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Suppression of alcohol-cessation-oriented hyper-anxiety by the benzoflavone moiety of Passiflora incarnata Linneaus in mice.

A benzoflavone moiety has been reported recently to be responsible for the multifarious CNS effects of Passiflora incarnata Linneaus. In the light of the established usefulness of the benzoflavone moiety in counteracting the withdrawal effects of substances like morphine, cannabinoids and nicotine by the authors, the bioactive benzoflavone moiety (BZF) has been tested in mice treated with an addictive dose (2 g/kg, bid for 6 days) of ethyl alcohol, in order to evaluate its effectiveness in countering alcohol dependence. In a 7-day regimen, different groups of mice were administered vehicle, alcohol and alcohol+three doses (10, 20 and 50 mg/kg of the benzoflavone moiety) of P. incarnata; all treatments (chronic) being administered orally, twice daily for 6 days. Similarly, three other groups of mice were rendered addicts upon alcohol by administration of the addictive dose (2 g/kg, bid for 6 days) of ethyl alcohol, and a single acute administration of 10, 20 and 50 mg/kg dose of benzoflavone moiety was given on the 7th day. In both, chronic and acute administrations, the benzoflavone moiety prevented significantly the expression of withdrawal effects of alcohol as there was a significant decrease in anxiety oriented behavior in mice that received benzoflavone moiety of P. incarnata. The chronic administration of P. incarnata with alcohol had better preventive effects than the single acute treatment with P. incarnata in alcohol-dependent mice.

Alcoholism↗

Antimicrobial and antiproliferative activity of Peucedanum nebrodense (Guss.) Strohl.

Acetone extract of Peucedanum nebrodense (Guss.) Strohl., a rare endemic species from the Madonie mountains (Sicily), was tested in vitro for its antimicrobial activity against bacterial reference strains and antiproliferative activity against K562 (human chronic myelogenous leukemia), HL-60 (human leukemia) and L1210 (murine leukemia) cell lines. The acetone extract showed antiproliferative IC50 values in the range of 14-0.27 microg/ml.

Acetone↗

The in vitro effects of Hypericum species on human leukocyte myeloperoxidase activity.

Myeloperoxidase (MPO) is a major component of the antimicrobial system of polymorphonuclear neutrophils. The heme enzyme MPO catalyzes the conversion of hydrogen peroxide and chloride to hypochlorous acid. Hypochlorous acid is the major strong oxidant produced by neutrophils and may contribute to inflammatory tissue damage. It was reported that certain antiinflammatory drugs are capable of inhibiting MPO activity and this inhibition may account for their antiinflammatory effect. Hypericum L. is a genus of about 400 species, widespread throughout the world. Some species of genus exhibit a significant antiinflammatory activity beside their several pharmacological properties such as antidepressant, diuretic, antihelmintic, and antibacterial. In this study, we investigated the in vitro effects of three Hypericum species, which exhibit antiinflammatory activity, on human polymorphonuclear leukocyte MPO activity. We found that each extract of Hypericum species reduced the peroxidative and chlorinating activity of human leukocyte MPO in concentration-dependent manner. The antiinflammatory activity of these species may be related with inhibition of MPO activity.

Anti-Inflammatory Agents↗

Evaluation of Tanacetum larvatum for an anti-inflammatory activity and for the protection against indomethacin-induced ulcerogenesis in rats.

Oral administration of the chloroform extract from Tanacetum larvatum (Griseb. ex Pant.) Kanitz caused a dose-dependent anti-inflammatory effect in the carrageenan-induced rat paw oedema test. The obtained anti-inflammatory effect was 8.6, 32.8, 37.0 and 49.5% for the extract doses of 25, 50, 100 and 200mg/kg, respectively, being statistically significant at a dose of 50mg/kg. Indomethacin had a strong anti-inflammatory effect of 73.4% at a dose of 8mg/kg, but large gastric lesions were detected. When the plant extract in the highest tested dose (200mg/kg) was concomitantly given with indomethacin, the anti-inflammatory effect was slightly enhanced, but the gastric lesions were significantly reduced. The anti-inflammatory and anti-ulcer activity may be mainly due to the inhibition of DNA binding of the transcription factor NF-kappaB by components of the plant extract. This was proven in an electrophoretic mobility shift assay at a concentration of 50microg/ml. Due to its anti-inflammatory as well as anti-ulcer effects, Tanacetum larvatum should especially be used combined with those drugs that are known both for their strong anti-inflammatory activities and the ulcerogenic side effects such as NSAIDs.

Animals↗

Osmitopsis asteriscoides (Asteraceae)-the antimicrobial activity and essential oil composition of a Cape-Dutch remedy.

