Anti-inflammatory intestinal activity of Arctium lappa L. (Asteraceae) in TNBS colitis model

Ethnopharmacological relevance

In Brazilian traditional medicine, Arctium lappa (Asteraceae), has been reported to relieve gastrointestinal symptoms.

Aim of the study

In the present study, we investigated the effects of the lactone sesquiterpene onopordopicrin enriched fraction (ONP fraction) from Arctium lappa in an experimental colitis model induced by 2,4,6 trinitrobenzene sulfonic acid and performed experiments to elucidate the underlying action mechanisms involved in that effect.

Materials and methods

ONP fraction (25 and 50 mg/kg/day) was orally administered 48, 24 and 1 h prior to the induction of colitis and 24 h after. The inflammatory response was assessed by gross appearance, myeloperoxidase (MPO) activity, tumor necrosis factor alpha (TNF-α) levels and a histological study of the lesions. We determined cyclooxygenase (COX)-1 and -2 protein expressions by western blotting and immunohistochemistry assays.

Results

TNBS group was characterized by increased colonic wall thickness, edema, diffuse inflammatory cell infiltration, increased MPO activity and TNF-α levels. On the contrary, ONP fraction (25 and 50 mg/kg) treatment significantly reduced the macroscopic inflammation scores (p<0.05 and p<0.01, respectively) and morphological alterations associated with an increase in the mucus secretion. Similarly, the degree of neutrophil infiltration and the cytokine levels were significantly ameliorated. Moreover, COX-2 expression was up regulated in TNBS-treated rats. In contrast, ONP fraction (50 mg/kg) administration reduced COX-2 overexpression.

Conclusions

We have shown that the ONP fraction obtained from Arctium lappa exert marked protective effects in acute experimental colitis, confirming and justifying, at least in part, the popular use of this plant to treat gastrointestinal diseases.     

On the potential of Tephrosia purpurea as anti-Helicobacter pylori agent

Aim of the study

Since Tephrosia purpurea (Linn.) Pers. (Fabaceae) has traditional use in curing different types of wounds including gastroduodenal ulcers, it was of interest to evaluate the in vitro anti-Helicobacter pylori activity profile of the plant extract and its fractions with a view to examining its therapeutic potential, if any.

Materials and methods

Employing clinical isolates and standard strains of Helicobacter pylori, the extract and fractions were bioevaluated in terms of MIC and MBC values, acid stability, time-kill kinetics, drug resistance, and synergistic potential.

Results

The methanolic extract showed promising activity against clinical isolates and standard strains of Helicobacter pylori, including metronidazole-resistant strains. Fractionation of the extract revealed the n-hexane and chloroform fractions to possess marked activity. The extract and the less polar fractions remained functionally active in acidic condition similar to stomach environment, exhibited consistent bacteriostatic activity during repeated exposure, and demonstrated synergism, complete or partial, even with antibiotic-resistant strains.

Conclusion

Apolar fractions of Tephrosia purpurea may have therapeutic potential in combating Helicobacter pylori mediated gastroduodenal disorders.     

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.     

HPLC测定藏药螃蟹甲中5个环烯醚萜苷的含量

目的:建立RP-HPLC同时测定藏药螃蟹甲中5种环烯醚萜苷的含量.方法:色谱柱为Symmetry C18(4.6mm×150mm,5μm),流动相为乙腈(A)-水(B)梯度洗脱,0～5min,7%A,5～10min,7%～12%A,10～40min,12%A;流速1.0ML·min-1;柱温20℃,检测波长235nm.结果:sesamoside,山栀苷甲酯,7,8-dehydropenstemoside,penstemoside和8-0-乙酰山栀苷甲酯分别在0.050～0.650(r=0.9993),0.050～0.350(r=0.9995),0.040～0.280(r=0.9994),0.010～0.070(r=0.9996),0.040～0.280(r=0.9997)g·L-1与峰面积线性关系良好;平均加样回收率均96%～104%,RSD均小于5.0%(n=6).结论:此方法简便、准确,重复性好,结果稳定,可作为螃蟹甲药材的质量控制方法.     

