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.     

Cytotoxic sesquiterpenes and lignans from Saussurea deltoidea

Two new sesquiterpenes deltoiden A (1) and deltoiden B (2), and two new lignans deltoignan A (9) and deltoignan B (10), together with 14 known compounds, including six sesquiterpenes 3-8 and three lignans 11-13, were isolated from the whole plant of Saussurea deltoidea. Compounds 3-8 and 11-17 were isolated for the first time from this plant. Their structures were established by spectroscopic analysis, including 2D-NMR spectroscopic techniques. Cytotoxicities of compounds 1-13 were tested against three cancer cell lines A549, Hela and SMMC-7721. Results showed that 5, 6 and 7 exhibited cytotoxicity against SMMC-7721 with the IC(50) values of 6.49, 9.53, 1.23 μg/ml, 5 and 7 against A549 with the IC(50) values of 4.99 and 5.35 μg/ml, 5, 6, 7, 13 against Hela with the IC(50) values of 1.40, 4.75, 0.93 and 5.42 μg/ml, respectively. The structure-activity relationships of sesquiterpenes 1-8 were discussed on the base of cytotoxic results.     

Cytotoxic activity of embelin from Lysimachia punctata

A major benzoquinone pigment, embelin (1), was isolated from the underground parts of Lysimachia punctata. Compound 1 showed a significant cytotoxic activity in vitro against B16 and XC cell lines with ED50 values of 13 microg/ml and 8 microg/ml, respectively.     

A new cytotoxic guaianolide from Chrysanthemum boreale

A new cytotoxic guaianolide was isolated from Chrysanthemum boreale Makino. The structure of guaianolide was elucidated as 8-acetoxy-4,10-dihydroxy-2,11(13)-guaiadiene-12,6-olide (1). Compound 1 exhibited cytotoxic activity (IC(50)< or =4 microg/ml) against all five human cancer cell lines tested.     

The antiplasmodial activity of spermine alkaloids isolated from Albizia gummifera

In the present study the methanolic extract of Albizia gummifera was fractionated into various fractions. These fractions were tested against choroquine sensitive (NF54) and resistant (ENT30) strains of Plasmodium falciparum. All other fractions apart from the alkaloidal fraction showed low activity with IC 50 above 3 microg/ml. The alkaloidal fraction exhibited strong activity against NF54 and ENT30 with IC 50 of 0.16+/-0.05 and 0.99+/-0.06 microg/ml, respectively. Five known spermine alkaloids were isolated from the alkaloidal fraction. These alkaloids exhibited activities against NF54 and ENT30 with IC 50 ranging from 0.09+/-0.02 to 0.91+/-0.10 microg/ml. Four of the alkaloids were further evaluated for in vivo activity against rodent malaria parasite Plasmodium berghei. The alkaloids showed percentage chemosuppression of parasitaemia in mice ranging from 43 to 72%. The use of the extracts A. gummifera for treatment of malaria in traditional medicine seems to have a scientific basis.     

Antineoplastic activity of selected constituents of Duguetia glabriuscula

The cytotoxic effects of seven constituents isolated from Duguetia glabriuscula were evaluated against Hep2 human larynx carcinoma cells. The cytotoxicity exhibited by beta-sitosterol was as strong as that of cis-platin. (+)-Alloaromadendran-10,14beta-diol caused inhibition of cellular growth with IC50 values lower than 25 microg/ml, a feature that was considered as revealing significant activity. Polycarpol showed borderline cytotoxicity, whereas the other compounds were inactive.     

A new epicatechin gallate and calpain inhibitory activity from Orostachys japonicus

Calpains are calcium-dependent proteases that cleave a variety of intracellular substrates. The overactivation of mu-calpain is associated with a wide range of disease conditions. To search for calpain inhibitors from natural products, the phytochemical constituents of the ethyl acetate fraction of the whole plant of Orostachys japonicus (Crassulaceae) were studied. The various chromatographic separation of this fraction led to the isolation of a new tannin, (-)-epicatechin 5-gallate (1) along with 9 known compounds. Their structures were elucidated by spectroscopic and chemical analyses. Among them, (-)-epicatechin 5-gallate (1) and kaempferol (9) exhibited moderate inhibitory activity against mu-calpain with IC(50) values of 18.0+/-2.9 and 15.4+/-2.0 microg/ml, respectively.     

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.     

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.     

Cytotoxic activity screening of some indigenous Thai plants

The 50% ethanolic extracts from 14 plant species used in Thai traditional folklore were screened for cytotoxic activity against a malignant human hepatoma (HepG2) cell line and a normal African green monkey kidney (Vero) cell line. The extracts of Polyalthia evecta and Erythroxylum cuneatum showed potent anticancer activity in the HepG2 cell line with IC(50) of 70+/-3 microg/ml and 64+/-4 microg/ml, respectively. P. evecta demonstrated more selectivity to the HepG2 than the Vero cell (selectivity index>14.3) indicating its potential for biopharmaceutical use.     

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.     

