in a 4-day test at a dose rate of 200 mg/kg/day.

Results

Inhibitory concentrations (IC₅₀) values of between 3.14 and 75 μg/ml, up to 69% chemosuppression of parasites growth and over 80% survivorship of treated mice were observed.

Conclusion

The two medicinal plants, Warburgia ugandensis and Zanthoxylum usambarense possess bioactive compounds against malaria parasites and could be exploited for further development into malaria therapy.     

In vivo and in vitro anti-inflammatory properties of Achyrocline alata (Kunth) DC

Ethnopharmacological relevance

Achyrocline alata is a locally marketed (Mato Grosso do Sul/ Brazil) herb used in folk medicine as an anti-inflammatory and a sedative. Evaluate the anti-inflammatory properties of Achyrocline alata in both in vivo and in vitro models.

Materials and methods

A hydroethanolic extract from inflorescences of Achyrocline alata (HEAa) was characterized by HPLC-DAD and compared to standards (chlorogenic acid; isoquercetrin; quercetin; 4,2?,4?-trihydroxy-6?-methoxychalcone; gnaphalin; 3-O-methyl-quercetin; 3,5-dicaffeoyl-quinic acid and 4,5-dicaffeoyl-quinic acid). The in vivo anti-inflammatory properties of the HEAa (4, 20 and 100 mg/kg, per os) were evaluated using the following animal models: carrageenan-induced paw edema in rats, carrageenan-induced vascular permeability and peritonitis in mice and an acetic acid-induced writhing model to test antihyperalgesic activity in mice. In vitro assays were performed to study the effects of the HEAa (0.16, 0.8 and 4 mg/ml) on the cell viability, cell spreading and production of NO and H₂O₂ in stimulated macrophages.

Results

The A. alata extract inhibited the development of edema and vascular permeability, reduced polymorphonuclear cell recruitment in the acute peritonitis assay and decreased the amount of writhing induced by acetic acid. The HEAa did not increase NO/H₂O₂ production, while it did inhibit production when the macrophages were stimulated by LPS or PMA at all tested concentrations. In the presence of HEAa, macrophage spreading did not increase even after stimulation with LPS. Additionally, the HEAa was nontoxic to macrophages at all tested concentrations.

Conclusions

The HEAa displayed anti-inflammatory and antihyperalgesic effects, which supports the use of this plant in folk medicine. These effects might be due to the flavonoids and phenylpropanoids derivatives present in the HEAa.     

Quantitative evaluation of therapeutic effect of Liriope platyphylla on phthalic anhydride-induced atopic dermatitis in IL-4/Luc/CNS-1 Tg mice

Ethnopharmacological relevance

A variety of previous pharmacological studies have suggested that Liriope platyphylla may exert beneficial biological effects on inflammation, diabetes, neurodegenerative disorder, obesity, and atopic dermatitis (AD).

Aim of the study

The therapeutic effect of aqueous extract of Liriope platyphylla (AEtLP) on AD was quantified using the luciferase report system in IL-4/Luc/CNS-1 transgenic (Tg) mice.

Materials and methods

Alteration of the luciferase signal was quantified in IL-4/Luc/CNS-1 Tg mice co-treated with phthalic anhydride (PA) and AEtLP for 2 weeks using the IVIS imaging system. Phenotypes of AD were assessed by ear thickness analysis, measurement of immune-related organ weights, ELISA, and histological and pathological analysis in Tg mice.

Results

A strong luciferase signal was detected in the abdominal region of IL-4/Luc/CNS-1 Tg mice treated with only PA. However, this signal was significantly reduced in IL-4/Luc/CNS-1 Tg mice co-treated with PA+AEtLP in an AEtLP concentration-dependent manner. Especially, three organs, the thymus, pancreas, and submandibular lymph node (SL), showed a high signal response to PA treatment. Furthermore, to verify whether or not alteration of the luciferase signal is associated with AD, these disease response phenotypes were measured in the same group of mice. Common allergenic responses including increases in ear thickness, lymph node weight, IgE concentration, and infiltrated mast cells were detected in IL-4/Luc/CNS-1 Tg mice treated with PA. However, these responses were dramatically decreased by AEtLP treatment for 2 weeks.

Conclusion

These results indicate that the luciferase signal may successfully reflect the therapeutic effects of AEtLP in IL-4/Luc/CNS-1 Tg mice. Further, we suggest additional evidence that Liriope platyphylla may be considered as an effective therapeutic drug for the treatment of AD.     

Investigation of antihyperglycaemic activity of aqueous and petroleum ether extract of stem bark of Pongamia pinnata on serum glucose level in diabetic mice

Aim of the study

The aim of the study was to evaluate the antihyperglycaemic activity of aqueous (PPSB-AQE) and petroleum ether (PPSB-PEE) extract of stem bark Pongamia pinnata in alloxan induced diabetic mice.

Materials and methods

Diabetes was induced in mice by alloxan (80 mg/kg, i.v.). After acute and subacute treatment serum glucose was determined. OGTT was performed in PPSB-PEE pretreated animals.

Results

PPSB-PEE (25, 50, 100, 200 and 400 mg/kg) showed significant reduction in serum glucose level in acute and subacute studies. The antihyperglycaemic effects of PPSBPE (100, 200 and 400 mg/kg) showed onset at 2 h and peak effect at 6 h and the effect was sustained until 24th h with 400 mg/kg. In subacute study, antihyperglycaemic effect was observed on 21st day. In PPSBPE treated mice the body weight was not reduced in contrast to that in vehicle group. In OGTT, increased glucose utilization was observed.