Cytotoxic effects of Echinacea purpurea flower extracts and cichoric acid on human colon cancer cells through induction of apoptosis

Ethnopharmacological relevance

Echinacea is a top-selling herbal supplement that acts as immunostimulant. It has been used to treat common cold, coughs, bronchitis and upper respiratory infections. It is also a popular product used in anticancer therapy. The cytotoxic effects of Echinacea on cancer cells are still not clear. The aims of this study were to provide a preliminary validation of the effects of 50% aqueous ethanol extract of Echinacea purpurea flowers and its major compound, cichoric acid, on human colon cancer cells Caco-2 and HCT-116.

Materials and methods

The cytotoxic effects of Echinace flower extracts and cichoric acid on cell viability, telomerase activity, DNA fragmentation, β-catenin, caspase-9, and cleavage of poly-ADP-ribose polymerase (PARP) of human colon cancer cell were examined.

Results

The results showed a significant inhibition of proliferation in E. purpurea flower extract and cichoric acid in a dose- and time-dependent manner. Cichoric acid treatment decreased telomerase activity in HCT-116 cells. Moreover, cichoric acid effectively induced apoptosis in colon cancer cells, which were characterized by DNA fragmentation, activation of caspase-9, cleavage of PARP and downregulation of β-catenin.

Conclusions

Our data indicate that cichoric acid has a strong growth-inhibitory effect against colon cancer cells, presumably resulting from the reduced telomerase activity and the induction of apoptosis. The exact mechanism of action should still be determined in future studies. Overall, the effects of 50% aqueous ethanol extract of E. purpurea flowers and cichoric acid may have provided in vitro evidence for the use as chemotherapeutic agents.     

In vitro estrogenic activity of Asplenium trichomanes L. extracts and isolated compounds

Ethnopharmacological relevance

Asplenium trichomanes was used as an expectorant, anti-cough remedy, laxative, emmenagogue, abortifacient and for irregular menses.

Aim of the study

To investigate the in vitro estrogenic activity of Asplenium trichomanes extracts and isolated compounds and their ability to activate ERα and ERβ.

Materials and methods

Leaves infusion (IF), decoction (DC) and methanol extract (ME) were prepared. MCF7/EREluc cell line which expresses endogenous ERα, and SK-NBE cells transiently transfected with the estrogen receptors (ERα and ERβ) were used for the estrogenic activity assays. Phytochemical investigations were performed (CC, HPLC, etc.) and structure of isolated compounds were achieved on the basis of 1D and 2D NMR techniques and HR-MS spectrometry.

Results

IF and ME were active in our MCF7 model; selectivity for the ERβ receptor was observed in the SK-NBE test. Two new phenol derivatives, 4-vinyl-phenol-1-O-[α-l-rhamno(1 → 6)-β-d-glucopyranosyde] (1) and kaempferol-3-O-α-[2′acetyl]-arabinofuranosyl-7-O-α-l-rhamnopyranoside (2) were isolated with six known compounds (3–8). Compounds 2–4, 7 and 8 showed selectivity for the activation of the ERβ receptor although with a moderate activity compared with 17-β-estradiol.

Conclusion

Further investigations about the estrogenic effects of this plant are needed but our data can, at least in part, explain some of its traditional use as emmeagogue.     

Chemical constituents and antibacterial property of the essential oil of the roots of Cyathocline purpurea

Ethnopharmacological relevance

Cyathocline purpurea (D. Don.) O. Ktze. (Asteraceae) is a rare existence Indian medicinal plant and traditionally has antimicrobial property.

Aim of the study

The aim of the present study was to identify chemical composition of the essential oil from the roots of Cyathocline purpurea and to screened in vitro antibacterial activity against eight human pathogenic bacteria.

Materials and methods

The essential oil of roots was analyzed by using GC–FID and GC–MS. The antibacterial activity of oil was tested against four Gram-positive and four Gram-negative bacteria and antibacterial activity was determined by the tube dilution method.

