Conservation strategy for Pelargonium sidoides DC: Phenolic profile and pharmacological activity of acclimatized plants derived from tissue culture

Ethnopharmacological relevance

Pelargonium sidoides DC (Geraniaceae), a popular medicinal plant used in folk medicine in the treatment of respiratory-related infections has gained international prominence due to its usage in several herbal formulations. This has led to high demand and the subsequent decimation of wild populations.

Aim of the study

Using plant tissue culture techniques, Pelargonium sidoides plants were cloned in vitro, acclimatized under greenhouse conditions and evaluated for their phytochemical content and pharmacological activity.

Methods

Phenolic content in extracts of in vitro-derived, greenhouse-acclimatized and wild Pelargonium sidoides plants were analyzed using UPLC-MS/MS. The oxygen radical absorbance capacity (ORAC), 2,2-diphenyl-1-picryl hydrazyl (DPPH) radical scavenging activity and minimum inhibitory concentration (MIC) of the extracts against bacterial and fungal strains were evaluated.

Results

Similarities in phenolic profiles were identified confirming the chemical signatures that characterize Pelargonium sidoides plants. Extracts of greenhouse-acclimatized and wild plants exhibited comparable antimicrobial and antioxidant properties.

Conclusions

Overall, the study highlights the potential of integrating plant tissue culture technologies in conservation strategies of medicinal plants. In particular, the results strongly suggest the feasibility of both large-scale cultivation and plant part substitution as alternative solutions to the current destructive overharvesting practices of wild Pelargonium sidoides populations.     

A historical, scientific and commercial perspective on the medicinal use of Pelargonium sidoides (Geraniaceae)

Ethnopharmacological context

A detailed review of the ethnobotany and commercial history of Pelargonium sidoides is presented, together with a brief summary of pre-clinical and clinical scientific results that support the use of the plant in modern, evidence-based phytomedicines. The aim is to identify the main factors responsible for the success in product development.

Materials and methods

The literature studied includes all modern scientific papers and also old documents and books that are no longer readily accessible.

Results

Available ethnobotanical information shows that several tuberous Pelargonium species (including Pelargonium sidoides) are important traditional medicines with a rich ethnobotanical history. A summary of the interesting history of the commercial development of Stevens’ Cure or Umckaloabo in Europe is presented. Scientific evidence for the efficacy of the product, mainly as a treatment for acute bronchitis, is reviewed. These include numerous in vitro studies as well as 18 clinical studies. The botanical identity of the plant and its complex mixture of coumarins and other chemical constituents are summarised.

Conclusions

The use of Pelargonium stems or tubers for a variety of ailments (including the complications of dysentery) is an important but hitherto under-estimated part of traditional medicine in southern Africa. Key elements in the successful development of Pelargonium sidoides from a profound traditional remedy to a highly successful phytomedicine include the choice of species, a favourable cost–benefit ratio, innovative marketing over many years, good scientific evidence of the botanical and chemical identity of the product and convincing proof of concept.     

Antibacterial activity of Helleborus bocconei Ten. subsp. siculus root extracts

Aim of the study

Roots of Helleborus bocconei Ten. subsp. siculus (Schiffner) Merxm. & Podl. are widely used in veterinary folk medicine in Sicily (Italy) to diagnose and cure lower respiratory tract infections in cattle. This study intended to evaluate the in vitro antibacterial activity of the methanolic root extract of Helleborus bocconei Ten. subsp. siculus, and of the bufadienolide and ecdysteroid fractions extracted from its roots, against strains belonging to species commonly associated with respiratory tract infections.

Materials and methods

The phytochemical screening of the previously prepared plant extracts was carried out by chemical, thin-layer chromatography and spectroscopic methods. The in vitro antibacterial activity of the extracts against seven different standard bacterial strains was evaluated by broth microdilution.

Results

According to the present study, Helleborus bocconei Ten. subsp. siculus roots contain bufadienolides and ecdysteroids, and the extracts containing these compounds, as well as the crude methanolic root extract, show antibacterial activity against microorganisms responsible for respiratory infections. In particular, the bufadienolide extract has the highest inhibitory activity against all the tested organisms, and, as the other extracts, shows the lowest MIC values (100 μg/ml) against Moraxella catarrhalis and Streptococcus pneumoniae.

Conclusions

Since the roots of Helleborus bocconei Ten. subsp. siculus contain substances with antibacterial activity, the traditional use of this plant may also derive from its antibacterial properties.     

