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In vitro study of the antioxidant and immunomodulatory activity of aqueous infusion of Bidens pilosa.

Bidens pilosa is an annual plant from tropical America with anti-inflammatory properties in hepatitis, laryngitis, headache and digestive disorders, among others. Its wide pharmacological applications can be attributed to its chemical composition, with inhibitory effects on pathogenic microorganisms and flavonoids, which show strong antioxidant capacities. We investigated the antioxidant activity of an aqueous infusion of Bidens pilosa by studying its protective effect on the hemolysis induced by an initiator of radicals such as 2,2'-azobis(2-amidinopropane) dihydrochloride (AAPH). The immunomodulatory activity of the infusion was tested using whole blood cells. Cytokine production increased in whole blood stimulated or not by lipopolysaccharides (LPSs). The infusion is also characterized by its capacity to protect erythrocytes from the phototoxic effect of chlorpromazine, which allows its use as a potential photoprotector. Finally, it did not show ocular irritation, as demonstrated by the effect on hemoglobin denaturation. This study supports the health benefits of the ingestion of the infusion.

Adjuvants, Immunologic↗

Reduction of MTT by aqueous herbal extracts in the absence of cells.

The tetrazolium salt 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) is used to determine cell viability in assays of cell proliferation and cytotoxicity. MTT is reduced in metabolically active cells to yield an insoluble purple formazon product. However, in the present study, we demonstrate that some botanical extracts can reduce MTT in the absence of living cells. Treatment of these extracts with iodoacetic acid (IAA) to alkylate free thiol groups inhibited their ability to reduce MTT, indicating that free thiols in the botanical extracts are responsible, at least in part, for the reduction of MTT to the formazon product. These results suggest that caution must be taken when interpreting the results of experiments using the MTT assay to measure the effects of botanical extracts on cell growth.

Drugs, Chinese Herbal↗

Platelet anti-aggregant property of some Moroccan medicinal plants.

It is known that blood platelets may present some dysfunction linked to cardiovascular pathologies such as arterial hypertension. The aim of this work is to examine the in vitro anti-aggregant effect of five medicinal plants among which three were reported as antihypertensive in oriental Morocco: Arbutus unedo (Ericaceae), Urtica dioïca (Urticaceae), and Petroselinum crispum (Apiaceae). The two other plants were Cistus ladaniferus (Cistaceae) and Equisetum arvense (Equisetaceae). The results obtained showed that all extracts produced a dose-dependent inhibition of thrombin and ADP-induced aggregation. The calculated IC50 (half-maximal inhibition of thrombin and ADP-induced aggregation) was found to be identical in all plant extracts while Urtica dioïca had a higher IC50 value. The effect of plants could be related in part to the polyphenolic compounds present in their extracts suggesting their involvement in the treatment or prevention of platelet aggregation complications linked to cardiovascular diseases. Phytochemical separation must be carried out to identify the active principles responsible for the anti-aggregant effect and elucidate their mechanisms of action.

Animals↗

Hypoglycaemic effect of Teucrium polium: studies with rat pancreatic islets.

The aquous extract of Teucrium polium (Labiatae) has long being used in Iran as a hypoglycaemic aid without any knowledge about its probable side effects and mode of action. In an effort to assess the claimed hypoglycaemic property of the crude drug and to get some knowledge about the mechanism of action, the crude extract (0.5 g plant powder per kg body weight) was administered orally to a group of streptozotocin diabetic rats for six consecutive weeks. A significant decrease (64%) in blood glucose concentration was observed in the treated animals compared to the untreated diabetic rats, without any measurable effects on the major biochemical factors. In addition, the crude extract significantly enhanced the blood insulin level by almost 160% compared to the untreated diabetic rats. The insulinotropic property of the Teucrium polium extract was further assessed by an in vitro investigation using isolated pancreatic rat islets. Our data indicated that Teucrium polium crude extract is able to enhance insulin secretion by almost 135% after a single dose of plant extract (equivalent to 0.1 mg plant leaf powder per mL of the culture medium) at high glucose concentration (16 mmol/L). Meanwhile, the time pattern of insulin secretion was not affected by the plant extract compared to the untreated islets. These data clearly show that the plant extract, probably without metabolic transformation, is able to reduce high blood glucose levels through enhancing insulin secretion by the pancreas.