Results

The main constituents of the oil were thymohydroquinone dimethyl ether (57.4%) and β-selinene (14.0%), among twenty five identified compounds, which represented 90.1% of the total oil. The oil was found active against Gram-positive bacteria with minimal bactericidal concentration (MBC) values in the range of 0.26–0.57 mg/mL.

Conclusions

This is the first report on the chemical composition and antibacterial activity of the essential oil of roots of Cyathocline purpurea. The observation of MBC assay suggested that the Gram positive microorganisms were susceptible to essential oil, while oil was found to be resistant against Gram-negative bacteria, and the oil has bactericidal property.     

Alpha-amylase inhibitory activity of two Anthocleista species and in vivo rat model anti-diabetic activities of Anthocleista djalonensis extracts and fractions

Ethnopharmacological relevance

Anthocleista djalonensis (A. Chev) and Anthocleista vogelii Planch are plants being used in West Africa traditionally to treat various diseases such as malaria, hernia, hypertension, stomach aches, hemorrhoids, syphilis, and diabetes. Diabetes causes about 5% of all deaths globally each year. Chemotherapeutic agents such as biguanides, sulfonylureas, and thiozolidinediones are available for the treatment of diabetes, however, they have undesirable side effects. The need for newer, more effective and less toxic drugs is imperative and the biodiversity of Nigeria has a high potential for drug discovery based on plants used in the ethnomedicine.

Aim of the study

To investigate the leaves, stem bark and roots of these plants for their probable alpha-amylase inhibitory activities and establish their anti-diabetic activities. The overall goal is do bioassay-guided fractionation and isolation of active anti-diabetic compounds.

Materials and methods

Powdered samples (leaves, stem bark and roots) macerated with 80% aqueous methanol were evaluated in vitro using alpha-amylase inhibitory assay while in vivo investigations were carried out on hyperglycemic rats. Diabetes was induced in albino rats by an intraperitoneal injection of alloxan monohydrate (80 mg/kg). Plant extracts (1 g/kg) were given orally for 7 days, while blood glucose levels were monitored using a one touch glucometer. The crude methanol extracts found to be most active were further partitioned into hexane and ethyl acetate fractions which were also tested in vivo on the diabetic animals.

Results

The leaves and stem bark crude methanol extracts of Anthocleista djalonensis gave comparable α-amylase inhibition of 73.66% and 72.90%, respectively which were quite higher than the 38.93% and 22.90% of the same plant parts given by Anthocleista vogelii. The crude stem bark extract of Anthocleista djalonensis exhibited significant peak blood glucose reduction on day 6 (72.59%, p<0.05) which was higher than the leaves or roots which gave 45.73% and 47.46% (p<0.05), respectively The stem bark ethyl acetate fraction of Anthocleista djalonensis gave reduction in blood glucose level of 60.86% (p<0.05).

Conclusion

From our results, the leaves, stem bark and whole root of both plants exhibited α-amylase inhibitory activities with Anthocleista djalonensis also showing good anti-diabetic activities in vivo indicating that they contain active principles for the management of diabetes. There is justification for the use of the plants traditionally to manage diabetes.     

Hymenaea stigonocarpa Mart. ex Hayne: A tropical medicinal plant with intestinal anti-inflammatory activity in TNBS model of intestinal inflammation in rats

Ethnopharmacological relevance

Stem bark and fruit pulp of Hymenaea stigonocarpa Mart ex. Hayne (Fabaceae) has been popularly used to treat inflammation and gastrointestinal diseases including ulcers, diarrhea and gastric pain. The aim of this study was to investigate the intestinal anti-inflammatory activity of a methanol extract derived from the stem bark and diet with fruit pulp of Hymenaea stigonocarpa in the TNBS model of intestinal inflammation in rats.