Evaluation of an aqueous-ethanolic extract from Pelargonium sidoides (EPs® 7630) for its activity against group A-streptococci adhesion to human HEp-2 epithelial cells

Aim of the study

The root extract of Pelargonium sidoides DC (Geraniaceae), EPs^® 7630, is currently used to treat respiratory tract infections. The therapeutic benefits are largely related to the modulation of the non-specific immune system. The present study was designed to investigate the anti-adhesive activity of this herbal medicine with Streptococcus pyogenes as model microorganism and to identify the underlying biologically active principle.

Materials and methods

Adherence of fluorescent-labelled group A-streptococci (GAS) to human epithelial (HEp-2) cells was assessed by flow cytometry. Anti-adhesive properties of the parent extract as well as a methanol-soluble (MSF) and a methanol-insoluble fraction (MIF) derived thereof were examined. Treatment with skin powder produced polyphenol-free samples which were included for comparison. Anti-adherence studies were extended to a series of highly purified proanthocyanidins including homogenous epicatechin- and catechin-based polyflavans, a ‘mixed’ procyanidin sample, an A-type proanthocyanidin mixture as well as a prodelphinidin test substance.

Results

After pre-treatment of GAS with EPs^® 7630 or its subfractions MIF and MSF at concentrations of 30 μg/ml, adhesion of the pathogen to HEp-2 cells was inhibited by ca. 45%, ca. 35% and ca. 30%, respectively. However, following preincubation of cells with the extract and the fractions no effect was observed. This finding indicates that the anti-adhesive effects are due to interactions with binding factors on the bacterial surface. Since polyphenol-free samples proved to be inactive, proanthocyanidins appear to represent the anti-adhesive principle. Comparative studies with chemically defined proanthocyanidins revealed that the prodelphinidin nature, i.e. the pyrogallol B-ring elements of constituent flavanyl units, represented an important structural feature of the anti-adhesive potential of this herbal medicine.

Conclusions

The current data provide strong evidence for a potent anti-adhesion principle of the Pelargonium sidoides root extract related to specific proanthocyanidins. This finding suggests an interaction with bacterial binding sites in a specific rather than non-specific manner. However, the blocked adhesion molecules remain to be identified. The anti-adhesive mechanism may well contribute to the anti-infective activity of EPs^® 7630 at an early time point of a bacterial infection.     

Antidiarrhoeal activity of Geranium incanum Burm. f. (Geraniaceae) leaf aqueous extract in mice

Ethnopharmacological relevance

Geranium incanum Burm. f. (Geraniaceae) is used in South Africa especially in rural communities by traditional medicine practitioners to treat diarrhoea. However, scientific evidence does not exist in any literature to corroborate the claim of therapeutic success of the plant species in diarrhoea.

Aim of study

The study intended to investigate the antidiarrhoeal activity of the leaf aqueous extract of Geranium incanum in mice.

Materials and Methods

Castor oil induced diarrhoeal test was used to assess the antidiarrhoeal activity of Geranium incanum. Gastrointestinal tract transit of charcoal meal test was used to assess the antipropulsive activity of the plant extract while the acute toxicity study and phytochemical analysis were carried out using well established protocols and methods.

Results

The antidiarrhoeal activity of Geranium incanum was investigated by studying the effect of leaf aqueous extract of the plant species on castor oil-induced diarrhoea in mice. The leaf aqueous extract of Geranium incanum significantly reduced faecal output in castor oil -induced diarrhoea and also significantly reduced the number of diarrhoeal episodes. Geranium incanum significantly delayed the onset of diarrhoea induced by castor oil and significantly reduced the number of animals exhibiting diarrhoea. Loperamide, a standard antidiarrhoeal drug, produced similar effects to the leaf aqueous extract of Geranium incanum on castor oil-induced diarrhoea. Both Geranium incanum and loperamide significantly reduced the intestinal propulsion of charcoal meal in mice. The phytochemical analysis of the leaves revealed the presence of tannins, saponins particularly steroidal saponin, and flavonoids. The LD₅₀ of the plant species obtained was greater than 4000 mg/kg (p.o.).

Conclusion

The data obtained indicate that the leaf aqueous extract of Geranium incanum has both antidiarrhoeal and antipropulsive activities The data also show that the plant material given orally may be safe and/or non toxic in mice. However, further investigation on the acute toxicity and on the mechanism of the antidiarrhoeal effect of the plant species needs to be carried out.     