Animals↗

Hepatoprotective and anti-inflammatory activities of Ballota glandulosissima.

Water extract of Ballota glandulosissima Hub.-Mor & Patzak (Lamiaceae) (BG) was investigated for anti-inflammatory activity using the carrageenan-induced rat paw oedema test and for hepatoprotective effect on carbon tetrachloride (CCl(4))-induced hepatotoxicity in rats. Biochemical parameters of hepatic damage such as serum aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP) and bilirubin concentrations were determined. CCl(4) (0.8 mL/kg i.p. for 7 days) treatment increased the serum AST, ALT, ALP and bilirubin levels significantly as compared to controls. Treatment of animals with BG (100 mg/kg, i.p.) +CCl(4) (0.8 mL/kg i.p.) for 7 days significantly ameliorated the levels of AST, ALT and ALP elevated by the CCl(4) treatment alone. The results of biochemical tests were also confirmed by histopathological examination. BG together with CCl(4) treatment decreased the balloning degeneration but did not produced apoptosis of hepatocytes, centrilobular and bridging necrosis observed in the CCl(4) treatment alone. BG, at 100 mg/kg per os, showed a significant reduction (34.22%) in rat paw oedema induced by carrageenan. The reference anti-inflammatory drugs etodolac (50 mg/kg, p.o.) and indomethacin (3 mg/kg, i.p.) significantly reduced the oedeme by 43.42 and 95.70%, respectively. The present study reveals that the water extract of Ballota glandulosissima possesses promising protective activity against CCl(4) induced hepatic damage and anti-inflammatory activity in rats.

Animals↗

The efficacy of Sphaeranthus senegalensis Vaill extract against diarrhoea in rats.

The aqueous extract of Sphaeranthus senegalensis (Asteraceae) was investigated for anti-diarrhoeal activity in rats. Its effect on castor oil-induced diarrhoea and fluid accumulation and on gastrointestinal (charcoal meal) test was evaluated. Results showed that pre-treatment for 30 min with the extract at 50, 100 and 200 mg/kg, p.o. causes a dose-dependent protection against castor oil-induced diarrhoea and intraluminal fluid accumulation and inhibited gastrointestinal transit motility. These results suggest that the plant contain active constituents that may be useful against diarrhoea.

Animals↗

Prospect for anthelminthic plants in the Ivory Coast using ethnobotanical criteria.

Sixty plant species were collected in the Ivory Coast on the basis of an ethnobotanical literature using the following three criteria: activity against worms, diarrhoea and/or abdominal pain. Eighty six plant extracts were prepared using 90% ethanol and tested for potential anthelminthic activities with a larvicidal test of Haemonchus contortus. 25.6% of the extracts showed a high activity, 12.8% were active or marginally active and the remaining 61.6% were inactive. The fact that a relatively high percentage of the plants species (50%) had an activity can be explained by the initial preselection of the plants on the basis of ethnobotanical indications.

Animals↗

The ambrosanolide cumanin inhibits macrophage nitric oxide synthesis: some structural considerations.

Since its role in inflammatory diseases was recognized, nitric oxide (NO) has become an important mediator to evaluate anti-inflammatory agents. Sesquiterpene lactones, which occur in several medicinal plants, inhibit the NO production in macrophage-like cells. This action is probably due to a 1,4 addition reaction between its alpha,beta-unsaturated carbonyl group with sulfhydryl (SH)-containing compounds. For this reason it is believed that these compounds are cytotoxic, which restricts their therapeutic use. In this contribution, the ability of the ambrosanolide-type sesquiterpene lactone cumanin (from the Asteraceae Ambrosia psilostachya) to inhibit NO biosynthesis was evaluated in lipopolisaccharide-induced peritoneal murine macrophages and its cytotoxicity was assessed in the MTT assay. Cumanin showed a potent inhibitory effect in NO production (IC(50) = 9.38+/-0.38 microM) with low cytotoxicity. The 1,4-addition reaction of thiols was slow, which does not explain the inhibition of NO production but does explain the low cytotoxicity of cumanin with respect to other lactones.