Material and methods

The intestinal anti-inflammatory activity of stem bark extract (100, 200 and 400 mg/kg) and fruit pulp (10% and 5% in diet) was measured against the intestinal inflammatory process induced by TNBS (trinitrobenzesulphonic acid) in rats. The protective effects were evaluated as follows: evaluation of intestinal damage (damage score, extension of lesion, colon weight/length ratio), incidence of diarrhea and adherence to adjacent organs, colon glutathione (GSH) and malondialdehyde (MDA) contents, myeloperoxidase (MPO) and alkaline phosphatase (AP) activities. In addition, in vitro studies on lipid peroxidation in rat brain membranes and phytochemical profile were performed with both stem bark and fruit pulp.

Results

Treatment with 100, 200 and 400 mg/kg of stem bark extract and 10% fruit pulp flour showed protective effects in the TNBS-induced colon damage, which was related to inhibition of MPO and AP activities, reduction in colon MDA content, and counteraction of GSH depletion induced by inflammatory process. A concentration-dependent inhibitory effect on the lipid peroxidation in rat brain membranes for stem bark and fruit pulp was determined, with an IC₅₀ value of 5.25±0.23 μg/mL and 27.33±0.09 μg/mL, respectively. Similar phytochemical composition was observed in fruit and stem bark, including mainly flavonoids, condensed tannins and terpenes.

Conclusions

Stem bark extract and fruit pulp flour of Hymenaea stigonocarpa prevented TNBS-induced colonic damage in rats and this protective effect were associated to an improvement of intestinal oxidative stress. The observed anti-inflammatory and antioxidant effects may be associated to the presence of flavonoids and tannins in the stem bark and fruit pulp of Hymenaea stigonocarpa.     

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

Ethnopharmacological relevance

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

Aim of the study

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

Materials and methods

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

Results

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

Conclusions

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

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.     

Anticonvulsant activity of hydroalcoholic extracts from Erythrina velutina and Erythrina mulungu

The anticonvulsant effects of hydroalcoholic extracts (HAEs) from the stem bark of Erythrina velutina and Erythrina mulungu on pentylenetetrazole (PTZ) and strychnine-induced seizure tests and the potentiation of pentobarbital-induced sleeping time in mice with the extracts were examined in this study. These medicinal plants belong to the Fabaceae family and are popularly used in Brazil for their effects on the central nervous system. The extracts of Erythrina velutina (intraperitoneally or orally) and Erythrina mulungu (intraperitoneally) were administered in mice at single doses (200 or 400mg/kg). While Erythrina velutina and Erythrina mulungu did not exhibit any protector effect in PTZ-induced seizures, at any dose, an increase in the latency of convulsion and in the death time was observed with both doses and routes of Erythrina velutina and at higher dose of Erythrina mulungu, in strychnine-induced seizure. No alteration was observed with Erythrina velutina and Erythrina mulungu on sleeping latency at both doses as compared to control (362.8+/-59.5). However, the sleeping time was increased in both plants as compared to control (943.8+/-129.6). In conclusion, we showed that the hydroalcoholic extracts of Erythrina velutina and Erythrina mulungu have anticonvulsant effects only in the strychnine-induced seizure model, suggesting their possible action in glycine system and a potentiation of pentobarbital sleeping time, suggesting depressant action in the central nervous system.     

Antitubercular activity of Arctium lappa and Tussilago farfara extracts and constituents

Ethnopharmacological relevance

Arctium lappa and Tussilago farfara (Asteraceae) are two plant species used traditionally as antitubercular remedies. The aim of this study was (i) to screen Arctium lappa and Tussilago farfara extracts for activity against Mycobacterium tuberculosis and (ii) to isolate and identify the compound(s) responsible for this reputed anti-TB effect.

Materials and methods

The activity of extracts and isolated compounds was determined against Mycobacterium tuberculosis H₃₇R_v using a high throughput spot culture growth inhibition (HT-SPOTi) assay.

