Antinociceptive activity of fruits extracts and “arrope” of Geoffroea decorticans (chañar)

Ethnopharmacological relevance

Geoffroea decorticans (chañar) fruits and their derivate product (arrope) have been traditionally used as food and a folk medicine for the treatment of a wide variety of diseases including bronchopulmonary disorders and to relieve dolorous process.

Aim of the study

In order to evaluate the pharmacology action of this plant, studies were performed of antinociceptive and antioxidant activities.

Materials and methods

The aqueous and ethanolic extracts and arrope of chañar were evaluated in various established pain models, including chemical nociception induced by subplantar formalin and intraperitoneal acetic acid and thermal nociception method, such as tail immersion test in rats. To examine the possible connection of the opioid receptor to the antinociceptive activity of extracts and arrope it was performed a combination test with naloxone, a non-selective opioid receptor antagonist.

Results

The aqueous extract and arrope (1000 mg/kg) caused an inhibition of the pain in formalin test in the first phase, similar to morphine and decrease in the second phase. In a combination test using naloxone, diminished analgesic activity of aqueous extract and arrope were observed, indicating that antinociceptive activity is connected with the opioid receptor. The aqueous extract and arrope, caused an inhibition of the writhing response induced by acetic acid. Central involvement in analgesic profile was confirmed by the tail immersion test, in which the aqueous extract and arrope showed a significant analgesic activity by increasing latency time. The aqueous extract showed higher antioxidant activity than the arrope, it may be due to the cooking process.

Conclusions

This study has shown that the aqueous extract and arrope of Geoffroea decorticans (chañar) fruits, does possess significant antinociceptive effects. It is further concluded that aqueous extract with maximum inhibition of free radical is the most potent extract amount tested extracts. At the oral doses tested the aqueous extract and arrope were non-toxic. The present results justifies their popular use and constitutes the first validation study of the antinociceptive action.     

Substantiation of the ethnopharmacological use of Conyza sumatrensis (Retz.) E.H.Walker in the treatment of malaria through in-vivo evaluation in Plasmodium berghei infected mice

Ethnopharmacological relevance

Scientific validation of ethnopharmacologically used plants and their utilization for therapeutic interventions can be a source of affordable treatment especially for neglected diseases in endemic areas. Conyza sumatrensis is a plant which finds its use in treating malaria like fevers but lacks proper scientific validation. Our study has tried to address this gap by authenticating its traditional use for the treatment of malaria.

Aim of the study

Evaluate the antimalarial activity of extracts derived from Conyza sumatrensis for its ethnopharmacological validation.

Materials and methods

Shade dried leaves were extracted with varying concentrations of ethanol and concentrated for bio-evaluation. Swiss albino mice infected with 1×10⁶ parasitized red blood cells, were orally administered with test extracts for 7 days in two sets of experiments. The first set was used to evaluate alcoholic, hydroalcoholic and aqueous extracts while the second set was used to evaluate the dose response of alcoholic extract ranging from 500–1600 mg/kg. Mean survival time, parasitaemia and haemoglobin levels were considered to interpret the antimalarial potential. Phytochemical analysis for the presence of flavonoids, alkaloids tannins, total phenolics, riboflavin and thiamine was also carried out.

Results

Among the three extracts administered at 1000 mg/kg, chemo suppression was significantly (p<0.001) observed in the alcoholic extract (62.59±12.52%) followed by hydroalcoholic (41.81±19.04%, p<0.01) and aqueous (32.04±19.04%, P<0.05) indicating that the active constituents leach out in ethanol. The dose response study involving the ethanol extract concluded the optimum dose to be 1000 mg/kg, as also evidenced by the haemoglobin levels.

Conclusion

The plant exhibits moderate antimalarial activity which can be further prospected for active fractions or pure molecules for adjunctive therapy.     

Cholesterol-reducer,antioxidant and liver protective effects of Thymbra spicata L. var. spicata

Ethnopharmacological relevance

Thymbra spicata is a member of the Lamiaceae family; leaves of this plant have recently gained much popularity as a remedy to combat hypercholesterolaemia.

