Growth inhibitory effect of ethyl acetate-soluble fraction of Cynara cardunculus L. in leukemia cells involves cell cycle arrest, cytochrome c release and activation of caspases.

An extract of artichoke Cynara cardunculus L. (CCE) has been shown to exhibit antioxidant and antigenotoxic properties. In this study, the ability of CCE to inhibit the growth of L1210 and HL-60 leukemia cells was studied. Treatment of leukemia cells with a variety of concentrations of CCE (500-2500 microg/microL) for 24 h resulted in dose-dependent inhibition of leukemia cell growth. The cell growth inhibition was accompanied by G(0)/G(1) cell cycle arrest and by a loss of cells in S phase. Futhermore, apoptosis detected as a sub-G(0) cell population and apoptotic DNA fragmentation was observed. More detailed analyses of apoptosis induced by CCE in HL-60 cells revealed that apoptosis progressed through the caspase-9/-3 pathway, as release of cytochrome c, caspase-9/-3 activations and specific proteolytic cleavage of poly(ADP-ribose) polymerase. Taken together, the results suggest that CCE exerts an antiproliferative activity on leukemia cells and induces apoptosis of these cells through a mitochondrial/caspase dependent pathway.

Antigenotoxic effect of extract from Cynara cardunculus L.

The extract of artichoke Cynara cardunculus L. (CCE) was investigated for its potential antigenotoxic and antioxidant effects using four experimental model systems. In the Saccharomyces cerevisiae mutagenicity/antimutagenicity assay, CCE significantly reduced the frequency of 4-nitroquinoline-N-oxide-induced revertants at the ilv1 locus and mitotic gene convertants at the trp5 locus in the diploid Saccharomyces cerevisiae tester strain D7. In the simultaneous toxicity and clastogenicity/anticlastogenicity assay, it exerted an anticlastogenic effect against N-nitroso-N'-methylurea-induced clastogenicity in the plant species Vicia sativa L. On the contrary, despite CCE not being mutagenic itself, in the preincubation Ames assay with metabolic activation, it significantly increased the mutagenic effect of 2-aminofluorene in the bacterial strain Salmonella typhimurium TA98. In the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay, CCE exhibited considerable antioxidant activity. The SC50 value representing 0.0054% CCE corresponds to an antioxidant activity of 216.8 microm ascorbic acid which was used as a reference compound. Although the mechanism of CCE action still remains to be elucidated, different possible mechanisms are probably involved in the CCE antigenotoxic effects. It could be concluded that CCE is of particular interest as a suitable candidate for an effective chemopreventive agent.

[Constituents of Lilium candidum L. and their antioxidative activity]. / Obsahové látky Lilium candidum L. a ich antioxidacná aktivita.

The paper deals with the separation and identification of a flavonoid glycoside from the petals of Lilium candidum L. and the antioxidative properties of the ethanolic extract of the flowers and selected compounds isolated from this species. The isolated flavonoid glycoside was identified as isorhamnetin-3-O-rutinoside by acid hydrolysis, TLC comparison with authentic samples, and UV and mass spectra. Isorhamnetin rutinoside was isolated from Lilium candidum L. for the first time. The antioxidative activity of the ethanolic extract of the flowers and some isolated compounds were determined using DPPH assays.

[Flavonoids--main constituents of the leaves of Holodiscus discolor (Pursh) Maxim]. / Flavonoidy--hlavné obsahové látky listov Holodiscus discolor (Pursh) Maxim.

The paper deals with the isolation and identification of constituents of the leaves of Holodiscus discolor (Pursh) Maxim. (Rosaceae). Three flavonoid glycosides of flavonol type were isolated from the methanolic extract: kaempferol-3-O-rhamnoside, quercetin-3-O-glucoside (isoquercitrin) and quercetin-3-O-rhamnoside (quercitrin). Isolates were identified by physical-chemical data, by comparison with authentic samples and literature data. The above-mentioned compounds were isolated from Holodiscus discolor (Pursh) Maxim. for the first time.

[Ouabain: from an arrow poison to a new steroidal hormone]. / Ouabaín--od sípového jedu k novému steroidnému hormónu.

For more than 200 years, cardiotonic glycosides have been used for the treatment of congestive heart failure. Ouabain is a well-known arrow poison obtained from different Acokanthera or Strophanthus species. Much information has now accumulated that this plant toxin and its congeners are mammalian steroid hormones involved in the pathophysiology of cardiovascular diseases. There is an interesting fact that 50% patients with essential hypertension have elevated levels of endogenous ouabain. A better knowledge of the interactions of these compounds with the hormones of salt and water metabolism might help to improve the diagnosis and therapy of hypertension.

A new flavonoid: tinctosid from Anthemis tinctoria L.

Patuletin 7-O-beta-D-(6"-caffeoylglucoside) was isolated from the methanolic extract of the flowers of Anthemis tinctoria L. (Asteraceae). The isolated compound was identified by spectroscopic means and by comparison with authentic samples after enzymatic hydrolysis. A new flavonoid glycoside, tinctosid, from Anthemis tinctoria L. was isolated from a plant source for the first time.