Results

The n-hexane extracts of both plants, the ethyl acetate extract of Tussilago farfara and the dichloromethane phase derived from the methanol extract of Arctium lappa displayed antitubercular activity (MIC 62.5 μg/mL). Further chemical investigation of Arctium lappa led to the isolation of n-nonacosane (1), taraxasterol acetate (2), taraxasterol (3), a (1:1) mixture of β sitosterol/stigmasterol (4), isololiolide (5), melitensin (6), trans-caffeic acid (7), kaempferol (8), quercetin (9), kaempferol-3-O-glucoside (10). Compounds isolated from Tussilago farfara were identified as a (1:1) mixture of β sitosterol/stigmasterol (4), trans-caffeic acid (7), kaempferol (8), quercetin (9), kaempferol-3-O-glucoside (10), loliolide (11), a (4:1) mixture of p-coumaric acid/4-hydroxybenzoic acid (12), p-coumaric acid (13). All compounds were identified following analyses of their physicochemical and spectroscopic data (MS, ¹H and ¹³C-NMR) and by comparison with published data. This is the first report of the isolation of n-nonacosane (1), isololiolide (5), melitensin (6) and kaempferol-3-O-glucoside (10) from Arctium lappa, and of loliolide (11) from Tussilago farfara. Amongst the isolated compounds, the best activity was observed for p-coumaric acid (13) (MIC 31.3 μg/mL or 190.9 μM) alone and in mixture with 4-hydroxybenzoic acid (12) (MIC 62.5 μg/mL).

Conclusions

The above results provide for the first time some scientific evidence to support, to some extent, the ethno-medicinal use of Arctium lappa and Tussilago farfara as traditional antitubercular remedies.     

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).     

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.     

Diuretic activity of the ethanol and aqueous extracts of the surface layer of Poria cocos in rat

Ethnopharmacological relevance

Poria cocos Wolf (Polyporaceae) is a well-known traditional East-Asian medicinal fungus. the epidermis (“Fu-Ling-Pi” in Chinese) of the sclerotia is used as a diuretic. This study was conducted to evaluate of ethanol extract (EE) and aqueous extract (AE) of the diuretic activity of Fu-Ling-Pi in saline-loaded rats.

Material and methods

The EE and AE were orally administered to rats. Urinary excretion rate, pH and electrolyte excretion were measured in the urine of saline-loaded rats.

Results

Urinary excretion rates were significantly increased by the EE. The three doses of AE only produced a slight increase urinary output. The EE had little or no effect on K⁺ excretion, but did indeed induce a notable excretion of Na⁺, that was in agreement with the urinary excretion. The three doses of AE produced an increase Na⁺ and K⁺ excretion, but did not arrive at statistical significance.

Conclusions

The present study confirmed that the not aqueous but ethanol extracts of the epidermis of Poria cocos presents a remarkable diuretic effect.     

In vivo antimalarial activity of Keetia leucantha twigs extracts and in vitro antiplasmodial effect of their constituents

Ethnopharmacological relevance

The West African tree Keetia leucantha (Rubiaceae) is used in traditional medicine in Benin to treat malaria. The twigs dichloromethane extract was previously shown to inhibit in vitro Plasmodium falciparum growth with no cytotoxicity (>100 µg/ml on human normal fibroblasts).

Materials and methods

The dichloromethane and aqueous extracts of twigs of K. leucantha were evaluated in vivo against Plasmodium berghei NK 173 by the 4-day suppressive test and in vitro against a chloroquine-sensitive strain of Plasmodium falciparum (3D7) using the measurement of the plasmodial lactate dehydrogenase activity. Bioguided fractionations were realized and compounds were structurally elucidated using extensive spectroscopic analysis.

Results

The in vivo antimalarial activity of K. leucantha dichloromethane and aqueous twigs extracts were assessed in mice at the dose of 200 mg/kg/day. Both extracts exhibited significant effect in inhibiting parasite growth by 56.8% and 53.0% (p<0.0001) on day 7-postinfection. An LC–MS analysis and bioguided fractionations on the twigs dichloromethane extract led to the isolation and structural determination of scopoletin (1), stigmasterol (2), three phenolic compounds: vanillin (3), hydroxybenzaldehyde (4) and ferulaldehyde (5), eight triterpenic esters (6–13), oleanolic acid and ursolic acid. The antiplasmodial activity of the mixture of the eight triterpenic esters showed an antiplasmodial activity of 1.66±0.54 µg/ml on the 3D7 strain, and the same range of activity was observed for isolated isomers mixtures.