Aim of the study

To evaluate the antihypercholesterolaemic, antioxidant and anti-steatohepatitic activities of the diethyl ether (DEE), ethyl acetate (EtOAc) and remaining aqueous (RA) extracts from Thymbra spicata var. spicata in mice.

Materials and methods

In this study, diethyl ether, ethyl acetate and remaining aqueous extracts of Thymbra spicata L. var. spicata P.H.Davis (Lamiaceae) were evaluated for the effects on the plasma total cholesterol (TC), high-density lipoprotein (HDL), low-density lipoprotein (LDL), triglyceride (TG) and glucose; blood malondialdehyde (MDA) and reduced glutathione (GSH); erythrocyte superoxide dismutase (SOD) and catalase activity (CAT) in mice fed with high-fat diet (HFD).

Results

The HFD induced an increase in plasma TC, TG, LDL, MDA concentrations compared to control group. However, administration of DEE with HFD reduced TC, LDL, TG and MDA concentrations, while increased HDL concentration, as well as GSH, SOD and CAT activities compared to HFD. The other extract from the plant was RA, which also showed a similar activity profile with DEE except CAT. On the other hand, administration of EtOAc extract with HFD decreased plasma TC, TG and MDA, while GSH concentration was increased. Histopathologically, best liver conditions were observed in DEE and lesser in RA extracts. Based on the results obtained in this investigation it is suggested that the DEE and partially RA extracts of Thymbra spicata var. spicata displayed significant antihypercholesterolaemic, antioxidant and anti-steatohepatitic activities. HPLC analysis of the DEE extract of Thymbra spicata var. spicata revealed the presence of carvacrol (44.13%).

Conclusion

The observed cholesterol-reducer, antioxidant and liver protective effects of the DEE and partially of RA extracts of Thymbra spicata which contain mainly carvacrol indicates that these extracts possess some potential medicinal value and explain their ethnomedical use.     

Anti-inflammatory and analgesic effects of ethanol and aqueous extracts of Pterocephalus hookeri (C.B. Clarke) Höeck

Aim of the study

This study evaluates the anti-inflammatory and analgesic activities of the ethanol and aqueous extracts of a Tibetan herb Pterocephalus hookeri (C.B. Clarke) Höeck to provide experimental evidence for its traditional use such as cold, flu and rheumatoid arthritis.

Materials and methods

Investigations on the analgesic effects of P. hookeri (C.B. Clarke) Höeck were carried out, including hot-plate test and acetic acid-induced writhing. The anti-inflammatory activities were observed by utilizing the following models: carrageenin-induced edema of the hind paw of rats, cotton pellet-induced granuloma formation in rats, acetic acid-induced permeability, and xylene-induced ear edema in mice. The effects of the administration of indomethacin were also studied.

Results

It has been shown that the ethanol and aqueous extracts significantly increased the hot-plate pain threshold and reduced acetic acid-induced writhing response in mice. The ethanol and aqueous extracts remarkably inhibited the increase in vascular permeability induced by acetic acid and ear edema induced by xylene. The ethanol extract also significantly decreased the carrageenin-induced rat paw edema perimeter and inhibited the increase of granuloma weight.

Conclusion

The results show that the ethanol and aqueous extracts have both central and peripheral analgesic activities and as anti-inflammatory effects, supporting the traditional application of this herb in treating various diseases associated with inflammation and pain.     

Davilla elliptica and Davilla nitida: Gastroprotective,anti-inflammatory immunomodulatory and anti-Helicobacter pylori action

Ethnopharmacological relevance

Davilla elliptica and Davilla nitida are species commonly found in the Brazilian Cerrado biome.

Aim of the study

Based on ethnopharmacological and phytochemical analyses, methanolic extracts from leaves of Davilla elliptica (EDE) and Davilla nitida (EDN) were evaluated for their anti-ulcer, anti-inflammatory, immunological and anti-Helicobacter pylori activities.