Serviceberry [Amelanchier alnifolia (Nutt.) Nutt. ex. M. Roem (Rosaceae)] leaf extract inhibits mammalian α-glucosidase activity and suppresses postprandial glycemic response in a mouse model of diet-induced obesity and hyperglycemia

Ethnopharmacological relevance

The use of medicinal plants for the treatment of diseases usually comes from the belief that they present low toxicity due their natural origin. However, it is necessary a toxicological and pharmacological evaluation for these plants. Tropaeolum majus is a medicinal plant used in popular medicine to treat several diseases, including cardiovascular disorders, urinary tract infections and asthma. Even though several studies proved its therapeutic effects, there are few toxicological studies with this species.

Aim of the study

The present study was carried out to evaluate the subchronic toxicity of the hydroethanolic extract obtained from leaves of T. majus (HETM) in Wistar rats.

Material and methods

Male and female Wistar rats received three doses of HETM (75, 375 and 750 mg/kg) for 28 days. After the treatments biochemical, hematological and histopathological parameters were analyzed.

Results

No significant alterations in the animal's body weight gain, relative organs weight, serum biochemical analysis, hematological or histopathological analyses of liver, kidneys and spleen were observed.

Conclusions

These results demonstrate the absence of subchronic toxicity due to oral treatment with HETM for 28 days in Wistar rats. However, other toxicological studies are necessary to evaluate the total safety of this plant.     

Water extract of Cinnamomum cassia Blume inhibited human respiratory syncytial virus by preventing viral attachment,internalization, and syncytium formation

Ethnopharmacological relevance

Cinnamomum cassia Blume is a popular traditional Chinese herbal medicine that has been used to manage respiratory tract disease, including common cold and chronic bronchitis for thousand years. Human respiratory syncytial virus (HRSV) is one of the leading causes of severe lower respiratory tract illness worldwide. No effective therapeutic modality against HRSV infection has been proved. It is unknown whether Cinnamomum cassia is effective against HRSV.

Aim of the study

This study tested the hypothesis that Cinnamomum cassia can effectively decrease HRSV-induced plaque formation and syncytium formation in respiratory mucosal cell lines.

Materials and methods

Antiviral activity of the hot water extract of Cinnamomum cassia against HRSV was tested by plaque reduction assay in both human upper (HEp-2) and low (A549) respiratory tract cell lines. Its ability to inhibit the synthesis of viral fusion (F) protein was examined by Western blot assay.

Results

Cinnamomum cassia dose-dependently inhibited HRSV-induced plaque formation in both HEp-2 and A549 cell lines (p<0.0001). Cinnamomum cassia was more effective when given before viral infection (p<0.0001) mainly by inhibition of viral attachment (p<0.0001) and internalization (p<0.0001). Cinnamomum cassia could inhibit F protein production and syncytium formation to interfere with HRSV spreading.

Conclusions

Cinnamomum cassia prevented airway epithelia from HRSV infection through inhibiting viral attachment, internalization and syncytium formation. Cinnamomum cassia could be a candidate to develop therapeutic modalities to manage HRSV infection in the future.     

Assessment of the genotoxic and mutagenic properties of Himatanthus articulatus bark extracts used as phytotherapeutic drug in the Amazon

Ethnopharmacological relevance

Himatanthus articulatus (Apocynaceae) is a plant native to the Amazon, popularly used to treat external ulcers, tumors, inflammations, cancer, syphilis and malaria.

Aim of the study

To investigate the in vivo genotoxic and mutagenic potential of this plant, using the comet assay and the micronucleus test.

Material and methods

Female and male adult mice were treated with 500 mg/kg, 1000 mg/kg or 2000 mg/kg of Himatanthus articulatus aqueous or ethanolic bark extracts by gavage for two consecutive days. In addition, blood slides were exposed to hydrogen peroxide (ex vivo) to evaluate the anticlastogenic effect using the comet assay. The HPLC analyses indicated plumieride as the main constituent of both extracts from Himatanthus articulatus barks.

Results

No differences between genders were observed. Micronuclei were observed only in the group treated with the highest dose of both extracts. Conversely, lower doses of these extracts showed protective effects to DNA against damage induced by hydrogen peroxide, indicating an important antigenotoxic effect.

Conclusions

The toxicological evaluation indicated that the extracts are non-genotoxic and reduce the clastogenic damage induced by hydrogen peroxide. In part, this result can be atributted to the phytochemical profile of Himatanthus articulatus, which presents iridoids and phenolic compounds.     