[Anticomplement activity of saponins from Cynara cardunculus L]. / Antikomplementová aktivita saponínov z Cynara cardunculus L.

Triterpene saponins of ursane and oleane type isolated from the involucral bracts of Cynara cardunculus L. (Asteraceae) were investigated in in vitro assays for their activity on the complement system. The anticomplementary activity of bidesmosidic saponins on the classical pathway activation of the complement was higher than the activity of monodesmosidic saponins, but esterification of the carboxylic group of glucuronic acid in the sugar residue resulted in a significant decrease in anticomplementary activity.

Cytotoxic effects of plant extracts from the families Fabaceae, Oleaceae, Philadelphaceae, Rosaceae and Staphyleaceae.

A human transformed line of HeLa cells was treated with extracts prepared from Gymnocladus dioicus, Holodiscus discolor, Stephanandra tanakae, Ligustrum delavayanum, Ligustrum vulgare and Staphylea pinnata. The study evaluating the influence of the active extracts on HeLa cell division also reveals their acute, delayed and combined effect. A 35% degradation of HeLa cells was found after 72 h treatment with 62.5 microg/mL of the extract isolated from Stephanandra tanakae. A 100% lysis of HeLa cells was observed after 72 h treatment with a 125 microg/mL concentration of the extract prepared from Gymnocladus dioicus. The extracts from Ligustrum devayanum and Ligustrum vulgare were specifically effective only with HeLa cells. On the other hand, the extract prepared from Gymnocladus dioicus was effective on the bacteria and on the HeLa cells.

The effect of Ligustrum delavayanum on isolated perfused rat heart.

BACKGROUND: Extract of ligustrum leaves (Ligustrum delavayanum Hariot [Oleaceae]) is well known in traditional Chinese medicine. One of the active components, oleuropein, displays vasodilating and hypotensive effects. OBJECTIVE: To analyze the effect of 0.008% lyophilized extract of ligustrum dissolved in 0.5% ethanol on heart function. ANIMALS AND METHODS: Experiments were done on isolated rat hearts perfused by the Langendorff method in control conditions and during ischemic-reperfusion injury. RESULTS: Application of ligustrum induced positive inotropic and vasodilating effects in spontaneously beating hearts. Pretreatment of the hearts with ligustrum reduced left ventricular diastolic pressure measured during reperfusion and improved left ventricular contraction compared with hearts without any pretreatment. Ligustrum significantly suppressed the incidence and duration of cardiac reperfusion arrhythmias, expressed as G-score, from 7.40+/-0.58 in nontreated rats to 1.97+/-0.50. DISCUSSION: Application of ligustrum or ethanol alone induced changes in coordination between atria and ventricles during ischemia-reperfusion injury. The 'g-score', a new parameter summing the incidence and duration of atrioventricular blocks, atrioventricular dissociation and cardiac arrest, is introduced. The g-scores with ligustrum pretreatment were higher during ischemia than during reperfusion. Ethanol significantly depressed myocardial contractility and coronary flow, and nonsignificantly decreased heart rate of isolated rat hearts. Electrical changes observed during coronary reperfusion in the presence of ethanol were accompanied by deterioration of contractile function. CONCLUSIONS: Ligustrum had a significant protective effect on rat myocardium against ischemic-reperfusion injury. Ethanol partially attenuated the protective effect of ligustrum.

[Nonpolar components of the leaves of Philadelphus coronarius L]. / Nepolárne obsahové látky listov Philadelphus coronarius L.

The paper deals with the isolation of constituents from light petrol and chloroform extracts of the leaves of Philadelphus coronarius L., Saxifragaceae. From the light petrol extract uvaol and 3 beta,28-dihydroxyoleanane-11(12),13(18)-diene were isolated, while coumarins (umbelliferone, scopolin), stigmasteryl-3 beta-D-glucoside and the alcane type carbohydrate-C29H60 were isolated from the chloroform extract. The isolated compounds were identified by spectroscopic means and by comparison with standards and the literature data.

[Monodesmosidic saponins in Cynara cardunculus L]. / Monodezmozidové saponíny z Cynara cardunculus L.

From an ethanolic extract of the flower buds of Cynara cardunculus L. (Asteraceae), two monodesmosidic saponins, cynarasaponin B and a new cynarasaponin K, were isolated. The isolated compounds were identified by spectroscopic means and by comparison with standards and the literature data.

[Constituents of the leaves of Holodiscus discolor (Pursh) Maxim]. / Obsahové látky listov Holodiscus discolor (PURSH) MAXIM.

The paper deals with the isolation of constituents from light petrol and methanol extracts of the leaves of Holodiscus discolor (PURSH) MAXIM., Rosaceae. beta-sitosterol and taraxasterol were isolated from the light petrol extract, luteolin-7-O-glucoside was isolated from the methanol extract. The isolated compounds were identified by spectroscopic means and by comparison with authentic samples.

[Constituents of the leaves of Ligustrum delavayanum Hariot]. / Obsahové látky listov Ligustrum delavayanum Hariot.