The essential oil composition and antimicrobial activity of Osmitopsis asteriscoides, a medicinal plant used in traditional herbal preparations in South Africa has been investigated. Three different antimicrobial methods (disc diffusion, minimum inhibitory concentration by micro-titer plate and time-kill studies) were comparatively evaluated against Candida albicans, Staphylococcus aureus and Pseudomonas aeruginosa. A preliminary screening was done using the disc diffusion method on nine bacterial and four fungal isolates. Minimum inhibitory concentrations showed some correlation with the disc diffusion method. However, time-kill studies appear to be a more superior method for determining antimicrobial activity of volatile compounds such as essential oils. Two moderately susceptible and one resistant organism were selected to further demonstrate the variability between the three methods. The antimicrobial activity of the essential oil, tested by means of time-kill methodology at concentrations ranging from 0.5 to 2% (v/v) indicate a strong fungicidal activity against Candida albicans and the oil was also found to be bacteriostatic against Staphylococcus aureus in a concentration-dependent manner. The essential oil rapidly reduced viable counts of Pseudomonas aeruginosa, but regrowth was noted after 240 min. The results have been generated in duplicate in separate microbiology laboratories using different time-kill methods and the results are congruent. The two major essential oil components camphor and 1,8-cineole were investigated indicating the positive antimicrobial efficacy of 1,8-cineole independently and in combination with camphor. In addition to (-)-camphor and 1,8-cineole, 40 compounds were identified by GC-MS in the hydro-distilled essential oil. The high concentration of cineole and camphor and their synergistic effect is presented as a possible explanation for the traditional use of Osmitopsis asteriscoides for treating microbe-related illnesses.

Anti-Infective Agents↗

Anti-inflammatory activity and effect on gastric acid secretion of dehydroleucodine isolated from Artemisia douglasiana.

The effect of Dehydroleucodine (DhL) on gastric acid secretion in rats was investigated at a dose of 40 mg/kg, while its anti-inflammatory effect was investigated in two experimental models: arthritis induced by Freund's adjuvant carrageenan- and cotton pellet-induced granuloma. DhL did not inhibit gastric acid secretion, suggesting that its anti-ulcerogenic effect can be attributed to its action on the mucosa defense factors. On the other hand, DhL inhibited both chronic and acute adjuvant carrageenan-induced inflammation phases, being most effective in the chronic phase. In the granuloma test, DhL also inhibited inflammation. It is suggested that the anti-inflammatory activity of DhL may be attributed to interference with multiple targets on the level of transcription factors, such as NF-kappaB, and cytokines.

Animals↗

Effects of aqueous extracts of Satureja hortensis L. on rhinosinusitis treatment in rabbit.

Satureja hortensis L. (Lamiaceae) is an annual herb that used as traditional folk medicine in Eastern Anatolia region of Turkey for treatment of different infectious diseases and disorders. This study was designated to investigate anti-inflammatory effect of aqueous extract (250 mg/kg) of Satureja hortensis. Therapeutic potential of Satureja hortensis as an anti-inflammatory agent was examined by measurement of NO* metabolites and histological changes in a rabbit model of rhinosinusitis. The results showed that both activity of NOS enzyme and concentration of NO* metabolites were significantly reduced by topical administration of Satureja hortensis extract. Histological examination demonstrated no edema and/or reduced inflammation in therapy group as compared to the control. Thus, the data suggest Satureja hortensis extract may have the potential to be used as anti-inflammation agent, and can be used in the treatment of rhinosinusitis diseases.

Animals↗

Stability of the constituents of Calendula, milk-thistle and passionflower tinctures by LC-DAD and LC-MS.

As a part of our investigations on the stability of tinctures, we evaluated 40 and 60% v/v tinctures of Calendula flower, Milk-thistle fruit and Passionflower. These preparations are widely employed in phytotherapy, thus Calendula is used externally for anti-inflammatory properties, Milk-thistle and Passionflower are employed for hepatic injuries and in tenseness with difficulty in falling asleep, respectively. Aim of this work was to assess the chemical stability of their active or marker constituents from accelerated and long-term testing by using HPLC. For Calendula flower and Passionflower active constituents are not known, however, flavonoids seem to have a crucial importance for the activity, and thus are considered the markers of Calendula and of Passionflower. Active constituents of Milk-thistle are represented by silymarin that is a phytocomplex mainly constituted by three flavolignans: silybin, silychristin and silydianin. Our investigation showed a very low thermal stability of the constituents from accelerated and long-term testing and determined by HPLC-DAD and -MS analyses and was related both to the class of flavonoids and water content of the investigated tinctures. Thus, shelf-lives at 25 degrees C of the most stable tincture (Passionflower 60% v/v) was about 6 months and only about 3 months the stability of Milk-thistle tinctures.

Calendula↗

Development of LC-MS method for determination of ursolic acid: application to the analysis of ursolic acid in Staphylea holocarpa Hemsl.