Anti-inflammatory and phytochemical properties of twelve medicinal plants used for treating gastro-intestinal ailments in South Africa

Ethnopharmacological relevance

The investigated medicinal plants are commonly used for the treatment of pains and cramps related to gastro-intestinal tract infections in South African traditional medicine.

Aims of the study

This study aimed to evaluate the ability of the plant extracts to inhibit cyclooxygenase enzymes. Phytochemical analysis was also carried out in the quest to determine some plant metabolites that may be responsible for the observed anti-inflammatory activity.

Materials and methods

The cyclooxygenase assay was used to test for the anti-inflammatory activity of the plant extracts using cyclooxygenase-1 and -2 (COX-1 and COX-2) enzymes. Total phenolic compounds including condensed tannins, gallotannins and flavonoids were quantitatively determined using spectrophotometric methods. Qualitative tests for alkaloids and saponins were also carried out.

Results

Most of the plant extracts evaluated showed dose dependent activity against COX-1 and/or COX-2 enzymes. Agapanthus campanulatus root dichloromethane extract showed the highest COX-2 inhibitory activity (83.7%) at 62.5 μg/ml. The presence and/or amounts of phenolics, condensed tannins, gallotannins, flavonoids, alkaloids and saponins varied with plant parts and species.

Conclusion

The results support the use of the investigated plant in treating pain and cramp related to gastro-intestinal tract infections. To some extent, the observed anti-inflammatory activity could be attributed to the various plant secondary metabolites detected in the plant materials.     

Drosera rotundifolia and Drosera tokaiensis suppress the activation of HMC-1 human mast cells

Ethnopharmacological relevance

Several Northern Hemisphere Drosera species have been used in the therapy of respiratory tract infections as the traditional medicine Droserae Herba.

Aim of the study

To determine the anti-inflammatory effects of Drosera species and to investigate a substitute material for Droserae Herba, we examined the effect of extracts of Drosera rotundifolia, Drosera tokaiensis and Drosera spatulata on activated T cell membrane (aTc-m)-induced inflammatory gene expression in HMC-1 human mast cells.

Materials and methods

Drosera rotundifolia, Drosera spatulata and Drosera tokaiensis were collected in Japan. Herbs were extracted with 80% EtOH, and subsequently applied to OASIS HLB column. HMC-1 cells were treated with each Drosera column-adsorbed fraction for 15 min, and subsequently added to aTc-m and incubated for 16 h. Inflammatory gene and protein expressions were determined by DNA microarray, RT-PCR and Western blotting.

Results

Drosera rotundifolia and Drosera tokaiensis fractions, but not the Drosera spatulata fraction, suppressed inflammatory gene expression induced by aTc-m in HMC-1 cells.

Conclusions

Drosera rotundifolia and Drosera tokaiensis suppressed activation of HMC-1 cells induced by aTc-m. Since the Drosera tokaiensis fraction was more effective than the traditionally used Drosera rotundifolia, Drosera tokaiensis is a likely substitute as a source of Droserae Herba.     

A new protoberberine alkaloid from Meconopsis simplicifolia (D. Don) Walpers with potent antimalarial activity against a multidrug resistant Plasmodium falciparum strain

Ethnopharmacological relevance

The aerial components of Meconopsis simplicifolia (D. Don) Walpers are indicated in Bhutanese traditional medicine for treating malaria, coughs and colds, and the infections of the liver, lung and blood. This study is to validate the ethnopharmacological uses of this plant and also identify potent antimalarial drug leads through bioassays of its crude extracts and phytochemical constituents.

Materials and methods

Meconopsis simplicifolia (D. Don) Walpers was collected from Bhutan and its crude MeOH extract was subjected to acid-base fractionation. Through repeated extractions, separations and spectroscopic analysis, the alkaloids obtained were identified and tested for their antimalarial and cytotoxicity activities.

Results

Phytochemical studies resulted in the isolation of one new protoberberine type alkaloid which we named as simplicifolianine and five known alkaloids: protopine, norsanguinarine, dihydrosanguinarine, 6-methoxydihydrosanguinarine and oxysanguinarine. Among the five of the alkaloids tested, simplicifolianine showed the most potent antiplasmodial activities against the Plasmodium falciparum strains, TM4/8.2 (chloroquine–antifolate sensitive strain) and K1CB1 (multidrug resistant strain) with IC₅₀ values of 0.78 μg/mL and 1.29 μg/mL, respectively. The compounds tested did not show any significant cytotoxicity activities against human oral carcinoma KB cells and normal Vero cells of African kidney epithelial cells.