Conclusions

It is concluded that PPSB-PEE but not PPSB-AQE showed antihyperglycaemic activity.     

Aqueous ethanol extract of the fruit of Xylopia aethiopica (Annonaceae) exhibits anti-anaphylactic and anti-inflammatory actions in mice

Ethnopharmacological relevance

Xylopia aethiopica has been traditionally used in the form of the dried fruit decoction to treat bronchitis, asthma, arthritis and rheumatism in Ghana, Nigeria and Cameroon. Aim of the study is to evaluate the anti-anaphylactic and anti-inflammatory effects of a 70% aqueous ethanol extract of the fruits of Xylopia aethiopica.

Materials and methods

Systemic anaphylaxis was induced by the injection of either compound 48/80 or lipopolysaccharide, LPS and survival rates of mice monitored for 1 h or 7 days respectively while IgE-mediated anaphylaxis in a local allergic reaction was studied in the pinnal inflammation model in mice. Clonidine-induced catalepsy in mice was used to evaluate the indirect antihistamine effect of Xylopia aethiopica, XAE. The effects of XAE assessed on the maximal and total oedema responses in the carrageenan-induced paw oedema in mice was used to evaluate the anti-inflammatory action of the extract.

Results

Administered at 30, 100, 300 and 1000 mg kg⁻¹ p.o., XAE dose dependently suppressed compound 48/80-induced mouse systemic anaphylactic shock and offered 63% protection to mice against LPS-induced endotoxic shock at a dose of 300 mg kg⁻¹. In addition, the extract (30–300 mg kg⁻¹) in a dose dependent manner significantly inhibited by 23–62% the mouse pinnal inflammation. Clonidine-induced catalepsy in mice was significantly suppressed in a dose and time dependent manner when administered both prophylactically and therapeutically. In the same doses, when administered before the induction of the mouse carrageenan-induced paw oedema, the mean maximal swelling attained during 6 h was reduced to 41.02±6.94%, 35.61±4.30%, and 29.09±4.90% of the inflamed control response respectively and total paw swellings induced over the 6 h were also dose-dependently and significantly suppressed to 74.84±14.84%, 63.95±9.37%, and 48.13±10.90% of the inflamed control response respectively. Administered after the induction of the carrageenan paw oedema the mean maximal swelling attained during 6 h was suppressed to 49.84±3.95%, 43.62±1.01%, and 35.97±1.34% of the inflamed control response respectively while the total paw swellings induced over the 6 h were also dose-dependently and significantly suppressed at 100 and 300 mg kg⁻¹ to 72.39±4.38% and 60.81±3.25% of the inflamed control response respectively.

Conclusion

These findings suggest that XAE inhibits mast cell-dependent immediate allergic reactions and exhibit anti-inflammatory actions through the inhibition of histamine release from mast cells via stabilizing the cell membrane. Our results contribute towards validation of the traditional use of Xylopia aethiopica in the treatment of bronchitis, asthma, arthritis and rheumatism.     

Acute and sub-chronic toxicity of HPLC fingerprinted extract of Conyza sumatrensis (Retz.) E.H. Walker in rodents

Ethnopharmacological relevance

Conyza sumatrensis (CS) is an extensively used medicinal herb in the tropics for varied ailments related to pain, inflammation and malaria. Though in constant folkloric use, scientific validations are proving valuable.

Aim of the study

Evaluate the safety profile of methanol extract from CS in mice and rats through acute and sub-chronic toxicity studies respectively.

Material and methods

Acute toxicity study involved the single oral administration of CS at 1000, 2000 and 3000 mg/kg in mice, while the sub chronic toxicity was carried upon in rats at doses 250, 500 and 1000 mg/kg/day for 28 days. Besides body weight, general behaviour and mortality, serum biochemical parameters and liver histology were assessed after 7 and 28 days for acute and sub-chronic study respectively. The parameters were again checked on days 14 and 56 in order to assess the recovery from damage, if any. HPLC fingerprinting of the aqueous and methanol extract was performed through C18 column using water: acetonitrile as mobile phase with observations at 240 nm.

Results

In the acute toxicity test, single oral dose of 1000, 2000 and 3000 mg/kg of CS did not result in any behavioural changes or mortality, indicating non toxicity. In sub-chronic toxicity studies in rats, no mortality was observed at 250, 500 and 1000 mg/kg/day when administered orally for a period of 28 days. Except Serum Glutamate Pyruvate Transaminase (SGPT) level in acute study and Alkaline Phosphatase (ALP), SGPT and Serum Glutamate Oxaloacetate Transaminase (SGOT) level in sub-chronic study, all the observational, haematological and biochemical parameters studied showed non-significant changes. Histological examination of liver did not reveal any treatment-related effects in any of the studies. Moreover, haematological and biochemical changes orchestrated by CS got normalised after 14 and 56 days post-treatment in acute and sub-chronic toxicity respectively. The HPLC fingerprint could resolve 11 and 28 peaks from aqueous and methanol extracts respectively.

Conclusion

The experiments indicate the methanol extract to be safe even at high and repeated doses in pre-clinical studies even though the constituents are more than in aqueous extract.