Antibacterial activity of tannin constituents from Phaseolus vulgaris, Fagoypyrum esculentum, Corylus avellana and Juglans nigra

Tannins were fractionated from acetonic extract preparations of phenolic compounds from Phaseolus vulgaris, Fagoypyrum esculentum, Corylus avellana and Juglans nigra. Wide variations in antibacterial activities ranging from MICs of 62.5 to 500 microg/ml were apparent. Of particular note was a relatively high level of activity (62.5 to 125 microg/ml) for all extracts against Listeria monocytogenes.     

Antioxidative and acute antiinflammatory effects of Torreya grandis

The present study was undertaken to investigate the antioxidative and antiinflammatory activities of the ethanolic extract of seeds of Torreya grandis (EST). Exposure of human dermal fibroblasts to the extract at 50 and 250 microg/ml showed significant protective effect against hydrogen peroxide (300 microM). EST not only protected cell survival from H(2)O(2)-induced toxicity, but also inhibited the H(2)O(2)-induced LDH release significantly. It was also found that EST at 100 and 1000 microg/ml showed scavenging activities of radicals and reactive oxygen species with 29.8% and 100.0% of inhibition against DPPH radical and 41.2% and 98.4% against superoxide radicals in the xanthine/xanthine oxidase system, respectively. Topically applied EST dose-dependently inhibited arachidonic acid (AA)- and 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ear edema in mice.     

Antioxidant activity of polyphenols from solid olive residues of c.v. Coratina

The antioxidant profile of extracts from solid olive residue (SOR) of c.v. Coratina, a cultivar widely diffused in the south of Italy, using both cell-free and cell-based experimental models, was investigated. A total hydroalcoholic extract (polyphenols content 19.7%) and a purified extract (Oleaselecttrade mark) (polyphenols content 35.1%) were tested for their ability to quench the stable free radical DPPH, the peroxyl radicals (ORAC assay), by monitoring the loss in fluorescence of R-phycoerythrin induced by the peroxyl radical generator AAPH and their ability to inhibit the cumene hydroperoxide-induced lysis of rat red blood cells (RBC). The total hydroalcoholic extract showed IC(50) 26.96+/-1.53 microg/ml in the DPPH assay, that 10 microg/ml were equivalent to 2.11+/-0.12 microg/ml Trolox (ORAC assay) and IC(50) 1.7+/-0.20 microg/ml in the RBC hemolysis. The Oleaselect extract was 4 to 5 folds more active than the hydroalcoholic extract in all the experimental models, with IC(50) values of 7.36+/-0.38 microg/ml in the DPPH test and of 0.38+/-0.03 microg/ml in RBC; the antioxidant activity in the ORAC assay was slightly greater than that of Trolox (10 microg/ml equivalent to 11.45+/-0.40 microg/ml). The scavenging effect of the extract in the ORAC assay was compared to that of verbascoside (the main polyphenol component) and of caffeic acid (the basic constituent of verbascoside): the results indicate that caffeic acid (10 microg/ml equivalent to 35.70+/-2.95 microg/ml Trolox) is more potent than verbascoside (10 microg/ml equivalent to 15.42+/-1.21 microg/ml Trolox) in entrapping peroxyl radicals. Finally the antioxidant activity of the Oleaselect extract was confirmed in human umbilical endothelial cells (EC) exposed to the site-specific peroxyl radical inducer AAPH, where a massive lipid peroxidation process (marker the fluorescence probe BODIPY) takes place, paralleled by a marked loss of cell viability (calcein assay). The purified extract (1-20 microg/ml) pre-incubated with EC for 1 h dose-dependently inhibited both the lipid-peroxidation damage and cell death. Taking into account the total polyphenol content, these results clearly indicate a greater antioxidant activity for the purified extract, due to a cooperative antioxidant interaction among its polyphenol constituents.     

Antifungal activity of Agapanthus africanus extractives

The ethanolic extract of the rhizomes of Agapanthus africanus showed antifungal activity. In bioassay guided fractionation, n-butanol fraction exhibited significant activity against human pathogens. A saponin, (25R)-spirost-7-en-2alpha,3beta,5alpha-triol-3-O-[alpha-L-rhamnopyranosyl(1-->2)-[beta-D-galactopyranosyl (1-->3)] beta-D-glucopyranoside (1), responsible for the antifungal activity and having MIC value of 15.6 microg/ml against Trychophyton mentagrophytes and Sporothrix schenekii, was isolated and identified as active constituent of the plant.     

Amoebicidal and giardicidal compounds from the leaves of Zanthoxylum liebmannianun

The crude ethanol extract from the leaves of Zanthoxylum liebmannianum exhibited inhibitory effect on the reproduction of trophozoites of Entamoeba histolytica (IC(50)=3.48 microg/ml) and Giardia lamblia (IC(50)=58.00 microg/ml). From this extract, asarinin, hyperin, beta-sitosterol, and beta-sitosterol glucoside were isolated. Among them, asarinin was the most active with IC(50) values of 19.86 microg/ml for E. histolytica and 35.45 microg/ml for G. lamblia. The remaining compounds showed moderate activity against both parasites.     