Conclusions

This study validated the traditional uses of the plant for the treatment of malaria and identified a new alkaloid, simplicifolianine as a potential antimalarial drug lead.     

Antimalarial alkaloids from a Bhutanese traditional medicinal plant Corydalis dubia

Ethnopharmacological relevance

Corydalis dubia is used in Bhutanese traditional medicine as a febrifuge and for treating infections in the blood, liver and bile which correlate to the signs and symptoms of malarial and microbial infections.

Aim of the study

To validate the ethnopharmacological uses of the plant and to discover potential new therapeutic drug leads.

Materials and methods

C. dubia was collected from Bhutan and the alkaloids were obtained using acid–base fractionation and separation by repeated column and preparative plate chromatography. The alkaloids were identified from analysis of their physiochemical and spectroscopic data and were tested for antiplasmodial, antimicrobial and cytotoxicity activities.

Results

A systematic extraction and isolation protocol yielded one new natural product, dubiamine, and seven known isoquinoline alkaloids, scoulerine, cheilanthifoline, protopine, capnoidine, bicuculline, corydecumbine and hydrastine. Among the four alkaloids tested, scoulerine showed the best antiplasmodial activity with IC₅₀ values of 5.4 μM and 3.1 μM against the antifolate sensitive and the multidrug resistant P. falciparum strains: TM4/8.2 and K1CB1, respectively. None of the alkaloids tested showed significant antimicrobial or cytotoxicity activities.

Conclusions

The antiplasmodial test results, of the isolated alkaloid components, are commensurated with the ethnopharmacological uses of this plant.     

In vivo analgesic activity,toxicity and phytochemical screening of the hydroalcoholic extract from the leaves of Psidium cattleianum Sabine

Ethnopharmacological relevance

Psidium cattleianum Sabine is extensively used in Brazilian traditional medicine to treat several diseases including painful disorders. Aim of the study to investigate the toxicity and the possible analgesic activities of the hydroalcoholic extract from the leaves of Psidium cattleianum Sabine (ELPCS), to support its use in folk medicine. To screen the major phytochemical constituents of this extract and evaluate their antioxidant activity.

Materials and methods

ELPCS was assessed for its antioxidant activity using the DPPH model. Its analgesic activity was examined using mouse models of acetic acid-induced writhing and hot plate paw licking models. The major phytochemical constituents of the extract were screened; their toxicity on LLC-MK2 mammalian cells was evaluated.

Results

ELPCS exhibited significant peripheral analgesic activity at doses of 60, 80, 100, 200 and 400 mg/kg in mice, but it did not display central analgesic activity and not was toxic to LLC-MK2 cell (LD₅₀>400 µg/mL). The extract exhibited free radical scavenging activity as evidenced by IC₅₀ values (15.9 µg/mL) obtained by the DPPH method. Phytochemical screening detected flavonoids, saponins, cardiac glycosides, anthraquinones, and tannins.

Conclusions

The results of the experimental studies proved the analgesic activity of ELPCS and supported the traditional use of this plant.     

Zataria multiflora Boiss. (Shirazi thyme)—An ancient condiment with modern pharmaceutical uses

Ethnopharmacological relevance

Zataria multiflora Boiss. (ZM) is a thyme-like plant belonging to the Lamiaceae family that grows wild only in Iran, Pakistan and Afghanistan. This plant with the vernacular name of Avishan-e-Shirazi (Shirazi thyme) in Iran is a valuable medicinal and condimental plant. It has several traditional uses as an antiseptic, carminative, stimulant, diaphoretic, diuretic, anesthetic, anti-spasmodic and analgesic.

Aim of the study

This paper reviews the ethnopharmacology, pharmacology, toxicology, modern pharmaceutical uses and phytochemistry of Zataria multiflora, and highlights the gaps in our knowledge deserving further research.

Materials and methods

All relevant databases were searched for the terms “Zataria”, “Zataria multiflora”, “Shirazi thyme” and “Iranian thyme” without limitation up to 24th October 2012. Information on Zataria multiflora was collected via electronic search using Pubmed, Scopus, Web of Science and SID (for articles in Persian language), and local books on ethnopharmacology.

Results

ZM has played an important role in Iranian traditional medicine. In light of the modern pharmacological and clinical investigations, ZM is a valuable medicinal and condimental plant that has anti-microbial, antioxidative, anti-inflammatory, spasmolytic and anti-nociceptive properties. The oil of ZM contains high percentages of oxygenated monoterpenes, in particular thymol and carvacrol, and exhibits excellent anti-microbial properties.