Ambrosia↗

Toxicological studies of the aqueous extract from Achyrocline satureioides (Lam.) DC (Marcela).

Achyrocline satureioides (Lam.) DC (Marcela) is known to possess a broad spectrum of pharmacological, medicinal and therapeutic properties. Previous studies have demonstrated various protective abilities of the marcela extracts against various pathological conditions. However, no extensive safety studies have been conducted on these extracts to date. In this paper, we evaluated the acute toxicity (dose levels of 30-300 mg/kg) of an aqueous extract of marcela, administered intraperitoneally and orally in mice and rats. The acute oral maximun tolerable dose in repeated administration during 4 h (1, 3 until 5 g/kg) was also studied in rats. The extract had low acute toxicity when administered intraperitoneally and no toxicity upon oral administration. The LD(50) of aqueous extracts of marcela was found to be greater than 5 g/kg when administered once via gastric intubation to rats. Weight gain, toxicity signs, enzymatic studies (transaminases and phosphatases) and histological evaluation of several organs indicated that the extract was devoid of acute toxicity. These acute studies demonstrated that an aqueous extract of marcela obtained after a 2% infusion is safe and did not cause any detrimental effects in vivo under the conditions investigated in this study.

Achyrocline↗

Hepatoprotective and free radical scavenging activities of phenolic petrosins and flavonoids isolated from Equisetum arvense.

Hepatoprotective activity-guided fractionation of the MeOH extract of Equisetum arvense L. (Equisetaceae) resulted in the isolation of two phenolic petrosins, onitin (1) and onitin-9-O-glucoside (2), along with four flavonoids, apigenin (3), luteolin (4), kaempferol-3-O-glucoside (5), and quercetin-3-O-glucoside (6). Among these, compounds 1 and 4 exhibited hepatoprotective activities on tacrine-induced cytotoxicity in human liver-derived Hep G2 cells, displaying EC(50) values of 85.8 +/ -9.3 microM and 20.2 +/- 1.4 microM, respectively. Silybin, used as a positive control, showed the EC(50) value of 69.0 +/- 3.3 microM. Compounds 1 and 4 also showed superoxide scavenging effects (IC(50) = 35.3 +/- 0.2 microM and 5.9 +/- 0.3 microM, respectively) and DPPH free radical scavenging effect (IC(50) of 35.8 +/- 0.4 microM and 22.7 +/- 2.8 microM, respectively). These results support the use of this plant for the treatment of hepatitis in oriental traditional medicine.

Cell Line, Tumor↗

Effect of Tribulus terrestris on nicotinamide adenine dinucleotide phosphate-diaphorase activity and androgen receptors in rat brain.

Tribulus terrestris L. (Zygophyllaceae) have been used as an aphrodisiac both in the Indian and Chinese traditional systems of medicine. Administration of Tribulus terrestris extract (TT) increased sexual behaviour and intracavernous pressure both in normal and castrated rats and these effects were probably due to the androgen increasing property of TT. The objective of the present study is to evaluate the effect of TT on nicotinamide adenine dinucleotide phosphate-diaphorase (NADPH-d) activity and androgen receptor (AR) immunoreactivity in rat brain. Twenty-four adult male Sprague-Dawley rats were divided into two groups of twelve each. Group I was treated with distilled water and Group II was treated with TT at the dose of 5mg/kg body weight orally, once daily for 8 weeks. Following treatment transcardiac perfusion was done with Ringer lactate, 4% paraformaldehyde and 30% sucrose. The brain tissue was removed and sections of the paraventricular (PVN) area of hypothalamus were taken for NADPH-d and AR immunostaining. There was an increase in both NADPH-d (67%) and AR immunoreactivity (58%) in TT treated group and these results were statistically significant compared to the control. Chronic treatment of TT in rats increases the NADPH-d positive neurons and AR immunoreactivity in the PVN region. Androgens are known to increase both AR and NADPH-d positive neurons either directly or by its conversion to oestrogen. The mechanism for the observed increase in AR and NADPH-d positive neurons in the present study is probably due to the androgen increasing property of TT. The findings from the present study add further support to the aphrodisiac claims of TT.