Ursolic acid is a hydroxy pentacyclic triterpene, which has a chemoprotective activity in human. A reliable and reproducible liquid chromatography-mass spectrometric assay (LC-MS) was developed for the determination of ursolic acid in laboratory-made mixtures and in leaves and twigs extracts of Staphylea holocarpa Hemsl. The methanolic solution of the extracted ursolic acid was chromatographically analyzed using Shim Pack CLC-CN, C18 (150 x 6 mm, 5 mu) column and a mobile consisting of methanol-1% acetic acid solution (4:1) at a flow rate of 1.0 ml min(-1). The mass spectrometer (LCQ-Finnigan) was programmed in the positive single ion monitoring (SIM) to permit detection and quantitation of ursolic acid in MS-SIM mode at m/z 439.2, 411.2 and 390.9. Linear correlation (r > 0.99) of the peak area and the concentration of ursolic acid over the concentration range 0.25-10 microg ml(-1) was obtained. The relative standard deviation (%R.S.D.) and percentage deviation from the nominal concentrations (%DEV) were found to be 3.03-3.59% and -4.5 to +6.2%, respectively. Analysis of laboratory-made mixtures containing known concentrations of ursolic acid, as quality control samples, gave a mean recovery percentage of 97.8%. Application of the proposed method for the analysis of leaves and twigs extracts of S. holocarpa Hemsl. gave mean percentage contents of ursolic acid of 0.95 and 0.25%, respectively.

Chromatography, Liquid↗

Safflower polysaccharides activate the transcription factor NF-kappa B via Toll-like receptor 4 and induce cytokine production by macrophages.

Two active polysaccharide fractions (SF1 and SF2) purified from dried safflower petals (Carthamus tinctorius L.) stimulated the synthesis of various cytokines by peritoneal macrophages. In a number of cell types, SF1 and SF2 induced a rapid degradation of IkappaB alpha essential for the activation of the transcription factor NF-kappaB. Toll-like receptor 4 (TLR4), but not TLR2, was expressed in all cell lines that responded to SF1 and SF2. Enforced expression of TLR4 and MD-2 rendered responsiveness to SF1 and SF2. Moreover, these safflower polysaccharides failed to induce the production of TNF-alpha and NO by peritoneal macrophages prepared from C3H/HeJ mice that have a point mutation in the Tlr4 gene. Thus, these observations clearly indicate that safflower polysaccharides activate the NF-kappaB signaling pathway via TLR4.

Animals↗

Trichloroethylene uptake by apple and peach trees and transfer to fruit.

A greenhouse study was conducted to quantify 14C-trichloroethylene (TCE) uptake and transfer into the edible fruit of apple and peach trees. Trees were subsurface irrigated with solutions of 14C [TCE] that bracketed groundwater concentrations (5 and 500 microg/L) found in residential areas surrounding Hill Air Force Base, UT, where trace amounts of TCE had been found in several fruits during a preliminary field survey. Nondosed control trees were grown within the canopy of the dosed trees and in a separate greenhouse. Tissue samples were analyzed for 14C and TCE using combustion/liquid scintillation counting (LSC) and headspace/gas chromatography/mass spectrometry (HS/GC/MS). Tissue was also extracted and analyzed by GC/MS for dichloroacetic acid (DCAA), trichloroacetic acid (TCAA), and trichloroethanol (TCEt), three specific TCE metabolites that have been previously identified in laboratory and field studies. No 14C was detected in the nonexposed control trees. Exposed trees contained levels of 14C that were proportional to the exposure concentration. 14C concentrations were greatest in leaves followed by branches and fruits. At the end of the study, TCE was detected only in roots implying that the 14C in the leaves, branches, and fruit was associated with unidentified nonvolatile TCE transformation products and/or is nonextractable. However, TCAA and DCAA were positively identified only in leaves collected during the first year from an apple tree exposed to the high dose treatment. Additional data for other chemicals and fruittrees are needed to better understand the potential transfer of organic compounds to edible fruit.

Carbon Isotopes↗

Identification of AtENT3 as the main transporter for uridine uptake in Arabidopsis roots.