Conclusions

Overall, antimicrobial property appears to be the most interesting studied biological effect of ZM. The lack of a comprehensive phytochemical analysis of ZM is an important limitation that can be noted regarding most of the previous studies.     

Validation of use of a traditional remedy from Bridelia grandis (Pierre ex Hutch) stem bark against oral Streptococci

Aim of the study

Bridelia grandis (Pierre ex Hutch) (Euphorbiaceae) is a medicinal plant traditionally used in Cameroon by pygmies Baka as a remedy for oral cavity affection. Bioassay-guided stem bark extracts were investigated for their in vitro antimicrobial properties as well as their phytochemical constituents.

Materials and methods

The first extraction was carried out according to the traditional use. Further extractions were carried out with solvents of different polarity such as methanol (MeOH), ethyl acetate (EtOAc) and mixtures of MeOH–H₂O. The antimicrobial activity of the extracts against oral Streptococci was evaluated on the basis of the minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) by the macrodilution method; the bacterial surface hydrophobicity was also evaluated.

Results

Water, methanol and mixtures methanol–water extracts, exhibited antibacterial activity with MIC between 0.5 and 2 mg/ml justifying the traditional use of Bridelia grandis stem bark for oral cavity affection. Preliminary phytochemical analysis was performed on the most active extract (methanol) using appropriate tests and well established analytical screening methods, such as TLC and RP-HPLC/DAD.

Conclusions

The data obtained indicate that tannins constitute the chemical family responsible for the biological activity.     

Hepatoprotective studies on Sida acuta Burm. f.

Ethnopharmacological relevance

Sida acuta Burm. f. (Malvaceae) is used in Indian traditional medicine to treat liver disorders and is useful in treating nervous and urinary diseases and also disorders of the blood and bile.

Aim of the study

Evaluation of the hepatoprotective properties of the methanolic extract of the root of Sida acuta (SA) and the phytochemical analysis of SA.

Materials and methods

The model of paracetamol-induced hepatotoxicity in Wistar rats, liver histopathological observations, hexobarbitone-induced narcosis and in vitro anti-lipid peroxidation studies were employed to assess the hepatoprotective efficacy of SA. Phytochemical assay of SA was conducted following standard protocols.

Results

Significant hepatoprotective effects were obtained against liver damage induced by paracetamol overdose as evident from decreased serum levels of glutamate pyruvate transaminase, glutamate oxaloacetate transaminase, alkaline phosphatase and bilirubin in the SA treated groups (50, 100, 200 mg/kg) compared to the intoxicated controls. The hepatoprotective effect was further verified by histopathology of the liver. Pretreatment with Sida acuta extract significantly shortened the duration of hexobarbitone-induced narcosis in mice indicating its hepatoprotective potential. Phytochemical studies confirmed the presence of the phenolic compound, ferulic acid in the root of Sida acuta, which accounts for the significant hepatoprotective effects observed in the present study.

Conclusion

The present study thus provides a scientific rationale for the traditional use of this plant in the management of liver disorders.     

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.     

Antinociceptive activity of aqueous extract and isolated compounds of Lithrea molleoides

Ethnopharmacological relevance

Lithrea molleoides (Vell.) Engl. (Anacardiaceae) is a medicinal plant commonly used in traditional medicine in South America.

Aim of the study

In the present study, the in vivo antinociceptive effect of L. molleoides' aqueous extract and its isolated compounds has been investigated.

Materials and Methods

Antinociceptive activity was evaluated through writhing, formalin and hot plate tests in mice. The phytochemical analysis was performed.

Results

The extract produced significant inhibition on nociception induced by acetic acid (ED50: 8.7 mg/kg, i.p.) and formalin (ED50: 7.7 mg/kg, i.p.) administered intraperitoneally and also orally. Yohimbine diminished the activity of the extract in the acetic acid test meanwhile haloperidol enhanced its effect. Two majority compounds, shikimic and vanillic acid were active in chemical nociceptive models used in this work, producing the highest inhibition of the writhing response at a dose of 30 mg/kg i.p. (55.4% and 57.1%, respectively) meanwhile at 100 mg/kg p.o. produced a slight response (23.3% and 23.9%, respectively).

Conclusions

These results suggest that L. molleoides' aqueous extract produced antinociception possibly related to the presence of shikimic and vanillic acid. The adrenergic and dopaminergic systems seem to be involved in the mechanism of antinociception of the extract.     

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.