Materials and methods

The gastroprotective action of both extracts was evaluated in rodent experimental models (HCl/ethanol, ethanol or NSAID). We also evaluated anti-inflammatory (carrageenin-induced rat hind paw edema), immunomodulatory (murine peritoneal macrophages) and antibacterial action of both extracts against a standard strain of Helicobacter pylori.

Results

EDE and EDN (500 mg/kg) were able to protect gastric mucosa against HCl/ethanol solution (EDE 63%; EDN 59%), absolute ethanol (EDE 95%; EDN 88%), and also against injurious effect of NSAID (EDE 77%; EDN 67%). When EDE and EDN were challenged with sulfhydryl depleter compound, the gastroprotective action of both extracts was completely abolished. EDE had gastroprotective effect related to increase of glutathione bioavailability and stimulated higher levels of NO, H₂O₂ and TNF-α production. Otherwise EDN showed better anti-Helicobacter pylori action than EDE. Neither extracts presented anti-inflammatory activity by oral route.

Conclusion

The phytochemical investigation showed that both extracts possess phenolic acid derivatives, acylglycoflavonoids and condensed tannins with evident quantitative variations that probably influenced the pharmacological differences between extracts.     

Anti-inflammatory activity of roots of Ecbolium viride (Forsk) Merrill

Ethnopharmacological relevance

Traditionally the aqueous extracts of dried roots of the plant Ecbolium viride are used for menorrhagia, rheumatism and jaundice.

Aim of the study

The aim was to evaluate the anti-inflammatory activity of Ecbolium viride extract in an in vivo model.

Materials and methods

The ethyl acetate fraction of Ecbolium viride root extract was prepared and administered orally to rats. The anti-inflammatory activity of Ecbolium viride was determined by carrageenan-induced paw edema and cotton pellet granuloma models.

Results

Oral administration of Ecbolium viride extract reduced inflammation significantly (P < 0.01) in both the carageenan paw edema and the cotton pellet granuloma models.

Conclusions

The results of the study supported the traditional use of Ecbolium viride in the treatment for inflammatory disease.     

Analgesic and anti-inflammatory effects of Cassia siamea Lam. stem bark extracts

Aim of the study

The present study was carried out to investigate analgesic and anti-inflammatory activities of Cassia siamea Lam stem bark extracts. We have also determined the cytotoxicity of each extract.

Materials and methods

C. siamea, a widespread medicinal plant traditionally used in sub-Saharan Africa, was collected in Congo Brazzaville. Stem bark was extracted with petroleum ether (CSE1), chloroform (CSE2), ethanol (CSE3) and water (CSE4). Analgesic, anti-inflammatory and antipyretic activities of these extracts were assessed in rats with hot plate test, paw pressure and carrageenan induced paw oedema. Cytotoxicity was assessed against KB and Vero cells.

Results

At the doses used (100, 200, and 400 mg/kg) ethanol and water extracts showed significant and dose-dependent analgesic and anti-inflammatory effects. None of the extracts had cytotoxic activity on KB and Vero cell lines and the most active extracts (CSE3 and CSE4) had no acute toxicity.

Conclusions

The study highlighted the analgesic and anti-inflammatory of C. siamea stem bark. Four major families of compounds present in the plant may explain these activities: triterpenes (lupeol, oleanolic acid, ursolic acid, friedelin, betulin), flavonoids (apigenin, kaempferol, luteolin), anthraquinones (emodin), phytosterols (stigmasterol, beta-sitosterol).     

Anti-nociceptive activity of Pereskia bleo Kunth. (Cactaceae) leaves extracts

Ethnopharmacological relevance

Local communities in Malaysia consume Pereskia bleo Kunth. (Cactaceae) leaves as raw vegetables or as a concoction and drink as a tea to treat diabetes, hypertension, rheumatism, cancer-related diseases, inflammation, gastric pain, ulcers, and for revitalizing the body.

Aim of the study

To evaluate anti-nociceptive activity of the extracts and vitexin, isolated for the first time in this species, in two analgesic models; formalin-induced licking and acetic acid-induced abdominal writhing.