Anti-plasmodial activity of Ailanthus excelsa

The anti-plasmodial activity of Ailanthus excelsa stem bark was investigated. The methanolic extract inhibited in vitro growth of chloroquine-sensitive (D10) and resistant strains (W2) of Plasmodium falciparum (IC50 4.6 and 2.8 microg/ml, respectively). The effect was retained in the chloroform fraction (3.1 and 2.1 microg/ml, respectively). The anti-plasmodial activity could be ascribed to the impairment of haemoglobin degradation through the inhibition of plasmepsin II activity (IC50 of 13.43+/-1.74 microg/ml) and of the haem detoxification to haemozoin.     

Anti-TB activity of Evodia elleryana bark extract

An ethyl acetate extract of bark from Evodia elleryana produced significant growth inhibition of Mycobacterium tuberculosis at concentrations only minimally inhibitory to human T cells. The crude extract yielded 95% inhibition of TB at 50 microg/ml. The crude extract yielded 29% growth inhibition of human T-cells in culture at that concentration.     

Preliminary antiproliferative effects of some species of Terminalia, Combretum and Pteleopsis collected in Tanzania on some human cancer cell lines

Methanolic extracts (25 microug/ml) of species belonging to the genera of Combretum, Terminalia and Pteleopsis, collected during a field expedition in Tanzania in 1999, were screened for their antiproliferative and cytotoxic effects against three human cancer cell lines (HeLa, cervical carcinoma; T 24, bladder carcinoma; and MCF 7, breast carcinoma). A leaf extract of Combretum fragrans and a fruit extract of C. zeyheri gave the strongest antiproliferative and cytotoxic effects of all the twenty-four extracts screened in this investigation. In contrast to the highly powerful leaf extract of C. fragrans, the root extract of this species gave no cytotoxic effects against the investigated cancer cell lines at a concentration of 25 microg/ml. The other investigated species of Combretum and Terminalia differed greatly in their cytotoxic potential. Root extracts of Terminalia sambesiaca and T. sericea gave the strongest cytotoxic effects of the five species of Terminalia used in this study. Eight of the twenty-four investigated plant extracts showed pronounced cytotoxic effects (<30% proliferation compared to the control) against the T 24 bladder cancer cells, seven against the HeLa cells and four against the MCF 7 cells.     

Dual inhibition of cyclooxygenase-1 and 5-lipoxygenase by aerial part of Bupleurum fruticescens methanol extract

The effect of the methanol extract from aerial parts of Bupleurum fruticescens on the release of eicosanoids and hydrolytic enzymes was determined on in vitro cell systems. The extract had a significant effect on 5-lipoxygenase (5-LOX) activity, inhibiting both LTB4 and 5(S)-HETE production with IC50 values of 112 microg/ml and 95 microg/ml, respectively. At concentrations of 200 microg/ml, the extract also inhibited cyclooxygenase-1 (90%) and elastase activities (54%). The 12-LOX activity in intact platelets was not affected; a fact, which suggests that phospholipase A2 (PLA2) activity, is not modified by the extract.     

Antibacterial activity and cytotoxicity of extractives from Ravenia spectabilis

A methanolic extract of Ravenia spectabilis, an isolated alkaloid, arborinine plus a fraction comprising arborinine and gamma-fagarine (VLC), showed mild to significant in vitro antibacterial activity. In a brine shrimp lethality bioassay, the extract and the fraction were found to exhibit moderate cytotoxicity having LC50 of 76.26 microg/ml and 14.98 microg/ml, respectively.     

Scavenging effect and antispasmodic activity of the essential oil of Cyclotrichium niveum

The radical scavenging and the spasmolitic activity of Cyclotrichium niveum essential oil were evaluated in vitro. It showed an IC(50) of 1750 microg/ml on DPPH method and dose dependently (0.1, 0.5 and 1 mg/ml) inhibits the contraction induced by carbachol on rabbit bladder from 15 to 100%. Moreover, it was able to inhibit the rat ileum muscle by 30 to 100%.     

Immunomodulatory effects of the methanolic extract of Epimedium alpinum in vitro

The effect of the methanolic extract of root and rhizome of Epimedium alpinum (MEEA) on phenotype and functions of rat lymphocytes in vitro was studied. It has been found that MEEA at lower concentrations (0.1 microg/ml and 1 microg/ml) significantly enhanced proliferation of splenocytes and thymocytes triggered by concanavalin A (Con A), whereas higher concentrations of the extract (50 microg/ml-500 microg/ml) were inhibitory. The stimulatory effect of MEEA on Con A-induced proliferation of splenocytes correlated with the up-regulation of interleukin-2 receptor alpha (IL-2Ralpha) expression. In addition, increased production of IL-2 was observed when a blocking IL-2Ralpha monoclonal antibody (mAb) was added to cell cultures. MEEA-suppressed proliferation of splenocytes was due to the inhibition of IL-2 production, the down-regulation of IL-2Ralpha expression and the induction of apoptosis. Cellular proliferation in the presence of inhibitory concentrations of MEEA higher than 50 microg/ml could not be restored by the addition of exogenous IL-2.     