Conclusions

This is the first report on the in vivo activity of K. leucantha extracts, the isolation of thirteen compounds and analysis of their antiplasmodial activity. The results obtained may partially justify the traditional use of K. leucantha to treat malaria in Benin.     

Antimicrobial activity of the extracts of Craniotome furcata (Lamiaceae)

Ethnopharmacological relevance

Craniotome furcata (Link.) O. Kuntze (Lamiaceae) is used in the traditional medicine for the treatment of cuts and wounds indicating antimicrobial activity.

Aim of the study

To validate the traditional medicinal claim, in vitro antimicrobial activity of the extracts was screened against eleven human pathogenic bacteria and fungi.

Materials and methods

The ethyl acetate (CE) and n-butanol (CB) extracts of the aerial parts of Craniotome furcata were tested against four Gram-positive bacteria, four Gram-negative bacteria and three fungi species. Antimicrobial activity was determined by the tube-dilution method.

Results

The CE and CB extracts showed antimicrobial activity against all of the tested microorganisms, with minimum inhibitory concentration (MIC) values in the range of 0.41–4.58 mg/ml.

Conclusions

The tested microbes Micrococcus flavus and Escherichia coli were highly susceptible to extract CE and antimicrobial activity of CB is comparable to that of extract CE against Escherichia coli and Staphylococcus faecalis while it is better than that of extract CE, against Klebsiella pneumoniae. Both the extracts were found less susceptible against tested fungi.     

Anti-spasmodic effects of Zizyphus lotus (L.) Desf. extracts on isolated rat duodenum

Aim of the study

The present study deals with the anti-spasmodic activity of the aqueous and the methanolic extracts of the leaves and the root barks of Zizyphus lotus (L.) Desf. on male rats.

Materials and methods

This activity was assessed on contractions of isolated rat duodenum, induced by acetylcholine, KCl, and BaCl₂ and compared with the effect of atropine and papaverine.

Results

Both extracts of leaves and root barks caused significant relaxation of spontaneous contractions and produced a concentration-dependent inhibition (P < 0.01–0.001) of contraction induced by spasmogenic agents.

Conclusion

These results indicate that Zizyphus lotus extracts contain anti-spasmodic constituents mediating their effect through cholinergic receptors and blockade Ca²⁺ influx. This could explain the traditional use of Zizyphus lotus in the treatment of the intestinal diseases.     

Characterization of the antinociceptive and anti-inflammatory activities from Cocos nucifera L. (Palmae)

Aim of the study

Cocos nucifera cultivated in Brazil is known as “coco-da-Bahia” or “coqueiro-da-Índia”. The tea from the husk fiber is widely used to several inflammatory disorders. Crude extract and fractions obtained from Cocos nucifera “common variety” were evaluated to test the anti-inflammatory and antinociceptive activities.

Materials and methods

Crude extract (CE, 50, 100, and 150 mg/kg), fraction 1 (F1, molecular weight lesser than 1 kDa, 1, 10, and 50 mg/kg), fraction 2 (F2, molecular weight higher than 1 kDa, 1, 10, and 50 mg/kg), and the references drugs morphine (5 mg/kg), acetilsalicilic acid (200 mg/kg), prometazine (30 mg/kg), and metisergide (5 mg/kg) were evaluated on models of analgesia and inflammation.

Results

CE, F1, and F2 significantly develop peripheral and central antinociceptive activity but with less effect on supra-spinal regions of the brain. Administration of the opioid antagonist, naloxone (5 mg/kg) inhibited the antinociceptive effect indicating that Cocos nucifera crude extract and fractions may be acting in opioid receptors. CE and F1 also inhibited rat paw edema induced by histamine, and serotonin.

Conclusions

results demonstrated that Cocos nucifera and its fractions have antinociceptive and anti-inflammatory activities which confirm the popular use of this plant in several inflammatory disorders.