From the chloroform part of Ligustrum delavayanum Hariot, leaves five constituents were isolated: tyrosol, esculetine, kempferol-7-O-rhamnoside, quercetine-3-O-glucoside, and quercetine. Further six constituents (probably malvidine, two secoiridoid glycosides, caffeic acid monosaccharide ester, quercetine monoglycoside (no hyperoside), and quercetine diglycoside (no rutinoside)) were isolated from the methanolic part of above mentioned drug.

[Comparison of the quality of Melissa officinalis L. cultivar Citra with Mellissas of European origin]. / Porovnanie kvality Melissa officinalis L. cv. Citra s medovkami európskeho pôvodu.

Within two vegetation periods, melissas from 17 European regions and the inland cultivar Citra were examined. Melissas differed in height, foliage, and essential oil content. In the cultivating conditions under study, two collections were possible in one year. In both experimental years at the stage just before blooming, or at the onset of blooming, plants 60-80 cm in height prevailed in the set. The share of leaves in the tops was 35-70%. In the second repeated harvest, plants with newly formed sprouts reached a height of 15-35 cm and had the best foliage (60-95%). The essential oil content in the leaves at the stage just prior to blooming, or at the onset of blooming, ranged from 0.06 to 0.16% (V/m), and the maximal essential oil content was in the plants from the second harvest (0.09-0.45%). The cultivar Citra was characterized by medium height (75-80 cm), stable values of foliage (1st harvest 55-60%, 2nd harvest 70-80%), and essential oil content (1st harvest 0.13%, 2nd harvest 0.23-0.27%).

Antibacterial activity of plant extracts from the families Fabaceae, Oleaceae, Philadelphaceae, Rosaceae and Staphyleaceae.

The selected plant extracts exhibited antibacterial activity. The strongest effect was manifested by extracts prepared from Gymnocladus dioicus, Amelanchier ovalis, Exochorda racemosa, Holodiscus discolor, Philadelphus microphyllus, Philadelphus coronarius and Pelargonium tabulare. The percentage inhibition of bacterial growth was 0-41.8%. In addition it was found that extracts isolated from Amelanchier ovalis, Exochorda racemosa and Pelargonium tabulare were specifically effective only against the bacterial strains tested.

Phenolic acids inhibit chloroplast mutagenesis in Euglena gracilis.

The mutagenicity (bleaching activity) of ofloxacin (43 microM) and acridine orange (AO) (13.5 microM) in Euglena gracilis is inhibited by plant phenolics. Caffeic acid (CA), p-coumaric acid (PCA), ferulic acid (FA) and gentisic acid (GA) (25, 50, 100 and 250 microM) exhibited a significant concentration-dependent inhibitory effect against ofloxacin-induced mutagenicity, which was very effectively eliminated by the highest concentration of all four of those phenolic acids. The mutagenicity of AO was also significantly reduced in the presence of CA, PCA and FA (25, 50, 100 and 250 microM). However, GA exhibited no significant activity, even at the concentration of 250 microM. Based on the UV spectrophotometric measurements, we suggest that the antimutagenic effect of CA, PCA, FA and GA resulted from the scavenging of reactive oxygen species (ROS) produced by ofloxacin. On the other hand, the reduction of AO-induced mutagenicity correlates with the binding capabilities of CA, PCA and FA, with the exception of GA.

[Occurrence and use of anthracenones]. / Niektoré aspekty výskytu a vyuzitia antracenónov.

The present paper aims to inform the pharmaceutical public about anthracenons and their natural producers. The first available mention dates from 1888 and the present authors also describe their synthesis and use in clinical practice.

[Apigenin-7-methylglucuronide from Cynara cardunculus L]. / Apigenín-7-metylglukuronid z Cynara cardunculus L.

From an ethanolic extract of the flower buds of Cynara cardunculus L. (Asteraceae), apigenin-7-methylglucuronide and chlorogenic acid were isolated. The isolated compounds were identified by spectroscopic means, by comparison with authentic samples and literature data.

[Detection of secretion of beta-galactosidase by plant cells]. / Prezentácia sekrécie beta-galaktozidázy rastlinnými bunkami.

A simple, sensitive and reproducible method of detection of extracellular beta-galactosidase was worked out. beta-Galactosidase secreted by the callus culture, or the roots of sprouting plants, hydrolyzes the substrate (6-bromo-2-naphthyl-beta-D-galactopyranoside) to produce beta-D-galactose and 6-bromo-2-naphthol, which after simultaneous azocoupling with hexazotized p-rosaniline, or basic fuchsine, produce a reddish brown compound, nearly insoluble in water (a diazonium salt). The colouring under the callus culture and around it, as well as the colouring of the roots of the sprouting plants, is a manifestation of the activity of extracellular beta-galactosidase by the objects under study. The intensity of the colouring is a measure of their enzymatic activity. The share of intracellularly localized enzyme represents the majority and the share of extracellular beta-galactosidase the minority.

[Curcumin as a potential antioxidant]. / Kurkumín ako potenciálne antioxidans.

Curcuma vera is one of the medicinal plants of traditional Chinese medicine. The plant is the natural source of one of natural antioxidative agents--curcumin. The present paper summarizes information about the properties of curcumin and presents the characteristics of Curcuma vera, its producer.