Materials and methods

Three and a half kilos of P. bleo leaves were extracted using Soxhlet apparatus with ethanol for 72 h. The crude ethanol extract was treated with activated charcoal overnight and subjected to a liquid–liquid partition yielding hexane, dichloromethane, ethyl acetate and butanol extracts. All extracts, including the crude ethanol and vitexin isolated from the ethyl acetate partition were tested for peripheral anti-nociceptive activity using formalin test and acetic acid-induced abdominal writhing, besides having their acute toxicity assays performed.

Results

The phytochemical analyses resulted in the isolation of vitexin (1), β-sitosterol glucoside (2) and β-sitosterol (3) isolated from the ethyl acetate, dichloromethane and hexane extracts, respectively. This is the first time vitexin and β-sitosterol glucoside are isolated from this species. The anti-nociceptive activities for all extracts were only moderate. Vitexin, which was isolated from the ethyl acetate extract did not show any activity in all models tested when used alone at the same concentration as it appears in the extract.

Conclusion

This study showed that all the extracts possess moderate anti-nociceptive activity. Vitexin is not the compound responsible for the anti-nociceptive effect in the ethyl acetate extract. Further investigations are needed to identify the compound(s) that might be responsible for the anti-nociceptive activity in this plant.     

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.     

Antioxidant and anti-inflammatory activities of the phenolic extracts of Sapium sebiferum (L.) Roxb. leaves

Ethnopharmacological relevance

The leaves of Sapium sebiferum have long been used in Traditional Chinese Medicine (TCM) for the treatment of eczema, shingles, edema, swelling, ascites, scabs, and snakebites, among other maladies.

Aim of this study

The present study aimed to investigate the antioxidant and anti-inflammatory effects of the phenolic extracts of Sapium sebiferum leaves using in vitro and in vivo models.

Materials and methods

The in vitro antioxidant activities of the extracts were measured using common chemical methods (total phenolic content; total flavonoid content; scavenging of DPPH·, ABTS+·, superoxide, and nitrite radicals; reducing power; β-carotene bleaching; and FTC assays). The in vivo topical anti-inflammatory activities were tested using the 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced dermatitis animal model. The SOD and CAT activities and the GSH content of ear tissue were also determined using test kits.

Results

The extracts of Sapium sebiferum leaves exhibited strong in vitro antioxidant activities. They also showed significant (P<0.001) and dose-dependent anti-inflammatory activities in an acute dermatitis model at the doses of 0.03 mg/ear, 0.1 mg/ear, and 0.3 mg/ear. The application of Sapium sebiferum leaf extracts increased the SOD and CAT activities and the GSH content relative to those of the TPA treatment group. The anti-inflammatory effect of the Sapium sebiferum leaf extract was positively correlated with its antioxidant activity.

Conclusion

These results demonstrate that Sapium sebiferum leaf extract is an effective anti-inflammatory agent in the TPA-induced dermatitis model, and its anti-inflammatory effect is related, at least in part, to its antioxidant activity.     

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.     

In vivo anti-inflammatory and wound healing activities of Centaurea iberica Trev. ex Spreng

Aim of the study

Several Centaurea species (Asteraceae) are used in Turkish folk medicine to alleviate pain and inflammatory symptoms in rheumatoid arthritis, high fever, head ache and for wound healing. Particularly, the aerial part of Centaurea iberica Trev. ex Spreng. has been practiced on wounds for healing. In order to evaluate the anti-inflammatory and wound healing activities of the plant, extracts were prepared with variety of solvents: hexane, chloroform, ethyl acetate and aqueous methanol (85%) from the aerial parts of Centaurea iberica.

Materials and methods

The incision by using tensiometer and excision models were used in order to assess the effect of the plant extracts on wound healing in mice and rats. Results were also evaluated histopathologically. In vivo inhibitory effect of the extracts on acetic acid-induced increase in capillary permeability was studied for the assessment of anti-inflammatory activity.

Results

The wound healing effect was comparatively evaluated with a reference ointment Madecassol^®. Noteworthy wound healing activity was observed for the ointment formulation prepared with 1% methanol extract. The results of histopathological evaluation supported the outcome of both incision and excision wound models. Moreover, the methanol extract exerted remarkable wound healing activity and also demonstrated a significant and dose-dependent anti-inflammatory activity.