Animals↗

Activity of a traditional South African epilepsy remedy in the GABA-benzodiazepine receptor assay.

Aqueous and ethanol extracts of six plants, Acrotome inflata, Aptosimum indivisum, Asparagus suaveolens, Barleria bolusii, Commiphora marlothii and Sesamum triphyllum, which constitute an ancient Northern Sotho remedy for epilepsy, Sehlare sa Seebana, was tested in the GABA(A)-benzodiazepine receptor binding assay. Both aqueous and ethanol extracts of Aptosimum indivisum and Asparagus suaveolens and the aqueous extract of Commiphora marlothii showed good dose-dependent activity. The ethanol extract of all six plants extracted together was more active that the aqueous extract. The results did not suggest a synergistic effect of the plant mixture.

Animals↗

Screening of antifungal agents using ethanol precipitation and bioautography of medicinal and food plants.

In the search for bioactive compounds, bioautography and ethanol precipitation of macromolecules (proteins, polysaccharides, etc.) of plant aqueous extracts were associated in an antifungal screening. Thus, the supernatants, precipitates (obtained by ethanol precipitation) and aqueous extracts were investigated of medicinal and fruit bearing plants used against skin diseases by the Brazilian population. The agar diffusion and broth dilution methods were used to assess the activity against three fungi: Candida albicans, Trichophyton rubrum and Cryptococcus neoformans. The results, evaluated by the diameter of the inhibition zone of fungal growth, indicate that six plant species, among the 16 investigated, showed significant antifungal activity. The minimal inhibitory concentration (MIC) was determined on plant extracts that showed high efficacy against the tested microorganisms. The most susceptible yeast was Trichophyton rubrum and the best antifungal activity was shown by Xanthosoma sagittifolium supernatant. The bioautography was performed only for the aqueous extracts and supernatants of those plants that showed antifungal activity against Candida albicans and Cryptococcus neoformans, using n-butanol/acetic acid/water (BAW) 8:1:1 to develop silica gel TLC plates. Clear inhibition zones were observed for aqueous extracts of Schinus molle (R(f) 0.89) and Schinus terebinthifolius (R(f) 0.80) against Candida albicans, as for supernatant of Anacardium occidentale (R(f) 0.31) against Cryptococcus neoformans. The separation of macromolecules from metabolites, as in the case of Anacardium occidentale, Solanum sp. and Xanthosoma sagittifolium, enhances antifungal activity. In other cases, the antifungal activity is destroyed, as observed for Momordica charantia, Schinus molle and Schinus terebinthifolius.

Animals↗

Antitussive effect of Carum copticum in guinea pigs.

Several therapeutic effects including anti-asthma and dyspnea have been described for the seeds of Carum copticum In previous studies the relaxant and anticholinergic (functional antagonism) effects, histamine (H(1)) inhibitory effect of Carum copticum have been demonstrated on guinea pig tracheal chains. In the present study the antitussive effect of this plant was evaluated. The antitussive effects of aerosols of two different concentrations of aqueous and macerated extracts and carvacrol, codeine, and saline were tested by counting the number of coughs produced due to aerosol of citric acid 10 min after exposing animals to aerosols of different solutions (for carvacrol n=5 and for other solutions n=6). The results showed significant reduction of cough number obtained in the presence of both concentrations of aqueous and macerated extracts and codeine (p<0.001 for extracts and p<0.01 for codeine). The cough number obtained in the presence of higher concentration of aqueous and macerated extracts was significantly less than those of lower concentrations (p<0.05 for both extracts). In addition the cough number obtained in the presence of both concentrations of aqueous and macerated extracts was significantly lower than that of codeine (p<0.05 to 0.001). However, carvacrol did not show any antitussive effect. These results indicated an antitussive effect of Carum copticum which was even greater than that of codeine at concentrations used. In addition the antitussive effect of Carum copticum was not due to its main constituent, carvacrol.