A new cytotoxic xanthone from Garcinia rigida

A new xanthone, yahyaxanthone (1), was isolated from Garcinia rigida leaves. Cytotoxicity evaluation showed that 1 was inhibitory to L1210 cell, with an IC50 value 4.08 microg/ml.     

Cytotoxicity and antibacterial activity of extractives from Wedelia calendulacea

The cytotoxicity and antibacterial activity of petroleum ether, chloroform and methanol extracts of Wedelia calendulacea were assayed by brine shrimp lethality bioassay and standardized disk diffusion method against 19 bacterial strains. Three diterpenes isolated from the plant were also evaluated for in vitro antibacterial activities. The LC50 for the crude extracts against the brine shrimp nauplii were found to be 4.59 microg/ml, 7.99 microg/ml and 14.88 microg/ml, respectively, whereas the positive control, vincristine sulfate showed an LC50 of 0.58 microg/ml. Among the crude extracts and pure compounds tested, (-)-kaur-16-en-19-oic acid isolated from the chloroform extract showed the highest inhibitory activity against most of the bacterial strains with mean zone of inhibition of 10-21 mm at 200 microg/disc.     

Antioxidant and hepatoprotective effect of Acanthus ilicifolius

The alcoholic extract of Acanthus ilicifolius leaves inhibited the formation of oxygen derived free radicals (ODFR) in vitro with IC(50) of 550 microg/ml, 2750 microg/ml, 670 microg/ml and 600 microg/ml (Fe(2+)/ascorbate system), 980 microg/ml (Fe(3+)/ADP/ascorbate system) for superoxide radical production, hydroxyl radical generation, nitric oxide radical formation and lipid peroxide formation, respectively. The oral administration of the extract (250 and 500 mg/kg) significantly reduced CCl(4) induced hepatotoxicity in rats, as judged from the serum and tissue activity of marker enzymes [glutamate oxaloacetate transaminase (GOT), glutamate pyruvate transaminase (GPT) and alkaline phosphatase (ALP)]. These results were comparable with those obtained with curcumin (100 mg/kg, p.o.).     

Bioactive plants from Argentina and Bolivia

Antibacterial and molluscicidal activities of methanol and chloroform extracts of 16 plant species belonging to the families Compositae and Melastomataceae were evaluated. The chloroform extract of Vernonanthura tweediana and the methanol extract of Senecio santelisis resulted to be very toxic to brine shrimp nauplii (LC(50)=1 microg/ml). Chloroform extracts of S. santelisis and Senecio leucostachys as well as the methanol extract of Wedelia subvaginata displayed molluscicidal effects on Biomphalaria peregrina showing LC(100)<100 microg/ml. Moderate antibacterial action was produced by the chloroform extracts of Flaveria bidentis, Grindelia scorzonerifolia and Vernonia incana against two strains of Staphylococcus aureus.     

Trypsin inhibitory activity of Lawsonia inermis

The ethanolic extract of Lawsonia inermis leaves and lawsone tested for trypsin inhibitory activity showed an IC(50) value of 64.87 and 48.6 microg/ml, respectively.     

In vitro spasmolytic effect of aqueous extract of Calotropis procera on Guinea-pig trachea smooth muscle chain

The aqueous extract of Calotropis procera was evaluated for its spasmolytic effect using in vitro trachea smooth muscle chain of Guinea-pig. The extract (50, 100 and 200 microg/ml) showed a dose-dependent relaxant activity probably exhibited through the direct relaxant action on the smooth muscle.     

Ocimum basilicum ethanolic extract decreases cholesterol synthesis and lipid accumulation in human macrophages

Macrophage lipid accumulation induced by low density lipoproteins (LDL) plays a pivotal role in atherosclerotic plaque development. Previous work showed that Ocimum basilicum extract, used as hypocholesterolemic agent by traditional medicine in Morocco, has hypolipidemic activity in rat acute hyperlipimidemia. This study investigated the effects of ethanolic extract of O. basilicum on lipid accumulation in human macrophages. As modification of LDL increase atherogenicity of the particles we evaluated the effects of the extract on LDL oxidation. The extract caused a dose-related increase of LDL-resistance to Cu(2+)-induced oxidation. Furthermore, at the dose of 60 microg/ml, significantly decreases the accumulation of macrophage lipid droplets induced by modified LDL evaluated as by red-oil staining. Cholesterol esterification and triacylglycerol synthesis in the cells were not affected. Macrophage treatment with 60 microg/ml, but not 20 microg/ml, of the extract reduced newly synthesized unesterified cholesterol by about 60% and decreased scavenger receptors activity by about 20-30%, evaluated by the internalization of cholesterol carried by [(3)H]CE-aggregated-LDL. The results suggest that O. basilicum ethanolic extract has the capability to reduce foam cell formation through the reduction of cholesterol synthesis and the modulation of the activity of surface scavenger receptors.     

Biological screening of Bangladeshi mango mistletoe bark extracts

The ethyl acetate extract of the Bangladeshi mango mistletoe (Loranthus globosus) bark was found to be most effective against both Gram (+) and Gram (-) bacteria and it also showed good cytotoxicity with a LC50 10.83 microg/ml.