Conclusion

The experimental study revealed that Centaurea iberica displays remarkable wound healing and anti-inflammatory activity.     

Anti-inflammatory and antinociceptive activities of the ethanolic extract of Bougainvillea xbuttiana

Ethnopharmacological relevance

Bougainvillea xbuttiana is widely distributed in Mexico and it is used as an analgesic in folk medicine.

Aim of the study

In the present study the in vivo antinociceptive and anti-inflammatory effects of the Bougainvillea xbuttiana ethanolic extract have been studied in mice.

Materials and methods

The phytochemical analysis was performed. Antinociceptive activity was evaluated through writhing and formalin test in mice. The anti-inflammatory activity was determined with the carrageenan-induced mice paw oedema model. IL-6, IL-10 and IFN-γ levels were determined by enzyme-like immunosorbent assay, whereas TNF and nitrite levels were detected by standard assay with L929 cells and colorimetric Griess reactive, respectively.

Results

The results showed that the ethanolic extract of the Bougainvillea xbuttiana has significant anti-inflammatory and antinociceptive activities, by inhibition of nociception induced by acetic acid and paw oedema. This extract also induced a decrease in TNF levels and an increase of IL-6, IFN-γ and NO levels that we observed up to 2 h. The highest levels of IL-10 were observed up to 4 h. The ratios of pro-/anti-inflammatory cytokines in sera from mice injected with the ethanolic extract, may be manifesting an anti-inflammatory status.

Conclusions

The present study provides convincing evidences that Bougainvillea xbuttiana extract possesses significant anti-nociceptive and anti-inflammatory effects.     

Antinociceptive and anti-inflammatory activities of Bowdichia virgilioides (sucupira)

Ethnopharmacological relevance

Bowdichia virgilioides Kunth (Leguminosae Papilonoideae) is a plant with anti-inflammatory activity used in folk medicine. The importance of this plant promoted its inclusion in Brazilian Pharmacopoeia.

Aim of the study

In order to evaluate the actions of this plant, studies were performed on antinociceptive and anti-inflammatory activities.

Materials and methods

The aqueous extracts (AE) of Bowdichia virgilioides inner bark and leaves were used at 100, 200, and 400 mg/kg. Antinociceptive activity of plant extract was evaluated by writhing, hot-plate and formalin tests. Anti-inflammatory activity was evaluated using paw oedema and peritonitis methods.

Results

Oral treatment with the AE of inner bark or leaves elicited inhibitory activity (P < 0.01) on acetic acid effect at 200 and 400 mg/kg, and reduced the formalin effect at the second-phase (200 and 400 mg/kg, P < 0.01), however it did not elicit any inhibitory effect on hot-plate test. The indomethacin inhibited the acetic acid-induced writhing and the formalin effect at the second-phase (P < 0.001), and the morphine reduced the both phases of formalin test (P < 0.001). Carrageenan-induced oedema formation and neutrophil migration into the peritoneal cavity were reduced with the AE of inner bark or leaves at 100, 200, and 400 mg/kg (P < 0.05), and by the reference compounds aspirin (P < 0.001) and dexamethasone (P < 0.001), respectively.

Conclusions

The AE of Bowdichia virgilioides shows antinociceptive and anti-inflammatory activities, supporting the folkloric usage of the plant to treat various inflammatory diseases.     

In vivo anti-inflammatory activities of Ocimum suave in mice

Ethnopharmacological relevance

Ocimum suave has been used in the Ethiopian traditional medicine to relieve pain, fever, inflammation and other disease conditions.

Aim of the study

The aim of the present study was to investigate the anti-inflammatory activities of the aqueous and ethanol leaf extracts and some fractions of Ocimum suave in mice.

Materials and methods

The crude extracts were screened for their anti-inflammatory activities on carrageenan-induced mouse paw edema at three dose levels. The butanol and aqueous fractions of the aqueous extract were also evaluated for their anti-inflammatory activities using carrageenan, histamine and serotonin-induced mouse paw edema at three dose levels. Normal saline and aspirin were employed as negative and positive control groups, respectively.