Animals↗

Evaluation of French Guiana traditional antimalarial remedies.

In order to evaluate the antimalarial potential of traditional remedies used in French Guiana, 35 remedies were prepared in their traditional form and screened for blood schizonticidal activity in vitro on Plasmodium falciparum chloroquine re4sistant strain (W2). Some of these extracts were screened in vivo against Plasmodium yoelii rodent malaria. Ferriprotoporphyrin inhibition test was also performed. Four remedies, widely used among the population as preventives, were able to inhibit more than 50% of the parasite growth in vivo at around 100 mg/kg: Irlbachia alata (Gentiananceae), Picrolemma pseudocoffea (Simaroubaceae), Quassia amara (Simaroubaceae), Tinospora crispa (Menispermaceae) and Zanthoxylum rhoifolium (Rutaceae). Five remedies displayed an IC50 in vitro < 10 microg/ml: Picrolemma pseudocoffea, Pseudoxandra cuspidata (Annonaceae) and Quassia amara leaves and stem, together with a multi-ingredient recipe. Two remedies were more active than a Cinchona preparation on the ferriprotoporphyrin inhibition test: Picrolemma pseudocoffea and Quassia amara. We also showed that a traditional preventive remedy, made from Geissospermum argenteum bark macerated in rum, was able to impair the intrahepatic cycle of the parasite. For the first time, traditional remedies from French Guiana have been directly tested on malarial pharmacological assays and some have been shown to be active.

Administration, Oral↗

Chemical composition, antimicrobial and antioxidant activity of the essential oil of Teucrium marum (Lamiaceae).

The chemical composition of the essential oil obtained from Teucrium marum subsp. marum (Lamiaceae) was analysed by GC/MS and 30 components were identified. Isocaryophyllene (20.24%), beta-bisabolene (14.73%), beta-sesquiphellandrene (11.27%), alpha-santalene (10.97%), dolichodial (9.38%) and, alpha-caryophyllene (7.18%) were the main components. The antimicrobial activity of the essential oil was assayed against four phytopathogenic fungi and Rhyzoctonia solani resulted to be the most sensitive microorganism with a MIC value of 250 ppm. The antioxidant activity of the essential oil was evaluated using the DPPH test, 5-lipoxygenase test and luminol/xanthine/xanthine oxidase chemiluminescence assay.

Antioxidants↗

Antibacterial properties of common herbal remedies of the southwest.

Curanderismo, widely practiced in the southwest, is an alternative medical system that has been neglected by scientific research. This project analyzed the antibiotic properties of 23 common herbal remedies used in South Texas to treat wounds and infections. Ethanolic tinctures and aqueous extracts of each plant were prepared and applied to blank diffusion disks. These disks were desiccated and used in Kirby-Bauer disk diffusion susceptibility tests on three bacteria: Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli. Control disks contained solvent only. The efficacy of the tinctures and aqueous extracts was compared to that of commercially prepared antibiotic diffusion disks. No inhibition was observed with the aqueous extracts. The various tincture-saturated disks produced zones of clearance ranging from 1 to 5 mm. Ten plants consistently inhibited bacterial growth of Staphylococcus aureus. None of the plants tested produced consistent inhibition of the two Gram-negative species, Pseudomonas aeruginosa and Escherichia coli. No zones of clearance were produced by the solvent-only control disks. The zones of clearance produced by commercial antibiotics were, on average, larger and more uniform than those produced by the tincture disks. Thus, it appears that some of the herbal remedies used in folk medicine are potentially effective antibacterial agents against Staphylococcus aureus.

Anti-Bacterial Agents↗