Previous studies have shown that Arabidopsis equilibrative nucleoside transporters (AtENTs) possess transport activities when produced in yeast cells and are differentially expressed in Arabidopsis organs. Herein, we report further analysis on the nucleoside transport activities and transcriptional patterns of AtENT members. The recombinant proteins of AtENTs 3, 6, and 7, but not those of AtENTs 1, 2, 4, and 8, were found to transport thymidine with high affinity. Contrary to previous suggestion that AtENT1 may not transport uridine, this work showed that recombinant AtENT1 was a pH-dependent and high-affinity transporter of uridine. When grown on MS plates, the AtENT3 knockout plants were more tolerant to the cytotoxic uridine analog 5-fluorouridine than wild-type plants and the knockout plants of AtENT1 or AtENT6. Consistent with this observation, the AtENT3 knockout line exhibited a significantly decreased ability to take up [(3)H]uridine via the roots when compared with wild-type plants and the plants with mutated AtENT1 or AtENT6. This indicates that AtENT3, but not AtENTs 1 and 6, is the main transporter for uridine uptake in Arabidopsis roots. The transcription of AtENTs 1, 3, 4, 6, 7, and 8 was regulated in a complex manner during leaf development and senescence. In contrast, the six AtENT members were coordinately induced during seed germination. This work provides new information on the transport properties of recombinant AtENT proteins and new clues for future studies of the in vivo transport activities and physiological functions of the different ENT proteins in Arabidopsis plants.

Aging↗

Effect of Centella asiatica on cognition and oxidative stress in an intracerebroventricular streptozotocin model of Alzheimer's disease in rats.

1. Centella asiatica, an Indian medicinal plant, has been described as possessing central nervous system activity, such as improving intelligence. In addition, we have demonstrated that C. asiatica has cognitive-enhancing and anti-oxidant properties in normal rats. Oxidative stress or an impaired endogenous anti-oxidant mechanism is an important factor that has been implicated in Alzheimer's disease (AD) and cognitive deficits seen in the elderly. 2. Intracerebroventricular (i.c.v.) streptozotocin (STZ) in rats has been likened to sporadic AD in humans and the cognitive impairment is associated with free radical generation in this model. Therefore, in the present study, the effect of an aqueous extract of C. asiatica (100, 200 and 300 mg/kg for 21 days) was evaluated in i.c.v. STZ-induced cognitive impairment and oxidative stress in rats. 3. Male Wistar rats were injected with STZ (3 mg/kg, i.c.v.) bilaterally on the days 1 and 3. Cognitive behaviour was assessed using passive avoidance and elevated plus-maze paradigms on the days 13, 14 and 21. Rats were killed on the day 21 for estimation of oxidative stress parameters (malondialdehyde (MDA), glutathione, superoxide dismutase and catalase) in the whole brain upon completion of the behavioural task. 4. Rats treated with C. asiatica showed a dose-dependent increase in cognitive behaviour in both paradigms. A significant decrease in MDA and an increase in glutathione and catalase levels were observed only in rats treated with 200 and 300 mg/kg C. asiatica. 5. The present findings indicate that an aqueous extract of C. asiatica is effective in preventing the cognitive deficits, as well as the oxidative stress, caused by i.c.v. STZ in rats.

Alzheimer Disease↗

Antimicrobial and antioxidant activities of three Mentha species essential oils.

The present study describes the antimicrobial activity and free radical scavenging capacity (RSC) of essential oils from Mentha aquatica L., Mentha longifolia L., and Mentha piperita L. The chemical profile of each essential oil was determined by GC-MS and TLC. All essential oils exhibited very strong antibacterial activity, in particularly against Esherichia coli strains. The most powerful was M. piperita essential oil, especially towards multiresistant strain of Shigella sonei and Micrococcus flavus ATTC 10,240. All tested oils showed significant fungistatic and fungicidal activity [expressed as minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC) values, respectively], that were considerably higher than those of the commercial fungicide bifonazole. The essential oils of M. piperita and M. longifolia were found to be more active than the essential oil of M. aquatica. Especially low MIC (4 microL/mL) and MFC (4 microL/mL) were found with M. piperita oil against Trichophyton tonsurans and Candida albicans (both 8 microL/mL). The RSC was evaluated by measuring the scavenging activity of the essential oils on the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and OH radicals. All examined essential oils were able to reduce DPPH radicals into the neutral DPPH-H form, and this activity was dose-dependent. However, only the M. piperita oil reduced DPPH to 50 % (IC50 = 2.53 microg/mL). The M. piperita essential oil also exhibited the highest OH radical scavenging activity, reducing OH radical generation in the Fenton reaction by 24 % (pure oil). According to GC-MS and TLC (dot-blot techniques), the most powerful scavenging compounds were monoterpene ketones (menthone and isomenthone) in the essential oils of M. longifolia and M. piperita and 1,8-cineole in the oil of M. aquatica.

Anti-Bacterial Agents↗

Dissectol A, an unusual monoterpene glycoside from Incarvillea dissectifoliola.

An unusual monoterpene glycoside named dissectol A ( 1) was isolated from the EtOH extract of Incarvillea dissectifoliola, and its structure was determined by 1D and 2D NMR data. The antimicrobial bioassays showed that dissectol A had modest inhibitory activity against Mycobacterium tuberculosis when compared to rifampicin in an agar diffusion assay.

Antitubercular Agents↗