Results

Both ethanol and aqueous extracts significantly decreased carrageenan-induced inflammation at all the three doses used. However, greater paw edema inhibition was observed with the aqueous extract. The two fractions also showed significant reduction of inflammation against inflammatory models in which the aqueous residue exhibited the highest inhibition.

Conclusions

From the present findings, it can be concluded that the ethanol and aqueous leaf extracts as well as butanol and aqueous fractions of Ocimum suave have shown anti-inflammatory properties.     

Anti-inflammatory,wound healing and in-vivo antioxidant properties of the leaves of Ficus amplissima Smith

Ethno pharmacological relevance

Ficus amplissima, commonly known as kal-itchchi, being used in folklore medicine, leaves juice is applied externally on old chronic wounds and the latex is applied on the wound.

Aim

There was no scientific evidence justifying the medicinal use of Ficus amplissima, therefore the present study was aimed at evaluation of anti-inflammatory, wound healing and in-vivo antioxidant activity of the plant.

Materials and methods

In the present study the acetone extract of Ficus amplissima leaves were studied for enzymatic antioxidant activity through different assays, anti-inflammatory by using carrageenan and histamine induced rat paw edema models (50 mg, 100 mg acetone extract) and wound healing activity by incorporating the two doses (1% (w/w) and 2% (w/w)) of acetone extract and simple ointment base B.P. in concentration of 0.5% (w/w) using excision and incision wound models in rats. In case of the excision wound model wound contraction and period of epithelization was studied while incision wound model was evaluated by determining tensile strength.

Results

Ficus amplissima leaves expressed the potent anti-inflammatory and in-vivo antioxidant activity where 100 mg acetone extract showed high activity. Treatment of wound with ointment containing 2% (w/w) acetone extract exhibited significant (P<0.001) wound healing activity.

Conclusion

The acetone extract of Ficus amplissima leaves exhibited better anti-inflammatory, wound healing and in-vivo antioxidant activity probably due to phenols constituents.     

Effects of leaf extracts from Croton zambesicus Müell. Arg. on hemostasis

Ethnopharmacological relevance

The leaf decoction of Croton zambesicus Müell. Arg. (Euphorbiaceae; syn. Croton amabilis Müell. Arg., Croton gratissimus Burch) is traditionally used in Benin to treat hypertension.

Aim of the study

As hypertension and thromboembolism are often associated in several cardiovascular diseases, we studied the potential effects of leaf extracts from Croton zambesicus on hemostasis.

Materials and methods

We prepared the dichloromethane and aqueous extracts from the air-dried leaves of Croton zambesicus and separated the aqueous extract in its aqueous and dichloromethane fractions. The potential effects of these four extracts/fractions were investigated on red blood cells integrity using spectrophotometric lysis assays, on primary hemostasis using platelet aggregation studies and on secondary hemostasis using calibrated automated thrombin generation assays and coagulation factors inhibition tests.

Results

In the in vitro testing, we found that none of the tested extracts/fractions exhibit hemolytic or antiplatelet activity. However, they display a moderate but significant anticoagulant activity which would be mediated through the direct inhibition of thrombin, FXa and TF/FVIIa. The active anticoagulant compound(s) seem to be mainly in the aqueous extract and especially in its aqueous fraction.

Conclusions

This experimental work reported for the first time the anticoagulant effect of leaf extracts from Croton zambesicus. These findings are of particular interest as the leaves from Croton zambesicus are commonly used in infusion by local population and may provide a new natural source for the development of original anticoagulant agents. Furthermore, this activity, associated with the vasorelaxant properties of some of its diterpenes may prove to be interesting for the prevention of cardiovascular diseases in traditional medicine.     