Antioxidant activity of isocytisoside and extracts of Aquilegia vulgaris

Two extracts (ethyl acetate and ethanol) and isocytisoside obtained from Aquilegia vulgaris were tested for their antioxidant and free radical scavenging activity in vitro. Inhibition both non-enzymatic (IC50: 150-219 microg/ml) and enzymatic (IC50: 23-60 microg/ml) microsomal lipid peroxidation was observed, the extracts being more active than isocytisoside. The substances tested appeared to be weak hydroxyl radical scavengers, showed very low TEAC values and moderate iron chelation ability. However, all preparations at the concentration 25 microg/ml inhibited superoxide anion formation at the range 47-68%. Despite of the lack of a potent free radical scavenging ability the substances tested demonstrated significant antioxidant activity. Relationship between this parameter and the content of phenolic groups was noticed.     

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.     

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.     

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.).     

Inhibition of Trypanosoma cruzi by plant extracts used in Chinese medicine

In this work, we assessed the effect of extracts obtained from 17 plants used in traditional Chinese medicine. These extracts were tested in vitro with the epimastigote form of Trypanosoma cruzi, clone Bra C(15) C(2), at 27 degrees C in F-29 medium at a concentration of 100 microg/ml in axenic cultures. Allopurinol was used as reference drug. Seven plant extracts showed inhibitory activities lower than 25%. Pueraria lobata, Mahonia beaei, Dictamus dasycarpus, Kochia scoparia, Sophora flavescens and Ligustrum lucidum showed effects with inhibition values between 25% and 60%, whereas Lithospermum erythrorhizon, Saussurea lappa, Melia toosendan and Cinnamomum cassia showed the greatest inhibitory activity of 100%. The IC(50) of these extracts were: 0.4, 2.4, 1.8 and 3.9 microg/ml, respectively. The MTT assay was made and did not show cytotoxic activity. These results allowed us to suggest that L. erythrorhizon, S. lappa, M. toosendan and C. cassia could be a source of new compounds against T. cruzi.     

Inhibition of Trypanosoma cruzi growth by medical plant extracts

This study describes the screening of extracts obtained from 18 plants and two fungi used in the Chinese and Mediterranean traditional medicines on epimastigote forms of Trypanosoma cruzi. The extracts were tested against epimastigote of T. cruzi Bra C15C2 clone in vitro at 27 degrees C and at a concentration of 250 microg/ml in axenic culture. Angelica dahurica, A. pubescens, A. sinensis, Astragalus membranaceus, Coptis chinensis, Haplophyllum hispanicum, Phellodendron amurense, Poria cocos, Ranunculus sceleratus and Scutellaria baicalensis showed significant effects against the parasite with a percentage of growth inhibition between 20 and 100%. C. chinensis and R. sceleratus showed the greatest activity with IC(50) values of 1.7 microg/ml for C. chinensis and 10.7 microg/ml for R. sceleratus. These activities are greater than that of allopurinol. C. chinesis and R. sceleratus extracts did not show cytotoxic effects on rat polimorphonuclear cells using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide and lactic dehydrogenase assays. These results allowed us to suggest that R. sceleratus and C. chinensis could be a source of new compounds clinically active against T. cruzi.     

beta-Glucosidase inhibitory activities of phenylpropanoid glycosides, vanicoside A and B from Polygonum sachalinense rhizome

The phenylpropanoid glycosides, vanicoside A and B, isolated from rhizomes of giant knotweed (Polygonum sachalinense) showed beta-glucosidase inhibitory activity, with IC(50) values of 59.8 and 48.3 mug/ml (59.9 and 50.5 muM), respectively. In contrast, p-coumaric acid and ferulic acid, corresponding to phenylpropanoyl moieties of vanicosides, exhibited very little inhibition.     

In vitro cytotoxicity of 11 Panamanian plants

Thirty-five crude extracts from 11 Panamanian plants, distributed in 10 genera and five families, were evaluated for their in vitro cytotoxicity. Four extracts exhibited an inhibition of cellular growth at IC(50) values lower than 25 microg/ml which was considered a significant activity.     

Flavonoids with antiplasmodial and cytotoxic activities of Macaranga triloba

A new flavanone derivative, malaysianone A (1), four prenylated flavanones, 6-prenyl-3'-methoxyeriodictyol (2), nymphaeol B (3), nymphaeol C (4) and 6-farnesyl-3',4',5,7-tetrahydroxyflavanone (5), and two coumarins, 5,7-dihydroxycoumarin (6) and scopoletin (7), were isolated from the dichloromethane extract of the inflorescences of Macaranga triloba. The structures of these compounds were elucidated based on spectroscopic methods including nuclear magnetic resonance (NMR-1D and 2D), UV, IR and mass spectrometry. The cytotoxic activity of the compounds was tested against several cell lines, with 5 inhibiting very strongly the growth of HeLa and HL-60 cells (IC(50): 1.3 μg/ml and 3.3 μg/ml, respectively). Compound 5 also showed strong antiplasmodial activity (IC(50): 0.06 μM).