Gastroprotective activity of Cenostigma macrophyllum Tul. var. acuminata Teles Freire leaves on experimental ulcer models

Ethnopharmacological relevance

Cenostigma macrophyllum Tul. var. acuminata Teles Freire (Leguminosae-Caesalpinioideae), popularly known in Brazil as “caneleiro”, is widely used in folk medicine against gastrointestinal diseases. In previous studies, the ethanol extract of leaves from Cenostigma macrophyllum Tul. var. acuminata Teles Freire had shown antinociceptive, anti-inflammatory, antibacterial, antioxidant and antiulcerogenic activities.

Aim of the study

The aim of this study was to assess the gastroprotective effect of the hydroalcoholic fraction of leaves of Cenostigma macrophyllum Tul. var. acuminata Teles Freire (Cm-FHA), as well as to elucidate the possible underlying mechanisms of action.

Materials and methods

Mice were used for the evaluation of the acute toxicity, and mice and rats to study the gastroprotective activity. The potential gastroprotective of Cm-FHA was assessed on different gastric ulcer models in rodents, such as absolute ethanol, HCl/ethanol, ischemia-reperfusion, cold restraint stress and indomethacin. The participation of prostaglandins, NO-synthase pathway and ATP-sensitive potassium channels (K_ATP) in gastroprotective activity of Cm-FHA were evaluated after treatment with a cyclooxygenase inhibitor (indomethacin), a NO-synthase inhibitor (L-NAME) and a K_ATP channel blocker (glibenclamide 5 mg/kg), respectively. Likewise, the catalase activity was determinated in order to assess the possible participation of antioxidant mechanisms.

Results

No signs of acute toxicity was observed after oral acute administration of Cm-FHA, considering the analyzed parameters. Likewise, Cm-FHA promoted a protective effect against gastric ulcers induced by absolute ethanol (lesion inhibition by 40% at both 100 and 200 mg/kg), HCl/ethanol (lesion inhibition by 50 or 48% at 100 or 200 mg/kg, respectively), ischemia-reperfusion (lesion inhibition by 49 or 90% at 100 or 200 mg/kg, respectively) and cold restraint stress (lesion inhibition by 63 or 76% at 100 or 200 mg/kg, respectively), as well as a increase of catalase activity was observed. Otherwise, Cm-FHA was not able to protect gastric mucosa against indomethacin-induced lesions. Nitric oxide release, the of K_ATP channels opening and antioxidant activity are the possibly involved in the Cm-FHA-induced gastroprotective activity.

Conclusion

This study corroborates the folk medicine use of Cenostigma macrophyllum for treatment of gastric ulcers, as well as reinforces this species as a valuable source of promising natural drugs with gastroprotective activity.     

Evaluation of the antinociceptive and anti-inflammatory effect of Caralluma dalzielii

Ethnopharmacological relevance

Caralluma dalzielii has been used for treating several ailments including convulsion, leprosy, snake bites, otitis (ear pain), fungal diseases and rheumatoid arthritis in Northern Nigeria. However there is no scientific evidence to support its use in literature. To evaluate the antinociceptive and anti-inflammatory properties of the aqueous extract of Caralluma dalzielii in animal models.

Materials and methods

The antinociceptive and anti-inflammatory properties were assessed using acetic acid induced writhing test in mice, sub plantar formalin induced nociception, the tail-flick test and formalin induced oedema in rats. Three doses of the extract (25, 50, 100 mg/kg) were used for the assessment.

Results

Caralluma dalzielii extract demonstrated strong dose-dependent antinociceptive and anti-inflammatory activities in all the models employed. All doses (25, 50, 100 mg/kg) produced a significant percentage inhibition (41.77, 77.11, and 90.76% in the early phase and 52.02, 85.35, 93.93% in the late phase) in the acetic acid writhing test and (42.85, 55.71, 86.43% in the early phase and 23.26, 37.98, 72.87 in the late phase) in the formalin induced nociception test, respectively. The tail-flick test showed a significant increase in the antinociceptive effect of the extract in both early and late phases when compared with the control. The inhibition of oedema in the formalin test was significant when compared to the control.

Conclusion

The results indicated that Caralluma dalzielii showed excellent antinociceptive and anti-inflammatory properties suggesting that its traditional use in the treatment of pains and inflammatory diseases may be valid.